ANTI-INFECTIVE DRUGS

1
 ANTIMICROBIALS
2
Antibacterials
Antivirals
Antifungals
Antiparasitics

Antimalarials
Antiprotozoals
Antituberculosis
 ANTIMICROBIALS
3
 ANTIMICROBIALS
4

Medications that prevent and treat

infections, vital to the health and well-
being of the society

Often assist the body’s defenses and

manage infections caused by bacteria,
viruses, and parasites
 BACTERIA AND ANTIBACTERIALS
5

Bacteria are microorganisms that invade

the human body through many routes like
the respiratory, gastrointestinal, and the
skin

Human immune response is activated once

bacteria invade the body.
As the body tries to rid itself of bacteria,
classic signs of inflammation, fever, and
lethargy begin to show up.
 BACTERIA AND ANTIBACTERIALS
6

The goal of antibiotic

therapy is to decrease
the population of
invading bacteria to a
point at which human
immune system can
effectively deal with the
invader
 BACTERIA AND ANTIBACTERIALS
7
ESTABLISHING THE PRESENCE OF
INFECTION

Before initiating antibiotic therapy, it is

important to establish the presence of an
infectious process

The isolation of an organism from a clinical

specimen does not always indicate the
presence of infection or mandate anti –
infective therapy
 BACTERIA AND ANTIBACTERIALS
8
A. NORMAL FLORA,
CONTAMINATION, COLONIZATION,
OR INFECTION

1. The human body harbors a number

of microorganisms that colonize
certain body systems called “normal
flora”, which are normally harmless
bacteria that occur naturally on the
skin, and in the respiratory,
gastrointestinal, and genitourinary
tracts.
 BACTERIA AND ANTIBACTERIALS
9
 Normal flora bacteria are located in
anatomic sites where pathogenic organisms
can cause disease. They often compete with
pathogenic organisms for nutrients, stimulate
cross – protective antibodies, and suppress
the growth of pathogenic organisms.

 Bacteria that compromise normal flora may

become pathogenic when host defenses are
impaired or when translocated to sterile
body sites during trauma, intravenous line
insertion, or surgery
 BACTERIA AND ANTIBACTERIALS
10

 Indiscriminate use of antibiotics can

alter or eradicate the protective
normal bacterial flora

 Patients who are hospitalized for more

than 48 hours can have their usual
normal flora replaced by the “normal
flora” of the hospital, which tend to be
gram – negative aerobes
 BACTERIA AND ANTIBACTERIALS
11
 BACTERIA AND ANTIBACTERIALS
12
SITES OF NORMAL FLORA COLONIZATION

SKIN UPPER RESPIRATORY TRACT

Diphtheroids (Corynebacterium sp) Bacteroides spp
Propionibacteriraceae Haemophilus spp
Bacillus sp Neisseria spp
Staphylococci Streptococci (anaerobic)
Streptococci

GASTROINTESTINAL TRACT GENITOURINARY TRACT

Bacteroides spp Lactobacillus spp
Clostridium spp Corynebacterium spp
Enterobacteriaceae (E. coli, Klebsiella spp) Enterobactriaceae – esp E. coli
Streptococci (anaerobic) Staphylococci (S. saprophyticus)
Enterococcus spp Streptococci
Fusobacterium spp
 BACTERIA AND ANTIBACTERIALS
13 2. BODY SITES THAT ARE STERILE include
the bloodstream, CSF, pleural fluid,
peritoneal fluid, pericardial fluid, synovial
fluid, bone, and urine (taken directly from
the bladder)

3. The isolation of an organism from a clinical

specimen does not always represent the
presence of infection – clinicians must
consider the clinical, laboratory and
radiographic evidence available to
differentiate between contamination,
colonization, or infection
 BACTERIA AND ANTIBACTERIALS
14
CONTAMINATION – an organism is
introduced into the clinical specimen
during the sample acquisition process.

EXAMPLE: isolation of coagulase negative

staphylococci in the blood of a patient
where blood was drawn via a peripheral
stick and the patient does not have signs
of infection (normal skin flora bacteria
contaminated the blood culture)
 BACTERIA AND ANTIBACTERIALS
15
COLONIZATION – an organism is
present at a body site but is not
invading hot tissue or eliciting host
responses

EXAMPLE: isolation of Pseudomonas

aeruginosa in a patient without fever,
cough, or infiltrate on chest x – ray
(pathogenic bacteria in patient
without clinical/radiologic signs of
pneumonia)
 BACTERIA AND ANTIBACTERIALS
16

INFECTION – a pathogenic organism is

present at a body site and is damaging
host tissues and eliciting host responses
and symptoms consistent with
infection.

EXAMPLE: isolation of Streptococcus

pneumoniae in the CSF of a patient
with fever, headache, photophobia,
and neck stiffness
 BACTERIA AND ANTIBACTERIALS
17
4. CLINICAL SIGNS OF INFECTION

LOCALIZED SYSTEMIC
Pain Fever
Inflammation Chills, rigors
Swelling Tachycardia
Erythema Tachypnea
Purulent discharge Malaise
Sputum production Hypotension
Cough Mental status changes
Abnormal discharge
 BACTERIA AND ANTIBACTERIALS
18
5. LABORATORY signs suggestive of
infection include:

 Elevated WBC count (peripheral

[leukocytosis] and at site of infection)
with a left shift
 Positive gram stain and culture
 Elevated erythrocyte sedimentation
rate (ESR) or C – reactive protein
(CRP)
 Positive antigen or antibody titers
 BACTERIA AND ANTIBACTERIALS
19

