Pharmacology of the

Antibiotics

Nurse Licensure Examination

Review
The anti-infectives
 ANTI-INFECTIVES
 Anti-infective agents are drugs that are
designed to act selectively on foreign
organisms that have invaded and
infected the body

 Anti-infectives- range from antibiotics,

antifungals, antiprotozoals,
antihelmintics, antivirals and
antimycobacterial.
General Mechanisms of Action of
anti-infective

 Some interfere with the

biosynthesis of bacterial cell WALL
 Some inhibit protein synthesis
 Some change the cell membrane
permeability
 Some inhibit DNA synthesis
Spectrum of Activity of Anti-
infectives
 Narrow spectrum anti-infectives affect
only a few bacterial types. The early
penicillin drugs are examples.
 Broad-spectrum anti-infectives affect
many bacteria. Meropenem is an
example. Because narrow spectrum
antibiotics are selective, they are more
active against those single organisms
than the broad spectrum antibiotics.
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.
 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
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. Superinfections
 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
The structure of Penicillin
Penicillin is a beta-lactam drug,
with a beta-lactam ring. The
group of penicillins is called
beta lactam antibiotics.
Penicillin
Pharmacodynamcs: 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.
 The bacterium will have weakened cell wall,
will swell and then burst from the osmotic
pressure within the cell.
Amoxicillin is well absorbed in the
GIT
Therapeutic Indications of
penicillin
The penicillins are indicated for
the treatment of streptococcal
infections.
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.
 Hypersensitivity reactions- rashes, pruritus,
fever. 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
IMPLEMENTATION
 Obtain culture and sensitivity testing results
to check if penicillin is the drug of choice
 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
 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.
 Provide patient teaching. 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.
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
 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
 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
 Pharmacodynamics; The mechanism of action of cephalosporins
– 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.
 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.
– 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
 Drug-Drug interactions
 Aminoglycosides- if given with cephalosporins may increase the risk of kidney toxicity
 Anti-coagulants- may experience increased bleeding tendencies
 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.
 The Nursing Process and Cephalosporins
 ASSESSMENT
 Patient History- The nsure must assess for cephalosporin and penicillin allergies. Pregnancy, lactation and kidney status must also be ascertained
 Physical Examination- baseline data for evaluation. Renal function should be checked by obtaining BUN and Creatinine levels, urine output monitoring and
temperature monitoring.
 DIAGNOSIS
 Pain related to GIT and CNS effects
 High risk for infection
 Fluid volume deficit
 Knowledge deficit
 Non-compliance with medication
 IMPLEMENTATION
 Check the culture and sensitivity results to determine if cephalosporin is the drug of choice
 Monitor renal function test prior to and periodically during therapy
 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.
 Provide safety measures including safety side-rails, adequate lighting and assistance with ambulation.
 Provide heath teaching and advise the patient to take safety precaution in changing positions carefully, avoid driving and hazardous tasks, drink fluids liberally,
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.
 EVALUATION
 Monitor patient response to the drug regimen
 Monitor for adverse effects and evaluate the effectiveness of comfort and safety measures
 The Aminoglycosides

