Pharmacology of the

Antibiotics

Nurse review
 The anti-infective drugs

 Anti-infective agents are drugs that

are designed to act selectively on
foreign organisms that have invaded
and infected the body
 The anti-infective drugs

Anti-infective drugs - range from

 Antibacterials
 Antifungals
 Antiprotozoals
 Antihelminthics
 Antivirals
 Antimycobacterial
General Mechanisms of Action
of anti-infective agents

The mechanisms are:

 Inhibition of the biosynthesis of
bacterial cell WALL
 Inhibition of protein synthesis

 Some change the cell membrane

permeability
 Some inhibit DNA synthesis
 Examples
CELL WALL penicillin,
INHIBITORS cephalosporin,
vancomycin
PROTEIN SYNTHESIS Macrolides,
INHIBITORS aminogylcosides
CELL WALL Ketoconazole
Permeability
DNA SYNTHESIS Quinolones
INHIBITORS
Spectrum of Activity of Anti-infectives

 Narrow spectrum

 Broad-spectrum
Spectrum of Activity of Anti-infectives

 Narrow spectrum anti-infectives

affect only a few bacterial types

 The early penicillin drugs are

examples.
Spectrum of Activity of Anti-infectives

 Broad-spectrum anti-infectives affect

many bacteria.
 Meropenem is an example.
 Because narrow spectrum antibiotics
are selective, they are more active
against single organisms than the
broad spectrum antibiotics.
Spectrum of Activity of Anti-infectives

Anti-infective agents can also be:

 Bacteriostatic

 Bactericidal
 Spectrum of Activity of Anti-
infectives
 Anti-infectives that interfere with the
ability of the cell to
reproduce/replicate without killing
them are called BACTERIOSTATIC
drugs.
 Tetracycline is an example.
 Spectrum of Activity of Anti-
infectives
 Antibiotics that can aggressively
cause bacterial death are called
BACTERICIDAL.

 These properties (-cidal and –static)

can also depend on the antibiotic
concentration in the blood.
Common Adverse Reactions to
Anti-infective Therapy
The most common adverse effects are
due to the direct action of the drugs
in the following organ system-
Neuro, nephro and GI system
Common Adverse Reactions to
Anti-infective Therapy
1. Nephrotoxicity
 Antibiotics that are metabolized
and excreted in the kidney most
frequently cause kidney damage..
Common Adverse Reactions to
Anti-infective Therapy
2. Gastro-intestinal toxicity
 Direct toxic effect to the cells of the
GI tract can cause nausea, vomiting,
stomach pain and diarrhea.
 Some drugs are toxic to liver cells
and can cause hepatitis or liver
failure.
Common Adverse Reactions to
Anti-infective Therapy
3. CNS toxicity
 When drugs can pass through the
brain barrier and accumulate in the
nervous tissues, they can interfere
with neuronal function.
Common Adverse Reactions to
Anti-infective Therapy
4. 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 to
Anti-infective Therapy
5. Super-infections
 Opportunistic infections that develop
during the course of antibiotic
therapy are called
SUPERINFECTIONS.
 The PENICILLINS
Narrow spectrum penicillins
 Penicillin G
 Penicillin V
Broad Spectrum Penicillins (aminopenicillin)
 Amoxicillin
 Ampicillin
 Bacampicillin
Penicillinase-resistant Penicillin (anti-staphyloccocal penicillins)
 Cloxacillin
 Nafcillin
 Methicillin
 Dicloxacillin
 Oxacillin
Extended-Spectrum penicillins (Anti-pseudomonal penicillins)
 Carbenicillin
 Mezlocillin
 Piperacillin
 Ticacillin
Beta-lactamase inhibitors
 Clavulanic acid
 Sulbactam
 Tazobactam
 Penicillin
Penicillin is a beta-lactam drug,
with a beta-lactam ring.