6. RADIOGRAPHIC signs of infection

 Infiltrate on chest x – ray in

patients with pneumonia
 Periosteal elevation and bony
destruction on a bone x – ray in a
patient with osteomyelitis
 BACTERIA AND ANTIBACTERIALS
20
7. ASSESSMENT OF THE SEVERITY OF THE
INFECTION

o Severity of patient’s infection is based on the

degree of abnormality in the parameters
mentioned
o Significant alterations in cardiac, respiratory
and CNS parameters may signify a serious,
life – threatening infections
o Severity of infection may influence the
choice, route of administration and dose of
antibiotics used
 BACTERIA AND ANTIBACTERIALS
21
8. COMMON BACTERIAL PATHOGENS BY SITE
OF INFECTION
Certain bacteria have a propensity to
commonly cause infection in particular body
sites or fluids
This information is used to guide the choice of
empiric antibiotic therapy before the results of
the gram stain, culture, and susceptibility
results are known. An antibiotic is empirically
chosen that has a spectrum of activity that
covers the most common causative bacteria at
the patient’s suspected infection site.
 BACTERIA AND ANTIBACTERIALS
22
NARROW SPECTRUM: the antibiotic has
activity against a limited group of bacteria
(eg. Penicillin has activity against some gram
– positive and gram – negative cocci, but not
gram – negative bacilli)

BROAD SPECTRUM: the antibiotic has activity

against a wide variety of bacteria, such as
gram – positive and gram – negative (eg.
Imipenem has activity against gram – positive
and gram – negative aerobes and anaerobes)
 HOW ANTIBIOTICS ARE USED
23

A. The treatment of infectious diseases is quite

different than other disease states requiring
drug therapy in a number of ways:
Antibiotics can be used to treat a suspected or
documented infection, or can be used to prevent
an infection from occurring in high – risk
patients
Anti – infective therapy is typically given for a
limited duration of therapy or a particular
number of days based on previous clinical data
for that infection type
 HOW ANTIBIOTICS ARE USED
24
B. EMPIRIC THERAPY
Antibiotics are administered that have activity against
the pathogens most likely causing a patient’s infection
based on the signs and symptoms of infection.
The site of infection may or may not be known, and
the culture results are pending, negative, or
unobtainable.
EXAMPLE: antibiotics are started in a patient with
community – acquired pneumonia who is unable to
expectorate a sputum sample; patient presents to the
hospital with signs of bacterial meningitis and
antibiotics are started after lumbar puncture
 HOW ANTIBIOTICS ARE USED
25
C. DIRECTED OR TARGETED THERAPY
Antibiotics are used to treat an established
infection where the site of infection, causative
pathogen, and antibiotic susceptibilities are
known.
EXAMPLE: a patient has bacteremia with
methicillin – susceptible Staphylococcus aureus
and is receiving intravenous nafcilin therapy
Antibiotic therapy is selected based upon the
susceptibility results of the infecting pathogen, and
is typically changed from the empiric antibiotic
originally chosen to a more narrow – spectrum
agent directed toward the pathogen
 HOW ANTIBIOTICS ARE USED
26
D. PROPHYLACTIC THERAPY
Antibiotics are given to prevent the development
of infection during a procedure or
immunocompromised state when there is a
considerable risk of infection
EXAMPLES: antibiotics are given prior to surgical
procedures to prevent surgical site infections
Prophylaxis is administered for as long as the
patient is at risk, such as single dose antibiotic
therapy for surgical/dental prophylaxis or longer
durations of antibiotic therapy during
immunosuppressive states
 HOW ANTIBIOTICS ARE USED
27
E. COMBINATION THERAPY – may be
selected in a limited number of
circumstances for the treatment of infection:
To provide coverage against all organisms in a
mixed, polymicrobial infection where a single
antibiotic does not cover all the infecting
organisms – used to broaden bacterial
coverage
To take advantage of synergistic properties
when the antibiotics are used together
To decrease the emergence of resistance – only
for tuberculosis
HOW ANTIBIOTICS ARE USED
28
SYNERGY – the activity of the antimicrobial
combination is greater than that expected
from the additive activity of the individual
antimicrobials
(A+B) > A + B
EXAMPLE: ampicillin and gentamicin are
administered together in the treatment of
Enterococcal endocarditis in order to produce
bactericidal activity and achieve successful
eradication of the infection (alone, each agent
is bacteriostatic against Enterococcus)
 HOW ANTIBIOTICS ARE USED
29

ADDITIVE – the activity of the antimicrobial

combination is no greater than the sum of the
effects of each individual component (no
greater and no worse)

ANTAGONISM – the activity of the

antimicrobial combination is less than that
expected from the additive activity of the
individual antimocrobials
 ANTIBACTERIAL ACTIVITY
30

BACTERIOSTATIC – antimicrobial agents that

inhibit the growth of susceptible bacteria and
rely on host defenses to help kill the bacteria
and subsequently eradicate the infection.

