MEERA KHASHSHAN

Cell Wall Synthesis Inhibitors

Penicillin
Natural penicillin β-lactamase resistant Broad spectrum Extended spectrum

Examples penicillin G, penicillin V Oxacillin, Cloxacillin, Dicloxacillin, Ampicillin, Amoxicillin Carbenicillin, Ticarcillin,
Flucloxacillin, Methicillin Mezlocillin, Piperacillin
ROA penicillin G→ IM, IV IV, oral Oral IM, IV
penicillin V→ oral Or IM (ampicillin)
Spectrum Gram +ve spp “streptococcus staphylococcus aureus, minimal to Effective against Gram +ve Pseudomonas and Gram –ve
pneumonia, streptococcus pyogenes”. no activity against Gram -ve and –ve bacteria. used to bacteria
And few Gram –ve cocci “Treponema bacteria treat: pharyngitis, sinusitis.
pallidum, Neisseria gonorrhoeae” Amoxicillin→ prophylaxis of
infective endocarditis, peptic
ulcer
B-lactamase Yes No Yes Yes
susceptibility
Notes Short half-life, when combined with Unlike MRSA, MSSA can be treated They are combined with clavulanic acid or sulbactam to cover
Benzathine or Procaine→ longer half- by methicillin (may cause B-lactamase producing becteria
life nephrotoxicity)

Natural Penicillin
Penicillin G, Benzyl-penicillin, Penicillin V, Phenoxymethylpenicilln Penicillin G derivatives
crystalline penicillin
ROA Parenteral route (IV or IM) Enteral route (given orally) Parenteral route (IM)
Duration of action Short: 30 min Short: 30-60 min Very long duration of action+
Spectrum Narrow: active against G+ bacteria Narrow: active against G+ bacteria
Notes - Benzathine penicillin G is given as depot injection-
Duration of action is 2-4 weeks
-Procaine penicillin- Duration of action is 1-2 days

Indications Gram +ve spp “streptococcus pneumonia, streptococcus pyogenes”. And few Gram –ve cocci “Treponema pallidum, Neisseria gonorrhoeae”
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Cephalosporin
Generation 1st 2nd 3rd 4th 5th
Examples Cephalexin (oral), Cefaclor, cefuroxime Cefotaxime (IV+IM), Cefepime (IV+IM) Ceftraroline (IV+IM)
cephazolin (IV) (cross BBB) ceftriaxone(IV+IM, ↑ h1/2,
cross BBB), cefixime(PO),
ceftazidime
(antipseudomonal activity)
Spectrum GP -More GN (Salmonella -More GN (E.coli, Salmonella Broad spectrum against Broad spectrum against
enterica) enterica, Hemophilus both GP and GN both GP and GN
-less GP influenza)
-less GP (Staphylococcus
aureus (bone infections),
Streptococcus pneumonia)
Therapeutic Uses Streptococcus 1st generation+ meningitis+pneumonia, 1st +3rd generations+ MRSA
pharyngitis (strep salmonella (typhoid typhoid fever, UTI infection, nosocomial infections,
throat), fever), E. coli Gonorrhea, bone infections anti-pseudomonal
MSSA,Pneumonia, 2nd
line for UTI
Pregnancy Category B B B B B

Notes good alternative for

penicillin G

Carbapenems Monobactams Vancomycin Bacitracin

Examples Imipenem & Doripenem Aztreonam
ROA parenterally [IV infusion or IV or inhalational (cystic Oral (pseudomembranous topically
bolus] fibrosis) colitis), IV infusion
Spectrum Broad spectrum against both Against GN bacteria only (E. Against GP bacteria only Against GP bacteria only
GP and GN Coli, P. aeruginosa)
Indications Anaerobic bacteria, E. coli, P. aeruginosa MRSA Skin infections
Pseudomonas aeruginosa,
Acinetobacter

Side Effects
B-lactamase resistant penicillins Nephrotoxicity mainly in methicillin
Penicillins Allergy/ GIT upset
Monobactams Allergy/ Superinfection and pseudomembranous colitis
Vancomycin Nephrotoxicity (avoid combination), Anaphylaxis, Pain at injection site, Red man Syndrome (avoided by slow IV infusion or
Diphenhydramine)
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Protein Synthesis Inhibitors

Aminoglycosides Macrolides Lincosamides Tetracyclines Chloramphenicol

Examples Neomycin (topical, oral), Erythromycin, Lincosamide, Clindamycin Tetracycline,
Gentamycin, Amikacin , Clarithromycin, Doxycycline,
Streptomycin (TB) Azithromycin, Minocycline ( cross
Fidaxomicin BBB), Tigecycline
Oral (all)
Spectrum aerobic GN ( Broad spectrum except Broad spectrum, GP bacteria broad spectrum, Broad spectrum including
Pseudomonas, Klebsiella) fidaxomycin except Clostridium Difficile more on GP anaerobes