The group of penicillins is called

beta lactam antibiotics.
 Penicillin
The action of Penicillins

 The penicillin and penicillinase-

resistant penicillins produce
BACTERICIDAL effects by
interfering with the ability of
susceptible bacteria from
biosynthesizing the framework of
the cell wall.
 Penicillin

 Thebacterium will have

weakened cell wall, will
swell and then burst from
the osmotic pressure within
the cell.
 Penicillin
Pharmacokinetics:

Amoxicillin is well absorbed in the

GIT. This in NOT affected by food
intake!!
 Penicillin
Therapeutic Indications of
penicillin
 The penicillins are indicated
for the treatment of
streptococcal infections
 Syphilis
 Tetanus
 Adverse Effects of Penicillins
 GI system effects- the major adverse
effects of penicillin therapy involve
the GIT.
 Nausea, vomiting, diarrhea,
abdominal pain, glossitis, stomatitis,
gastritis, sore mouth and furry
tongue.
 The reason for some of these effects
(superinfection) is associated with
the loss of bacterial flora.
 Adverse Effects of Penicillins
 Hypersensitivity reactions- rashes,
pruritus, fever and urticaria
 These indicate mild allergic reaction.
Wheezing and diarrhea may also
occur.
 Anaphylaxis can also happen leading
to shock or death. It occurs in 5-10%
of those receiving penicillins.
 Pain and inflammation on injection
sites
 Nursing Considerations for
Penicillin
 Obtain culture and sensitivity
testing
 Monitor the renal status and
function regularly
 Administer the correct dosage and
stress the importance of completing
the full course and duration of
therapy even though the patient
experiences relief earlier in the
treatment
 Nursing considerations
 Monitor the site of injection and the signs
and symptoms related to the drug
administration
 Provide small frequent meals, frequent
mouth care, ice chips or sugarless candy to
suck if stomatitis and sore mouth occurs
 Tell the patient to drink a lot of fluids and
eat nutritious foods.
 Advise to report difficulty of breathing,
severe diarrhea, dizziness, weakness and
vaginal itching.
 Nursing Consideration
EVALUATION
 Monitor patient response to
therapy
 Monitor for adverse effects and
evaluate the effectiveness of
health teaching
 Monitor the effectiveness of
comfort and safety measures
 Penicillin

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 THE CEPHALOSPORINS

The cephalosporins
also belong to the
beta-lactam group
of antibiotics
 THE CEPHALOSPORINS

 First Generation cephalosporin

 Second generation cephalosporin

 Third Generation cephalosporin

 Fourth generation cephalosporin

 THE CEPHALOSPORINS
 First Generation cephalosporins- are
largely effective against the same
gram-positive organisms affected by
penicillin.

 Second generation cephalosporins-

are effective against those strains as
well as Haemophilus influenza,
Entreobacter aerogenes and Nesseria
sp. These drugs are less effective
against gram positive bacteria
 THE CEPHALOSPORINS
 Third Generation cephlosporins- are
relatively weak against gram-positive
bacteria but more potent against
gram-negative bacteria, to include
Serratia marcescens.

 Fourth generation cephalosporins-

are developed to fight against the
resistant gram-negative bacteria. The
first drug is cefepime.
 First generation cephalosporins
 cefadroxil
 Cefazolin
 Cephalexin
 Cephalotin
 Cephapirin
 Cephadrine
 Second Generation cephalosporins
 Cefaclor
 Cefamandole
 Cefonizind
 Cefotetan
 Cefoxitin
 Cefmetazole
 Cefprozil
 Cefuroxime
 Third Generation Cephaosporins
 Cefnidir
 Cefixime
 Cefoperazone
 Cefotaxime
 Cefpodoxime
 Ceftazidime
 Ceftibuten
 Moxalactam
 Fourth Generation Cephalosporin
 Cefepime
 Cephalosporin
 The mechanism of action
 The cephalosporins are primarily
BACTERICIDAL.
 They interfere with the cell-wall
building ability of bacteria when they
divide.
 They prevent the bacteria from
biosynthesizing the framework of
their cell wall.
 The weakened cell wall will swell and
burst causing cell death.
 Cephalosporin
 Pharmacokinetics
 Only a few cephalosporins are
administered orally, most are
administered parenterally.
 Their half-lives are short and they
are excreted mainly in the urine.

