ATB Clinical Practice

Review of Anti-infectives in Clinical Practice
. !" #$%!&'", ., . ( *
+), BCPS.
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Antibacterial agents Sodium fusidate 46
Penicillins Colistin 49
Natural penicillins 2 Fosfomycin 49
Aminopenicillins 4 Nitrofurantoin 49
Antistaphylococcal penicillins 6 Spectinomycin 51
Antipseudomonal penicillins 7 Chloramphenicol 51
Cephalosporins Thiamphenicol 51
1st generation cephalosporins 9 Antimycobacterial agents
2nd generation cephalosporins 10 Antituberculous agents 54
3rd generation cephalosporins 12 Antileprotic agents 60
4th generation cephalosporins 16 Antifungal agents
5th generation cephalosporins 17 Amphotericin B 63
Carbapenems 19 Azole antifungals 65
Aztreonam 22 Echinocandins 69
Macrolides and ketolides 23 Miscellaneous antifungals 71
Aminoglycosides 27 Antiviral agents
Fluoroquinolones 30 Antivirals active against HSV and VZV 73
Tetracyclines and glycylcyclines 34 Antivirals active against CMV 75
Sulfonamides and trimethoprim 37 Antivirals active against HBV and HCV 77
Lincosamides 39 Antivirals active against influenza viruses 86
Nitroimidazoles 41 Antiretrovirals 87
Miscellaneous antibacterials Antiparasitic agents
Glycopeptides 42 Antimalarial agents 97
Lipoglycopeptides 42 Antiprotozoal agents 104
Linezolid 46 Anthelminthic agents 107
Quinupristin/dalfopristin 46
Daptomycin 46
a+2'* b 57 c

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Antibacterial agents
Penicillins
Penicillins +$d4''*e thiazolidine ring ('f*$g6+hg'+$ S 6i26)

jg+#2 beta-lactam ring f#2
+$4+f##2'5$g side chain hg'5l pharmacokinetic/pharmacodynamic profiles, antibacterial activity f##2'
a(1)
Beta-lactams (penicillins, cephalosporins, carbapenems, monobactams) +$% 57 &#g lm
intracellular pathogens
2 Rickettsia spp., Legionella spp. jg'm6bi2 host cells a6 f*%6a+2+$n*#2

jo5$ga+2+$n'h**"
2 Mycoplasma spp., Ureaplasma spp., Chlamydia spp. jg'm6p57 cd666o'
' peptidoglycan)(1)
&1# "f& penicillins %+ 3-10% hg'+e type I hypersensitivity (immediate hypersensitivity
reactions)
2 urticaria, angioedema, anaphylaxis, anaphylactic shock ni5$gf&6#l#g'l*12+ penicillins l
tj2+$4+$g6'#2f&b+6 penicillins jgu f*%mf&b+t' beta-lactams *12+jgu 6(1)
n*a+2&'%'4"jgu af2 4*jga m$6, 5'2', njg, drug fever, serum sickness, interstitial nephritis,
hepatotoxicity, neurotoxicity (
2
), hematologic abnormalities (
2 neutropenia, thrombocytopenia)(1)
Natural penicillins
Natural penicillins a+m
jo Penicillium spp. d6#' a+2n2%f#2'd4''j
'4%"(1)
Spectrum of activity : natural penicillins 44*1+ Streptococcus pyogenes (GABHS), viridans group
streptococci, penicillin-sensitive Streptococcus pneumoniae (PSSP), Gram-negative bacteria '
(Neiserria
meningitidis, Treponema pallidum, Leptospira spp.), anaerobes '
(
2 Peptostreptococcus spp.,
Clostridium tetani, Clostridium perfringens, Pasteurella multocida)(1-3)
Clinical uses : vmm16'4'l
natural penicillins ld4#
jo5$g m Streptococcus pyogenes (GAS
pharyngitis), viridans group streptococci (streptococcal endocarditis), PSSP (respiratory tract infections),
Treponema pallidum (syphilis), Leptospira spp. (leptospirosis), Clostridium tetani (5%6), Clostridium
perfringens (gas gangrene)(1, 2)
Mechanisms of resistance : lvmm1 natural penicillins +$bb#p57 c42b'f4 jg'm
jo
f45$$62lw2+$jo6(1)
o Natural penicillins ti5*6d6ah+" penicillinases (beta-lactamases) hg''mf45$$6*6

2 Staphylococcus spp., Neiserria spp., Haemophilus influenzae, Enterobacteriaceae, anaerobes '

(1)
o Natural penicillins m PBP1a, PBP2b, PBP2x b' Streptococcus pneumoniae '6&71" (PRSP)
aa+2(1)$
o Natural penicillins +$ side chain e benzene ring 5ld+*1*a+2
o (hydrophobic) 2'n*ln2
outer membrane porins b' GNB 2lw2a+2a
2 E. coli, Proteus mirabilis, Salmonella spp.,
Shigella spp.(1)

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#$%& 1 Natural penicillins
Penicillin V Pencillin G
Penicillin G benzathine
(phenoxymethyl penicillin) (benzylpenicillin)
250-500 mg PO q 6 hr 1o, 2o, early latent syphilis : 2.4
(%52 1
gd+' j million units IM single dose(2, 3)
2-4 million units IV q 4 hr
*' 2
gd+')(2, 3) Late latent syphilis : 2.4 million units
(l 4 million units IV q 4 hr l
bl
Recurrent rheumatic fever IM weekly x 3 "# #2(2, 3)
(4) neurosyphilis, meningitis,
prophylaxis : 250 mg PO q 12 hr Recurrent rheumatic fever
endocarditis)(2, 3)
prophylaxis : 1.2 million units IM 51 3-
4 " (j*%4o')(5)
Absorption 60-73%(3, 4)
0.15 mcg/mL *'|$ 1.2 million units
20 mcg/mL *'l 12 million IM(2) (6tiih+m*+jobi2
Cmax 5-6 mcg/mL *'%5 500 mg(2)
units/day IV(2) %f*j62'
u 5l+$%6l
*j#g+(6))
Plasma protein
65-70%(2, 3) 60-65%(2, 3) 60%(4)
binding
Vd 0.5 L/kg(3) 0.3 L/kg(3)
#f2'5$g6 Blister fluid, urine, peritoneal fluid, pleural fluid, middle ear fluid, intestinal mucosa, bone, gallbladder, lungs, female
%m6aa$ reproductive tissues, bile, inflamed meninges(2)
CSF penetration
(non-inflamed, < 10%(3) < 1%, 5%(3)
inflamed meninges)
Bile penetration a+2+$b+i*(3) 500%(3)
Urine excretion 80% (unchanged)(2, 3) 80% (unchanged)(2, 3)
t la## 0.5
gd+'(3) 0.5
gd+'(3)
t l ESRD 8
gd+'(3) 5.1
gd+'(3)
#'bl
l
2(2, 3) l
2(2, 3) a+2#'(4)
d4a#
#'l

6
l
2(2, 3) l
2(2, 3)
*'5 HD
#'bl
a+2#'(3) a+2#'(3)
d4#
Pregnancy cat. B(2, 3) B(2, 3) B(2, 3)
Allergic potential i'(3) i'(3) i'(3)
< 0.06 mcg/mL (S), 0.12-1.0 mcg/mL (I), > 2 mcg/mL (R) for S.
pneumoniae (non-meningeal, oral therapy)(2)
< 2 mcg/mL (S), 4 mcg/mL (I), > 8 mcg/mL (R) for S. pneumoniae (non-
MIC breakpoint
meningeal, parental therapy)(2)
< 0.06 mcg/mL (S), > 0.12 mcg/mL (R) for S. pneumoniae (meningeal
isolates)(2)
(2, 3)
Hypersensitivity
2 maculopapular or morbilliform rash (1-4%), anaphylaxis (0.004-0.0015%)
(2, 3)
Drug fever
(2, 3)
Interstitial nephritis
ADRs (2, 3)
Seizure +&+jgl
lbi', a+2a*b6lni65$g+$5'b'a#&2'
l
penicillin G l syphilis m5l Jarish-Herxheimer reaction (ab g jg'm**2 6
endotoxin m
jo5$gti5*6) hg'a+2l
2f&6(2, 3)

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#$%& 1 Natural penicillins (#2)
Penicillin V Pencillin G
Penicillin G benzathine
(phenoxymethyl penicillin) (benzylpenicillin)
Penicillin V 200,000 units = 125 lvmm16'4'e drug of choice vmm16'l
l syphilis f*%
mg(4) l Streptococcus pyogenes ' recurrent rheumatic fever(4, 6)
Penicillin V 400,000 units = 250 pharyngitis, neurosyphilis,
6*%*6o a 6+ l
|$ b
(4) (2)
mg leptospirosis *+52o, #6+$41+# e local
Penicillin G 6i2 li f6|$ anesthetics l#(4, 6)
+6#1
jg 'm# 6a+2 5 l%&% |$ 2.4 million units 4f2'|$
(1) *+jo%d&b'*% 1.2 million units
l%5a56 penicillin G
benzathine e 6& hg'+$vw
bf4*6e
2'u
if6f*% Dry syrup : 62.5 mg/5 mL, 125 Injections : 1 million units/vial, 5 Injections : 1.2 million units/vial
4+f'5$g+$l mg/5 mL million units/vial
%5a56 Tablets : 125 mg, 250 mg
Aminopenicillins
Spectrum of activity : +$bb#p57 c4*6 natural penicillins f#244*1+ Enterococcus faecalis
(Enterococcus faecium +jo#2 penicillins) f*%+$p57 #c 2 GNB +bo(7) jg'm# + amino group l side
chain 5l6+$4+
o+bo (hydrophilic) 2'n*ln2 outer membrane porins b' GNB '
a$bo

2 E. coli, Proteus mirabilis, Salmonella spp., Shigella spp.(1) m$ol
aminopenicillins 2+ beta-
lactamase inhibitors (clavulanic acid, sulbactam) 6'5l44*1+ beta-lactamase producing strains b' H.
influenzae, Moraxella catarrhalis f*% penicillin-resistant anaerobes (Bacteroides fragilis) 6(2)
Clinical uses : amoxicillin, amoxicillin-clavulanate +l
ld4#
jof45$$6l5' 6lm2

2 pharygitis, tonsillitis, sinusitis, acute otitis media hg'2lw2 m S. pneumoniae, H. influenzae, M.
catarrhalis m$o6'l
l community-acquired pneumonia (CAP) 6(2, 3) amoxicillin-clavulanate,
ampicillin-sulbactam 6'l
l bite wounds (human, dog, cat), lung abscesses hg'+ m anaerobes(2)
Mechanisms of resistance : vmm1
jof45$$6*6
5o' Gram-positive (S. aureus), Gram-negative
(Haemophilus influenzae, Enterobacteriaceae) f*% anaerobes +$'ah+" beta-lactamases +5*6
aminopenicillins a m'+$l2+ beta-lactamase inhibitors (calvulanic acid, sulbactam) &jgb66bb#
p57 lc 'bo(1, 7)
#$%& 2 Aminopenicillins
Amoxicillin-Clavulanate Ampicillin-Sulbactam
Amoxicillin Ampicillin
(Augmentin, Amoksiklav) (Unasyn)
500-1,000 mg PO q 8 hr 500/125 mg PO q 8 hr
500 mg PO q 6 hr
bl
(3-4 g/day = high dose l
j 875/125 mg PO q 12 hr(2, 1.5-3 g IV q 6 hr(2, 3)
j 1-2 g IV q 4-6 hr(2, 3)
$#
jo DRSP)(2, 3) 3)
Absorption 74-92%(2, 3) 90%/ 60%(3) 40-50%(2, 3)

3-6 mcg/mL *'
12 mcg/mL (amoxicillin) f*% 2 109-150 mcg/mL *'l
4-5 mcg/mL *' %5 500 mg(2),
Cmax mcg/mL (clavulanate) *' 2 g ampicillin/1 g
%5 250 mg(2) 47 mcg/mL *'l 2 g IV
%5 875/125 mg(2) sulbactam IV(2)
af* 1
gd+'(2)

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#$%& 2 Aminopenicillins (#2)
Plasma protein
20%(2, 3) 20%/ 25-30%(2, 3) 20%(2, 3) 28%/ 38%(2, 3)
binding
Vd 0.26 L/kg(3) 0.26/ 0.3 L/kg(3) 0.25 L/kg(3) 0.25/ 0.38 L/kg(3)
CSF penetration
(non-inflamed, 1%, 8%(3) 1%, 1%(3) 1%, 10%(3) < 10%(3)
inflamed meninges)
Bile penetration 3,000%(3) 3,000%(3) 3,000%(3) a+2+$b+i*(3)
Urine excretion 80% (unchanged)(2, 3) 80%/ 40% (unchanged)(2, 3) 90% (unchanged)(2, 3) 80%/ 80% (unchanged)(2)
t la## 1.3
gd+'(2, 3) 1.3
gd+'(2, 3) 0.8-1
gd+'(2, 3) 1-1.2
gd+'(2, 3)
t l ESRD 16
gd+'(3) 16
gd+'(3) 10
gd+'(3) 9
gd+'(3)
#'bl
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 3)
d4a#
#'l

6
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 3)
*'5 HD
#'bl
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
d4#
Pregnancy cat. B(2, 3) B(2, 3) B(2, 3) B(2, 3)
Allergic potential i'(3) i'(3) i'(3) i'(3)
(2)
< 0.06 mcg/mL (S), > 0.12 mcg/mL (R) for S. pneumoniae (meningeal isolates)
(2)
< 0.06 mcg/mL (S), 0.12-1.0 mcg/mL (I), > 2 mcg/mL (R) for S. pneumoniae (non-meningeal, oral therapy)
(2)
MIC breakpoint < 2 mcg/mL (S), 4 mcg/mL (I), > 8 mcg/mL (R) for S. pneumoniae (non-meningeal, parenteral therapy)
(2)
< 8 mcg/mL (S) for Enterobacteriaceae, ampicillin-sensitive enterococci
Sulbactam MIC 4 mcg/mL (S), 8 mcg/mL (I), 16 mcg/mL (R) for A. baumannii
njg (d njgm%& g+i'bo+jg+$ EBV infectious mononucleosis, a2+ allopurinol, HIV infection, lymphocytic
leukemias)(2, 3)
(2, 3)
4*jga m$6, GI upset +&l ampicillin, ampicillin-sulbactam
ADRs (2, 3)
5'2' +&l amoxicillin-clavulanate (d6|&%l), ampicillin, ampicillin-sulbactam
(2)
Drug fever
(2, 3)
Interstitial nephritis, LFT abnormalities (&6+)
+ a+2 5 l 5 '2 ' Inducible chromosomal Inducible chromosomal
jg 'm6ti i h + m beta-lactamases (AmpC) 5$g beta-lactamases (AmpC)
5' a j 'm Enterobacter spp., 5$g ' m Enterobacter
(2, 3)
+i" Citrobacter freundii, spp., Citrobacter freundii,
Morganella morganii, Serrratia Morganella morganii,
marcescens, Pseudomonas Serrratia marcescens,
aeruginosa m%a+2ti66o'd6 Pseudomonas aeruginosa
+6#1 (2)
clavulanate, sulbactam m % a +2 ti 6 6o ' d 6
clavulanate, sulbactam(2)
Sulbactam +$ p 57 c #
Acinetobacter baumannii
l
l b 1 g of
salbactam IV q 4 hr (max.
9-12 g of sulbactam/day)(2)

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#$%& 2 Aminopenicillins (#2)
Dry syrup : 125 mg/5 Dry syrup : 156 mg Dry syrup : 125 mg/5 Dry suspension : 250
mL, 250 mg/5 mL (125/31.25 mg)/5 mL, 228 mg mL mg/5 mL
Capsules : 250 mg, (200/28.5 mg)/5 mL, 312 mg Capsules : 250 mg, 500 Tablets : 375 mg, 750
500 mg (250/62.5 mg)/5 mL, 457 mg mg mg
(400/57 mg)/5 mL Injections : 250 mg/vial, Injections : 750 mg
if6f*%
Tablets : 375 mg (250/125 500 mg/vial, 1 g/vial (500/250 mg)/vial, 1.5 g
4+f'5$g+$l
mg), 625 mg (500/125 mg), (1,000/500 mg)/vial, 3 g
%5a56
1 g (875/125 mg) (2,000/1,000 mg)/vial
Injections : 600 mg
(500/100 mg)/vial, 1.2 g
(1,000/200 mg)/vial, 2.2 g
(2,000/200 mg)/vial
Antistaphylococcal penicillins (penicillinase-resistant penicillins)

ld4''+$ bulky side chains hg'
26'b5*6b'ah+" staphylococcal beta-lactamases m'
+tl
ld4#
jo5$g mf45$$65$g' beta-lactamases
2 Staphylococcus aureus (|&%
MSSA), Staphylococcus epidermidis (|&% MSSE) a(1, 2, 7) f#2b$6b'+$ bulky side chains 4j 5l6b
h**"b'f45$$6
jgu a6 (f5a+2+p$ 57 #c 2 GNB *6)(1)
Spectrum of activity : antistaphylococcus penicillins +$p57 c44*1+ Staphylococcus spp. a$ f#2+$p57 c#
Streptococcus spp. #g2 natural penicillins m'a+26 +l
antistaphylococcal penicillins ld4#
jo
Streptococcus pyogenes, Streptococcus pneumoniae(1, 2)
#$%& 3 Antistaphylococcal penicillins
Cloxacillin Dicloxacillin Nafcillin Oxacillin
(6) (2, 6)
250-500 mg q 6 hr 125-500 mg q 6 hr
( %52 1 (250-500 mg q 6 hr l$

+. j*' 2
+.) moderate to severe
bl
1-2 g IV q 4-6 hr(2, 3) 1-2 g IV q 4-6 hr(2, 3)
j 500 mg-1 g IV q 4-6 infections(2, 6)
hr(6) ( %52 1

+. j*' 2
+.)
Absorption 40-60%(6) 35-50%(2, 6) - -
7-18 mcg/mL *' 40-57 mcg/mL *'l 500 40-57 mcg/mL *'l 500
Cmax
%5 500 mg(2) mg IV(2) mg IV(2)
Plasma protein
93-95%(6) 95-98%(2, 6) 90%(2, 3) 90-94%(2, 3)
binding
Vd 0.24 L/kg(3) 0.2 L/kg(3)
CSF penetration
(non-inflamed, 1%, 20%(3) 1%, 10%(3)
inflamed meninges)
Bile penetration 100%(2, 3) 25%(3)

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#$%& 3 Antistaphylococcal penicillins (#2)
Cloxacillin Dicloxacillin Nafcillin Oxacillin
30% (unchanged), 10-20%
Urine excretion 50-70%(2, 6) 10-30% (unchanged)(3) 39-66% (unchanged)(3)
(metabolite)(6)
t la## 0.5-1.5
gd+'(2, 6) 0.5-2
gd+'(2, 6) 0.5
gd+'(2, 3) 0.5
gd+'(2, 3)
t l ESRD 4
gd+'(3) 1
gd+'(3)
#'bl
a+2#'(2) a+2#'(2) a+2#'(2, 3) a+2#'(2, 3)
d4a#
#'l

6
a+2#'(2) a+2#'(2) a+2#'(2, 3) a+2#'(2, 3)
*'5 HD
#'bl a+2#'(3)
a+2#'(2) a+2#'(2) a+2#'(2, 3)
d4# f#2l
64+%+%'
(2) (2, 3) (2, 3)
Pregnancy cat. B B B B(2, 3)
(3)
Allergic potential i' i' i' i'(3)
(2)
0.25 mcg/mL for S. epidermidis
MIC breakpoint (2)
2 mcg/mL for S. aureus
(2, 3)
njg, LFT abnormalities, hepatitis, interstitial nephritis, leucopenia
ADRs (2, 3)
Phlebitis m'4 6d6 IV infusion +
6f5h+n2' (pus), inflamed bone and joints a Oxacillin +$p57 c#2 Staphylococcus spp. a+2#2'm
+6#1 $(6) nafcillin f#2+$1# "njg f*% hepatitis i'2(2)
(2)
Nafcillin +$1# " neutropenia i'2 oxacillin
Dry syrup : 125 mg/5 Dry syrup : 62.5 mg/5 a+2+$ m 2 6l%5 a+2+$ m 2 6l%5
mL, 250 mg/5 mL mL a56 a56
if6f*%
Capsules : 250 mg, 500 Capsules : 250 mg, 500
4+f'5$g+$l
mg mg
%5a56
Injections : 500 mg/vial,
1 g vial
Antipseudomonal penicillins (extended-spectrum penicillins)

Antipseudomonal penicillins af2 piperacillin, ticarcillin, carbenicillin d6l%5a56+$|&% piperacillin
Spectrum of activity : ld4''+$ polar side chains (
2 piperazine ring) 5l6+tn2 outer
membrane porins b' GNB a$bo f*%5#25*6b' beta-lactamases a$ 2 aminopenicillins m'
44*1+ GNB a'bo(1, 2)
o 44*1+ Streptococcus spp., MSSA, MSSE, Enterococcus spp., H. influenzae, E. coli, K.
pneumoniae, Ps. aeruginosa, Bacteroides spp., oral anaerobes(2, 7)
o l piperacillin 2+ tazobactam (beta-lactamase inhibitor) 5l6+$bb#44*1+ Gram-
positive bacteria
2 MSSA 6(1)
Clinical uses : +l
l$5$g#'l44*1+
jo Pseudomonas aeruginosa
2 febrile neutropenia,
#
jol immunocompromized hosts(2)
#$%& 4 Antipseudomonal penicillins
Piperacillin-Tazobactam (Tazocin)
3.375 g IV q 6 hr(3)
bl
(ml 3.375 g IV q 4 hr j 4.5 g IV q 6 hr l$ nosocomial pneumonia, pseudomonal
infections, severe infections)(2)

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#$%& 4 Antipseudomonal penicillins (#2)
Piperacillin-Tazobactam (Tazocin)
Cmax 209 mcg/mL *'l 3.375 g IV(2)
Plasma protein binding 16-45%/ 30%(2, 3)
Vd 0.3/ 0.21 L/kg(3)
Blister fluid, urine, peritoneal fluid, pleural fluid, middle ear fluid, intestinal mucosa, bone,
#f2'5$g6%m6aa$
gallbladder, lungs, female reproductive tissues, bile, inflamed meninges(2)
CSF penetration
1%, 30%(3)
(non-inflamed, inflamed meninges)
Bile penetration 6,000%(3)
Urine excretion 60%/ 80% (unchanged)(3)
t la## 1-1.5
gd+'/ 8
gd+'(2, 3)
#'bld4a# l
2(2, 3)
#'l

6*'5 HD l
2(2, 3)
#'bld4# a+2#'(3)
Pregnancy category B(2, 3)
Allergic potential i'(3)
16/4 mcg/mL for Enterobacteriaceae, Gram-negative non-lactose fermenters (6 Ps.
aeruginosa)(2)
MIC breakpoint (2)
64/4 mcg/mL for Ps. aeruginosa f#24l
piperacillin/tazobactam + AMGs l Ps.
aeruginosa 5$g+$ MIC 32-64 mcg/mL
njg, eosinophilia, leucopenia, thrombocytopenia (+jgl
# #2 > 21 ), prolonged PT
ADRs
and aPTT, LFT abnormalities
g4(2, 3)
+mj m' piperacillin/tazobactam l Ringers lactate solution &%m##%
+6#1 calcium ion(3) 6$g Zosyn m'i##d6& g+ EDTA disodium f*% sodium citrate &jg*
##%b'#6(8)
if6f*%4+f'5$g+$l%5a56 Injections : 2.25 g (2,000/250 mg)/vial, 4.5 g (4,000/500 mg)/vial
#$%& 5 1bb#p57 bc ' penicillins f#2*%

(1, 2)
Class Gram-positive Gram-negative Anaerobes
PSSP, GABHS, viridans group N. meningitidis, Treponema,
Natural penicillins Clostridium
streptococci Leptospira, Pasteurella multocida
Antistaphylococcal
MSSA, MSSE a+244*1+ a+244*1+
penicillins
PSSP, GABHS, viridans group
N. meningitidis, H. influenzae, PEK,
Aminopenicillins streptococci, E. faecalis, Listeria Clostridium, Borrelia
Shigella, Salmonella
monocytogenes
Aminopenicillins + 44*1+ H. influenzae f*% GNB
streptococci, E. faecalis, Listeria Clostridium, Bacteroides
beta-lactamase inhibitors +bo
monocytogenes, MSSA, MSSE
Extended spectrum N. meningitidis, H. influenzae,
streptococci, E. faecalis, Listeria Clostridium, Bacteroides
penicillins most enteric GNBs, Ps. aeruginosa
monocytogenes, MSSA, MSSE

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Cephalosporins
Cephalosporins +$d4''*e dihydrothiazine ring ('f*$g6+hg'+$ S 6i26)

jg+#2 beta-
lactam ring f#2+$4+f##2'5$g side chains 2 b' hg'5l pharmacokinetic/pharmacodynamic profiles,
antibacterial activity f##2'a (f2'6e generation 1st t' 5th #+bb#p57 )c (1)
d4''*b' cephalosporins 5#25*6d6 beta-lactamases a$2 penicillins
Mechanisms of resistance :
jof45$$6*6
+$jo6 cephalosporins n2*6*a
o Cephalosporins a+2+tm PBP5 hg'&lf45$$6'

2 Enterococcus spp., Listeria
monocytogenes(1)
o 6n2 outer membrane porins b' GNB '
a6
2 Ps. aeruginosa(1)
o 6tib5' efflux pump b' GNB '

2 Ps. aeruginosa(1)
o 6ti5*6ad6ah+" extended-spectrum beta-lactamases (ESBLs) f*% AmpC beta-lactamases
hg''m GNB *6

2 E. coli '6&71", Klebsiella pneumoniae '6&71", Enterobacter
spp., Citrobacter freundii, Morganella morganii, Serrratia marcescens, Pseudomonas aeruginosa(1, 2)
e*12+65$g+$df&f type I hypersensitivity (immediate hypersensitivity reactions)
2 urticaria,
angioedema, anaphylaxis, anaphylactic shock d6%+ 5-10% b'ni5$gf&6l*12+ penicillins m%+$f&b+
6l*12+ cephalosporins a m'+$4f%2a+24l
cephalosporins lni5$g+$%# f&6*12+ penicillins f
1f' (severe immediate hypersensitivity)(1)
n*a+2&'%'4"jgu af2 5'2', njg, drug fever, LFT abnormalities, hematologic abnormalities (
2
hemolytic anemia, reversible neutropenia, thrombocytopenia) m$o cephalosporins '
5$g+$+i2 N-
methylthiotetrazole (NMTT)
2 cefoperazone, cefoxitin, cefotetan, cefamandole 6' 5 l
hypoprothrombinemia 6(1)
1st generation cephalosporins

1st generation cephalosporins +$p57 c#2 Staphylococcus spp. $5$g1l6*12+ cephalosporins jg'm
+$ side chain 5$g' beta-lactam ring m5*6b' staphylococcal beta-lactamases f#2a+2+t
'm beta-lactamases b' GNB 2lw2 (6 Proteus mirabilis, E. coli, Klebsiella pnemoniae)(1)
Spectrum of activity : 44*1+ Streptococcus pyogenes (GABHS), MSSA, MSSE, Gram-negative
bacteria '
(Proteus mirabilis, E. coli, Klebsiella pnemoniae = PEK)(1, 2) f#2a+2+$p57 c#2 PRSP, H.
influenzae, anaerobes, spirochetes(1-3)
Clinical uses : pharyngitis, tonsillitis, uncomplicated SSSIs, UTIs, bone and joint infections, surgical
prophylaxis (cefazolin)(2)
1st generation cephalosporins +$5o'if6%5 af2 cephalexin, cefadroxil f*%6|$ 4j cefazolin
#$%& 6 First generation cephalosporins
Cephalexin
Cefadroxil Cefazolin
(Keflex)
bl
500 mg PO q 6 hr(2, 3) 500-1,000 mg PO q 12 hr(2, 3) 0.5-1 g IV q 6-8 hr(2, 3)
Absorption 90-99%(2, 3) 90-99%(2, 3)
Cmax 18-38 mcg/mL *'%5 500 mg(2) 16 mcg/mL *'%5 500 mg(2) 188 mcg/mL *'l 1 g IV(2)
Plasma protein
5-15%(2, 3) 20%(2, 3) 70-90%(2, 3)
binding

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#$%& 6 First generation cephalosporins (#2)
Cephalexin
Cefadroxil Cefazolin
(Keflex)
Vd 0.35 L/kg(3) 0.31 L/kg(3) 0.2 L/kg(3)
#f2'5$g6 Pleural fluid, synovial fluid, bone, Pleural fluid, synovial fluid, bone,
Pleural fluid, synovial fluid, bone(2)
%m6aa$ purulent sputum of inflamed bronchi(2) wound secretions(2)
#f2'5$g6
CNS(2) CNS(2) CNS(2)
%m6aa6
CSF penetration < 10%(3) < 10%(3) < 10%(3)
Bile penetration 200%(3) 20%(3) 300%(3)
Urine excretion > 90% (unchanged)(3) 70-90% (unchanged)(2, 3) 80-100% (unchanged)(2, 3)
t la## 0.7-1
gd+'(2, 3) 1.5
gd+'(2) 1.8
gd+'(2, 3)
t l ESRD 16
gd+'(3) 22
gd+'(3) 40
gd+'(3)
#'bl
l
2(2, 3) l
2(2, 3) l
2(2, 3)
d4a#
#'l

6*'
l
2(2, 3) l
2(2, 3) l
2(2, 3)
5 HD
#'bl
a+2#'3, 4) a+2#'3, 4) a+2#'3, 4)
d4#
Pregnancy cat. B(2, 3) B(2, 3) B(2, 3)
Allergic potential i'(3) i'(3) i'(3)
< 1 mcg/mL (S), 2 mcg/mL (I),
> 4 mcg/mL (R) for
MIC breakpoint Enterobacteriaceae(2)
< 8 mcg/mL (S), 16 mcg/mL (I),
> 32 mcg/mL (R) for S. aureus(2)
ADRs njg, 5'2', drug fever(2, 3)
Dry syrup : 125 mg/5 mL, 250 mg/5 a+2+$m26l%5a56 Injections : 1 g/vial
if6f*% mL
4+f'5$g+$l Capsules : 250 mg, 500 mg
%5a56 Extended release film-coated tablets :
750 mg (Sporidin AF)
2nd generation cephalosporins

2nd generation cephalosporins f2'e 2 *12+626 4j
o True cephalosporins (cefaclor, cefuroxime) +$p57 c#2 MSSA, MSSE, Streptococcus pyogenes
(GABHS) a+2#2'm 1st generation cephalosporins(1, 3) +$p57 c#2 PEK a$bo f*%44*1+a'
bo (44*1+ Haemophilus influenzae, Enterobacteriaceae, Neiserria spp. = HEN 6)(1)
o Cephamycins (cefminox, cefoxitin, cefotetan) +$+i2 methoxy & g+b+5$g beta-lactam ring 5l+$
p57 c#2 anaerobes '

2 Bacteroides fragilis f#2iw$6p57 c#2 Gram-positive bacteria
(staphylococci, streptococci)(1, 2, 7)
Clinical uses :
o Cefaclor, cefuroxime +l
l pharyngitis, tonsillitis, LRTIs, uncomplicated SSSIs, bone and joint
infections, UTIs(2)

1506 424
2 2556 10
o Cephamycins +l
l intra-abdominal infections (peritonitis, intra-abdominal abscess),
gynecological infections, surgical prophylaxis, diabetic foot infection(2, 3)
2nd generation cephalosporins +$5o'if6%5 af2 cefaclor, cefuroxime axetil f*%6|$ af2
cefuroxime sodium, cefoxitin, cefotetan, cefamandole
#$%& 7 Second generation cephalosporins
Cefaclor Cefuroxime axetil (Zinnat) Cefminox Cefoxitin
(Distaclor) Cefuroxime sodium (Zinacef )
(Meicelin) (Cefxitin)
Cefuroxime axetil : 250-500 mg PO
q 12 hr(2, 3)
250-500 mg PO q 8 hr, 1-3 g IV q 12 hr 1-3 g IV q 6-8 hr(2, 3)
bl
Cefuroxime sodium : 0.75-1.5 g IV
375 mg PO q 12 hr(2, 3) (max. 6 g/day) (max. 12 g/day)
q 6-8 hr(3) (l gonorrhea l 1 g IM
single dose)(2, 3)
Absorption 80-93%(2, 3) 52%(2, 3)
8-9 mcg/mL *' 4 mcg/mL *'%5 250 mg(2), 98.4 mcg/mL *'l 1 g 110 mcg/mL *'l 1
Cmax
%5 500 mg(2) 100 mcg/mL *'l 1.5 g IV(2) IV(9) g IV(2)
Plasma protein
25-50%(2, 3) 30-50%(2, 3) 61-68%(6, 9) 65-80%(2, 3)
binding
Vd 0.3 L/kg(3) 0.15 L/kg(3) 0.12 L/kg(3)
Pleural fluid, synovial
#f2'5$g6 Soft tissue interstitial Pleural fluid, synovial fluid, bone,
fluid, bone, pelvic
%m6aa$ fluid, middle ear(2) inflamed meninges(2)
tissue(2)
#f2'5$g6
CNS, sputum(2) CNS(3) CNS(2)
%m6aa6
CSF penetration
(non-inflamed, < 10%(3) < 10%(3) < 10%(3)
inflamed meninges)
Bile penetration 60%(3) a+2+$b+i*(3) 250%(3)
Urine excretion 60-85% (unchanged)(3) 90-100% (unchanged)(2, 3) 80% (unchanged)(9) 85% (unchanged)(3)
t la## 0.8
gd+'(2, 3) 1.2-1.5
gd+'(2, 3) 2-2.5
gd+'(6, 9) 0.8-1
gd+'(2, 3)
t l ESRD 3
gd+'(3) 17
gd+'(3) 21
gd+'(3)
#'bl
a+2#'(2, 3) l
2(2, 3) l
2 l
2(2, 3)
d4a#
#'l

6*'
l
2(2, 3) l
2(2, 3) l
2(2, 3)
5 HD
#'bl
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
d4#
Pregnancy cat. B(2, 3) B(2, 3) B B(2, 3)
Allergic potential i'(3) i'(3) #g(3)
1 mcg/mL for S. 0.5 mcg/mL (IV), 1 mcg/mL (oral) < 8 mcg/mL (S), 16
(2) (2)
pneumoniae for S. pneumoniae mcg/mL (I), > 32
MIC breakpoint 8 mcg/mL for < 8 mcg/mL (S), 16 mcg/mL (I), > mcg/mL for
(2) (2)
Staphylococcus spp., 32 mcg/mL for Enterobacteriaceae Enterobacteriaceae
Haemophilus spp.(2)
(2, 3)
njg, 5'2', drug fever, serum sickness (d6|&% cefaclor)
Cefoxitin, cefotetan, cefamandole +$+i2 N-methylthiotetrazole (NMTT) ld4'' 5l prolonged PT and aPTT
ADRs
a (jg'm6' clotting factors) +jga2+ anticoagulants, antiplatelets m& g+4+$g6'#2%
*j m$o6'5l disulfiram-like reactions +jga2+f**"(3)

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#$%& 7 Second generation cephalosporins (#2)
Cefaclor Cefuroxime axetil (Zinnat) Cefminox Cefoxitin
(Distaclor) Cefuroxime sodium (Zinacef) (Meicelin )
(Cefxitin)
a+2 +% f5h + a5$g 6jg 1
2 'f*%4 m 6i2 l *12 + cephamycins hg ' 4 4 *1 +
URIs jg 'm+$ 6 f*% respiratory secretions a$(3) anaerobes
2 Bacteroides fragilis f*%a+2ti
p57 c#2 S. pneumoniae IV cefuroxime sodium + l
l 5*6d6 ESBLs f#2ti5*6ad6 AmpC beta-
a+2 $ f*%f5h + b i2 surgical prophylaxis n2#lmf*% lactamases(3)
+6#1 respiratory secretions a 5' (cardiothoracic surgery) +l
l surgical prophylaxis n2#l
2 '
42b'm(2, 3) +l
l treatment and prophylaxis 5' (intra-abdominal surgery), n2#l1'
'
1 + f&5 6" 6 +l
of H. influenzae type b (Hib) (gynecologic and obstetric surgery)(3)
jg 'm#6+$
# 5$g meningitis jg 'm6+$ CNS
ni66+(2) penetration #g(3)
Dry suspension : 125 Dry suspension : 125 mg/5 mL, Injections : 1 g/vial Injections : 1 g/vial
mg/5 mL, 250 mg/5 mL 250 mg/5 mL (cefuroxime axetil)
if6f*% Capsules : 125 mg, Tablets : 250 mg, 500 mg
4+f'5$g+$l 250 mg, 500 mg (cefuroxime axetil)
%5a56 Modified release Injections : 750 mg/vial, 1.5 g/vial
tablets : 375 mg (cefuroxime sodium)
(Distaclor MR)
3rd generation cephalosporins

3rd generation cephalosporins +$ side chain e aminothiazolyl group 5ln2 outer membrane porins b'
GNB a,$ & g+4++tlm (affinity) PBPs f*%5#25*6b' beta-lactamases b' GNB
*6
(1)
Spectrum of activity :
o +$p57 c#2 staphylococci (MSSA, MSSE) 6*' f#2+$p57 c#2 Streptococcus pneumoniae (5o' PSSP
f*% PRSP) $bo +jg5$6 2nd generation cephalosporins(1-3)
o 44*1+ GNB a'2 2nd generation cephalosporins af2 PEK + HEN + S (Serratia
spp.)(1)
o 44*1+ spirochetes '

2 Leptospira interrogans (
jo2d4 leptospirosis), Borrelia
burgdorferi (
jo2d4 Lyme disease)(1, 2)
o Ceftazidime f*% cefoperazone 44*1+ Pseudomonas aeruginosa 6 (ceftazidime +$
antipsudomonal activity $2 cefoperazone) f#2p57 c#2 S. aureus b' ceftazidime *6a(1, 7)
Clinical uses : l
ld4#
jo S. pneumoniae (URIs, pneumonia, meningitis), Enterobacteriaceae
2lw2 (UTIs, intra-abdominal infections, intrapelvic infections, gonorrhea, septicemia)(1, 2)
Oral 3rd generation cephalosporins +til
l IV-oral switch therapy l CAP, AECB, sinusitis, acute otitis
media, UTIs(2)
a+24l
3rd generation cephalosporins l GNB '

2 Enterobacter spp., Citrobacter freundii,
Morganella morganii, Serratia marcescens, Providencia spp. f+ in vitro susceptibility m%ln* sensitive
#+ jg'mlvmm1&jo6b'
jo*2$o+bo d6' inducible chromosomal beta-
lactamases (AmpC) l%2'(1, 2)

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#$%& 8 Oral third generation cephalosporins
Cefdinir Cefixime Cefpodoxime Ceftibuten Cefditoren pivoxil

(Omnicef ) (Cefspan ) proxetil (Banan ) (Cedax ) (Meiact)
200 mg PO q 8 hr,
200-400 mg PO q 12 200-400 mg PO q 12
300 mg PO q 12 hr,
bl
hr (gonorrhea l
400 hr (gonorrhea l
400 400 mg PO q 24 hr(3) 400 mg PO q 12 hr(3)
600 mg PO q 24 hr(2,
3) mg single dose)(2, 3) mg single dose)(2, 3)
16%(3)
Absorption 16-25%(2, 3) 30-50%(2, 3) 50%(2, 3) 80%(3) (4%5#
5'2')
1.60 mcg/mL *'
%5 300 mg, 3-5 mcg/mL *' 3 mcg/mL *'
Cmax
2.87 mcg/mL *' %5 400 mg(2) %5 200 mg(2)
%5 600 mg(2)
Plasma protein
60-73%(2, 3) 65%(2, 3) 21-40%(2, 3) 65%(3) 88%(3)
binding
Vd 0.35 L/kg(3) 0.1 L/kg(3) 0.9 L/kg(3) 0.2 L/kg(3) 0.13 L/kg(3)
Gallbladder, tonsillar,
#f2'5$g6 Pleural fluid, synovial maxillary sinus Pleural fluid, synovial
%m6aa$ fluid, bone(2) tissue, middle ear, fluid, bone(2)
prostatic fluid(2)
CSF penetration
(non-inflamed, a+2+$b+i*(3) < 10%(3) < 10%(3) < 10%(3) a+2+$b+i*(3)
inflamed meninges)
Bile penetration a+2+$b+i*(3) 800%(3) 100%(3) a+2+$b+i*(3) a+2+$b+i*(3)
12-18% 40-50% 29-33%
Urine excretion 56% (unchanged)(3) 20% (unchanged)(3)
(unchanged)(2, 3) (unchanged)(2, 3) (unchanged)(2, 3)
t la## 1.7
gd+'(2, 3) 3.1
gd+'(2, 3) 2-3
gd+'(2, 3) 2.4
gd+'(3) 1.5
gd+'(3)
t l ESRD 3
gd+'(3) 11
gd+'(3) 9.8
gd+'(3) 22
gd+'(3) 5
gd+'(3)
#'bl
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(3) l
2(3)
d4a#
#'l

6
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(3) l
2(3)
*'5 HD
#'bl
a+2#'(3) a+2#'(3) a+2#'(3) a+2#'(3) a+2#'(3)
d4#
Pregnancy cat. B(2, 3) B(2, 3) B(2, 3) B(3) B(3)
Allergic potential i'(3) i'(3) i'(3) i'(3) #g(3)
0.5 mcg/mL for S. 1 mcg/mL for 0.5 mcg/mL for S.
(2) (2)
pneumoniae Haemophilus spp. pneumoniae(2)
MIC breakpoint 1 mcg/mL for 2 mcg/mL for
Staphylococcus spp., Staphylococcus spp.,
Haemophilus spp.(2) Haemophilus spp.(2)
njg, hepatitis,
ADRs njg, 5'2'(2, 3) njg, 5'2'(2, 3) hypersensitivity njg(3) njg(3)
pneumonitis(3)
+jg %5& +
Antacids *i
Drug interaction iron supplement m
h+6(3)
5l1mm%+$$f'(2)

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#$%& 8 Oral third generation cephalosporins (#2)
Cefdinir Cefixime Cefpodoxime Ceftibuten
Cefditoren pivoxil
(Omnicef) (Cefspan) proxetil (Banan )
(Cedax)
(Meiact)
rd
+$ p 5 7 c $ #2 + l
l e oral 3 gen. +$ p 57 c #2 MSSA,
+l
l sinusitis,
respiratory pathogens gonorrhea, LRTIs(3) cephalosporin &$6 ' S. pneumoniae 6
tonsillitis, pharyngitis,
(S. pneumoniae, H. f5a+2 +$ p 57 c #2 # $ 6 5$g 4 4*1 + +(3)
AECB, CAP, SSTIs(3)
influenzae) m'+l
MSSA(2, 3) MSSA(3) (SSTIs l
Cefditoren +t
l CAP, AECB, 400 mg PO q 12 % #1 carnitine
(3)
pharyngitis hr)(2, 3) metabolism m'a+24
+6#1 l
al acute otitis l
6 $o l ni 6
media, pharyngitis, carnitine deficiency
tonsillitis, sinusitis, j hereditary
AECB(2, 3) carnitine metabolism
disorders &%m
5 l metabolic
encephalopathy(3)
Dry suspension : Dry suspension : Dry syrup : 40 Dry suspension : Fine granules : 50
if6f*%
125 mg/5 mL 100 mg/5 mL mg/5 mL, 80 mg/5 36 mg/mL mg/sachet
4+f'5$g+$l
Capsules : 100 mg Capsules : 100 mg mL Capsules : 400 mg Tablets : 100 mg
%5a56
Tablets : 100 mg
#$%& 9 Intravenous third generation cephalosporins

Cefotaxime Ceftriaxone Cefoperazone-sulbactam Ceftazidime
(Claforan)
(Rocephin ) (Sulperazon) (Fortum)
1-2 g IV q 12-24 hr 2-4 g (1:1) IV q 12 hr,
1-2 g IV q 8-12 hr
1-2 g IV q 4-6 hr(2, 3) (l meningitis l 2 g IV q 1.5-6 g (2:1) IV q 12 hr
(l meningitis, severe
bl
(l meningitis l 2 g IV q 12 hr, l gonorrhea l (l meningitis l 4 g (1:1)
infections l 2 g IV q 6-8
4-6 hr)(2) 125-250 mg IM single j 6 g (2:1) IV q 12 hr hg'
hr) (max. 8 g/day)(2, 3)
dose)(2, 3) e max. dose)(3)
430 mcg/mL
(cefoperazone), 90 mcg/mL
100 mcg/mL *'l 1 g 150 mcg/mL *'l 1 g
Cmax (sulbactam) *'l 60 mcg/mL *'|$ 1 g IV(2)
IV(2) IV(2)
3 g cefoperazone/1.5 g
sulbactam IV(10)
Plasma protein
30-50%(2, 3) 85-95%(2, 3) 90%(3) < 10%(2)
binding
Vd 0.25 L/kg(3) 0.08-0.3 L/kg(3) 0.17 L/kg(3) 0.36 L/kg(3)
#f2'5$g6
Pleural fluid, synovial fluid, bone, inflamed meninges, intracranial abscesses(2)
%m6aa$
CSF penetration
(non-inflamed, 1%, 10%(3) 1%, 10%(3) 1%, 10%(3) 1%, 20%(3)
inflamed meninges)
Bile penetration 75%(3) 500%(3) 1,200%(3) 50%(3)
20-36% (unchanged) +
Urine excretion 15-25% (desacetyl active 33-67% (unchanged)(2, 3) 20% (unchanged)(3) 80-90% (unchanged)(2, 3)
metabolite)(2, 3)

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#$%& 9 Intravenous third generation cephalosporins (#2)
(Claforan) (Rocephin) (Sulperazon) (Fortum)
1.8-2.4
gd+'
t la## 1-1.5
gd+'(2, 3) 8
gd+'(2, 3) (cefoperazone)(3, 10) 1.9
gd+'(2, 3)
1
gd+' (sulbactam)(10)
t l ESRD 15
gd+'(3) 16
gd+'(3) 2.4
gd+'(3) 21
gd+'(3)
#'bl
l
2(2, 3) a+2#'(2, 3) a+2#'(3) l
2(2, 3)
d4a#
#'l

6
l
2(2, 3) a+2#'(2, 3) a+2#'(3) l
2(2, 3)
*'5 HD
#'bl
a+2#'(2, 3) a+2#'(3) a+2#'(3) a+2#'(3)
d4#
B(2, 3)
(f#24*$*$g6'l 3rd
Pregnancy cat. B(2, 3) B(3) B(2, 3)
trimester &%m5l
5 kernicterus)(3)
Allergic potential *'(3) i'(3) #g(3) i'(3)
< 0.5 mcg/mL for S. < 0.5 mcg/mL for S. Sulbactam MIC 4 8 mcg/mL for Gram-
pneumoniae (meningitis), < pneumoniae (meningitis), < mcg/mL (S), 8 mcg/mL (I), negative non-lactose
1 mcg/mL for S. 1 mcg/mL for S. 16 mcg/mL (R) for A. fermenters including Ps.
pneumoniae (non- pneumoniae (non- baumannii aeruginosa(2)
(2) (2)
meningitis) meningitis) < 4 mcg/mL (S), 8
< 8 mcg/mL (S), 16-32 < 0.5 mcg/mL for beta- mcg/mL (I), > 16 mcg/mL
mcg/mL (I), > 64 mcg/mL hemolytic Streptococcus (R) for
MIC breakpoint (R) for S. aureus(2) spp.(2) Enterobacteriaceae (2)
< 0.5 mcg/mL for beta- < 1 mcg/mL (S), 2

hemolytic Streptococcus mcg/mL (I), > 4 mcg/mL
spp.(2) (R) for Enterobacteriaceae,
< 1 mcg/mL (S), 2 S. viridans(2)
mcg/mL (I), > 4 mcg/mL < 8 mcg/mL (S), 16-32
(R) for S. viridans, mcg/mL (I), > 64 mcg/mL
Enterobacteriaceae(2) (R) for S. aureus(2)
njg, 5'2', biliary sludge
prolonged PT and aPTT
( m##%b' njg,
(+&+jgl
l
(jg'm6'
calcium ceftriaxone l5' bi', a+2a*b
ADRs njg, 5'2', phlebitis(2, 3) clotting factors hg'm# '
o$ +&+jgl
6 > 2 6lni65$g+$5'b'
l vitamin K prophylaxis l
" j +jg l
l b a#&2'), phlebitis(2, 3)
ni6'6)(3)
i'), phlebitis(2, 3)
+jga2+f**"
Drug interaction a+2+$(3) a+2+$(3) m%5 l disulfiram-like a+2+(3)
$
reactions(3)
44*1 + MSSA, S. e cephalosporin &$6' +$p57 c# Pseudomonas +$p57 c# Pseudomonas
pneumoniae (5o' PSSP f*% #$65$g 6f*% aeruginosa (n * b ' aeruginosa 6(3) jg'm
PRSP), Bacteroides 4 o ' a jg ' m 6 +$ cefoperazone) f*% l side chain +$
+6#1
fragilis(3) albumin binding i'+ hg' Acinetobacter baumannii carboxypropyl group f#25
Cefotaxime f*% albumin m%5 5$g e (n*b' sulbactam) 6(3) l i w $ 6 p 5 7 c #2
ceftriaxone e preferred drug reservoir 426u Sulbactam +$p57 c# staphylococci (+$ affinity #2