Therapeutic Uses Septicemia (in alternative of penicillin Osteomyelitis, against Chlamydia, peptic brain abscess, meningitis,
combination with in case of penicillin Anaerobes, MSSA and MRSA, ulcer, Acne, Cholera typhoid, paratyphoid,
vancomycin) allergy acne vulgaris, Malaria, salmonella, ocular infection
actinomycetes (Lincomycin) LAST CHOICE

Pregnancy Category D B (Fidaxomicin, CONTRAINDICATED CONTRAINDICATED

Erythromycin, D
Azithromycin)
C (Clarithromycin)
Ribosomal subunit 30s 50s/ fidaxomycin binds 50s 30S 50s
to sigma subunit
Bactericidal/ Bactericidal bacteriostatic but Bacteriostatic Bacteriostatic Bacteriostatic
Bacteriostatic bactericidal in high dose
ROA Parenteral except oral IV or orally (Clindamycin) Oral or IV orally, parenterally (IM or IV)
Neomycine (oral) IM & IV (Lincomycin) (doxycycline, or drops
minocycline)

Aminoglycosides
Macrolides
Fidaxomicin
Clindamycin
Tetracycline, Doxycycline,
Minocycline, Tigecycline
Chloramphenicol
Side Effects
Ototoxicity, Nephrotoxicity (most in Neomycin), Neuromuscular paralysis, Allergy
GI upset, Cholestatic jaundice, Ototoxicity, QT prolongation, contraindicated in hepatic dysfunction
GI upset, Anemia, neutropenia, cross reaction with macrolides, expensive
Risk of pseudomembranous colitis
GI upset, Superinfection & diarrhea, Deposition in growing bones & teeth, Hepatotoxicity, Vestibular problems,
Photosensitivity, Teratogenicity
Aplastic anemia, Bone marrow suppression, Hemolytic anemia in G6PD deficiency, Grey Baby Syndrome, Liver enzyme
inhibition, GI Upset, Superinfections
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Nucleic acid synthesis inhibitors

Flouroquinolones
1st 2nd 3rd 4th
Examples Nalidixic acid Ciprofloxacin Levofloxacin , Ofloxacin Moxifloxacin , Gemifloxacin ,
Delafloxacin
Spectrum mainly against GN , low GP mainly against GN and more GP Same second generation coverage + Delafloxacin: P.aeruginosa,
coverage coverage than first generation more GP such as: streptococci , MSSA , MRSA
Mycobacterium (levofloxacin),
pseudomonas
Therapeutic Uses severe systemic infections of community-acquired pneumonia UTI (except Moxifloxacin) ,
p.aerogenosa, traveler’s prostatitis, respiratory
diarrhea infections

ANTIFOLATE DRUGS
Sulfonamides Trimethoprim Co-trimoxazole
Examples Sulfisoxazole, Sulfamethoxazole, Sulfadiazine trimethoprim + sulfamethaxazole together
(only orally), Silver sulfadiazine (only topically)

Spectrum broad spectrum : GP and GN similar to sulfa drugs but better in UTI
because it has less side effects
ROA Orally, Parenterally, Topically orally Orally, IV
Therapeutic Uses Sulfamethoxazole+ Trimethoprim for Prostatitis, Vaginal infections UTIs, prostatitis, respiratory infections, MRSA
pneumocystis/ sulfonamides+ pyrimethamine ( skin and soft tissues ), Fungal infections
for toxoplasmosis

Side Effects
Flouroquinolones nausea , vomiting , diarrhea, headache , convulsions, Tendon rupture, Peripheral neuropathy, Arrhythmias
Sulfonamides Hypersensitivity “Stevens-Johnson syndrome” ,Crystalluria, Hemolytic anemia, Kernicterus,
Trimethoprim Hyperkalemia, folic acid deficiency
Co-trimoxazole Nephrotoxicity
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Miscellaneous antibiotics

SSS
Metronidazole Linezolid& Daptomycin Polymyxin Methenamine Fosfomycin
Tedizolid
MOA Result in a toxic Protein synthesis Interfere with Bind LPS in outer Formaldehyde Interfere with cell
compound causing inhibitor, bind to 50s membrane membrane formation wall synthesis
DNA fragmentation depolarization
ROA Oral or parenteral IV or inhalation
(polymyxin E)
Spectrum Anaerobes, parasites GP, anaerobes, GP bacteria P.aeruginosa,
enterococci acinetobacter
Indications C.difficle, bacterial MRSA or VRE (not MRSA, VRE Polymyxin E is used Mainly used in Part of the first line
vaginosis first line) in Multi drug management of UTI therapy for UTI and
resistant (MDR) when urine pH is acute cystitis
bacterial infections reduced
Side effects GI related, dizziness, Serotonin syndrome, Musculoskeletal Very toxic (produce
metallic taste, reversible toxicity Nephrotoxicity &
disulfiram-like myelosuppression neurotoxicity )
reaction