 Contraindications and Precautions

 The drugs are contraindicated in
patients with known allergies to
cephalosporins and penicillins.
 Cephalosporin
Adverse Effects
 GI system- Nausea, vomiting,
diarrhea, anorexia, abdominal pain
and flatulence are common effects.
 CNS – headache, dizziness, lethargy
and paresthesias have been reported.
 Renal system- nephrotoxicity in
individuals with pre-existing renal
disease
 Hypersensitivity
 Cephalosporin
Drug-Drug interactions
 ALCOHOL- many patients experience
a disulfiram-like reactions when taken
with some specific cephlosporins
( cefamandole, cefoperazone or
moxalactam).
 The patient may experience flushing,
headache, nausea, vomiting and
muscular cramps. This may occur
even up to 72 hours of cephalosporin
discontinuance.
 Cephalosporin
IMPLEMENTATION
 Check the culture and sensitivity
results

 Monitor renal function test prior to

and periodically during therapy
 Cephalosporin
 Ensure that the patient receives the
full course of cephalosporins as
prescribed for the duration specified.
Advise the patient to consume all the
drugs even though signs/symptoms
may resolve earlier in the course.
 Provide small frequent meals as
tolerated, mouth care, ice chips if
stomatitis occurs.
 Cephalosporin
 Provide safety measures including
safety side-rails, adequate lighting
and assistance with ambulation.
 Provide heath teaching and advise
the report severe reactions to the
drug and AVOID alcoholic beverages
for 72 hours after completing the
drug.
 Take medication with food if gastric
irritation occurs.
 Cephalosporin
EVALUATION
 Monitor patient response to the
drug regimen
 Monitor for adverse effects and
evaluate the effectiveness of
comfort and safety measures
 Cephalosporin

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 The Aminoglycosides

The following are the aminoglycosides

1. Gentamycin
2. Tobramycin
3. Amikacin
4. Netilmicin
5. Kanamycin
 The Aminoglycosides

Mechanism of action
 These are BACTERICIDAL.
 They inhibit protein synthesis in
susceptible strains of gram-
negative bacteria, leading to loss
of functional integrity of the
bacterial cell membrane, which
causes cell death.
 The Aminoglycosides
Therapeutic Use of the Aminoglycosides
 These drugs are used to treat serious
infections caused by gram-NEGATIVE
bacteria.

 These drugs are contraindicated in

known allergies to aminoglycosides,
in patients with renal failure, hepatic
disease, pre-existing hearing loss,
myasthenia gravis, Parkinson’s,
pregnancy and lactation.
 The Aminoglycosides
Adverse Effects of Aminoglycosides
 CNS- irreversible deafness, vestibular
paralysis, confusion, depression,
disorientation, numbness, tingling and
weakness related to drug effects.
 Kidney- renal toxicity, which may
progress to renal failure caused by the
direct toxicity of the aminoglycosides.
 Hema- bone marrow depression
resulting from direct drug effect may
lead to immune suppression and super-
infection.
 Ototoxicity
 The Aminoglycosides

Adverse Effects of Aminoglycosides

 GI system- nausea, vomiting,
diarrhea, weight loss, stomatitis and
hepatic toxicity
 Skin effects- photosensitivity,
purpura, rash, urticaria and
exfoliative dermatitis
 Cardiac- palpitations, hypotension
or hypertension
 The Aminoglycosides

Drug to drug interactions

 Diuretics- increased incidence of
ototoxicity, nephrotoxicity and
neurotoxicity.
 Anesthetics and Neuromusular
blockers- increased
neuromuscular blockage and
paralysis may be possible
 Penicillin- synergistic action
 The Aminoglycosides
Implementations
 Monitor the patient regularly for
signs of nephrotoxicity,
neurotoxicity, ototoxicity and bone
marrow depression
 The Aminoglycosides