1506 424
2 2556 15
#$%& 9 Intravenous third generation cephalosporins (#2)
(Claforan) (Rocephin) (Sulperazon )
(Fortum)
IV cephalosporins l **26 free drug 62' Acinetobacter baumannii l
PBPs b' staphylococci
pneumonia, #2jg'(1) lb 1 g of salbactam **')(1)
meningitis 5$g m S. l 2 g IV q 24 hr l IV q 4 hr (max. 9-12 g of
pneumoniae jg 'm+$ tissue level i'2 1 g IV q sulbactam/day)(2)
% 5 7 &a+2 #2 ' f#2
12 hr &%6m e cephalosporins a+2$g
6 + ceftriaxone +2 albumin a g+#+jgl > 1 # 5$g +tf5h + b i2
g/dose(2)
&% 6&$ 6 ' *% biliary tract 5$g+$1#a
+6#1 4o'(2) +l
l pneumonia, $(3) m '+$ % 5 7 &$ +
meningitis 5$g m S. l hepatobiliary
pneumoniae(3) infections
2 cholangitis,
44*1+ GNB l UTIs, cholecystitis(11)
intra-abdominal infections,
intrapelvic infections f*%
44*1+ MSSA, group A
streptococci l SSTIs(3)
if6f*% Injections : 500 mg/vial, Injections : 250 mg/vial, Injections : 1 g (500/500 Injections : 500 mg/vial,
4+f'5$g+$l 1 g/vial, 2 g/vial 500 mg/vial, 1 g/vial, 2 mg)/vial, 1.5 g (1,000/500 1 g/vial, 2 g/vial
%5a56 g/vial mg)/vial
4th generation cephalosporins

4th generation cephalosporins +tn2 outer membrane porins b' GNB a$f*%, m PBPs
a*6
(PBP2, PBP3 b' E. coli f*% PBP3 b' P. aeruginosa), 5#2 beta-lactamases *6

(+t' AmpC beta-lactamases)(1, 12)
Spectrum of activity : 44*1+ Streptococcus pneumoniae (5o' PSSP f*% PRSP), S. aureus f*%
44*1+ GNB a'2 3rd genearation cephalosporins af2 PEK + HENS + Pseudomonas
aeruginosa, Enterobacteriaceae 2lw2 (jg'm5#25*6d6 inducible AmpC beta-lactamases 5$g
'm Enterobacteriaceae)(1, 2) f#2f5a+2+$p57 c#2 anaerobes(1)
Clinical uses : +l
l$5$g#'l44*1+
jo Pseudomonas aeruginosa (+6&71"5$gjo#2
ceftazidime 6), AmpC-producing Enterobacteriaceae
2 serious sepsis, nosocomial infections (HAP,
VAP, UTIs, intra-abdominal infections), febrile neutropenia(2, 3, 6)
#$%& 10 Fourth generation cephalosporins
Cefepime Cefpirome
(Maxipime) (Cefrom)
1-2 g IV q 8-12 hr
bl
1-2 g IV q 12 hr
(l meningitis l 2 g IV q 8 hr)(2, 3)
Cmax 193 mcg/mL *'l 2 g IV(2) 80-90 mcg/mL *'l 1 g IV
Plasma protein binding 20%(2, 3) < 10%(6)
Vd 0.29 L/kg(3) 14-19 L
Blister fluid, bronchial mucosa, peritoneal fluid,
#f2'5$g6%m6aa$
prostate, CNS(2)

1506 424
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#$%& 10 Fourth generation cephalosporins (#2)
Cefepime Cefpirome
(Maxipime) (Cefrom)
CSF penetration
(non-inflamed, inflamed 1%, 15%(3) Poor(6)
meninges)
Bile penetration 10%(3)
Urine excretion 80% (unchanged)(2, 3) 80-90% (unchanged)
t la## 2-2.2
gd+'(2, 3) 1.4-2.3
gd+'(6)
t l ESRD 18
gd+'(3)
#'bld4a# l
2(2, 3) l
2
(2, 3)
#'l

6*'5 HD l
2 l
2
(3)
#'bld4# a+2#' a+2#'
(2, 3)
Pregnancy cat. B B
(3)
Allergic potential *'
8 mcg/mL (S), 16 mcg/mL (I), 32 mcg/mL (S) for
Enterobacteriaceae, Gram-negative non-lactose
fermenters (e.g. Ps. aeruginosa)(2)
< 0.5 mcg/mL for S. pneumoniae (meningitis), < 1
MIC breakpoint mcg/mL for S. pneumoniae (non-meningitis)(2)
< 0.5 mcg/mL for beta-hemolytic Streptococcus
spp.(2)
< 1 mcg/mL (S), 2 mcg/mL (I), > 4 mcg/mL (R) for
S. viridans(2)
ADRs njg, 5'2', drug fever, phlebitis(2, 3)
if6f*%4+f'5$g+$ Injections : 1 g/vial Injections : 1 g/vial
l%5a56
5th generation cephalosporins (anti-MRSA cephalosporins)

Spectrum of activity : ceftalorine f*% ceftobiprole +tm PBP2a b' MRSA f*%m PBP5 b'
Enterococcus faecalis a f#2 ceftalorine ti5*6ad6 ESBLs f*% AmpC beta-lactamases 5$g'm GNB
'6&71" (
2 ESBL-producing E. coli, ESBL-producing Klebsiella pneumoniae, Enterobacteriaceae '

) f*%a+244*1+ Bacteroides fragilis(6, 13) m$o ceftalorine 6'a+244*1+ Ps. aeruginosa, A.
baumannii 6 lb%5$g ceftobiprole 5#2 5 *6d6 AmpC beta-lactamases m'44*1+ Ps.
aeruginosa(13)
Clinical uses : l
l cSSSIs 5$g m Staphylococcus aureus (a5o' MSSA, MRSA, VISA) j
Staphylococcus epidermidis (a5o' MSSE, MRSE), CAP 5$g m PRSP, d4#
jo5$g m vancomycin-
resistant E. faecalis, HENPEK(2, 6, 13)
#$%& 11 Fifth generation cephalosporins
Ceftalorine fosamil Ceftobiprole
(Teflaro) (Zeftera)
500 mg IV (30-60 min infusion) q 12 hr(13)
bl
600 mg IV (1 hr infusion) q 12 hr(2, 13)
(serious infections ml 500 mg IV (2 hr infusion) q 8 hr)
Plasma protein
< 20%(6, 13) 16%(13)
binding

1506 424
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#$%& 11 Fifth generation cephalosporins (#2)
Ceftalorine fosamil Ceftobiprole
(Teflaro) (Zeftera)
Vd 0.37 L/kg (16-28.3 L)(6) 18 L(13)
#f2'5$g6
Lung tissue (penetration 42%)(13)
%m6aa$
b5'v%e*(6, 13)
Urine excretion b5'v%e*(13)
64% (unchanged)
t la## 2.5-3
gd+'(6, 13) 3-4
gd+'(13)
#'bl
l
2(2) l
2(13)
d4a#
#'l

6
l
2(2) l
2(13)
*'5 HD
#'bl
a+2+$b+i*(2) a+2+$b+i*(13)
d4#
Pregnancy cat. a+2+$b+i*(2) a+2+$b+i*(13)
< 0.25 mcg/mL for MSSE, S. pneumoniae
< 0.5 mcg/mL for MSSA
< 0.25 mcg/mL for MSSA, MSSE, S. pneumoniae (13)
(2) < 2 mcg/mL for MRSA
< 1 mcg/mL for Enterobacteriaceae
MIC breakpoint (2) < 8 mcg/mL for E. faecalis
< 2 mcg/mL for MRSA
8 mcg/mL (S), 16 mcg/mL (I), 32 mcg/mL (S) for
< 4 mcg/mL for E. faecalis
Enterobacteriaceae, Gram-negative non-lactose fermenters
(e.g. Ps. aeruginosa)
njg , 4*jg a m$ 6 , 5 '2 ', Clostridium difficile- njg , 4*jg a m$ 6 , 5 '2 ', Clostridium difficile-
ADRs associated diarrhea, phlebitis, $% (4%), a+2* associated diarrhea, phlebitis, taste disturbances (15%)(13)
(3.1%)(2)
Drug interaction a+2e substrate, inhibitor, inducer b' CYP450(2) a+2+$
44*1+ MRSA (m PBP2a), PRSP (m PBP2x), 44*1+ MRSA (m PBP2a), PRSP (m PBP2x),
E. faecalis (m PBP5) f#2a+2+$p57 c#2 Ps. aeruginosa(6, E. faecalis (m PBP5), Ps. aeruginosa, AmpC-producing
13)
Enterobacteriaceae(13)
(2) (13)
+$b2'l
l CAP, complicated skin-structure infections +$b2'l
l cSSSIs
2 diabetic foot
FOCUS I f*% FOCUS II study $65$6%2' STRAUSS 1 study $65$6%2' ceftobiprole
ceftaroline fosamil ceftriaxone l moderate to severe (500 mg IV q 12 hr) vancomycin (1 g IV q 12 hr) l
CAP &2+$ clinical cure rate a+2#2' (82.6% f*% 76.6% cSSSIs &2+$ clinical cure rate a+2#2'm (93.3% f*%
#+* ) f*%+jg 4%" |&%*12 + 5$g #
jo S. 93.5% #+*)(13)
pneumoniae &2 ceftalorilne fosamil +$ response rate i' STRAUSS 2 study $ 6 5$ 6 %2 '
+6#1 262'+$64w (86% f*% 69% #+*)(2) ceftobiprole monotherapy (500 mg IV q 8 hr)
CANVAS I f*% CANVAS II study $65$6 vancomycin (1 g IV q 12 hr) + ceftazidime (1 g IV q 8 hr)
%2' ceftaroline fosamil monotherapy vancomycin + l diabetic foot with mixed bacterial cSSSIs &2+$
aztreonam l cSSSIs 1,378 6 (45-49% b'ni6l clinical cure rate a+2#2'm (90.5% f*% 90.2% #+*)
#
jo MRSA) &2+$ clinical cure rate a+2#2' (13)
(85.9% f*% 85.5% #+*)(2) $65$6%2' ceftobiprole monotherapy
(500 mg IV q 8 hr) linezolid + ceftazidime l
nosocomial pneumonia &2a+2f##2' f#2+jg 4%"
|&%*12+ VAP &2 ceftobiprole +$ cure rate #g2
linezolid + ceftazidime(13)

1506 424
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#$%& 12 1bb#p57 bc ' cephalosporins f#2*%12(1, 2)
Generation Gram-positivea Gram-negativeb Anaerobes
Staphylococci (MSSA, MSSE) $5$g1
1st PEK a+244*1+
S. pneumoniae (|&% PSSP)
Staphylococci (MSSA, MSSE) *'
2nd HENPEK a+244*1+
S. pneumoniae (|&% PSSP)
Cephamycins a+244*1+ HENPEK 44*1+
Staphylococci (MSSA, MSSE) (6 ceftazidime) HENPEKS (+ Pseudomonas |&%l '

2
3rd
S. pneumoniae (5o' PSSP f*% PRSP) ceftazidime, cefoperazone) Leptospira, Borrelia
Staphylococci (MSSA, MSSE) HENPEKS + Pseudomonas + AmpC-
4th a+244*1+
S. pneumoniae (5o' PSSP f*% PRSP) producing Enterobacteriaceae
Staphylococci (MSSA, MSSE, MRSA, MRSE) HENPEKS (+ Pseudomonas, AmpC-
th
5 S. pneumoniae (5o' PSSP f*% PRSP) producing Enterobacteriaceae |&%l a+244*1+
Enterococcus faecalis (ampicillin-sensitive, VRE) ceftobiprole)
a b
FGHIF#J cephalosporins 12 1-4 a+244*1+ Enterococcus spp., #'a+2l
2 GNB 6&71"5$g' extended spectrum beta-lactamases
(&%te ESBL-producing strains m%l
1st-3rd generation cephalosporins a+2an*)(7)
Carbapenems
Carbapenems e beta-lactams 5$g+$d4''f##2'm penicillins f*% cephalosporins 5l+$bb#

p57 c'2 af2 d+*1*42b'*f*%+$%m1 (e zwitterion) 5ln2 special porins (
2 OprD) l outer
membrane b' GNB a, d4''5#25*6d6ah+" beta-lactamases *6
(+t' ESBLs,
AmpC beta-lactamases), m PBPs a*6
(PBP1a, PBP1b, PBP2, PBP3, PBP4, PBP6)(1, 2, 14)
Clinical uses : carbapenems e6#f45$$65$g+$bb#p57 c'5$g1lvmm1 m'+'al
l
d4#
jo5$g1f'j*+*ml
6*12+jg
2 Pseudomonas aeruginosa, Acinetobacter baumannii,
Burkholderia pseudomallei (melioidosis), ESBL-producing organisms, AmpC-producing Enterobacteriaceae(1)
Mechanisms of resistance : *ajo6 carbapenems b'
jof45$$6'

o Pseudomonas aeruginosa jo#2 carbapenems l6*' (acquired resistance) d6
jo*'
outer membrane porins (OprD) (5ljo imipenem > meropenem, doripenem) +t'' efflux
pumps (
2 MexAB-OprM, MexEF-OprN) &jgb6 (MexAB-OprM 5ljo#2 meropenem f*%
doripenem f#26'a#2 imipenem, MexEF-OprN 5ljo#2 meropenem > imipenem), 'ah+"
carbapenemases (5ljo#2 imipenem, meropenem, doripenem)(1, 15)
o GNB '
jo #2 carbapenem l6* ' (acquired resistance) d6 'ah+"
carbapenemases
2 KPC-producing Klebsiella pneumoniae, carbapenem-resistant
(1)
Enterobacteriaceae (CRE)
o Enterococcus faecium f*% MRSA jo#2 carbapenems d6
jo+$' PBPs #2'
ahg'6a+2
+tma(1)
o Carbapenems +$d cross hypersensitivity beta-lactams jgu 42b'#g m'l
a42b'
*6lni5$g+$%# f& penicillins(3)

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#$%& 13 Carbapenems
Imipenem/cilastatin Meropenem Ertapenem Doripenem

(Tienam ) (Meronem ) (Invanz ) (Doribax)
Gram-negative bacteria 2lw2 af2 HENPEKS, ESBL-producing organisms, AmpC-producing Enterobacteriaceae
(
2 Enterobacter spp., Citrobacter spp.), Pseudomonas aeruginosa, Acinetobacter baumannii (HMINOP ertapenem 5$ga+2
44*1+ Ps. aeruginosa, Acinetobacter spp.)(1, 2)
Spectrum of (1-3)
Anaerobic bacteria 2lw2
2 Bacteroides fragilis (6 Clostridium difficile)
activity
Gram-positive bacteria '
af2 MSSA, MSSE, Streptococcus pneumoniae (5o' PSSP, PRSP), Listeria
monocytogenes, Enterococcus faecalis(1, 2)
(2)
Carbapenems 51
a+244*1+ MRSA, Stenotrophomonas maltophilia, E. faecium
*12+626 Type 2 carbapenems Type 2 carbapenems Type 1 carbapenems Type 2 carbapenems
500-1,000 mg IV q 6-8 hr 1-2 g IV q 8 hr
(2, 3) 500-1,000 mg IV q 8 hr(2,
bl
(severe infections l 1 g IV (meningitis l 2 g IV q 8 1 g IV/IM q 24 hr 16)
q 6-8 hr)(2, 3) hr)(2, 3)
40 mcg/mL *'|$ 500 mg 26 mcg/mL *'l 500 mg 155 mcg/mL *'l 1 g 23 mcg/mL *'l 500 mg
Cmax (2) (2) (2)
IV IV IV IV infusion(2)
Plasma protein
15-25%/ 40%(2, 3) 2%(2, 3) 85-95%(2, 3) 8%(2, 16)
binding
Vd 0.2 L/kg(3) 0.35 L/kg(3) 8.2 L/kg(2, 3) 16.8 L (8-55 L)(2, 16)
Synovial fluid (41%
#f2'5$g6 Pleural fluid, interstitial fluid, peritoneal fluid, pancreatic Retroperitoneal fluid, bile,
penetration), bone (13-19%
%m6aa$ tissue, reproductive organs(2) urine(2)
penetration)(2)
#f2'5$g6
Sputum, bile, aqueous
%m6aa a+2+$b+i*(2) gallbladder(2)
humor, bone, CSF(2)
6
CSF penetration
(non-inflamed, 10%, 15%(3) 10%, 15%(3) a+2+b$ +i*(3) a+2+$b+i*(16)
inflamed meninges)
Bile penetration 1%(3) a+2+$b+i*(3) a+2+$b+i*(3)
40% (unchanged) + 70% (unchanged) + 18%
Urine excretion 70-76% (unchanged)(2, 3) 70% (unchanged)(2, 3)
40% (active metabolite)(2, 3) (metabolite)(2)
t la## 1
gd+'(2, 3) 1
gd+'(2, 3) 4
gd+'(2, 3) 1-1.1
gd+'(2, 16)
t l ESRD 4
gd+'(3) 7
gd+'(3) 14
gd+'(3) 8.8
gd+'(16)
#'bl
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 16)
d4a#
#'l

6
l
2(2, 3) l
2(2, 3) l
2(2) l
2(2)
*'5 HD
#'bl
a+2#'(3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(16)
d4#
Pregnancy cat. C(2, 3) B(2, 3) B(2, 3) B(2)
Allergic potential #g(3) #g(3) #g(3) #g
< 1 mcg/mL (S), 2 < 1 mcg/mL (S), 2 < 0.25 mcg/mL (S), 0.5 < 1 mcg/mL (S), 2
mcg/mL (I), > 4 mcg/mL mcg/mL (I), > 4 mcg/mL mcg/mL (I), > 1 mcg/mL mcg/mL (I), > 4 mcg/mL
(R) for (R) for (R) for (R) for
MIC breakpoint Enterobacteriaceae(2) Enterobacteriaceae(2) Enterobacteriaceae(2) Enterobacteriaceae(2)
< 4 mcg/mL (S), 8 < 4 mcg/mL (S), 8
mcg/mL (I), > 16 mcg/mL mcg/mL (I), > 16 mcg/mL
(R) for Gram-negative non- (R) for Gram-negative non-

1506 424
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#$%& 13 Carbapenems (#2)
Imipenem/cilastatin Meropenem Ertapenem Doripenem

(Tienam ) (Meronem ) (Invanz ) (Doribax)
lactose fermenters lactose fermenters
MIC breakpoint including Ps. aeruginosa, including Ps. aeruginosa,
Acinetobacter spp.(2) Acinetobacter spp.(2)
Imipenem 5l
a 1.5-2% m'4*$*$g6'l
imipenem/cilastatin ld4#
jol%%5
2*'
2 meningitis jlni5$g+$4+n # b'+'6i22 f*%%+%'l
lnii'61, ni6d4a#jo' (4
b#+ CrCl)(1-3)
ADRs (1-3)
meropenem 5l
62 imipenem m'l
a*6l meningitis
(16)
Ertapenem, doripenem +$d
62 imipenem, meropenem jg'm+$ GABA-A receptor affinity #g2
(2, 3)
Carbapenems 51
5l phlebitis a
(3)
+jgl
imipenem 2+65$g* seizure threshold (
2 ganciclovir) m%#1l
a'26
Drug interaction (2)
Carbapenems 51
+jgl
2+ valproic acid m5l%6 valproic acid l*j#g*'
Imipenem ti5*662' +$ b 2 ' l
l meningitis, Ertapenem +$ spectrum +$p57 c#2 Ps. aeruginosa
d 6 a h +" intra-abdominal infections, f42 carbapenems # f*% Acinetobacter spp.
dehydropeptidase-I (DHP-I) complicated SSTIs(2) jg u 4j QGR S TSUJ G $ 2 imipenem f*%
5$g a # m ' # ' l 2 + Meropenem +$b$ 4j Pseudomonas spp., meropenem j g 'm6+$
(2)
cilastatin hg ' e DHP-I +tl l bi ' (2 g Acinetobacter spp., affinity #2 PBP3 i'2
inhibitor &jgl imipenem IV q 8 hr) &jg Enterococcus spp.(3, 7) f#2+$ +$ b 2 ' l
l nosocomial
6 ' 4 ' % 5 7 & ( l meningitis d65l b$ 4j 6&$6'*% pneumonia, complicated
#2 1:1)(1-3)
6(2) 4o'(3) UTIs, complicated intra-
Imipenem mm%a+2 jo l IV infusion > 1
gd+' + l
l d4# abdominal infections,
(2)
b + meropenem j l$ critically ill
jo ESBL-producing SSTIs
jg 'm imipenem a+2ti patients ml extended organisms f*% anaerobes l IV infusion > 1
gd+'
b 5' efflux pump infusion (> 4 hr) &jg& g+ +$ b 2 'l
l community- j l$ critically ill
$ 6 meropenem T>MIC(2) acquired pneumonia (CAP), patients ml extended
+6#1 (3)
(MexAB-OprM) complicated UTIs, infusion (> 4 hr) &jg& g+
+$ b 2 ' l
l nosocomial complicated intra- T>MIC d64mj m'l
pneumonia, UTIs, intra- abdominal infections, acute NSS 500 mL &%+$4+
(2)
abdominal infections, pelvic infections, 4'#+2l D5W
gynecologic infections, complicated SSSIs
septicemia, IE, SSTIs, (including diabetic foot
bone and joint infections(2) without osteomyelitis),
b 500 mg 4 IV elective colorectal surgical
infusion 20-30 5$, b prophylaxis(2)
1,000 mg 4 IV infusion
40-60 5$ &%lf
IV push m%#1l

f*% phleblitis(3)
if6f*% Injections : 1 g (500/500 Injections : 500 mg/vial, Injections : 1 g/vial Injections : 500 mg/vial
4+f'5$g+$l mg)/vial 1 g/vial
%5a56

1506 424
2 2556 21
Aztreonam
e6#$6l*1+2 monobactams +$p57 c2f45$$6 (bactericidal) d666o''n'h**"(1, 2, 17)

Spectrum of activity : 44*1+|&% Gram-negative bacteria af2 HENPEKS, Pseudomonas aeruginosa
jg'm6ma|&% PBPs b' GNB f*%5#25*6b' beta-lactamases *6
(a+244*1+ Gram-
positive bacteria f*% anaerobes)(1, 2)
Clinical uses : UTIs, pneumonia, septicemia, skin and soft tissue infections, intra-abdominal infections,
gynecologic infections 5$g m GNB(2, 17)
jg'm aztreonam 44*1+|&% GNB +j aminoglycosides f#2a+2+$& #2a#f*%i m'ml
e
5'*jlni5$g$g6'#2 & #2a#m AMGs (renal-sparing alternative)(1, 17) f*%6'+$p57 c#2 gentamicin-
resistant strains 6(17)
Mechanisms of resistances : Enterobacteriaceae f*% Pseudomonas aeruginosa '6&71" jo#2 aztreonam
l6*' (acquired resistance) d6
jo*' outer membrane porins j'ah+" beta-lactamases
+5*66(1)
Aztreonam a+2+$ cross hypersensitivity beta-lactams *12+jgu m'l
a42b'*6lni5$g+$%# f&6
penicillins j cephalosporins(1-3)
#$%& 14 Aztreonam
Aztreonam
1-2 g IV q 6-8 hr (max. 8 g/day)
bl

(meningitis l 2 g IV q 6 hr)(2, 3)
Cmax 125 mcg/mL *'l 1 g IV(2)
Plasma protein binding 56%(2, 3)
Vd 0.11-0.22 L/kg(2, 3)
#f2'5$g6%m6aa$ %m6a$5g2'6 +t' prostatic tissue, aqueous humor, inflamed meninges(2)
CSF penetration
1%, 40%(3)
Urine excretion 60-70%(3)
t la## 1.7-2
gd+'(2, 3)
t l ESRD 7
gd+'(3)
#'bld4a# l
2(2, 3)
#'l

6*'5 HD l
2(2, 3)
#'bld4# a+2#'(3) jm* 20-25%(2)
Pregnancy cat. B(2, 3)
Allergic potential #g(3)
(2)
< 4 mcg/mL (S), 8 mcg/mL (I), > 16 mcg/mL (R) for Enterobacteriaceae
MIC breakpoint < 8 mcg/mL (S), 16 mcg/mL (I), > 32 mcg/mL (R) for Gram-negative non-lactose fermenters
including Ps. aeruginosa(2)
ADRs 4*jga m$6, 5'2', LFTs & g+bo
g 4, njg, transient eosinophilia, phlebitis(2, 3)
if6f*%4+f'5$g+$l%5a56 a+2+$m26l%5a56

1506 424
2 2556 22
Macrolide and Ketolides
Macrolides f*% ketolides +$d4''*e macrocyclic lactone ring

jg+#2+i2o#*(1)
Mechanism of action : p57 c66o'5$g 50s subunit of ribosome (domain V) b'f45$$6 2'n*l
joa+2+t
'd#$a(1, 2) m$o telithromycin 6'+$ alkyl-aryl side chain & hg'm binding site a$g'#f2'
(domain II) 5lm 50s af2bof*%tib5' efflux pumps a62 f*%6'4'+$p57 cl macrolide-
resistant strains 5$g+$ domain V binding site *$g6f*'a(1, 2)
Spectrum of activity : macrolides 44*1+f45$$6*6*12+ af2 Gram-positive bacteria '
(S.
pyogenes (GABHS), S. pneumoniae, MSSA), Gram-negative bacteria '
(Haemophilus influenzae '6
&71", Neisseria spp., Bordetella pertussis), atypical bacteria '
(Chlamydia spp., Mycoplasma spp.,
Legionella pneumophila, Rickettsia spp.), spirochetes '
(Treponema pallidum, Leptospira interrogans,
Borrelia burgdorferi), mycobacteria '
(Mycobacterium avium complex, Mycobacterium leprae) f#2p57 ca+2
d2a+22l*12+
jol (a+ f#2a+22h62' Jack of all trades, master of none)(1) f#26'tj2e65$g+$
%d6
"+ d6|&%l respiratory infections f*%d4#
jo'

2 atypical pathogens, MAC
infections (|&% clarithromycin, azithromycin), gonorrhea (|&% azithromycin)
Clinical uses: URIs (pharyngitis, tonsillitis, sinusitis), AECB, community-acquired pneumonia (CAP),
uncomplicated SSSIs, MAC prophylaxis/treatment, syphilis, gonococcal infections(2)
jof45$$6*6
+$jo6*12+ macrolides n2*6*a
2
o *n2 outer membrane b'
jo GNB(1)
o ' efflux pump &jgb6mh**"
2 S. pneumoniae +$ mef gene hg'' efflux pump(1)
o *$g6f*' binding site ribosome 5lm6a**' (enzyme-mediated ribosome binding site
alteration)
2 S. pneumoniae +$ erm gene hg'5l methylation b' binding site ribosome hg'
jo6n2*a$o+5l job+j51#6l*12+ macrolides(1, 18) +t'6jg5$gm 50s
binding site $6
2 clindamycin, quinopristin/dalfopristin
#$%& 15-1 Macrolides and ketolides
Roxithromycin Clarithromycin Azithromycin
Erythromycin
(Rulid)
(Klacid ) (Zithromax)
14-membered ring 14-membered ring 14-membered ring 15-membered ring
*12+626
macrolides(1) macrolides(1) macrolides(1) azalides(1)
500 mg PO q 12 hr
250-500 mg PO q 6 hr 150 mg PO q 12 hr 500 mg loading dose then
bl
j 1,000 mg PO q 24 hr
j 0.5-1 g IV q 6 hr(2, 3) j 300 mg PO q 24 hr (19)
250 mg PO q 24 hr(2, 3)
(Klacid MR 2 tab OD)(2, 3)
50% 50-55%(2, 3) 35-37%(2, 3)
Absorption 20-50%(2, 3) (4%52 (4%52 (4%52
&%
%*ih+) &%
%*ih+) &%*ih+)
0.1-2 mcg/mL *' 7.9 mcg/mL, 10.8 2-3 mcg/mL * ' 0.4 mcg/mL * '
% 5 5 0 0 mg mcg/mL, 12.24 mcg/mL %5 500 mg(2) %5 500 mg af*
(erythromycin base, * ' %5 150 mg, 2
gd+' (l5$g 5 b'
Cmax stearate, ethyl succinate)(2) 300 mg, 450 mg #+* )(2)
(19)
2 mcg/mL * ' 3.63 mcg/mL *'l 500
% 5 5 0 0 mg mg IV af* 1
gd+' (l
(erythromycin estolate)(2) 5$g 5 b')(2)

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#$%& 15-1 Macrolides and ketolides (#2)
Erythromycin
(Rulid) (Klacid) (Zithromax)
3-4 mcg/mL *'l 500
mg IV(2)
Plasma protein
70-90%(2, 3) 87-96% 42-72%(2, 3) 10-50%(2, 3)
binding
Vd 0.5 L/kg(3) 3 L/kg(3) 31 L/kg(3)
%+lh**"4+b+bi'
%+l PMNs 4+b+b
#f2'5$g6 Most body tissue and %+lh**"4+b+bi' (10-100 52b'4+b+b
i' (30 52b'4+b+b
%m6aa$ fluids(2) (2)
l*j)
2 PMNs,
l*j)
fibroblasts(2)
#f2'5$g6
%m6aa CNS(2) CNS, aqueous humor(2)
6
CSF penetration 2-13%(2, 3) < 10%(3) < 10%(3)
Bile penetration a+2+$b+i*(3) a+2+$b+i* 7,000%(3) > 3,000%(3)
#e* #e* #e* #e*(2, 3)
Metabolism
(N-demethylation)(2, 3) (descladinose metabolite) (14-hydroxy metabolite)(2, 3) (demethylation)
Urine excretion 5% (unchanged)(3) 7% 20% (unchanged)(3) 6% (unchanged)(3)
12
gd+'(2, 3)
t la## 1.4-2
gd+'(2, 3) 10.5-12
gd+'(19) 5-7
gd+'(2, 3)
(intracellular t 68
gd+')
a+2#'
#'bl l
2
a+2#'(2, 3) a+2#' (f#2l%+%'l
l
d4a# (+jg CrCl < 10)(2, 3)
CrCl < 10)(2, 3)
#'l

6
a+2#'(2, 3) a+2#'(3) a+2#'(2, 3)
*'5 HD
a+2#'(3) l
2
#'bl
(m#'l severe (l severe hepatic a+2#'(2, 3) a+2#'(2, 3)
d4#
hepatic impairment)(2) impairment)
B(2, 3)
(*$*$g6' erythromycin
Pregnancy cat. B C(2, 3) B(2, 3)
estolate lw '+$4"
&%$g6'#2 hepatotixicity)
Allergic potential #g(3) #g #g(3) #g(3)
< 0.25 mcg/mL (S), 0.5 < 0.5 mcg/mL (S), 1
mcg/mL (I), > 1 mcg/mL mcg/mL (I), > 2 mcg/mL
(R) for Staphylococcus (R) for Streptococcus
MIC breakpoint spp.(2) spp.(2)
< 8 mcg/mL (S), 16 < 4 mcg/mL (S) for
mcg/mL (I), 32 mcg/mL (R) Haemophilus spp.(2)
for Haemophilus spp.(2)
(1-3)
4*jga m$6, 5', 5'2' (d6|&% erythromycin jg'm6%#1*g' motilin)
(1-3)
Hepatotoxicity
2 #, $h2 (4%+%'l
lni5$g+$d4#6i22 f*%# #+f', LFTs)
QTc prolongation, TdP (4%+%'l
2+6jg5$g5l QTc prolongation, l
lni5$g+$ arrhythmias j
ADRs
heart block 6i22)(1-3)
(2)
Ototoxicity (reversible dose-dependent hearing loss)
(2)
IV erythromycin, IV azithromycin 5l phlebitis a

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Erythromycin
(Rulid ) (Klacid ) (Zithromax)
Erythromycin f*% clarithromycin e CYP1A2, CYP3A4 inhibitor 5l%65$ge Azithromycin +$# 6
CYP1A2, CYP3A4 substrates i'bo(1, 2)
2 + amiodarone, procainamide, cisapride % 2 ' 6 6 2
m5l QTc prolongation j TdP(3), + digoxin, ergot alkaloids, phenytoin, macrolides # jg (2, 3)
Drug interaction
carbamazepine, valproic acid, cyclosporine, theophylline 5l%6*2$oi'bom jg 'm 6 6o ' CYP3A4
m %& (3), + statins & g+4+$g6'#2 myopathy, rhabdomyolysis(3), + warfarin &$6'*6(1, 2)
(3)
5l INR i'bo
(1)
Erythromycin, roxithromycin, clarithromycin +$p57 c#2 GNB 62 azithromycin jg'm azithromycin +$d4''5$g
ti1'lf5n2 outer membrane b' GNB (H. influenzae, M. catarrhalis, N. gonorrhoeae, E. coli, Salmonella
spp., Shigella spp.) a$bo(2)
Azithromycin f*% telithromycin +$djo6#g f*%an*$
jo5$gjo#2 14-membered ring macrolides (erythromycin,
roxithromycin, clarithromycin) jg'm+$d4''5$gf##2'a(3)
Erythromycin +$b 2'l
af2 pharyngitis, tonsillitis, sinusitis, acute otitis media, AECB, pertussis, CAP,
uncomplicated SSSIs, preoperative bowel preparation (2+ neomycin)(2) m$o6'+$ off-label use l diabetic
gastroparesis &jg& g+ GI motility(20)
a+24l
erythromycin e6fl URIs jg'm&1# "jo6 erythromycin b' S. pneumoniae
l%5a56i't' 65%
Clarithromycin +$b2'l
4*6 erythromycin f#2m$o6'l
l Helicobacter pylori eradication therapy (2+ PPIs
+6#1
f*% amoxicillin), ' (6$g6) f*% MAC infections (2+ ethambutol + rifabutin)(2, 21)
(3)
Klacid MR +$ GI side effects #g2 clarithromycin if6+7+
Azithromycin +$b2'l
4*6 clarithromycin f#2m$o6'l
l urethritis and cervicitis 5$g m N. gonorrhoeae, C.
trachomatis, syphilis, chancroid, ' (6$g6) f*% MAC infections (2+ ethambutol + rifabutin),
leptospirosis, scrub typhus, toxoplasmosis (2+ pyrimethamine), falciparum malaria (2+
artesunate)(2, 21)
Azithromycin +$ Vd i'+ (6%+ljo6jgi') hg'm%426u ti**26i2%f*j#2a$*'61l
6
2
l6 5 m%5l+$ serum therapeutic level t' 10 (1)

bl
b' azithromycin l indications |&% af2 2 g PO single dose (prolonged-release granules, Zmax ) l
acute bacterial sinusitis, CAP(2, 3), 2 g PO single dose (capsules) l gonococcal infections(2, 3), 1 g PO single dose
(capsules) l chlamydial infections, chancroid(2, 3), 1,000-1,250 mg PO once weekly l MAC prophylaxis(2, 3)
Dry syrup : 125 mg/5 mL Tablets : 100 mg, 150 Dry suspension : 125 Dry suspension : 200
(estolate), 200 mg/5 mL mg, 300 mg mg/5 mL mg/5 mL, 100 mg/sachet
if6f*% (ethylsuccinate) Tablets : 250 mg, 500 Capsules : 250 mg
4+f'5$g+$l Tablets : 250 mg, 500 mg Prolonged-release
%5a56 mg (stearate) Modified release tablets : granules : 2 g/bottle
500 mg (Klacid MR) (Zmax)
Injections : 500 mg/vial Injections : 500 mg
#$%& 15-2 Macrolides and ketolides

Midecamycin Spiramycin Telithromycin
(Midecamycin Meiji, Miotin) (Rovamycine) (Ketek)
*12+626 16-membered ring macrolides 16-membered ring macrolides 14-membered ring ketolides(1, 17)
1,000 mg (3 million units) PO q 800 mg PO q 24 hr x 5 (sinusitis, AECB)(2,
400 mg PO q 8-12 hr 3)
bl
8-12 hr
(max. 1,200 mg/day)
(max. 3,000 mg/day) 800 mg PO q 24 hr x 7-10 (CAP)(2, 3)
57%(2, 3)
Absorption 30-40%
(%52j*'a)

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(Midecamycin Meiji, Miotin) (Rovamycine) (Ketek)
2.5 mcg/mL *'%5 a 3.3 mcg/mL *'%5 2-2.9 mcg/mL *'%5 800 mg af* 1
Cmax
f* 1-2
gd+' 2,000 mg (6 million units)
gd+'(2)
Plasma protein
10% 60-70%(2, 3)
binding
Vd 2.9 L/kg(2, 3)
%+ljo 6jgi' (2-8 52b'4+b+bl
#f2'5$g6 Lungs, spleen, kidney, liver, Lungs, tonsils, infected sinuses,
*j)
2 bronchial mucosa, epithelial lining
%m6aa$ gallbladder, subcutaneous tissue bones, saliva
fluid, alveolar macrophages(2)
Metabolism #e* #e* #e* (70%)(2, 3)
Urine excretion 4-5% 10% 13% (unchanged)(2, 3)
t la## 2.5
gd+' 8
gd+' 10
gd+'(2, 3)
#'bl l
2
a+2#'
d4a# (+jg CrCl < 30)(2, 3)
#'l

6
a+2#'(2, 3)
*'5 HD
#'bl a+2#'(2, 3)
d4# f#2ll
64+%+%'
Pregnancy cat. C(2, 3)
Allergic potential #g #g #g(3)
ADRs 4*6 macrolides m$o6'm5
l $ %, ' $ 6 , #&2 , &h
ADRs ADRs 4*6 erythromycin
(diplopia), %*+jo2f'a6 (m'+$b
+l
lni6 myasthenia gravis)(1-3)
Midecamycin 66o' CYP3A4 Spiramycin a+2 +$ # 6 e strong CYP3A4 inhibitor +$# 6
l % * ' ( +j %2 '6 jg 'ma+2 6 6o ' 4*6 erythromycin(1, 2)
(3)
roxithromycin, clarithromycin) CYP3A4 +$ b +l
2 + cisapride , 5 l %
ergot alkaloids i'bo , & g+4+$g6'#2 statin-
associated myopathy(3), m5l INR i'bo+jg
l
2+ warfarin(3)
16-membered ring macrolides +$p57 c#2 Gram-positive bacteria H. influenzae, Bodetella pertussis, atypical
(GABHS, S. pneumoniae, MSSA) a+2 #2 'm erythromycin, pathogens (Chlamydia, Mycoplasma,
roxithromycin Legionella) a#2 telithromycin f#2
S. pneumoniae 5$gjo#2 14- f*% 15-membered ring macrolides d6 Enterobacteriaceae jo #2 6$o , p57 c #2
' efflux pump (mefA, mefE gene) m%6'4'a#2 16-membered ring Neisseria spp. mycobacterium f*% spirochete
macrolides, clindamycin, quinupristin/dalfopristin 6'a+2+$+(1, 2, 17)
a'll
l respiratory infections

2 CAP 5$g m S. pneumoniae (5o' PSSP,
+6#1
PRSP, macrolide-resistant strains), H.
influenzae, M. catarrhalis, Mycoplasma
pneumoniae, Chlamydophila pneumoniae(1, 2,
17)
f45$ $ 6 '6& 71" jo #2 telithromycin

d6*$g6f*' ribosome binding site 5o' 2
#f2' (domain II f*% domain V) 5l6a+2
+tma

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2 2556 26

(Midecamycin Meiji , Miotin ) (Rovamycine ) (Ketek)
Dry syrup : 200 mg/ 5 mL Tablets : 500 mg (1.5 million a+2+$m26l%5a56
if6f*% (Miotin) units)

4+f'5$g+$l Tablets : 200 mg (Miotin )
%5a56 Capsules : 200 mg
(Midecamycin Meiji)
Aminoglycosides
Aminoglycosides (AMGs) +$d+*1*42b'lw2f*%+$%m1 f#26'n2 outer membrane porins b' GNB a
f*%6hg'+$%m1m%m outer membrane hg'+$%m1* 5l i
g4 (transient holes)(1) (d6#
AMGs n2bi2h**" Gram-positive bacteria aa+2$ jg'm+$n'h**" f*%a+2+$ porins)(1, 2)
Mechanism of action : p57 c66o'5$g 30s subunit of ribosome b'f45$$6 2'n*l
joa+2+t'd#$
a(1, 2) d625$g AMGs m%at'+6 #'n2 cytoplasmic membrane hg'e active transport 5$g 6&*''
d6l
oxygen f*% active proton motive force m'e#1n*5$g AMGs a+2+$p57 c#2 anaerobes f*%p57 caa+2$
l%ef*%ah m
2 abscess(1)
Spectrum of activity : AMGs +$p57 c$+ (excellent activity) #2 GNB
2 H. influenzae, Enterobacteriaceae,
Ps. aeruginosa(1, 2) m$o streptomycin, kanamycin 6'+$p57 c#2 Mycobacterium tuberculosis, MAC 6(1)
Clinical uses : +l
lb#g&jg +p57 c (synergistic dosing) cell wall-active agents (beta-lactams j
vancomycin) ld4#
jof45$$6f+*f*%f+ jg'm beta-lactams j vancomycin m%
66o'' cell wall 5l AMGs bh**"a+bo(2) f*%a+24l
AMG monotherapy l serious infections
(6 $ UTIs)(2, 7)
Mechanisms of resistance : &jo6*12+ AMGs 42b'#g f+2m%+$l
+2 50 #+ d6
jo6m n2*a*2$o
o ' efflux pump &jgb6mh**"
o 'ah+" 5$g *$g 6 f*'d4' '6 (AMG-modifying enzymes)
2 acetyltransferases,
nucleotidyltransferases, phosphotransferases 5l6a+2+tm ribosome a$#2a(1, 18)
o *$g6f*' binding site ribosome 5lm6a**'
AMGs +a+2job+l*12+ jg'm6f#2*%#+$ side chain 5$gm&%
2
jo5$gjo#2 gentamicin, tobramycin
m6'a#2 amikacin(2)
#$%& 16 Aminoglycosides
Amikacin
Gentamicin Tobramycin Streptomycin
(Amikin)
15-20 MKD 5-7 MKD 5-7 MKD 15 MKD j 1 g IM q 24
(b synergy 7.5 MKD) (b synergy 2.5-3 MKD) (b synergy 2.5 MKD) hr (t61 > 60 4*
bl
a, b, c
l OD jf2'l51 12 l OD jf2'l51 8 l OD jf2'l51 8 *j 750 mg IM q 24 hr)(2,

gd+' a(2, 3)
gd+' a(2, 3, 7)
gd+' a(2, 3) 3)

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#$%& 16 Aminoglycosides (#2)
Amikacin
(Amikin)
17-25 mcg/mL *'l 7.5 6 mcg/mL *'l 1.5 6 mcg/mL *'l 1.5 mg/kg 25-50 mcg/mL *'l 1 g
Cmax
mg/kg IV a 1-2
gd+'(2) mg/kg IV(2) IV(2) IM(2)
Plasma protein
0-10%(2, 3) 0-10%(2, 3) 0-10%(2, 3) 0-10%(2, 3)
binding
Vdd, e 0.25 L/kg(3) 0.3 L/kg(3) 0.24 L/kg(3) 0.26 L/kg(3)
#f2'5$g6 Extracellular fluid, ascetic fluid, pericardial fluid, pleural fluid, synovial fluid, lymphatic fluid, peritoneal fluid,
%m6aa$ endolymph i
ol, kidneys(2)
#f2'5$g6
Bile, aqueous humor, bronchial secretions, abscesses, sputum, CSF(2)
%m6aa6
CSF penetration
(non-inflamed, 15%, 20%(3) 0%, 20%(3) 0%, 20%(3) 20%(3)
inflamed meninges)
Bile penetration 30%(3) 30%(3) 30%(3) a+2+$b+i*(3)
Urine excretion 95% (unchanged)(2, 3) 95% (unchanged)(3) 95% (unchanged)(3) 90% (unchanged)(2, 3)
t la## 2-4
gd+'(2, 3) 2.5
gd+'(3) 2-4
gd+'(2, 3) 2-4
gd+'(2, 3)
t l ESRD 50
gd+'(3) 48
gd+'(3) 56
gd+'(3) 100
gd+'(3)
#'bl
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 3)
d4a#
#'l

6*'
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 3)
5 HD
#'bl
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
d4#
Pregnancy cat. D(2, 3) D(2, 3) D(2, 3) D(2, 3)
Allergic potential #g(2, 3) #g(3) #g(2, 3) #g(3)
16 mcg/mL (S) for 4 mcg/mL (S) for 4 mcg/mL (S) for
Enterobacteriaceae, Ps. Enterobacteriaceae, Enterobacteriaceae, Gram-
(2)
MIC breakpoint aeruginosa Gram-negative non- negative non-lactose
lactose fermenters fermenters including Ps.
including Ps. aeruginosa(2) aeruginosa(2)
Nephrotoxicity m AMGs &a 5-10% jg'm AMGs %+l proximal tubular cells a42b'i' f#2+*e
# a, f' af2 & urine casts, serum creatinine f*% BUN i'bo, +a+2+$%v%6 (non-oliguric
ARF)(1)
vmm6$g 6'#2 AMG nephrotoxicity af2 i' 61, +$5'b'a#&2 '6i22 , hypovolemia, a2+
nephrotoxic agents jgu, l
6 > 7 , Ctrough 5$gi'(1, 2)
Ototoxicity m AMGs f2'e
- Cochlear toxicity (&a%+ 30% b' otoxicity m AMGs) ni6miw$6a6 l
2'4*jg4+t$gi'
(decreased high frequency hearing) f*%+a+2*e# (irreversible)(1, 2)
ADRs
- Vestibular toxicity (&a%+ 60% b' otoxicity m AMGs) ni6m%+$h, +1 (vertigo), +$$6'li
(tinnitus), #%#1 (nystagmus) hg' vestibular toxicity + bo2 cochlear toxicity(1, 2)
vmm6$g6'#2 AMG ototoxicity af2 i'61, +$5'b'a#&2'6i22, hypovolemia, a2+ ototoxic
agents jgu, l
6 > 3 , Cpeak 5$gi', +$%# 4l4446 AMG ototoxicity(2)
Neuromuscular blockade (
2 apnea, paralysis) hg'+&7" rapid infusion m'#'l IV infusion > 30-60 5$ f*%l

64+%+%'lni6 myasthenia gravis(2)

, chemical meningitis, radicular pain (l$5$gl intrathecal j intraventricular injection), bronchospasm (l$
5$gl aerosolized AMG)

