Introduction to Antibiotics

• Antibiotics agents are used to treat infections

• and sometimes as a means of prophylaxis
• (to prevent infections before they occur).
 ATBs

• Antibiotics are drugs used to treat bacterial

infections.
• Mechanisms: Kill bacteria or inhibit growth.
Antibiotics can act to destroy an infective Pathogen
(bactericidal)
• or to prevent the pathogen from reproducing
(bacteriostatic).

•Importance: Understanding classification helps in

effective treatment and managing side effects.

 Antibiotics classification
• ATBs can be classified Based on Mechanism of
Action
• Different mechanisms of action of ATBs are:
• Inhibitors of Cell Wall Synthesis
• Inhibitors of Protein Synthesis
• Inhibitors of Nucleic Acid Synthesis
• Inhibitors of Metabolic Pathways
 Inhibitors of Cell Wall Synthesis

• Beta-Lactams:
• Penicillins: Penicillin G, Amoxicillin
• Cephalosporins: Cephalexin, Ceftriaxone
• Carbapenems: Imipenem, Meropenem
• Monobactams: Aztreonam

• Mechanism: Inhibit bacterial cell wall synthesis

leading to cell lysis.
 Inhibitors of Protein Synthesis
• Aminoglycosides: Gentamicin, Amikacin
• Mechanism: Bind to 30S ribosomal subunit, causing
mistranslation.
• Macrolides: Erythromycin, Azithromycin
• Mechanism: Bind to 50S ribosomal subunit, inhibit
protein synthesis.
• Tetracyclines: Doxycycline, Minocycline
• Mechanism: Bind to 30S ribosomal subunit, prevent
protein synthesis.
• Chloramphenicol & Clindamycin: Similar
mechanism to macrolides.
 Inhibitors of Nucleic Acid Synthesis
• Quinolones/Fluoroquinolones: Ciprofloxacin,
Levofloxacin
• Rifamycins: Rifampin
 Inhibitors of Metabolic Pathways

• Sulfonamides: Sulfamethoxazole
• Mechanism: Block folic acid synthesis.

• Trimethoprim: Often combined with

sulfamethoxazole (TMP-SMX)
• Mechanism: Inhibit dihydrofolate reductase.
Classification Based on Chemical Structure

• Penicillins: Beta-lactam ring.

• Cephalosporins: Beta-lactam ring with
different structure.
• Macrolides: Macrolide ring structure.
• Tetracyclines: Four-ring structure.
• Aminoglycosides: Amino-sugars linked by
glycosidic bonds.
• Fluoroquinolones: Fluorine atom in structure.
 Classification Based on Spectrum
of Activity
• Broad-Spectrum Antibiotics: Effective against a
wide range of bacteria.
• Examples: Amoxicillin, Ciprofloxacin, Doxycycline.

• Narrow-Spectrum Antibiotics: Effective against

specific bacteria.
• Examples: Penicillin G (Gram-positive), Aztreonam
(Gram-negative).
 Classification based on Clinical Use of
Antibiotics
Respiratory Infections: UTI:

• Penicillins: Amoxicillin • Sulfonamides:

• Macrolides: Sulfamethoxazole

Azithromycin • Fluoroquinolones:

• Fluoroquinolones: Ciprofloxacin

Levofloxacin • Cephalosporins:

Ceftriaxone
 Classification based on Clinical Use of
Antibiotics
Skin Infections: .
• .
• Penicillins: Dicloxacillin

• Cephalosporins:

Cephalexin

• Macrolides:

Erythromycin
 Indications of ATB
• Treatment of existing infection
• Prevention of infection
• A. Inhibitors of cell wall synthesis
VI. Antibacterial Agents

• 1. Penicillins
• 2. Cephalosporins
• 3. Other antibacterial agents that act on cell walls
• B. Disrupters of cell membranes
• 1. Polymyxins
• 2. Tyrocidins
• C. Inhibitors of protein synthesis
• 1. Aminoglycosides
• 2. Tetracyclines
• 3. Chloramphenicol
• 4. Other antibacterial agents that affect protein synthesis
• a. Macrolides
• b. Lincosamides
• D. Inhibitors of nucleic acid synthesis
• 1. Rifampin
• 2. Quinolones
• E. Antimetabolites and other antibacterial agents
• 1. Sulfonamides
• 2. Isoniazid
• 3. Ethambutol
• 4. Nitrofurans
Antibiotic Mechanisms of Action
Alteration of
Cell Membrane
Polymyxins
Bacitracin
Neomycin

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 Penicillins classification
• Natural penicillins
• Penicillin G and penicillin V (also
known as penicillin V potassium) are
natural penicillins. Providers use
natural penicillins to treat a range of
infections, including strep throat,
syphilis and Lyme disease. Penicillin
G comes in IV form. Penicillin V is
in the form of a tablet.
 Semi-synthetic penicillins
• Semi-synthetic penicillins include:
• Penicillinase-resistant
penicillins. Nafcillin, oxacillin and
dicloxacillin are penicillinase-
resistant penicillins. They come in
both IV and pill form and are often
used to treat staphylococcus
infections.
 Aminopenicillins (Penicillinase
non-resistant penicillins)
• Amoxicillin and ampicillin are
aminopenicillins. Amoxicillin is one of
the most commonly used penicillins.
• Providers use it to treat ear
infections, UTIs, pneumonia and
other common infections.
• It comes in a pill or liquid you can
swallow.
 Extended-spectrum
penicillins.
• Piperacillin is an extended-spectrum
penicillin.
• Providers use it for hard-to-treat
infections, like Pseudomonas
aeruginosa.
 Combination penicillins

• Penicillin can be combined with other

drugs, called beta-lactamase
inhibitors,
• to help them work better.
• Beta-lactamase inhibitors work by
preventing bacterial enzymes (beta-
lactamases) from destroying the
antibiotic.
 Combination
• Some penicillin/beta-lactamase
inhibitor combinations include:
• Augmentin® (amoxicillin and
clavulanic acid).
• Unasyn® (ampicillin and sulbactam).
• Zosyn® (piperacillin and
tazobactam).
 Uses of Penicillins
• Natural Penicillins:
• Streptococcus and Staphylococcus infections
• Syphilis, Rheumatic fever prophylaxis
• Aminopenicillins:
• Otitis media, sinusitis, respiratory tract infections,
UTIs
• Penicillinase-Resistant Penicillins:
• Penicillinase-producing Staphylococcus aureus
• Extended-Spectrum Penicillins:
• Hospital-acquired pneumonia, Pseudomonas
infections
 Contraindications
• Allergy to Penicillin:
• Hypersensitivity or anaphylactic reactions
• Caution:
• Patients with renal impairment (dose adjustment
needed)
 Side Effects
• Common:
• Gastrointestinal: Nausea, vomiting, diarrhea
• Oral/vaginal candidiasis
• Serious:
• Allergic reactions: Rashes, urticaria, angioedema
• Anaphylaxis: Life-threatening allergic reaction
• Hemolytic anemia, leukopenia, thrombocytopenia
(rare)
• Seizures (in high doses/renal impairment)
 Nursing Considerations
• Allergy Assessment:
• Check the patient's allergy history before
administration
• Monitor for Hypersensitivity:
• Watch for allergic reactions, especially with the first
dose
• Dosage Adjustments:
• Adjust for renal impairment
• Administration:
• Oral: With food if GI upset occurs
• IV: Monitor infusion site
 Nursing Considerations (Continued)
• Superinfections:
• Monitor for signs (oral thrush, vaginal yeast infections)
• Patient Education:
• Complete full course of therapy
• Drug Interactions:
• Probenecid: Increases serum penicillin levels
• Oral contraceptives: Reduced efficacy, use additional
contraception
• Laboratory Monitoring:
• Monitor renal/hepatic function and blood counts
 Cephalosporin Antibiotics
• Overview
• Broad-spectrum antibiotics, classified into five
generations.
• Inhibit bacterial cell wall synthesis.
• Effective against both gram-positive and gram-negative
bacteria.
 Generations of Cephalosporins
• First Generation
• Cephalexin, Cefazolin
• Second Generation
• Cefuroxime, Cefoxitin
• Third Generation
• Ceftriaxone, Ceftazidime
• Fourth Generation
• Cefepime
• Fifth Generation
• Ceftaroline
 Uses of Cephalosporins
• First Generation
• Skin and soft tissue infections, UTIs, surgical prophylaxis.
• Second Generation
• Respiratory tract infections, otitis media, sinusitis.
• Third Generation
• Severe infections: Meningitis, pneumonia, complicated
UTIs.
• Fourth Generation
• Hospital-acquired infections, febrile neutropenia.
• Fifth Generation
• MRSA infections, community-acquired bacterial
pneumonia.
 Contraindications
• Allergy to Cephalosporins
• Hypersensitivity reactions.
• Cross-Sensitivity
• Caution in patients with a history of penicillin allergy.
• Renal Impairment
• Dosage adjustment needed.
 Common Side Effects
• Gastrointestinal
• Nausea, vomiting, diarrhea.
• Superinfections
• Oral or vaginal candidiasis.
• Serious Side Effects
• Allergic Reactions
• Rash, urticaria, anaphylaxis (rare).
• Hematologic
• Neutropenia, thrombocytopenia (rare).
• Renal Effects
• Interstitial nephritis (rare).
• C. difficile Infection
 Nursing Considerations - Part 1
• Allergy Assessment
• Assess for cephalosporin and penicillin allergies
before administration.
• Monitor for Hypersensitivity
• Watch for signs of allergic reactions, especially
with the first dose.
• Dosage Adjustments
• Adjust dosages in patients with renal impairment.
 Nursing Considerations - Part 2
• Administration
• Oral: Take with food if gastrointestinal upset occurs.
• IV: Monitor the infusion site for irritation or phlebitis.
• Superinfections
• Monitor for signs of superinfections like oral thrush or
vaginal yeast infections.
• Patient Education
• Emphasize the importance of completing the full
antibiotic course.
 Nursing Considerations - Part 3
• Drug Interactions
• Anticoagulants: Enhanced anticoagulant effect.
• Nephrotoxic Drugs: Increased risk of kidney damage.
• Laboratory Monitoring
• Monitor renal and hepatic function during prolonged
therapy.
• C. difficile Risk
• Educate patients to report severe diarrhea.
 Aminoglycoside Antibiotics
• Overview
• Potent antibiotics that inhibit bacterial protein synthesis.
• Effective against gram-negative bacteria and some gram-
positive bacteria.
• Commonly used drugs include Gentamicin, Amikacin,
and Tobramycin.
 Mechanism of Action
• Bactericidal:
• Bind to the bacterial 30S ribosomal subunit,
leading to the production of faulty proteins.
• Concentration-Dependent Killing:
• Higher concentrations lead to more rapid bacterial
killing.
 Uses of Aminoglycosides
• Severe Infections:
• Septicemia, complicated UTIs, and intra-abdominal
infections.
• Respiratory Tract Infections:
• Used in combination with other antibiotics for serious
infections like pneumonia.
• Endocarditis:
• Often used in combination with other antibiotics.
• Tuberculosis:
• Streptomycin is used as a second-line agent in multi-drug
resistant TB.
 Contraindications
• Renal Impairment:
• Caution is required due to nephrotoxicity risk.
• Myasthenia Gravis:
• Can exacerbate muscle weakness.
• Pregnancy:
• Can cause fetal harm, including congenital deafness.
 Common Side Effects
• Nephrotoxicity:
• Kidney damage; monitor renal function.
• Ototoxicity:
• Hearing loss and balance issues; irreversible in some
cases.
• Neuromuscular Blockade:
• Can lead to respiratory paralysis.
 Serious Side Effects
• Ototoxicity:
• Irreversible hearing loss, particularly with prolonged use.
• Nephrotoxicity:
• Acute kidney injury, especially in patients with pre-
existing renal conditions.
• Allergic Reactions:
• Rash, fever, and anaphylaxis (rare).
 Nursing Considerations - Part 1
• Dosage Monitoring:
• Monitor peak and trough levels to avoid toxicity.
• Renal Function:
• Assess renal function before and during therapy (BUN,
creatinine).
• Hearing Assessment:
• Monitor for signs of ototoxicity, such as tinnitus or
hearing loss.
 Nursing Considerations - Part 2
• Hydration:
• Ensure adequate hydration to reduce the risk of
nephrotoxicity.
• Neuromuscular Function:
• Monitor for signs of neuromuscular blockade, especially
in patients with pre-existing neuromuscular disorders.
• Patient Education:
• Instruct patients to report any changes in hearing,
balance, or urination.
 Nursing Considerations - Part 3
• Drug Interactions:
• Increased risk of nephrotoxicity when used with other
nephrotoxic drugs (e.g., vancomycin, diuretics).
• Dosing Adjustments:
• Adjust dosages based on renal function and drug levels.
• Caution in Elderly:
• Higher risk of toxicity due to decreased renal function.
 Macrolide Antibiotics
• Overview
• Broad-spectrum antibiotics that inhibit bacterial protein
synthesis.
• Effective against gram-positive bacteria and some gram-
negative bacteria.
• Common examples include Erythromycin, Azithromycin,
and Clarithromycin.
 Mechanism of Action