Normal host defenses are required for clinical

success of bacteriostatic agents, used with
caution in immunocompromised patients.
Macrolides, ketolides, tetracyclines,
sulfonamides, clindamycin
 ANTIBACTERIAL ACTIVITY
31

BACTERICIDAL – antimicrobial agents that

kill susceptible bacteria in the absence of
host defenses.
Bactericidal activity is considered essential
in the treatment of infections located in
sites where host defenses are not adequate
including the meninges, heart valves, and
bone, and in patients with impaired host
defenses.
Aminoglycosides, vancomycin,
fluoroquinolones, metronidazole
 COMMON ADVERSE REACTIONS
32

The most common adverse effects are

due to the direct action of the drug in
the following organ – systems

NEPHROTOXICITY
Antibiotics that are metabolized and
excreted in the kidney most frequently
cause kidney damage
 COMMON ADVERSE REACTIONS
33

GASTROINTESTINAL TOXICITY
Direct toxic effect to the cells of the GI
tract can cause nausea, vomiting,
stomach pain, and diarrhea.

HEPATOTOXICITY
Some drugs are toxic to liver cells and
can cause hepatitis or liver failure
 COMMON ADVERSE REACTIONS
34

CNS TOXICITY

When drugs can pass through the

brain barrier and can
accumulate in the nervous tissues,
they can interfere with neuronal
function
 COMMON ADVERSE REACTIONS
35

HYPERSENSITIVITY

Most protein antibiotics can induce

the body’s immune system to
produce allergic responses.

Drugs are considered foreign

substances and when taken by the
individual, it encounters the body’s
immune cells
 COMMON ADVERSE REACTIONS
36
SUPERINFECTIONS

Opportunistic infections that develop

during the course of antibiotic therapy

Antimicrobial drug suppresses part of the

normal flora, susceptible to drug

Drug resistant organism proliferates to

an extent which allows an infection to be
established
37
CLASSIFICATION OF ANTIBIOTICS
 AMINOGLYCOSIDES
38

A group of antibiotics indicated for

infections caused by gram – negative
aerobic bacilli

They were replaced by newer, less toxic

drugs in treating less serious infections
because these drugs have potentially
serious adverse effects
 AMINOGLYCOSIDES
39
THERAPEUTIC ACTION

Exert bactericidal effect through

inhibition of protein synthesis in
susceptible strains of gram – negative
bacteria.

They bind to a unit of the bacteria

ribosomes and cause misreading of the
genetic code leading to cell death
 AMINOGLYCOSIDES
40
INDICATIONS

 Infections caused by susceptible strains:

Pesudomonas aeruginosa, Escherichia coli,
Proteus sp., Klebsiella – Enterobacter –
Serratia group, Citrobacter sp, and
Staphylococcus sp.

 Serious infections susceptible to penicillin

when penicillin is contraindicated
 AMINOGLYCOSIDES
41
POINTS TO REMEMBER

CHILDREN
Age group very sensitive to GI and
CNS adverse effects of antibiotics

Monitor nutritional and hydration

status while on therapy

Superinfection: Oral candidiasis

 AMINOGLYCOSIDES
42
ADULTS

They have the tendency to cure simple

manifestations with antibiotics

Educate them that antibiotics are effective

only for certain bacteria and not for simple
manifestations like common colds, which
may be viral

Storage of unused pills for future infections

 AMINOGLYCOSIDES
43

OLDER ADULTS

Assessing the problem and obtaining

appropriate specimens for culture is
especially important with the population

Older patients may be more susceptible

to adverse effects of antibiotic therapy
 AMINOGLYCOSIDES
44
CONTRAINDICATIONS AND CAUTIONS

Known allergy to aminoglycosides

Renal or hepatic disease can be

exacerbated by aminoglycosides and may
interfere with metabolism and excretion
of these drugs

Preexisting hearing loss can be intensified

by toxic drug effects on the auditory
nerve
 AMINOGLYCOSIDES
45

Active infection with herpes or

mycobacterial infections can be
worsened by the effects of an
aminoglycoside on normal defense
mechanisms

Myasthenia gravis or parkinsonism can

be exacerbated by the effects of a
particular aminoglycosides on the
nervous system
 AMINOGLYCOSIDES
46
Lactation. Aminoglycosides are excreted
in the breastmilk and can potentially
cause serious effects in the infant.

Amikacin should not be used for longer

than 7 – 10 days because it is
particularly toxic to the bone marrow,
kidneys, GI

Streptomycin is only for special situations

because it is very toxic to the 8th cranial
nerve & kidney
 AMINOGLYCOSIDES
47
ADVERSE EFFECTS

CNS
ototoxicity, irreversible deafness,
vestibular paralysis, confusion,
depression, disorientation,
numbness, tingling, weakness

RENAL
Renal failure
 AMINOGLYCOSIDES
48

HEMATOLOGY
bone marrow depression
leading to immunosuppression
and resultant superinfections

GASTROINTESTINAL
nausea, vomiting, diarrhea,
weight loss, stomatitis,
hepatotoxicity
 AMINOGLYCOSIDES
49

CARDIOVASCULAR
palpitations, hypotension,
hypertension

HYPERSENSITIVITY REACTIONS
purpura, rash, urticaria,
exfoliative dermatitis
 AMINOGLYCOSIDES
50
INTERACTIONS
Drug to drug interactions involved in
aminoglycoside use:
Penicillins, cephalosporins, ticarcillin:
synergistic bactericidal effect
Diuretics: increased incidence of
ototoxicity, nephrotoxicity, and
neurotoxicity
Anesthetics, nondepolarizing NM
blockers, succinylcholine, citrate
anticoagulated blood: increased NM
blockade with paralysis
 CARBAPENEMS
51

These are a relatively new class of broad –

spectrum antibiotics effective against gram
– positive and gram – negative bacteria