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2 2556 28
Amikacin
(Amikin)
a2+ nephrotoxic drugs jgu (
2 amphotericin B, vancomycin, colistin, foscarnet, cidofovir, pentamidine,
NSAIDs, cyclosporine, cisplatin, contrast media) & g+4+$g6'#2 nephrotoxicity +bo(2)
(2)
Drug interaction a2+ ototoxic drugs jgu (
2 cisplatin, loop diuretics, macrolides) & g+4+$g6'#2 ototoxicity +bo
a2+65$g66o' NMJ (
2 nondepolarizing neuromuscular blocking agents, colistin) & g+4+$g6'#2
neuromuscular blockade(2)
l f once daily l f once daily l f once daily
dosing : Cpeak 65-75 dosing : Cpeak 16-24 dosing : Cpeak 16-24
mcg/mL, Ctrough < 4 mcg/mL, Ctrough < 1 mcg/mL, Ctrough < 1
mcg/mL(2) mcg/mL(2) mcg/mL(2)
Therapeutic
lf q 12 hr : Cpeak lf q 8 hr : Cpeak 8- lf q 8 hr : Cpeak 8-
serum
20-30 mcg/mL (25-35 10 mcg/mL, Ctrough 1-2 10 mcg/mL, Ctrough 1-2
concentrations
mcg/mL $ severe infxs, mcg/mL(2) mcg/mL(2)
pneumonia, pseudomonal
infections), Ctrough < 10
mcg/mL(2)
(1, 2)
Gentamicin e AMG 5$g 6+l
+5$g1 f*%44*1+ enterococci Streptomycin l
l
nd
Tobramycin +$ spectrum 4*6 gentamicin (6 a+244*1+ enterococci m'a+24l
tuberculosis (e 2
enterococcal infections) 'o
jo5$gjo#2 gentamicin +m%jo tobramycin 6(1) line drug) f*% enterococcal
(2, 7)
Amikacin f*% tobramycin +$p57 c# Ps. aeruginosa $2 gentamicin f#2b$6b' endocarditis ($ jo #2
amikacin 4j f5a+2+$p57 c#2 enterococci(1, 2) gentamicin d6l
2 +
(2)

jo 5$gjo #2 gentamicin, tobramycin m%6'a#2 amikacin jg'm amikacin +$ s-4 ampicillin)
amino 2-hydroxybutyryl (AHB) side chain
26'5*66m AMG-modifying Streptomycin e AMG
enzymes(2) 5$g+$ otoxicity i'5$g1 (2
Neomycin +$|&%if6%5 hg'm%a+2tiih+m5' l
l2 lw2e vestibular toxicity)

jo l*a2 n2#l
2 '5 ' (preoperative bowel preparation) d6l2 + f#2+$ nephrotoxicity #g5$g1
erythromycin, * +
jof45$$6l*a&jg hepatic encephalopathy f*%n+ (2, 3)
l6+fm4 (Mybacin)(1, 2)
a
AMGs +l
+p57 c (synergy) 6*12+jgu
2 beta-lactams d6l
lb#g
2l
AMGs e6$g6 (monotherapy) +$|&%l UTIs 52o(2)
b
b6 AMGs #'4#+ ideal body weight (jl
actual body weigh t+$42
+6#1
#g2 IBW jl
dosing body weight t actual body weight i'2 IBW +) jg'm
6%m6#|&%l25$geo(2)
c
6f once daily dosing (OD) *4+e& #2a#f*%& #2ia f#2a+2
4l once daily dosing lni5$g+$5'b'a#&2' (CrCl < 60 mL/min) j
5'b'a#a+24'5$g, enterococcal endocarditis, %5$g+$ Vd i'bo (edema, ascites,
pregnancy)(2)
d
Vd & g+bo l%5$g2'6+$4g'oj+$o%+l
2'#2'u
2 edema, ascites,
trauma, septic shock, burns, pregnancy hg'm#'& g+b AMGs m# (2)
e
Vd **' l%5$g2'6+$o6*'
2 dehydration, obesity (+$ab++2o) hg'
m#'*b AMGs m# (2)
%+%'l AMGs f intrathecal (IT) j intraventricular (
2 amikacin 10-40
mg IT q 24 hr, gentamicin 5 mg IT q 24 hr) &%+$ neurotoxicity
2
, chemical
meningitis, radicular pain hg' m#6'f*% sodium bisulfite hg'et+li#
#(2)
+$l aerosolized AMGs (
2 tobramycin 300 mg NB q 12 hr) &jg#
jo5$g

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Amikacin
(Amikin)

2 Pseudomonas aeruginosa, Acinetobacter baumannii f#2#'l2+ IV AMGs
+ &%&2662'$6l%6ljo6jga+2&$6'& hg'm5l jo 6a
(2)
+n+ AMGs l*%*6 sodium bicarbonate, beta-lactams
Injections : 250 mg/2 Injections : 20 mg/2 a+2 +$ m 2 6l%5 Injections : 1 g/vial, 5
mL, 500 mg/2 mL mL, 80 mg/2 mL a56 g/vial
if6f*%
Beads : 7.5 mg per
4+f'5$g+$l
PMMA bead (Septopal
%5a56
v ' l%i &jg
osteomyelitis)
Fluoroquinolones
Mechanism of action : p57 c66o'ah+" topoisomerases 2

af2 topoisomerase II (DNA gyrase) f*%
topoisomerase IV hg'441+ DNA supercoiling d66m%bmah+"*'m
2'5$g+$#6 DNA f* 5
l6 DNA a+2+t
jg+#24j (relegation) 2'n*l
jo#662'(1, 2, 17)
Spectrum of activity : 44*1+ Gram-positive bacteria '
(GABHS, S. pneumoniae, viridans group
streptococci, MSSA) f*% Gram-negative bacteria 2lw2 af2 HENPEK, Salmonella, Shigella (+ Ps.
aeruginosa |&% ciprofloxacin, levofloxacin, moxifloxacin), anaerobes '
, atypical bacteria (Chlamydia,
Chlamydophila, Mycoplasma, Legionella), mycobacteria (M. tuberculosis, MAC)(1-3)
Clinical uses : FQs 2lw2 (6 moxifloxacin) l
l UTIs jg'm44*1+ GNB f*%tib5'
v%e*lia+2*$g6f*', prostatitis, gastrointestinal infections, intra-abdominal infections, SSTIs,
osteomyelitis(2, 3) m$o respiratory FQs (ciprofloxacin, levofloxacin, moxifloxacin) 6'l
l sinusitis, AECB,
pneumonia 6(2, 3)
FQs +$l
26lvmm1 jg'm oral bioavailability $6$g6+ (70-99%) +% IV-oral switch therapy f*%
+$n*a+2&'%'4"42b'6 f#26*12+$o+$b$6 4j jo642b''26(1)
Gatifloxacin (Tequin) titm5'#*+jg 2008 jg'm+$6'25l hypoglycemia j
hyperglycemia lni65$ga6*o#*l*j(17)
#$%& 17-1 Fluoroquinolones
Norfloxacin Ofloxacin Ciprofloxacin Levofloxacin Moxifloxacin
(Lexinor) (Tarivid) (Ciprobay) (Cravit) (Avelox)
*12+626 2nd gen. FQs(17) 2nd gen. FQs(17) 2nd gen. FQs(17) 3rd gen. FQs(17) 4th gen. FQs(17)
250-750 mg PO/IV q
250-750 mg PO q 12 24 hr
200-400 mg PO q 12 hr, 400 mg IV (1 hr (UTIs l
250-500 400 mg PO/IV (1 hr
bl
400 mg PO q 12 hr(2) (2, 3) (2, (2, 3)
hr infusion) q 8-12 hr mg/day, sinusitis, infusion) q 24 hr
3) pneumonia, SSTIs l

(2, 3)
750 mg/day)

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#$%& 17-1 Fluoroquinolones (#2)
30-40%
Absorption 95-98%(2, 3) 50-85%(2, 3) 98-99%(2, 3) 90%(2, 3)
(#5'2')(2)
4.6 mcg/mL *' 2.5-4.3 mcg/mL 5.7 mcg/mL *'
%5 400 mg(2) * ' %5 750 %5 500 mg(2) 4.5 mcg/mL *'
1.4-1.8 mcg/mL *'
Cmax 5.2-7.2 mcg/mL mg(2) 6.2 mcg/mL *'l %5 400 mg
%5 400 mg(2)
*'l 400 mg IV(2) 4.6 mcg/mL *'l 500 mg IV(2) af* 2
gd+'(2)
400 mg IV(2)
Plasma protein
10-15%(2) 32%(3) 13-43%(2, 3) 24-38%(2, 3) 48-50%(2, 3)
binding
Vd 1.7 L/kg(3) 2 L/kg(3) 2.5 L/kg(3) 1.3 L/kg(3) 2.7-3.5 L/kg(2, 3)
Kidneys, prostatic Kidneys, prostatic Kidneys, prostatic Kidneys, prostatic
tissue, testicle, tissue, female tissue, female tissue, female
seminal fluid, female reproductive tissues, reproductive tissues, reproductive tissues,
reproductive tissues, lungs, sputum, lungs, sputum, sputum, maxillary
#f2'5$g6 sputum, maxillary phagocytic cells, phagocytic cells, sinus mucosa,
%m6aa$ sinus mucosa, gallbladder, bile, gallbladder, bile, tonsils, blister fluid,
(2)
tonsils, blister fluid, liver liver, skin, fat, gallbladder, bile,
(2)
gallbladder, bile, muscle, bone, liver
(2)
liver cartilage, inflamed
meninges(2)
CSF penetration
(non-inflamed, < 10%(3) 10%, 26%(3) 16%(3) < 10%(3)
inflamed meninges)
Bile penetration 1,500%(3) 3,000%(3) a+2+$b+i*(3) a+2+$b+i*(3)
70% (unchanged and 68-90% 50-70%
Urine excretion 87% (unchanged)(2, 3) 20% (unchanged)(3)
metabolites)(2) (unchanged)(2, 3) (unchanged)(2, 3)
t la## 4
gd+'(2) 6-7
gd+'(2, 3) 4
gd+'(2, 3) 7
gd+'(2, 3) 12-13
gd+'(2, 3)
t l ESRD 40
gd+'(3) 8
gd+'(3) 12
gd+'(3)
#'bl
l
2(2) l
2(2, 3) l
2(2, 3) l
2(2, 3) a+2#'(2, 3)
d4a#
#'l

6
l
2(2) l
2(2, 3) l
2(2, 3) l
2(2, 3) a+2#'(2, 3)
*'5 HD
#'bl
a+2#'(2) a+2#'(2, 3) a+2#'(2, 3) a+2+$b+i*(2, 3) a+2#'(3)
d4#
Pregnancy cat. C(2) C(2, 3) C(2, 3) C(2, 3) C(2, 3)
Allergic potential #g(3) #g(3) #g(3) #g(3) #g(3)
< 1 mcg/mL (S), 2 < 1 mcg/mL (S), 2 < 1 mcg/mL (S), 2 < 0.5 mcg/mL (S),
mcg/mL (I), > 4 mcg/mL (I), > 4 mcg/mL (I), > 4 1 mcg/mL (I), > 2
mcg/mL (R) for mcg/mL (R) for mcg/mL (R) for mcg/mL (R) for
Staphylococcus Enterobacteriaceae, Staphylococcus Staphylococcus
MIC breakpoint spp.(2) Ps. aeruginosa, spp.(2) spp.(2)
< 2 mcg/mL (S), 4 Acinetobacter spp., < 2 mcg/mL (S), 4 < 1 mcg/mL (S), 2
mcg/mL (I), > 8 Staphylococcus spp., mcg/mL (I), > 8 mcg/mL (I), > 4
mcg/mL (R) for S. Enterococcus spp.(2) mcg/mL (R) for mcg/mL (R) for S.
pneumoniae(2) Enterobacteriaceae, pneumoniae(2)

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Ps. aeruginosa,
Acinetobacter spp.,
S. pneumoniae,
Enterococcus spp.(2)
(2, 3, 17)
4*jga m$6, dyspepsia &a 5-10%
Tendinitis, Achilles tendon rupture (e class effect) d6vmm6$g6' af2 61 > 60 , a2+ corticosteroids, +$
(1-3, 17)
5'b'a#&2'
Arthropathy 4*$*$g6'l
FQs lw '+$4" f*%ni5$g61 < 18 jg'm&2+$n*#2%i2b'#"5*'5$g
6'a+2d##+6(17)
(1, 2, 17)
CNS side effects
2 $%, '$6, a+2* &%+ 5%

(2lw2&l IV ciprofloxacin) 4%+%'l
lni6d4*+
, ni5$g+$5'b'a#&2', a
ADRs
2+ NSAIDs, foscarnet(2, 3, 17)
QTc prolongation, TdP (2lw2&l IV moxifloxacin, IV gatifloxacin) 4%+%'l
2+ proarrhythmic drugs
(
2 amiodarone, procainamide, cisapride) j lni 5$g+$ arrhythmias j heart block 6i22, uncontrolled
hypocalcemia(1-3, 17)
(2, 17)
n*a+2&'%'4"#2n '
2 njg (1-2%), photosensitivity
+$'6'%12 FQs 5l C. difficile-associated diarrhea a2626#m1*
$&*1+ 2 jgu(2)
(2)
n*a+2&' %'4"jgu 5$g&a+226 af2 leucopenia, LFT abnormalities
3+ 2+ 2+ 2+ 2+ 2+
FQs 51# chelation polyvalent cations (Al , Mg , Ca , Fe , Zn , Bi )
2 antacids, buffered didanosine (+$
magnesium-based antacids li##), sucralfate, calcium supplements, +f*%n* #"m+, enteral feeding, iron
supplements, bismuth subsalicylate) 5l6ih+a**' m'4l2' > 2
gd+'(2, 3, 17)
(2)
Sevelamer *ih+b' moxifloxacin m'4l moxifloxacin 2 > 2
gd+'
Drug interaction
a2+ anti-arrhythmic drugs (class Ia f*% class III)
2 quinidine, procainamide, amiodarone, sotalol m
2' +l QTc prolongation(2)
Ciprofloxacin e CYP1A2 inhibitor # 6 theophylline, phenytoin, warfarin (CYP1A2 substrates) 5l
%6l*jb'6*2$oi'bomm %& (3)
b 2 ' l
* b' Ofloxacin 4j +$ piperazine side Levofloxacin +$ +$ methoxy group
norfloxacin a f 2 racemic mixture b' chain 5 l +$ PK/PD $ 2 f*% 5$g#f2' C8 5l+$
infectious diarrhea, dextro-form (a+2 +$ antipseudomonal potency i ' 2 p 5 7 c #2 anaerobes
(1, 3)
UTIs, prostatis, p57 c ) f*% levo-form activity f#2p57 c#2 ofloxacin %+ 2 (
2 Bacteroides
spontaneous (+$p57 c) 62'*%52u Gram-positive 52(1-3) fragilis) & g + bo f*%
(1)
bacterial peritonitis bacteria (MSSA, S. 441 * + Gram- *d jo6
(2)
(SBP) prophylaxis pneumoniae) **'(7) positive bacteria (
2 (2, 3) f#25lp57 c#2
m'a+24l
l severe PSSP, PRSP, GNB **' d6|&%
infections 5$g m MSSA) a$(2, 7) f*%+$ Ps. aeruginosa
+6#1 S. pneumoniae antipseudomonal (antipseudomonal
activity (bl
750 activity #g 2
mg/day)(1, 3) ciprofloxacin f*%
+$ levofloxacin)(2)
levofloxacin +l
l e FQ 5$g
H. pylori eradication 4 4 *1 + Gram-
therapy (2+ PPI positive bacteria (
2
+ amoxicillin j PSSP, PRSP,
metronidazole) l6 MSSA) a$5$g1(2, 7)
5$gjo clarithromycin(3)

1506 424
2 2556 32
e FQ &$ 6 '#
$ 6 5$g a +2 l
l UTIs
jg'm6tib
(2, 3)
5'v%6
Tablets : 100 mg, Tablets : 100 mg, Tablets : 250 mg, Tablets : 100 mg, Tablets : 400 mg
200 mg, 400 mg 200 mg, 300 mg 500 mg 250 mg, 500 mg Injections : 400
Modified release Injections : 250 mg/250 mL
if6f*% tablets : 500 mg, 1 g mg/50 mL, 500
4+f'5$g+$l (Cifran OD) mg/100 mL, 750
%5a56 Injections : 100 mg/150 mL
mg/50 mL, 200
mg/100 mL, 400
mg/200 mL
#$%& 17-2 Fluoroquinolones

Prulifloxacin Sitafloxacin Rufloxacin
(Darflox) (Gracevit) (Uroflox)
*12+626 4th generation FQs 4th generation FQs 2nd generation FQs
50 mg PO q 12 hr(24),
600 mg PO q 24 hr x 10 (AECB,
400 mg IV (1 hr infusion) q 24 hr (l 400 mg lf #+6 200 mg
bl
complicated lower UTIs) j single
severe systemic infections 5$g m PO q 24 hr x 7-9 (26, 27)
dose (uncomplicated lower UTIs(22, 23)
MRSA, VRE)(25)
Absorption 70-94%(28, 29) 50%(27)
4.65 mcg/mL *'%5 500
2.56-4.4 mcg/mL *'%5 400
Cmax 2 mcg/mL *'%5 600 mg(23) mg(28), 5.53 mcg/mL *'l 400 mg
mg af* 2
gd+'(26, 27, 30)
IV (1 hr-infusion)(28)
Plasma protein
41-59%(22, 23) 50%(29) 60%(30)
binding
Vd 1,231 L(22) 1.46-2.5 L/kg(31) (150-180 L)(28) 109.5-132 L(26, 30)
Urine, inflammatory fluid, bronchial
#f2'5$g6 mucosa, alveolar macrophages,
Lungs, PMNs, macrophages(23)
%m6aa$ respiratory epithelial lining cells,
prostatic tissue, bile(27)
Urine excretion 17-23% (li ulifloxacin)(22) 50-70% (unchanged)(24, 28, 29) 50%(27, 30)
t la## 7.6-10
gd+'(22, 23) 4.4-7
g d+'(25, 28, 29, 31) 30-40
gd+'(26, 27, 30)
#'bl
l
2(22) l
2(24) l
2(27)
d4a#
#'l

6
a+2+$b+i*(22) a+2+$b+i*(24) a+2#'(27)
*'5 HD
#'bl
a+2+$b+i*(22) a+2+$b+i*(24) a+2#'(27)
d4#
CSF penetration Poor(22) a+2+$b+i*(24) 57%(27)
Pregnancy cat. a+2+$b+i*(22) a+2+$b+i*(24)
Allergic potential #g #g

1506 424
2 2556 33
Prulifloxacin Sitafloxacin Rufloxacin

(Darflox ) (Gracevit ) (Uroflox)
(25) (27)
4*jga m$ 6, 5 ', 5 '2 ' 4*jga m$6, 5'2' 4*jga m$6, 5'2'
(22, 23) (25) (27)
njg, photosensitivity njg, photosensitivity
ADRs QTc prolongation f#2+$d #g QTc prolongation ($ a IV CNS side effects
2 $%,
2 moxifloxacin, ciprofloxacin(22) sitafloxacin bi') '$6, a+2*(27)
(22)
njg, 4, photosensitivity
3+ 2+ 2+ 2+ 2+ 2+
FQs 51# chelation polyvalent cations (Al , Mg , Ca , Fe , Zn , Bi ) 5l6ih+a**' m'4l2'
Drug interaction > 2
gd+'(3, 17)
(22, 23)
Prulifloxacin 5l AUC f*% t b' theophylline & g+bo%+ 15%
e prodrug +jg i h + m%ti 44*1+ S. pneumoniae, MSSA, +$p 57 c#2 enteric GNB 62
*$g 6 f * ' 62 ' e MRSA, VRE, H. influenzae, Moraxella norfloxacin, +$p57 c#2 Ps. aeruginosa
ulifloxacin(22, 23) catarrhalis, Enterobacteriaceae, 62 ciprofloxacin f*%+$p 57 c#2
(24, 25,
Ulifloxacin +$p57 c#2 GNB $2 anaerobes, atypical pathogens MSSA, MSSE, atypical pathogens
28, 29)
FQs # jg u (5o'
jo l
1+
f*%l 62 FQs jg , a+2 4 4*1 +
d'&6*)
2 Haemophilus spp., 6 *%4o ' a jg 'm+$ anaerobes(27)
Moraxella catarrhalis, E. coli, post-antibiotic effect > 6
gd+'(25) +$b 2'l
l UTIs, gastrointestinal
+6#1
Klebsiella spp., Proteus spp., +$b 2'l
l UTIs, URIs, CAP, infections, respiratory tract
(24) (27)
Morganella spp., Ps. aeruginosa AECB infections
m$o6'44*1+ Gram-positive
bacteria
2 MSSA, S.
(22, 23)
pneumoniae
+$ b 2 ' l
l UTIs, infectious
(22, 23)
diarrhea, AECB
if6f*% Tablets : 132.1 mg (equivalent to Tablets : 50 mg Tablets : 200 mg
4+f'5$g+$l ulifloxacin 100 mg)
%5a56
Tetracyclines and Glycylcyclines
Mechanism of action : 66o'f45$$6 (bacteriostatic) d6m5$g 30s subunit of ribosome b'f45$$6 2'n*l

joa+2+t'd#$a(1, 2, 17)
Spectrum of activity : 44*1+ Gram-positive bacteria '
(
2 PSSP), Gram-negative bacteria '

(
2 H. influenzae, N. meningitidis, Vibrio spp.), anaerobes '
(
2 Clostridium spp., Borrelia burgdorferi),
spirochetes (
2 Treponema pallidum), atypical pathogens (Chlamydia, Mycoplasma, Rickettsia)(1, 2, 17)
lvmm1&jo6*12+ tetracyclines lf45$$6*6

2 PRSP, S. aureus, coliform bacteria, Shigella
spp., Proteus spp.(17)
Clinical uses : 55*b'6*12+ tetracyclines lvmm1 4j l
ld4#
jo atypical pathogens

2 Chlamydia spp., Mycoplasma spp., Ureaplasma spp., Rickettsia spp.(2)
Mechanisms of resistance : jo6*12+ tetracyclines m n2 2 *a 4j ' efflux pump &jgb6
mh**", ' ribosomal protection proteins &jgbb'a+2l6bm 30s subunit of ribosome

1506 424
2 2556 34
#$%& 18 Tetracyclines and glycylcyclines
Tigecycline
Tetracycline Doxycycline Minocycline
(Tygacil)
*12+626 1st generation tetracyclines 2nd generation tetracyclines 2nd generation tetracyclines Glycylcyclines(1, 17)
100 mg IV/PO q 12 hr
(l severe infections ml 100 mg IV/PO q 12 hr 100 mg IV loading dose
(2, 3)
bl
250-500 mg PO q 6 hr 200 mg q 12 hr x 3 j 200 mg IV/PO q 24 then 50 mg IV (30-60 min
then 100 mg q 12 hr a)(2, hr(2, 3) infusion) q 12 hr(2, 3)
3)
Absorption 60-80%(2, 3) 90-93%(2, 3) 90-95%(2, 3)

2-3.5 mcg/mL * '
1.5-2.2 mcg/mL *' %5 200 mg(2)
Cmax 1.5-2.1 mcg/mL(2) 0.87 mcg/mL(2)
%5 250 mg(2) 4.2 mcg/mL *'l 200
mg IV(2)
Plasma protein
20-67%(2) 25-91%(2, 3) 55-88%(2, 3) 71-89%(2, 3)
binding
Vd 0.7 L/kg(3) 0.75 L/kg(3) 1.5 L/kg(3) 8 L/kg(3) j 500-700 L(2)
Epithelial lining fluid (1.32
52 b'% 6l*j ),
alveolar macrophages (78
#f2'5$g6 Pleural fluid, bronchial secretions, sputum, ascetic fluid, synovial fluid, aqueous and 52 b'% 6l*j ),
%m6aa$ vitreous humor, prostatic fluid(2) gallbladder (23 52b'
%6l*j), bone and
joint (31-58% b'%6
l*j)(2)
CSF penetration
(non-inflamed, 5%, 5%(2, 3) 25%, 25%(2, 3) 50%, 50%(3) 11%(2)
inflamed meninges)
Bile penetration 1,000%(3) 3,000%(3) 1,000%(3) 3,800%(3)
Urine excretion 60% (unchanged)(3) 20-40% (unchanged)(3) 4-19% (unchanged)(3) 22% (unchanged)(3)
t la## 6-11
gd+'(2, 3) 18-22
gd+'(2, 3) 15-16
gd+'(2, 3) 42
gd+'(2, 3)
t l ESRD 108
gd+'(3) 18-22
gd+'(3) a+2+$b+i*(3) 42
gd+'(3)
#'bl *$*$g6'l
(2, 3) a+2#'(2, 3)
a+2#'(2, 3) a+2#'(2, 3)
d4a# (*jl
doxycycline f5) (*jl
doxycycline f5)
#'l

6
*$*$g6'l
(2, 3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
*'5 HD
a+2#' a+2#' a+2#'
#'bl (3)
(*$*$g6'l severe hepatic a+2#' (|&% severe hepatic
(|&% severe hepatic
d4#
impairment)(2, 3) impairment)(2, 3) impairment)(2, 3)
Pregnancy cat. D(2, 3) D(2, 3) D(2) D(2, 3)
Allergic potential #g(3) #g(3) #g(3) #g(3)
< 0.12 mcg/mL for
PSSP, PRSP, E. faecium
(Van-R)
< 4 mcg/mL (S), 8 mcg/mL (I), > 16 mcg/mL (R) for Enterobacteriaceae, Staphylococcus
MIC breakpoint < 0.25 mcg/mL for E.
spp., Enterococcus spp.(2)
faecium (Van-S), MSSA
< 0.5 mcg/mL for MRSA,
VISA

1506 424
2 2556 35
#$%& 18 Tetracyclines and glycylcyclines (#2)
Tigecycline
(Tygacil)
4*jga m$6, 5', esophageal ulceration 4%56*'55$(1-3) 4 *jg a m$ 6 ,
(2, 3)
Photosensitivity #'f%lni6*$*$g6'fm f*%+jon+
dyspepsia, '$6(2, 3)
(2, 17)
Fanconi syndrome (proximal renal tubules iw$65' 5l+$ glucose, amino Photosensitivity
acids, phosphate, bicarbonate g+lv%) ml
65$g+61(2) BUN elevation
(2, 3)
(2, 3)
Hepatotoxicity +&+jgl
tetracycline > 2 g/day, w '#o'4", ni6d4a#, l
65$g LFT abnormalities
ADRs +61(1-3) # 2 , amylase
v*$g6e$5j*j' +jgl
l61 < 8 f*%5l4"5$g+a6 elevation(2, 3, 17)
%2'#o'4"(1, 2) v *$g 6 e $ 5j
Minocycline 5l blue-black hyperpigmentation of skin and mucous membranes a *j' +jgl
l61 < 8
+jgl
# #2%6%6(2, 3) f*%5l4"5$g+
a6%2'#o'4"(1)
Tetracyclines chelation polyvalent cations (Al3+, Mg2+, Ca2+, Fe2+, Zn2+, Bi2+) +jg l
2 + warfarin

2 antacids, sucralfate, calcium supplements, +f*%n* #"m+, enteral feeding, m5l INR i'bo 4
iron supplements, bismuth subsalicylate) 5l6ih+a**' m'4l2' > 2
gd+' # #+ INR l*
+jgl
6
2+(2, 3, 17)
CYP450 inducers (
2 phenytoin, phenobarbital, carbamazepine) m5l%6
tetracyclines l*j**'(3)
a+2 6 +l
f * lv m m1 6 + l
+ 2 4 4 *1 + community- +$ glycylamido group
(l
doxycycline +2) tetracycline &% 6 acquired MRSA (CA- 5$g * 6 g ' b '
f#26'4'+$l
l infectious &$6'*% 2 4o'(1, 2) MRSA) f*% M. leprae 6 tetracycline ring 5l6a+2
(3)
diarrhea e drug of choice l ( #2 ' m tetracycline, tib5' efflux pump
*$ *$g 6 'l
l w ' +$ lyme disease doxycycline)(2) f*%6'm 30s subunit a
4"f*%61 < 8 (1, 3) (e lyme disease l Minocycline 6 ' +$ f2bo
w '+$4" j61 < 8 +l
e DMARDs l bb#p57 c'
l l
amoxicillin, rheumatoid arthritis $6 + 44*1+ GNB 5$gjo6
erythromycin, cefuroxime (3) (
2 MDR-A. baumannii,
f5 j t 1 f'l l
*$ *$g6 'l
l w ' +$ CRE), Gram-positive
ceftriaxone, penicillin G) 4"f*%61 < 8 (1, 3) bacteria 5$g jo 6 (
2
6 ' 4 '+$ l
l CAP MRSA, MRSE, VISA, VRE,
(2 + beta-lactams), PRSP) f*% atypical
scrub typhus(3) pathogens(1, 2, 17) f#2a +2
+6#1
Doxycycline e65$g4 44*1+ Ps. aeruginosa,
*j l
l ni 6 5$g +$ Proteus spp., Providencia
5 ' b ' a # & 2 ' spp.(2)
+ 2 minocycline, +$ b 2 ' l
l complicated
tetracycline jg 'm+$ intra-abdominal infections,
1 # " worsening cSSSIs, CAP(2, 3)
azotemia #g2(2) a+2 4 l
l
*$ *$g 6 'l
l w ' +$ severe infections +
4"f*%61 < 8 (1, 3) bacteremia jg 'm+$
meta-analysis &2
a tigecycline & g+4+
$g6'#2#6+jgl

severe infections(2) m%
l
tigecycline l critically ill

1506 424
2 2556 36
#$%& 18 Tetracyclines and glycylcyclines (#2)
Tigecycline
(Tygacil)
patients 4l 2 +
carbapenems j colistin(2)
% + % ' l
l
bacteremia jg 'm6+$
+6#1 %m6ljo 6jg $ 5
l +$ 4 +b + b l*j
42b'#g(2, 3)
4*$*$g6'l
lni5$g
+$61 < 18 (3)
if6f*% Capsules : 250 mg Capsules : 100 mg a+2 +$ m 2 6l%5 Injections : 50 mg/vial
4+f'5$g+$l a56
%5a56
Sulfonamides and trimethoprim
Mechanism of action : p57 c66o'ah+"l%*$g6 folic acid (dihydrofolate, FH2) e folinic acid
(tetrahydrofolate, FH4) hg'me#2'4%" DNA(1)
o Sulfonamides +$d4''4*6 para-aminobenzoic acid (PABA) 66o'ah+" dihydropteroate synthase
ffb2'b(2)
o Trimethoprim +$d4''4*6 FH2 66o'ah+" dihydrofolate reductase a+2l*$g6 FH2 e FH4(2)
Mechanisms of resistance : jo sulfonamides f*% trimethoprim m m
jo*$g6f*'d4''b'
ah+" 5 l 6b m a+2 a ,
jo * 6b i2 h**",
jo ' PABA l+ bo m+t
%
sulfonamides lmah+"
#$%& 19 Sulfonamides and trimethoprim
Sulfamethoxazole-Trimethoprim, Trimethoprim
Sulfadiazine
Cotrimoxazole (Bactrim) (Trimethop)
Treatment dose : 5 mg/kg of TMP Treatment dose : 1-1.5 g PO q 6
IV/PO q 6-8 hr (15-20 MKD)(2) hr (2, 21)
Treatment dose : 5 mg/kg PO q 8
bl
(meningitis l 5 mg/kg IV q 6 hr)(3) Secondary prophylaxis for
hr(2, 21)
PCP prophylactic dose : 400/80- toxoplasmosis : 500 mg PO q 6 hr(2)
800/160 mg PO q 24 hr(2, 21)
90-100%(2, 3)
Absorption Well absorbed(2) 90-100%(2)
(IV-oral switch therapy lb52)(1)
105/ 9 mcg/mL *'l 800/160 mg IV q
Cmax 100-150 mcg/mL(2) 2 mcg/mL *'%5 200 mg(2)
8 hr(2)
Plasma protein
70%/ 44-62%(2, 3) 38-48%(2) 45%(2)
binding
Vd 0.36/ 2.0 L/kg(2, 3) 0.29 L/kg(2) 2.7 L/kg(2)
Aqueous humor, middle ear, lungs,
#f2'5$g6
sputum, seminal fluid, prostatic fluid,
%m6aa$
bile, bone(2)

1506 424
2 2556 37
#$%& 19 Sulfonamides and trimethoprim (#2)
Sulfadiazine
CSF penetration
(inflamed 40%(3) 40-60%(2) 13-44%(2)
meninges)
15-40% (acetylated metabolite) f*%
Urine excretion 10-30%/ 50-70%(2, 3) 50-70%(2)
30-44% (unchanged)(2)
t la## 8-9/ 10-11
gd+'(3) 7-17
gd+'(2) 8-10
gd+'(2)
t l ESRD 42-80
gd+'(3)
#'bl l
2(2, 3) l
2(2)
l
2(2)
d4a# f*%4*$*$g6'l
l CrCl < 10 f*%4*$*$g6'l
l CrCl < 10
#'l

6
l
2(2, 3) a+2+$b+i*(2) l
2(2)
*'5 HD
#'bl a+2#'(2, 3) a+2#'(2)
a+2+$b+i*(2)
d4# f#2ll
64+%+%' f#2ll
64+%+%'
Pregnancy cat. C(2) C(2) C(2)
Allergic potential i'+(3) i'+
< 38/2 mcg/mL (S), > 76/4 mcg/mL
(R) for Enterobacteriaceae and Gram-
MIC breakpoint negative non-Enterbacteriaceae,
Staphylococcus spp.,
(2)
Stenotrophomonsa maltophilia
(2, 21) (21)
4*jga m$6 +&+jg6l
lbi'
2 l PCP 4*jga m$6
(1, 2, 17, 21)
ab, njg, 4, photosensitivity Macrocytic anemia, leucopenia,
(2, 21)
Severe hypersensitivity syndrome
2 erythema multiforme, exfoliative thrombocytopenia
dermatitis, SJS, TEN hg'ni 65$g#
jo HIV m%+$4 +$g6 '#2 f&6 Hyperkalemia ml
TMP
sulfonamides i'bo 10 52 +jg5$64# (3, 17) bi' (jg'm TMP +$d4''
(1-3, 17,
Macrocytic anemia, leukopenia, thrombocytopenia, methemoglobinemia 4*6 triamterene hg'e potassium-
21) (1-3, 17)
ADRs f*% acute hemolytic anemia +jgl
lni6 G-6-PD deficiency sparing diuretics)(2)
(1, 3, 17)
Hyperkalemia ml
TMP bi'
g l5' v% jg 'm#n*b'6 (crystalluria) m'# 'f%l
ni6jg+o+u l%2'5$gl
6(2, 21)
(1, 3)
LFT abnormalities, hepatitis
+l
lw '+$4"a#+156 f*%l561#g2 2 j &%m5
l5 kernicterus(2, 3, 17)
l
2+65$ge folate antagonists j 65$g 5 'b'ab%i (
2 methotrexate, pyrimethamine,
zidovudine, azathioprine e#) & g+4+1f'b' macrocytic anemia, leucopenia(3)
Drug interaction
Sulfonamides +$ albumin affinity i' +ta*25$g6jg5$gm albumin a
2 phenytoin, warfarin, sulfonylureas 5
l66i2li % (free form) +bo hg'm %& a
2 phenytoin toxicity, over INR, hypoglycemia #+*(2, 3)
e drug of choice l ' / e drug of choice l m 6i2 l *12 + substituted 2,4-
(17)
d4#
jo '

2 PCP, toxoplasmosis (l 2 + diaminopyrimidines
toxoplasmosis, Stenotrophomonas pyrimethamine f*% leucovorin)(2, 21) 6 +l
2 + sulfamethoxazole
+6#1 maltophilia, nocardiosis(2, 3, 17, 21) m6'l
l malaria 5$g jg'ml
TMP e6$g6+
m$o6'l
l AECB, shigellosis, m chloroquine-resistant P. jo6(2, 17)
salmonellosis, melioidosis(2, 17) falciparum (l2 + quinine f*% l
l mild to moderate
+$p57 c#2 Gram-positive bacteria pyrimethamine)(2) PCP (l2+ dapsone)(2, 21) j

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#$%& 19 Sulfonamides and trimethoprim (#2)
Sulfadiazine
(PSSP, community-acquired MRSA, l
e 6 $g 6 l uncomplicated
MSSE, Listeria monocytogenes), Gram- UTIs(2, 17)
negative bacteria '
(HENPEK,
Shigella, Salmonella)(1, 2, 7, 17) f#2a+2
44*1+ enterococci(1)
a+24l
cotrimoxazole e6fl
UTIs jg'm&1# "
jo6 cotrimoxazole b' E. coli i'
+6#1 + (> 60%)
norcardiosis #'l
lb
i' 4j (400/80 mg) 4-6 tab BID
jg'm#' peak conc. (2 hr post-
dose) 100-150 mcg/mL(2)
Single strength tablets (SS) = SMX
400 mg + TMP 80 mg(3)
Double strength tablets (DS) = SMX
800 mg + TMP 160 mg(3)
Suspension : 200/40 mg per 5 mL Tablets : 500 mg Tablets : 200 mg
if6f*%
Tablets : 100/20 mg (pediatric
4+f'5$g+$l
tablets), 400/80 mg, 800/160 mg
%5a56
Injections : 400/80 mg per 5 mL
Lincosamides
Machanism of action : 66o'f45$$6 (bacteriostatic) d6m5$g 50s subunit of ribosome 2'n*l

joa+2+t
'd#$a f*%66o'' toxin b'
jo (
2 streptococci, staphylococcal toxic shock syndrome)(1, 2, 17)
Spectrum of activity : 44*1+|&% Gram-positive bacteria (
2 MSSA, community-acquired MRSA,
GABHS, S. pneumoniae, Corynebacterium diphtheriae) f*% anaerobes (
2 oral anaerobes, Bacteroides
fragilis, Clostridium spp. 6 C. difficile)(1-3, 7, 17) a+2+$n*#2 Gram-negative bacteria
Clinical uses : SSTIs, respiratory infections (
2 aspiration pneumonia, lung abscesses), intra-abdominal
infections (m B. fragilis) f*% intra-pelvic infections (m B. fragilis)(2, 17)
Mechanisms of resistance : lincosamides m 50s subunit of ribosome 5$g#f2'$6 macrolides 'o
f45$$65$gjo6#2 erythromycin d6 methylation b' binding site +m%job++5$g*12+ lincosamides 6(1,
2)
#$%& 20 Lincosamides
Clindamycin Lincomycin
(Dalacin) (Lincocin)
300-450 mg PO q 6-8 hr(2, 3, 21) 500 mg PO q 6-8 hr j 600 mg IM q 12-24 hr j
bl

600-900 mg IV q 6-8 hr(2, 3) 600-1,000 mg IV q 8-12 hr(32) (max. 8 g/day)
90%(2, 3)
Absorption 20-30%
(IV-oral switch therapy lb52)

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#$%& 20 Lincosamides (#2)
(Dalacin) (Lincocin)
(2) (32)
2.5 mcg/mL *'%5j|$ 150 mg 11.6 mcg/mL *'l 600 mg IM af* 1
gd+'
Cmax (2) (32)
10 mcg/mL *'l 600 mg IV 15.9 mcg/mL *'l 600 mh IV infusion 2
gd+'
Plasma protein
85-94%(2, 3) 70-75%
binding
Vd 1 L/kg(3)
#f2'5$g6 Ascitic fluid, pleural fluid, synovial fluid, bone, bile, Bone, aqueous humor, bile, peritoneal fluid, pleural fluid,
%m6aa$ saliva(2) synovial fluid(32)
#f2'5$g6
CNS(2, 33) CNS(32)
%m6aa6
Urine excretion 10% (unchanged) + 3.6% (active metabolite)(2, 3) 1.8-30.3%(32)
t la## 2.4
gd+'(2, 3) 4-6
gd+'(32)
t l ESRD 4
gd+'(3) 10-20
gd+'
#'bl l
2(32)
a+2#'(2, 3)
d4a# (|&% severe renal impairment)
#'l

6*'
a+2#'(2, 3) a+2#'(32)
5 HD
#'bl l
2 l
2(32)
d4# (|&% severe hepatic impairment)(2) (|&% severe hepatic impairment)
CSF penetration
(non-inflamed, < 100%(3)
inflamed meninges)
Pregnancy cat. B(2, 3) C(32)
Allergic potential #g(3) #g
(2)
MIC breakpoint 0.5 mcg/mL for Staphylococcus spp.
(2)
4*jga m$6, 5'2'5$ga+2a m C. difficile (10-30%)
C. difficile-associated diarrhea (AAD) &a 0.01-10% b'nil
6 clindamycin d6 oral clindamycin 5l AAD
ADRs 262 IV clindamycin(3)
(3)
Neuromuscular blockade (apnea, respiratory paralysis)
(2, 17)
n*a+2&'%'4"jgu 5$gm& af2 njg, eosinophilia, leucopenia, thrombocytopenia
a clindamycin, lincosamide 2+65$g66o' NMJ (nondepolarizing neuromuscular blocking agents,
Drug interaction colistin) & g+4+$g6'#2 neuromuscular blockade(2, 3, 17)
(3)
a clindamycin 2+ theophylline m5l%6 theophylline l*ji'bo
(3) (17,
+ l
l SSTIs, aspirate pneumonia l
6*'lvmm1 jg'm+$ clindamycin +f5
m$o6'l
'/ PCP lni65$ga+2+tl
33)
cotrimoxazole, dapsone, pyrimethamine a
2 G-6-PD +$b2'l
ld4#
jo S. aureus, Streptococcus spp.
deficiency (l2+ primaquine) f*%e5'*jl
2 SSSIs, bone and joint infections, respiratory tract
toxoplasmosis lni65$ga+2+tl
sulfadiazine infections(32)
a (l2+ pyrimethamine)(2, 21) +lf IV bolus &%m neuromuscular
+6#1
Antibiotic-associated diarrhea (AAD) m65*6 blockade, cardiopulmonary arrest #'mjm'l+$4+
normal flora l*alw2 2'n*l overgrowth b' C. b+b 10 mg/mL f*%l IV infusion d6 600-1,000 mg
difficile hg'a+2ti5*6d6 clindamycin d6 AAD 5$g1f' m% drip 1
gd+', 2 g drip 2
gd+', 3 g drip 3
gd+', 4 g
5$g1 4j pseudomembranous colitis (PMC) hg'+$#6 drip 4
gd+'(32)
b'h**"1n'*alw2 me#6t'
$ #a ni6
m%+$ab, 5', bloody stools(17)

1506 424
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#$%& 20 Lincosamides (#2)

(Dalacin ) (Lincocin)
if6f*% Capsules : 150 mg, 300 mg Capsules : 500 mg
4+f'5$g+$l Injections : 150 mg/mL, 300 mg/2 mL, 600 mg/4 mL, Injections : 600 mg/2 mL
%5a56 900 mg/6 mL
Nitroimidazoles
Mechanism of action : Nitro group 5$g

jg+#2 five-membered ring m% % reduction ae toxic
free radicals hg'a5*6 DNA molecules 2'n*l
jo#6l5$g1 d6 anaerobic bacteria +$ low redox potential
electron transport proteins hg'+tl electrons f2 nitro group a lb%5$g aerobic bacteria a+2+$d#$
$o
5l nitroimidazoles +$p57 c44*1+|&% anaerobes f*% microaerophilic bacteria (
2 Helicobacter pylori)
(microaerophilic bacteria 4j
jo5$gm w# d#a$l%5$+g $h m6)(1, 2)
Clinical uses : anaerobic infections
2 intra-abdominal infections, intrapelvic infections, SSTIs, bone and joint
infections, meningitis, brain abscess, intestinal amebiasis, amebic liver abscess, trichomoniasis, bacterial
vaginosis, giardiasis, C. difficile-associated diarrhea, periodontal disease(2)
o Anaerobic bacteria +a+2jo6 metronidazole f#2+$jo6+en*m5$g
jo+$5'b'
electron transport proteins **' 2'n*l nitro group ti*$g6e toxic free radicals 6*'(1)
o Microaerophilic bacteria (Helicobacter pylori) +$jo6 metronidazole +2 anaerobic bacteria (m
&jo6t' 20-30%) f#26'a+25*ajo65$g
m(1, 2)
#$%& 21 Nitroimidazoles
Metronidazole Tinidazole
(Flagyl) (Fasigyn)
2,000 mg PO q 24 hr x 2-5 (bacterial vaginosis,
bl
250-500 mg IV/PO q 6-8 hr(2, 3) intestinal amebiasis, amebic liver abscess)
(trichomoniasis, giardiasis l single dose)(2, 34)
90-100%(2, 3)
Absorption 90-100%(34)
(IV-oral switch therapy lb52)(1)
Cmax 20-25 mcg/mL *'%5j|$ 500 mg(2) 48 mcg/mL *'%5 2,000 mg(2, 34)
Plasma protein binding 20%(2, 3) 12%(34)
Vd 0.25-0.85 L/kg(3) 50 L(2, 34)
#f2'5$g6%m6aa$ Saliva, bile, seminal fluid, bone, liver, liver abscesses, lungs, vaginal secretions, CSF(2)
CSF penetration
30%, 100%(2, 3)
Bile penetration a+2+$b+i*(3)
Urine excretion 77% (unchanged + metabolites)(2, 3) 20-25% (unchanged)(2, 34)
t la## 6-14
gd+'(3) 12-14
gd+'(2, 34)
t l ESRD 14
gd+'(3)
#'bld4a# a+2#'(2) a+2#'(2, 34)
#'l

6*'5 HD a+2#'(2) l
2(2)

1506 424
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#$%& 21 Nitroimidazoles (#2)
Metronidazole Tinidazole

(Flagyl ) (Fasigyn)
l
2
#'bld4# a+2#'(2)
(|&%l severe hepatic impairment)(2, 3)
Pregnancy cat. B (f#24*$*$g6'l
l 1st trimester)(2, 3) C(2, 34)
Allergic potential #g(3) #g
(2, 3, 17)
4*jga m$6, 5', epigastric discomfort
(2, 3, 17)
Metallic taste, furry tongue
ADRs (2, 3, 17)
CNS side effects
2 $%, '$6, h, aseptic meningitis,

(2, 3, 17)
Peripheral neuropathy +&+jgl
# #2e*
+jg a 2 + f**"m % disulfiram-like +jg a 2 + f**"m % disulfiram-like
reaction (4*jga m$6 $% f' lmg reaction #'*$*$g6'jg+f**"l%2'5$g
lm#)(2, 3) #'*$*$g6'jg+f**"l l
6 f*%* ' 61 l
6 72
g d+' (jg 'm
%2'5$gl
6f*%*'61l
6 48
gd+' tinidazole +$ t 62 metronidazole)
+jg a 2 + disulfiram m5l acute
Drug interaction
toxic psychosis(2, 3) 461l
disulfiram > 2
" 2l
metronidazole(2)
(2, 3)
+jga2+ warfarin m5l INR i'bo
Phenytoin, phenobarbital m5 l %
metronidazole **'(2, 3)
l
intra-abdominal infections, intrapelvic infections 5$g m anaerobic bacteria f551
(
2
B. fragilis, Gardnerella, Prevotella, Clostridium spp. +t' C. difficile) f*% protozoa (
2 Entamoeba
+6#1
histolytica, Trichomonas vaginalis, Giardia lamblia)(1-3, 17)
(2, 3)
m$o metronidazole 6'e drug of choice l C. difficile-associated diarrhea

Suspension : 200 mg/5 mL (Flagyl-S ) Tablets : 500 mg
if6f*%4+f'5$g+$l
Tablets : 200 mg, 400 mg
%5a56
Injections : 500 mg/100 mL
Miscellaneous antibiotics
HTZ&P[ %&\]O\P^S#_Ì]ZaT Gram-positive bacteria

Mechanism of action : Glycopeptides f*% lipoglycopeptides e62f45$$6 (bactericidal) p57 c66o'
'n'h**" d66m D-alanyl-D-alanine (D-ala-D-ala) 5$g*6 peptide side chain b' peptidoglycan 5l
a+2
jg+b+%2'6 (cross-linking)(1, 2)
Spectrum of activity : 44*1+ Gram-positive bacteria 2lw2 af2 Staphylococcus spp. (MSSA, MSSE,
MRSA, MRSE, VISA), Streptococcus pneumoniae (PSSP, PRSP), Entorococcus spp. (E. faecalis, E. faecium),
Clostridium difficile f#2a+2+$p57 c#2 Gram-negative bacteria jg'm6+$bd+*1*lw2a+2+tn2 outer
membrane porins a(1)
Mechanisms of resistance : vancomycin-resistant S. aureus (VRSA) f*% vancomycin-resistant Enterococcus
spp. (VRE) jo#2 glycopeptides (vancomycin f*% teicoplanin) d6
jo*$g6f*' D-alanyl-D-alanine e D-
alanyl-D-lactate 5l6a+2+tma$#2a(1, 17)

1506 424
2 2556 42
#$%& 22 Glycopeptides and lipoglycopeptides
Vancomycin Teicoplanin
Dalbavancin Telavancin Oritavancin
(Edicin) (Targocid)
*12+6 Glycopeptides(1, 3, 17) Glycopeptides(3) Lipoglycopeptides(13) Lipoglycopeptides(13) Lipoglycopeptides(13)

jo +$ MIC < 1 Septicemia/bacteremia, 1,000 mg IV l day 7.5-10 mg/kg IV 200 mg (1.5-3
mcg/mL: 15 mg/kg osteomyelitis : 400-800 1 then 500 mg IV l (infusion > 1 hr) q 24 mg/kg) IV q 24 hr(13)
IV q 12 hr (max. 20 mg (6-12 mg/kg) IV q 12 day 8 (l6 51 7 hr(2, 13) (BSIs l 5-10
mg/kg IV q 8 hr)(2, 3) hr x 3 doses then 400 )(13) mg/kg/day) (13)
l critically ill mg (6 mg/kg) IV q 24

patients 4l hr(35)
loading dose 6 : Septic arthritis : 800
25-30 mg/kg (j mg (12 mg/kg) IV q 12
20-25 mg/kg lni5$g+$ hr x 3 doses then 800
5 ' b ' a # mg (12 mg/kg) IV q 24
bl