 The following are the aminoglycosides
 1.Gentamycin
 2.Tobramycin
 3.Amikacin
 4.Netilmicin
 5.Kanamycin
 Pharmacodyanmics:
 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.
 Therapeutic Use of the Aminoglycosides
 These drugs are used to treat serious infections caused by gram-NEGATIVE bacteria.
 Contraindications and Precautions with the use of Aminoglycosides
 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.
 Adverse Effects of Aminoglycosides
 CNS- irreversible deafness, vestibular paralysis, confusion, depression, disorietnation, 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 superinfection.
 GI system- nausea, vomiting, diarrhea, weight loss, stomatiits and hepatic toxicity. The effects are due to the direct GI irritation, loss of bacterial flora and toxicity to mucucs membrane and liver as
the drugs are metabolized.
 Skin effects- photosensitivity, purpura, rash, urticaria and exfoliative dermatitis
 Cardiac- palpitaions, hypotension or hypertension
 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 Nursing Process and Aminoglycosides
 ASSESSMENT
 Patient History- the nurse assesses the allergy to aminoglycosides, history of renal and hepatic disease, parkinsonism, myasthenia gravis, existing hearing loss, active herpes infecion, current
pregnancy and lactation.
 Physical examination- baseline data should be obtained. Auditory and CNS assessement must be done prior to thrapy. Culturea nd sensitivity specimen must be sent to laboratory. Renal and hepatic
function tests should be checked.
 DIAGNOSIS
 Pain related to GU, CNS effects
 Sensory-Perceptual alteration
 Potential for infection
 Fluid volume excess related to nephrotoxicity
 Knowledge deficit
 IMPLEMENTATION
 Check the culture and sensitivity results to determine if aminoglycosides are the drug of choice.
 Monitor the course of therapy. Ensure that the patient receives the correct dose and duration of treatment.
 Monitor the patient regularly for signs of nephrotoxicity, neurotoxicity, ototoxicity and bone marrow depression to effectively arrange for discontinuation of drug or decreased dosage as appropriate
 Provide safety measures to protect the patient if CNS effects occur.
 Provide small, frequent meals as tolerated, frequent mouth care and ice chips or sugarless and to provide relief and maintain nutrition
 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.
 EVALUATION
 Monitor patient response to the drug, adverse effects and effectiveness of comfort measures
 Evaluate the effectiveness of teaching and compliance to regimen.
 The Macrolides
 The macrolides are
 Azithromycin
 Clarithromycin
 Dirithromycin
 Erythromycin
 Pharmacodynamics: Mechanism of Action of the Macrolides
– The macrolides are primarily BACTERICIDAL and sometimes bacteriostatic. 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.
 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.
 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.
 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.
 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
 Drug-Drug Interactions
 Digoxin- increased level of dioxin can occur
 Anticoagulants, theophyllines and corticosteroids- increased effects of these drugs due to impaired hepatic metabolism
 Astemizole- when used with macrolides, will cause fatal cardiac arrhythmias
 Clindamycin or lincomycin – should not be given with erythromycin because they compete for receptor sites.
 The Nursing Process and Macrolides
 ASSESSMENT
 Patient History- the nurse should obtain history of allergy, current pregnancy or lactation before administering the drug
 Physical Examination- Assess baseline data and perform C/S before instituting therapy. The nurse then obtains information about the status of the liver and kidney, skin and GI system.
 DIAGNOSIS
 Pain related to GI, CNS effects
 Potential for infection related to super infections
 Knowledge deficit regarding drug therapy
 IMPLEMENTATION
 Check culture and sensitivity results to ensure that macrolides are the drug of choice
 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
 Provide health teaching and emphasize that the patient should take safety precautions including changing position slowly, drinking liberal amounts of fluids, and reporting severe reactions.
 EVALUATION
 Monitor patient response to the drug and adverse effects
 Evaluate the effectiveness of comfort and safety measures and the effectiveness of health teaching
 The Lincosamides
 These agents are similar to the Macrolides but are more
toxic. They are bactericidal and bacteriostatic depending on the
dose.
 The following are the Lincosamides:
 Clindamycin
 lincomycin
 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
 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
 Pharmacodynamics: The Mechanism of Action of Tetracyclines
– The tetracyclines inhibit protein synthesis in susceptible bacteria leading to the inability of the bacteria to multiply.
 Therapeutic indications of the Tetracycline
– Tetracyclines are effective against a wide range of bacteria. They are primarily BACTERIOSTATIC.
 Contraindications and Precautions in the use of Tetracyclines
– These agents are contraindicated in the presence of known allergy to tetrayclines and the tartrazine dye. 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.
 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
 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
 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 Nursing Process and Tetracyclines
 ASSESSMENT
 Patient History- The nurse screens the patient for allergy to tetracyclines and tartrazine. She should elicit history of renal and liver diseases, pregnancy, lactation, and AGE. Tetracyclines have adverse effects on
the bones and teeth.
 Physical Examination- this should be performed to establish baseline data for monitoring. Culture and sensitivity tests should be done and evaluation of kidney and liver status should be done.
 DIAGNOSIS
 Diarrhea
 Alteration in Nutrition: LTBR related to GI effects
 Alteration in skin integrity related to rash and photosensitivity
 Knowledge deficit regarding drug therapy
 IMPLEMENTATION
 Check the culture and sensitivity results to ensure that tetracyclines are the drug of choice
 Monitor renal and liver status/function tests periodically
 Emphasize the need to complete the recommended duration of therapy
 Provide small frequent meals if tolerated only
 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
 EVALUATION
 Monitor response to tetracycline and adverse effects
 Evaluate the effectiveness of teaching an comfort
 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. oxacillin
 4. norfloxacin
 5.Levfofloxacin
 6.Sparfloxacin
 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.
 Therapeutic Use of the Fluoroquinolones
– ]These agents are indicated for the treatment of infections caused by susceptible strains of gram-negative bacteria
including E. coli., Proteus, pseudomonas, Strep and Staph spp.
 Contraindications and Precautions
– Known drug allergy to these agents contraindicate their use. 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.
 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
 Drug-Drug Interaction
 Iron salts, Sucralfate, mineral supplements and antacids- all of these will decrease the effectiveness of the
fluoroquinolones
 Quinidine, Procainamide, terfenadine, henothiazines- can prolong the QT interval and when used with the
fluoroquinolones