THERAPEUTIC ACTION
Bactericidal effect by inhibiting cell
membrane synthesis in susceptible bacteria
leading to cell death
 CARBAPENEMS
52
INDICATIONS

Serious intraabdominal, urinary tract, skin

and skin structure, bone and joint, and
gynecological infections

Infections caused by susceptible strains: S.

pneumoniae, H. influenza, E. coli, K.
pneumoniae, P. aeruginosa
 CARBAPENEMS
53
CONTRAINDICATIONS AND
CAUTIONS

o Known allergy to carbapenems or

beta – lactams
o Seizure disorders exacerbated by
drugs
o Meningitis where safety is not
established
o Lactation is not known whether drug
can cross into breast milk or not
 CARBAPENEMS
54
CONTRAINDICATIONS AND
CAUTIONS

o Known allergy to carbapenems or

beta – lactams
o Seizure disorders exacerbated by
drugs
o Meningitis where safety is not
established
o Lactation is not known whether drug
can cross into breast milk or not
 CARBAPENEMS
55

ADVERSE EFFECTS

GI: pseudomonas colitis, C. difficile

diarrhea, nausea, vomiting, dehydration
and electrolyte balance

CNS: headache, dizziness, altered mental

state

Superinfections
 CARBAPENEMS
56
INTERACTIONS

Valproic acid: carbapenems reduce

serum valproic acid and this can
increase risk of seizures

Imipenem and ganciclovir can cause

seizures

Meropenem and probenecid can lead

to toxic levels of meropenem
 CEPHALOSPORINS
57

First introduced in the 1960s

There are currently four generations

of cephalosporins, each with specific
spectrum of activity

These are similar drugs in structure

and activity
 CEPHALOSPORINS
58

THERAPEUTIC ACTION

Exert bactericidal and bacteriostatic

effects by interfering with the cell –
wall building activity of bacteria
during cell division.

They prevent the bacteria from

biosynthesizing the framework of their
cell walls
 CEPHALOSPORINS
59

INDICATIONS

FIRST GENERATION cephalosporins

are effective against the same
gram positive bacteria affected by
penincillin G, as well as gram –
negative bacteria P. mirabilis, K.
pneumoniae, E. coli
 CEPHALOSPORINS
60

INDICATIONS

SECOND GENERATION
cephalosporins are effective against
previously mentioned strains as well
as H. influenza, Neisseria spp. These
are less effective against gram
positive bacteria
 CEPHALOSPORINS
61

INDICATIONS

THIRD GENERATION
cephalosporins are effective against
all of the previously mentioned
strains.
They are relatively weak against
gram – positive against gram –
negative bacilli
 CEPHALOSPORINS
62

INDICATIONS

FOURTH GENERATION
cephalosporins are active against
gram – negative and gram –
positive organisms, including
cephalosporin – resistant
staphylococci and P. aeruginosa
 CEPHALOSPORINS
63
CONTRAINDICATIONS AND
CAUTIONS

Known allergy to cephalosporins and

beta lactams. Cross – reactions are
common.

Hepatic or renal impairment. These

drugs are toxic to the kidneys and could
interfere with the metabolism and
excretion of the drugs
 CEPHALOSPORINS
64

Pregnancy and lactation. Potential effects on

the fetus and infant are not known; use only
if benefits clearly outweigh the potential risk
of toxicity to the fetus or infant

Reserve cephalosporins for appropriate

situations because cephalosporin – resistant
bacteria are appearing in increasing
numbers. Perform culture and sensitivity test
before start of therapy
 CEPHALOSPORINS
65
ADVERSE EFFECTS

GI : nausea, vomiting, diarrhea, anorexia,

abdominal pain, pseudomembranous colitis
CNS : headache, dizziness, lethargy,
paresthesias
Nephrotoxicity in patients who have
predisposing renal insufficiency
Superinfections
Phlebitis and local abscess at the site of IM
injection and/or IV administration
 CEPHALOSPORINS
66
INTERACTIONS
Aminoglycosides : increased risk of
nephrotoxicity
Oral anticoagulants : increased bleeding

Alcohol : avoided for 72 hours after

discontinuation of the drug to prevent
disulfiram – like reaction (flushing,
throbbing headache, nausea and vomiting,
chest pain, palpitations, dyspnea, syncope,
vertigo, convulsions, etc)
 FLUOROQUINOLONES
67

A relatively new synthetic class of antibiotics

with a broad spectrum of activity

THERAPEUTIC ACTION
Interfere with the action of DNA enzymes
necessary for growth and reproduction of
bacteria
Has little cross – resistance but misuse of this
drug for a short time will lead to existence of
resistant strains
 FLUOROQUINOLONES
68

INDICATIONS
Treating infections (respiratory, urinary tract, and
skin) caused by susceptible strains: E. coli, P.
mirabilis, Klebsiella pneumoniae, Proteus
vulgaris, etc

Ciprofloxacin was approved in 2001 for

prevention of anthrax infection in areas that
might be exposed to germ warfare. It is also
effective against typhoid fever
 FLUOROQUINOLONES
69

CONTRAINDICATIONS AND CAUTIONS

Known allergy to fluoroquinolones

Pregnancy and lactation. Potential effects

on the fetus and infant are not known; use
only if benefits clearly outweigh the potential
risk of toxicity to the fetus or infant
 FLUOROQUINOLONES
70

Seizures can be exacerbated by the drug’s

effects on cell membrane channels

Fluoroquinolones are associated with

damage to developing cartilage, therefore
not recommended for growing children
 FLUOROQUINOLONES
71
ADVERSE EFFECTS
GI : nausea, vomiting, diarrhea, dry mouth
CNS : headache, dizziness, insomnia, depression
Immunological : bone marrow depression

Risk for tendinitis and tendon rupture in patients

over age 60, on concurrent steroids, and those
with renal, heart, or lung transplants
Photosensitivity and severe reactions so advise
patient to avoid sun and ultraviolet light
exposure and to use protective clothing and
sunscreens
 FLUOROQUINOLONES
72

INTERACTIONS
Iron salts, sucralfate, mineral supplements,
antacids: increased therapeutic effects of
fluoroquinolones. Administration should be
separated by at least 4 hours.