&2'6i22)(2) hr(35)
CNS infections:
15 mg/kg IV q 8 hr
j 22.5 mg/kg IV q
12 hr(2)
Clostridium
difficile colitis, S.
aureus enterocolitis:
125-500 mg PO q 6
hr(2, 3)
Cmax 312 mcg/mL 46.2 mcg/mL *'
7.1 mcg/mL *'l 3
20-50 mcg/mL *' f*% mean Css 35 108 + 26 mcg/mL l 200 mg IV(37)
Cmax mg/kg IV af* 3-4
l 1 g IV(2) mcg/mL *'l *'l 10 mg/kg IV(2) 137 mcg/mL *'

gd+'(35)
1,120 mg IV(13, 36) l 800 mg IV(37)
Plasma protein
50-60%(2, 3) 90-95%(35) 90%(2, 13) 86-90%(13, 37)
binding
0.11 L/kg(13)
Vd 0.7 L/kg(3) 0.6 L/kg(35) 0.11-0.13 L/kg(2, 13)
(7.85-11.3 L)(36)
Blister fluid Liver, kidney, spleen,
(penetration 40%), lungs, epithelial
Pericardial fluid,
#f2'5$g6 Blister fluid, synovial Bone, blister fluid, pulmonary epithelial lining fluid, blister
pleural fluid, ascetic
%m6aa$ fluid, bone(35) macrophages(36) lining fluid fluid,
fluid, synovial fluid(2)
(penetration 73%), macrophages(13)
bone(2)
#f2'5$g6
%m6aa Lungs, bone, CSF CSF(35) CSF(36)
6
CSF
0%, 15%(3) Poor(35) 2%(2)
penetration
90% 80% 33.5-40% 5%
Urine excretion 64-76%(2)
(unchanged)(2, 3) (unchanged)(35) (unchanged)(13, 36) (unchanged)(13, 37)
147-258
gd+'(13) 132-356
gd+'(37)
t la## 4-6
gd+'(2, 3) 70-100
gd+'(35) 6-9
gd+'(2, 13)
(6-11 ) (5.5-15 )

1506 424
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#$%& 22 Glycopeptides and lipoglycopeptides (#2)
(Edicin) (Targocid)
t l ESRD 180
gd+'(3) 15-25
gd+'(2)
l
2(13, 36)
#'bl
l
2(2, 3) l
2(35) (|&% severe renal l
2(2, 13)
d4a#
impairment)
#'l

6
l
2(3) a+2#'(35) a+2+$b+i*(2)
*'5 HD
#'bl
a+2#'(2, 3) a+2#'(13) a+2#'(2)
d4#
Pregnancy cat. C(2, 3) B(35) B(2)
< 2 mcg/mL (S), 4- < 1 mcg/mL for
8 mcg/mL (I), > 16 MSSA, MRSA,
mcg/mL for S. vancomycin-sensitive
aureus(2) E. faecalis(2)
MIC breakpoint
< 4 mcg/mL (S) for < 0.12 mcg/mL for
Enterococcus spp.(2) S. pyogenes, S.
agalactiae, S.
(2)
anginosus
Red man syndrome (njg f' 4 d65g a ni6+ d65g a ni6+ d65g a ni6+
l 4 ) + +jg infusion 56a$ f#2m+$ab, 56a $ f#2 m+$ 56a $ f#2 m+$
rate a m%#1*g'$# $ % , 4*jg a mild taste $ % , 4*jg a
+$ f#2a+2me true allergy, 'ad6l m$6(13) disturbance (33%), m$6, 4+n #
IV infusion > 1-2
gd+'(1-3, 35) 4*jg a m$ 6 (14- $g 6 ,
Nephrotoxiciy + +jga6bi', l
27%), $%(2, 13) phlebitis, injection-
6e *, a 2 + nephrotoxic Red man site rxs, elevated
agents jgu
2 AMGs, amphotericin B(2, 17) syndrome ( ' a transaminases(13, 37)
+&7" Ctrough 5$gi' (> 15 mcg/mL) d6l IV infusion > 1
Ototoxicity m hearing loss, tinnitus, 4+
gd+')(2)
n # l5'# +&+jg+$%6i'+ Nephrotoxicity (&
ADRs
(+ & 7" Cpeak), a 2 + ototoxic sCr > 1.5 mg/dL a
agents
2 AMGs(1, 17) 6% l*12 + 5$g a
(17)
Anaphylaxis, rash , hypotension, drug telavancin lb%5$g
fever(2, 3) & 2% l*12+5$ga
(2, 35)
Phlebitis, 5$g|$ vancomycin)(2)
(1-3, 35)
Leukopenia, thrombocytopenia QTc prolongation
Teicoplanin +$ % 5 7 &a+2 #2 'm > 60 msec (1.5% l
vancomycin f#2 teicoplanin +$ 1 # " *12 + 5$g a
nephrotoxicity, red man syndrome, rash #g telavancin lb%5$g
2(35, 38) & 0.6% l*12 + 5$g
a vancomycin)(2)
a2 + nephrotoxic drugs jg u a 2+6
(
2 amphotericin B, AMGs, colistin, NSAIDs, 5$g m5 l QTc
cisplatin, cyclosporin) & g + 4+$g 6 '#2 prolongation (
2
Drug interaction
nephrotoxicity +bo(3) antiarrhythmic drugs,
moxifloxacin,
macrolides) & g+4+

1506 424
2 2556 44
(Edicin) (Targocid)
$g 6 ' #2 QTc
prolongation +bo
m'4*$*$g6'l

2+(2)
Cpeak 30-40 mcg/mL,
Ctrough 15-20 mcg/mL
(BSIs, bacteremia,
infective endocarditis,
osteomyelitis, severe
Therapeutic
SSTIs pneumonia,
serum
meningitis
2
concentrations
necrotizing fasciitis)
j Ctrough 10-15
mcg/mL (mild
infections 5$g m

jo MIC #g)(2)
44*1+ MSSA, MRSA, VISA (l VISA Dalbavancin, oritavancin +$ lipophilic side chain ld+*1* 5l high
#'l
vancomycin bi'bo 4j 2 g IV q 12 protein binding f*%+$ half-life 6+(13, 37)
hr), PSSP, PRSP, Entorococcus spp. '6 Dalbavancin +$b2'l
l cSSSIs, catheter-related BSIs 5$g
&71," C. difficile(1, 3, 17) m MSSA, MSSE, MRSA, MRSE, VRSA, vancomycin-sensitive E.
'a l
l d4#
jo 1 f'5$g m faecalis, VRE (6 vanA resistance)(13, 36) d6&2+$% 57 &l
MRSA (jl
l MSSA lni5$gf& cSSSIs a+2#2'm linezolid (600 mg IV q 12 hr x 14 ) f*%+$
penicillins, cephalosporins 62'1f')
2 % 57 &i'2 vancomycin (1 g IV q 12 hr x 7 ) l
IE, bacteremia, osteomyelitis, SSTIs, BSIs(13)
pneumonia(2, 3, 17) b$b' dalbavancin 4j 6&$6'"*%4o' m'l
+$l vancomycin d6|$bd&'+' fni6a f*%a+2me#'# #+%6l*j(13)
( intraventricular) j
2 ' a b * ' Telavancin f*% oritavancin p57 c 6 6o ' cross-linking b'
(intrathecal) &jg CNS infections lb peptidoglycan f*%6'5l rapid depolarization b' bacterial cell
20-30 mg q 24 hr(2) membrane f*% permeabilization (dual mechanism) 5l2f45$$6a
l systemic infections # 'l IV 62' (rapidly bactericidal activity)(2, 13, 36, 37)
+6#1 vancomycin jg'm6a+2tiih+m5' Telavancin +$b2'l
l cSSSIs, nosocomial pneumonia 5$g
( 17) f#2 +$ l vancomycin d6 m MSSA, MSSE, MRSA, MRSE, VISA, VRSA, vancomycin-
%5 &jg #
jo l5' sensitive E. faecalis, vancomycin-sensitive E. faecium, VRE (+t'

2 C. difficile colitis, staphylococcal vanA resistance)(2, 13) d6 ATLAS I f*% ATLAS II &2 telavancin (10
enterocolitis(1, 2, 17) mg/kg/day) +$% 57 &a+2#2'm vancomycin (1 g IV q 12 hr) l
Teicoplanin l6f IV bolus (slow push cSSSIs f*%l ATTAIN &2 telavancin (10 mg/kg/day) +$% 57 &
> 5 5$) a j IV infusion &$6' 30 5$ a+2#2'm vancomycin (1 g IV q 12 hr) l HAP 5$g m MRSA(13)
a(35) Telavancin +t 4%" coagulation test (PT, INR,
aPTT, activated clotting time) m'4#62'*j*'l6 23

g d+' (2l6dta)(2)
(2)
Telavancin +$ lung penetration $2 vancomycin
Telavancin e concentration-dependent bactericidal d64+$
AUC/MIC 50-100 j total telavancin AUC/MIC 404(2)
Oritavancin +$b 2'l
l cSSSIs, bacteremia 5$g m
MSSA, MSSE, MRSA, MRSE, VISA, VRSA, vancomycin-sensitive E.

1506 424
2 2556 45
(Edicin) (Targocid)
faecalis, VRE(13, 37) d6&2 oritavancin (200 mg/day j 1.5-3
mg/kg/day) +$ % 5 7 &l cSSSIs a+2#2'm vancomycin +
cephalexin f#2+$%6%*o2 (5-6 f*% 11-12 #+*)
+6#1 f*% oritavacin (5-10 mg/kg/day) +$% 57 &l S. aureus BSIs a+2
#2'm vancomycin(13)
Oritavancin m lung surfactants (+j daptomycin) m'ma+2
+tl
l#
jo5$ga(13)
if6f*%
Injections : 500 Injections : 200 a+2+$m26l a+2+$m26l a+2+$m26l
4+f'5$g+$l
mg/vial, 1 g/vial mg/vial %5a56 %5a56 %5a56
%5a56
#$%& 23 Linezolid, quinupristin-dalfopristin, daptomycin, sodium fusidate

Linezolid Quinupristin-Dalfopristin Daptomycin Sodium fusidate
(Zyvox) (Synercid) (Cubicin) (Fucidin)
*12+6 Oxazolidinones(1, 3, 17) Streptogramins(1, 3, 17) Lipopeptides(1, 3, 17) Fusidanes(6)
SSTIs l 4 mg/kg IV q
24 hr(2, 3)
250-500 mg PO q 8-12
Bacteremia, IE l 6
hr(39) (& g+e 1 g PO q 8
mg/kg IV q 24 hr (max. 12
600 mg IV/PO q 12 hr(2, 3) 7.5 mg/kg IV q 8-12 hr(2, 3) hr a l severe, deep-
mg/kg/day)(2, 3)
bl
(%52j*' (#'mjm'l D5W 52o, seated infections, MRSA)(6,
(l IV infusion > 30 5$ 39)
a) +l
NSS) (4%5#5 '
d6mjm'l NSS 52o
2'&%*ih+
+ l
* % * 6 5$g +$
6)
dextrose, +|$ b
*+)(2, 3)
100%(1-3)
Absorption (IV-oral switch therapy l 69-90%(6, 39)
b52)(1)
33 mcg/mL * '
%5 500 mg (#
12.7 mcg/mL *' 5 mcg/mL *'l 7.5 mg/kg 58 mcg/mL,
Cmax 5'2')(39)
%5 600 mg(2) IV(2) AUC 494 mcg*hr/mL(2)
25 mcg/mL * '
%5 500 mg(39)
Plasma protein
31%(2, 3) 50-56%/ 15%(2, 3) 92%(2, 3) 97%(6)
binding
Vd 0.64 L/kg(3) j 50 L(2) 0.45/ 0.24 L/kg(3) 0.096 L/kg(2, 3) 0.42-0.52 L/kg(39), 12 L(6)
Subcutaneous fat, kidney,
#f2'5$g6
jo6jg#2'u, blister fluid(2) muscle, prostate, pus,
%m6aa$
blister fluid, synovial fluid(39)
ti *$g 6 f*'5$g # d6 ti*$g6f*'5$g#e RP 62lw2tib5'a# 62lw2ti*$g6f*'5$g
% oxidation f* 12536 (pristinamycin IIA lia+2*$g6f*' +$&$6' # f*b5'o$e
Metabolism b 5'o $ e * derivative) hg ' e active 2 65$g ti *$g 6 f*' *(6, 39)
(70%)(2) metabolite f*b5' e inactive metabolite(2)
o$e*(2)

1506 424
2 2556 46
#$%& 23 Linezolid, quinupristin-dalfopristin, daptomycin, sodium fusidate (#2)
Urine excretion 30% (unchanged)(2, 3) 20% (unchanged)(2, 3) 78-80% (unchanged)(2, 3) < 1% (unchanged)(6, 39)
CSF penetration
(non-inflamed, 70%(3) < 10%(3) 2%, 5%(2, 3) Poor(6, 39)
inflamed meninges)
Pregnancy cat. C(2, 3) B(3) B(2, 3) C
t la## 4.2-5.4
gd+'(2, 3) 3.1/ 1
gd+'(3) 8.1
gd+'(2, 3) 10-16
gd+'(6, 39)
t l ESRD 7.1
gd+'(3) 3.1/ 1
gd+'(3) 29.8
gd+'(3)
#'bl l
2
a+2#'(2, 3) a+2#'(2, 3) a+2#'(39)
d4a# (+jg CrCl < 30)(2, 3)
#'l

6
a+2#'(2, 3) a+2+$b+i*(2, 3) a+2#'(3) a+2#'(6)
*'5 HD
a+2#' l
2
#'bl (2, 3)
a+2#' (f#24*$*$g6'l severe (l moderate to severe a+2#'(39)
d4# (3)
hepatic impairment) liver impairment)(2)
(3) (3)
Allergic potential #g #g
2 mcg/mL for 1 mcg/mL for 1 mcg/mL for
Enterococcus spp.(2) Staphylococcus spp. f*% Staphylococcus spp.(2)
MIC breakpoint
4 mcg/mL for Enterococcus faecium(2) 4 mcg/mL for
(2) (2)
Staphylococcus spp. Enterococcus spp.
Mild thrombocytopenia Infusion-related reactions Reversible myopathy 4*jga m$6, 5',
(2-4%), anemia, leukopenia ( 4 +f' 5$g (* +jo , * +jo 5'2'(6, 39)
m direct bone marrow l 6 ), phlebitis (bo 2f', myasthenia gravis LFT abnormalities (+
suppression, +&l65$g 4+b+b6 4l65' , creatine kinase &+jg l
6 lbi'j
l
6# #2 > 2 " central venous catheter)(1-3) (CPK) elevation) hg'+&7" e*), cholestatic
m'4# #+ CBC 51 1 Myalgia, arthralgia(1-3) ab6i' f*% jaundice (&l IV route
" +jg a 6 > 2 Hyperbilirubinemia(1-3) a6e* m'4 +2 oral route)(6, 39)
(2, 17)
" j l65$g+$4+ LFT abnormalities # #+*+jo Injection site reactions,
$g 6 '#2 %*j , +$ $ % , 4 *jg a * + jo 2 f ' f * % phlebitis (IV route)(6)
ADRs
thrombocytopenia 6i22, m$6, 5'2'(1-3) serum CPK 51 1 ")(1- njg, 4
(6)
+$ platelet disorders 6i22, Mild to severe AAD(2, 17) 3)

a antiplatelets(1-3, 17) Phlebitis
(1)
(2, 17)
Optic neuropathy, LFT abnormalities
(2, 17)
peripheral neuropathy 4 BUN elevation
(1)
5+'+jga njg
6 > 2 "(2, 3) $ %, 4*jg a
(1, 3, 17)
4*jga m$6, 5 '2', m$6, 5'ni
(1, 2, 17)
njg
(1-3,
Linezolid +$41+# e e CYP3A4 inhibitor +jgl
2+ statins m e CYP3A4 inhibitor
17)
monoamine oxidase (MAO) hg'5 l %65$ge & g+4+$g6'#2 myopathy/ +jg l
2 + cyclosporine,
inhibitor +t # CYP3A4 substrates i'bo rhabdomyolysis m ' 4 protease inhibitors, statins,
6 tyramine-riched
2 amiodarone, & m 61 l
statins warfarin m%5 l % 6
Drug interaction
foods hypertensive dihydropyridine-CCBs,
g 4l%2 '5$g a *2$oi'bo
(2, 3)
crisis diltiazem, cisapride, daptomycin(2, 3) *$*$g6'l
sodium
+jg a 2 + SSRIs, midazolam, ergotamine, fusidate 2 + statins
tricyclic antidepressants carbamazepine, statins(3, 17) &%& g+4+$g6'#2

1506 424
2 2556 47
(TCAs), sympathomimetics rhabdomyolysis(39, 40)
(
2 pseudoephedrine),
pethidine m5 l
serotonin syndrome (ab,
Drug interaction % %2 6, g , 4+
i# *$g6 f*'a) m'
# '61 l
6 *2 $o 62 '
6 1 4 2 l
linezolid(1-3, 17)
p57 c d 6m 50s p57 c d 6m 50s p57 c d 6f5# l p 5 7 c d 6 m
subunit of ribosome 5l subunit of ribosome (66o' 6jg 1 + h**" b 'f45$ $ 6 elongation factor G (EF-G)
a+2+t
jg++ 30s '4%"d#$)(1, 2) e ion-conducting ribosome a+2 l
subunit a (66o'+# Dalfopristin 5 l channels 5 l rapid translocation of peptidyl
e 70s) 2'n*la+2 conformation change b' depolarization 2'n*lh**" tRNA (66o''4%"
' peptide bond (66o' ribosome 5 l m #6(1-3, 17) d#$ ) (39) f#2 e
'4%"d#$)(1, 2, 17) quinupristin af2bo(1, 2, e 6 5$g 2 f 4 5$ $ 6 bactericidal (6)
17)
44*1+ MRSA, VISA, (bactericidal) S. aureus a 44*1 + Gram-positive
VRSA, VRE (5o' E. faecalis 44*1+ MRSA, VISA, 5$g 1 , concentration- bacteria 2 l w2
f*% E. faecium), PRSP(1-3, GISA, VRSA, VRE (|&% dependent killing, +$ post- (d6|&% MSSA, MRSA)
17)
f#2a+2+$n*#2 GNB &% E. faecium), PRSP(1-3, 17) antibiotic effect t' 6 f #2 a +2 +$ p 5 7 c #2 GNB
6ti b 65' efflux +$ b 2 ' l
l VRE
gd+'(2, 3) jg 'm6a+2 +tn2
pump a(1) bacteremia, cSSTIs m 44*1+ MRSA, VISA, outer membrane porins(6, 39)
e drug of choice l MRSA, MRSE(2, 17) GISA, VRSA, VRE, +$ b 2 ' l
l
MRSA jo 6 streptogramins PRSP(1-3, 17) f#2a+2+$p57 c#2 staphylococcal infections
pneumonia(2, 7) a 3 *a a f 2 +$ GNB jg 'm6+$ b
2 bone and joint
b $ 6b' linezolid 4j conformation change b' d+*1*lw2 a+2+tn2 infections, meningitis,
e bacteriostatic 5 l binding site 50s subunit outer membrane porins a cerebral abscess, SSSIs,
+6#1
m
joa
(2) of ribosome 5l6bm (1)
sepsis, IE(6, 39)
l 2003 g + +$ 6' a+2a$#2a, 'ah+" +$ b 2 ' l
l cSSSIs, +l
l561#g2
jo 6 linezolid b' + 5 * 6 6 ( enzyme bacteremia, right-sided IE 1 j &%m5l
MRSA, VRE d6*6 inactivation), ' efflux 5$g m MRSA, VRE(1, 2, kernicterus a (jg'm6
&71"b' cfr gene 5l pump b6mh**"(1) 17)
fb2'b bilirubin lm
single amino acid mutation Macrolides, lincosamides, a +2 + t l
l albumin)(39)
b' ribosome(1, 2) streptogramins (MLS) m #
jo 5$g a jo 6 fusidic acid
50s subunit of ribosome jg ' m 6 m lung b' S. aureus, S.
5$g#f2'$6 surfactants 5 l +$ 4 + epidermidis m
jo 6d6*$g 6 f*' b+b5$g site of infection a+2 *6& 71"b' FusA gene
binding site m%5ljo6 &$6'&(1, 2, 17) 5l EF-G m fusidic
b+5o' 3 *12+(1) acid a 6*' j FusB
gene & g+' inducible
protein 5$gbb'a+2a6m
EF-G(39) f*%jo6
b' GNB m'
modifying enzymes j
efflux pump(39)

1506 424
2 2556 48

(Zyvox ) (Synercid ) (Cubicin) (Fucidin)
if6f*% Tablets : 600 mg a+2 +$ m 2 6l%5 Injections : 500 mg/vial Tablets : 250 mg
4+f'5$g+$l Injections : 600 mg/300 a56
%5a56 mL
HTZ&P[ %&\]O\P^S#_Ì]ZaT Gram-negative bacteria

#$%& 24 Colistin, fosfomycin, nitrofurantoin
Colistin
Fosfomycin Nitrofurantoin
(Polymyxin E)
*12+6 Polymyxins(3) Phosphonic acid derivatives Nitrofurans(3)
3 g PO q 24 hr (%5#5'
2', l single dose UTIs
5-7.5 mg/kg loading dose then 2.5-5
l&w ' jl 3 UTIs
mg/kg/day IV f2'l q 8-12 hr
l&
6)(2, 3, 41) 100 mg PO q 12 hr 62'6 7
(l intrathecal, nebulized, continuous
bl
1-8 g IV q 8-12 hr (max. 24 g/day) (%5&+
26& +g
IV infusion a6)(2, 3)
(MRSA, ESBL-producing GNB l
2 ih+6)(2, 3)
d65ga l 300-400 mg LD then
g/day, MDR-Ps. aeruginosa l 4
150 mg IV q 12 hr
g/day f*% MRSA meningitis,
intraocular infections l 24 g/day)(41)
Absorption 37-42% (#5'2')(2, 3, 41) 80%(2, 3)
64-128 mcg/mL *'%5 3
50-150 mcg in urine *'%5
Cmax 5-7.5 mcg/mL *'l 500 mg IM(2) g(2)
(41) 100 mg(2)
AUC 673 mg/L*hr *'l 8 g IV
Plasma protein
< 10%(3) 0-3%(2, 3, 41) 20-60%(2, 3)
binding
Vd 15.8 L/kg(3) 2 L/kg(3), 15-30 L(41) 0.8 L/kg(3)
6 %5 : Bladder wall,
#f2'5$g6 kidneys, prostate, seminal vesicles(2)
Urine, kidneys(2)
%m6aa$ 6|$ : muscle, interstitial fluid,
subcutaneous tissue, ocular tissue(41)
#f2'5$g6
Synovial fluid, pleural fluid, pericardial
%m6aa CNS(41) Serum (very low)(2)
fluid(2)
6
CSF penetration
(non-inflamed, 5%, 25%(2, 3) a+2+$b+i*(3) a+2+$b+i*(3)
inflamed meninges)
60% (unchanged) +
Urine excretion 90% (unchanged)(2, 3) 20-44% (unchanged)(2, 3)
40% (active metabolite)(2, 3)
1.5-8
gd+'(2, 3)
t la## 5.7
gd+'(2, 3) 0.4-0.5
gd+'(2, 3)
(7.4-14
gd+' l ICU patients)(2)
t l ESRD 48
gd+'(3) 50
gd+'(3) 1
gd+'(3)
6%5 : a+2#' (f#2l
62'
#'bl l
2
l
2(2, 3) %+%'+jg CrCl < 10)(2, 3)
d4a# (41) f*%4*$*$g6'+jg CrCl < 30(2, 3)
6|$ : **' 50% +jg CrCl < 50

1506 424
2 2556 49
#$%& 24 Colistin, fosfomycin, nitrofurantoin (#2)
Colistin
(Polymyxin E)
#'l

6
l
2(2, 3) l
2(2, 3) *$*$g6'l
(2, 3)
*'5 HD
#'bl
a+2#'(3) a+2#'(3) a+2#'(3)
d4#
Pregnancy cat. C(2, 3) B(2, 3) B(2, 3)
Allergic potential #g(3) #g(3) *'(3)
< 2 mcg/mL (S), 4 mcg/mL (I), > 8
mcg/mL (R) for Ps. aeruginosa, non-
MIC breakpoint Enterobacteriaceae(2)
< 2 mcg/mL (S), > 4 mcg/mL (R)
for Acinetobacter spp.(2)
(2,
Nephrotoxicity (acute tubular 4*jga m$6, 5'2', GI upset 4*jg a m$ 6 , 5 '2 ' (17)
3, 41)
necrosis) *e# a, +&7" (macrocrystalline formulation +$ GI
(41)
b65$ga, &a 14-20% d6+ $%, '$6, 2f' side effects #g2)(2)
*'a colistin > 4 (2, 3) LFT abnormalities (2, 3, 41)
Acute hypersensitivity pneumonitis
(2, 3, 41)
Neurotoxicity (

*6 thrombocytosis, eosinophilia (a b , a , jg 6 , pulmonary
+j*65, +1, '$6, h infiltrates, eosinophilia)(2, 3, 17)
, slurred speech, blurred vision, Interstitial pulmonary fibrosis (+
respiratory arrest) &a 3.5%(2, 3) &+jgl
# #2jlni5$g+$
a, bronchospasm, acute 5'b'a#&2')(2, 3)
ADRs
respiratory distress syndrome (ARDS) Peripheral neuropathy (+&+jgl

& a m l nebulized lbi ' , ni 5$g +$ 5 'b'a#
colistimethate(2) &2')(2, 3, 17)
CNS side effects
2 $%,
'$6, +1(17)
(2, 3, 17)
Hepatitis, cholestatic jaundice
Methemoglobinemia, hemolytic
anemia +jg l
l ni 6 G-6-PD
(2)
deficiency
a2+ nephrotoxic drugs Calcium carbonate *ih+ a 2 + metronidazole,
jg u (
2 amphotericin B, AMGs, fosfomycin m5' (2) linezolid, stavudine, didanosine %6%
cidofovir, foscarnet, vancomycin, 6 & g +4 + $g 6 '#2 peripheral
NSAIDs, cisplatin, cyclosporin) & g+ neuropathy(2)
4+$g6'#2 nephrotoxicity +bo(2, Magnesium-based antacids *
Drug interaction 3)
ih+ nitrofurantoin(17)
a2+65$g66o' NMJ (
2 Probenecid, sulfinpyrazone 5l
AMGs, nondepolarizing muscle nitrofurantoin ti b5'v%
relaxants) & g + 4 + $g 6 ' #2 6*' (*% 5 7 &l
neuromuscular blockade(2, 3) UTIs)(17)
e cationic detergent hg'p57 c p57 c2f45$$6 (bactericidal) e bacteriostatic (l4+b+b
2 f45$ $ 6 (bactericidal) d6m d 6 6 6o ' a h +" enolpyruvyl i'e bactericidal) p57 cd66ti
lipopolysaccharides (LPS) l cell transferase hg'mel'4%" *$g 6 f * ' d 6 flavoproteins
+6#1
membrane b'
jo5lh**"g(2) n'h**"(2, 17, 41) (bacterial enzyme systems) ae
44*1+ Gram-negative bacteria 44*1+ MSSA, MRSA, GISA, active intermediates hg ' 5 *6

2 Ps. aeruginosa, A. baumannii, VRE, Streptococcus spp., ESBL- ribosomal proteins, DNA, RNA(2, 17)

1506 424
2 2556 50
#$%& 24 Colistin, fosfomycin, nitrofurantoin (#2)
Colistin
(Polymyxin E)
Enterobacteriaceae f#2 Proteus spp., producing GNB, quinolone-resistant 44*1+ Gram-positive bacteria
Serratia marcescens, Providencia E. coli (QREC), Ps. aeruginosa(2, 3, 41) (S. aereus, E. faecalis) f*% Gram-
spp., Burkholderia spp., 6|$l
e6$g6 j 2+6 negative bacteria (PEK,
(17)
Stenotrophomonas spp., Bacteroides jg l bone and joint Enterobacter)
fragilis, Prevotella spp., infections, meningitis 5$g m S. +$ b 2 ' l
l VSE/VRE
Fusobacterium +jo#2 colistin f*% aureus f*%l
l surgical prophylaxis catheter-related bacteriuria f*%
a+244*1+ Gram-positive bacteria(2) 2 transurethral resection of uncomplicated UTIs 52o (a+2+$n*l
+'al
ld4#
jo prostate, colorectal surgery(41) systemic infections)(2, 3)
MRD-Gram-negative bacteria
2 l6|$ (fosfomycin sodium) +$
MDR-Ps. aeruginosa, MDR- +dh$6+42b'i' (330 mg of
Acinetobacter baumannii, sodium #26 1 +) l
6lb
carbapenamase-producing Klebsiella i'm5l serum sodium i'bo f*%
pneumoniae, carbapenem-resistant m5lni6 CHF +$ a
Enterobacteriaceae (CRE)(2, 3, 7) (41)
Nubulized colistimethate l 80 mg l# "5 *' &2 IV

(mjm'l NSS 3 mL) &251 8-12 fosfomycin +t' /*4+
+6#1
gd+' jl$ recurrent infections e & #2 a # f * % & #2 i m 6
l 160 mg &251 8
gd+', 4#$6+ cisplatin, AMGs, amphotericin B,
l
l+2u (freshly prepare) f*%5 o'+jg colistin a f#26'a+25*a5$gf2

(41)
*%*6n'6a > 24
g d+' &%
colistimethate m%ti hydrolyze e 6 % 5 ( fosfomycin
colistin hg'5l acute respiratory trometamol, Monurol) l
l
distress syndrome (ARDS) a(2, 3) uncomplicated cystitis 52o l
a+2
l meningitis 5$g m a n * upper UTIs, urosepsis,
Ps. aeruginosa j A. baumannii m systemic infections(2, 3)
l colistin 5-10 mg IT q 24 hr j
amikacin 10-40 mg IT q 24 hr 2+
IV colistin 6(3)
66i2li colistimethate sodium
(colistin methanesulfonate) hg'm%ti
hydrolyze e colistin l2'6
Colistimethate 80 mg (1 million
units) = colistin 33.3 mg(2, 3)
Injections : colistimethate sodium Granules : 3 g/sachet (fosfomycin a+2+$m26l%5a56
if6f*%
150 mg of colistin/vial (Colistate 150) tromethamine, Monurol)
4+f'5$g+$l
Injections : 1 g/vial, 2 g/vial
%5a56
(fosfomycin sodium, Fosmicin)
#$%& 25 Spectinomycin, chloramphenicol, thiamphenicol

Spectinomycin
Chloramphenicol Thiamphenicol
(Trobicin)
*12+6 Aminocyclitols(3, 17, 42) Nitrobenzene derivatives(17, 43) Nitrobenzene derivatives(17)
2 g IM single dose 500 mg PO q 8 hr
50-100 mg/kg/day f2'l51 6
gd+',
bl
gonococcal urethritis, gonococcal (gonorrhea l 2,500 mg PO single
250-500 mg IV/PO q 6 hr(2, 3)
proctitis(3, 17, 42) dose)

1506 424
2 2556 51
#$%& 25 Spectinomycin, chloramphenicol, thiamphenicol (#2)
Spectinomycin
(Trobicin)
500 mg IV q 8 hr j 750 mg IV q
12 hr (1.5 g/day)
(2, 3, 43)
Absorption 80-90%
100 mcg/mL *'l 2 g IM af* 1
Cmax 10-13 mcg/mL *'%5 1 g(43)

gd+'(42)
Plasma protein
20%(3) 50-60%(2, 3)
binding
Vd 0.25 L/kg(3) 1 L/kg(3)
Liver, kidneys, saliva, ascetic fluid,
#f2'5$g6 pleural fluid, synovial fluid, aqueous
%m6aa$ and vitreous humor, inflamed
meninges(2)
Urine excretion 70-80% (unchanged)(3, 42) 10-30% (unchanged)(2, 3)
t la## 1.5-2
gd+'(3, 42) 2.5
gd+'(2, 3)
t l ESRD 4.7-29.3
gd+'(3, 42) 3
gd+'(3)
#'bl
a+2#'(3) a+2#'(2, 3, 43) l
2(43)
d4a#
#'l

6
a+2#'(3) l
2(2, 3)
*'5 HD
#'bl
a+2#'(3) a+2#'(3)
d4#
CSF penetration
(non-inflamed, < 10%(3) 90%, 90%(3)
inflamed meninges)
Pregnancy cat. B(3) C(2, 3)
Allergic potential #g(3) #g(3)
(3, 42)
5$g|$6 Myelosuppression (+$5o'f dose-dependent reversible f*% idiosyncrasy
4*jga m$6, nab g,
2 aplastic anemia)(1-3, 17) d6 thiamphenicol +$ dose-dependent reversible
$%, '$6, a+2*(3, 42) myelosuppression 1f'2 chloramphenicol f#2a+2+$ idiosyncratic aplastic
(& ADRs *2$oa+226 jg'me anemia 62' chloramphenicol (
jg2e&% thiamphenicol a+2+$ p-nitro
l6f single dose)(17, 42) group)(43)
(2, 3)
Hepatotoxicity (+&+jgl
6bi' > 4 g/day j# #2)
ADRs
Gray baby syndrome hg'&l5f 5$g+a6 d6|&%55$g
4*2 jg 'm% glucuronidation 6'5'a+2#+5$g m'
f'&
2 m$ 6 , gray cyanosis, 6lm f*%a+2 +g +,
vasomotor collapse mt'$6
$ #)(2, 17, 43)
(1)
Optic neuritis
(17)
njg, angioedema, anaphylaxis (&6+)
5 l % 6 cyclophosphamide, barbiturates, phenytoin, warfarin,
sulfonylureas) l*ji'bo(2, 3, 17, 43)
Drug interaction Paracetamol, protease inhibitors 5l%6 chloramphenicol i'bomm
& a(2, 17, 43)
(2, 43)
Phenobarbital, rifampicin m5l%6 chloramphenicol **'
e bacteriostatic p57 c d 6m p57 cd6fb2'b transfer RNA e chloramphenicol analog d6
+6#1
30s subunit of ribosome (66o' lm peptidyl transferase f55$g p-nitro group 6

1506 424
2 2556 52
#$%& 25 Spectinomycin, chloramphenicol, thiamphenicol (#2)
Spectinomycin
(Trobicin)
'4%"d#$)(17, 42) cavity 50S subunit of ribosome methylsulfonyl group 5l6*%*6o
44*1+ Gram-positive bacteria (66o''4%"d#$)(43) a$bof*%4'#+bo(43)
*6
(GABHS, S. pneumoniae, e65$g+$bb#p57 c' bb#p57 c '+j
MSSE), Gram-negative bacteria *6 + 4 4 *1 + Gram-positive chloramphenicol f#2 +$ p 5 7 c #2

(HENPEK, Salmonella, Shigella) bacteria, Gram-negative bacteria, Enterobacteriaceae f*% E. faecalis
d6|&% N. gonorrhoeae (+t' anaerobic bacteria, Chlamydia, $2 chloramphenicol(43)
penicillinase-producing strains) a#2 Mycoplasma, Coxiella, Rickettsia, l
l respiratory
6$+(42) Leptospira, Treponema f#26+$n*a+2 infections, gonorrhea, chancroid,
+$ b 2 'l
l gonococcal & ' % ' 4" 5$g 6 f ' 4j typhoid fever(43)
infections 52 o (42) f#2 a +2 l
l myelosuppression 5llvmm1l
vmm16'l
62'f&2*6l1
pharyngeal gonorrhea jg 'm6 |&%$5$gme52o(43) #"
+6#1 f5h+bi2 mucosal secretions a l
|&%l'b 2 'l
52 o
2
a+2(3,
$ 42) very severe pneumonia, scrub typhus
+$ % 5 7 & l l j w ' +$ 4 " ( l
f 5
gonorrhea a+2 #2 'm ceftriaxone doxycycline), empiric treatment
(drug of choice) m'e65'*jl bacterial meningitis lni5$gf&
$5$gni6f& beta-lactams(42) penicillins, cerebral abscess,
mastoiditis, septic arthritis, typhoid
fever(2, 3, 43)
lvmm1+$|&%if6|$ (e
6441+& ) 26%5ti
taf*jg'm&2 aplastic
anemia +(3)
if6f*% Injections : 2 g/vial Injections : 1 g/vial Capsules : 250 mg, 500 mg
4+f'5$g+$l Injections : 500 mg/vial, 750
%5a56 mg/vial
Antimycobacterial agents
+6d4f45$$6 (Mycobacterium spp.) ef45$$65$+g $4+& 4j n'h**"%6

oab+ (mycolic
acid and acyl lipids) f*%2lw2+$f2'#
+ (slow-growing bacteria) (
2 M. avium complex +$ doubling
time 10-12
gd+', M. tuberculosis +$ doubling time 20
gd+', M. laprae +$ doubling time 14-20 ) 5l+$
d4
f*% fjo'(1, 17, 44, 45)
Mycobacterium spp. 5$g+$4+4w5'4* af2 M. tuberculosis (5l d4), M. laprae (5l d4
jo), M. avium complex (5l MAC infections), nontuberculous mycobacteria (NTM) (5l #
jo5$g
hg'+$4*6d4, #2+o*j', n ', disseminated disease)
jo*2$o+# #2d6+nl*

ni6e*
2 6lj$6
1+
f jm 4265 t'4%" &
4
e#(1) f*%+f'd4lni5$g+$i+ 41+&2' (immunocompromised hosts) d6|&%ni#
jo
HIV(1)

1506 424
2 2556 53
Antibacterial agents 2lw2 +$p57 c#2#|&%f45$$65$gf2'# f#2 Mycobacterium spp. e
jo5$gf2'#

+m'+a+2#'#26 me#'l
antimycobacterial agents 2+*6
&jg'jo6 f*%
le*(1, 17)
Antituberculous agents
HcM (first-line agents) 5$gl

l tuberculosis af2 isoniazid, rifampicin, pyrazinamide, ethambutol,
streptomycin (#'5$g 26) l
li#6+# 2 HRZE(S)/ 4 HR(1, 17, 21)
HdT$ (second-line agents) af2 amikacin, kanamycin, cycloserine, ethionamide, para-aminosalicylate
(PAS), capreomycin, fluoroquinolones '
(levofloxacin, moxifloxacin, ofloxacin) (#'5$g 27) l
l$+$b
+l
first-line drugs j
jod4jo6*6b (multi-drug resistant tuberculosis, MDR-TB)
2 i#6 6
K5OPEZ/ 12-18 OPEZ j 6 K5O(P)EtCs(Z)/ 12-18 O(P)EtCs(Z)(1, 17, 21)
#$%& 26 First-line antituberculous agents
Isoniazid (INH) Rifampicin Pyrazinamide (PZA) Ethambutol
300 mg PO q 24 hr 450-600 mg PO q 24 hr 20-25 MKD PO q 24 hr 15-20 MKD PO q 24 hr
bl

j 5 MKD(3, 44, 45) j 10 MKD(2, 3, 44, 45) (max. 2,000 mg/day) (3, 44, 45)
(max. 1,600 mg/day)(3, 44, 45)
Absorption 90%(2, 3) 95%(2, 3) 90%(2, 3) 75-80%(2, 3)
3-7 mcg/mL *'%5 7-9 mcg/mL *'%5 30-50 mcg/mL *' 2-5 mcg/mL *'%5
Cmax
300 mg(2) 600 mg(2) %5 20-25 mg/kg(2) 25 mg/kg(2)
Plasma protein
0-15%(2, 3) 75-80%(2, 3) 10-17%(2, 3) 20-22%(2, 3)
binding
Vd 0.57-0.76 L/kg(2, 3) 0.93 L/kg(3) 0.9 L/kg(3) 2 L/kg(3)
Lungs, sputum, pleural
Liver, lungs, bile, pleural
#f2'5$g6 fluid, ascetic fluid, skin, Kidneys, lungs, saliva,
fluid, prostate, seminal Liver, lungs, CSF(2)
%m6aa$ saliva, muscle, caseous erythrocytes(2)
fluid, bone, saliva, CSF(2)
tissues, CSF(2)
#f2'5$g6
%m6aa CSF(2)
6
CSF 50%, 50%(3)
90%, 90%(2, 3) 85-100%(2, 3) 1%, 40%(3)
penetration (bl TB meningitis m'
(bl TB meningitis m' (bl TB meningitis m' (bl TB meningitis m'
(non-inflamed, 52b# jml

52b# ) 52b# ) #'& g+e 25 MKD)
inflamed) bi' 600 mg q 12 hr(2))
Bile
a+2+$b+i*(3) 7,000%(3) a+2+$b+i*(3) a+2+$b+i*(3)
penetration
ti *$g 6 f * ' d 6 N- ti *$g 6 f*'5$g # a e ti *$g 6 f*'5$g # a e '2ti*$g6f*'5$g#
acetyltransferase 2 (NAT) 25-desacetylrifampicin hg' pyrazoic acid hg'e active (2)
Metabolism
ae acetylisoniazid hg'a+2 e active metabolite(2, 44) metabolite(2)
+$p57 (2,
c 44)
75-95% 3-30% (metabolite +
Urine excretion (2) 10% (unchanged)(3) 50% (unchanged)(3)
(inactive metabolite) unchanged)(2, 3)
t la## 0.5-4
gd+'(2, 3) 2-5
gd+'(2, 3) 9-9.5
gd+'(2, 3) 3-4
gd+'(2, 3)
t l ESRD 1
gd+'(3) 11
gd+'(3) 26
gd+'(3) 10
gd+'(3)
#'b a+2#'(2, 3, 44, 45) l
2(44, 45) l
2(3, 17, 44, 45)
a+2#'(2, 3)
ld4a# (j* 50% l CrCl < 10) (**j 3 /") (**j 3 /")

1506 424
2 2556 54
#$%& 26 First-line antituberculous agents (#2)
#'l

6
l
2(3) a+2#'(2, 3) a+2#'(3) a+2#'(3)
*'5 HD
a+2#'(2, 3)
l
64+%+ % ' l
(f#2 l
64+%+ % ' a+2+$b+i*
#'b moderate hepatic impair.
f*% +l
l acute liver (f#24*$*$g6'l severe a+2#'(3)
ld4# f * % *$ *$g 6 ' l severe
disease, ni 5$g +$ % # INH- hepatic impairment)(3)
hepatic impairment(2, 3)
induced hepatotoxicity(2))
Pregnancy cat. C(2, 3) C(2) C(2, 3) B(2, 3)
Allergic
#g(3) *'(3) #g(3) #g(3)
potential
< 1 mcg/mL (S), 2
mcg/mL (I), > 4 mcg/mL
MIC breakpoint
(R) for Staphylococcus
spp.(2)
# (
# (+ e
# (
Optic neuritis
hepatocellular necrosis, & cholestatic jaundice, &a hepatocellular necrosis, (retrobulbar neuritis) +&
a 0.6-1%), transient 1%), LFT abnormalities +& 7"b65$ga), +jg l
l bi ' 2 15
elevation of transaminases (&a 10-15%)(1-3, 17, 44, 45) LFT abnormalities(1-3, 17, 44, MKD, m5lni6+$
45)
(&a 10-20%, + bo 4# #+ LFTs 51 +' **' (decreased
l
2' 2-3 jf5$g g+l
" x 3 j f Non-gouty polyarthralgia visual acuity) f*%#$
6, +&lni5$g+$61 > 40 mo# #+51j x 3 (m&at' 40%, f'b$6 (red-green color
j*'(3, 17)
, ni 5$g+$ d 4# 6i2 2 , ni 5$g d6l NSAIDs)(2) blindness) 4# #+
jg + 1 e %m j jg + v % 1 m m% o # Hyperuricemia (m5l +'51jl%2'5$g
, w ' +$ 4 " j & g ' 'jg o*6 $+-f'(2, 3, 17, d4 5" j %#1 l a66i2(1, 3, 17, 44, 45)
44, 45) (3, 17,
4*1 # , ni 5$g e slow (l
$v%+- d45" a f#2a+2#' njg, ab (drug fever)
acetylator)(2, 3, 17, 44, 45) f' e #2'2ni 6 l urate-lowering agents 45)
t& LFTs n # l l4+2++jll
6a ni6a+2+$)(1, 3, 17, Hyperuricemia (m5l
(45) 44, 45)
# #+ 2 4o ' / " ) d4 5" j %#1 l
m2m% g+**'m'# #+ 4*jg a m$ 6 , jg 4*jg a m$ 6 , jg d45" a f#2a+2# '
"*%4o' m*i2# (44, 45) (2, 3, 17, 44, 45) l urate-lowering agents
ADRs (3, 17,
f * % 4 61 l
+jg Flu-like syndrome (ab njg, ab (drug fever) ni6a+2+$)(1, 3, 45)
transaminases > 5 x ULN(2) g , $ %, 45)
Peripheral neuropathy
(3)
(3) (3)
Peripheral neuropathy %i) & 0.4-0.7% b'ni Sideroblastic anemia Metalic taste
(3, 17)
d6|&%lni6, 5$gl
rifampicin f 2 4o'/ Mental confusion
HIV, uremia, alcoholism, "(2, 3, 17, 44, 45)
(2, 3, 44,
malnutrition, w '+$4 ", njg, ab (drug fever)
(4l vitamin B6 15- 45)
50 mg/day 2 +6 &jg Hemolytic anemia,
(1,
'n*a+2&'%'4"$o) thrombocytopenia, acute
2, 17, 44, 45)
renal failure ( bo#'

, coma (+&l$ 61 l
6 5 5$ f* % +
a INH b)(44, 45) *+l
$)(2, 3, 44, 45)
(1-3, 17,
njg, ab (drug fever)
45)
Drug-induced lupus,
autoantibodies(3, 45)

1506 424
2 2556 55
(3, 17)
Hemolytic anemia
Neuropsychiatric change
lnii'61(2, 3, 17)
Isoniazid e potent Rifampicin e potent l PZA 2 + % 5
CYP450 inhibitor (CYP2C9, CYP450 inducer d6|&% alcohol, INH, rifampicin ethambutol 2+ antacids
CYP2C19, CYP2E1)(45) CYP3A4(2, 3, 17, 44, 45) & g+4+$g6 '#2 # (Al3+, Mg2+), buffered
(3)
l
INH 2 + l
rifampicin 2+ didanosine (+$ Mg2+-based
alcohol, rifampicin, PZA INH 2'*$g6 INH antacid li##) *
& g+4+$g6 '#2 # l e toxic metabolite ih+ ethambutol(3, 44)
(3)
(monoacetylhydrazine)(3, 45)
l
INH 2 + l
rifampicin 2+
phenytoin, carbamazepine, protease inhibitors (PIs),
benzodiazepines, alfentanil, NNRTIs (nevirapine,
theophylline 5l% efavirenz, delavirdine),
6*2$oi'bo(3, 17, 44, 45) estrogens (oral
l
INH 2 + contraceptives), macrolides
warfarin 5l INR i'bo (6 azithromycin), azole
(2, 3, 44)
antifungals, digoxin,
l
INH 2 + phenytoin, sulfonylureas,
ketoconazole, itraconazole warfarin, cyclosporine f*%
Drug 5 l % 6 6 jg u 5$g e CYP3A4
interaction ketoconazole, itraconazole substrate 5l%6
**'(2, 3) *2$o**'(2, 3, 17, 21, 44, 45)
%5 INH
2 + antacids (Al3+,
Mg2+) *ih+ INH
4 % 5 antacids
*' INH 62'6 2
gd+'
(2, 3, 17, 44)
% 5 INH
2+ tyramine-containing
foods
2 6fb' a"
m hypertensive crisis
(jg'm INH +$p57 c66o'
monoamine oxidase a
6)(3)
l
INH 2 +
SSRIs, pethidine m
serotonin syndrome(17)
p57 cd666o'ah+" p57 cd666o'ah+" p57 c4 *6 INH 4j p57 cd666o'ah+"
4 w l ' 4 % " DNA-dependent RNA 6 6o ' ah+" 4 w l 5$g$g6b''4%"
mycolic acid hg ' e polymerase b'f45$$6(1, '4%" mycolic acid f#2 cell wall b'
2, 17)
+6#1 '4" % 4 wb' cell 6 $o + t 2 M. mycobacteria(1)
envelope f*%m e bactericidal f tuberculosis a $ |&%l e bacteriostatic (5$g
metabolism of proteins, concentration-dependent % 5$g e ( acidic b 6 #g ) j
(17, 44, 45)
nucleic acid, lipids, killing 44*1+ environment)(1, 45) bactericidal (5$gb6i')