Antituberculosis medications
Isoniazid
MOA Inhibits enzymes that synthesis
mycolic acid
Absorption Oral (100% bioavailability),
parenteral
Side effects Rash, fever, drug-induced SLE,
vitamin B6 deficiency, hepatitis,
jaundice, make OCP ineffective
Rifampin
Block RNA polymerase
Oral, parenteral
Hepatitis, rash, fever, GI upset, make
OCP ineffective, orang discoloration
of body fluids into orange color

Initial phase Continuation phase

2 months 4 months
Rifampin, isoniazid, pyrazinamide, Rifampin. Isoniazid
ethambutol
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Disease Bacteria Treatment

Pneumonia Streptococcus pneumoniae Penicillin, Ampicillin, Amoxicillin, Cefotaxime,
ceftriaxone, cefixime
Pharyngitis, Strep throat Streptococcus pyogenes Penicillin, Ampicillin, Amoxicillin, Cephalexin,
cephazolin
Gonorrhea Neisseria gonorrhea (STD) Penicillin
Cefotaxime, ceftriaxone, cefixime (DOC)
Syphilis Treponema pallidum (STD) Penicillin
Peptic ulcer H.pylori Amoxicillin (if allergic→ metronidazole )+
Clarithromycin+ proton pump inhibitor
(triple therapy)
Tetracycline, Doxycycline, Minocycline,
Tigecycline + metronidazole (quadruple therapy)
Infective endocarditis (prophylaxis) Amoxicillin
Methicillin susceptible Methicillin, Cephalexin, cephazolin , Clindamycin
staphylococcus aureus Levofloxacin , Ofloxacin
(MSSA)
pseudomonas aeruginosa Piperacillin, Cefepime, Imipenem, Doripenem
Cefazidime, Aztreonam, Aminoglycosides,
Ciprofloxacin , ciprofloxacin, Levofloxacin,
delafloxacin, polymyxin
Pseudomembranous colitis Clostridium difficile Vancomycin or Metronidazole (DOC)
Fidaxomicin
UTI Escherichia coli fosfomycin + trimethoprim: first line “DOC”
fluoroquinolone , ciprofloxacin: second line
Cephalexin, cephazolin (2nd line in pregnancy)
Cefotaxime, ceftriaxone, cefixime, cefaclor,
cefuroxime, Aztreonam, Sulfonamides, Co-
trimoxazole
Typhoid fever Salmonella enterica Cefaclor, cefuroxime, Cefotaxime, ceftriaxone,
cefiximess
Pneumonia Hemophilus influenzae Cefotaxime, ceftriaxone, cefixime (DOC)
Erythromycin, Clarithromycin, Azithromycin
Bone infections Staphylococcus aureus Cefotaxime, ceftriaxone, cefixime
Methicillin resistant Vancomycin (DOC)
staphylococcus aureus Clindamycin, Ceftaroline , Tigecycline,
(MRSA) Delafloxacin, Co-trimoxazole (skin and soft
tissues), daptomycin
Nosocomial infections in ICU Acinetobacter Cefepime, Imipenem & Doripenem, polymyxin
Anaerobic bacteria Imipenem & Doripenem, Clindamycin,
Chloramphenicol, metronidazole
VRE Daptomycin
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Disease Bacteria Treatment

traveler’s diarrhea Ciprofloxacin
Mycobacterium infection Levofloxacin
Community acquired pneumonia Levofloxacin , Ofloxacin
chol vulgaris Minocycline, Tigecycline (DOC)
Clindamycin, Tetracycline, Doxycycline,
Malaria Quinine+ Clindamycin
P.aerogenosa Moxifloxacin , Gemifloxacin , Delafloxacin
Cystitis Flouroquinolones except Moxifloxacin
Prostatitis Flouroquinolonesv, Trimethoprim, Co-
trimoxazole
Toxoplasmosis Pyrimethamine+ Sulfonamides (DOC)
Cholera Doxycycline (DOC)
Vaginal infections (vaginitis) Trimethoprim
Fungal infections pneumocystis jirovecii Trimethoprim+ sulfamthoxazole “co-
trimoxazole”(DOC)
Klebsiella Aminoglycosides
Chalmydia Doxycycline (DOC)
azithromycine
Actinomycetes infection Lincomycin
Osteomyelitis Clindamycin
Meningitis Cefotaxime, ceftriaxone, cefixime (DOC)
Cefaclor, cefuroxime
Septicemia Aminoglycosides with Vancomycin
Neuromuscular paralysis Neostigmine
Skin infections Bacitracin+ Polymyxin B+ Neomycin
Bacterial vaginosis metronidazole
Tuberculosis Mycobacterium tuberculosis Isoniazid and rifampin
Acute cystitis Fosfomycin
Multi drug resistant (MDR) Polymyxin E
bacterial infections
 MEERA KHASHSHAN