• Bacteriostatic:
• Bind to the 50S ribosomal subunit of bacteria,
inhibiting protein synthesis.
• Bactericidal at High Doses:
• Can kill bacteria at higher concentrations.
 Uses of Macrolides
• Respiratory Tract Infections:
• Pneumonia, bronchitis, pharyngitis, and sinusitis.
• Skin and Soft Tissue Infections:
• Cellulitis, impetigo.
• Sexually Transmitted Infections:
• Chlamydia, gonorrhea.
• Gastrointestinal Infections:
• H. pylori eradication (Clarithromycin as part of
combination therapy).
• Alternative for Penicillin-Allergic Patients:
• For infections like strep throat and syphilis.
 Contraindications
• Allergy to Macrolides:
• Hypersensitivity to macrolides.
• Liver Dysfunction:
• Avoid in patients with significant liver impairment.
• Drug Interactions:
• Caution with drugs metabolized by the liver, such
as statins and warfarin.
 Common Side Effects
• Gastrointestinal:
• Nausea, vomiting, diarrhea, abdominal pain.
• Taste Disturbance:
• Metallic taste (common with Clarithromycin).
• Mild Skin Reactions:
• Rash, pruritus.
 Serious Side Effects
• QT Prolongation:
• Risk of arrhythmias, especially in patients with pre-
existing heart conditions.
• Hepatotoxicity:
• Elevated liver enzymes and liver dysfunction.
• Ototoxicity:
• Reversible hearing loss with high doses or prolonged
use.
 Nursing Considerations - Part 1
• Allergy Assessment:
• Check for a history of macrolide allergy.
• Cardiac Monitoring:
• Monitor ECG in patients with a history of arrhythmias.
• Liver Function:
• Monitor liver enzymes during prolonged therapy.
 Nursing Considerations - Part 2
• Administration:
• Oral: May be taken with food to reduce GI upset.
• IV: Administer slowly to prevent phlebitis.
• Patient Education:
• Advise patients to complete the full course of
therapy.
• Warn about potential drug interactions with other
medications.
 Nursing Considerations - Part 3
• Drug Interactions:
• Avoid co-administration with drugs that can cause QT
prolongation.
• Monitor INR levels in patients on warfarin.
• Gastrointestinal Effects:
• Educate patients to report severe diarrhea, which could
indicate antibiotic-associated colitis.
 Fluoroquinolone Antibiotics
• Overview
• Broad-spectrum antibiotics that inhibit bacterial DNA
synthesis.
• Effective against a wide range of gram-negative and
gram-positive bacteria.
• Common examples include Ciprofloxacin,
Levofloxacin, and Moxifloxacin.
 Mechanism of Action

• Bactericidal:
• Inhibit bacterial DNA gyrase and topoisomerase IV,
preventing DNA replication and transcription.
• Broad Spectrum:
• Active against both gram-positive and gram-
negative bacteria, including Pseudomonas
aeruginosa.
 Uses of Fluoroquinolones
• Respiratory Tract Infections:
• Community-acquired pneumonia, and chronic bronchitis
exacerbations.
• Urinary Tract Infections:
• Complicated and uncomplicated UTIs, including
pyelonephritis.
• Gastrointestinal Infections:
• Traveler's diarrhea, typhoid fever.
• Bone and Joint Infections:
• Osteomyelitis.
• Anthrax Exposure:
• Ciprofloxacin is used as a prophylaxis and treatment.
 Contraindications
• Allergy to Fluoroquinolones:
• Known hypersensitivity to any fluoroquinolone.
• Pediatric and Geriatric Patients:
• Not recommended for children under 18 (due to the
potential for joint and tendon damage).
• Pregnancy and Breastfeeding:
• Avoid due to potential effects on fetal cartilage
development.
 Common Side Effects
• Gastrointestinal:
• Nausea, vomiting, diarrhea, abdominal pain.
• CNS Effects:
• Dizziness, headache, insomnia.
• Skin Reactions:
• Rash, photosensitivity.
• Serious Side Effects
• Tendonitis and Tendon Rupture:
• Increased risk, particularly in older adults and those on corticosteroids.
• QT Prolongation:
• Can lead to serious arrhythmias, especially when taken with other QT-
prolonging drugs.
• Peripheral Neuropathy:
• Risk of irreversible nerve damage.
• CNS Effects:
 Nursing Considerations - Part 1
• Allergy Assessment:
• Check for history of fluoroquinolone allergy.
• Tendon Assessment:
• Monitor for signs of tendon pain, swelling, or
inflammation.
• Cardiac Monitoring:
• Monitor ECG in patients with risk factors for QT
prolongation.
 Nursing Considerations - Part 2