Quinidine, procainamide, pentamidine,

tricyclics, phenothiazines: severe to fatal
cardiac reactions due to increased QT
interval and/or torsades de pointes
 FLUOROQUINOLONES
73

INTERACTIONS

Theophylline: increased theophylline

levels because these two drugs have the
same metabolic effect

Steroids: increased CNS stimulation

 PENICILLINS
74

Penicillin was the first antibiotic introduced

for clinical use.

Various modifications were subsequently

made to address resistant strains and to
decrease drug adverse effects.

Penicillinase – resistant antibiotics were

developed to address penicillin resistant
bacteria
 PENICILLINS
75

THERAPEUTIC ACTION
Exert bacterial effect by interfering with
the ability of susceptible bacteria to build
their cell walls when they are dividing.

These drugs prevent the bacteria from

biosynthesizing the framework of the cell
wall, the bacteria with weakened cell walls
swell and then burst from osmotic pressure
within the cell
 PENICILLINS
76

INDICATIONS

Treatment of streptococcal infections

(pharyngitis, tonsillitis, scarlet fever,
endocarditis)

Treatment of meningococcal
meningitis if given at high doses
 PENICILLINS
77

CONTRAINDICATIONS AND CAUTIONS

Known allergy to penicillins and
cephalosporins

Renal disease. Drug excretion is reduced.

Pregnancy and lactation. No adequate

studies on the effect on fetus but these
drugs can cause diarrhea and
superinfections may occur in the infant.
 PENICILLINS
78
ADVERSE EFFECTS

GI : nausea, vomiting, diarrhea, abdominal

pain, glossitis, stomatitis, gastritis, sore mouth,
furry tongue
Pain and inflammation at the injection site can
occur with injectable forms of the drug

Hypersensitivity reactions : rash, fever,

wheezing, anaphylaxis with repeated exposures
Superinfections, eg. yeast infections
 PENICILLINS
79

INTERACTIONS

Tetracyclines: decrease in effectiveness

of penicillins

Parenteral aminoglycosides:
inactivation of aminoglycosides
 SULFONAMIDES
80
TRIMETHOPRIM-SULFAMETHOXAZOLE

Drugs that inhibit folic acid synthesis

THERAPEUTIC ACTION
The desired and beneficial action is
To inhibit folic acid synthesis required as
precursors of RNA and DNA. They competitively
block paraaminobenzoic acid to prevent
synthesis of folic acid in susceptible bacteria that
synthesize their own folates for the production
of RNA and DNA
 SULFONAMIDES
81
INDICATIONS

Treatment of infections caused by

susceptible strains: Chlamydia trachomatis,
some strains of H. influenza

No longer used much but they remain an

inexpensive and effective treatment of UTIs
and trachoma, especially in developing
countries where cost is an issue
 SULFONAMIDES
82

INDICATIONS

Can also be used in treatment of sexually

transmitted diseases

Sulfasalazine is used in treatment of

ulcerative colitis and rheumatoid
arthritis
 SULFONAMIDES
83
CONTRAINDICATIONS AND CAUTIONS

Known allergy to sulfonamides,

sulfonylureas, or thiazide diuretics. Cross –
sensitivity can occur.

Renal disease. Increased toxic effects of the

drug.

Pregnancy. Can cause birth defects.

Lactation. Increased risk for kernicterus,
diarrhea, and rash in infants.
 SULFONAMIDES
84
ADVERSE EFFECTS

GI : vomiting, diarrhea, abdominal pain,

anorexia, stomatitis, and hepatic injury
Renal : crystalluria, hematuria, proteinuria,
toxic nephrosis

CNS : headache, dizziness, vertigo, ataxia,

convulsions, depression
Bone marrow depression
Dermatological: photosensitivity, rash,
hypersensitivity reactions
 SULFONAMIDES
85

INTERACTIONS

Tolbutamide, tolazamide, glyburide,

glipizide, chlorpropamide : increased risk
for hypoglycemia

Cyclosporine : increased risk of

nephrotoxicity
 TETRACYCLINES
86

Semisynthetic antibiotics based on the

structure of a common soil mold

THERAPEUTIC ACTION
Inhibit protein synthesis leading to inability
of the bacteria to multiply.
The affected protein is similar to protein
found in human cells so these drugs can be
toxic to humans at high concentrations
 TETRACYCLINES
87
INDICATIONS

Treatment of infections caused by

susceptible strains: Rickettsiae, H. influenzae,
Shigella sp

Adjunct in treatment of protozoal infections

 TETRACYCLINES
88
CONTRAINDICATIONS AND CAUTIONS

Known allergies to tetracyclines or to

tartrazine

Pregnancy and lactation. Effect on

developing bones and teeth

Fungal, mycobacterial, or viral ocular

infections. Ophthalmic preparations can kill
both undesired bacteria and normal flora
 TETRACYCLINES
89

CONTRAINDICATIONS AND CAUTIONS

Use in caution in children below age of 8.