 The Sulfonamides
 These are called sulfa drugs that inhibit folic acid synthesis. Folic acid is necessary for the synthesis of purine and pyrimidine precursprs of DNA and RNA. Humans cannot
produce folic acid and must obtin it form the diet. While bacteria need to manufacture their own folic acid inside their cell structure.
 The following are the sulfonamides:
 1.Sulfazalazine
 2.Sulfamethoxazole
 3. Sulfadiazine
 4.Sulfixoxazole
 Pharmacodynamics: The Mechanism of Action of Sulfonamides
– 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.
 Therapeutic indications
– The spectrum of activity includes the following bacteria- Chlamydia, Nocardia, Haemophilus, E, coli and Proteus. Sulfa drugs are
used to treat trachoma and brain abscess.
 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.
 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
 Drug-Drug Interaction
 Tobultamide, tolazamide, glyburide, glipizide, acetohexamide or chlorpropamide (all are oral Anti-diabetic agents) can increase the risk of hypoglycemia if taken with the sulfa drugs
 The Nursing Process and the Sulfonamides
 ASSESSMENT
 Patient History- The nurse screens for known allergy to sulfonamides, sulfonylureas and thiazide diuretics because of cross sensitivity. Elicit history of renal disease and current
pregnancy/lactation
 Physical Examination- PE should be performed to establish baseline data for assessing the drug effectiveness. Culture and sensitivity should be performed before instituting therapy. The
nurse should also monitor the renal status. CBC should be performed to establish a baseline data to monitor for adverse effects.
 DIAGNOSIS
 Pain related to GI, CNS and skin effects of the drug
 Sensory-Perceptual alteration related to CNS effects
 Alteration in nutrition related to multiple GI effects
 Knowledge deficit regarding drug therapy
 IMPLEMENTATION
 The nurse checks the culture and sensitivity results to ensure that sulfa drugs are the drug of choice
 Monitor renal functions test periodically. Discontinue drug if hypersensitivity reaction occurs.
 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.
 Implement health teaching. Emphasize that the patient should avoid operating dangerous machinery, drinking liberal amount of fluids, maintain nutrition and to report severe drug reactions.
 EVALUATION
 Monitor patient response to the drug. Monitor for adverse effects
 Evaluate effectiveness of the teaching plan and monitor the effectiveness of safety and comfort measures