• Administration:
• Oral: Administer with or without food, avoid with dairy
products or antacids containing magnesium or
aluminum.
• IV: Infuse slowly to reduce the risk of irritation.
• Patient Education:
• Advise patients to report any tendon pain immediately.
• Instruct to avoid excessive sunlight or UV light exposure
due to photosensitivity risk.
 Nursing Considerations - Part 3
• Drug Interactions:
• Avoid concurrent use with other QT-prolonging drugs.
• Monitor INR in patients on warfarin.
• Renal Function:
• Adjust dosages in patients with renal impairment.
• Gastrointestinal Effects:
• Educate patients to report severe diarrhea, which could
indicate C. difficile-associated colitis.
 Tetracycline Antibiotics
• Overview
• Broad-spectrum antibiotics that inhibit bacterial protein
synthesis.
• Effective against a wide range of gram-positive and
gram-negative bacteria, as well as some intracellular
organisms.
• Common examples include Tetracycline, Doxycycline,
and Minocycline.
 Mechanism of Action
• Bacteriostatic:
• Bind to the 30S ribosomal subunit of bacteria,
inhibiting protein synthesis.
• Broad-Spectrum:
• Active against various bacteria, including atypical
pathogens like Mycoplasma and Chlamydia.
 Uses of Tetracyclines
• Respiratory Tract Infections:
• Atypical pneumonia (e.g., Mycoplasma pneumoniae),
bronchitis.
• Skin and Soft Tissue Infections:
• Acne vulgaris, rosacea.
• Sexually Transmitted Infections:
• Chlamydia, syphilis (alternative to penicillin).
• Tick-Borne Diseases:
• Lyme disease, Rocky Mountain spotted fever.
• Other Infections:
• H. pylori eradication (as part of combination therapy), anthrax.
 Contraindications
• Pregnancy and Breastfeeding:
• Risk of fetal harm (tooth discoloration, inhibited
bone growth).
• Children Under 8 Years:
• Permanent tooth discoloration and potential
impact on bone growth.
• Allergy to Tetracyclines:
• Known hypersensitivity to tetracyclines.
 Common Side Effects
• Gastrointestinal:
• Nausea, vomiting, diarrhea, abdominal pain.
• Photosensitivity:
• Increased risk of sunburn.
• Tooth Discoloration:
• Permanent yellowing or graying of teeth in
children.
 Serious Side Effects
• Hepatotoxicity:
• Liver damage, especially in high doses or during
pregnancy.
• Renal Toxicity:
• Exacerbation of renal dysfunction in patients with
pre-existing kidney issues.
• Esophageal Ulceration:
• Risk of esophageal irritation or ulceration if taken
without adequate fluids.
 Nursing Considerations - Part 1
• Allergy Assessment:
• Check for history of tetracycline allergy.
• Pregnancy and Age:
• Contraindicated in pregnant women and children
under 8 years old.
• Liver and Kidney Function:
• Monitor liver and renal function, especially during
long-term therapy.
 Nursing Considerations - Part 2
• Administration:
• Oral: Take on an empty stomach with a full glass of
water, avoid taking with dairy products, antacids,
or iron supplements.
• Remain upright for 30 minutes after taking to
prevent esophageal irritation.
• Patient Education:
• Instruct patients to use sunscreen and protective
clothing to avoid photosensitivity reactions.
• Educate patients on the importance of completing
the full course of therapy.
 Nursing Considerations - Part 3
• Drug Interactions:
• Avoid concurrent use with antacids, calcium,
magnesium, or iron supplements due to reduced
absorption.
• Monitor for Superinfections:
• Watch for signs of secondary infections like oral
thrush or vaginal yeast infections.
• Report Side Effects:
• Instruct patients to report severe gastrointestinal
symptoms, signs of liver dysfunction, or rash.
 Sulfonamide Antibiotics
• Overview
• Broad-spectrum antibiotics that inhibit bacterial
folic acid synthesis.
• Often used in combination with other antibiotics
to enhance efficacy.
• Common examples include Sulfamethoxazole-
Trimethoprim (Bactrim), Sulfadiazine, and
Sulfasalazine.
 Mechanism of Action
• Bacteriostatic:
• Inhibit the synthesis of dihydrofolic acid, which is
essential for bacterial DNA and protein synthesis.
• Synergistic Effect:
• Often combined with Trimethoprim for a more
effective bactericidal action.
 Uses of Sulfonamides
• Urinary Tract Infections (UTIs):
• Commonly used for uncomplicated UTIs.
• Respiratory Infections:
• Acute exacerbations of chronic bronchitis,
Pneumocystis jirovecii pneumonia.
• Gastrointestinal Infections:
• Traveler’s diarrhea, shigellosis.
• Skin and Soft Tissue Infections:
• MRSA skin infections.
• Rheumatic Fever Prophylaxis:
• Prevent recurrent episodes in penicillin-allergic
patients.
 Contraindications
• Allergy to Sulfonamides:
• Known hypersensitivity to sulfa drugs.
• Pregnancy and Newborns:
• Risk of kernicterus and other complications in the
third trimester and neonates.
• Renal or Hepatic Impairment:
• Use with caution in patients with significant
kidney or liver dysfunction.
 Common Side Effects
• Gastrointestinal:
• Nausea, vomiting, diarrhea.
• Skin Reactions:
• Rash, photosensitivity.
• Hematological:
• Mild leukopenia or anemia.
 Serious Side Effects
• Stevens-Johnson Syndrome (SJS) and Toxic
Epidermal Necrolysis (TEN):
• Severe skin reactions that require immediate medical
attention.
• Hematologic Reactions:
• Agranulocytosis, aplastic anemia, thrombocytopenia.
• Renal Toxicity:
• Risk of crystalluria and renal damage, especially with
dehydration.
 Nursing Considerations - Part 1
• Allergy Assessment:
• Verify patient history for sulfa drug allergies.
• Renal Function:
• Monitor BUN and creatinine levels before and during
treatment.
• Hydration:
• Encourage patients to drink plenty of fluids to
prevent crystalluria.
 Nursing Considerations - Part 2
• Administration:
• Oral: Take with a full glass of water, and may be taken
with food to reduce GI upset.
• Patient Education:
• Advise patients to avoid direct sunlight or wear
protective clothing due to photosensitivity risk.
• Monitoring:
• Observe for skin reactions, signs of blood dyscrasias, and
superinfections.
 Nursing Considerations - Part 3
• Drug Interactions:
• Monitor for interactions with anticoagulants (e.g.,
warfarin) and hypoglycemic agents.
• Pediatric Use:
• Avoid in infants less than 2 months old due to the risk of
kernicterus.
• Report Side Effects:
• Instruct patients to report symptoms like rash, sore
throat, fever, or unusual bruising.
 Metronidazole Antibiotics
• Overview
• An antibiotic and antiprotozoal medication.
• Effective against anaerobic bacteria and certain
protozoa.
• Commonly known by the brand name Flagyl.
 Mechanism of Action
• Bactericidal and Antiprotozoal:
• Disrupts DNA synthesis and causes cell death in
anaerobic bacteria and protozoa.
• Selective Toxicity:
• Only targets organisms with anaerobic
metabolism.
 Uses of Metronidazole
• Anaerobic Bacterial Infections:
• Intra-abdominal infections, bacterial vaginosis, and
abscesses.
• Protozoal Infections:
• Trichomoniasis, giardiasis, and amebiasis.
• Clostridium difficile Infections:
• Used in the treatment of mild to moderate C. difficile-
associated diarrhea.
• Preoperative Prophylaxis:
• Given before colorectal surgery to prevent infection.
• H. pylori Infection:
• Part of combination therapy for peptic ulcer disease.
 Contraindications
• Hypersensitivity:
• Known allergy to metronidazole or nitroimidazole
derivatives.
• Alcohol Use:
• Avoid alcohol during treatment and for at least 48 hours
after the last dose to prevent a disulfiram-like reaction.
• First Trimester of Pregnancy:
• Contraindicated during the first trimester due to
potential teratogenic effects.
 Side Effects
1.Gastrointestinal:
1.Nausea, vomiting, diarrhea, metallic taste
2.Central Nervous System:
1.Headache, dizziness, seizures, peripheral neuropathy
3.Allergic Reactions:
1.Rash, pruritus, rare anaphylaxis
4.Hematologic:
1.Rarely causes leukopenia, neutropenia
5.Other:
1.Dark urine (harmless)
 Nursing Considerations
1. Assessment:
1. Monitor for infection signs and hypersensitivity
2. Administration:
1. Oral, IV, or topical; complete full course of therapy
3. Avoidance of Alcohol:
1. Educate on avoiding alcohol during and 48 hours post-treatment
4. Monitoring:
1. Regular blood counts for prolonged therapy
5. Neurological Effects:
1. Watch for numbness, tingling, or seizures
6. Hydration:
1. Encourage fluid intake to prevent dehydration
7. Patient Education:
 Carbapenems
• A class of broad-spectrum β-lactam antibiotics
• Includes imipenem, meropenem, ertapenem, and
doripenem
• Effective against a wide range of Gram-positive
and Gram-negative bacteria, including multi-drug
resistant strains
 Mechanism of Action
• Inhibit bacterial cell wall synthesis
• Bind to penicillin-binding proteins (PBPs), inhibiting
the final stage of peptidoglycan synthesis
• Leads to cell lysis and death of the bacterium
• Resistant to most β-lactamases, which makes them
effective against resistant bacteria
 Uses
1. Severe or High-Risk Bacterial Infections:
1. Used for serious infections like sepsis, pneumonia, and
complicated intra-abdominal infections
2. Multi-Drug Resistant (MDR) Infections:
1. Effective against bacteria resistant to other antibiotics,
including extended-spectrum β-lactamase (ESBL) producing
organisms
3. Complicated Urinary Tract Infections (UTIs):
1. Including pyelonephritis
4. Bacterial Meningitis:
1. Meropenem is used for meningitis due to its ability to
penetrate the blood-brain barrier
5. Skin and Soft Tissue Infections:
 Contraindications
• Hypersensitivity:
• History of severe allergic reaction to carbapenems or
other β-lactam antibiotics (penicillins, cephalosporins)
• CNS Disorders:
• Caution in patients with a history of seizures, especially
with imipenem, which may lower the seizure threshold
• Liver Impairment:
• Adjustments may be necessary in patients with severe
hepatic impairment
• Pregnancy and Breastfeeding:
• Use only if clearly needed, as data on safety are limited
 Side Effects
1. Gastrointestinal:
1. Nausea, vomiting, diarrhea, and abdominal pain
2. Central Nervous System:
1. Headache, dizziness, seizures (particularly with high doses of
imipenem)
3. Allergic Reactions:
1. Rash, pruritus, anaphylaxis (in severe cases)
4. Hematologic:
1. Anemia, leukopenia, thrombocytopenia
5. Renal:
1. May cause nephrotoxicity, especially in patients with pre-existing
renal impairment
6. Superinfection:
1. Risk of secondary infections like Clostridium difficile-associated
 Nursing Considerations
1. Assessment:
1. Monitor for signs of infection and assess for any history of allergy to β-lactam
antibiotics
2. Dosage and Administration:
1. Administer intravenously, ensure the correct dosing, especially in renal impairment
3. Monitoring:
1. Monitor renal and liver function tests periodically
4. Neurological Effects:
1. Observe for signs of CNS toxicity, such as seizures; take caution in patients with
CNS disorders
5. Superinfection:
1. Monitor for signs of superinfection, such as prolonged diarrhea
6. Patient Education:
1. Educate patients about potential side effects and the importance of completing the
full course of therapy
7. Drug Interactions:
1. Be aware of possible interactions with other drugs, especially those that lower the
seizure threshold
 Therapeutic Actions and Indications
• The carbapenems are bactericidal.
• They inhibit cell membrane synthesis in susceptible
• bacteria, leading to cell death.
• These drugs are used to treat serious infections
• caused by susceptible strains of S. pneumoniae,
• Haemophilus infl uenzae, Moraxella catarrhalis,
• S. aureus,Streptococcus pyogenes, E. coli,
Peptostreptococcus,Klebsiella pneumoniae,
• Clostridium clostridiiforme,Eubacterium lentum,
• Bacteroides fragilis, Bacteroides distasonis,
• Bacteroides ovatus, Bacteroides thetaiotamicron,
• Bacteroides uniformis, Proteus mirabilis, P. aeruginosa,
 ANTIMYCOBACTERIALS
• Mycobacteria—the group of bacteria that contain the
• pathogens that cause tuberculosis and leprosy—are classifi
• ed on the basis of their ability to hold a stain even in
• the presence of a “destaining” agent such as acid. Because
• of this property, they are called “acid-fast” bacteria. The
• mycobacteria have an outer coat of mycolic acid that
• protects them from many disinfectants and allows them
• to survive for long periods in the environment. It may be
• necessary to treat these slow-growing bacteria for several
• years before they can be eradicated.
• Mycobacteria cause serious infectious diseases. The
• bacterium Mycobacterium tuberculosis causes tuberculosis,
• the leading cause of death from infectious disease
• in the world. For several years the disease was thought to
• be under control, but with the increasing number of people
• with compromised immune systems and the emergence
• of resistant bacterial strains, tuberculosis is once
• again on the rise.
• Mycobacterium leprae causes leprosy, also known
• as Hansen’s disease, which is characterized by disfi guring
• skin lesions and destructive effects on the respiratory
• tract.
 OTHER ANTIBIOTICS
• There are other antibiotics that do not fi t into
the large
• antibiotic classes These drugs—the ketolides,
lincosamides,
• lipoglycopeptides, macrolides, and
monobactams—
• work in unique ways and are effective against
• specifi c bacteria
 LIPOGLYCOPEPTIDES
• The lipoglycopeptides class of antibiotics was
fi rst introduced
• in 2010. At this time, televancin (Vibativ) is the
• only approved drug in the class.
ANTIRETROVIRAL DRUGS (ARVs)