Can potentially damage developing bones
and teeth.

Hepatic and renal dysfunction. Drugs are

concentrated in the bile and are excreted in
the urine
 TETRACYCLINES
90
ADVERSE EFFECTS

GI : nausea, vomiting, diarrhea, abdominal

pain, glossitis, dysphagia, fatal hepatotoxicity

Skeletal and bones: weakening in the

structure and causing staining and pitting of
teeth and bones

Dermatological: photosensitivity and rash

Superinfection
 TETRACYCLINES
91
ADVERSE EFFECTS

Local : pain and stinging with topical or

ocular applications
Hematologic: hemolytic anemia, bone
marrow depression

Hypersensitivity reactions: urticarial,

anaphylaxis
Intracranial hypertension
 TETRACYCLINES
92
INTERACTIONS
Penicillin G: decreased effectiveness of
penicillin G
Oral contraceptives: decreased effectiveness
of oral contraceptives and additional form of
birth control is needed

Digoxin: increased digoxin toxicity

Calcium salts, magnesium salts, aluminum
salts, bismuth salts, iron, urinary alkalinizers,
and charcoal: decreased absorption of
tetracyclines
 OTHER ANTIBIOTICS
93

KETOLIDES a class of antibiotics introduced

in 2004 indicated for treatment of mild to
moderate community acquired pneumonia
caused by susceptible bacteria

LINCOSAMIDES are similar to macrolides

but they are more toxic. They are used to
treat severe infections when penicillin or
other less toxic antibiotics cannot be used
 OTHER ANTIBIOTICS
94

LIPOGLYCOPEPTIDES are antibiotics

introduced in 2010. They are used to treat
complicated skin and skin – structure
infections caused by susceptible strains of
gram – positive organisms

MONOBACTAM ANTIBIOTICS are indicated

for treatment of gram – negative
enterobacterial infections
 OTHER ANTIBIOTICS
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MACROLIDES are antibiotics that interfere

with protein synthesis in susceptible bacteria.
They are used to treat respiratory infections
and urethritis in adults and otitis media and
tonsillitis in children.

Erythromycin is the drug of choice for

Legionnaire’s disease and infections caused by
C. diphtheria, Ureaplasma sp, Mycoplasma
pneumonia and chlamydial infections
 OTHER ANTIBIOTICS
96
THERAPEUTIC ACTION

Ketolides and lincosamides block protein

synthesis leading to cell death. Ketolamides
are structurally the same with macrolides.

Lipoglycopeptides inhibit bacterial cell wall

synthesis by interfering with polymerization
and cross-linking of peptidoglycans. They
bind to the bacterial membrance and
disrupt the membrane barrier function
causing bacterial cell death.
 OTHER ANTIBIOTICS
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Macrolides bind to the bacterial cell

membrane and change protein function.
This prevents bacteria from dividing and
cause their cell death.

Monobactam disrupts bacterial cell wall

synthesis and promote leakage of cellular
contents and cell death.
 OTHER ANTIBIOTICS
98
CONTRAINDICATIONS
Ketolides: telithromycin with antiarrhythmics
and antilipidemics can cause serious adverse
effects. It might also cause potentially fatal
respiratory failure in patients with myasthenia
gravis.
Lincosamides: use in caution in patients with
hepatorenal insufficiency. Usage in pregnancy
and lactation is only indicated if benefit clearly
outweighs the risk to the fetus or neonate. The
same is true with lipoglycopeptides,
macrolides, and monobactams.
 OTHER ANTIBIOTICS
99
INTERACTIONS
Ketolides: loss of therapeutic effects if combined with rifampin,
phenytoin, carbamazepine, phenobarbital; increased serum levels of
digoxin and metoprolol; increased GI toxicity with theophylline
Lipoglycopeptides: increased risk for prolonged QT interval if combined
with drugs known to cause prolonged QT interval

Macrolides: food in the stomach decreases absorption of oral macrolides.

Antibiotic should be taken on an empty stomach with a full, 8-oz glass
of water 1 hour before or at least 2-3 hours after meals.
Monobactams: incompatible in solution with nafcillin, cephradine, and
metronidazole.
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
100
NURSING ASSESSMENT
Assess for the mentioned cautions and
contraindications (e.g. drug allergies, CNS depression,
CV disorders, etc.) to prevent any untoward
complications.
Perform a thorough physical assessment (other
medications taken, CNS, skin, respirations, and
laboratory tests like renal functions tests and
complete blood count or CBC) to establish baseline
data before drug therapy begins, to determine
effectiveness of therapy, and to evaluate for
occurrence of any adverse effects associated with
drug therapy.
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
101

Perform culture and sensitivity tests at

the site of infection to ensure
appropriate use of the drug.

Conduct orientation and reflex

assessment, as well as auditory testing
to evaluate any CNS effects of the drug
(aminoglycosides).
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
102
NURSING DIAGNOSES
Acute pain related to GI or CNS drug effects
Deficient fluid volume and imbalanced
nutrition: less than body requirements related
to diarrhea

Disturbed sensory perception (auditory)

related to CNS drug effects
Risk for infection related to bone marrow
suppression (aminoglycosides) and repeated
injections (cephalosporins).
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
103
IMPLEMENTATION WITH RATIONALE

 Check culture and sensitivity reports to

ensure that this is the drug of choice for
this patient.