1506 424
2 2556 56
carbohydrates 6(1, 2, 17, 44) f 4 5$ $ 6 * 6
5$g e bacteriostatic j
(17, 44, 45)
e bacteriostatic l j m M. bactericidal bo 4+ +$p57 c#2 M. tuberculosis

resting M. tuberculosis f*% tuberculosis
2 MAC, M. b+b6lh**"(17, 45) f*% MAC (1, 17, 44)
d6b
e bactericidal l rapid laprae, S. aureus, Neisseria + t 2 M. l
l MAC
dividing M. tuberculosis(17, meningitidis, H. influenzae, tuberculosis a|&%5$g 6i2 infections 4j 15 MKD PO q
45)
MDR-Ps. aeruginosa, MDR- l%f*+5$ge 24 hr ( 2 +
2 M. tuberculosis a5o' A. baumannii(1, 2, 17, 44) (6lh**" f*% caseating clarithromycin j
lh**"f*%h**"(1, 45) jo6 rifampicin granulomas)( 1 , 4 5 ) m ' +$ azithromycin) (3, 17)
jo 6 INH m m*6& 71"b '6$ 5$g % d 6

" 6 l jo6 ethambutol
*6&71"b'6$5$g' ' RNA polymerase continuation phase m*6& 71"b '6$ 5$g
a h +" catalase- (rpoB gene) 5l target jo 6 PZA m 'ah+"5$ge+6
peroxidase hg'me#2 site *$g6f*'a(1, 44) *6&71"b'6$5$g' p57 (1) c
*$g6 INH le active ++$jo662' pyrazinamidase hg ' e lf DOT 4j 37.5-
form j +$ *6& 71" +jgl
monotherapy(1, 2) ah+" 5$g l
l *$g 6 50 MKD (2-4 g) 2 4o'/
b'6$ 5$g l
'ah+" 5$g Rifampicin m%tiih+a PZA le pyrazanoic acid " j 22.5-30 MKD
m e l '4 % " 6 * ' l ni 6 AIDS, (active form)(1, 2) (1.2-2.4 g) 3 4o'/"(44,
mycolic acid(1) , ni 5$g +$ v w lf DOT 4j 40-
45)
l f direct $g 6 i h + hg ' m 50 MKD (2-4 g) 2 4o'/ Ethambutol e65$gi
observe therapy (DOT) 4j e #1 g ' b'4+ " j 30-37.5 MKD 4 +
jo a $ + ( very
15 mg/kg (900 mg) 3 4o'/ *+*l(44) (1.5-3 g) 3 4o'/"(44, 45) hygroscopic) m ' + 6i2 l
"(3, 44, 45) lf DOT 4j 10 if film-coated tablets
+6#1 l Asians & slow mg/kg (600 mg) 2-3 4o'/ &jg ' + n
acetylators %+ 10- "(3, 44, 45)
20% hg'm%+$424g'
$ #b' t l
l staphylococcal
INH 6boe 3-4
gd+' infections (2+6jg) m%
(l fast acetylators m%+$42 l 300 mg PO q 12 hr
4g'
$ # < 2
gd+') 5l (staphylococcal PVE l
slow acetylators $g6'#2 300 mg PO q 8 hr)(2, 3)
neurotoxicity, hepatotoxicity Rifampicin 6 ' l
e
+bo(44) chemoprophylaxis lni 5$g
ni 65$g5 2 e slow + n
jo N. meningitidis
acetylator 4l
lb (ab * ' f2 ), H.
150 mg/day (*b*' influenzae type b (Hib) d6
50%)(3) l 600 mg PO q 12 hr x 2
INH monotherapy l
l (2, 17)
latent Rifabutin (6'a+2+$m26
tuberculosis (4j ni 6+$ l%5a56) e65$g+$
positive tuberculin test f#2 PK f*% ADRs 4* 6
a+2 & active pulmonary rifampicin f#2 +$ drug
lesions) 5o'lnilw2f*% interactions 62 m'
d6l 5 MKD 6-9 + t l 2 + PIs,
j(2, 17, 21, 44, 45) efavirenz a f #2 # ' *
b6 rifabutin *'(3, 17, 44)
if6f*% Tablets : 100 mg Caps : 300 mg, 450 mg Tablets : 500 mg Tablets : 400 mg, 500
4+f'5$g+$l Tablets : 600 mg mg
%5a56

1506 424
2 2556 57

Rifafour e-275 , Rimstar 4-FDC tablets %6 isoniazid 75 mg, rifampicin 150 mg, pyrazinamide 400 mg,
ethambutol 275 mg (o < 50 . l 3 tab hs, > 50 kg l 4 tab hs)

if6n+ Rifater tablets %6 isoniazid 80 mg, rifampicin 120 mg, pyrazinamide 250 mg

(fixed dose Rimactazid tablets %6 isoniazid 75 mg, rifampicin 150 mg (o < 50 . l 3 tab hs, > 50 kg l 4 tab
combination) hs)

Rifinah 150 capsules %6 isoniazid 100 mg, rifampicin 150 mg (o < 50 . l 3 cap hs)

Rifinah 300 capsules %6 isoniazid 150 mg, rifampicin 300 mg (o > 50 . l 2 cap hs)
#$%& 27 Second-line antituberculous agents

Cycloserine Ethionamide p-Aminosalicylate (PAS) Capreomycin
1 g j 15-30 MKD IM q
4 g PO q 8-12 hr(44, 45) 24 hr x 5-7 /"
250 mg PO q 12 hr 250-500 mg PO q 12 hr
(max. 12 g/day) l
2' 2-4 jf mo
bl
j 10-15 MKD(2, 3, 44, 45) j 15-20 MKD(2, 3, 44, 45)
(%5&+ x 2-3 /"(2, 3, 44)
(max. 1,000 mg/day) (max. 1,000 mg/day)
& g+ih+6(46)) (750 mg j 10 MKD lni
5$g+$61 > 60 (44))
Absorption 70-90%(2, 3) 99-100%(2, 3)
10 mcg/mL *'%5 2.2 mcg/mL *'%5 7-8 mcg/mL *'%5
Cmax a+2+$b+i*(2)
250 mg(2) 500 mg(2) 4 g af* 1-2
gd+'(46)
Plasma protein
a+2+$b+i*(2, 3) 10-30%(2, 3) 60-70%(46) a+2+$b+i*(2, 3)
binding
Vd 0.2 L/kg(3) a+2+$b+i*(3) 0.4 L/kg(3)
Lungs, sputum, pleural
#f2'5$g6 jo6jg#2'u, caseous
fluid, bile, ascetic fluid, jo6jg#2'u, CSF(2) Urine(2)
%m6aa$ tissue(46)
synovial fluid, lymph, CSF(2)
#f2'5$g6
%m6aa CSF(46)
6
CSF
penetration 90%, 90-100%(3) 100%(3)
(non-inflamed, (bl TB meningitis m' (bl TB meningitis m' < 10%(3)
inflamed 52b# ) 52b# )
meninges)
ti*$g6f*'5$g#d6 N-
acetyltransferase a e
ti*$g6f*'5$g#ae
Metabolism inactive metabolites
2
sulfoxide metabolite(2)
acetyl-PAS, para-
(46)
aminosalicyluric acid
50-70% (metabolites) +
Urine excretion 60-70% (unchanged)(2, 3) 1% (unchanged)(3) 50-60% (unchanged)(2, 3)
14-33% (unchanged)(46)
t la## 10-25
gd+'(2, 3) 3-4
gd+'(2, 3) 0.75
gd+'(46) 3-6
gd+'(2, 3)
t l ESRD a+2+$b+i*(3) 9
gd+'(3) 23
gd+'(46) 30
gd+'(3)
#'b l
2(3, 44, 45) l
2(2) l
2(46)
l
2(2, 3)
ld4a# (a+2f%+jg CrCl < 50(2)) (*b+jg CrCl < 30) (4*$*$g6'l
)

1506 424
2 2556 58
#$%& 27 Second-line antituberculous agents (#2)
#'l

6
l
2(3) a+2+$b+i*(3) a+2#'(44) l
2(2, 3)
*'5 HD
#'b l
2 (l severe hepatic
a+2#'(2, 3) a+2#'(2, 3)
ld4# impairment)(3)
Pregnancy cat. C(2, 3) X(2) C(2, 3)
Allergic
#g(3) #g(3) *'(3)
potential
Dose-related neurotoxicity 4*jg a m$ 6 , jg 4*jg a m$ 6 , jg
Nephrotoxicity (tubular
(h+, , 5'm # , , metallic taste, , 5 ', 5 '2 ' dysfunction, acute tubular
g , b+7 , delirium, 5 ', LFT abnormalities (+$bo*'l
6af* 1-2 necrosis) 4*6 AMGs, &
4 2 # #6,
) m ' 4 (4 g+lb 250 mg q " ) , steatorrhea a 20-36%(2, 3, 17)
*$*$g6'l
cycloserine 12 hr f*& g+5$*% 250 mg, (malabsorption syndrome), Ototoxicity (vestibular >
lni 65$g+$%# epilepsy % 5 6 & + LFT abnormalities(44-46) auditory)
2 vertigo,
jd45'm #
(2, 3, 17, 44, 2'j2
26 Hemolytic anemia, tinnitus, hearing loss &a
45)
* GI side effects a)(2, 3, leukopenia, 11%(2, 3, 17)
17, 44, 45)

+ & 7" agranulocytosis, 5$g |$ 6b
(17)
b6 d6&a 3% +jg CNS side effects
2 thrombocytopenia *+(2, 3)
l
500 mg/day f*% 8% +jg $ %, ' $ 6 , g , Hypersensitivitry Leukopenia,
(2, 3)
l
1,000 mg/day, 'a h+, #'*, olfactory reactions
2 njg, 4, ab, eosinophilia
ADRs d6l vitamin B6 50-200 abnormalities(2, 3, 45) a +2 6 # , b , njg, ab (drug fever)
(2, 3)
mg/day)(2, 44, 45) Peripheral neuropathy

(3,
mononucleosis-like Hypokalemia
(2)
(2, 17)
Peripheral neuropathy syndrome, eosinophilia(17,
3) 44, 46)
Orthostatic hypotension
(45)
njg, ab (drug fever) Gynecomastia, 4 & ( goiter) +
(2, 3,
impotence, menorrhagia myxedema(44, 45)
44, 45)
n f & f '
(photodermatitis), (44)
4 & ( goiter) +
hypothyroidism(2, 44, 45) n+
2'(3, 44, 45)
(3, 44, 45)
Hypoglycemia
l
cycloserine l
ethionamide l
PAS 2 + l
capreomycin
2 + ethambutol, 2+ cycloserine & g+ rifampicin rifampicin ti 2+ AMGs, vancomycin
ethionamide & g+4+ 4+$g 6 '#2 CNS side i h + a * *' jg 'ml & g + 4 + $g 6 ' #2
$g6'#2 CNS side effects effects(2, 3) PAS tablets +$ betonite nephrotoxicity, ototoxicity(2,
('2'h+ '$6)(2, 3) l
ethionamide (adsorbent) e
26(17) 3, 17)
l
cycloserine 2+ INH & g+4+ l
PAS 2 + l
capreomycin
Drug 2+ alcohol & g+4+ $g 6 ' #2 # f * % ethionamide & g+4+ 2+65$g66o' NMJ (
2
interaction $g6'#2
(3) peripheral neuropathy(3) $g6'#2 4&(44) AMGs, nondepolarizing
l
cycloserine l
ethionamide muscle relaxants) & g+4+
2+ phenytoin 5l 2+ ethambutol & g+ $g 6 ' #2 neuromuscular
% phenytoin & g+i'bo(2, 4+$g 6 '#2 GI side blockade(2)
3) (3)
effects f*% neuritis
l
ethionamide
2+ rifampicin, PZA

1506 424
2 2556 59
#$%& 27 Second-line antituberculous agents (#2)
& g+4+$g6 '#2 #
(3)
l
ethionamide
Drug 2 + thiacetazone
interaction additive toxicity(3)
l
ethionamide
2+ PAS & g+4+
$g6'#2 4&(44)
(17)
p57 c66o' cell wall p57 c 6 6o ' mycolic p 5 7 c d 6 6 6o ' e bacteriostatic
synthesis d6fb2'b D- acid synthesis f#26'a+2 ah+" l folic acid e injectable agent l
alanine(2, 17) 5*af2
(2) synthesis(17) MDR-TB 5$gjo#2 amikacin
(17, 44) (17)
+6#1 e bacteriostatic j e bactericidal e bacteriostatic j kanamycin(3)
bactericidal bo 4+ d4' ''2 4* 6
b+b6lh**"(17) isoniazid f*% thiacetazone
f#2a+2 cross resistance(44)
if6f*% Capsules : 250 mg Tablets : 250 mg Tablets : 1,000 mg a+2 +$ m 2 6l%5
4+f'5$g+$l a56
%5a56
Antileprotic agents
65$gl
ld4jo (leprosy) af2 dapsone, clofazimine, rifampicin(1, 17) d6*ji#6m%& m
m +
jol6d4 '$o
fgIhijOfkNH UMlmg$SU_P_M j#H gHgINUMMl

+$ 6d45$g 1 f' a f 2 65$g%551 : dapsone 100 mg OD +
borderline tuberculoid 5$g#m clofazimine 50 mg OD
&
jo jta+2&
jof#2+$ > RNGM
ni6
jo+
6 # f2 ' , mid-borderline, 65$g%5j*%4o' : rifampicin 600 mg 24 j
(multibacillary leprosy, MB)
borderline lepromatous, + clofazimine 300 mg
lepromatous
Nerve involvement > 2
+$ 6d45$g a +2 1 f' a f 2 65$g%551 : dapsone 100 mg OD
indeterminate, tuberculoid, RNGM
ni6
jo6
borderline tuberculoid 5$g#m 65$g%5j*%4o' : rifampicin 600 mg 6 j
(paucibacillary leprosy, PB)
a+2&
jo f*%+$ 1-5 #f2'
Nerve involvement 0-1
#$%& 28 Antileprotic agents

Clofazimine
Dapsone
(Lamprene)
*12+6 Sulfones(3, 17) Phenazine dye(17, 47)
100 mg PO q 24 hr(2, 3, 21) 50 mg PO q 24 hr(47) (%56&+)
bl

(1-2 MKD lni6) (50 mg OD x 2-3 4o'/" lni6)

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#$%& 28 Antileprotic agents (#2)
Clofazimine
Dapsone
(Lamprene)
Absorption 85-100%(2, 3) 45-62%(47)
0.7 mcg/mL *'%5 100 mg,
Cmax 3.1-3.3 mcg/mL *'%5 100 mg(2)
1.0 mcg/mL *'%5 300 mg(47)
Plasma protein
50-90%(2, 3)
binding
Vd 1.2 L/kg(3)
Fatty tissues, macrophages, mesenteric lymph nodes,
#f2'5$g6
Skin, muscle, kidneys, liver, sputum(2) adrenal glands, subcutaneous fat, liver, bile, gallbladder,
%m6aa$
spleen, small intestine, muscle, bone, skin(47)
CSF
100%(3)
penetration
ti*$g6f*'5$g#ae monoacetyl and diacetyl
Metabolism
metabolites(2)
Urine excretion 10-20% (unchanged) + 70-85% (metabolites)(2, 3)
t la## 25-30
gd+'(2, 3) 70 (long-term use)(47)
t l ESRD 30
gd+'(3)
#'b
a+2#'(2, 3)
ld4a#
#'l

6
a+2#'(2, 3)
*'5 HD
#'b
a+2#'(3)
ld4#
Pregnancy cat. C(2, 3) C(47)
Allergic
i'(3)
potential
(2, 3)
4*jga m$6, jg n ' +$ + $
+&i j o # * % + ( pink-brown
Hemolytic anemia +jgl
lni6 G-6-PD deficiency pigmentation) &a 75-100% b'ni65$gl
6$o d6m%
(f*%m&al4# 5$ga dapsone > 200 mg/day), '#&a6la+2$g" (ni6'65$g n*a+2&'
methemoglobinemia, leukopenia(2, 3, 17) %'4" $o m+$ %h + 1 f' t ' bo 2 # #6) f#2
CNS side effects
2 $%, '$6, #&2, +t*e# a*'61l
6*6j-e(17, 47)
ADRs tinnitus,
, a+2*, %%26, 5'm #(2, 3) n 'f'f*%*e% (ichthyosis) (8-28%), njg
(2, 3)
#, cholestatic jaundice 4 (1-5%)(17, 47)
(2, 3) (17, 47)
njg, ab (drug fever) v% 1mm% 'jg o# +% +$$o#*-f'
(3)
Mononucleosis-like syndrome hg'e#6t'
$ #a GI side effects
2 4*jga m$6, 5', 5'2'
m5 l d 4jo a l
2 'f (paradoxical (40-50%)(17, 47) f*%m& sever abdominal symptoms
effect)(17) (splenic infarction, bowel obstruction, GI bleeding)(47)
l dapsone 2+ antacids, buffered didanosine (+$
magnesium-based antacids li##) *ih+
b' dapsone(3) jg'm#'6lih+6
l dapsone 2 + zidovudine, pyrimethamine,
Drug
trimethoprim & g+4+$g6'#2 myelosuppression(3)
interaction
l dapsone 2+ rifampicin %6 dapsone
**'(3)
l dapsone 2+ probenecid %6 dapsone
& g+bo(17)

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#$%& 28 Antileprotic agents (#2)
Clofazimine
Dapsone
(Lamprene)
p57 cd666o'ah+" dihydropteroate synthase f p57 c d 6m mycobacterial DNA 2 ' n*l
jo
fb2'b (+j sulfonamides)(2, 3, 17) f2 ' # f*%m w # d#a * *' (17) +$ anti-inflammatory
(17)
e bacteriostatic #2 M. laprae activity m'
26* erythema nodosum leprosum reactions
Dapsone e drug of choice ld4jo51 6(17, 47)
+6#1 %5(2) f#2&jo6a%+ 40%(17) e bactericidal #2 M. leprae f*%e bacteriostatic #2
b2'l
jgu b' dapsone af2 PCP prophylaxis (l
M. avium complex(17)
e6$g6), mild to moderate PCP treatment (l
2+ l
l multibacillary leprosy (MB) f*%
trimethoprim), malaria prophylaxis and treatment, d4 mycobacterial infections jgu
2 M. avium complex
n ''
(dermatitis herpetiformis)(2, 3, 17, 21) (MAC), M. bovis(17, 47)
if6f*% Tablets : 100 mg Capsules : 50 mg
4+f'5$g+$l
%5a56
Antifungal agents
YEASTS Polyenes Azoles Echinocandins
Candida species AMB FLC ITC VRC PSC CPF MCF ANF
C. albicans S S S S S S S S
C. tropicalis S S S S S S S S
C. parapsilosis S S S S S S S S
C. glabrata S to I S to R S to R S to R S S S S
C. krusei S to I R S to R S S S S S
C. lusitaniae S to R S S S S S S S
Cryptococcus spp. S S S S S R R R
Trichosporon spp. R R R S S R R R
MOLDS Polyenes Azoles Echinocandins

Aspergillus species AMB FLC ITC VRC PSC CPF MCF ANF
A. fumigates S R S S S S S S
A. flavus S R S S S S S S
A. terreus R R S S S S S S
Fusarium solani S to R R R S S R R R
Scedosporium spp. R R R S S* R R R
Zygomycetes (Rhizopus,
S R R R S R R R
Mucor, Absidia species)
DIMORPHIC FUNGI
Histoplasma spp. S S S S S R R R
Coccidioides spp. S S S S S R R R
Blastomyces spp. S S S S S R R R
FGHIF#J *|&% Scedosporium apiospermum (Pseudallescheria boydii) 52o 5$ga#2 posaconazole

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Amphotericin B
Amphotericin B e6l*12+ polyenes hg'p57 cd6m ergosterol l cell membrane b'

jo e
nonaqueous f*% aqueous pores hg'm%5l+$g b' intracellular cations (K+, Mg2+, Ca2+)(2, 21, 48)
#$%& 29 Amphotericin B formulations
Amphotericin B Amphotericin B lipid Amphotericin B colloidal
Liposomal amphotericin B
deoxycholate complex (ABLC) dispersion (ABCD)
(L-AmB) (Ambisome)
(Fungizone) (Abelcet) (Amphotec, Amphocil)
Multilamellar vesicle with
Unilamellar liposome(21) Disk-shaped bilayer(21)
ribbonlike structure(21)
0.7-1 mg/kg IV q 24 hr 3-6 mg/kg IV q 24 hr(2, 3, 21,
5 mg/kg IV q 24 hr 3-6 mg/kg IV q 24 hr
bl
(drip 2-4
gd+')(2, 3, 21, 48) 48)
(zygomycosis #'ll
(drip 2
gd+')(2, 3, 21, 48) (drip 3-4
gd+')(2, 3, 21, 48)
max. dose 1-1.5 MKD bi' 4j 10-15 MKD(2))
0.5-3.5 mcg/mL *'l 0.4- 13-49 mcg/mL *'l 2.5 0.9-2.5 mcg/mL *'l 5 2-9 mcg/mL *'l 4 mg/kg
Cmax
0.7 mg/kg IV(2) mg/kg IV(2) mg/kg IV(2) IV(2)
Plasma protein
90%(2, 3) 90%(3) 90%(3) 90%(3)
binding
Vd 4 L/kg(2, 3) 131 L/kg(3) 131 L/kg(3) 4 L/kg(2, 3)
Inflamed pleura,
#f2'5$g6 peritoneum, synovium, Liver and spleen concentration i'2 f*% kidney concentration #g2 conventional
%m6aa$ aqueous humor, vitreous amphotericin B(2)
humor, peridcardial fluid(2)
CSF
2-3%(2, 3, 48) f#2&$6'&l cryptococcal meningitis
penetration
Urine excretion 5% (unchanged)(3) 5% (unchanged)(3) 5% (unchanged)(3) 5% (unchanged)(3)
t la## 15 (2, 3) 100-153
gd+'(2, 3) 173
gd+'(2, 3) 25-39
gd+'(2, 3)
t l ESRD 48 (3) a+2+$b+i*(3) 173
gd+'(3) 29
gd+'(3)
a+2#'(2, 3)
#'b
(4*jl
lipid a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
ld4a#
formulation +jg CrCl < 10)
#'l

6
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
*'5 HD
#'b
a+2#'(3) a+2#'(3) a+2#'(3) a+2#'(3)
ld4#
Pregnancy cat. B(2, 3) B(2, 3) B(2, 3) B(2, 3)
Allergic
#g(3) #g(3) #g(3) #g(3)
potential
Nephrotoxicity ( n2 2 *a 4j acute tubular necrosis f*% afferent arteriole vasoconstriction) +&7"b6
f*%%6%*5$ga d6vmm6$g6' af2 a6lb%+i' (large cumulative dose), +$5'b'a#&2'6i2
2, i'61, 66l# a, volume depletion, +$ hypokalemia, ni6l ICU, a nephrotoxic agents l
'ad6 aggressive hydration, salt loading (NSS 10-15 mL/kg 2f*% 1 L l%2' 6)(2, 3, 21, 48, 49)
(2, 3, 21, 48, 49)
ADRs Electrolyte abnormalities
2 hypokalemia, hypomagnesemia, hypocalcemia, hyponatremia
Infusion-related reactions
2 ab g, 4*jga m$6, $% *+jo + bo*'ma6af* 1-2

gd+' f*%m4'6i2 2-4
gd+', 'ad6 premedication 30-60 5$2l6 6 paracetamol 500-1,000 mg (j
ibuprofen 10 mg/kg) 2+ H1-antihistamines (
2 chlorpheniramine 10 mg IV) jtni6+$1f'ml
corticosteroids 6 (
2 hydrocortisone 25-50 mg IV) f*%' infusion-related chills 5$g1f' ad6l pethidine 25-50

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#$%& 29 Amphotericin B formulations (#2)
Amphotericin B Amphotericin B lipid Amphotericin B colloidal
Liposomal amphotericin B
deoxycholate complex (ABLC) dispersion (ABCD)
(L-AmB) (Ambisome)
(Fungizone) (Abelcet) (Amphotec, Amphocil)
mg IV(2, 3, 21, 48)
**j (phlebitis) hg''ad6mjm'6l+$4+b+ba+2 0.1 mg/mL, infusion time > 4
gd+'
f*%4 5$g**jblw2 (central line)(3, 21)
(2, 3)
4+*j#g
(2, 3, 21, 48, 49)
Myelosuppression (anemia, agranulocytosis, thrombocytopenia)
Conventional L-AmB ABLC ABCD

ADRs Test dose 4+$ a+2#' a+2#' 4+$
Fever 44-47% 17% 14% 55%
Chill/rigors 54-56% 18% 18% 77%
Nephrotoxicity 34-47% 19% 28% 8%
HypoK+ 12-29% 7% 5% 26%
HypoMg2+ 11-26% 20% a+2+$b+i* 6%
.
a2+ nephrotoxic agents jgu (
2 AMGs, vancomycin, colistin, foscarnet, cidofovir, pentamidine, NSAIDs,
cyclosporine, cisplatin, contrast media) & g+4+$g6'#2 nephrotoxicity +bo(2, 3)
Drug (2, 3)
Amphotericin B 5l hypokalemia, hypomagnesemia hg'& g+4+$g6'#2 digoxin toxicity +bo
interaction (2)
a2+ diuretics, corticosteroids m2' +l hypokalemia +bo
(2)
a2+ pentamidine m2' +l nephrotoxicity f*% hypocalcemia +bo
Invasive aspergillosis, Lipid formulations +$ % 57 &a+2#2 'm conventional amphotericin B f#2 +$
zygomycosis #'llb nephrotoxicity f*% infusion-related reactions #g2 (jg'm lipid complexes m%ti
i' (1-1.5 MKD) jg'm macrophages m f*%2'a6' cell membrane b'
jo +25$gm%a6'h**"2'6
Aspergillus spp., mo amphotericin B m%ti**26m lipid complexes 62'
u(21)) f#2#'ll
Zygomycetes (Rhizopus bi'2 f*%+$4f&'2 (f#2m41+42&%
26%642l
m265$gm%#'l
l
spp., Mucor spp., Absidia if* amphotericin B nephrotoxicity)(3, 21, 48-50)
spp.) a#2 amphotericin B b2'
$ol*$g6+l
lipid formulations af2 a+2#'#2*'ab
&$6'%*'(2, 3, 48) %+ (cumulative dose) > 500 mg, +$5'b'a#&2'6i22 (sCr > 2.5 mg/dL
(DOC aspergillosis j CrCl < 25 mL/min), +$5'b'a#f62*' (sCr & g+boe > 2.5 mg/dL lnilw2
4j voriconazole f*% DOC j& g+boe > 1.5 mg/dL l), severe acute administration-related toxicity, a
zygomycosis 4j nephrotoxic drugs jg2+6(2, 48)
+6#1 posaconazole) mj m'l 5% dextrose in water (D5W) 52o (+mjm'l*%*65$g+$ sodium
(3, 21)
6f chloride e2%
2 NSS, 5%DN/2 &%m5l ##%)
a d6llb 2 52b'
daily dose f#2#'a+2 1.5
mg/kg(21)
+jgni6 & #2a#m
conventional amphotericin
B m& m*b6*'
j *$g 6 a l
lipid
formulations(3, 48)
mjm'l 5% dextrose in
water (D5W) 52o(3, 21)
if6f*% Injections : 50 mg/vial Injections : 50 mg/vial a+2 +$ m 2 6l%5 Injections : 50 mg/vial
4+f' a56

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Azole antifungals
Azole antifungals p57 cd666o''4%" ergosterol hg'e'4"%4wb' fungal cell

membrane(2, 21, 48)
#$%& 30-1 Azole antifungals
Ketoconazole Fluconazole Itraconazole
(Nizoral) (Diflucan) (Sporal)
*12+626 Imidazoles(2, 3) Triazoles(2, 3) Triazoles(2, 3)
Candida spp., Histoplasma spp., Candida spp. (6 C. glabrata, C. Candida spp., Cryptococcus
Spectrum of Blastomyces spp., Paracoccidioides krusei), Cryptococcus neoformans, neoformans, Histoplasma spp.,
activity spp., Sporothrix spp., Histoplasma spp., Coccidioides spp., Coccidioides spp., Blastomyces spp.,
(21)
dermatophytes Blastomyces spp.(3, 21) Aspergillus spp.(21)
Histoplasmosis, blastomycosis, Cryptococcal meningitis (prophylaxis Histoplasmosis, aspergillosis(2, 21)
coccidioidomycosis, and treatment), candidiasis
Clinical uses paracoccidioidomycosis, superficial (prophylaxis and treatment)(2, 21)
fungal infections (candidiasis,
(2, 21)
dermatophytosis)
400 mg PO q 24 hr x 6-12 j 200 mg PO q 12-24 hr(2, 3, 21) (400
(non-meningeal cryptococcosis)(2) mg/day l aspergillosis,
1,200 mg IV/PO q 24 hr (+ histoplasmosis, blastomycosis,
flucytosine 100 MKD) x 6 " penicillosis, sporotrichosis)(2)
(cryptococcal meningitis, consolidation 200 mg PO q 24 hr (vaginal
phase)(2) candidiasis l 3 , esophageal
200 mg PO q 24 hr m2 CD4 > candidiasis l 14 )(2)
100 cells/mm3 62'6 6 j 200 mg PO q 12 hr x 1 "/
(cryptococcal meningitis, maintenance j (pulse therapy for
bl
200 mg PO q 12-24 hr(2, 3, 21)
phase)(2) onychomycosis *+jl 2 pulses,
150 mg PO single dose (vaginal *5 l 3 pulses)(2)
candidiasis)(2)
200 mg PO q 24 hr (oropharyngeal
candidiasis l 7-14 , esophageal
candidiasis l 14-21 )(2)
800 mg IV/PO loading dose then
400 mg IV/PO q 24 hr (candidemia)(2,
3, 21)
55% (capsules),
Absorption 82%(3) 90-100%(2, 3, 21)
90% (oral solution)(2, 3, 21)
6.72 mcg/mL *'%5 400
mg(2) 2 mcg/mL *'%5 200 mg q
Cmax 4.2 mcg/mL *'%5 200 mg(2)
3.9-5 mcg/mL *'l 100 mg IV a 12 hr (steady-state conc.)(2)
f* 6 (2)
Plasma protein
84-99%(2, 3) 11-12%(2, 3) 90-99%(2, 3)
binding
Vd 2 L/kg(3) 0.7 L/kg(3) 10 L/kg(3)
#f2'5$g6 Liver, pituitary gland, adrenal glands, Kidneys, skin, nail, blister fluid, saliva, Liver, skin, nail, bone, adipose tissue,
%m6aa$ lungs, kidneys, bladder, bone marrow, sputum, prostate, CSF(2) endometrium, cervical mucus,

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#$%& 30-1 Azole antifungals (#2)
#f2'5$g6 myocardium, various glandular bronchial fluid(2)
%m6aa$ tissue(2)
< 10%(3)
CSF 50-94%(2, 3)
< 10%(3) f#2&$6'&l cryptococcal
penetration (meningeal dose 400 mg q 24 hr)(3)
meningitis, coccidioidal meningitis(2)
62 lw2 ti *$g 6 f*'5$g # e
hydroxyitraconazole (active
Metabolism 6'2ti*$g6f*'5$g#(2) 6'2ti*$g6f*'5$g#(2)
metabolite) f*% inactive metabolite(2,
21)
60-80% (unchanged) + 11% (active 1% (unchanged) + 35%

Urine excretion 70% (unchanged)(3)
metabolite)(2, 3, 21) (metabolites)(2, 3)
t la## 6-8
gd+'(2, 3) 27-30
gd+'(2, 3, 21) 21
gd+'(3, 21)
t l ESRD 20
gd+'(3) 100
gd+'(3) 35
gd+'(3)
#'b l
2(2, 3) a+2#'(2, 3)
a+2#'(2, 3)
ld4a# (**' 50% +jg CrCl < 50)(2, 21) (4*$*$g6' IV form l CrCl < 50)
#'l

6
a+2#'(2, 3) l
2(2, 3) l
2(2, 3)
*'5 HD
#'b *$*$g6'l
l severe hepatic
a+2#'(2, 3) a+2#'(2, 3)
ld4# impairment(2, 3)
Pregnancy
C(2, 3) C(2, 3) C(2, 3)
category
Allergic
#g(3) #g(3) #g(3)
potential
< 8 mcg/mL (S), 16-32 mcg/mL (I), >
MIC breakpoint
64 mcg/mL (R) for C. albicans(2)
(2, 3, 21)
4*jga m$6, jg, 5'
(2, 3, 21)
Transaminase elevation, hepatitis (d6|&% ketoconazole)
QTc prolongation, arrhythmias (+&7"b6)(2, 3)
ADRs
Adrenal insufficiency, #+d#l&
6 (gynecomastia), 4+#'5'&**' (decreased libido), '4
#a+2
fb'# (impotence) &|&%l ketoconazole jg'm666o''4%" steroid hormones, +&+jgl
bi'
2
600-800 mg/day(2, 3, 21)
Azoles (6 fluconazole) #'6lih+6 'o+jga azoles 2+65$g5l gastric pH i'bo (
2
PPIs, H2RAs, antacids, buffered didanosine) m%5l6tiih+a6*' #'l
2+ antacids 4%5
azoles 2 > 1
gd+' j%5 azoles *' antacids > 2
gd+'(3, 21) f*%/j %56&+4jg'jg+5$g+$
4+e
2 o+, o*+(2)
(21)
Azoles e CYP3A4 inhibitor +jgl
2+ CYP3A4 substrates m5l%6*2oi'bom &
2
- Cisapride, quinidine & g+4+$g6'#2 QTc prolongation, TdP(2, 3, 21)
Drug - Ergot alkaloids & g+4+$g6'#2 ergotism(2, 3, 21)
interaction - Statins (simvastatin, lovastatin) & g+4+$g6'#2 myopathy(2, 3, 21)
- Warfarin INR i'bo, & g+4+$g6'#2 bleeding(3, 21)
- Sulfonylureas & g+4+$g6'#2 hypoglycemia(3)
- Midazolam, alprazolam, triazolam & g+4+$g6'#2 oversedation(2, 3, 21)
- Phenytoin & g+4+$g6'#2 CNS toxicity(21)
(3, 21)
CYP450 inducers (phenytoin, carbamazepine, rifampicin) 5l%6 azoles **'
(21)
Itraconazole e P-glycoprotein inhibitor 6 +jgl
2+ P-gp substrates
2 digoxin m5l%6i'bo

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Fluconazole e CYP2C9 f*% Itraconazole oral solution +$ oral
CYP3A4 inhibitor (lb < 400 availability i ' 2 itraconazole
mg/day m%66o'|&% CYP2C9, l capsules 'o*$g6f*'if
6m+$n*#2%6l*j(2, 3) (100
b > 400 mg/day m%66o' CYP2C9
f*% CYP3A4)(21) mg liquid = 200 mg capsule(2))
Itraconazole capsules 4
%5&+ &%ih+a
$ 2 %5#5 '2 ' (oral
bioavailability 90% f*% 40%
#+* ) 2 itraconazole oral
+6#1 solution 4%5#5 '2'
&%*ih+6 30%(2, 3)
(3)
l IV #' infusion > 1
gd+'
Itraconazole injection +$
hydroxypropyl-beta-cyclodextrin e
solubilizer hg'm+$%+lni5$g+$
5'b'a#&2' m'4*$*$g6'
l
6if|$lni5$g+$ CrCl < 50
mL/min(3, 21)
6 6o ' CYP3A4 a f '2
fluconazole
Tablets : 200 mg Capsules : 50 mg, 100 mg, 150 Oral solution : 10 mg/mL
if6f*%
mg, 200 mg Capsules : 100 mg
4+f'5$g+$l
Injections : 100 mg/50 mL, 200
%5a56
mg/100 mL
#$%& 30-2 Azole antifungals

Voriconazole Posaconazole
(Vfend) (Noxafil)
*12+626 2 generation triazoles(2, 3)
nd
2 generation triazoles(2, 3)
nd
Candida spp. 51

, Aspergillus spp., Histoplasma spp.,
Candida spp. 51
, Aspergillus spp., Histoplasma spp.,
Coccidioides spp., Cryptococcus neoformans,
Spectrum of Coccidioides spp., Cryptococcus neoformans,
Scedosporium spp., Fusarium spp., Zygomycetes
activity Scedosporium apiospermum, Fusarium spp. (a+244*1+
(Rhizopus spp., Mucor spp., Absidia spp.)(48) (bb#
Zygomycetes)(2, 48)
p57 c'5$g1)
Invasive aspergillosis, candidiasis f*% invasive fungal
Resistant candidiasis (d6|&% C. glabrata, C. krusei),
Clinical uses infections 5$ga+2#'#26jg (salvage therapy)
2
invasive aspergillosis, pseudollescheriasis(21)
zygomycosis(2, 48)
Oral dosing (for invasive aspergillosis) : 200 mg PO q 8 hr (prophylaxis for invasive aspergilosis
- o < 40 kg l 200 mg PO q 24 hr f then 100 and candidiasis l high-risk patients
2 GVHD,
mg PO q 12 hr (severe diseae j#'a+2#+5$g l prolonged neutropenia)(2, 3, 48)
bl
& g+e 150 mg PO q 12 hr)(2, 3, 21) 100 mg PO q 12 hr f then 100 mg PO q 24 hr x
- o > 40 kg l 400 mg PO q 12 hr f then 200 13 (oropharyngeal candidiasis)(2)
mg PO q 12 hr (severe diseae j#'a+2#+5$g l 200 mg PO q 6 hr j 400 mg PO q 8-12 hr (invasive
& g+e 300 mg PO q 12 hr)(2, 3, 21) candidiasis, oropharyngeal and pharyngeal candidiasis 5$g

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(Vfend ) (Noxafil)
(2, 3, 48)
IV dosing : 6 mg/kg IV q 12 hr f then 4 mg/kg IV jo#2 fluconazole j itraconazole)
q 12 hr (maintenance dose *$g6e oral form a)(2, 3, 21)
Absorption 96%(2, 3, 21) Well absorbed(2)
583-1,103 mcg/mL *'%5 200 mg q 8 hr &+
Cmax 2.51-4.6 mcg/mL(2)
(steady-state concentration)(2)
Plasma protein
58%(2, 3) 98%(2, 3)
binding
Vd 4.6 L/kg(2, 3) 1,774 L(2, 3)
CSF 90%(3)
a+2+$b+i*(3)
penetration (meningeal dose = usual dose)(3)
62lw2ti*$g6f*'5$g#d6 CYP2C19 (e*),
62lw2ti*$g6f*'d6 UDP glucuronidation (phase
Metabolism CYP2C9, CYP3A4 ae N-oxide voriconazole (inactive
II enzyme)(2)
metabolite)(2, 48)
Urine excretion 2% (unchanged) + > 80% (metabolite)(2, 3) b5'1mm%e* (66-71% in faces)(2, 3)
t la## 6
gd+'(3, 21) 35
gd+'(2, 3)
t l ESRD 6
gd+'(3) 35
gd+'(3)
(2, 3, 21)
#'b a+2#'
a+2#'(2, 3)
ld4a# (4*$*$g6' IV form l CrCl < 50)
#'l

6
l
2(2, 3) a+2#'(2, 3)
*'5 HD
l
2(2, 3, 21)
#'b a+2#'(2, 3)
* maintenance dose e 2 mg/kg IV q 12 hr l mild to
ld4# f#24l
64+%+%'
moderate hepatic impairment (Child-Pugh class A and B)(2)
Pregnancy cat. D(2, 3) C(2, 3)
Allergic
i'(3) #g(3)
potential
i#'5$g 30-1
(2, 3, 21, 48)
$%, , hallucinations, encephalopathy (d6|&% voriconazole)
4+n # $g6+'
g4
2 blurred vision, photopsia, altered color discrimination, appearance of
ADRs
bright spots and wavy lines, photophobia (&a%+ 20-30% b'ni5$gl
6 voriconazole, +&7"b6, + bo
l"f5$gl
6 f*%*e# a+jg61l
6 4*$*$g6'bb$g6&%)(2, 3, 21, 48)
(3)
l RCTs +$6'njgm voriconazole t' 20% f*%& SJS a6, photosensitivity
Posaconazole ti*$g6f*'d6 UDP glucuronidation
'o+jgl
2+65$ge UDP inducers (
2 rifampicin,
Drug
i#'5$g 30-1 phenytoin) m5l% posaconazole **'t' 50%(2, 3)
interaction
Posaconazole e P-gp substrate f*% CYP3A4 inhibitor
(+$# 6+j azoles #jgu)(2, 3)
4%56#5'2' (2*' > 1
gd+' 4%5& + (d6|&% high-fat meal)
j*' > 2
gd+') jg'm*ih+6 &%
26& g+ih+6 2-6 52(2, 3, 48)
(d6|&% high-fat food)(2, 3) f+26m%+$ half-life 6 f#24f2'%5 2-4 4o'/
(2, 21)
l IV #' infusion > 1-2
gd+' &jg& g+ih+6(2)
+6#1
Voriconazole injection +$ sulfobutyl ether-beta-
cyclodextrin e solubilizer hg'm+$%+lni5$g+$
5'b'a#&2' m'4*$*$g6'l
if|$lni5$g
+$ CrCl < 50 mL/min(2, 3, 21)

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(Vfend ) (Noxafil)
(2)
Non-linear PK profile (dose-dependent half-life )
Genetic polymorphism b' CYP2C19 +$n*#2%6
voriconazole d6&2 intermediate metabolizer f*% poor
metabolizer +$ AUC b' voriconazole i'2 homozygous
extensive metabolizer 2-4 52
if6f*% Tablets : 50 mg, 200 mg Oral suspension : 40 mg/mL
4+f'5$g+$l Injections : 200 mg/vial
%5a56
Echinocandins
Echinocandins p57 cd666o' beta(1,3)-D-glucan synthase hg'eah+"4wl' D-glucan hg'e

'4"%4wb' fungal cell wall(2, 21, 48)
#$%& 31 Echinocandins
Caspofungin Micafungin Anidulafungin

(Cancidas ) (Mycamine ) (Eraxis)
Spectrum of 44*1+|&% Candida spp. (+t'
5$gjoj42b'jo#2 amphotericin B, azoles
2 C. lusitaniae, C. krusei, C.
activity glabrata, C. tropicalis) f*% Aspergillus spp. (A. fumigatus, A. terreus, A. niger, A. flavus)(2, 21, 48)
l
e salvage therapy l invasive candidiasis, invasive aspergillosis 5$g*+*j a+2+tl
conventional
Clinical uses
amphotericin B, lipid formulations of amphotericin B, itraconazole(2, 48)
70 mg IV loading dose then 50 mg 100-150 mg IV q 24 hr (invasive 200 mg IV loading dose then 100
IV q 24 hr (invasive candidiasis, candidiasis treatment)(2, 3, 21, 48) mg IV q 24 hr (candidemia
(2, 3, 21, (2, 3, 21, 48)
invasive aspergillosis treatment) 50 mg IV q 24 hr (invasive treatment)
bl
48) (2, 3, 48)
candidiasis prophylaxis) 100 mg IV loading dose then 50
50 mg IV q 24 hr (invasive mg IV q 24 hr (esophageal
(48)
candidiasis prophylaxis) candidiasis treatment)(2)
8.6 mcg/mL *'l 200 mg loading
(2) 16.4 mcg/mL *'l 150 mg IV q 24
Cmax 9.39 mcg/mL then 100 mg IV q 24 hr (steady-state
hr (steady-state concentration)(2)
concentration)(2)
Plasma protein
97%(2, 3) > 99%(2, 3) 84-99%(2, 3)
binding
Vd a+2+$b+i*(3) 0.39 L/kg(2, 3) 30-50 L(2, 3)
#f2'5$g6
Liver Erythrocytes Liver
%m6aa$
Echinocandins +$4+b+bl CSF #g jg'm+$d+*1*blw2 f*% high protein binding f#2ma+2l
2bmll

CSF
fungal meningitis &% amphotericin B, itraconazole hg'+$4+b+bl CSF #g
2 6'+$% 57 &l
penetration
cryptococcal meningitis(48)
*6#5'4+$62'
u
Metabolism 62lw2ti*$g6f*'5$g# d6% hydrolysis f*% N-acetylation(48)
(slow chemical degradation)(2, 48)
1.4% (unchanged) +
Urine excretion 11% (unchanged)(3) < 1% (unchanged)(3)
41% (metabolite)(2, 3)
t la## 9-11
gd+'(2, 3) 10-15
gd+'(3) 40-50
gd+'(2, 3)
t l ESRD 10
gd+'(3) 10-15
gd+'(3) 40-50
gd+'(3)

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#$%& 31 Echinocandins (#2)
Caspofungin Micafungin Anidulafungin
(Cancidas) (Mycamine) (Eraxis)
#'b
a+2#'(2, 3, 48) a+2#'(2, 3, 48) a+2#'(2, 3, 48)
ld4a#
#'l

6
a+2#'(2, 3, 48) a+2#'(2, 3, 48) a+2#'(2, 3, 48)
*'5 HD
l
2(2, 3, 48) a+2#'(2, 3)
#'b
l 70 mg loading then 35 mg IV q 24 f#24l
64+%+%'l severe a+2#'(2, 3)
ld4#
hr l moderate hepatic impair.(2, 48) hepative impairment(48)
Pregnancy cat. C(2, 3) C(2, 3) C(2, 3)
(2, 21, 48) (2, 21, 48)
Infusion-related reactions Infusion-related reactions Infusion-related reactions (njg 4
(2, 48) (48)
Phlebitis Phlebitis *+& + 6lmb 4+
(2, 48) (48)
Hypokalemia Hypokalemia *j#g) +&+jg IV infusion rate >
(2, 48) (2, 48)
ADRs LFT abnormalities LFT abnormalities 1.1 mg/min(2, 3, 21, 48)
(2, 3) (2, 3) (2, 48)
njg, ab (drug fever) 4*jga m$6, 5'2' Phlebitis
(2, 48)
Hypokalemia
(2, 48)
LFT abnormalities
Caspofungin e CYP3A4 l micafungin 2 + Anidulafungin a+2 $g 6 b '
substrate m ' # 6 itraconazole m%5 l AUC b' CYP450 system (a+2e substrate,
CYP3A4 inducers/inhibitors
2 micafungin & g+bo%+ 11%(2) inhibitor, inducer) m'+$d #
CYP3A4 inducers (phenytoin, l micafungin 2+ nifedipine 66jg6+(2, 3)
carbamazepine, rifampicin, efavirenz) m%5l AUC b' micafungin & g+bo l anidulafungin 2 +
5l % caspofungin **' (3, 48) %+ 18%(2, 3, 21) cyclosporine m%5 l AUC b'
(4& g+b caspofungin e 70 l micafungin 2+ sirolimus anidulafungin & g+bo%+ 22%(2)
Drug
mg IV q 24 hr(2)) m%5l AUC b' micafungin & g+bo
interaction
l caspofungin 2 + %+ 21%(2, 3, 21)
cyclosporine m%5 l AUC b'
caspofungin & g+bo%+ 35%(21,
48)
l caspofungin 2 +

tacrolimus m%5 l AUC b'
tacrolimus **'%+ 20%(21, 48)
+mjm' caspofungin l*%*65$g+$ dextrose f*% IV infusion > 1
gd+' Infusion rate # 'a+2 1.1
(2, 3) (2, 3)
mg/min
l highly-resistant organisms m& g+ caspofungin maintenance dose e l
20% ethanol e diluent (nin* #
70 mg IV q 24 hr a(3) l+&+6)
+6#1
$65$6%2' caspofungin, micafungin amphotericin B l
candidemia &2+$% 57 &a+2f##2' f#21# "& #2a##g2(2, 48)
Caspofungin f*% micafungin +$l
lni6 2 anidulafungin
6'a+2+$b+i*% 57 &f*%4+*6(48)
if6f*% Injections : 50 mg/vial, 70 mg/vial Injections : 50 mg/vial Injections : 100 mg/vial
4+f'5$g+$l
%5a56

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Miscellaneous antifungals
#$%& 32 Miscellaneous antifungals

Terbinafine Nystatin
Griseofulvin
(Lamisil) (Mycostatin)
Dermatophytes (Microsporum spp., Dermatophytes (Microsporum spp.,
Spectrum of
Epidermophyton spp., Trichophyton Epidermophyton spp., Trichophyton Candida spp.(2)
activity
spp.)(2) (a+244*1+ Candida spp.) spp.)(2) (a+244*1+ Candida spp.)
Dermatophytosis Dermatophytosis Oropharyngeal candidiasis,
Clinical uses (2, 3)
(d6|&% onychomycosis) (d6|&% onychomycosis)(2) vaginal candidiasis(2)
500-1,000 mg PO q 24 hr x 4-6 500,000-1,000,000 units (5-10 mL)
" (griseofulvin micronized)(2, 3) 250 mg PO q 24 hr x 1 "(2, 3) +*o f* *j *% 3-5 4o '
bl
375-750 mg PO q 24 hr x 4-6 " (*+j l 6 ", *5 l 12 (oropharyngeal candidiasis)(2, 21)
(griseofulvin ultramicronized)(2, 3) ")(2) 100,000 units (1 vaginal tablets)
(onychomycosis l 4 j)
2'4* *%4o' x 14 (2)
50%
Absorption 70-80%(2, 3) 0%(2)
(70% +jg%5&+ fatty meal)(3)
0.8-1.5 mcg/mL (serum conc.) *'
Cmax 0.8 mcg/mL *'%5 500 mg(2)
%5 250 mg(2)
Plasma protein
84%(3) 99%(2, 3)
binding
Vd a+2+$b+i*(3) 13.5 L/kg(3)
#f2'5$g6 Stratum corneum, dermis, epidermis,
%m6aa$ nails, adipose tissue(2)
CSF
a+2+$b+i*(3) < 10%(3)
penetration
62lw2ti*$g6f*'5$g#ae
Metabolism 62lw2ti*$g6f*'5$g#(2)
6-demethylgriseofulvin(2)
Urine excretion 1% (unchanged)(3) 70-75%(2, 3)
t la## 9
gd+'(2, 3) 22-26
gd+'(2, 3) 4
gd+'(2)
t l ESRD 22
gd+'(2, 3) a+2+$b+i*(3)
#'b
a+2#'(2, 3) *$*$g6'l
l CrCl < 50(2, 3) a+2#'(2)
ld4a#
#'l