Nshutiyukuri Claudine
RN,CCTN,MSCN
 ARVs
• Viruses cause a variety of conditions.
• A single virus particle is composed of
• a piece of DNA or RNA inside a protein coat.
• To carry on any metabolic processes, including
• replication, a virus must enter a cell.
• Once a virus has fused with a cell wall and injected
• its DNA or RNA into the host cell, that cell is altered
• that is, it is “programmed” to control the metabolic
• processes that the virus needs to survive.
 ARVs
• The virus, including the protein coat, replicates in the host cell
.
• When the host cell can no longer carry out its own metabolic
functions
• because of the viral invader, the host cell dies and releases
the new
• viruses into the body to invade other cells.
• Because viruses are contained inside human cells
• while they are in the body, researchers have
difficulty
• developing effective drugs that destroy a virus
without
• harming the human host.
 ARVs
•
Antiretroviral drugs are a group of drugs
• work by blocking different stages of
viral cycle. When used in combination,
they function as a biochemical tag team.
 ARVS
• For the purpose of this module, We will focus
on drugs used in HIV/Aids.
 II.2.Goals of Antiretroviral Therapy

Control of viral replication

Prevention or delay of progressive

immunodeficiency

Delayed progression to AIDS

Prolonged Survival

Decreased selection of
resistant virus
 II.3. Efficacy of these goals can be
measured in 3ways:

• Clinically, by a reduction in the number and

frequency of opportunistic infections (OIs)
• Immunologically, by a gradual and steady rise
in the CD4+ cell count
• Virologically, by a decrease in the viral load,
ideally to undetectable levels within 6 months
after initiation of ART
 II.4.Principles of AR therapy

• Antiretroviral agents must be used in

combination for effective treatment of HIV
infection
• Highly Active Antiretroviral Therapy has led
to life expectancies approaching the general
population
• Drug toxicities and the emergence of drug
resistance compromise the efficacy of
antiretroviral agents
 II.4.Principles of AR therapy
Cont’
• Adequately prepare the patient before initiation
of treatment.
• ARV treatment is never an emergency with the
exception of AEB (accidental exposure to blood).
• Prescribe to the patient the drugs that are most
suited to his/her mode of life; drugs with less
frequent dosing are better respected than those
with multiple daily doses (single daily dose is the
ideal treatment).
 Note
• For the best adherence, the patient’s
readiness is the most important aspect in
deciding the time to start antiretroviral
treatment and the near perfect
adherence(>95% ) is almost needed for long
term viral suppression and clinical success.
 II.4.Principles of AR therapy
Cont’d...

• Adequately inform the patient on how he needs

to take his/her drugs and any possible side
effects. A lot of preparatory work must be done
by the different categories of care providers to
ensure adherence.
• Ensure that the patient has people around
him/her who can act as treatment buddies to
support him/her throughout his/her treatment;
and if he wishes, ensure he gets group support
from the community (CDC, 2012).
 II.5. Clinical benefits of antiretroviral therapy

• Antiretroviral therapy increases life expectancy

• Antiretroviral drugs reduce TB and other
opportunistic infections
• Antiretroviral drugs prevent HIV transmission
and reduce incidence
 II.6. ARV Classification
Five approved classes of drugs in the HAART
regimens
1. Nucleoside reverse transcriptase inhibitors
(NRTIs)
2. No-nucleoside reverse transcriptase inhibitors
(NNRTIs)
3. Protease inhibitors( PIs )
4. Entry inhibitors (EIs)
5. Integrase inhibitors
• Each class of ARTs medications interrupts HIV
replication at any direct point in the viral cycle
CCR5
Antagonists

Fusion
Inhibitor NRTIs,
Entry NNRTIs
Inhibitors

Reverse
Transcriptase
Inhibitors
Integrase Protease
Inhibitors Inhibitors
 II.7. Currently Available Drugs

• Nucleoside analogue reverse transcriptase inhibitors

– Zidovudine (AZT, Retrovir)
– Lamivudine (3TC, Epivir)
– Stavudine (D4T, Zerit)
– Didanosine (DDI, Videx)
– Zalcitabine (DDC)
– Abacavir (Ziagen)
• Nucleotide reverse transcriptase inhibitors
– Tenofovir (Viread)
 Currently Available Drugs

• Non-nucleoside reverse transcriptase inhibitors

– Nevirapine (viramune)
– Delavirdine (rescriptor)
– Efavirenz (sustiva)
• Fusion Inhibitors or Entry inhibitors
– Enfuvirtide (T-20)
 Currently Available Drugs
• Protease Inhibitors
• Indinavir (crixivan)
• Nelfinavir (viracept)
• Ritonavir (norvir)
• Saquinavir soft gel (fortovase)
• Amprenavir (agenerase)
• Lopinavir/ritonavir (kaletra)
• Amprenavir/ritonavir
 Currently Available Drugs

• Integrase inhibitors
1. RALTERGRAVIR
2. ELVITEGRAVIR
3. DOLUTEGRAVIR
 II.11. ARVs and breastfeeding

2013
National agencies should decide between promoting mothers with HIV to either
breastfeed and receive ARV interventions or to avoid all breastfeeding
Where the national choice is to promote BF, mothers whose infants are HIV
uninfected or of unknown HIV status should:
• exclusively breastfeed their infants for the first six months of life
• introduce appropriate complementary foods thereafter, and continue
breastfeeding for the first 18 months of life
• breastfeeding should then only stop once a nutritionally adequate and safe diet
without breast-milk can be provided
(strong recommendation, high-quality evidence for the first 6 months;
low-quality evidence for the recommendation of 18 months)
II.12. WHAT ART REGIMEN TO
START WITH
 First line ART regimen options in Adults

• There are four options recommended in first

line regimen for adults with more than 15
years old:
 NRTI NNRTI
1 Tenofovir(TDF) Efavirenz(EFV)
+Lamivudine(3TC)*
2 Tenofovir(TDF) Nevirapine(NVP)
+Lamivudine(3TC)*
3 Abacavir(ABC)+ Efavirenz(EFV)
Lamivudine(3TC)*
4 Abacavir(ABC)+ Nevirapine(NVP)
Lamivudine(3TC)*
*Lamivudine can be substituted by FTC
 Note:
• If contre indication to Efavirenz then give,
Niverapine
• If contre indication to TDF then give Abacavir
Molecule Dosage

Tenofovir(TDF) 300 mg once a day

Abacavir(ABC) 300 mg twice a day or 600 mg once a day

Lamivudine(3TC) 150 mg twice a day or 300 mg once a day

Emtricitabine(FTC 200 mg once a day

)
Efavirenz(EFV) 600 mg once evening

Nevirapine(NVP) 200 mg once a day for 14 days and then 200

mg twice a day
 Prescription of ART first line regimen in
adults
• TDF + 3TC + EFV (FDC): TDF 300mg + 3TC 300mg + EFV 600mg
• ABC + 3TC + EFV: ABC 600mg+ 3TC300mg+ EFV 600mg
(Evening*)
• ABC** + 3TC + NVP:
• Initial Phase (15 Days): ABC 600mg + 3TC 300mg + NVP (200 mg
OD)
• Maintenance phase: ABC600mg+ 3TC300mg(OD) + NVP (200 mg
BID)
• (*) Encourage taking drugs in the evening before 8:00pm due to
daytime side effects of EFV
• (**) Give the formulation of ABC 600mg to facilitate once daily dosage
• TDF + 3TC + NVP: TDF 300mg + 3TC 300mg (OD) + NVP 200mg
(Twice a day).
 Note
• Note: The association of 3 NRTIs
(ABC+3TC+AZT) is possible but because of the
reduced potency should not be considered
except in cases of extreme necessity or after
expert opinion.
Recommended Regimens for Second-
line ART
First-line Regimens Second-line Regimens

TDF+3TC + EFV/NVP AZT+3TC+ATV/r or LPV/r *

ABC+ 3TC+EFV/NVP AZT+3TC+ATV/r or LPV/r *

AZT+ 3TC+EFV/NVP TDF+ 3TC+ATV/r or LPV/r *

 Note

* In case of Hepatitis B co-infection, maintain

TDF: AZT + TDF + 3TC + ATV/r or LPV/r
Molecule Dosage

ATV/r 300 mg 300/100 mg orally

/100 mg (FDC) once a day

LPV/r 200mg/50 400/100 mg twice a

mg (FDC) day
 Note
• For TDF, ABC, AZT refers to the dosing table for
the first line regimen
• NB: The pill burden for Lop/rit regimen is 2
pills twice a day compared to ATV which is one
pill once per day (Both in combination with
NRTIs.
Genotyping and Third Line Initiation

Recommended Regimens for Third-line ART:

• Any patient on the second-line with VL > 2,000
copies/ml based on two consecutive viral load
measurements after 3 months with adherence
support is eligible for third-line ART.
• Identification of treatment failure to the
second-line follows the following algorithm.
 VL at 6M of ART Initiation then every 12 M

VL<2,000 copies/ml VL>2,000 copies/ml

Maintain 2nd line and continue VL monitoring every 12M. (If Address possible treatment failure causes (Adherence,
VL>1,000 copies, Check in 6M) Dosage, Drug interaction, poor absorption).
Perform Genotyping (2tubes EDTA with 4 ml of blood to be
sent to NRL within 24 hours

If VL>2,000

If VL1,000-2,000; ask HIV Expert advice Result available in 2M?