 Ensure that patient receives full course

of aminoglycosides as prescribed,
divided around the clock to increase
effectiveness and decrease the risk for
development of resistant strains of
bacteria.
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
104

 Monitor infection site and presenting signs and

symptoms throughout course of drug therapy
because failure of these manifestations to
resolve may indicate the need to reculture the
site.

 Provide safety measures to protect the patient

if CNS effects (e.g. confusion, disorientation,
numbness) occur.
 NURSING CONSIDERATIONS FOR ANTIBIOTICS
105

 Educate client on drug therapy to

promote understanding and compliance.

 Provide the following patient teaching:

safety precautions (e.g. changing
positions, avoiding hazardous tasks, ec.),
drinking lots of fluids and to maintain
nutrition even though nausea and
vomiting may occur, report difficulty
breathing, severe headache, fever,
diarrhea, and signs of infection.
 ANTI-
MYCOBACTERIAL
DRUGS

106
 ANTIMYCOBACTERIALS
107
These are antibiotics used in the treatment of
infections caused by pathogens responsible
for tuberculosis and leprosy

Mycobacterium tuberculosis causes

tuberculosis, the leading cause of death from
infectious disease in the world

Mycobacterium leprae causes leprosy or

Hansen’s disease, characterized by disfiguring
skin lesions and destructive effects on the
respiratory tract
 ANTIMYCOBACTERIALS
108

THERAPEUTIC ACTION

Act on the DNA and/or RNA of the

bacteria, leading to lack of growth and
eventually to bacterial death

INDICATIONS
Treatment of tuberculosis and leprosy
 ANTIMYCOBACTERIALS
109

CONTRAINDICATIONS & CAUTIONS

Known allergies to antimycobacterials

Pregnancy. Adverse effects on fetus.

Safest antituberculosis regimen in
pregnancy isoniazid, ethambutol, and
rifampin
 ANTIMYCOBACTERIALS
110

CONTRAINDICATIONS & CAUTIONS

Severe CNS dysfunction. Exacerbated

by the effects of the drug

Hepatic or renal dysfunction. Interfere

with the metabolism and excretion of
drugs
 ANTIMYCOBACTERIALS
111
ADVERSE EFFECTS

CNS: neuritis, dizziness, headache, malaise,

drowsiness, and hallucinations
GI: nausea, vomiting, anorexia, stomach
upset, abdominal pain

Rifampin, rifabutin, and rifapentine can

cause discoloration of body fluids from urine
to sweat and tears. They may stain orange-
tinged and may permanently stain contact
lenses.
 ANTIMYCOBACTERIALS
112
INTERACTIONS

Rifampin and INH in combination: increased

toxic liver reactions

Rifampin and rifabutin with beta blockers,

corticosteroids, OCPs, oral anticoagulants,
methadone, phenytoin, verapamil,
ketoconazole : increased metabolism and
decreased drug effectiveness
 ANTITUBERCULOSIS
113
Caused by a slow growing bacterium called
Mycobacterium tuberculosis.

Tuberculosis (TB) is a disease that has

affected mankind for centuries and dates as
far back as ancient Egyptian times.

The disease is spread by coughing, talking,

spitting or sneezing which spreads the
mycobacteria through the air in tiny
droplets of water which are inhaled in to the
lungs.
 ANTITUBERCULOSIS
114

The difficulty in managing tuberculosis is the

prolonged treatment duration, the
emergence of drug resistance and co-
infection with HIV/AIDS.

Now infects approximately one third of the

world’s population and causes 8 million new
cases of TB each year resulting in around 2
million deaths worldwide
 ANTITUBERCULOSIS
115
The resurgence has been caused due to
three main reasons:

The available chemotherapy is not very

efficacious and has to be given as a
precise combination over a period of
months (poor compliance).
Drug resistant strains of the
mycobacterium are not susceptible to the
available drugs.
There is also a strong epidemiological
coexistence between TB with HIV.
 ANTITUBERCULOSIS
116
 ANTITUBERCULOSIS
117
FIRST LINE SECOND LINE
-Isoniazid (INH) -Cycloserine
-Rifampicin (Rifadin) -Kanamycin
-Ethambutol -Ethonamide
-Pyrazinamide -Para-aminosalicylic acid
-Streptomycin
 ANTITUBERCULOSIS
118

Active tuberculosis is treated with drug

combination for 6-9 mos.

Multidrug-resistant strain (MDR-TB) are

medicated for 1 year up to 2 years

These are given before meals

 ANTITUBERCULOSIS
119
ISONIAZID (INH)

Given 1 hr before or 2 hrs after meals because food

may delay absorption.
Given at least 1 hr before antacids.
Instruct to notify physician for signs of hepatoxicity
(jaundice), and neurotoxicity, numbness of
extremities.
Administer with Vitamin B6 (pyridoxine) to
counteract the neurotoxic side effects (peripheral
neuritis).
Avoid alcohol.
 ANTITUBERCULOSIS
120
RIFAMPICIN

Used as a first line drug in the treatment of

tuberculosis

Also used in the treatment of leprosy (combined

with dapsone), endocarditis, osteomyelitis,
pneumonia

Given on an empty stomach with 8 0z. of

water, 1 hour before or 2 hours after meals
and avoid taking antacids with medications.
 ANTITUBERCULOSIS
121

RIFAMPICIN

Hepatotoxic thus avoid alcohol.

Elevated SGPT level

Instruct the client that urine, feces, sweat, and

tears will be red-orange in color.