6
a+2#'(2, 3) *$*$g6'l
(2, 3) a+2#'(2)
*'5 HD
a+2#'(2, 3)
#'b *$*$g6'l
l chronic and active
f#24l
64+%+%'l severe a+2#'(2)
ld4# liver disease(2, 3)
hepative impairment(3)
Pregnancy cat. C(2, 3) B(2, 3) B(2)
Allergic
*'(3) #g(3)
potential
4*jga m$6, 5'j, 5'2', * o Transaminase elevation, hepatitis, 4*jga m$6, 5'2', b+* o(2)
m* o, +1+(2, 3) cholestasis(2, 3)
(2, 3) (2, 3)
$%, '$6, , #&2 4*jga m$6, GI upset
ADRs (2, 3)
Photosensitivity 4+n # $g6+'
(2, 3)
Leukopenia (+'&e$b$6)(3)
(3)
Hypersensitivity reactions Leukopenia, lymphopenia

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#$%& 32 Miscellaneous antifungals (#2)
Terbinafine Nystatin
Griseofulvin
(Lamisil) (Mycostatin)
(drug eruption, erythema multiforme, njg 4 , erythema multiforme,
TEN, SJS)(2) SJS(2, 3)
(3) (3)
m%#1l SLE ab (drug fever)
l griseofulvin 2+ alcohol l terbinafine 2+ alcohol,
disulfiram-like reaction(3) hepatotoxic drugs (
2 HIV protease
l griseofulvin 2 + oral inhibitors, nevirapine, isoniazid,
contraceptives, warfarin %6 macrolides)(2)
*2$o**'(2, 3) l terbinafine 2 +
l griseofulvin 2 + cimetidine %6 terbinafine
Drug
barbiturates %6 griseofulvin & g+bo(2, 3) (4*$g6e ranitidine,
interaction
**'(2) famotidine(2))
l terbinafine 2 +
phenobarbital, rifampirin %6
terbinafine **'(2, 3)
l terbinafine 2 +
cyclosporine cyclosporine **'(2)
p57 cd6m keratin precursor p57 c d 66 6o ' sterol Nystatin oral suspension ni6+
cells(2) synthesis(2) l4+2++jll
6#g jg'm
Ultramicronized form tiih+m % 6l* i ' + (250-550 6 +$
# a +2 $ m *$g 6 e
5' $ 2 micronized form mg/mL *'%5 250 mg PO q clotrimazole lozenges f5(2, 21)
+6#1
%+ 1.5 52(3) 24 hr x 3-18 ")(2)
4%5 micronized form &+ +$% 57 &i'2 pulse dose
high-fat meal &jg& g+ih+6(3) itraconazole l
(2)
onychomycosis
Tablets : 125 mg, 500 mg Tablets : 250 mg Oral suspension : 100,000
if6f*% units/mL
4+f'5$g+$l Vaginal tablets : nystatin 100,000
%5a56 units + di-iodohydroxyquin 100 mg +
benzalkonium chloride 7 mg
Antiviral agents
HSV VZV CMV HBV HCV HIV Influ.A Influ.B
Acyclovir, famciclovir, valaciclovir
Foscarnet
Ganciclovir, valganciclovir, cidofovir
Adefovir dipivoxil, telbivudine, entecavir
Lamivudine, tenofovir disoproxil fumarate (TDF)
Interferon-alpha 2b, peginterferon-alpha 2a
Peginterferon-alpha 2b, ribavirin, boceprevir, telaprevir
Amantadine, rimantadine
Oseltamivir, zanamivir

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Antivirals active against HSV and VZV
#$%& 33 Antivirals active against HSV and VZV

Acyclovir Valaciclovir Famciclovir
Foscarnet
(Zovirax) (Valtrex) (Famvir)
200 mg PO 5 4o'/ 2 g PO q 12 hr x 1 250 mg PO q 8 hr j 40 mg/kg IV q 12 hr x 2-
j 400 mg PO q 8 hr x 5- (herpes labialis)(2, 3) 500 mg PO q 12 hr x 7 3 " (HSV)
7 (herpes labialis, 1 g PO q 12 hr x 7-10 (1st episode of herpes 60 mg/kg IV q 8 hr x 3
herpes genitalis)(2, 3) (1st episode of herpes infection)(2, 3) " (acyclovir-resistant
800 mg PO 5 4o'/ genitalis, adult varicella)(2) 125 mg PO q 8 hr j HSV/ VZV)(2, 3)
(varicella, mild chickenpox 500 mg PO q 12 hr x 7- 250-500 mg PO q 12 hr x 7 90 mg/kg IV q 12 hr
l 5 , herpes zoster l 10 (recurrent herpes (recurrent herpes (j 80 mg/kg IV q 8 hr) x
bl

7-10 )(2, 3) genitalis)(2) infection)(2) 14-21 then 90-120
10 mg/kg IV q 8 hr j 1 g PO q 8 hr (herpes 500 mg PO q 8 hr mg/kg IV q 24 hr (CMV
800 mg PO q 6 hr (severe zoster l 7-10 , HSV (varicella l 5 , herpes infections)(2, 3, 21)
chickenpox l 7-10 , meningitis/ encephalitis l zoster l 7-10 , HSV
HSV or VZV meningitis/ 10 )(2) meningitis/ encephalitis l
encephalitis l 3 ")(2, 10 )(2, 3)
3)
10-30%(2, 3)
55%(2, 3)
Absorption (+jgb6i'bo m%+$ oral 77%(2, 3) 12-22%(2)
(3-5 52b' acyclovir)
bioavailability **'(2))
1.2 mcg/mL * ' 3.3-3.7 mcg/mL *' 3.3-4.2 mcg/mL *' 0.57 mcg/mL *'l 57
%5 400 mg(2) %5 500 mg(2) %5 500 mg(2) mg/kg IV(2)
1.6 mcg/mL * ' 4.6-5.5 mcg/mL * '
%5 800 mg(2) %5 1 g(2)
Cmax
9.8 mcg/mL *'l 5
mg/kg IV(2)
22.9 mcg/mL *'l 10
mg/kg IV(2)
Plasma protein
9-33%(2, 3) 14-18%(2, 3) 20%(2, 3) 14-17%(2, 3)
binding
Vd 0.7 L/kg(3) 0.7 L/kg(3) 1.1 L/kg(3) 0.5 L/kg(3)
Kidneys, liver, intestines, lungs, aqueous humor, tears,
#f2'5$g6
muscle, spleen, breastmilk, uterine, vaginal mucosa, Bone, cartilage(2)
%m6aa$
semen, amniotic fluid, CSF(2)
CSF 90% (non-inflamed),
50%(2, 3) 50%(2, 3) 50%(3)
penetration 100% (inflamed)(3)
Urine excretion 45-79% (unchanged)(2, 3) 80-89% (acyclovir)(2) 60-65% (penciclovir)(2, 3) 80-87% (unchanged)(2, 3)
t la## 2.5-3
gd+'(2, 3) 2.5-3.3
gd+'(2, 3) 2-3
gd+'(2, 3) 2-4
gd+'(2, 3)
t l ESRD 5
gd+'(3) 14
gd+'(3) 13
gd+'(3) 25
gd+'(3)
#'b l
2(2, 3)
l
2(2, 3) l
2(2, 3) l
2(2, 3)
ld4a# f*%*$*$g6'+jg CrCl < 20(3)
#'l

6
l
2(2, 3) l
2(2, 3) l
2(2, 3) l
2(2, 3)
*'5 HD
#'b
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
ld4#

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#$%& 33 Antivirals active against HSV and VZV (#2)
Foscarnet
(Zovirax) (Valtrex) (Famvir)
Pregnancy cat. C(2, 3) B(2, 3) B(2, 3) C(2, 3)
Allergic
#g(3) #g(3) #g(3) #g(3)
potential
(2)
4*jga m$6 $ %, '$6 , g , Nephrotoxicity (sCr > 2
(2, 3)
Crystalluria (d6|&%+jgl rapid IV infusion, large IV
(+&7"b6) mg/dL &a 37%, +&
(2, 3)
dose, +$5'b'a#&2'6i22, dehydration) 4*jg a m$6, 5 '2 ' +jg dehydration, a
(2, 3)
$ % , ' $ 6 , g , % % 2 6 ,
, 2 + nephrotoxic
hallucinations, encephalopathy (d6|&%+jglbi'l agents)(2, 3, 21)
(2, 3)
ni5$g+$5'b'a#&2', nii'61) Electrolyte abnormalities
(2)
Phlebitis, %464j' infusion site (IV form) (&a 8-15%)
2
(2)
njg 4 hypocalcemia,
(2)
Transaminase elevation hypokalemia,
hypomagnesemia,
hypophosphatemia (m
tetany)(2, 3, 21)
ADRs Nephrogenic diabetes
insipidus(3)
(2,
3)
4 *jg a m$ 6 , GI

upset(2, 3)
Myelosuppression
2
anemia(2, 3, 21)
CNS side effects
2
$ % ,
, g ,
hallucinations(2, 3)
f n * 6 5$g ' 4
#
(penile ulcers)(2, 21)
l acyclovir 2+ nephrotoxic agents & g+4+ l famciclovir 2+ l foscarnet 2+
$g6'#2 nephrotoxicity(3) digoxin 5 l % nephrotoxic agents (
2
(3)
l acyclovir 2+ theophylline 5l% digoxin i'bo amphoterin B, AMGs,
(2, 3)
theophylline i'bo cidofovir, cisplatin,
l acyclovir 2 + pethidine & g + % cyclosporine) & g+4+
(2)
norpethidine l*j $g6'#2 nephrotoxicity(2, 3)
l foscarnet 2+
Drug IV pentamidine & g+
interaction 4+$g6'#2 nephrotoxicity
f*% hypocalcemia(2, 3)
l foscarnet 2+
imipenem, ciprofloxacin
& g+4+$g6'#2
(2, 3)
l foscarnet 2+
zidovudine & g+4+
$g6'#2 anemia(3)

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#$%& 33 Antivirals active against HSV and VZV (#2)
Foscarnet
(Zovirax ) (Valtrex) (Famvir)
Acyclovir ti*$g6d6 viral thymidine kinase e e prodrug d6 99% e pyrophosphate
acyclovir monophosphate f*%*$g 6 #2 d6 cellular b'6m%ti *$g 6 f*'5$g analog b'
catalase e acyclovir triphosphate (active form) hg'66o' #f*%5' ae phosphonoacetic acid
viral DNA polymerase(2) penciclovir f*%*$g6 #2 p 5 7 c d 6 m 5$g
Valaciclovir e prodrug hg'm%ti*$g6f*'d6 valine e penciclovir pyrophosphate binding site
hydrolase 5$g#ae acyclovir(2, 3) triphosphate (active form) b' viral DNA polymerase
lnii'61 44b6 acyclovir #+ IBW &jg hg ' 6 6o ' viral DNA (foscarnet a+2#'ti*$g6
*$*$g6'ab6i' a(3) polymerase (2, 3)
d6 viral thymidine kinase
4*j l
famciclovir, 62' acyclovir m'a+2job+
valacyclovir +2 )(2, 21)
acyclovir lni6i+ 41+ +$ b 2 ' l
l acyclovir-
+6#1
#g ( immunocompromized resistant HSV/HZV f*%
patients) jg'm+$ oral ganciclovir-resistant CMV)(2,
bioavailability i'2(2) 21)
' & #2 a # d6

adequate hydration 6
NSS 2-3 L/day(2, 3, 21)
1 g foscanet #'mjm'
l NSS > 150 mL f*%l
slow IV infusion < 1
mg/kg/min (> 2
gd+')(2, 3,
21)
Tablets : 200 mg, 400 Tablets : 500 mg Tablets : 125 mg, 250 a+2+$m26l%5
if6f*%
mg, 800 mg mg a56
4+f'5$g+$l
Injections : 250 mg/10
%5a56
mL, 500 mg/20 mL
Antivirals active against CMV
#$%& 34 Antivirals active against CMV

Ganciclovir Valganciclovir Cidofovir
(Cymevene) (Valcyte) (Vistide)
5 mg/kg IV q 12 hr x 14-21 900 mg PO q 12 hr x 14-21 5 mg/kg IV (1-hr infusion) 51 1
(induction phase) then 5 mg/kg IV q (induction phase) then 900 mg PO q " x 2 d (induction phase)
24 hr j 1 g PO q 8 hr m2 CD4 24 hr m2 CD4 > 100 cells/mm3 then 5 mg/kg IV (1-hr infusion) 51 2
> 100 cells/mm3 62'6 3-6 j 62' 6 3-6 j (maintenance "(2, 21)
(maintenance phase)(2, 3, 21) (CMV phase)(2, 3, 21) (CMV retinitis and l2+ probenecid 2 g PO 2
bl

retinitis and extraocular CMV extraocular CMV infections) l cidofovir 3
gd+' f*% 1 g PO *'
infections) infusion m 2 f*% 8
gd+' &jg*
4.5 mg ocular implant 51 6-9 j nephrotoxicity (probenecid 6 6o '
(2 + oral valganciclovir +) tubular secretion of cidofovir)(2)
(CMV retinitis)(2)
5% (#5 '2'), 6-9% (& + 60% (&+)(2, 3, 21)
Absorption
), 28-31% (&+ fatty meal)(2, 3) (10 52b' oral ganciclovir)

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#$%& 34 Antivirals active against CMV
5.61 mcg/mL *'%5 900 mg
Cmax 9.5-11.6 mcg/mL *'l 5 mg/kg IV(2) 19.6 mcg/mL *'l 5 mg/kg IV(2)
(&+)(2)
Plasma protein
1-2%(2, 3) 1-2%(2, 3) 0.5%(2)
binding
Vd 0.74 L/kg(3) 0.7 L/kg(2)
#f2'5$g6
Intraocular(2)
%m6aa$
CSF
7-67%(3) 70%(3)
penetration
Urine excretion 90-99% (unchanged)(2, 3) 90% (ganciclovir)(2, 3) 80-100% (unchanged)(2)
4
gd+' (serum), 17-65
gd+' (active intracellular
t la## 2.5-4
gd+'(2, 3)
18
gd+' (intracellular)(2, 3) metabolite)(2)
t l ESRD 28
gd+'(3) 67.5
gd+'(3)
#'b l
2(2, 3)
l
2(2, 3) +l
+jg CrCl < 50 j sCr > 1.5(2)
ld4a# f*%*$*$g6'+jg CrCl < 10(2, 3)
#'l

6
l
2(2, 3) *$*$g6'l
(2, 3) l
2(2)
*'5 HD
#'b
a+2#'(2, 3) a+2#'(2) a+2#'(2)
ld4#
Pregnancy cat. C(2, 3) C(2, 3) C(2)
Allergic
i'(3) #g(3)
potential
Myelosuppression (anemia, moderate to severe neutropenia, Nephrotoxicity (proteinuria, serum
thrombocytopenia, aplastic anemia)(2, 3, 21) 4# #+ CBC 2-3 4o'/" creatinine elevation, proximal tubular
& ANC < 500 cells/mm3 l616jl G-CSF, platelet count < 25,000 dysfunction, metabolic acidosis,
cells/mm3 j Hb < 8 g/dL l616(2) Fanconi syndrome (normoglycemic
CNS side effects
2 $%, '$6, , hallucinations, g,
glycosuria, hypophosphatemia,
(+&7"b6)(2, 3, 21) hypouricemia) &%+ 25%,
(2, 3, 21) (2, 21)
GI side effects
2 4*jga m$6, 5'2', GI upset, stomatitis +&7"b6
ADRs (3) (2, 21)

, peripheral neuropathy Neutropenia (&%+ 15%)
(2, 21)
LFT abnormalities ADRs m porbenecid (5$gl2+
(3)
Retinal detachment cidofovir) af2 ab g, $%
(2, 3)
njg, ab (drug fever) , GI side effects, njg (m& ml
antipyretics, antihistamines,
antiemetics &jg' ADRs *2$o)
(2)
l ganciclovir 2+ cytotoxic drugs, pyrimethamine, 5-flucytosine, a2+ nephrotoxic agents
interferons & g+4+1f'b' myelosuppression(2, 3) jgu (
2 amphotericin B, AMGs,
l ganciclovir 2 + zidovudine & g +4+$g6 '#2 severe vancomycin, colistin, foscarnet,
myelosuppression (#'l
2+ zidovudine a+24 300 mg/day(2, 21) pentamidine, NSAIDs, cyclosporine,
Drug (2, 3)
l ganciclovir 2+ imipenem & g+4+$g6'#2
cisplatin, contrast media) & g+4+
interaction (3)
l2+ probenecid 5l% ganciclovir, valganciclovir i'bo $g6'#2 nephrotoxicity +bo # '
l oral ganciclovir 2+ didanosine 5l% didanosine & g+bo 61 nephrotoxic agents 62'6 1
111%, IV ganciclovir 5l% didanosine & g+bo 50-70%(2) " 2l cidofovir(2)

1506 424
2 2556 76
#$%& 34 Antivirals active against CMV (#2)
Probenecid (5$gl 2+ cidofovir)
Drug 66o' tubular secretion b' acyclovir,
interaction beta-lactams, zidofovir, tenofovir
5l%6*2$oi'bo(2)
Ganciclovir ti *$g 6 d6 viral Valganciclovir e prodrug hg'm%ti Cidofovir ti *$g 6 d6 cellular
protein kinase b' CMV e *$g6f*'62'5$gn'*af*% enzyme e cidofovir diphosphate
ganciclovir triphosphate (active form) # ae ganciclovir(2, 3, 21) (active form) hg'66o' viral DNA
hg'66o' viral DNA polymerase(2, 21) Oral valganciclovir 900 mg l AUC polymerase(2, 21)
Induction phase l CMV 29 mcg hr/mL hg'52 IV ganciclovir a+2 l
e 6fl CMV
#'l IV form 52o(3) 5 mg/kg(2, 3) retinitis (DOC 4j oral valganciclovir)
Ganciclovir intraocular implant 4*jl
valganciclovir +2 jg 'm+$ & #2 a#i ' f#2 +$ b $ 4j
+6#1
(Vitrasert) l
l CMV ganciclovir l51 $ (6 CMV 6 " * % 4 o ' f * % +$
retinitis d6v'l vitreous humour hg' prophylaxis l liver transplant % 5 7 &l ganciclovir-resistant
m%**26#6 1 mcg/hr a 6- patients)(3) CMV(2)
9 j f#2#'l2+ valganciclovir ' & #2 a # d 6 adequate
900 mg PO q 24 hr +(2, 21) hydration 6 NSS > 1 L 2
cidofovir infusion f*%l probenecid(2,
21)
if6f*% Injections : 500 mg/vial Tablets : 450 mg a+2+$m26l%5a56

4+f'5$g+$l
%5a56
Antivirals active against HBV and HCV
#$%& 35-1 Oral nucleos(t)ide analogues

Adefovir dipivoxil Tenofovir disoproxil fumarate Lamivudine (3TC)
(Hepsera) (Viread) (Zeffix)
*12+6 Adenosine analogue(51, 52) Adenosine analogue(51, 52) Cytidine analogue(51, 52)
Chronic hepatitis B lnilw2 Chronic hepatitis B lnilw2
b2'l
Chronic hepatitis B lnilw2(2, 51)
f*% > 12 (2, 51) f*%(2, 51)
100 mg PO q 24 hr x 1 (chronic
hepatitis B)(2, 51, 52) (2j*'
10 mg PO q 24 hr x 48-92 "(2, 3, 300 mg PO q 24 hr(2, 3, 51)
bl
51, 52) a)
(2j*'a) (2j*'a)
150 mg PO q 12 hr j 300 mg
PO q 24 hr (HIV)(2, 3, 51)
25-30% (#5'2'),
Absorption 59%(2, 3) 86%(2, 3)
40% (&+ fatty meal)(2, 3)
Cmax 18.4 + 6.26 ng/mL(2) 296 + 90 ng/mL(2) 3 mcg/mL(2)
Plasma protein
< 4%(2, 3) < 7.2%(2, 3) 36%(2, 3)
binding
Vd 0.4 L/kg(2, 3) 1.3 L/kg(2, 3) 1.3 L/kg(2, 3)
CSF
a+2+$b+i*(3) a+2+$b+i*(3) 15%(3)
penetration

1506 424
2 2556 77
#$%& 35-1 Oral nucleos(t)ide analogues (#2)
32% (unchanged)(3)
Urine excretion 45% (unchanged)(3) 5' glomerular filtration f*% active 71% (unchanged)(2, 3)
tubular secretion(2, 3)
7.5
gd+'(3, 52), 11-17
gd+'(2, 3), 5-7
gd+'(2, 3),
t la##
16-18
gd+' (intracellular)(2) 12-50
gd+' (intracellular)(2) 12
gd+' (intracellular)(2)
t l ESRD 9
gd+'(3) a+2+$b+i*(3) 20
gd+'(3)
#'b
l
2(2, 3, 51) l
2(2, 3, 51) l
2(2, 3, 51)
ld4a#
#'l

6
a+2+$b+i*(3) l
2(2, 3) l
2(2)
*'5 HD
#'b
a+2#'(2, 3) a+2#'(2, 3) a+2#'(2, 3)
ld4#
Pregnancy cat. C(2, 3) B(2, 3) C(2, 3)
Allergic
#g(3) #g(3) #g(3)
potential
Nephrotoxicity &a+226ll
Nephrotoxicity, renal tubular GI side effects
2 4*jga m$6,
HBV (10 mg/day) f#2+&l acidosis, Fanconi syndrome 5', 5'2'(2)
(2)
$l
HIV (30-120 mg/day), +$ (normoglycemic glycosuria, $%
(2, 3)
5'b'a#&2'6i22, a hypophosphatemia, hypouricemia, Lactic acidosis (&6+)
2+ nephrotoxic agents(2, 51, 52) proteinuria) +&lni5$g+$ 5' #2 (+$ 6'lni 6
GI side effects
2 4*jga m$6, b'a#&2 '6i2 2 , a 2 + )(2)
5 ' , 5 ' j , 5 ' 2 ' , nephrotoxic agents(2, 3, 51)
dyspepsia(2, 3) GI side effects
2 4*jga m$6,
(2, 3)
$%, 2f' 5', 5'j, 5'2'(2, 3)
(2) (3)
Lactic acidosis (&6+) $%, 2f'
(2)
ADRs Fanconi syndrome (&6+) Asymptomatic elevation of CPK
(2)
#2 (&6+) (&a 12%)(2)
Transaminase elevation (&a 4-
5%)(2)
(2)
Amylase elevation (&a 9%)
Bone density **', $g 6 '#2
%i (4# #+ BMD lni65$g
+$%# %i j+$4+$g6'#2
osteopenia)(2, 3, 51)
Lactic acidosis with hepatic
steatosis (&6+)(2, 3)
Adefovir a+2$g6 b ' CYP450 TDF a+2 $g 6 b ' CYP450 3TC a+2 $g 6 b ' CYP450
system (a+2e substrate, inhibitor, system (a+2e substrate, inhibitor, system (a+2e substrate, inhibitor,
inducer) m'+$d # 6 inducer) m'+$d # 6 inducer) m'+$d # 6
6jg6+(3) 6jg6+(2, 3) 6jg6+(2, 3)
Drug
l adefovir 2+ ibuprofen l TDF 2+ adefovir & g+
interaction
5 l AUC b' adefovir & g+ bo 4+$g 6 '#2 nephrotoxicity m' 4
23%(2) *$*$g6'l
2+(51)
l adefovir 2+65$g66o' l TDF 2 + valaciclovir,
tubular secretion (
2 probenecid) atazanavir, lopinavir/ritonavir 5l

1506 424
2 2556 78
5l% adefovir i'bo(2) % TDF i'bo(2, 3)
Drug l TDF 2+ didanosine
interaction & g+4+$g6'#2 virologic failure m'
4*$*$g6'l
2+(3)
+$% 57 &5o'l treatment-nave +$% 57 &5o'l wild-type HBV RCTs &2l 3TC 100 mg/day
patients f*%65$g*+*m f*% 3TC-resistant HBV(51, 52) x 1 * HBV DNA level a, 5l
6 3TC (3TC-resistant HBV)(2, 52) RCTs &2l TDF 300 mg/day ALT *e# , *f*%
RCTs &2l adefovir 10 +$ virologic efficacy f*% overall fibrosis b'# a 50-60% b'
mg/day x 48 " +$ni65$g+$ ALT response rate i'2 adefovir 10 ni6 f*%& loss of HBeAg 30%(52)
*e# 48-72%, +$ liver histology mg/day 5o'lni 6 HBeAg-positive
$bo 53-64%, +$ HBV DNA **' 3.6- f*% HBeAg-negative(51)
% 57 &
log copies/mL(52) l TDF * HBV DNA a 3-4
l
adefovir 2+ 3TC
26* log 5$g* 24 "(52)
jo 6 3TC l treatment-nave
patients a (resistance rate 43% f*%
15% #+*), +$# ALT *e
# i'2, * HBV DNA a+2
(51)
Adefovir monotherapy +$jo6

TDF +$jo6
2 3TC d6&
3TC monotherapy +$jo6i'
2 3TC monotherapy d6& resistance rate 0% 5$g* 48 ", d6& resistance rate 16-32% l 1
resistance rate 0% 5$g* 78 "(2) 3% 5$g * 96 ", 30% 5$g* 240 , 42% l 2 , 60-70% l 5 )(51) m'
f*% 15-18% 5$g* 192 "(52) ")(51) a+2f%ll
3TC monotherapy f#2
jo6 l l
2 + 6jg (
2 interferons,
nucleoside analogues jgu)(52)
jo6 3TC m*6&71"
b' HBV DNA polymerase 5$g YMDD
motif (184 V mutation)(52)
Adefovir dipivoxil e prodrug hg'm% +$p57 c#2 HBV f*% HIV m'+l
l ti *$g 6 f*'6lh**" d 6
ti*$g6f*'ae adefovir f*%ti HIV-HBV coinfected patients(3, 51, 52) phosphorylation e lamivudine
*$g 6 f * ' 6 l h * *" d 6 +$ b $ a f 2 6 *%4o ' , triphosphate (active form) hg'66o'
phosphorylation e cidofovir mitochondrial toxicity #g2 NRTIs DNA polymerase b' HBV(2, 52)
diphosphate (active form) hg'66o' #jgu(2) +$p57 c#2 HBV f*% HIV m'+l
l
DNA polymerase b' HBV f*%5l 4# #+ BUN, sCr, urinalysis HIV-HBV coinfected patients(2, 52)
chain termination(2, 51, 52) %2'l
6 f*%*$*$g6'l
2+ +$ b $ a f 2 6 *%4o ' ,
+$p57 c#2 HBV, HIV, HSV, CMV f#2 nephrotoxic agents(3, 51) mitochondrial toxicity #g2 NRTIs
a ' l l
l chronic a+2461l
655$5l&%m #jgu, 4ti(2, 51)
+6#1
hepatitis B 52o(52) 5l HBV flare up (exacerbation +$%d6
"l'j HBV
Adefovir +$ % 57 &l chronic of hepatitis)(2, 3, 51) infection m*it26#(52)
hepatitis B #g 2 entecavir, a+2461l
655$5l&%m
telbivudine, tenofovir(2) 5l HBV flare up (exacerbation
4# #+ BUN, sCr, urinalysis of hepatitis)(2, 3, 51)
%2'l
6 f+m%e l
b #g
(52)
a+2461l
655$5l&%m
5l HBV flare up(2, 3, 51)

1506 424
2 2556 79
if6f*% Tablets : 10 mg Tablets : 300 mg Tablets : 100 mg
4+f'5$g+$l
%5a56
#$%& 35-2 Oral nucleos(t)ide analogues

Telbivudine Entecavir
(Sebivo) (Baraclude)
*12+6 Thymidine analogue(2, 51, 52) Cyclopentyl guanosine analogue(2, 51, 52)
b2'l
Chronic hepatitis B lnilw2(2, 51) Chronic hepatitis B lnilw2 f*%612 > 16 (2, 51)
0.5 mg PO q 24 hr x 48 " (nucleoside-nave
patients)(2, 3, 51, 52)
600 mg PO q 24 hr(2) (2, 3, 51)
bl
1 mg PO q 24 hr (3TC-refractory patients)
(2j*'a)
4%56#5'2' (2 j *' > 2

gd+') jg'm*ih+6 18-20%(2, 51, 52)
Absorption Well absorbed(2)
(2)
3.69 mcg/mL *'%5 600 mg q 24 hr 4.2 ng/mL *'%5 0.5 mg q 24 hr
Cmax
(steady-state concentration)(2) 8.2 ng/mL *'%5 1 mg q 24 hr
(2)
Plasma protein
13%(2)
binding
Urine excretion 62-73% (unchanged)(2, 3)
(2)
t la## 40-49
gd+' 128-149
gd+'(2, 3), 15
gd+' (intracellular)(2)
#'b
l
2(2, 3, 51, 52) l
2(2, 3, 51, 52)
ld4a#
#'l

6
l
2(2) a+2#'(3)
*'5 HD
#'b
a+2#'(2) a+2#'(2, 3)
ld4#
Pregnancy cat. B(2) C(2, 3)
(2, 3)
CK elevation (&a 9%), myopathy m bo*'l
6 GI side effects
2 4*jga m$6, 5', 5'2'
(2, 3)
# #2 *6 " j *6j 4 % ' $%, 2f', a+2*
(3)
$g6*+jolni5$ga telbivudine 2+6jgu 5$g+$ URIs, a
ADRs n*#2*+jo
2 statins(2, 51, 52) Lactic acidosis (&6+)
(2)
(2)
Peripheral neuropathy d6|&%+jg a 2 + njg, n+2' (&6+)
pegIFN(2, 51)
(2)
Lactic acidosis (&6+)
Telbivudine a+2$g6b ' CYP450 system (a+2e Entecavir a+2$g6 b ' CYP450 system (a+2e
Drug
substrate, inhibitor, inducer) m'+$d # 66 substrate, inhibitor, inducer) m'+$d # 66
interaction
jg6+(2) jg6+(2)
RCTs &2l telbivudine 600 mg/day x 52 " RCTs &2l entecavir 0.5 mg/day x 48 " *
% 57 & * HBV DNA a > 5 log copies/mL 2+ loss of HBeAg HBV DNA a 5.0-6.9 log copies/mL, loss of HBeAg 21%,
j+$ ALT *e# %+ 75% b'ni 6(52) ALT *e# 68-78% b'ni 6(52)
(2, 3, 52)
Telbivudine +$ resistance rate 3-4% 5$g* 1 , 8.6% (l Entecavir +$% 57 &l 3TC-resistant HBV f#2
jo6 HBeAg-negative patients), 21.6% (l HBeAg-positive ni5$g46jo#2 3TC m%+$djo entecavir i'2 nave
patients) 5$g* 2 (2, 51, 52) patients(2, 51)

1506 424
2 2556 80
Telbivudine Entecavir

(Sebivo ) (Baraclude)
HBV 5$g jo #2 telbivudine + m%jo #2 3TC 6 Resistance rate l 3TC-refractory patients 6-7% 5$g*
(L180M/M204V double mutation, M204I mutation) f#2m 48 ", 15% 5$g* 96 ", 46% 5$g* 192 "
6'a#2 adefovir (6 A181V mutation)(2, 51, 52) (51)
jo6 Resistance rate l nucleoside-nave patients 0.2% 5$g

* 48 ", 0.5% 5$g* 96 ", 1.2% 5$g* 192
")(51, 52)
(52)
HBV 5$gjo#2 entecavir +6'a#2 adefovir
(2, 52) (2, 52)
p57 c66o' DNA polymerase b' HBV p57 c66o' DNA polymerase b' HBV
(2) (2)
+$p57 c#2 HBV 52o (a+2+$p57 c#2 HIV) +$p57 c#2 HBV f*% HIV
+$b$ af2 in vitro activity i'2 3TC, adefovir f*%jo +$b$ af2 in vitro activity i'2 3TC, adefovir f*%+$
6#g2f*%
2 3TC(2) jo6#gl nave patients(2, 51, 52)
+6#1 4*$*$g6'l
telbivudine 2+ 3TC &%&2+$ 4*$*$g6'l
entecavir 2+ 3TC, entecavir
% 57 &#g2 telbivudine monotherapy(51) 2+ telbivudine jg'mjo6 3TC f*% telbivudine
(51)
a+2461l
655$5l&%m5l HBV flare m%2'n*ljo#2 entecavir 6
up (exacerbation of hepatitis)(2, 3, 51) a+2461l
655$5l&%m5l HBV flare
up (exacerbation of hepatitis)(2, 3, 51)
if6f*% Tablets : 600 mg Tablets : 0.5 mg, 1 mg
4+f'5$g+$l
%5a56
#$%& 36 Interferon alfa and thymosin alfa-1

Recombinant interferon Thymosin alfa-1
Peginterferon alfa-2a Peginterferon alfa-2b
alfa-2b (thymalfasin)
(Pegasys) (Peg-Intron)
(Intron-A) (Zadaxin)
Branched peg chain, Linear peg chain,
Peg chain - -
40 kDa(51) 12 kDa(51)
HBV, HCV
b2'l
HBV, HCV lnilw2(2, 51) HBV, HCV(2, 51) HBV, HCV(53)
lnilw2f*%(2, 51)
10 million units |$bl# 1.6 mg j 0.9 mg/m2
n '/|$b*+ 3 4o'/ |$ b l# n ' 2 4o ' /
bl
f*% " j 5 million units " (monotherapy j
%6%*l *%4o ' (HBeAg-positive l
2 + IFN alfa-2b,
(53)
HBV patients l 16-24 ", lamivudine a)
HBeAg-negative patients l
> 48 ")(2)
Combination therapy : 3 180 mcg |$bl#n ' Combination therapy :
1.6 mg |$bl#n ' 2
million units |$ b l# "*%4o' 1.5 mcg/kg |$bl#n ' 4o'/" (l
2 + IFN
bl
n '/|$b*+ 3 4o'/ (5o' monotherapy f*% "*%4o'(2, 51) alfa-2b 3 million units 3
l HCV " x 48 "(2, 51) combination therapy)(2, 51)
Monotherapy : 1 mcg/kg 4o'/", pegIFN alfa +
|$ b l#n ' " * % ribavirin a)(53)
4o'(2, 51)
ANC < 750
ANC < 750 3
b 3 cells/mm j platelet <
cells/mm l * e 135
l HCV 80,000 cells/mm3 l*e
mcg/week(2)

1506 424
2 2556 81
#$%& 36 Interferon alfa and thymosin alfa-1 (#2)
(Pegasys) (Peg-Intron)
platelet < 50,000 0.5 mcg/kg/week(2)
cells/mm3 l * e 90 ANC < 500
mcg/week(2) 3
cells/mm j platelet <
ANC < 500 50,000 cells/mm3 l616
cells/mm3 j platelet < (2)
25,000 cells/mm3 l616

(2)
24 " (genotype 2 24 " (genotype 2 24 " (genotype 2

j 3)(2, 51) j 3)(2, 51) j 3)(2, 51)
%6%*l
48 " (genotype 1 48 " (genotype 1 48 " (genotype 1
HCV
j 4)(2, 51) j 4, HIV-HCV coinfected j 4)(2, 51)
a+22 genotype lu)(2, 51)
Absorption 80% absorption m SQ, IM site(2)
100 pg/mL(2) 20,000 pg/mL(2) 1,000 pg/mL(2)
Cmax
(steady-state conc.) (steady-state conc.) (steady-state conc.)
(2)
Excretion b5'o$e*
(2, 51)
t la## 2-5
gd+' 77-160
gd+'(2, 51) 40
gd+'(2, 51)
#'b a+2#'(2, 51)
(51) l
2(51) l
2(51)
ld4a# f#2l
64+%+%'
#'l

6
a+2#'(2) a+2#'(2) a+2#'(2)
*'5 HD
#'b
a+2#'(2) a+2#'(2) a+2#'(2)
ld4#
Pregnancy cat. C(2) C(2) C(2)
Neuropsychiatric effects (20-50%)
2 2&*$6, h+, #'*, a+2*,
, 4*1+4*g', 4 2##6 d6+ bo6l 3 jf 4# #+*2$o62'
l*
f*%lf#2 g f*%%+%'l
e& lni5$g+$%# l
&# , ni5$g+$
vw5'm #6i2 + f*%+l
lni5$g+$%5'm #1f'5$g6'441+a+2a(2, 51)
Influenza-like symptoms (50-98%)
2 ab g, $%, 2&*$6, *+jo
b + bo6l 6
gd+'*'|$6 f*%4'6i2 2-12
gd+', m& ml
NSAIDs &jg5(2, 51)
(2, 51)
GI side effects (20-65%)
2 4*jga m$6, jg, 5', 5'2'
ADRs (2, 51)
Myelosuppression (anemia, neutropenia, thrombocytopenia)
(51)
Injection site reactions
(2)
Proteinuria
(2)
njg, n+2' (m&t' 25%)
ADRs 5$g&a+226 af2 thyroid disorders (thyroiditis, hyperthyroidism, hypothyroidism),
LFT abnormalities, pulmonary disorders (a jg6), retinopathy, decreased or loss of
vision, diabetes mellitus, pancreatitis, psoriasis, SLE, myocardial infarction, colitis, serious
infections, severe rash (erythema multiforme, SJS, TEN)(2, 51)
l IFN 2+ cytotoxic drugs, pyrimethamine, 5-flucytosine, ganciclovir, zidovudine
Drug (2, 51)
& g+4+1f'b' myelosuppression
interaction (2)
l IFN 2+ phenobarbital, theophylline 5l%6*2$oi'bo

1506 424
2 2556 82
#$%& 36 Interferon alfa and thymosin alfa-1 (#2)
(Pegasys ) (Peg-Intron)
ni6 chronic hepatitis B 5$g+#'$#2 IFN alfa j pegIFN alfa af2 l HBeAg-
pretreatment ALT a+2i'+, baseline serum HBV DNA #g, +$*%5'&67 56b' positive chronic hepatitis B
h**"#a+21f'j+$a+2+, #
jo HBV genotype A j B(51) &2 *12 + 5$g a thymosin

l
3TC 2+ pegIFN alfa-2a (Pegasys ) l chronic hepatitis B +$ resistance rate alfa-1 +$ ni 65$g negative
#g2 3TC monotherapy (3TC resistance rate 5$g* 48 " 1-4% f*% 27-32% HBV DNA f*% ALT *
#+*)(51) e # i'2*12+5$g a
l
pegIFN alfa 2+ ribavirin l treatment-nave chronic hepatitis C +$ early IFN-alfa(53, 54)
% 57 &
virologic response rate 65-72%(51) l thymosin alfa-1
2 + pegIFN alfa +
ribavirin l chronic hepatitis
C 5$g*+*m pegIFN +
ribavirin +2 &2
+ t & g + sustained
virologic response a(55)
jo 6 lvmm16'a+2&jo IFN alfa, pegIFN alfa b' HBV(51)
Interferons e glycoprotein cytokine 5$g+$p57 c%#1i+ 41+ (immunomodulating Thymosin alfa-1 e

activity), p57 c#h**"+%' (antineoplastic activity), p57 c#a (antiviral activity)(2)
synthetic peptide 5$g+t
PegIFN alfa +$b$j conventional IFN alfa af2 t 62 ( 6"*%4o'),
% #1 T-lymphocyte
sustained virologic response rate i'2, +$n*a+2&'%'4"#g2 (jg'm+$f2'b'
differentiation and
%6l*j62)(2, 51) maturation, %#1 NK cell
+6#1
l
IFN j PegIFN monotherapy l chronic hepatitis C a +$b+l
ribavirin f#2 activity (immunomodulating
response rate m%#g2l
2+ ribavirin (combination therapy)(51) activity) f*%+$ p 57 c #
4# #+ CBC 2l
6 f*%%2'l
6 ("5$g 2 f*%mo51 6 "), thyroid h**" + % ' (antineoplastic
function tests (TFTs) 2l
6 f*%%2'l
6 (51 12 "), EKG 2l
6(2) activity), p57 c # a
(antiviral activity)(53)
Injections : 3 million Injections : 135 Injections : 50 mcg/vial, Injections : 1.6 mg/vial
if6f*% units/vial, 5 million units/vial mcg/syringe, 180 80 mcg/vial, 100 mcg/vial
4+f'5$g+$l Multidose pen : 18 mcg/syringe
%5a56 million units/pen, 30 million
units/pen
#$%& 37 Oral anti-HCV agents

Ribavirin Boceprevir Telaprevir

(Copegus , Rebetol ) (Victrelis ) (Incivek)
*12+6 Guanosine analogue(2) HCV NS3/4A protease inhibitors(2)
HCV (l
2+ IFN alfa j pegIFN HCV genotype 1-infected patients (l
2+ pegIFN alfa + ribavirin) 5o'l
b2'l

alfa), RSV(2, 3) treatment-nave patients f*%ni5$g*+*m IFN + ribavirin(2)
+jg l
2+ IFN alfa-2b (Intron- 800 mg PO q 8 hr x 24-32 " 750 mg PO q 8 hr x 12 "f
A) : 1,000 mg/day (< 75 kg) j (%5&+j2') (%5&+ fatty meal > 20 g of
bl
f*%
1,200 mg/day (> 75 kg) x 48 "(2, (2) fat)(2)
%6%*l 3, 51)
l treatment-nave patients f*% l treatment-nave patients f*%

+jg l
2 + pegIFN alfa-2a undetectable 5$g* 8 " m%l HCV-RNA undetectable 5$g* 4 f*%
(Pegasys) l HCV genotype 1 f*% boceprevir 24 "(2) 12 " m%l pegIFN alfa +

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#$%& 37 Oral anti-HCV agents (#2)
(Copegus, Rebetol) (Victrelis) (Incivek)
4 : 1,000 mg/day (< 75 kg) j 1,200 l treatment-experienced patients ribavirin #2$ 12 "(2)
mg/day (> 75 kg) x 48 "(2, 3, 51) (partial response j relapse) f*% l treatment-nave patients f*%
+jg l
2 + pegIFN alfa-2a undetectable 5$g* 8 " m%l HCV-RNA detectable < 1,000 IU/mL
(Pegasys) l HCV genotype 2 f*% boceprevir 32 "(2) 5$g* 4 f*%/j 12 " m%l
3 : 800 mg/day x 24 "(2, 51) l$ HCV-RNA detectable 5$g* pegIFN alfa + ribavirin #2$ 36
+jgl
2+ pegIFN alfa-2b (Peg- 8 ", < 100 IU/mL 5$g* 12 "(2)
bl
f*% Intron) : 800 mg/day (< 65 kg), 1,000 " , undetectable 5$g * 24 l treatment-experienced patients
%6%*l mg/day (66-85 kg), 1,200 mg/day (86- " m%l boceprevir 32 " (no response, partial response j
105 kg), 1,400 mg/day (> 105 kg) x #+6 pegIFN + ribavirn $ 12 relapse #2 pegIFN alfa + ribavirin) m%
48 "(2, 51) " (+ 48 ")(2) l pegIFN alfa + ribavirin #2$ 36
(51)
f2'l*% 2 4o' lni 6 cirrhosis 5$g+$ HCV-RNA "(2)
detectable 5$g* 8 ", < 100
IU/mL 5$g* 12 ", undetectable
5$g* 24 " m%l boceprevir 32
"(2)
Hb < 10 g/dL j**' > 2
ni 651 65$g+$ HCV-RNA > 100 ni65165$g+$ HCV-RNA > 1,000
g/dL l*e 600 mg/day(2)
b IU/mL 5$g* 12 " l616 IU/mL 5$g* 4 j 12 " l61
Hb < 8.5 g/dL l616 f*%
jg 'ma+2+$%d6
"(2) 6 jg'ma+2+$%d6
"(2)
ml erythropoetin(2)
64%(2, 3)
ih+& g+bo 237% +jg%5
Absorption (ih++bo+jg%5&+ 65%(2)
(2) &+ high fat meal(2)
high fat meal )
Cmax 5.1 mmol/L *'%5 600 mg(2) 1.7 mcg/mL(2) 3.51 mcg/mL(2)
Plasma protein
0%(2, 3) 75%(2) 59-76%(2)
binding
Vd 10 L/kg(3), 802 L(2) 772 L(2) 252 L(2)
#f2'5$g6 Plasma, respiratory tract secretion,
%m6aa$ red blood cells, CSF(2)
CSF
67%(2)
penetration
Excretion 40% (unchanged in urine)(3) 82% (in feces)(2)
0.5-2
gd+' (oral or IV),
t la## 3.4
gd+'(2) 9-11
gd+'(2)
40 (erythrocyte intracellular)(2)
t l ESRD a+2+$b+i*(3)
#'b
*$*$g6'+jg CrCl < 50(2, 3, 51) a+2#'(2) a+2#'(2)
ld4a#
#'l

6
*$*$g6'l
(2, 3)
*'5 HD
#'b (2, 3) (2) a+2#'(2)
a+2#' a+2#'
ld4# f*%*$*$g6'l moderate liver impair.
(2, 3, 51)
Pregnancy cat. X B(2)
Hemolytic anemia (+&7"b Myelosuppression : anemia (Hb < Myelosuppression : anemia ( g+
6 + bo 6l 2-4 " ) , 8.5 g/dL &a 6%), neutropenia (& bol 4 "f &a 36%),
ADRs
leukopenia(2, 3) a 25%), severe neutropenia (ANC < lymphopenia (< 500 cells/mm3 &a
(2)
af', dyspnea ($&26) 500 cells/mm3 &a 8%), 15%), thrombocytopenia (platelet <

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#$%& 37 Oral anti-HCV agents (#2)
(Copegus, Rebetol) (Victrelis) (Incivek)
GI side effects
2 4*jga m$6, thrombocytopenia (< 50,000 cells/mm3 50,000 cells/mm3 &a 3%)(2)
jg, 5'(2, 3) &a 3%)(2) GI side effects
2 4*jga m$6,
(2)
$%, 2&*$6, a+2* CNS side effects
2 $%, 5'2'(2)
(3, 51)
njg 4, ab (drug fever) 2&*$6, '1' , a+2*(2) njg (56%), 4 (37%)
(2)
ADRs (2, 3, 51)
Hyperuricemia, gout GI side effects
2 4*jga m$6, Anorectal discomfort, hemorrhoids,
(2, 3)
Hyperbilirubinemia n # (dysguesia), 5'2' rectal pruritus and buring(2)
(2) (2)
Severe rash
2 SJS, DRESS
(2)
njg, n+2', n f'
l ribavirin 2+ cytotoxic Boceprevir f*% telaprevir e CYP3A4 substrate f*% inhibitor, P-gp
drugs, pyrimethamine, 5-flucytosine, substrate 5l %65$ge CYP3A4 substrates i' bo +l
2+
ganciclovir, zidovudine, interferons alfuzosin, phenytoin, carbamazepine, phenobarbital, ergotamine, cisapride,
& g + 4 + 1 f ' b ' anemia simvastatin, lovastatin, drospirenone, high-dose sildenafil, tadalafil, midazolam,
Drug (myelosuppression)(2, 3, 51) triazolam(2)
interaction l ribavirin 2+ didanosine *$ *$g6 'l
boceprevir 2 + HIV protease inhibitors, NNRTIs,
(ddI) & g+ intracellular conc. b' maraviroc, raltegravir(2)
didanosine 5l lactic acidosis, *$*$g6'l
telaprevir 2+ darunavir/ritonavir, fosamprenavir/ritonavir,
pancreatitis, liver failure mt'bo lopinavir/ritonavir(2)
$6
$ # m'+6$ol
2+(2, 51)
RCT &2l peg-IFN + PROVE-1 study &2l
ribavirin 4 " (lead-in period) #+ telaprevir + peg-IFN + ribavirin 12
6 boceprevir + peg-IFN + ribavirin "f #+6 peg-IFN alfa-2a +
24 " l HCV genotype 1 mono- ribavirin 24-48 " l HCV
infected patients +$ sustained genotype 1 mono-infected treatment-
virological response (SVR) i'2*12+ nave patients +$ sustained virological
5$ga peg-IFN + ribavirin 44 " response (SVR) i'2*12+5$ga
(2)
peg-IFN alfa-2a + ribavirin 48 "
% 57 & RCT &2l peg-IFN + (2)
ribavirin 4 " (lead-in period) #+
6 boceprevir + peg-IFN + ribavirin
32 " l HCV genotype 1 mono-
infected patients 5$g suboptimal
response j relapse +$ sustained
virological response (SVR) i'2*12+
5$g retreatment 6 peg-IFN + ribavirin
44 "(2)
jo6 +$ cross resistance %2'6l*1+2 HCV NS3/4A protease inhibitors(2)
w '6m w&71" f*%
65$g+$4i2
ew '+$4" #'41+ 62'6
+6#1 2 7$l%2'5$gl
ribavirin f*%#2a
$ 62 ' 6 6 j * ' 61 6
(jg'm6%+l2'6)(2, 51)
if6f*% Tablets : 200 mg a+2+$m26l%5a56 a+2+$m26l%5a56
4+f'5$g+$l Capsules : 200 mg
%5a56