Implementations
 Ensure that patient is hydrated at all
times during the drug therapy to
minimize renal toxicity
 Provide teaching to the patient to
take safety precaution such as
changing position slowly and
avoiding driving/hazardous tasks,
drink liberal amounts of fluids, avoid
exposure to other infections, and to
report severe reactions.
 The Aminoglycosides

EVALUATION
 Monitor patient response to the drug,
adverse effects and effectiveness of
comfort measures
 Evaluate the effectiveness of
teaching and compliance to regimen.
 Aminiglycosides

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 The Macrolides

The macrolides are

 Azithromycin
 Clarithromycin
 Dirithromycin
 Erythromycin
 The Macrolides
Mechanism of Action of the Macrolides

 They exert their effect by binding

to the bacterial cell ribosomes and
changing or altering protein
production/function

 This will lead to impaired cell

metabolism and division.
 The Macrolides

 Pharmacokinetics
 Erythromycin is destroyed
by the gastric juice, which
is why slats are added to
stabilize the drug.
 Food does not interfere
with the absorption of the
macrolides.
 The Macrolides

Therapeutic Use of Macrolides

 These are indicated for the
treatment of the following
conditions:
 Steptococcal infection,
Mycoplasma infection, Listeria
infection and group A beta
hemolytic strep infection.
 The Macrolides
Contraindications and Precautions in the Use
of Macrolides
 These agents are contraindicated in
the presence of known allergy to any
macrolide, because cross-sensitivity
occurs.
 Caution should be used in patients
with hepatic dysfunction that could
alter the metabolism of the drug; in
lactating women because of drug
excretion in breast milk and in
pregnant women because potential
adverse effects on the developing
fetus.
 The Macrolides

Adverse Effects of Macrolides

 GI system- abdominal cramping, anorexia,
diarrhea, vomiting and
pseudomembranous colitis.
HEPATOTOXICITY can occur if the drug is
taken in high doses with other hepatotoxic
drugs.
 CNS- confusion, abnormal thinking and
uncontrollable emotions.
 Hypersensitivity reactions
 The Macrolides

IMPLEMENTATION
 Monitor hepatic function test prior to
therapy
 Ensure that patients receive the full course
of therapy
 Monitor sings and symptoms of adverse
reactions
 Provide small, frequent meals as tolerated,
provide mouth care and ice chips
 Provide safety measures to protect patient
if CNS effects occur
 Macrolides

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 The Lincosamides

These agents are similar to the

Macrolides but are more toxic.

 Clindamycin
 lincomycin
 The Lincosamides

Pharmacodynamics: The Mechanism of

Action of Lincosamides
 These agents penetrate the cell
membrane and bind to the ribosome in
the bacterial cytoplasm to prevent the
protein production
 The Lincosamides

Side effects and Adverse Reactions

 GIT- GI irritation, nausea, vomiting and
stomatitis
 Allergic reactions

Drug Interactions
 Lincomycin and clindamycin are
incompatible with aminophyline,
phenytoin, barbiturates and ampicillin.
 The Tetracyclines
These agents were first isolated from
Streptomyces aureofaciens
The following are the tetracyclines
 Short-acting tetracyclines
 tetracycline
 oxytetracycline
 Intermediate acting tetracyclines
 demeclocycline
 methacycline
 Long acting tetracyclines
 doxycycline
 minocycline
 The Tetracyclines

Pharmacodynamics
 Thetetracyclines inhibit
protein synthesis in
susceptible bacteria
leading to the inability of
the bacteria to multiply.
 The Tetracyclines
Contraindications and Precautions in the use of Tetracyclines
 It is not recommended for use in
pregnancy and lactation because the
drug can affect the bones and teeth,
causing permanent discoloration and
sometimes arrest of growth.