VERY IMPORTANT

 Alternative for penicillin (penicillin resistant patient) : 1st generation cephalosporins

 In case of penicillin allergy: macrolides (erythromycin mainly)
 Peptic ulcer patients that are allergic to penicillin: quadruple therapy instead of triple therapy
 Gray baby syndrome, hemolytic anemia in G6PD deficiency, aplastic anemia are associated with
chloramphenicol
 Very high risk of pseudomembranous colitis: clindamycin )‫(بقتل كل البكتيريا وبخليها تاخد راحتها لحالها بالفلورا‬
 Liver enzyme inhibitors: clarithromycin, erythromycin, chloramphenicol, ciprofloxacin(→high
concentration of warfarin and more bleeding)
 Liver enzyme inducer: rifampin
 Contraindicated in pregnancy: aminoglycosides, tetracyclines, chloramphenicol, trimethoprim (first
trimester)
 Best to cross BBB and treat meningitis: 3rd generation cephalosporins
 Tetracyclines are bacteriostatic even in high doses
 Aminoglycosides, 4th generation of fluoroquinolones, Sulfonamides are excreted unchanged in
urine→ used in UTI
 Ceftazidime and Cefaprazon are the only drugs from the 3rd generation that treat pseudomonas
aeruginosa
 In cephalosporins, as we go down the generations the GN bacteria is covered more. In
fluoroquinolones as we go down the generations the GP bacteria is covered more
 Ciprofloxacin is used for treatment and prevention of traveler’s diarrhea
 Cefepime, imipenem, doripenem, polymyxin treat nosocomial pneumonia while ofloxacin,
levofloxacin treat community acquired pneumonia
 Moxifloxacin is the only fluoroquinolone that isn’t used to treat UTI because it’s extensively
metabolized in liver
 QT prolongation is caused by moxifloxacin and macrolides
 Tendonitis and tendon rupture is caused by 4th generation of fluoroquinolones
 Food interaction happens with: 4th generation of fluoroquinolones, tetracyclines
 Aminoglycosides+ penicillin→ synergistic effect
 Cefuroxime is the only 2nd generation cephalosporins that cross BBB
 Imipenem+ cilastatin→ reduce nephrotoxicity
 To avoid red man syndrome (caused by vancomycin) administrate the drug slowly infusion and give
antihistamine drugs such as Diphenhydramine
 Aminoglycosides (post antibiotic effect) and daptomycin are given as single large dose because they
are concentration dependent
 Macrolides aren’t favored in UTI treatment because they have very minimal percent excretion in
urine (except for Clarithromycin, which has a little bit high value)
 Lincosamides, Chloramphenicol, Carbapenems are effective against anaerobes
 Tetracyclins, flouroquinolones shouldn’t be given with metals or dairy products
 Taken on an empty stomach: tetracyclines, isoniazid
 When methylation to 50s happens, the bacteria is resistant to both macrolides and lincosamides
because they bind in the same place
lincosamides ‫ ما بنقدر نعطيه‬macrolides ‫ لل‬resistance ‫يعني لو مريض عنده‬
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 Tetracyclines are contraindicated in children less than 8 years (to avoid teeth discoloration)
 Absorption of 4th generation of flouroquinolones is decreased if given with Ca, Fe & Al
 Sulfonamides have antiparasitic activity: sulfonamides with pyrimethamine→ DOC in toxoplasmosis
 Sulfonamides may cause steven Johnson syndrome, they are contraindicated in neonates (cause
kernicterus and neonates have undeveloped BBB)
 Metallic taste and disulfiram-like reaction are associated with Metronidazole
 Linezolid and tedizolid are not concentration dependent→ give the same dose in oral or parenteral
administration
 Daptomycin is not used for pneumonia because it’s antagonized by surfactant
 Rifampin turns body fluids into orange so patients should wear glasses instead of contact lenses
 Isoniazid antidote is pyridoxine, there is no antidote for rifampin
 Rifampin in never used as a single agent in treating active TB
 Rifampin should be replaced with rifabutin in case of HIV positive patients
 Methenamine is not co-administered with sulfonamides. They will bind to each other & none of them will
be effective.

“Pharmacology is benefited by the prepared mind. You need to know what you
are looking for” - Siddhartha Mukherjee
🙂 ‫ناس‬ ‫ دوا كويس ورخيّص وابن‬:‫تذكروا احنا دايما بندور على‬