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Antivirals active against influenza viruses
#$%& 38 Antivirals active against influenza viruses

Oseltamivir Zanamivir
Amantadine Rimantadine
(Tamiflu, GPO-A-Flu) (Relenza)
*12+6 M2 inhibitors(2) M2 inhibitors(2) Neuraminidase inhibitors(2) Neuraminidase inhibitors(2)
Spectrum of
Influenza A virus(2, 3) Influenza A virus, influenza B virus(2)
activity
b2'l
'f*% influenza A(2) 'f*% influenza A, influenza B, avian influenza(2)
b : 100 mg PO b : 100 mg PO b (nilw2) : 75 b (nilw2) : 2.5
q 12 hr(2) j 200 mg PO q 12 hr 6l 48
gd+' mg PO q 12 hr 6l 48 mg inhalations q 12 hr
q 24 hr(3) 6l 48
gd+' f5$gf' 7
gd+'f5$gf' 6l 48
g d+'f5$g
f5$gf' 5 (2) (4*b*'l 5 (2) f' 5 (2)
(2)
nii'61, ni6d4a#, ni6 b' (nilw2) : 75 b' (nilw2) : 5
(2, 3)
b ' : 100 mg d4#1f' ) mg PO q 24 hr *'+n mg inhalations q 24 hr
PO q 12 hr *'+n
jo x b' : 100 mg
jo x 7 (2) (% 57 & 84%)(2)
10 (2) PO q 12 hr(2, 3) b ( > 1 ) :
bl
< 15 kg l 30 mg q 12 hr,
15-23 kg l 45 mg q 12 hr,
23-40 kg l 60 mg q 12 hr,
> 40 kg l 75 mg q 12 hr
6l 48
gd+'f5$gf'
5 (2)
b ( > 1 ) :
52b f#2l q 24
hr(2)
Absorption 90%(3) 90-96%(2, 3) 75%(2) 4-17%(2)
17-142 ng/mL *'l 10
0.3 mcg/mL *'%5 0.25 mcg/mL (plasma), 348 mcg (active drug) *'
Cmax mg inhalation af* 1-2
2.5 mg/kg(2) 0.42 mcg/mL (mucus)(2) %5 75 mg q 12 hr(2)

gd+'(2)
Plasma protein
60-67%(2, 3) 40%(2, 3) 42%(2) < 10%(2)
binding
Vd 6.6 L/kg(3) 4.5 L/kg(3) 23-26 L(2)
#f2'5$g6 Saliva, nasal secretion,
Respiratory secretions(2) (2)
%m6aa$ lung tissues(2)
CSF 15% (non-inflamed),
a+2+$b+i*(3)
penetration 20% (inflamed)(3)
Urine excretion 90% (unchanged)(3) < 1% (unchanged)(2) > 80% ( active metabolite)(2)
t la## 16-24
gd+'(2, 3) 6-9
gd+'(2) 6-10
gd+'(2) 2.5-5.1
gd+'(2)
t l ESRD 192
gd+'(3) 38
gd+'(3)
#'b l
2(2, 3)
l
2(2, 3) l
2(2) a+2#'(2)
ld4a# +jg CrCl < 10
#'l

6
a+2#'(2) a+2#'(2, 3) l
2(2) a+2#'(2)
*'5 HD
l
2(2, 3) l
2(2)
#'b (2)
l
2 |&% severe hepatic +jg moderate hepatic a+2#'(2)
ld4#
impairment impairment

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#$%& 38 Antivirals active against influenza viruses (#2)
Oseltamivir Zanamivir
Amantadine Rimantadine
(Tamiflu, GPO-A-Flu) (Relenza)
Pregnancy cat. C(2, 3) C(2, 3) C(2) B(2)
Allergic
#g(3) #g(3)
potential
CNS side effects
2 $%, '$6, a+2*, GI side effects (&a 10- a , bronchospasm
, b+7 , &i a+2
(dysarthria), g , h, 20%)
2 4*jg a m$ 6 , d6|&%lni6 COPD,
#*j4', *'n , visual hallucination, psychosis,
5'2' +$bo+jgl
asthma(2)
d6|&%lnii'61, ni5$g+$5'b'a#&2', ni5$g+$ 6#2 a f*%%5 GI side effects
2
%# d4*+
(2, 3) 6*'
26a(2) 4*jga m$6, 5'2'(2)
Anticholinergic effects (#&2 , f ' 4f ' , CNS side effects
2 CNS side effects
2
ADRs
orthostatic hypotension, 5'ni, v%4g')(2, 3) a+2 * , , & , $%, '$6, &(2)
(2, 3) (2)
Livedo reticularis *'n , 4 2 # #6,
, LFT abnormalities
(2)
GI side effects
2 4*jga m$6 h+*', +# (2)
Cardiovascular effects : acute exacerbation of heart njg, erythema multiforme,
failure, cardiac arrhythmia, QTc prolongation(2, 3) SJS(2)
(2)
njg, eczematoid dermatitis, photosensitivity
(3)
l
2+ alcohol & g+ CNS side effects l
2+ probenecid
l
2+ anticholinergic agents (
2 benztropine, 5l%6 oseltamivir
benzhexol, TCAs, H1-antihistamines) & g + & g+bo 2.5 52(2)
Drug anticholinergic effects(2, 3)
(3)
interaction l
2+ CNS stimulants & g+ CNS stimulation
(3)
l
2+ digoxin 5l%6 digoxin i'bo
l
2+ probenecid, triamterene, trimethoprim
5l%6 amantadine i'bo (*m65'a#)(2)
m6'|*21b' WHO (1+&7" 2553) &
vmm1&jo6*12+$bo ' pandemic (H1N1) 2009, jo6 oseltamivir b' pandemic influenza A (H1N1) 2009
jo6 (2)
seasonal influenza A (H3N2), influenza B i' virus lni6 245 6 d6516+$*6&71"5$g#f2'
H275Y hg'6'a#26 zanamivir(2)
p57 c66o' ion channel function of M2 protein b' p57 c66o' neuraminidase b' influenza virus 2'n*
influenza A 2'n*la+2 viral uncoating(2) #2 virus particle aggregation and release(2)
vmm1a+2f%ll
f* jg 'm&1# " jo
+6#1
6i'(2)
Rimantadine +$ anticholinergic effects #g 2
(2, 3)
amantadine
if6f*% a+2 +$ m 2 6l%5 a+2 +$ m 2 6l%5 Capsules : 30 mg, 45 mg, Inhaler : 5 mg/dose
4+f'5$g+$l a56 a56 75 mg rotadisk (l
2 +
%5a56 Suspension : 12 mg/mL Diskhaler)
Antiretrovirals
i#6#a5$+g $% 57 &i' (highly active antiretroviral therapy, HAART) %6 NRTIs 2
(NRTI
backbone) 2+6#al*12+jg$ 1
(NNRTIs, protesase inhibitors, integrase inhibitors)(56, 57)
i#6#a5$g DHHS guideline 2013 ( + ) f*%f5'#m m |6f*%if*ni#
jo
a$f*%ni6" %
# &.. 2553 (%5a56) f%e'$o

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cPN$M#NoN_P_opHcUgM`jcUMlijO#_Ì]ZaT
DHSS guideline 2013
IT]QTN%cUgijOfkNHIT`q g`]#_ fr s.t. 2553
Preferred regimens
2
+ EFV 6 + EFV2
AZT + 3TC
TDF + 3TC/FTC1 + Boosted PIs (ATV/rtv, DRV/rtv) + NVP7
TDF + 3TC/FTC1
+ Raltegravir + LPV/rtv
Alternative regimens
3
+ Rilpivirine
1 AZT + 3TC6 + Boosted PIs (ATV/rtv, DRV/rtv,
TDF + 3TC/FTC + Boosted PIs (fosAPV/rtv, LPV/rtv) 1
TDF + 3TC/FTC SQV/rtv)
+ Elvitegravir/cobicistat4
+ EFV
+ EFV
+ Rilpivirine d4T + 3TC8
+ NVP9
ABC + 3TC/FTC5 + Boosted PIs (ATV/rtv, DRV/rtv, ddI + 3TC
+ Boosted PIs (LPV/rtv, ATV/rtv,
fosAPV/rtv, LPV/rtv) ABC + 3TC5
DRV/rtv, SQV/rtv)
+ Raltegravir
FGHIF#J 1TDF/FTC
jg4 Truvada, 2TDF/FTC/EFV
jg4 Atripla, 3TDF/FTC/RPV
jg4 Complera,
4
TDF/FTC/ELV/COBI
jg4 Stribild, 5ABC/3TC
jg4 Epzicom, Kivexa, 6AZT/3TC
jg4 Combivir, Zilavir,
7
AZT/3TC/NVP
jg4 GPO-VirZ250, 8d4T/3TC
jg4 Lastavir, 9d4T/3TC/NVP
jg4 GPO-VirS30
#$%& 39-1 Nucleos(t)ide reverse transcriptase inhibitors (NRTIs)

Zidovudine (AZT) Stavudine (d4T) Lamivudine (3TC) Emtricitabine (FTC)
*12+626 Thymidine analogue Thymidine analogue Cytosine analogue Cytosine analogue
651#l*12+ NRTIs e prodrug hg'm%#'ti# ++i2#6lh**" (celluar phosphorylation) le triphosphate
*ap57 c form m'm%p57 ca (active) d6tia' proviral DNA lbo# reverse transcription 5l chain termination
f*%6'm reverse transcriptase ffb2'b6(56, 57)
< 60 kg: 30 mg PO q 12 hr
< 50 kg: 2 mg/kg PO q 12 200 mg (tablets/
> 60 kg: 40 mg PO q 12 hr (21)
200 mg PO q 8 hr, hr capsules) PO q 24 hr(21)
bl
(t o > 60 kg a+2 +
250-300 mg PO q 12 hr(21) > 50 kg: 150 mg PO q 12 240 mg (syrup) PO q 24
ml 30 mg PO q 12 hr
hr, 300 mg PO q 24 hr(21) hr(21)
a&jg* ADRs)(21)
(21) (21) (21) (21)
F 60% F 78-86% F 82-86% F 93%
(21) (21) (21) (21)
Serum t 1.1
g d+' Serum t 1
g d+' Serum t 3-6
g d+' Serum t 8-10
g d+'
Intracellular t 7
gd+' Intracellular t 4-7.5 Intracellular t 18-22 Intracellular t 39
gd+'
(21)

g d+'(21)
g d+'(21) (21)
(21) (21) (21)

m*#" n2 BBB a$ n2 BBB a$ n2 BBB a$ m6 : b5'
m6 : zidovudine m6 : b5' m6 : b5' a # e * ( unchanged)
glucuronide tib5' a # % + 50% a # % + 70-79% (#'b#+ CrCl)(21)
a # (# ' b # + (unchanged) (#'b (unchanged) (#'b
CrCl)(21) #+ CrCl)(21) #+ CrCl)(21)
a 2 + 65$g l
2 +
5'b'ab%i
2 cotrimoxazole m5l
cytotoxic drugs, cidofovir, %6 3TC i'bo(21)
ganciclovir, valganciclovir,
Drug interaction
interferons, cotrimoxazole,
pyrimethamine & g+4+
1 f ' b ' anemia,
neutropenia(21)

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#$%& 39-1 Nucleos(t)ide reverse transcriptase inhibitors (NRTIs) (#2)
Zidovudine (AZT) Stavudine (d4T) Lamivudine (3TC) Emtricitabine (FTC)
Class effects 4j mitochondrial toxicity jg'm NRTIs +t66o' DNA polymerase-gamma hg'eah+"4w
l'4%" mitochondrial DNA 2'n*l mitochondrial dysfunction lactic acidosis with hepatic steatosis d6
$6'* NRTIs 5$g5l mitochondrial toxicity m+a6 '$o ddC > d4T + ddI > d4T > ddI > AZT > 3TC,
FTC, ABC, TDF(21)
Specific ADRs : Specific ADRs : ni 6 + 5 6 a $ , Specific ADRs :
myelosuppression (anemia, lipoatrophy (+&+jgl
6 ADRs 5$g & a ' af 2 hyperpigmentation 5$g+j
neutropenia, asymptomatic > 6 j ), peripheral $ %, a+2 * , 5 (&a 3% l
2' 3
ADRs
macrocytosis), myalgia, neuropathy (& 10-30% 4*jg a, 5 ', 5 '2 ' jf5$gl
6), njg(21)
myopathy, skin and nail d6|&%lni6, (21) ADRs jgu : 4*jga,
(21)
hyperpigmentation a 2 + neurotoxic 5'2', $%(21)
ADRs jgu : GI side drugs), hypertriglyceridemia
effects, flu-like symptoms (21)
($%, 2&*$6, ADRs jgu : GI side
a+2*)(21) effects, elevated LFTs(21)
+$p57 cl activated T- +$p57 cl activated T- +$ p 57 c l resting +$ p 57 c l resting
lymphocytes(21) lymphocytes(21) macrophages(21) macrophages(21)
a+2l
2+ d4T &% a+2l
2+ AZT &% +$p57 c#2 HBV f*% HIV +$p57 c#2 HBV f*% HIV
e thymidine analogue e thymidine analogue m ' f % l
l HIV-HBV m ' f % l
l HIV-HBV
+j hg ' m % +j hg ' m % coinfected patients coinfected patients
+6#1
antagonism f*% cross antagonism f*% cross a+2l
2+ FTC &% a+2l
2+ 3TC &%
resistance resistance e cytosine analogue e cytosine analogue
+j hg ' m % +j hg ' m %
antagonism f*% cross antagonism f*% cross
resistance resistance
Capsules : 100 mg, 250 Capsules : 15 mg, 20 Tablets : 150 mg, 300 Capsules : 200 mg
mg, 300 mg (Antivir, mg, 30 mg, 40 mg (Stavir) mg (Epivir, Lamivir) Syrup : 10 mg/mL

Retrovir ) Syrup : 1 mg/mL Syrup : 10 mg/mL FDC tablets : TDF/FTC

Syrup : 10 mg/mL (Stavir ) (Lamivir) (Truvada), TDF/FTC/EFV
if6f*% (Antivir)
FDC tablets : d4T/3TC FDC tablets : AZT/3TC, (Atripla ), TDF/FTC/RPV

4+f' Fixed dose combination (Lastavir ), d4T/3TC/NVP AZT/3TC/NVP, d4T/3TC, (Complera ), TDF/FTC/

(FDC) tablets : AZT/3TC (GPO-VirS30 ) d4T/3TC/NVP, ABC/3TC ELV/COBI (Stribild)
(Combid 300, Zilavir),
AZT/3TC/NVP (GPO-

VirZ250 )
#$%& 39-2 Nucleos(t)ide reverse transcriptase inhibitors (NRTIs)

Tenofovir disoproxil fumarate
Didanosine (ddI) Abacavir (ABC)
(TDF)
Acyclic nucleotide analogue of
*12+626 Adenosine analogue Adenosine analogue
adenosine
< 60 kg: 125 mg PO q 12 hr(21) 300 mg PO q 12 hr,
bl
300 mg PO q 24 hr(21)
> 60 kg: 200 mg PO q 12 hr(21) 600 mg PO q 24 hr(21)
(21)
F 40% (ih+6 F 83% F 40% (
26& g+ih+6

m*#" m'#'%5#5'2')(21) Serum t 1.5
g d+' 4%5&+)(21)
(21) (21)
Serum t 1.6
g d+' Intracellular t 12-26
g d+' Serum t 10-17
g d+'

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#$%& 39-2 Nucleos(t)ide reverse transcriptase inhibitors (NRTIs) (#2)
Tenofovir disoproxil fumarate
Didanosine (ddI) Abacavir (ABC)
(TDF)
(21) (21) (21)
Intracellular t 12-20
g d+' (carbovir triphosphate) Intracellular t > 60
g d+'
(21)
m 6 : b 5'a# n2 BBB a$ m6 : b5'a#e*
%+ 50% (# ' b#+ m6 : ti*$g6f*'d6 (glomerular filtration f*% tubular

m*#" CrCl)(21) alcohol dehydrogenase #+ 6 secretion) (#'b#+ CrCl)(21)
glucuronyl transferase, 11-13%
(unchanged) b5'a# (a+2# '
b#+ CrCl)(21)
l ddI buffered tablets/ powder +$ a ABC 2+ alcohol a ddI 2+ TDF 5l
magnesium-based antacids hg' 5l ABC ti m
*' % 6 %6 ddI i'bo 44-60% mm
chelation FQs, tetracyclines, * i ' bo 41% (jg 'mfb2 ' b l
& m6 m'4*b ddI e 200
ih+b'65$g#'6% ah+" alcohol dehydrogenase)(21) mg/day (< 60 kg) j 250 mg/day (>
l i h + ( ketoconazole, 60 kg)(21)
itraconazole, RPV, ATV, IDV, a TDF 2+ ATV 5
Drug interaction
RTV)(21) l%6 ATV **' 'om%l

a ddI 2+ TDF 5l 2+m%#'l
boosted ATV +
%6 ddI i'bo 44-60% mm
& m6 m'4*b ddI e 200
mg/day (< 60 kg) j 250 mg/day (>
60 kg)(21)
Class effects 4j mitochondrial toxicity (i#'5$g 39-1)
Specific ADRs : peripheral Specific ADRs : hypersensitivity Specific ADRs : nephrotoxicity
neuropathy (&a 13-35% d6|&% reactions hg ' m1 f'
2 SJS, (renal tubular dysfunction, proteinuria,
l ni 6 , a 2 + TEN, DRESS lni6'#ab Fanconi syndrome) 4# #+
neurotoxic drugs
2 d4T, INH), njg fn*l 6jg1# urinalysis f*% sCr 2f*%%2'l

pancreatitis (&a 5-7% d6|&%l 5'%6lm +jg '*2 6 &2 CrCl **'lb
ni 5$g +$ % # # 2 j a# l 61 l
6 5 5$ f * &f&56" f*% 6(21)
ADRs
5'&2', a2+ alcohol, +*+l
6$(21) ADRs jgu : GI side effects,
IV pentamidine # '+$ # #+ ABC hypersensitivity syndrome $%(21)
serum amylase e%6%), 5'2' + & 7" 6$ HLA-B*5701
( m magnesium-based antacids haplotypes (l#2 '%5+$
li##)(21) #m6$$o2l6 ABC)
ADRs jgu : GI side effects,
2&*$6, jg(21)
(21) (21)
+$p57 cl resting macrophages +$ cross resistance ddI, 3TC +$p57 c#2 HBV f*% HIV m'f%l

Enteric-coated capsules +$b$2 l HIV-HBV coinfected patients
+6#1 buffered ddI tablets/ powder 4j l6 6'4'+$% 57 &l HIV 5$gjo#2
(21)
*%4o'a, 5l 5'2'62 NRTIs jg
(21)

Chewable buffered tablets : 25 mg, Tablets : 300 mg (Ziagenavir ) Tablets : 300 mg (Viread)
125 mg, 200 mg (Divir) Syrup : 20 mg/mL FDC tablets : TDF/FTC

Buffered powder : 30 mg, 60 mg, FDC tablets : ABC/3TC (Epzicom , (Truvada), TDF/FTC/EFV (Atripla),
if6f*%
115 mg, 167 mg, 170 mg, 230 mg, Kivexa) TDF/FTC/RPV (Complera),
4+f'
285 mg per sachet (Divir) TDF/FTC/ ELV/COBI (Stribild)
Enteric-coated cap : 125 mg, 200
mg, 250 mg, 400 mg (Videx EC)

1506 424
2 2556 90
#$%& 40-1 Non-nucleoside reverse transcriptase inhibitors (NNRTIs) 125$g 1
Nevirapine (NVP) Efavirenz (EFV) Delavirdine (DLV)
st (21) st (21)
*12+626 1 generation NNRTIs 1 generation NNRTIs 1 generation NNRTIs(21)
st
6l*12+ NNRTIs +$d4''4+$f##2' f#2m5$g hydrophobic pocket $6 reverse transcriptase b' HIV-1
*ap57 c fa+2fb2'b (noncompetitively binding) 5l active site b'ah+"*$g6f*'a (conformation change) a+2+%+
'4%" DNA(56, 57)
+$% 57 &$a+2#2'm protease inhibitors (PIs) f#2+$b$2 PIs lf'25$gn2 BBB a,$ metabolic side effects 62
% 57 &
f#2 1st generation NNRTIs +$b6 4j genetic barrier #g (jo6a f++$*6&71"b'6$&$6'#f2'$6)
200 mg PO q 24 hr l 14 f 600 mg PO q 24 hr(21)
bl
(lead-in period) mom'lb# (%562 &jg*$*$g6' 400 mg PO q 8 hr(21)
200 mg PO q 12 hr(21) CNS side effects)
(21) (21)
F 90-93% F 42% f#2m%ih+a+bo+jg F 85%
(21) (21)
Serum t 25-30
gd+' (l
%6% %5&+ high fat meal Serum t 5.8
g d+'
6), 45
gd+' (
2' 14 f)(21) Serum t 40-55
g d+'
(21)
n2 BBB a62 NVP
(21)
n2 BBB a$ m6 : ti*$g6f*'d6 m6 : ti *$g6f*'d6

m*#" m6 : ti*$g6f*'d6 CYP3A4 e * mo inactive CYP3A4 e * mo inactive
CYP3A4 e * mo inactive metabolites m%tib5'a# 14- metabolites m%tib5'a# 51%
metabolites m%tib5'a# 80% 34% f*%5'1mm% 16-61%(21) (+$ < 5% 5$g b 5'a#li a+2
(+$ < 5% 5$g b 5'a#li a+2 *$g6f*')(21)
*$g6f*')(21)
NVP e CYP3A4 substrate f*% EFV e CYP3A4 substrate f*% DLV e CYP3A4 substrate f*%
inducer m ' # '% ' l
2 + inducer m'#'%'l
2+6jg inhibitor (#2 'm NVP hg ' e
CYP3A4 inhibitors (azole antifungals, +j NVP(21) CYP3A4 inducer)(21)
protease inhibitors), CYP3A4 *$*$g6'%5 EFV &+ *$ *$g 6 ' %5 DLV
Drug interaction
inducers (rifampicin, antiepileptics), high fat meal &%m%5l Cmax i' 2 + anticids j buffered ddI
CYP3A4 substrates (oral +m CNS side effects(21) (#'l62')(21)
contraceptives, statins, ergot
(21)
alkaloids, midazolam, triazolam)
Specific ADRs : njg (diffuse MP Specific ADRs : CNS side effects Specific ADRs : njg (DLV <
rash amt' SJS, TEN) d6 NVP 5 ($ %, '$6 , '2'h+, a+2 NVP)(21)
l njga+5$g1l NNRTIs * , b+7 , , v 6, ADRs jgu : $%, elevated
(&a 30-50%), elevated LFTs, %5*, 5'm # ) LFTs(21)
ADRs
hepatitis m1f't'bo$6
$ # + *2 $o + $ bo *' l
6 af* 2-4
&l&w ', ni5$g+$ CD4 i'(21) ", njg (EFV < DLV < NVP),
elevated LFTs(21)
(21)
ADRs jgu : GI side effects
jo6 +jg jo6 1st generation NNRTIs #l#g' m% job+51#(21)
Lead-in period (14 f) 4l e NNRTI &$6'#$65$g DHHS a+2 f % l l
e 6fl initial
NVP lb4g'g' &jga+2l+$% guideline 2013 f%e preferred regimen jg'mb+i*% 57 &
6 l *j i ' a & % 6 ' +$ regimen(21) 5'4* +$6f*%a+2
m
(21)
autoinduction a+2#+5$g +l
EFV lw ' #o ' 4"
+l
NVP lni6w '5$+ g $ CD4 > (pregnancy category D) jg'm+$
3
+6#1 250 cells/mm jni6
65$g+$ CD4 6'2 5 l 5 i
2
> 400 cells/mm3 jg'm+$d meningomyelocele(21)
severe hepatitis m NVP ai'(21)
l NVP d$6b%4*1#
+t*f&2
jo m+i2
5f a(21)

1506 424
2 2556 91
#$%& 40-1 Non-nucleoside reverse transcriptase inhibitors (NNRTIs) 125$g 1 (#2)
Nevirapine (NVP) Efavirenz (EFV) Delavirdine (DLV)

Tablets : 200 mg (Neravir ) Capsules/ tablets : 50 mg, 200 Tablets 100 mg, 200 mg

Syrup : 10 mg/mL (Neravir ) mg, 600 mg (Stocrin)
if6f*%
FDC tablets : AZT/3TC/NVP (GPO- FDC tablets : TDF/FTC/EFV
4+f'
VirZ250), d4T/3TC/NVP (GPO- (Atripla)
VirS30)
#$%& 40-2 Non-nucleoside reverse transcriptase inhibitors (NNRTIs) 125$g 2

Etravirine (ETV) Rilpivirine (RPV)
nd (21)
*12+626 2 generation NNRTIs 2 generation NNRTIs(21)
nd
200 mg PO q 12 hr(21) 25 mg PO q 24 hr(21)

bl

(4%5&+&jg& g+ih+6) (4%5&+&jg& g+ih+6)
(21)
Serum t 20-60
g d+' #'64+el%&%lih+6

m*#" m 6 : ti *$g 6f*'d6 CYP3A4, 2C9, (pH-dependent absorption)(21)
2C19(21) m6 : ti*$g6f*'d6 CYP3A4 e*
(21)
ETV e CYP3A4 inducer f*%e CYP2C9, 2C19 RPV e CYP3A4 substrate m'#'%'l
2+
inhibitors(21) CYP3A4 inhibitors, CYP3A4 inducers(21)
Drug interaction l RPV 2+65$g5l gastric pH i'bo (
2
PPIs, H2RAs, antacids, buffered didanosine) m%5l6ti
ih+a6*'(21)
(21)
Specific ADRs : njg, njg1f'
2 SJS Specific ADRs : njg, CNS side effects ($%,
ADRs ADRs jgu : 4*jga m$6, $%, peripheral a+2*, h+, *'n ), lipodystrophy, QTc prolongation
neuropathy(21) (+&7"b6)(21)
6l*12+ 2nd generation NNRTIs 6'4'+$p57 c# 1st generation NNRTI-resistant strains 2lw2 jg'm+$*6
jo6
&71"b'6$4*%#f2'(21)
nd
a'll
l treatment-experienced patients e 2 generation NNRTI 5$g DHHS guideline 2013
+6#1 52o &%vmm16'+$a+2+&l treatment- f%l alternative regimen treatment-nave
nave patients patients(21)
if6f*%
Tablets : 100 mg (Intelence ) Tablets : 25 mg (Endurant )
4+f'
#$%& 41-1 Protease inhibitors (PIs)

Saquinavir (SQV) Ritonavir (RTV) Indinavir (IDV)
PIs p57 c66o' viral protease hg'eah+"5$gmel#626 HIV polyproteins le subunits #2'u 5$gm%a
%e mature virions(56, 57)
Boosted PI 4j l
protease inhibitor 2+ low-dose ritonavir (100-200 mg/day) &jg& g+ bioavailability f*%
*ap57 c
serum concentration b' protease inhibitor hg'
26* ++65$g#'%5 (* pill burden), *4+t$gl
%56, *4+me5$gm%#'%52j*', *d jo6 f*%
% drug interaction
CYP450 inducer '
a6(56, 57)
(21) (21)
Boosted : 1000 mg/100-200 mg rtv Full dose : 600 mg PO q 12 hr Unboosted : 800 mg PO q 8 hr
(21)
PO q 12 hr (l
2'fl 300 mg PO q 12 hr x 2 Boosted : 800 mg/100-200 mg rtv
mo 400 mg PO q 12 hr x 3 PO q 12 hr(21)
bl

f*% 500 mg PO q 12 hr x 8 )
Boosting dose : 100-400 mg/day
f2'l*% 1-2 4o'(21)

1506 424
2 2556 92
#$%& 41-1 Protease inhibitors (PIs) (#2)
Saquinavir (SQV) Ritonavir (RTV) Indinavir (IDV)
F 4% (4%5&+ F 65-75% (4%5& + F 65% (4%52 1
j 6l 2
gd+'*')(21) )(21)
gd+' j*' 2
gd+', m
(21) (21)
Serum t 1-2
g d+' Serum t 3-5
g d+' %5& ++jo u 5$g +$
m 6 : ti*$g6 f*'d6 m 6 : ti*$g6 f*'d6 ab+#gf*%d#$#g)(21)

m*#" CYP3A4 e* CYP3A4 > 2D6 > 2C9/10(21) Serum t 1.5-2
g d+'
(21)
n2 BBB a42b'$

m6 : ti*$g6f*'d6
CYP3A4 e*, b5'a# 20%
lia+2*$g6f*'(21)
SQV e CYP3A4 substrate f*% RTV e most potent CYP3A4 IDV e moderate CYP3A4
least potent CYP3A4 inhibitor(21) m' inhibitor, potent CYP2D6 inhibitor(21) inhibitor(21)
# ' % ' l
2 + CYP3A4 m'#'%'l
2+6jg+j l IDV 2+ antacids, ddI
inhibitors (azole antifungals, SQV buffered tablets/ powder (+$
grapefruit juice), CYP3A4 inducers RTV e glucuronosyl transferase magnesium-based antacids) *
(rifampicin, NVP, EFV, antiepiletics), inducer 5l% 5 7 &b' oral ih+b' IDV hg'#'6%
Drug interaction CYP3A4 substrates (cisapride, ergot contraceptives, thyroxine, lih+(21)
alkaloids, simvastatin, lovastatin, theophylline **' +jgl
2+(21) l IDV 2+ ATV 2' +
midazolam, triazolam) l RTV 2+ antacids, ddI l indirect
buffered tablets/ powder (+$ hyperbilirubinemia 4*$*$g6'l

magnesium-based antacids) * 2+(21)
ih+b' RTV hg'#'6%
lih+(21)
Class effects af2
Insulin resistance, type 2 DM (8-10% d6|&%lni6, +$%# d4l44, nii'61 &al PIs
51
f#2 ATV, SQV &65$g1)(21)
Dyslipidemia (40-70% m& hypercholesterolemia, triglyceridemia &al PIs 51
d6|&% LPV f#2 ATV
&65$g1)(21)
(21)
Lipodystrophy (& 10-84% m+$*'&1', gynecomastia, buffalo hump, ab+%+l
2'5')
Lipoatrophy and peripheral wasting (f+#, fbb*$, f d6vmm6$g6' af2 o#6, nii'61,
advanced AIDS)
Osteopenia/ osteoporosis (vmm6$g6' af2 a long-term corticosteroids, chronic alcoholism, IV drug user, l

ADRs testosterone, advanced AIDS)(21)

Hepatotoxicity (asymptomatic transaminase elevation, jaundice d6vmm6$g6' af2 HIV-HBV coinfection, HIV-HCV
coinfection, alcoholism, +$5'b'#f626i22)(21)

Spontaneous bleeding lni6 hemophilia
ADRs jgu : GI side effects Specific ADRs :

(&a Specific ADRs : g la#
(4*jg a m$6 , 5 ', 5'2 '), 25%),
*6+j*65 (&a 5- (nephrolithiasis) (&a 4-8%, m
$%(21) 6%), n # (dysguesia)(21) #6#n*l52a# 'ad6l
ADRs jgu : GI side effects ni6jg+o > 1.5-2 L/day), indirect
(4*jg a m$6 , 5 ', 5'2 '), hyperbilirubinemia(21)
2f'(21) ADRs jgu : GI S/E, $%
(21)
Soft-gelatin cap : 200 mg Soft-gelatin capsules : 100 mg Capsules : 200 mg, 400 mg
(Fortovase) (Norvir) (# 'f
2#i6 , t (Inavir, Crixivan)
if6f*%
Capsules : 200 mg (Invirase ) #i66i2a 1 j)
4+f'
Tablets : 400 mg (Saquivir ), 500 Syrup : 80 mg/mL (Rinavir )
mg (Invirase)

1506 424
2 2556 93
Nelfinavir (NFV) Fosamprenavir (fosAPV) Lopinavir (LPV)
Unboosted : 750 mg PO q 8 hr Boosted : 700 mg/100 mg rtv PO q Boosted : 400 mg/100 mg rtv PO q
j 1,250 mg PO q 12 hr(21) (a+2#' 12 hr j 1,400 mg/200 mg rtv PO q 12 hr (Kaletra 2 tab q 12 hr j
bl
lf boosted &% low-dose RTV 24 hr(21) Aluvia 4 tab q 12 hr)
+$%d6
"l& g+% NFV 6) 800 mg/200 mg rtv PO q 24 hr (a
|&%l treatment-nave patients)
F 20-80% (4%5& + %52j *'a Tablets %52 j * '
jb+)(21) (21)
a, syrup #'%5&+
(21) (21)
Serum t 3.5-5
g d+' Tmax of APV l 1.5-4
g d+' (21)

m*#" (21) (21)
m 6 : ti*$g6 f*'d6 Serum t 7-11
g d+' Serum t 4-6
g d+'
(21)
CYP3A4, CYP2C9 e* m 6: ti *$g6 f*'d6 m 6: ti *$g 6 f*'d6
CYP3A4 e*(21) CYP3A4 e*(21)
NFV e moderate CYP3A4 fosAPV e moderate CYP3A4 LPV e moderate CYP3A4
inhibitor(21) inhibitor(21) inhibitor, CYP2D6 inhibitor(21)
l
LPV/rtv 2+ EFV, NVP
Drug interaction
hg'e CYP3A4 inducer %6
LPV **'62'+$6 4w #'& g+
be 800/200 mg rtv PO q 12 hr
Class effects af2 insulin resistance, type 2 DM, dyslipidemia, lipodystrophy, lipoatrophy and peripheral wasting,
osteopenia/ osteoporosis, hepatotoxicity, spontaneous bleeding in hemophilia(21) (i#'5$g 41-1)
ADRs jgu : moderate to severe Specific ADRs : njg , Specific ADRs : severe
diarrhea (&a 15-32%, 6 hypersensitivity reactions (+$6' hypertriglyceridemia ( a#o'f#2j
ADRs l antidiarrheal agents j SJS j 1% jg'mld4''6 f 5$g l
6 ), pancreatitis
(21)
calcium carbonate), 4*jga m$6 +$ sulfonamide moiety 6i2),
( % f 5 h m severe
, elevated LFTs(21) hypertriglyceridemia)(21)
(21)
ADRs jgu : GI side effects ADRs jgu : GI side effects,
2&*$6, 2f'(21)
NFV-containing regimens +$ fosAPV e prodrug b' e PI 5$gf5'if*ni#
% 5 7 & 6 2 LPV/rtv- amprenavir (APV) hg'm%tiih+a$
jo
a$ &.. 2553 (a56) f%
containing regimens l treatment- bo e* pill burden(21) e preferred regimen ($5$g l

nave patients NNRTIs a+2a)
viral load at' 4 l
+6#1
treatment-nave patients
6 ' 4'a n *$ l ni 65$g 46* + *
ml
PI-containing regimen + 1
i# (LPV e 2nd generation PI hg'+$
genetic barrier i'2 1st gen. PIs)
Tablets : 250 mg, 625 mg Tablets : 700 mg Soft-gelatin capsules :

(Viracept ) Syrup : 50 mg/mL 133.33/33.33 mg rtv (Kaletra) (#'
Powder : 50 mg/g f
2#i6)

Tablets : 100/25 mg rtv (Aluvia ),
if6f*% 133.33/33.33 mg rtv

4+f' (Lopinavir/ritonavir GPO ), 200 mg/50
mg rtv (Kaletra)
Syrup : 80 mg/20 mg rtv per mL
(Kaletra) (#'f
2#i6, t
#i66i2a 2 j)

1506 424
2 2556 94
Atazanavir (ATV) Darunavir (DRV) Tipranvir (TPV)
Unboosted : 400 mg PO q 24 hr Boosted : 600 mg/100 mg rtv PO q Boosted : 500 gm/200 mg rtv PO q
(a | & % l treatment-nave 12 hr j 800 mg/100 mg rtv PO q 12 hr(21)
patients)(21) 24 hr(21)
bl
Boosted : 300 mg/100 mg rtv PO q
24 hr (l treatment-experienced
patients, a2 + EFV, NVP,
TDF)(21)
(21)
F 35-70% (4%5& + F 82% (4%5&+) 4%5&+
+jo u, *$ *$g 6 ' high fat (21) Serum t 6
g d+'
(21)
(21)
meal) Serum t 15
g d+' m6 : ti*$g6f*'d6
(21) (21)

m*#" Serum t 7
g d+' m 6 : ti*$g6 f*'d6 CYP3A4 e*
(21)
m 6 : ti*$g6 f*'d6 CYP3A4 e*
CYP3A4 e * , b5'a# 7%
lia+2*$g6f*'(21)
ATV e moderate CYP3A4 DRV e moderate CYP3A4 TPV e moderate CYP3A4
inhibitor(21) inhibitor(21) inhibitor, CYP2D6 inhibitor(21)
l ATV 2+ PPIs, H2RAs, l TPV 2 + antacids
Drug interaction antacids, ddI buffered tablets/ powder %6 TPV **' 23%
(+$ magnesium-based antacids) *
ih+b' ATV hg'#'6%
lih+(21)
Class effects af2 insulin resistance, type 2 DM, dyslipidemia, lipodystrophy, lipoatrophy and peripheral wasting,
osteopenia/ osteoporosis, hepatotoxicity, spontaneous bleeding in hemophilia(21) (i#'5$g 41-1)
Specific ADRs : indirect Specific ADRs : njg, njg1f' (+$ Specific ADRs : njg (+$6' SJS
hyperbilirubinemia ( & a 22-49% 6' SJS j 1% jg'ml j jg 'm ld 4 ' '6 +$
ADRs
+&7"b6), prolonged PR d4' '6+$ sulfonamide moiety sulfonamide moiety 6i2 ),
(21) (21)
interval, heart block 6i)2 hepatotoxicity, intracranial
ADRs jgu : GI side effects, hemorrhage (
jg 2 m66 6o '
$%(21) platelet aggregation)(21)
e PI 5$g DHHS guideline 2013 e PI 5$g DHHS guideline 2013 +$ b 2 ' l
|&%l highly PI-
f%e preferred regimen f%e preferred regimen experienced patients
+$ n *#2 insulin sensitivity f*% DRV e non-peptidic PI 5$g TPV e non-peptidic PI 5$g
serum lipid 62 PIs jg (lipid- d4''+$4+6j612 (flexibility) l d4''+$4+6j612 (flexibility) l
friendly PI)(21) l & $ HIV-1 protease l & $ HIV-1 protease
+6#1 * 6 & 71" 5$g # f 2 ' I50L f+2m%+$jo PIs #jgu f*#+ f+2m%+$jo PIs #jgu f*#+
m&%jo6 ATV (signature m'6'4'+$% 57 &$ l multiple-PI m'6'4'+$% 5 7 &$l multiple-PI
mutation) 5l
joa#2 ATV **' resistant HIV 2lw2 (> 90%) f+2 resistant HIV 2lw2 (> 90%) f+2
f#2*5la#2 PIs #jg+bo
jo m% +$ protease resistance
jo m% +$ protease resistance
mutations t' 16 #f2'#+ (DRV mutations *6#f2'#+ (TPV +$
+$ genetic barrier i'+)(21) genetic barrier i'+)(21)

if6f*% Capsules : 100 mg, 150 mg, 200 Tablets : 300 mg, 400 mg, 600 mg 250 mg capsules (Aptivus )
4+f' mg, 300 mg (Reyataz) (Prezista)

1506 424
2 2556 95
#$%& 41-4 Fusion inhibitors, CCR5 inhibitors, integrase strand-transfer inhibitors
Enfuvirtide (T-20) Maraviroc (MVC) Raltegravir (RAL) Elvitegravir (ELV)
Integrase strand-transfer Integrase strand-transfer
*1+2 6 Fusion inhibitors(58) CCR5 inhibitors(59)
inhibitors (INSTIs)(60) inhibitors (INSTIs)(61)
90 mg SC q 12 hr(58) 150 mg PO q 24 hr
bl
(2 mg/kg q 12 hr l) 300 mg PO q 12 hr(59) 400 mg PO q 12 hr(60) (2 + cobicistat 150
(61)
mg)
F 84.3% (*'l 90 mg F 23-33% (%5 %52 j * ' 4 %5 & +
SC)(58) 2j*'a)(59) a(60) (61)
Vd 5.5 L, plasma protein Vd 194 L, plasma Plasma protein binding Plasma protein binding
binding 92%(58) protein binding 76%(59) 83%(60) b' ELV 98-99%(61)
(59) (60)
Serum t 3.8
gd+' Serum t 14-18
gd+' Serum t 9
gd+' Serum t b' ELV +jg
m 6 : ti m 6 : ti m 6 : ti l2 + cobicistat (e

m*#"
*$g 6 f * 'd 6 protein *$g 6 f*'d6 CYP3A4 *$g 6 f * ' d 6 UDP selective CYP3A4 inhibitor
catabolism ae amino e * , b 5'a# glucuronidation (phase II
2 6& g+% 6 ELV l
acids(58) 23%(59) enzyme) f* b 5' *j) 13
gd+'(61)
o$(60) m 6 : ELV ti
*$g 6 f*'d6 CYP3A4
e*(61)
Enfuvirtide a+2$g6 b ' MVC e CYP3A4 l RAL 2+ PPIs, l ELV 2 +
CYP450 system (a+2e substrate m'#'%'l
TDF %6 RAL i'bo antacids %6 ELV
substrate, inhibitor, 2+ CYP3A4 inhibitors/ (6*%*6+bol%5$g **' # 'l2 ' > 2
inducer) m ' +$ d inducers e2')(60)
gd+'(61)
# 66jg6+ +jg l
MVC 2 + RAL a+2 $g 6 b ' ELV e CYP3A4
(58)
potent CYP3A4 inhibitors CYP450 system (a+2e subtrate f*% cobicistat e
(
2 PIs 6 TPV/rtv, substrate, inhibitor, CYP3A4 inhibitor m'# '
ketoconazole, itraconazole, inducer) m ' +$ d %'l
2+ CYP3A4
Drug interaction
clarithromycin) #'*b # 66jg6+ inhibitors (
2 ATV, LPV,
e 150 mg PO q 12 hr(59) (60)
ketoconazole) f*% CYP3A4
+jg l
MVC 2 + +jg l
RAL 2 + inducers (
2 rifampicin,
CYP3A4 inducers (
2 rifampicin (strong UGT1A1 antiepileptics), CYP3A4
EFV, ETV, rifampicin, inducer) RAL tib substrates (
2
phenytoin, carbamazepine, 5'o $ bo # '& g + antiarrhythmics, digoxin,
phenobarbital) #'& g+e be 800 mg PO q 12 macrolides, azole
600 mg PO q 12 hr(59) hr(60) antifungals) (61)
(59)
Local site reactions (& Hepatotoxicity * +jo , CPK Elevated sCr (& g+bo
(59)
98%
2 4, +, f', GI side effects elevation, myopathy(60) 0.1-0.2 mg/dL jg'm
(59)
, nodules, cysts, ab, a, URIs CNS side effects
2 cobicistat 6 6o ' tubular
(58)
ecchymosis) $%, '$6, $ % , ' $ 6 , secretion of creatinine,
Hypersensitivity a+2*(59) 2&*$6, h+, a+2 * e # * ' 61 l

(58)
reactions * +jo , CPK *(60) 6)(61)
ADRs
& g + 4 + $g 6 ' #2 elevation(59) GI side effects
(60)
GI side effects
(61)
bacterial pneumonia(58) Systemic allergic LFT abnormalities

(60)
reactions
2 njg , 4 ,
eosinophilia, IgE i'(59)
& g + 4+$g 6 '#2
myocardial infarction(59)

1506 424
2 2556 96
#$%& 41-4 Fusion inhibitors, CCR5 inhibitors, integrase strand-transfer inhibitors (#2)
Enfuvirtide (T-20) Maraviroc (MVC) Raltegravir (RAL) Elvitegravir (ELV)
p57 c 6 6o ' *+ p57 co CCR5 hg'
p57 c 6 6o ' integrase p57 c 6 6o ' integrase
+%2' viral envelope e co-receptor 5$g
hg ' e ah+" l (+j raltegravir)(61)
CD4 cell membrane(58) me #'l
l%#
viral DNA strand f5b ELV e NSTI 5$g DHHS
'al
l65$g*+* CD4 cell membrane(59)
a (integration) l host guideline 2013 f%e
m6*12+jgu (treatment- DNA(60)
'al
l65$g*+* alternative regimen(61)
experienced patients)(58) m6*12+jgu (treatment-
RAL e INSTI 5$g DHHS * viral load a$a+2#2'
+6#1 +1$6#f2'5$g|$a experienced patients)(59)
guideline 2013 f%e m TDF/FTC/EFV
jg6u (#b fb 5' 2 l
# ' # m
preferred regimen l (preferred regimen) 5o'l
f#2a+24|$l*%j) &jg treatment-nave patients(60)
tropism b' HIV (tropism treatment-nave f* %
' granulated testing) m%l
a#2+jg&2
* viral load a$l65$g treatment-experienced
lumps l#n '(58) e CCR5-tropic HIV-1
jo6*5o' 3 *12+ NRTIs, patients(61)
52o(59) NNRTIs, PIs (triple-class
resistant)(60)
Injection : 90 mg/vial Tablets : 150 mg, 300 Tablets : 400 mg Fixed dose combination
if6f*% (Fuzeon) mg (Celsentri) (Isentress) tablet : TDF 300 mg/ FTC
4+f' 200 mg/ ELV 150 mg/
COBI 150 mg (Stribild)
Antiparasitic agents
Antimalarial agents
i#6#+*$65$g guidelines for the treatment of malaria 2010 ('4"+6d*) f*%f5'

3 # l
ni6+*$6l%5a56 &.. 2557 f%e'$o
WHO guideline 2010 cPN$IN]fv_#_\PMMlijOfkNHGUI%H\PfgItQH 2557

Uncomplicated falciparum malaria
1st line antimalarial treatment 1st line regimen
4l
antimalarial drugs 2+ 2
boa d6*jl
65$g+$ Artesunate 5$g 1-3 + mefloquine 5$g 1-2 f*% primaquine 30 mg
*ap57 c#2' (anti-gametocyte) 4o'$6 l5$g 3
nd
f%ll
artemisinin-based combination therapy (ACT) 62' 2 line regimen
6 3 l uncomplicated falciparum malaria Quinine + doxycycline 7 f*%l primaquine 30 mg 4o'
Artemether-lumefantrine f*% artesunate + mefloquine +% $6 l5$g 7
&jo5$g%b' multidrug resistant P. falciparum
2 ft Quinine + clindamycin 7 f*%l primaquine 30 mg 4o'

$6#%|$6'l# $6 l5$g 7
Artemether-lumefantrine, artesunate + amodiaquine f*% wP`\]O
artesunate + sulfadoxine-pyrimethamine +%&jo 5$gft Artesunate l 4 mg/kg/day x 3 j 2 mg/kg/day x 7
f
2 o 50 kg l 4 tab PO q 24 hr x 3
l$5$ga+2+$ ACT m& ml amodiaquine + sulfadoxine- Mefloquine l 25 mg/kg f2'll5$g 1-2 j (250 mg tab) 3
pyrimethamine f5 tab lf f*% 2 tab l5$g 2
nd
2 line antimalarial treatment Quinine l 10 mg of quinine base/kg/day j (250 mg base tab)
Artesunate (2 mg/kg/day) or quinine (10 mg of sulfate 2 tab PO q 8 hr
salt/kg/day) PLUS tetracycline (4 mg/kg PO q 6 hr) or