 Tetracyclines are also avoided in

children less than 8 (eight) years of
age because of the potential damage
to the bones and permanent
discoloration of the teeth.
 The Tetracyclines

Adverse Effects of the Tetracycline

 GI system- nausea, vomiting, diarrhea, abdominal
pain, glossitis and dysphagia.
 Fatal hepatotoxicity related to tetracycline’s
irritating effect on the liver cells has been
reported.
 Musculoskletal- Tetracyclines have an affinity for
teeth and bones; they accumulate there, leading
to weakening of the bone/teeth and permanent
staining and pitting.
 Skin- photosensitivity and rash are expected.
 Less frequent- bone marrow depression,
hypersensitivity, super infections, pain and
hypertension
 The Tetracyclines

Drug-Drug Interactions
 Penicillin- if taken with tetracyclines, will
decrease the effectiveness of penicillin.
 Oral contraceptives- if taken with
tetracycline, will have decreased
effectiveness. Nurse must advise
alternative methods of contraception
 Digoxin- digoxin toxicity rises when
tetracyclines are used together
 The Tetracyclines

Drug-Food Interaction
 Dairy products- can complex with
tetracycline and render
unabsorbable.
 Tetracyclines should then be given
on an EMPTY stomach 1 hour before
meals or 2-3 hours after any meal or
other medications.
 The Tetracyclines
IMPLEMENTATION
 Check the culture and sensitivity
results
 Monitor renal and liver
status/function tests periodically
 Provide small frequent meals if
tolerated only
 The Tetracyclines
IMPLEMENTATION
 Protect the patient from exposure to
the sun with adequate clothing and
sunscreen
 Instruct the patient to take the meds
without food, with full glass of water,
adequate fluid intake, avoidance of
exposure to other infections and to
report severe drug reactions
 Provide information of alternative
contraceptive methods during the
course of therapy
 Tetracycline

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 The Fluoroquinolones
The fluoroquinolones are broad-spectrum
antibiotics. They are usually manufactured
synthetically and are associated with mild
adverse reactions.

The examples are:

1. Nalidixic acid
2. ciprofloxacin
3. ofloxacin
4. norfloxacin
[Link]
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 The Fluoroquinolones
Pharmacodynamics: Mechanism of
action of the Fluoroquinolones
 These agents enter the bacterial
cell by diffusion through cell
channel.
 Once inside they interfere with the
action of DNA enzymes (DNA
gyrase) necessary for the growth
and reproduction of the bacteria.
This will lead to cell death.
 The Fluoroquinolones

 Contraindications and Precautions

Pregnancy and lactation are also
contraindications.
These agents are found to cause
significant damage to the cartilages
such that they are given cautiously to
growing children and adolescents less
than 18 years of age
 The Fluoroquinolones
Adverse Effects of the Fluoroquinolones
 CNS- dizziness, insomnia, headache, and
depression related to possible effects on
the CNS membrane.
 GI system- nausea, vomiting, diarrhea and
dry mouth related to the direct effect on
the GIT
 Hema- bone marrow depression related to
the direct effect of the drug on the cells of
the bone marrow that rapidly turn over.
 Other effects- skin reactions, rash, fever
and photosensitivity
 Quinolones

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 Sulfonamides

The following are the

sulfonamides:
1. Sulfazalazine
2. Sulfamethoxazole
3. Sulfadiazine
4. Sulfixoxazole
 Sulfonamides

Pharmacodynamics
 The sulfa drugs competitively
block the para-amino benzoic
acid to prevent the synthesis
of folic acid in susceptible
bacteria that synthesize their
own folates for the production
of RNA and DNA.
 Sulfonamides