Rashes may appear while taking this drug

due to thrombocytopenia
 ANTITUBERCULOSIS
122
PYRAZINAMIDE (PZA)

Given for 2 months, a close analog of isoniazid

Largely bacteriostatic, but can be bactericidal

on actively replicating bacteria

Increase serum uric acid (gout arthralgia) and

cause photosensitivity

Hepatotoxicity is a major adverse effect

 ANTITUBERCULOSIS
123
ETHAMBUTOL

ADVERSE EFFECTS
Optic retro-bulbar neuritis
Red-green colour blindness → reduced visual
acuity
Dose-related Reversible
May be unilateral

*Examine visual acuity before starting treatment

*Impaired vision usually returns within a few
weeks of stopping intake
 ANTITUBERCULOSIS
124
STREPTOMYCIN

Aminoglycoside

Damage to the vestibular and auditory system

usually occurs in the first 2 months
The condition is reversible if the drug dosage is
reduced or the drug is stopped
Intermittent dosages (3x a week) are less likely
to cause serious toxicity
 ANTITUBERCULOSIS
125
ADVERSE EFFECT

Pain, rash, induration at injection site

Numbness around the mouth and tingling
sensation soon after injection
Cutaneous hypersensitivity
Vestibular and auditory nerve damage

Avoid use with other ototoxic and nephrotoxic

drugs
 ANTITUBERCULOSIS
126
TB DISEASE REGISTRATION GROUP – refers
to the classification of TB cases based on history
of previous treatment.

• New – has never had treatment for TB or

has taken anti-TB drugs for less than one
month

• Retreatment – has been treated before with

anti-TB drugs for at least one month. This
includes the following:
 ANTITUBERCULOSIS
127

1. RELAPSE – previously treated for TB and

declared cured or treatment completed,
but is presently diagnosed with active TB disease

2. TREATMENT AFTER FAILURE – previously

treated for TB but failed most recent course
based on a positive SM follow-up at five months
or later, or a clinically diagnosed
TB patient who does not show clinical
improvement anytime during treatment
 ANTITUBERCULOSIS
128

3. TREATMENT AFTER LOST TO FOLLOW-UP

– previously treated for TB but did not
complete treatment and lost to follow-up for
at least two months in the most recent course

4. PREVIOUS TREATMENT OUTCOME

UNKNOWN – previously treated for TB but
whose outcome in the most recent course is
unknown
 ANTITUBERCULOSIS
129

5. PATIENTS WITH UNKNOWN PREVIOUS TB

TREATMENT HISTORY – patients who do not
fit any of the categories listed above or
previous treatment history is unknown (this
group will be considered as previously treated
also)
 ANTITUBERCULOSIS
130

A PTB PATIENT IS CONSIDERED

NON-INFECTIOUS AFTER 2-3
WEEKS OF INITIATION OF
TREATMENT
(HINDI NA MAKAKAHAWA)
 ANTI-VIRAL
131

A virus is an infectious microbe consisting of

a segment of nucleic acid (either DNA or
RNA) surrounded by a protein coat.

A virus cannot replicate alone; instead, it

must infect cells and use components of the
host cell to make copies of itself.
 ANTI-VIRAL
132

Antiviral drugs inhibit viral multiplication,

but these drugs also interfere with the host
cell function because the viral
multiplication takes place with the host cell

CLASSIFICATION
Anti-herpes
Anti-influenza
Anti-hepatitis
Anti-retrovirus
 ANTI-VIRAL
133
ACYCLOVIR

• MOA: inhibits DNA polymerase and

incorporates itself into viral DNA

• Clinical Use: herpes simplex 1 and 2

and Varicella zoster

• Side Effects: skin irritation and

burning, crystalline nephropathy with
rapid infusion
 ANTI-VIRAL
134
FOSCARNET
• MOA: analog of pyrophosphate and competes
with it in viral DNA polymerase and reverse
transcriptase therefore inhibiting DNA synthesis
• Clinical Uses: CMV retinitis in
immunocompromised patients and acyclovir
resistant HSV
• Side Effects: renal toxicity, seizures,
hypocalcaemia, anemia
• Is deposited in bone and teeth.
• Hydrate patient to protect the kidneys
 ANTI-VIRAL
135
AMANTADINE

• MOA: prevents virus from entering susceptible

cells

• Clinical Uses: treatment/prophylaxis of

Influenza A in the elderly
• Side Effects: depression, CNS toxicity, CHF,
orthostatic hypotension, urinary retention

• RIMANTADINE is used for prophylaxis in

children
 ANTI-VIRAL
136 RIBAVIRIN
• MOA: unknown
• Clinical Uses: RSV in children
• Side Effects: decreased pulmonary function,
teratogenic in animals
• Is given via aerosol but is absorbed systemically •

OSELTAMIVIR
• MOA: analog of adenosine monophosphate
• Clinical Uses: chronic hepatitis B
• Side Effects: HA, asthenia (weakness and loss of
strength)
 ANTI-VIRAL
137 ANTI-RETROVIRALS
ZIDOVUDINE, DIDANOSINE, LAMIVUDINE

• MOA: nucleoside HIV reverse

transcriptase inhibitor
• Clinical Uses: HIV in combination therapy
• Zidovudine is used in the prevention of
maternal-fetal transmission
• Mom takes it prenatally then infant
takes it for 6 weeks
• Side Effects: peripheral neuropathy,
pancreatitis, myelosuppression with
Zidovudine