Yes No

Ask an HIV Expert (RBC, Mentors, and DH Clinician) for

Address the cause (Redo, Delay, Lost…)
Result Interpretation

Patient Eligible to 3rd Line?

No Yes

Adherence Support and Maintain or Adjust treatment Adherence Support and Maintain or Adjust treatment
according to Results according to Results
 NB:

• - Third line doses: Refer to Section below (Dose

tables)
• - Patients on 3rd line should receive nutrition
supplement (at least 400 kcal e.g. 500 ml of
porridge per dose)
• - Consider 2,000 Copies/ml as Genotyping
Threshold and 1,000 Copies as Treatment
Failure Threshold
• In Rwanda, the 3rd line regimen combination is:
RAL/ETV/DRV/r*
• - The 3rd line regimen must only be given upon expert
consultation and usually with the assistance of genotyping
test.
• - Before prescribing third-line therapy, the patient MUST
undergo extensive additional adherence counseling and
should have a treatment partner involved with assisting in
adherence.
• - Third-line regimens will only be prescribed at specialized
centers with trained providers.
• - Third line combination can be adjusted based on Genotyping
results and upon HIV Expert view
• -NRTI backbone may be necessary based on genotyping test or
in case of Hepatitis B co-infection
Dosing of Third Line Drugs

Molecule Dosage

Raltegravir 400 mg twice a day

Ritonavir 100 mg twice a day

Darunavir 600 mg twice a day

Etravirine 200 mg twice a day

Recommendations on Monitoring of Adult
Period Laboratory Clinical Psychosocial

Mo (Baseline) CD4, HBsAg, HCV Ab, CRAG TB and STI +

if CD4<200/ml Screening

M1 Creatinine (Clearence) if TDF + +

M2 None + +
M3 Creatinine (Clearence) if TDF TB and STI +
Screening

M6 VL, Creatinine (Clearence) if TB and STI +

TDF Screening

M12 VL, Creatinine (Clearence) if TB and STI +

TDF Screening
 Note:
• (1) VL shall be done at M6 after ART initiation thereafter
every 12 months
• In case of treatment failure, VL will be done 3 months
after adherence intervention
• (3) After the first year adherence shall be assessed
every 3 months in patients demonstrating excellent
adherence for the first year
• (3) After the first year, pharmacy refill shall be done
every 3 months (not monthly) coinciding with clinical and
adherence assessment
• (4) FBC, ALAT and amylase will be done if clinically
indicated
• (5) Genotyping is recommended for patients failing
second line or some special cases failing first line before
ART switching.
 II.14. Limitations and Barriers to
Treatment
• Antiretrovirals are unlikely to eradicate HIV
– Treatment is life-long
• Long-term toxicity
– Mitochondrial toxicity
– Lipid disorders
– Body composition abnormalities
• Drug Resistance
• Cost can also be a barrier for an individual
 II.14. Limitations and Barriers to
Treatment cont’d…

• Lack of transportation and other logistical

problems
• Some medications need to be refrigerated,
which may limit their usefulness in areas
where refrigeration is not available.
• The need for lifelong treatment
II.16. ARVs SIDE EFFECTS
 II.16 .SIDE EFFECTS OF ARV cont’d…
Common Side Effects of NRTIs:
– Mitochondrial Toxicity (associated with inhibition of
mitochondrial polymerase)
– Neuropathy
– Pancreatitis
– Hepatic Steatosis & Lactic Acidosis
• NRTI treatment should be suspended in the setting of rapidly
rising aminotransferase levels, progressive hepatomegaly, or
metabolic or lactic acidosis of unknown cause.
– Myelosuppression including neutropenia & severe
anemia especially in patients with advanced HIV disease
– Symptomatic myopathy / cardiomyopathy
 II.16 . SIDE EFFECTS OF ARV cont’d…
• Common Side Effects of NNRTIs:
• Rash, including Stevens-Johnson syndrome
• Hepatotoxicity (especially NVP)
• Drug-drug interactions
Dosing of Third Line Drugs

Molecule Dosage

Raltegravir 400 mg twice a day

Ritonavir 100 mg twice a day

Darunavir 600 mg twice a day

Etravirine 200 mg twice a day

Recommendations on Monitoring of Adult
Period Laboratory Clinical Psychosocial

Mo (Baseline) CD4, HBsAg, HCV Ab, CRAG TB and STI +

if CD4<200/ml Screening

M1 Creatinine (Clearence) if TDF + +

M2 None + +
M3 Creatinine (Clearence) if TDF TB and STI +
Screening

M6 VL, Creatinine (Clearence) if TB and STI +

TDF Screening

M12 VL, Creatinine (Clearence) if TB and STI +

TDF Screening
 Note:
• (1) VL shall be done at M6 after ART initiation thereafter
every 12 months
• In case of treatment failure, VL will be done 3 months
after adherence intervention
• (3) After the first year adherence shall be assessed
every 3 months in patients demonstrating excellent
adherence for the first year
• (3) After the first year, pharmacy refill shall be done
every 3 months (not monthly) coinciding with clinical and
adherence assessment
• (4) FBC, ALAT and amylase will be done if clinically
indicated
• (5) Genotyping is recommended for patients failing
second line or some special cases failing first line before
ART switching.
 II.14. Limitations and Barriers to
Treatment
• Antiretrovirals are unlikely to eradicate HIV
– Treatment is life-long
• Long-term toxicity
– Mitochondrial toxicity
– Lipid disorders
– Body composition abnormalities
• Drug Resistance
• Cost can also be a barrier for an individual
 II.14. Limitations and Barriers to
Treatment cont’d…

• Lack of transportation and other logistical

problems
• Some medications need to be refrigerated,
which may limit their usefulness in areas
where refrigeration is not available.
• The need for lifelong treatment
II.16. ARVs SIDE EFFECTS
 II.16 .SIDE EFFECTS OF ARV cont’d…
Common Side Effects of NRTIs:
– Mitochondrial Toxicity (associated with inhibition of
mitochondrial polymerase)
– Neuropathy
– Pancreatitis
– Hepatic Steatosis & Lactic Acidosis
• NRTI treatment should be suspended in the setting of rapidly
rising aminotransferase levels, progressive hepatomegaly, or
metabolic or lactic acidosis of unknown cause.
– Myelosuppression including neutropenia & severe
anemia especially in patients with advanced HIV disease
– Symptomatic myopathy / cardiomyopathy
 II.16 . SIDE EFFECTS OF ARV cont’d…
• Common Side Effects of NNRTIs:
• Rash, including Stevens-Johnson syndrome
• Hepatotoxicity (especially NVP)
• Drug-drug interactions
 II.16 . SIDE EFFECTS OF ARV cont’d…

• Common Side Effects of PIs:

• Hyperlipidemia
• Lipodystrophy
• Hepatotoxicity
• GI intolerance
• Glucose intolerance or diabetes mellitus
• Possibility of increased bleeding risk for
hemophiliacs
• Drug-drug interactions
 II.16 . SIDE EFFECTS OF ARV cont’d…

• Common Side Effects of entry inhibitors (EIs)

• Neutropenia and an increased risk of
pneumonia
 II.16. HAART Toxicities: Lipodystrophy
• Body habitus changes
– central fat accumulation
– peripheral fat wasting
• Risk factors
– female gender (maybe get it worse)
– older age
– HAART
– Protease Inhibitor use
Dorsocervical fat pad (“buffalo hump’) in HAART-treated patient
Dorsocervical fat pad and gynecomastia in patient on HAART
Peripheral Lipoatrophy
Facial Lipoatrophy
 II.16. Lipodystrophy:
Treatment Options cont’d…

• Switching Protease Inhibitors out of HAART

regimen
 II.17. ARV-based PEP and PreP PEP)

• ARV-based PEP is used to protect healthcare

workers who have been accidentally exposed
to HIV, in case of rape and/or any risky contact
with HIV infected body fluid.
• It should be started within 72 hours of
exposure.
 II.16 . HIV/HAART Toxicities:
Insulin Resistance cont’d…

• Progression to frank diabetes mellitus possible

• Monitor with fasting glucose values
• Improvement often seen with switching out of
PI-based regimens
• Some success w/t metformin (Glucophage™)
 II.17.PEP and PrEP cont’d
• The recommended post-exposure prophylaxis
drugs are based on the current second and
first line regimen:
• TDF + 3TC / FTC + ATV/r
• AZT + 3TC/ FTC + ATV/r (If no TDF or a
contraindication)
• TDF + 3TC/ FTC + EFV
 Pre-Exposure Prophylaxis, cont’d

• (PrEp)Pre-Exposure Prophylaxis is a new HIV prevention

method in which high risk (eg: sex workers ,MSM,
discordant couple …)people who do not have HIV take
daily pills to reduce their risk of becoming infected
• According to WHO (2015),Oral Pre-Exposure Prophylaxis
(containing TDF) should be offered as an additional
prevention choice for people at substantial risk of HIV
infection as part of combination prevention approaches
 Pre-Exposure Prophylaxis, cont’d
• The pill contains two medicines that are also
used to treat HIV and they can work to keep
the virus from taking hold in individual’s body.
• The drug used for PrEP consiste of a
combination of two HIV medications Tenofovir
and Emtricitabine. This combination is called
Truvada
NB: this pre-exposure prophylaxis is not yet
applied in Rwanda
 Read carefully the provided books:
Karch, A. M. (2013). Focus on
nursing pharmacology.
Philadelphia: Lippincott Williams &
Wilkins.
Jones & Bartlett Learning., & Jones
& Bartlett Publishers.
(2000). Nurse's drug handbook.
Sudbury, MA: Jones and Bartlett
Publishers.