1506 424
2 2556 97
WHO guideline 2010 cPN$IN]fv_#_\PMMlijOfkNHGUI%H\PfgItQH 2557
Uncomplicated falciparum malaria
doxycycline (3.5 mg/kg/day) or clindamycin (10 mg/kg PO q 12 Doxycycline l 3 mg/kg/day j (100 mg cap) 1 cap PO q 12 hr
hr) 7 Clindamycin l 10 mg/kg PO q 12 hr j (300 mg cap) 1 cap
F_$G%Shq PO q 12 hr
a#+f ll
quinine + clindamycin 7
a#+5$g 2-3 ll
artesunate + clindamycin 7 j
quinine + clindamycin 7
F_$\FOPGJ#
l#+# f#2*$*$g6' tetracycline, doxycycline,
dapsone
Severe or complicated falciparum malaria
\PijO\FR : artesunate 2.4 mg/kg IV/IM x 3 d l5$g 1 (
gd+' 1st line regimen
5$g 0, 12, 24) mo 2.4 mg/kg IV q 24 hr mo 2 mg/kg PO q Artesunate 2.4 mg/kg IV/IM x 3 d l5$g 1 (
gd+'5$g 0, 12, 24)
24 hr m4 7 PLUS tetracycline (4 mg/kg PO q 6 hr) or mo 2.4 mg/kg IV q 24 hr mo 4 mg/kg PO q 24 hr m4
doxycycline (3.5 mg/kg/day) or clindamycin (10 mg/kg PO q 12 5 PLUS mefloquine (250 mg tab) 3 tab lf f*% 2 tab l
hr) 7 5$g 2
\PI`xM\P high transmission area : artesunate (+jlnilw2) 2nd line regimen (\P low resistance area)
j artemether 3.2 mg IM on admission then 1.6 mg q 24 hr Quinine dihydrochloride 20 mg/kg loading (mjm'l D5W 1,000
j quinine 20 mg of dihydrochloride salt/kg on admission (IV mL drip in 4 hr) then 10 mg/kg IV (infused over 2 hr) q 8 hr
infusion or IM) then 10 mg/kg IV infusion (< 5 mg PLUS tetracycline 250 mg PO q 6 hr or doxycycline 100 mg PO
salt/kg/hr) q 8 hr q 12 hr 7
SEAQUAMAT study &2 severe falciparum malaria
6 IV artesunate +$##6#g2 IV quinine 62'+$64w
5't # (15% f*% 22% #+*, P = 0.0002) f*% quinine 6'+$
1# " hypoglycemia i'26 (RR = 3.2) 5l artesunate
tif%ae 1st line drug
P. vivax, P. ovale
Chloroquine 25 mg/kg f2'l 3 j (150 mg base tab) 4 tab
stat then 2 tab l$ 6
gd+' (6 tab l5$g 1) mo 2 tab PO q
24 hr l5$g 2-3 (+l 10 tab) PLUS primaquine (15 mg tab) 1-
2 tab PO q 24 hr #2$ 14 &jg2 hypnozoites (' relapse)
P. malariae, P. knowlesi
Chloroquine 25 mg/kg f2'l 3 j (150 mg base tab) 4 tab
stat then 2 tab l$ 6
gd+' (6 tab l5$g 1) mo 2 tab PO q
24 hr l5$g 2-3 (+l 10 tab) (P. malariae, P. knowlesi a+2+$
hypnozoites m'a+2#'l primaquine)
#$%& 42 Antimalarial agents *12+ quinoline derivatives

Chloroquine Primaquine Mefloquine Quinine
*12+626 4-aminoquinolines(52, 62, 63) 8-aminoquinolines(52, 62, 64) 4-methanolquinolines (52, 62, 65)
4-methanolquinolines(52, 62)
p 5 7 c d 6 m p 5 7 c 62 6 * 6 p 5 7 c d 6 m
plasmodial DNA f*% '4%" pyrimidine f*% hemoglobin b ' plasmodial DNA(2)
*a
62 6*6 hemoglobin mitochondrial Plasmodium spp.(2)
p57 c
(heme detoxification) b' electron transport chain(2)
Plasmodium spp.(2, 62, 63)

1506 424
2 2556 98
#$%& 42 Antimalarial agents *12+ quinoline derivatives (#2)
e blood schizonticidal e tissue-stage e blood schizonticidal
e blood schizonticidal
agent #2 P. falciparum, P. schizonticidal agent (liver agent #2 P. falciparum (5o'
agent #2 Plasmodium spp.
vivax f*%e gametocidal schizonts, hypnozoites) b' chloroquine-sensitive, 51
( + t '
Spectrum of agent #2 P. vivax, P. ovale, P. vivax, P. ovale f*%e chloroquine-resistant, chloroquine-resistant
activity P. malariae(17, 66) gametocidal agent #2 P. multiple drug-resistant
strains of P. falciparum)
falciparum(2, 17, 62, 64, 66) strains), P. vivax(2, 17, 66)
f*%e gametocidal agent
#2 P. vivax, P. ovale, P.
malariae(2, 17, 66)
' f*% non- ' relapses (radical mild to moderate acute malaria 5$g
falciparum malaria (P. cure) m P. vivax, P. acute malaria m P. m chloroquine-
vivax, P. ovale, P. malariae, ovale(2, 17, 64) falciparum, P. vivax(2, 17) resistant strains of P.
b2'l

P. knowlesi) f*% falciparum(2, 17)
chloroquine-sensitive P.
falciparum(2, 67)
600 mg base PO stat then 15-30 mg PO q 24 hr x uncomplicated uncomplicated
300 mg base l$ 6 14 &jg 2 hypnozoites falciparum malaria l 750 falciparum malaria l 500

gd+' mo 300 PO q 24 b' P. vivax, P. ovale(2) mg PO lf f*% 500 mg base PO q 8 hr (2+
hr l5$g 2-3(2) 30 mg PO single dose mg l 12
gd+'t+(2) doxycyline j
&jg2 gametocytes b' P. clindamycin) x 7 (2, 3)
falciparum(2, 64) severe or
bl

complicated falciparum
malaria l quinine
dihydrochloride 20 mg/kg
loading (drip in 4 hr) then
10 mg/kg IV (infused over 2
hr) q 8 hr(2, 17)
85%(2)
Absorption 89%(2) 96%(64) 80%(3)
(4%5&+)
53
ng/mL *'%5
> 1 mmol/L *'%5 15 mg(64) 7 mcg/mL *'%5
540-1,240 ng/mL *'
Cmax 26 mg of chloroquine base 104 ng/mL * ' 1,000 mg (steady-state
%5 1,000 mg(2)
d6f2'l 4 d(2) %5 30 mg (steady- concentrate)(2)
state concentrate)(2, 64)
Plasma protein
50-65%(2, 62) 75% 98-99%(2, 62) 70-95%(2, 3)
binding
Vd 200-300 L(64) 3 L/kg(3)
#f2'5$g6 Eyes, heart, kidneys, liver,
Erythrocytes, CSF(2)
%m6aa$ lungs, erythrocytes(2)
CSF
2-7%(2, 3)
penetration
ti*$g6f*'5$g#e
ti*$g6f*'5$g#e
ti*$g6f*'5$g#e amino-, hydroxy-, ti*$g6f*'5$g#e
Metabolism monodesethylchloroquine
carboxyprimaquine(2, 62, 64) hydroxylamine metabolites hydroxyquinine(2)
(active metabolite)(2, 62)
(inactive metabolites)(2)
41-47% (unchanged) + 3.6% (unchanged) +
Urine excretion 5%(2) 5% (unchanged)(2, 3)
7-12% (metabolite)(2, 67) 64% (metabolite)(64)

1506 424
2 2556 99
5.8
g d+' (primaquine)(2,
t la## 4 -2 j(2) 62, 64)
, 15
g d+' 14-21 (2, 62) 11-18
gd+'(2, 62)
(carboxyprimaquine)(64)
t l ESRD 14
gd+'(3)
#'b l
2(2) l
2(2, 3)
a+2#'(2, 64) a+2#'(2)
ld4a# (+jg CrCl < 10) (+jg CrCl <10)
#'l

6
a+2+$b+i*(2) a+2+$b+i*(2) a+2#'(2) a+2#'(2)
*'5 HD
#'b
l
2(2) a+2+$b+i*(2) a+2+$b+i*(2) a+2#'(2)
ld4#
Pregnancy cat. C(2) C(2) C(2) D(3), X(2)
(2, 3, 17, 67)
GI side effects
2 4*jga m$6, 5'2', 5'
CNS side effects
2 $%, '$6, , h,
(*$*$g6'j%+%'l
lni5 $g+$%# epilepsy)(2, 3, 67)
Cardiovascular side effects
2 lmg , lm#
j , 4+ *j #g j i ', lm# n m' %, QTc
prolongation(2, 3, 67)
(2, 3, 17)
njg, 4, njg1f' (
2 erythema multiforme, SJS, TEN) , %#1l psoriasis (67)
(2, 3, 67)
Hemolytic anemia +jgl
l G-6-PD deficiency (d6|&% primaquine 44' G-6-PD deficiency 2l6)
(2, 17)
ADRs Myelosuppression (mild anemia, leucopenia, neutropenia, agranulocytosis, pancytopenia)
(67)
*+jo2f' m%#1l myasthenia gravis a
(2)
(2)
ab, o*, n+2'
(2, 62)
Hypoglycemia (d6|&%l
IV quinine severe malaria lw '4")
Chloroquine f*% hydroxychloroquine 5l corneal opacities, retinopathy +jgl
# #2e* ($l
e
DMARD l rheumatoid arthritis, SLE) ni64a#m fundoscopy f*% visual fields 51 1 (2, 17, 67)
(2)
+jgl
chloroquine 2+ antacids *ih+ chloroquine #'l2' > 2
gd+'
(2, 3, 17)
+jgl
mefloquine 2+ chloroquine, quinine & g+4+$g6'#2
f*% cardiotoxicity
+jgl
mefloquine 2+ CYP3A4 inhibitors (ketoconazole, macrolides, PIs) %6 mefloquine & g+bo62'+$
64w5'4* 4*$*$g6'l
2+(2)
+jgl
mefloquine 2+ CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital) %6
mefloquine **'62'+$64w5'4* 4*$*$g6'l
2+(2)
Drug
+jg l
quinoline derivative antimalarials 2+ 65$g m5l QTc prolongation (
2 antiarrhythmic drugs,
interaction
macrolides, FQs, TCAs, antipsychotics, cisapride) & g+4+$g6'#2 QTc prolongation, TdP, cardiac arrest(2, 3, 17) 4
*$*$g6'l
2+
+jgl
quinoline derivative antimalarials 2+ zidovudine, ganciclovir, pyrimethamine, 5-flucytosine, interferons
& g+4+1f'b' myelosuppression(2)
+jgl
quinoline derivative antimalarials 2+ neuromuscular blocking agents (
2 pancuronium, succinylcholine)
& g+4+$g6'#2 neuromuscular blockade(3)
(17,
e suppressive agent e curative agent v m m1 & mefloquine- e5o' suppressive agent
62) (2, 17)
(' relapse) resistant P. falciparum + f*% curative agent(17)
l
e DMARD l l
2+ clindamycin l bol
$6#%|$6'l# l
nocturnal leg
rheumatoid arthritis, SLE PCP lni65$ga+2 d6|&%
6fa56-&+2 cramps a6(2)
+6#1 a6(62, 67) +t l
cotrimoxazole, f*%a56-+&i
(2, 65, 67) & m quinine
dapsone, pyrimethamine a a+2 6 +l
l b (cinchonism)

2 G-6-PD deficiency(21, 64) benign malaria jg'm+$ a f 2 +' n # ,
(67)
+ l
l G-6-PD 6jg5$g+$ ADRs #g2 tinnitus, $%, 4*jga
deficiency (&%m a+24l
mefloquine l m$6, lf' #f',

1506 424
2 2556 100
acute hemolytic anemia), malaria tni6 'jg , ab , , +
rheumatoid arthritis, SLE 4 6 a mefloquine # , 4+ *j #g ,
+6#1
(&%& g + 4+$g 6 '#2 prophylaxis +2(67) lm#n m'%(2, 17, 62)
granulocytopenia)(17, 64)
Syrup : 62.5 mg of Tablets : 15 mg Tablets : 250 mg Tablets : 300 mg of
chloroquine/5 mL quinine sulfate (5$652
Tablets : 250 mg of quinine base 250 mg)
chloroquine diphosphate Injections : 600 mg/2 mL
if6f*%
(5$652 chloroquine base
4+f'5$g+$l
150 mg)
%5a56
Injections : 322.6 mg of
chloroquine diphosphate/ 5
mL (5$6 52 chloroquine
base 193.5 mg/5 mL)
#$%& 43 Antimalarial agents *12+jgu

Atovaquone-Proguanil Artesunate Artemether-Lumefantrine Pyrimethamine
*12+626 Hydroxynaphthoquinones(52) Artemisinin derivatives (52)
Artemisinin derivatives(52) Diaminopyrimidines(52)
Atovaquone p57 c d 6 Artemisinin derivatives (artesunate, artemether, Pyrimethamine p57 cd6
6 6o ' mitochondrial arteether, dihydroartemisinin) p57 cd6 endoperoxide 6 6o' ah+" dihydrofolate
electron transport chain (free radical) 3 6 intraparasitic heme (l food reductase a+2 l *$g 6
*a b' P. falciparum f*% vacuole) 5l %+b' non-polymerizable redox- dihydrofolate (folic acid)
p57 c proguanil p57 cd666o' active heme f*%5 *6 plasmodial membrane e tetrahydrofolate (folinic
dihydrofolate reductase l phospholipids(2) acid)(2, 17)
' 4 % " Lumefantrine e broad schizoticidal agent
deoxythymidylate(2)
+$p57 c2 erythrocytic f*% e blood schizonticidal e blood schizonticidal e blood schizonticidal
Spectrum of exoerythrocytic forms b' agent f*% gametocidal agent f*% gametocidal agent +$ % 5 7 & l
activity Plasmodium falciparum(2, 17) agent #2 P. falciparum(2) agent #2 P. falciparum(2) chloroquine-resistant
strains of P. falciparum(2, 17)
' f*% acute severe falciparum acute ' f*% acute
uncomplicated falciparum malaria f*% mild to uncomplicated falciparum chloroquine-resistant
malaria l &jo 5$g 5$g +$ moderate falciparum malaria (a+2+$b2'l
l falciparum malaria (l

(2)
b2'l
1 # " chloroquine- malaria severe or 2 + sulfadoxine f*%
resistant, mefloquine- complicated falciparum quinine)(2, 17)
(2, 67)
resistant P. falciparum i' malaria)
(17)
Falciparum malaria Severe or complicated Uncomplicated Acute malaria :

prophylaxis : 250/100 mg falciparum malaria : 2.4 falciparum malaria : l pyrimethamine 50-75 mg
(1 tab) PO q 24 hr g+2 mg/kg IV/IM x 3 d l5$g ni l w2 (> 35 kg) l 2+ sulfadoxine 1,000-
bb#% 2 amt' 1 (
g d + ' 5$g 0 , 1 2 , 2 4 ) Coartem (20/120 mg) 4 1,500 mg single dose(2, 3)
bl

1 " *'*mb# mo 2.4 mg/kg IV q 24 tab x 6 d (0, 8, 24, 36, CNS
%(2, 3) hr (l2 + mefloquine 48, 60
gd+')(2) toxoplasmosis : 200 mg PO
Falciparum malaria 6 t e quinine- Weight-based dosing : 5- loading dose then 50-75
treatment : 1,000/400 mg resistant strains)(2) 15 kg l 6 tabs/course, 15- mg PO q 24 hr (l
2+

1506 424
2 2556 101
#$%& 43 Antimalarial agents *12+jgu (#2)
(4 tab) PO q 24 hr x 3 (2, 25 kg l 12 tabs/course, sulfadoxine or clindamycin
3)
25-35 kg l 18 f*% leucovorin) > 6 "
(2)
tabs/course, 35-65 kg l
24 tabs/course, > 65 kg l Secondary prophylaxis of
24 tabs/course (f2'l 6 toxoplasmosis : 25-50 mg
d52u 5$g* 0, 8, PO q 24 hr (l
2+
24, 36, 48, 60)(2) sulfadoxine 0.5-1 g PO q 6
hr or clindamycin 300-450
mg Po q 6 hr f*%
leucovorin 15 mg) m2
bl
CD4 > 200 cells/mm3 62'
6 6 j(2)
Primary prophylaxis of
toxoplasmosis : 50 mg PO
weekly (2+ leucovorin
25 mg weelky f*% dapsone
50-100 mg daily) +jg CD4
< 100-200 cells/mm3 a
m2 CD4 > 200
3
cells/mm 62'6 3 j
(2)
23%/ 90%(3)
60-100% (bob6)(2)
(4%5&+ tiih+62'
Absorption (4 %5& + fatty 90%(3)
j+ &jg& g+ih+6 *'|$b*+(2)
meal)(2)
d6|&% fatty meal(2))
16 mcg/mL *'l 120 mg 0.13-0.31 mcg/mL *'
Cmax 24 mcg/mL (suspension)(2)
IV(2) %5 25 mg(2)
Plasma protein
99%/ 75%(2, 3) i'(2) 95% (artemether)(2) 80-87%(2, 3)
binding
5.4-8.6 L/kg (artemether),
Vd 3.5/ 42 L/kg(3) 0.2-1.5 L/kg(2) 2.5 L/kg(3)
3.8 L/kg (lumefantrine)(2)
#f2'5$g6 P. falciparum-infected Kidneys, lungs, liver,
Erythrocytes(2)
%m6aa$ erythrocytes(2) spleen(2)
CSF
< 1%(2) 13-26%(2)
penetration
Artesunate ti hydrolysis Artemether ti*$g6f*'
Atovaquone 2lw2a+2ti
62 ' d6ah+" 62 ' e
*$g6f*', proguanil ti
cholinesterases l plasma dihydroartemisinin (active
Metabolism *$g 6 f * ' 5$g # d 6
f * % jo 6jg a e metabolite)(2)
CYP2C19 e cycloguanil
dihydroartemisinin (active
(active metabolite)(2)
metabolite)(2)
b5'o$e*
20-30% (unchanged in
Excretion 94%/ 50% (unchanged in b5'o$e*(2)
urine)(2, 3)
faces)(2, 3)
45 5$ 0.8-7
+. (artemether),
t la## 48-72/ 12-21
gd+'(2, 3) 80-123
gd+'(2, 3)
(dihydroartemisinin)(2) 72-120
+. (lumefantrine)(2)

1506 424
2 2556 102
t l ESRD 60/ -
gd+'(3) 96
gd+'(3)
a+2#'(2) a+2#'(2, 3)
#'b
f#24*$*$g6'+jg CrCl < a+2#'(2) a+2#'(2) f#2l
64+%+%'l
ld4a#
30(2, 3) CrCl < 10(3)
#'l

6
a+2#'(2) a+2#'(2) a+2+$b+i*(2) a+2#'(2, 3)
*'5 HD
a+2#'(2) a+2#'
#'b
a+2+$b+i*(2, 3) a+2#'(2) l mild to moderate f#2l
64+%+%'l
ld4#
hepatic impairment severe hepatic impair.(3)
l
a l 2nd f*% 3rd l
a l 2nd f*% 3rd
(2, 3)
Pregnancy cat. C trimester, *$ *$g 6 'l 1st trimester, *$ *$g 6 'l 1st C(2, 3)
trimester(2) trimester(2)
Allergic
#g(3) #g(3)
potential
njg (&a 20%, +$ GI side effects
2 GI side effects
2 Myelosuppression af2
(2)
6' SJS) 4*jga m$6(2) 4*jga m$6, jg, megaloblastic anemia,
(2)
GI side effects
2 %lm#
5', 5'2'(2, 67) leucopenia,
4*jga m$6, jg, CNS side effects
2 Cardiac side effects
2 agranulocytosis,
5 ', 5 '2 ' (&a ' $ 6 , cerebellar lmg , QTc prolongation thrombocytopenia, aplastic
20%)(2, 3, 21) dysfunction ( h &ia+2 (%'l
2 +65$g m anemia + &+jg a
CNS side effects
2
),
(2) 5l QTc prolongation pyrimethamine bi '
$%, '$6, a+2 Hypersensitivity j +$ electrolyte j a 2 + folate
*(2, 3, 21) reactions (2)
abnormalities) (2, 67)
antagonists(2, 3, 17)
(2, 3)
ab, *+jo CNS side effects
2 bo l 6
ADRs
LFT abnormalities, $%, '$6, a+2 leucovorin 50-100 mg/day(2)
hepatitis(2, 21) * , 2 f ' ,
, GI side effects
2
cerebellar dysfunction ( 4*jga m$6, jg(2,
h #%#1)(2, 67) 17)
(2,
b , * +jo CNS side effects
2
67)
$%, '$6, a+2
(67)
njg, 4 *, g, h,
(2, 3)
+$6' SJS, TEN (m
m sulfadoxine 5$g l
2+)(2, 17)
+jg l
atovaquone Artesunate e CYP3A4 Artemether f*% +jg l
pyrimethamine
2+ zidovudine AUC substrate(2) lumefantrine e CYP3A4 2 + cotrimoxazole,
b' zidovudine & g + bo +jga2+ CYP3A4 substrate m'#'%'l
trimethoprim, dapsone, 5-
31%(2) inhibitors (macrolides, azole 2+ CYP3A4 inhibitors/ flucytosine, ganciclovir,
+jg l
atovaquone antifungals, PIs) m5 inducers(2) zidovudine, interferons
Drug 2 + tetracycline, l%6 artesunate i'bo +jg a2+65$g m & g + 4 + 1 f ' b '
(2)
interaction rifampicin AUC b' 5l QTc prolongation myelosuppression(2, 3)
atovaquone **' 40-50%(3, +jga2+ CYP3A4
(
2 antiarrhythmic drugs, +jg l
pyrimethamine
17)
inducers (rifampicin, macrolides, FQs, azole 2+ folic acid *
+jg l
atovaquone phenytoin, carbamazepine, antifungals, halofantrine, % 5 7 & b '
2+ metoclopramide phenobarbital) m5l other antimalarials, TCAs, pyrimethamine(3)
%6 atovaquone **'(2) %6 artesunate **'(2) antipsychotics, cisapride)(2)

1506 424
2 2556 103
+jg l
atovaquone
2+ chlorquine & g+
4+$g6'#2 fn*l
Drug
2'(3)
interaction +jg l
atovaquone
2+ typhoid vaccine 5
l % 5 7 &b' 4 h$
**'(3)
+$ % 5 7 &|&% P. b 2 ' l
b ' IV Artemether m
jo Pyrimethamine e drug
falciparum (5o' chloroquine- artesunate a f 2 severe + + ( parasitic of choice l
sensitive f*% chloroquine- falciparum malaria, high- biomass) a 62 ' toxoplasmosis (l
2 +
resistant strains)(2, 3) density parasitemia (> 5%), 2 lumefantrine +$55 sulfadiazine 1.5 g PO q 6
Atovaquone a+2+t%56a, m
jo 2 5$g *'*j hr j clindamycin 600 mg
monotherapy (750 mg PO acute respiratory distress jg 'm6ti b62' IV q 6 hr)(2, 3, 17)
q 12 hr x 21 ) l
e syndrome j severe
u(2) # 'l 2 + leucovorin
(2)
5'*jl mild to anemia (folinic acid) 10-25 mg/day
moderate PCP (A-a O2 Artemisinin-based &jg '
gradient < 35 mmHg, PaO2 combination therapy (ACT) myelosuppression(2, 21)
> 60 mmHg) f*%' a f 2 artesunate +
PCP (750 mg PO q 12 hr mefloquine, artemether-
+6#1
j 1,500 mg PO q 24 hr) lumefantrine +%
$ 5$g l
cotrimoxazle, uncomplicated falciparum
dapsone a+2a(2, 21) malaria l&jo5$g %b'
Atovaquone (1,500 mg multidrug resistant P.
PO q 12 hr) 2 + falciparum
2 ft
$6
pyrimethamine (200 mg #% |$6 'l# (+t'
loading dose then 75 mg %5a56)(2)
PO q 24 hr) f*% leucovorin
l
e5'*jl
toxoplasmosis $ 5$g l

sulfadiazine, clindamycin
a+2a(2)
if6f*% Tablets : atovaquone Tablets : 50 mg Tablets : artemether 20 Tablets : 25 mg
4+f'5$g+$l 250 mg + proguanil 100 mg Injections : 60 mg/vial mg + lumefantrine 120 mg
%5a56 (Malanil) (Coartem)
Antiprotozoal agents
Nitroimidazoles af2 metronidazole, tinidazole +$p57 c2 Entamoeba histolytica (intestinal amebiasis, amebic
liver abscess), Giardia lamblia (giardiasis), Trichomonas vaginalis (trichomoniasis)(2, 17) (i6*%$6& g+# +
41)

1506 424
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#$%& 44 Antiprotozoal agents
Diiodohydroxyquin
Pentamidine Paramomycin Nitazoxanide
(Iodoquinol)
Haloginated Nitrothiazolyl-salicylamide
*12+6 Aromatic diamidines(17, 68) Aminoglycosides
8-hydroxyquinolines derivatives
p 5 7 c d 6 p 5 7 c 6 6o ' 5$g 16s p 5 7 c d 6
nuclear metabolism, 66o' ribosomal RNA b'
jo pyruvate: ferredoxin
*a oxidative phosphorylation 2 ' n*l a +2 +t ' oxidoreductase (PFOR)
p57 c f*% biosynthesis of DNA, d#$a enzyme-dependent electron
RNA, protein, transfer reaction 2'n*l
(2, 17, 68)
phospholipid
job ATP(2, 17)
Spectrum of Cryptosporidium parvum,
Pneumocystis jiroveci(2, 17) Entamoeba histolytica(17) Entamoeba histolytica(17)
activity Giardia lamblia(2, 17)
e drug of choice l
d45 '2 '5$g
intestinal amebiasis, intestinal amebiasis
m Cryptosporidium
'f*% PCP extraintestinal or invasive 52o (a+2+$% 57 &l
b2'l
parvum(2)
(2nd line drug)(2) amebiasis (
2 amebic extraintestinal amebiasis
#
jo Giardia
liver abscess), balantidiasis &%6a+2tiih+m GI)
lamblia, Entamoeba
(2)
histolytica
PCP treatment : 4 mg/kg
IV (infused over 1 hr) q 24 500 mg PO q 6-12 hr(2, 3)
hr x 21 (2, 21) (immunocompromized
630-650 mg PO q 8 hr x 25-35 mg/kg/day f2'l q
bl
PCP prophylaxis : 300 patients l 4-6 ",
20 8 hr x 5-10
mg (mj'm'l SWFI 6 immunocompetent patients
mL) nebulization j*% l 3 )
4o'(2, 21)
Absorption 8% 0% a+2+$b+i*(2, 3)
0.5-3.4 mcg/mL *'l 4
mg/kg IV(2)
23.2 ng/mL in
Cmax
bronchoalveolar lavage
fluid * ' l 300 mg
nebulization(68)
Plasma protein
69%(2) 99.9%(2, 3)
binding
#f2'5$g6 Liver, kidneys, adrenal
%m6aa$ glands, spleen, lungs(2)
Urine excretion 4-17%(2) 4.6% < 10% (unchanged)(2, 3)
t la## > 4 "(2) 1-1.6
gd+'(2)
a+2#'(2, 3)
#'b
f#2l
64+%+%'l
ld4a#
CrCl < 10(3)
#'l

6
a+2#'(3)
*'5 HD
#'b
*$*$g6'l
(17) a+2#'(3)
ld4#
Pregnancy cat. C(2) C B(3)

1506 424
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#$%& 44 Antiprotozoal agents (#2)
Diiodohydroxyquin
(Iodoquinol)
Allergic
#g(3)
potential
Nephrotoxicity (&a 25- Optic neuritis, optic GI side effects
2 GI side effects
2
50% + *e # +jg atrophy, peripheral 4*jg a , 5 ', 5 '2 ' 4*jg a m$ 6 , 5 ',
61 l
6 , m IV neuropathy &a+jgl
6 +jg l
6 lbi' (> 3 5'2', 5'j(2, 3, 17)
pentamidine +2 lbi'f*%# #2 g/day)(17) $ %, ' $ 6 , ab ,
aerosolized pentamidine)(2, (17) $ 5$g +$f n*l* a
2 6jg 1m +i , flu-like
17)
GI side effects
2 ulcerative colitis m5l syndrome(2, 3, 17)
(3, 17)
Electrolyte abnormalities 4*jg a m$ 6 , 5 ', 6tiih+bi2%f*j v%+$$*j'b+

2 hypocalcemia, 5'2' m & #2if*%& #2a#
hypomagnesemia, ld4' '6+$ iodine a(17)
(2, 17, 21)
hypokalemia t' 64% m'4*$*$g6'
Hypoglycemia (2lw2 l
ni 6 5$g +$ thyroid
bo * 'l
6 5-7 ) disorders j ni 5$g +$ % #
j hyperglycemia(17, 21) f & iodine-containing
(2, 21)
Pancreatitis agents
2 iodinated
(17)
GI side effects
2 contrast media
4*jg a m$ 6 , 5 ', Papular or pustular
5 '2 ', n # acneiform eruptions, njg ,
(dysgeusia)(2, 17) 4, *+& , 4 5
a, bronchospasm * ' (pruritus ani)
l aerosolized pentamidine
ADRs
ml &2 beta2 agonist
2 &jg * respiratory
irritation(2, 17, 21)
(2, 17)
Phlebitis
Severe hypotension,
cardiopulmonary arrest
('d6l infusion > 60
5$, adequate hydreation
f*%lni6'6)(2, 17,
21)
Myelosuppression
2
leukopenia,
thrombocytopenia(2, 17)
LFT abnormalities,
hepatitis(2, 17)
CNS side effects
2
'$6, , a+2*,
g,
(2, 17)
njg, njg1f' (
2 SJS,
TEN)(2, 21)
l pentamidine Nitazoxanide a+2 e
Drug
2+ nephrotoxic agents CYP450 inhibitor, inducer
interaction
(
2 amphoterin B, AMGs, m'+$d # 6

1506 424
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#$%& 44 Antiprotozoal agents (#2)
Diiodohydroxyquin
(Iodoquinol)
cidofovir, vancomycin, 6jg6(2)
cisplatin, foscarnet,
cyclosporine) & g+4+
$g6'#2 nephrotoxicity(2, 3)
l IV pentamidine
Drug 2+ foscarnet & g+
interaction 4+$g6'#2 nephrotoxicity
f*% severe hypocalcemia(2,
3)
l IV pentamidine
2+ didanosine & g+
4+$g6'#2 pancreatitis(2)
IV pentamidine +$b2'l
6tiih+a6 m' 6a+2 ti i h + m ' ml
l C.
l severe PCP l p 5 7 c 2 Entamoeba p 5 7 c 2 Entamoeba difficile colitis 5$ga+2#'
$ 5$g l
cotrimoxazle, histolytica % 6 % histolytica, Salmonella spp., #2 6
clindamycin + primaquine trophozoites f*% cysts Shigella spp. |&%l*a metronidazole, oral
(17) (17) (2, 3)
a +2 a
2 G-6-PD |&%l*a vancomycin
deficiency(2)
Aerosolized pentamicin
+6#1 +$b2'l
l' PCP
l$ 5$g l
cotrimoxazole
j dapsone a+2a (+l
aerosolized l
PCP)(2)
l%2'l
64# #+
vital signs, blood sugar,
BUN, sCr(2)
Injections : 300 mg/vial Tablets : furazolidone 50 a+2 +$ m 2 6l%5 a+2 +$ m 2 6l%5
(Pentacarinat) mg + diiodohydroxyquin a56 a56
if6f*%
250 mg + neomycin 50 mg
4+f'5$g+$l
+ phthalylsulfathiazole 250
%5a56
mg + light kaolin 250 mg
(Disento)
Anthelminthic agents
Spectrum of activity(17) :
ALB MBD PYR IVM DEC NCL PZQ
&67 b (Ancylostoma duodenale, Necator americanus)
&67 aj (Ascaris lumbricoides)
&67 b++1 (Enterobius vermicularis)
&67 f+ (Trichuris trichiura)
&67 f4**$6 (Capillaria philippinensis)

1506 424
2 2556 107
ALB MBD PYR IVM DEC NCL PZQ
a f
&67 *$652o*j' (Wuchereria bancrofti, Brugia malayi)
&67 *$6l#n ' (Onchocerca volvulus, Mansonella spp., Loa loa) a
f

g
&67 #'m *6" (Strongyloides stercoralis)
e
Trichostrongylus orientalis
b
&67 #j+i (Taenia solium)
&67 #j (Taenia saginata)
&67 #j* (Diphyllobothrium latum), &67 #jf4% (Hymenolepis

nana), &67 #ji (H. diminuta), &67 #j1b (Dipylidium caninum)
c d
&67 a# (Echinococcus granulosus)
&67 la+ (Paragonimus spp.)
&67 la+# (Opisthorchis viverrini, Clonorchis sinensis, Fasciola

hepatica)
&67 la+*a (Fasciolopsis buski, Metagonimus yokogawai,

Heterophyes heterophyes)
&67 la+*j (Schistosoma spp.)
FGHIF#J al
2+ ivermectin j DEC, bneurocysticercosis, ccystic hydatid disease, de 2nd line e
drug, e drug of choice
trichostrongyliasis, fe 2nd line drug, ga|&% intestinal forms
#$%& 45-1 Anthelminthic agents

Albendazole Mebendazole
Pyrantel Ivermectin
(Zentel) (Fugacar)
Avermectins
*12+626 Benzimidazoles(17) Benzimidazoles(17) Tetrahydropyrimidines
(macrocyclic lactones)
p57 cd6m colchicine-sensitive site of beta-tubulin p57 cd6%#1 nicotinic p 5 7 c d 6 m
5la+2 polymerization of tubulin (' microtubules acetylcholine receptors b' glutamate-gated chloride
a+2 a) 66o'f2'h**", glucose uptake, parasite &67 f*%6 6o ' ah+" channels 5 l
motility 5l&67 #6l5$g1(2, 17) acetylcholinesterase hyperpolarization b' nerve
depolarization b' nerve f*% muscle cells(2)
*a
f*% muscle cells 5l m GABA-gated
p57 c
&67 e+&# f*%#6l chloride channels 5l+$
5$g1 (17) *g ' GABA
synapse +bo f*%& g +
postsynaptic binding of
GABA(2, 17)
Nematodes, some
Spectrum of Nematodes, arthropods
cestodes, protozoa (
2 Nematodes(17) Nematodes(17)
activity (
2 )(2, 17)
Cryptosporidium)(17)
Intestinal nematode Intestinal nematode
Onchocerciasis (river
Neurocysticercosis (m T.
infections (ascariasis, infections (ascariasis,
blindness), intestinal
solium), hydatid disease
hookworm infection, hookworm infection,
strongyloidiasis, lymphatic
b2'l
(m E. granulosus),
entorobiasis, trichuriasis)(2) entorobiasis,
filariasis, Loa loa,
intestinal nematode
trichostrongyliasis)
cutaneous larva migrans,
infection, microsporidiosis(2)
scabies(2)
Intestinal nematode Ascariasis : 500 mg PO Hookworm : 11 mg/kg Onchocerciasis,
bl
infections : 400 mg PO single dose j 100-200 PO q 24 hr (max. 1 g/dose) filariasis : 0.15 mg/kg PO
single dose(2) mg PO q 12 hr x 5 (2) x 3 single dose(2)

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#$%& 45-1 Anthelminthic agents (#2)
Pyrantel Ivermectin
(Zentel) (Fugacar)
Strongyloidiasis : 200-400 Hookworm : 500 mg PO Enterobiasis : 11 mg/kg Intestinal strongyloidiasis,
mg PO q 12 hr x 3 single dose j 100 mg PO single dose (max. 1 cutaneous larva migrans :
Neurocysticercosis : 400 PO q 12 hr x 3 (2) g/dose) (m#'lhol$ 0.2 mg/kg PO single dose
mg PO q 12 hr (15 Enterobiasis : 100 mg 2 ") (o 70 kg l 15 mg)(2)
mg/kg/day) x 8-30 (#' PO single dose (m#'l Trichostrongyliasis : 11 1 f' (severe
l 2 + systemic hot6'a+26)(2) mg/kg PO single dose scabies) : 0.2 mg/kg PO x
corticosteroids l
2 ' 1 Echinococcus : 40-50 (max. 1 g/dose) 2 d (%52' 2
" f &jg ' mg/kg/day f2'l q 8 hr(2) ")(2)
cerebral hypertensive
bl

episodes)(2, 17)
Hydatid (echinococcal)
disease : 400 mg PO q 12
hr (15 mg/kg/day) x 28
f* 14 m ' g +
%5l+2 (3 cycles)(2)
Microsporidiosis : 400
mg PO q 12 hr am2
CD4 > 200 cells/mm3(2)
5-10%(2)
ih+a6
(4 %5& + high
(4 %5& + high Well absorbed(2)
Absorption fat meal &jg& g+ih+
fat meal &jg& g+ih+ (4%5#5'2')
6)
6)(2, 17)
1.3 mcg/mL *'%5 0.3 mcg/mL *'%5 46 ng/mL *'%5
Cmax 0.05-0.13 mcg/mL
400 mg(2) 100 mg q 12 hr x 3 (2) 12 mg(2)
Plasma protein
70%(2) 93%(2)
binding
Cyst fluid, liver, omental fat,
#f2'5$g6 (2)
Bile, hydatid cyst, CSF pelvic, pulmonary cyst, Fat, liver(2)
%m6aa$ (2)
hepatic cyst
6ti*$g6f*'5$g# e
6ti*$g6f*'5$g# e
amino-, hydroxyl-,
Metabolism sulfoxide metabolite (active
hydroxyamino metabolites
form)(2)
(inactive metabolites)(2)
Urine excretion 2-5%(2) < 7% < 2%(2)
t la## 8-9
gd+'(2) 2.5-5.5
gd+'(2) 22-28
gd+'(2)
#'b
a+2#'(2) a+2#'(2) a+2#'(2)
ld4a#
#'l

6
a+2#'(2) a+2#'(2) a+2#'(2)
*'5 HD
#'b
a+2+$b+i*(2) a+2+$b+i*(2) a+2+$b+i*(2)
ld4#
Pregnancy cat. C(2) C(2) C C
(17)
Hepatotoxicity (&a Hepatotoxicity GI side effects
2 $%, '$6
ADRs
16%) 4# #+ LFTs 51 GI side effects
2 4*jg a m$6, jg, Mazzotti reaction (4+

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Pyrantel Ivermectin
(Zentel ) (Fugacar)
2 " l%2'5$gl
6(2, 4*jg a m$ 6 , 5 ', 5'2'(17) *j #g, ab, 4 ,
17)
5 '2 ' (2) (l65$g +$ & 67 $%, '$6 %if*%b)(2)
GI side effects
2 a j 6i2 m +m njg +$ 6 ' fatal
4*jg a m$ 6 , 5 ', 4*jg a 5 ' encephalopathy lni65$g
5'2'(2) 1f')(17) #
jo &67 * $ 6 Loa
(2)
$%, '$6 Myelosuppression loa(17)
(17)
ADRs ADRs 5$g&a 6+ (leucopenia, agranulocytosis, +, njg
(17)
a f 2 myelosuppression thrombocytopenia m&a GI side effects
(leucopenia, agranulocytosis, +jg l
l bi ' (40-50
thrombocytopenia, mg/kg/day l
pancytopenia 4# #+ echinococcosis)(2, 17)
CBC 51 2 " l
%2'5$gl
6(2, 17)
l albendazole, mebendazole 2+ phenytoin, l ivermectin 2+
carbamazepine, phenobarbital %6 albendazole, warfarin m5 l INR
Drug
mebendazole **'(17) i'bo(2)
interaction
l albendazole 2+ cimetidine %6
albendazole i'bo
Albendazole 400 mg Mean cure rate > 95% Ivermectin (0.15-0.2
single dose +$% 57 & l ascariasis, mg/kg PO single dose) +$
i'2 mebendazole l hookworm infection, % 5 7 & i ' 2
ascariasis, hookworm enterobiasis f*% 35-68% albendazole (200 mg PO q
+6#1
infection, trichuriasis(2) l trichuriasis(2) 12 x ) l
strongyloidiasis
(parasitological cure 83%
f*% 38% #+*)(17)
if6f*% Suspension : 100 mg/5 Suspension : 100 mg/5 Suspension : 500 mg/mL Tablets : 6 mg
4+f'5$g+$l mL, 200 mg/5 mL mL Tablets : 125 mg
%5a56 Tablets: 200 mg, 400 mg Tablets: 100 mg, 500 mg
#$%& 45-2 Anthelminthic agents

Diethylcarbamazine citrate (DEC) Niclosamide Praziquantel
*12+626 Piperazine derivatives Salicylanilides(69) Prazinoisoquinoline derivatives
6a+2+$n*2&67 *$6d6#' f#2 p 5 7 c d 6 6 6o ' oxidative p57 c d 6& g + cell membrane
%#1l host effector cells +5*6 phosphorylation f*%%#1 ATPase permeability 5l Ca2+ g m
*a
&67 5l& 67 b ATP m$o6 ' h**" 5l&67 #f*%e+&#
p57 c
66o' glucose uptake, 5*62 f*%6' 5 l vacuolization and
scolex 5l&67 *1mn'*a disintegration b'#&67 6(17, 70)
Spectrum of
Nematodes(17) Cestodes(69) Trematodes, some cestodes(17)
activity
Bancrofts filariasis, loiasis, Taeniasis (T. solium, T. saginata), Schitosomiasis (S. makongi, S.
onchocerciasis (river blindness), other intestinal cestode infections japonicum, S. mansoni, S.
b2'l

eosinophilic lung (tropical pulmonary (fish tapeworm, dwarf tapeworm, rat hematobium), liver fluke infections
eosinophilia) tapeworm, dog and cat tapeworm)(69) (Opisthorchis viverrini, Clonorchis

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2 2556 110
sinensis, Fasciola hepatica)(70)
Acute lymphatic filariasis : 6 T. saginata, T. solium : 2 g PO Schitosomiasis : 20 mg/kg PO q 4-
mg/kg/day (f2'l q 8 hr) x 14 single dose (500 mg tab. 4 + 4$o6 6 hr x 3 d(70)
d6m%lb#gl 2-3 f (
2 l*%$62*j)(69) Liver fluke : 25 mg/kg PO q 4-6 hr
(70)
day 1: 50 mg, day 2: 50 mg q 8 hr, H. nana, H. diminuta : 2 g PO x 3 d
2
day 3: 100 mg q 8 hr) &jg' f #+6 1 g PO q 24 hr x 6
(69)
3 6 1 f '5$g m
microfilariae ti5*662'++6
Loiasis : 9 mg/kg/day (f2'l q 8
hr) d6m%lb#gl 2-3 f
bl

Asymptomatic carriers : lmt'
b%+ (cumulative dose) 72
mg/kg
2 6 mg/kg weekly x 12
" j 6 mg/kg monthly x 12
j a
Tropical pulmonary eosinophilia
(TPE) : 6 mg/kg PO q 24 hr x 21
(t*eho l& g+be 6-12
mg/kg PO q 24 hr x 21-30 )
Absorption 80%(70)
4-5 mcg/mL *'%5 10 mg/kg 0.83 mcg/mL *'%5
Cmax
af* 3
gd+' 40 mg/kg (#5'2')(70)
#f2'5$g6 Hydrocele, liver, kidneys, adrenal
%m6aa$ glands, pituitary gland, lymph nodes
6 ti *$g 6 f * ' 5$g # e
Metabolism diethylcarbamazine-N-oxide, 1-ethyl
carbamyl-4-methyl piperazine
10-20% (unchanged) +
Urine excretion 80% (metabolites)(70)
3-11% (metabolites)
t la## 8
gd+' 0.8-3
gd+'(70)
#'bl
a+2#'(69) a+2#'(70)
d4a#
a+2#'(70)
#'bl
a+2#'(69) f#2l%+%'l
l moderate to
d4#
severe liver impairment
Pregnancy cat. X B(69) B(70)
GI side effects
2 4*jga m$6 GI side effects (&a 3-4%)
2 CNS side effects
2 $%,
, jg (l65$g+$& 67 aj 4*jga m$6, jg, 5 '2 ' ' $ 6 , '2 'h + (* ' %56
(69)
6i2 m +m 4*jg a ni 6a+2 4 b b$g 6 &%j
5'1f')(17) CNS side effects
2 $%, 5'5$g$g64jg'm)(70)
(17)
$%, '$6, '2'h+ '$6, '2'h+(69) 4gjo4g#, a+265'
(17, 70)
ADRs
Allergic reactions
2 4+, njg njg , 4 , 4 5 Cardiac side effects (+$6'
hg ' m **2 6 foreign (pruritus ani)(69) bradycardia, arrhythmia, AV blocks,
proteins m microfilariae 5$gti5*6 ectopic rhythms, ventricular
(17) (70)
fibrillation)
Encephalitis, retinal hemorrhage

1506 424
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&a l ni 65$g # &67 Loa loa
ADRs jg'm microfilariae ti5*662'
++6
l niclosamide 2+ alcohol l praziquantel 2 +
& g+ih+ niclosamide 5l CYP450 inducers (
2 rifampicin,
ADRs a m'#'*$*$g6'jg+ antiepileptics) % 6
f**"(69) praziquantel **'(70)
Drug interaction
l praziquantel 2 +
CYP450 inhibitors (
2 azole
antifungals, macrolides) %6
praziquantel i'bo(70)
Niclosamide l
intestinal +l
praziquantel l
cestode infections 52o jg'm6 ocular cysticercosis &%+jg&67
2a|&% adult forms f*%ih+ ti5*6 m% 6d4t5l#
m5' a 6 ( a(17, 70)
tissue cestode infections a+2a
2 +l
praziquantel lni5$g+$%#
cysticercosis, echinococcosis)(69) epilepsy &%& g+4+$g6'#2
Niclosamide e drug of choice l
(70)
&67 #j (T. saginata) Praziquantel +$b+ f*%e65$g
d6+$% 57 &i't' 90%(69) i4+
joa$ (hygroscopic) m'+
l&67 #j+i (T. solium) 6i2lif film-coated tablets(70)
#'l6t26
2 magnesium sulfate,
+6#1 electrolyte-polyethyleneglycol 6l
2
g d+' &jg 2 'b &67
&%a+2l6t26 &67 m%ti626
l2'6f*%m autoinfection a
(69)
+% T. solium lni5$g

m+$ neurocysticercosis +2
praziquantel jg'm5l
a6
2(69)
l
a62'*6lf*%w '+$
4"(69)
if6f*% Tablets : 50 mg, 300 mg chewable tablets : 500 mg Tablets : 600 mg

4+f'5$g+$l
%5a56
#NHRT%&fMv\PITMSdTP
AAD : antibiotic-associated diarrhea CAP : community-acquired pneumonia

AECB : acute exacerbation of chronic bronchitis CPK : creatine phosphokinase
AMGs : aminoglycosides CRE : carbapenem-resistant Enterobacteriaceae
AmpC : AmpC beta-lactamases cSSSIs : complicated skin and skin structure infections
BSIs : bloodstream infections DOT : directly observed treatment

1506 424
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DRESS : drug reaction with eosinophilia and systemic MRSA : methicillin-resistant Staphylococcus aureus
symptoms MRSE : methicillin-resistant Staphylococcus epidermidis
DRSP : drug-resistant Streptococcus pneumoniae MSSA : methicillin-sensitive Staphylococcus aureus
ESBL : extended spectrum beta-lactamases MRSE : methicillin-sensitive Staphylococcus epidermidis
FQs : fluoroquinolones NMJ : neuromuscular junction
GABHS : group A beta-hemolytic streptococci (Streptococcus NTM : non-tuberculous Mycobacterium
pyogenes) PBPs : penicillin-binding proteins
G-CSF : granulocyte-colony stimulating factor PCP : Pneumocystis jiroveci pneumonia
GISA : glycopeptides-intermediate Staphylococcus aureus PEK : Proteus mirabilis, Escherichia coli, Klebsiella
GNB : Gram-negative bacteria, Gram-negative bacilli pneumoniae
GVHD : graft-versus-host disease PRSP : penicillin-resistant Streptococcus pneumoniae
HAP : hospital-acquired pneumonia PSSP : penicillin-sensitive Streptococcus pneumoniae
HD : hemodialysis SSTIs : skin and soft tissue infections
HEN : Haemophilus influenzae, Enterobacter aerogenes, UDP : uridine diphosphate
Neisseria spp. URIs : upper respiratory tract infections
IBW : ideal body weight UTIs : urinary tract infections
IE : infective endocarditis VAP : ventilator-associated pneumonia
KPC : Klebsiella pneumoniae carbapenemase VISA : vancomycin-intermediate Staphylococcus aureus
LRTIs : lower respiratory tract infections VRE : vancomycin-resistant enterococci
MDR : multidrug-resistant VRSA : vancomcyin-resistant Staphylococcus aureus
MKD : mg/kg/day
ITMTO$T_$
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