Contraindications and precautions

 These agents are contraindicated to patients

with known allergy to sulfa drugs,
sulfonylureas and thiazide diuretics because
they share similar structures.
 It is not recommended for use in pregnancy
because it can cross the placenta and cause
birth defects and kernicterus.
 Lactating women who take these drugs will
excrete them in the breast milk potentially
causing kernicterus, diarrhea and rash in the
newborn.
 Sulfonamides
Adverse Effects of the Sulfonamides
 GI system- nausea, vomiting, diarrhea, abdominal
pain, anorexia, stomatitis and hepatic injury,
which are all related to the direct irritation of the
GIT and death of normal flora.
 Renal system- crystalluria, hematuria and
proteinuria which can progress to a nephrotic
syndrome.
 CNS- headache, dizziness, vertigo, ataxia,
convulsions and depression related to drug
effects on the nerves
 Hema- bone marrow depression related to drug
effects on the cells of the bone marrow that turn
over rapidly.
 Dermatologic effects- photosensitivity and rash
and hypersensitivity
 Sulfonamides
IMPLEMENTATION
 Monitor renal functions test periodically
 Administer the drug on an EMPTY stomach
1 hour before or 2 hours after meals with
full glass of water to ensure adequate drug
absorption
 Provide mouth care if with stomatitis or
mouth problems occur
 Monitor CBC and urinalysis periodically.
 Emphasize that the patient should avoid
operating dangerous machinery, drinking
liberal amount of fluids, maintain nutrition
and to report severe drug reactions.
 Sulfa

 Classify: ___________________________
 Dynamics: _________________________
 Kinetics: ___________________________
 Good Action: _______________________
 “Bad action”: _______________________
 Considerations: _____________________
 The anti tubercular

 Isoniazid
 Rifampicin
 Pyrazinamide
 Ethambutol
 Mechanisms of action
Isoniazid Interferes with DNA
synthesis of
bacterium
Rifampicin Interferes with RNA
synthesis
Pyrazinamide Interferes with
bacterial wall
synthesis
Ethambutol Prevent
multiplication
 Common Side effects
Isoniazid Interferes with B6
Peripheral neuritis
Rifampicin Red-orange discoloration of
the secretions
Hepatitis
Pyrazinamide Hyperuricemia

Ethambutol Optic neuritis

 Precautions
Isoniazid Liver impairment

Rifampicin Liver impairment

Pyrazinamide Liver impairment

Gout
Pregnancy
Ethambutol Liver impairment
Children less than 6 years
old
 General Responsibilities

 Advise patient to take the DRUGS as

prescribed
 Multiple drugs are taken to prevent
RESISTANCE
 Periodically check the liver function tests
 Supplemental Intake of Vitamin B6
 Anti-fungals

 These agents ALTER the fungal cell wall

causing fungal destruction
 Anti-fungals

 The “AZOLES”
 Ketoconazole
 CLotrimazole
 Miconazole
 IV: AMPHOTERICIN
 Antifungals

Indications
 Fungal infections

 Candidiasis

 Tinea
 Antifungals
Important side effects
 Hypersensitivity

 Headache

 Dizziness

 Pruritus

 Irritation

 AMPHOTERICIN: HYPOKALEMIA,
arrhythmia and kidney damage
 General Responsibilities

 Take the oral drugs with food

 Evaluate the liver test, kidney test and
CBC
 Institute safety measures
 FOR amphotericin: Evaluate ECG and
Potassium, administer steroid, evaluate IV
site, give with INFUSION pump
 Antivirals

 General Action
 These agents interfere with the DNA or
RNA synthesis and replication of the
virus
 Antivirals

 The “Vir”
 Acyclovir
 Famcyclovir
 Valacyclovir
 Gancyclovir
 AIDS anti-viral
 Zidovudine (AZT)
 Antivirals

 Precaution with use

 Hypersensitivity
 Pregnancy
 Renal and hepatic impairment
 Antivirals

 Adverse effects
 Anorexia
 Nausea
 Vomiting
 Bleeding
 Phlebitis
 Reportable : bone marrow depression
and nephrotoxicity
 Antivirals

Nursing responsibilities
 Monitor the CBC and liver/kidney
function
 Acyclovir may cause hypotension

 Provide comfort measures for

headache
 Aseptic techniques