THANK YOU
 Please
• Read carefully the provided books:
• Karch, A. M. (2013). Focus on nursing
pharmacology. Philadelphia: Lippincott
Williams & Wilkins.
• Jones & Bartlett Learning., & Jones & Bartlett
Publishers. (2000). Nurse's drug handbook.
Sudbury, MA: Jones and Bartlett Publishers.

Thank you
 ANTIFUNGAL DRUGS
• .
ANTIFUNGAL
 Antifungal drugs

Systemic & topical

some are fungistatic,

while others are fungicidal
Systemic antifungal drugs for systemic infections

.
 aCTION
• Binds to fungal cell membrane
(Ergosterol)

• Alters permeability & transport

• Fungal Cell death

 AMPHOTERICIN B

• Fungicidal drug at higher concentrations &

fungistatic at lower levels.

• due to its high side effects and high toxicity, it is

reserved for only life threatening fungal infection.
 Clinical use

For systemic disease:slow IV

o Local:
o Keratitis& corneal ulcers: drops, conjunctival irrigation,
o Candiduria: bladder irrigation
o Fungal arthritis: local injection
 INDICATIONS
Amphotericin is the drug of choice for:
-Disseminated histoplasmosis
-Disseminated and meningeal coccidioidomycosis
-Disseminated and meningeal cryptococcosis
-Invasive aspergillosis
-Deep candidiasis
-Mucormycosis
Amphotericin is an alternative drug for:
-Blastomycosis
-Paracoccidioidomycosis
-Extracutaneous sporotrichosis
[Amphotericin is preferred when these mycoses are rapidly
progressive, occur in immunocompromised host or
involve the CNS]
 Side effects
• Infusion related • Cumulative toxicity
Fever & chills,
Nephrotoxicity
Dyspnea,
K & Mg wasting
Nausea &vomiting,
Hypotension, Anemia (↓erythropoietin)
Convulsions

• To reduce the severity of the infusion-related reactions, pretreatment with an

antipyretic (acetaminophen), antihistamines, and antiemetics may be given.
 Side effects cont,d
(the therapeutic index of the drug is very narrow)
-Headache, arthralgias, nausea and vomiting fever and chills,
hyperpnea, shock-like fall in blood pressure (they may
appear during IV infusion and may be reduced by
concomitant administration of
antipyretics ,antihistamine,antivomitif )
-Malaise, weight loss
-Nephrotoxicity (azotemia , decreased GFR, renal tubular
acidosis, renal wasting of K+ and Mg++,). It is common (up
to 80% of patients) and may be severe
-Normocytic anemia, likely due to decreased production of
erythropoietin (frequent)
-Thrombophlebitis
-Delirium, seizures (after intrathecal injection)
 KEY POINTS

• AmphotericinB is not absorbed enterally; hence can be

given orally for intestinal candidiasis.

• Drug concentration achieved in infected skin is very low,

& hence ineffective against superficial fungal infections.

• Penetration in brain & CSF is poor (but extremely

effective in fungal meningitis when combined with 5-FC)
 FLUCYTOSINE (5-FC)
• narrow-spectrum fungistatic
• Water soluble
• Oral only,
Clinical use at present is confined to

combination therapy, either with:

 Amphotericin B for cryptococcal
meningitis , or
 Itraconazole for chromoblastomycosis
 Adverse Effects

Bone marrow toxicity with anemia, leukopenia,

thrombocytopenia,
• GI disturbances
• Mild & reversible liver dysfunction
 KEY POINTS

• Since this is a narrow-spectrum fungistatic, it is

mainly used as an adjuvant drug & not used as a sole
therapy.

• CSF penetration is excellent, hence it is combined

with AmphotericinB in fungal meningitis.
Azoles
 Ketoconazole
Imidazoles Miconazole
Clotrimazole

Azoles
Itraconazole
Fluconazole
Triazoles
Voriconazole
Posaconazole
 Mechanism of Action
Inhibition of fungal
cytochrome P450
enzymes

Reduction of
ergosterol synthesis
 Clinical Use
BROAD SPECTRUM OF ACTIVITY –
Candida,
Cryptococcus,
Blastomyces,
Histoplasma,
Coccidiodes ,
Dermatophytes
 Adverse Effects

Relatively nontoxic.

Minor GI upset

Abnormalities in liver enzymes

(inhibit cytochrome P450
enzymes)

Very rarely, clinical hepatitis

 KETOCONAZOLE

•(older, more toxic, replaced by itraconazole, but less

costly)
•Absorption variable (better in acidic medium)
•Penetration in brain & CSF is poor
•In high doses inhibits adrenocortical steroids
and testosterone synthesis, resulting in
gynecomastia in some males.
 ITRACONAZOLE

•Broad-spectrum antifungal with fungistatic

action
•Action: Inhibits fungal ergosterol synthesis like other
azoles

• Drug absorption is increased by food and by

low gastric PH.

•Penetration of drug in brain & CSF is poor.

• Much more selective than ketoconazole

 FLUCONAZOLE
Broad-spectrum Fungicidal drug;
•It is also somewhat effective against some Gram-
positive & anaerobic bacteria

•Of the orally administered fluconazole 94%

is absorbed;

•Penetration in brain & CSF is good, hence

used for cryptococcal meningitis
 Posaconazole

The newest triazole

It is the broadest spectrum member of the
azole family.
with significant activity against the agents
of zygomycosis and mucormycosis.
 ECHINOCANDINS

Caspofungin

Micafungin

Anidulafungin
 ECHINOCANDINS
Active against candida and
aspergillus, but not c neoformans or
the agents of zygomycosis and
mucormycosis.
 Adverse Effects

 Minor GI side effects

Flushing

 Elevated liver enzymes (caspofungin +

cyclosporine).

Histamine release during IV infusion.

Systemic antifungal drugs for Mucocutaneous infections
 GRISEOFULVIN

• Very insoluble, fungistatic

• Better absorption when given with fatty foods.

• It is deposited in newly forming skin where it
binds to keratin, protecting the skin from new
infection.
• Interferes with spindle formation in dividing
cells and therefore with mitosis
Adverse effects

• Allergic reaction
• photosensitivity
• Hepatitis
• Teratogenesis
 Terbinafine

• Synthetic allylamine.
• Orally Active.
• Dermatophytoses, especially onychomycosis .
• Keratophilic , fungicidal.
• Like the azole drugs, it interferes with ergosterol
biosynthesis, but rather than interacting with the
P450 system, terbinafine inhibits the fungal
enzyme squalene epoxidase. This leads to the
accumulation of the sterol squalene, which is
toxic to the organism.
 Adverse effects

Rare, mild, self-limiting

GI upset
Rash
Pruritis
Headache.
Topical antifungal
therapy
 NYSTATIN

• Only used topically: creams, ointments,

suppositories, and other
• Acts as amphotericin B
• It is not absorbed , unpleasant taste.
• Local candidal infections, oropharyngeal thrush,
vaginal candidiasis.
• adverse effects are rare.
 TOPICAL AZOLES

• Clotrimazole , Miconazole;
• Vulvovaginal candidiasis, oral thrush , dermatophytic
infections, including tinea corporis, tinea pedis, and tinea
cruris.
• Absorption is negligible, and adverse effects are rare.
• Topical and shampoo forms of ketoconazole for
seborrheic dermatitis and pityriasis versicolor.
 TOPICAL ALLYLAMINES

• Terbinafine and Naftifine

• Both are effective for treatment of tinea cruris
and tinea corporis.
• Terbinafine concentrates in skin and
especially at nail beds, making it quite useful
for fungal infection of nails
Read carefully the provided books:
Karch, A. M. (2013). Focus on nursing
.pharmacology. Philadelphia: Lippincott

Williams & Wilkins.

Jones & Bartlett Learning., & Jones &
Bartlett Publishers. (2000). Nurse's
drug handbook. Sudbury, MA: Jones
and Bartlett Publishers.

Thank you
 ANTIPARASITES DRUGS

Nshutiyukuri Claudine RN,CCTN,MSCN

 Antiparasitic drugs
• Antiparasitic drugs are a group of medications
• used in the management and treatment
• of infections by parasites, including :
• protozoa, helminths, and ectoparasites.
• Antiparasitic drugs include several classes
• of drugs that cover a broad range of diseases
• caused by parasites
Anti-protozoal
Drugs
• Protozoal infections may be one or more infection results
from the following:

Amoebiasis, trypanosomiasis, girdiasis, leishmaniasis,

trichomoniasis, Malaria, toxoplasmosis.
 Classification of anti-amoebic drugs

• Luminal amebicides: for treating intestinal infections.

( Diloxanide Furoate, Iodoquinol, Paromomycin, Metronidazole.)
• Tissue amebicides: used to destroy amoebae that have invaded
tissue, rapidly absorbed into the bloodstream and transported to
the site of infection.( Metronidazole, Tinidazole).

• For amebic liver abscess: .( Metronidazole, Tinidazole,

Diloxanide Furoate).
 Metronidazole & Tinidazole
• Metronidazole is an antibiotic, amebicide, and antiprotozoal

• Effectively eradicates intestinal and extraintestinal tissue

infections. (drug of choice in the treatment of extraluminal
amebiasis)
• It kills trophozoites but not cysts of E histolytica

• Tinidazole:Similar activity and a better toxicity ,Simpler

dosing regimens ( longer t½)

Mechanism of action
The reduced product is cytotoxic, it targets DNA & other
proteins, resulting in cell death.
Clinical use:
• Amoebiasis, Giardiasis, Trichomoniasis, Anaerobic infections,
Pseudomembranous enterocolitis, H. pylori – induced peptic ulcer,
Oral infections

Side effects:
• GI disturbance, Dry mouth, Metallic taste,
• headache, dizziness, dark urine.
• metronidazole has a disulfiram-like effect, so that Nausea and
Vomiting, flushing & tachycardia can occur if alcohol is ingested
during therapy.
• I.V.: seizures or peripheral neuropath
Drug interactions
- Potentiate Anticoagulant effect of Warfarin.
- Metabolism of Metronidazole induced by
Phenytoin & Phenobarbitone
- Cimetidine may inhibit it.

Contra-indications :
• First trimester of pregnancy
• Chronic alcoholism
 Emetine & Dehydroemetine
• Effective against tissue trophozoites of E histolytica, (not used nowadays
because of high systemic toxicity )

• Dehydroemetine is preferred: better toxicity profile.

• Acts by inhibiting protein synthesis

• used SC or IM.

Side effects:
• Injection site : pain, tenderness, and sterile abscesses.
• Cardiac side effects like myocarditis, tachycardia, Hypotension,
Cardiac arrhythmias
• Stiffness of muscles
 Diloxanide furoate

• Effective luminal amebicides ,

• Used with metronidazole to treat serious
intestinal and extraintestinal infections, by
unknown mechanism.
• Side effects:
GI disturbance, Headache, Rash, Pruritus.
 Nitazoxanide

• Used against Giardia lamblia

• The active metabolite, inhibits the pyruvate: ferredoxin
oxidoreductase pathway. (essential to anaerobic energy
metabolism.)
• Appears to have activity against metronidazole-resistant
protozoal strains
• Is well tolerated {Greenish tint to urine}
 Paromomycin Sulfate

• Not significantly absorbed from the GIT. (only as a

luminal amebicide).
• Action: Inhibits protein synthesis
• Side effect: GI disturbance, ototoxicity,
nephrotoxicity
 OTHER ANTIPROTOZOAL DRUGS

Trypanosomiasis
Leshmaniasis :
• Sodium
Pentamidine
stibogluconate
• Pentamidine
Suramin
• Amphotericin
Melarsoprol
• Miltefosine
Nifurtimox
• Benznidazole
 Pentamidine
• Active against trypanosomatid protozoans but toxicity is
significant.
• Parentrally or inhalation
• Only trace amounts appear in the CNS, ( not effective against
CNS african trypanosomiasis.)
• The mechanism of action may interfere with synthesis of RNA,
DNA and proteins.
 INDICATIONS
• Pneumocystosis
• African Trypanosomiasis (Sleeping Sickness)
• Leishmaniasis

Side effects: Highly toxic

• Rapid IV : Severe Hypotension, Tachycardia, Dizziness.
• IM : Pain at the injection site, Sterile abscesses.
• Inhaled : Cough, Dyspnea, Bronchospasm.
 Suramin
• Is the first-line therapy for early hemolymphatic East African trypanosomiasis .
• Does not enter the CNS .
• It acts by inhibiting enzymes of energy metabolism

• Side effects: common.

• Immediate reactions : Fatigue, N/V
• Rarely: Seizures, Shock.
• Later reactions :Paresthesias, Renal Abnormalities, Hemolytic Anemia.
 Nifurtimox

• Used for American trypanosomiasis (Chagas'

disease).
• It acts by generating toxic radicals
• Side effect: GI disturbance, fever, rash,
neuropathies, and seizures.
 Sodium Stibogluconate
• First-line agents for cutaneous and visceral leishmaniasis

• IV,IM

• Action: It acts by inhibiting glycolysis and fatty

acid oxidation
• A/E: Few but increases over the course of therapy.
• GI symptoms, fever, headache, myalgias, arthralgias,rash.

• IM: painful and lead to sterile abscesses.

• arrhythmias & nephrotoxicity

Antimalarial drugs
.
 CHLOROQUINE
 For treatment and chemoprophylaxis since the but drug
resistance developed .
Oral use

Antimalarial Action:
Highly effective blood schizonticide.

 Moderately effective against gametocytes of P vivax, P

ovale, and P malariae but not against those of P falciparum.
 Not active against liver stage parasites.
MECHANISM OF ACTION

Acts by :
concentrating in parasite food vacuoles,
preventing the biocrystallization of the hemoglobin
breakdown product, heme, into hemozoin, and
thus eliciting parasite toxicity due to the buildup of
free heme.
 INDICATIONS

1.Treatment.
2.Chemoprophylaxis.

3.Amebic Liver Abscess.

Drug of choice in the treatment of nonfalciparum and sensitive

falciparum malaria.

 It is still used to treat falciparum : safety, low cost, antipyretic

properties, and partial activity.

Does not eliminate dormant liver forms of P vivax and P ovale, and for

that reason Primaquine must be added for the radical cure of these
 ADVERSE EFFECTS

Usually very well tolerated

Pruritus, GI disturbance, headache, malaise, blurring of vision, and
urticaria

Rare : hemolysis in G6PD-deficient persons, impaired hearing,

agranulocytosis, alopecia, bleaching of hair, hypotension,

Large IM injections or rapid IV infusions : severe

hypotension and respiratory and cardiac arrest.
 QUININE & QUINIDINE

•First-line therapies for falciparum malaria.

•Oral administration and slow IV administration
•Higher plasma levels and half-life in infected persons than in
healthy controls, but toxicity is not increased, apparently because of
increased protein binding.
•Action: it may act like chloroquine
ANTIMALARIAL ACTION

Quinine:
 Is rapid-acting, highly effective blood schizonticide
against the 5 species of human malaria parasites.
.
CLINICAL USES:
PARENTERAL TREATMENT OF SEVERE FALCIPARUM MALARIA

Quinidine : parenteral treatment of severe

falciparum malaria. continuous IV infusion;
cardiac monitoring.
change to an effective oral agent as soon as the
patient has improved and can tolerate oral
 Adverse Effects

 Cinchonism or quinism :
 Hypersensitivity reactions
 Tinnitus,
 Hypoglycemia
 Headache,

 Nausea,  Too-rapid IV infusions :

 Dizziness, Severe hypotension
 Flushing,  IV Quinidine : ECG
 Visual Disturbances
 Black water fever
abnormalities.
 rare severe illness
 marked hemolysis ,
 hemoglobinuria
 MEFLOQUINE

Used in chloroquine-resistant strains of P falciparum and

other species.
Is chemically related to quinine.
Can only be given orally because severe local irritation
occurs with parenteral use.

Has strong blood schizonticidal activity against P

falciparum and P vivax,
 ADVERSE EFFECTS

GI disturbance, Rash, Dizziness,

Leukocytosis, Thrombocytopenia,
Aminotransferase Elevations
Arrhythmias , bradycardia.

Considered safe in young children and throughout

pregnancy.
 PRIMAQUINE

Hepatic stages of all human malaria parasites.

Chemoprophylaxis against all malarial species.
It is active against the dormant stages of p vivax and p ovale.
Acts against erythrocytic stage parasites, but this activity is too
weak to play an important role.
 ADVERSE EFFECTS

Generally well tolerated.

• GI disturbance, Headache
•Leukopenia, Agranulocytosis,
•Cardiac Arrhythmias, Hemolysis
Not to be given parenterally because it may induce marked
hypotension.
It should be avoided in pregnancy
INHIBITORS OF FOLATE SYNTHESIS

Pyrimethamine ,Proguanil
•Used in combination regimens, in the treatment and prevention of malaria.

•Slowly but adequately absorbed from the GIT.

Fansidar, a fixed combination of the sulfonamide sulfadoxine and

pyrimethamine .
Act slowly against erythrocytic forms of susceptible strains of all
human malaria species.
Proguanil also has some activity against hepatic forms.

Neither drug is adequately gametocidal or effective against the

persistent liver stages of p vivax or p ovale.
 MECHANISM OF ACTION

Selectively inhibit plasmodial dihydrofolate reductase, a key enzyme

in the pathway for synthesis of folate.
Sulfonamides and sulfones inhibit another enzyme in the folate
pathway, dihydropteroate synthase.

Side effects: GI Symptoms, Skin Rashes, Itching.

Proguanil: Mouth Ulcers, Alopecia .
Proguanil , Fansidar are considered safe in pregnancy
 Antibiotics acting on malaria
Folate antagonists and sulfonamides ,bacterial protein synthesis inhibitors
None should be used as single agents because their action is much slower
than that of standard antimalarials.
Tetracycline : erythrocytic schizonts , but not active against liver stages.
Doxycycline : falciparum malaria in conjunction with quinine, allowing a
shorter and better-tolerated course of that drug, it has also become a
standard chemoprophylactic drug,
Clindamycin , Azithromycin , Fluoroquinolones
 HALOFANTRINE & LUMEFANTRINE

Against erythrocytic (but not other) stages of all four malaria

species.
Side effects : GI disturbance, cough, rash, headache, pruritus, and
elevated liver enzymes.
 ARTEMISININ & ITS DERIVATIVES

Artemisinin: used orally.

Analogs are:
 Artesunate (water-soluble; oral, IM, IV and rectally),
Artemether (lipid-soluble; oral, IM, and rectally),
Dihydroartemisinin (water-soluble; oral).
They are very rapidly acting blood schizonticides against all human
malaria parasites, no effect on hepatic stages.
 MECHANISM OF ACTION

The parasite when it infects a RBC, it consumes Hb within its digestive

vacuole, liberating free heme, The iron in heme interacts with
Artemisinin producing reactive oxygen radicals which damage the
parasite leading to its death
 Or inhibition of a parasite calcium transporter.

Artemisinin-based combination therapy is now the standard for

treatment of uncomplicated falciparum malaria in nearly all areas
endemic for falciparum malaria.
 Side effects:
• GI disturbance, dizziness, neutropenia,
anemia,hemolysis, elevated liver enzymes,
allergic reactions.
 ANTIHELMINTIC DRUGS
BENZIMIDAZOLEs
1.ALBENDAZOLE:
 It possess broad-spectrum activity . It is the drug of
choice for treatment of
1. Hydatid disease and
2. Neurocysticercosis.
 It is also a major drug the treatment of (intestinal
nematodes) :
1. Ascariasis,
2. Trichuriasis,
3. Strongyloidiasis,
4. Enterobius vermicularis (pinworm),
5. Nector americanus, & Ancylostoma duodenale
(Hookworms) infections.
 Albendazole cont’d

Mechanism of action:

 Inhibits microtubule synthesis and glucose uptake

 It has larvicidal effects on hydatid disease, cysticercosis,

ascariasis, and hookworm infection.

 Also, ovicidal in ascariasis , ancylostomiasis

(hookworm), trichuriasis
 Pharmacokinetics of Albendazole:

• It is administered orally, and absorbed

erratically (unpredictable), absorption can be
increased with fatty meal.

• It is metabolized in the liver rapidly to its

active metabolite albendazole sulphoxide. (1 st
pass metabolism)
 Albendazole cont’d
 It has a plasma half life of 8-12 hours
 Sulphoxide is mostly (80%) protein bound , distributed
to the tissues and enters the bile, cerebrospinal fluid, and
the hydatid cyst.

 urinary excretion
 Clinical uses of albendazole:

 It is administered on empty stomach when used

against intraluminal parasites but with fatty meal
when against tissue parasites.

1. Ascariasis, trichuriasis, hookworm, pin worm

infection (intestinal):
Acheives 100% cure in pinworm infection and high
cure rates for others or marked reduction in eggs
counts.
2. Hydatid diseases:
Drug of choice, with meals.
Bone cyst may require treatment for 1 year.

 If patients are to be treated surgically, both albendazole

and praziquantel are used preoperatively for one month
to reduce cyst fluid leakage. After surgery albandazole
should be continued for a whole month.
 Albendazole cont’d

3.Neurocysticercosis: It is the drug of choice.

It is effective for symptomatic parenchymal and
interventricular cysts. Less effective in arachnoid cyst.
 It is superior to Praziquantel for neurocysticercosis for the
following:
1. Shorter course of treatment.
2. It is cheaper
3. It is co-administeration with steroid increases its absorption
4. It is better in penetration arachnoid space..
5. It is also effective for ocular cysts.

4. Other infections: Drug of choice in cutaneous and visceral

larvea migrans , intestinal cappillariasis, microsporidial
infections, gnathostomiasis, trichinosis, clonorchiasis,
opisthorchiasis, toxocariasis, and loiasis.
 Albendazole con’d

N.B:In intestinal nematodes, treatment in days

But in hydatid disease & Neurocysticercosis, the treatment take longer
duration

Adverse effects:
 In short term use there is no significant adverse effects.

 In long term use: abdominal distress, headache, fever, fatigue,

alopecia , increased liver enzymes , pancytopenia. Blood counts and
LFT should be carried out regularly.
Not given during pregnancy and in hypersensitive people.
Safety in children is not established in children below 2 years of age.
 MEBENDAZOLE (Vermox)
 it is a synthetic benzimidazole
 it has wider spectrum and is safe

Mechanism of action: Similar to albendazole

Effecacy influenced by: GI transit time, intensity of
infection, and strain of parasite.

It is also used to kill hook worm, pin worm , ascaris and

trichuris eggs.
 Mebendazole con’t

Pharmacokinetics:
1. Less than 10% of orally administered drug is absorbed
2. Absorption increases with fatty meals
3. Absorbed drug is 90% protein bound
4. It has half life of 2-6 hours
5. It is primarily excreted in bile.
 Mebendazole con’t
Clinical uses:

 It is taken orally before or after meal, tablets should be

chewed before swallowing.

 Ascaris lumbricoides , trichuris trichiura , hookworm and

trichstrongylus; It is useful drug in case of mixed infection
by these parasites.

 in adults and children over 2 years cure rate is 90-100 %

except hookworm but a marked reduction in worm burden
occurs
 Mebendazole indication cont’d
 Intestinal cappilliaris
 Trichinosis: It has limited efficacy against adult worm.
 Corticosteroids coadministered in sever infection.
 Mebendazole con’d
Adverse effects and precautions :
1. No adverse effects in short term therapy except for mild GI disturbances.

2. With high dose hypersensitivity reactions, agranulocytosis , alopecia,

elevation of liver enzymes.

3. Contraindicated in pregnancy in first trimestre.

4. Used with caution under 2 years of age may cause convulsion in this group.

5. Dug drug interaction: carbamazepine or phneytoin  ↓ conc.

6. Cimetidine  ↑ conc.

7. used with caution in cirrhosis

 Thiabendazole
 It is a benzimidazole. It is tasteless and insoluble in water.

 It is a chelating agent and forms stable complexes with metals

including iron but does not bind with calcium.

 It is rapidly absorbed orally

 It has half life of 1.2 hrs

It is completely metabolized in liver and 90% is excreted in

urine

 It can also get absorbed through the skin. Thus, could be

applied in creams.
 Thiabendazole con’d:

 Mechanism of action: similar to other benzimidazoles.

 It is ovicidal for some parasites.

 It also possesses immunosuppressive, antipyretic, and mild
antifungal and scabicidal (destroying the itch mite causing
scabies ) effects.
 Clinical uses:
 Should be given after meals and tablets should be
chewed

 For strongyloides (threadworms) infections:cure rate is

93%
 For cutaneous larval migrans thiabendazole cream is
effective and applied topically or given orally
 Also effective for intestinal capillariasis and scabiasis.
 Thiabendazole cont’d
 Adverse reactions and contraindications:
1. It is more toxic than other benzamidazoles
2. GI disturbances
3. Pruritus, headache, drowsiness, neuropsychiatric symptoms
rarely may cause tinnitus, bradycardia, hypotension,
hyperglycemia, convulsions, neutropenia and other adverse
effects may occur.
4. Irreversible live failure.
5. Fatal Stevens–Johnson syndrome (inflammation of the skin)
6. Not used in children below the weight of 15 kg, during
pregnancy, hepatic and renal diseases.
 PYRANTEL PAMOATE
 It is a broad-specturm antihelminthic
 It is not effective against trichuriasis (whipworms) and
trichostrongylus orientalis infections, yet oxantel
pamoate is considered effective against trichuriasis. Both
drugs can be combined for their synergistic effect.
 Pharmacokinetics:
 It is poorly absorbed orally. Active mainly against
luminal organisms.
 Half of the drug is excreted unchanged in the feces.
 Mechanism of action:
 It is a depolarizing neuromuscular blocking agent that
causes release of acetylcholine and inhibition of
cholinesterase leading to the paralysis of worms followed
by their expulsion from the GIT.
 Pyrantel pamoate (cont’d)
Efficacy and clinical uses:
 it is very effective against mature and immature luminal
organisms, but not effective against migratory stages in the
tissues or against ova

 Enterobius vermicularis (pinworm).

 Ascaris lumbricoids (common roundworm)

 Ancylostoma duodenale (hookworm) single dose for light

infection but a 3-day course is necessary for heavy infection
especially N americanus infection.
 Pyrantel pamoate cont’d:
Adverse effects are infrequent and mild.
1. GI disturbance
2. Drowsiness, headache ,insomnia.
3. Rash, fever
Contraindications:
1. Should not be used in liver diseases.
2. Pregnancy
3. In children under 2 years of age
 PIPERAZINE
 Only used for the treatment of ascariasis.
 It is readily absorbed orally and excreted in urine

Mechanism of action:
It causes paralysis of ascaris by blocking
acetylcholine at the myoneural junction, expelling
the live worm by normal peristalsis.
 Piperazine cont’d

• Treatment is continued for 3-4 days or

repeated after one week in case of heavy
infections.
 Piperazine cont’d
 Adverse effects:
1. GI disturbances
2. Neurotoxicity, allergic reactions serum sickness like
syndrome
 Contraindications
1. Epilepsy or chronic neurologic disease
2. Impaired liver or kidney functions
3. Pregnancy
4. Malnutrition
Drugs used for treating human intestinal nematodes (single
dose unless otherwise stated

Ascariasis Hookworm enterobius tricuris strongyloides

Piperazine ++ + ++ - -

Pyrantel pa ++ ++ ++ - -

Albendazole ++ ++ ++ + +

Mebendazole ++ ++ ++ + +

Thiabendazole n/a n/a n/a n/a ++

Ivermectin n/a n/a n/a n/a ++

 Drug treatment for tape worm(cestodes)
infection

• Niclosamide
• Praziquantel
• Albendazole
 NICLOSAMIDE
 It is useful for the treatment of adult tape worm (cestodes)
infestation
 Mechanism of action:
Adult worm is rapidly killed by inhibition of the oxidative
phosphorylation or stimulation of ATPase activity.
 has no effect on ova
 Pharmacokinetics:
 It is not absorbed from the gut
 Neither drug nor its metabolites are found in the blood or
urine.
 Niclosamide cont’d
 Clinical uses:
A. T. Saginata (Beef tape worm),T. solium (pork tapeworm), Diphyllobothrium
latum (fish tapeworm)
 In case of T. solium after 2 hrs of treatment, purge of magnesium sulphate should be
given to eliminate all mature segments.
 Not effective against cysticercosis or hydatid disease b/c it’s not absorbed from the
gut
 Hymenolepis nana
 H diminuta and Dipylidium caninum
 Alternative for Fasciolopsis buski, Heterophyes heterophyes, Metagonimus
yokogawi.
 Niclosamide cont’d
• Adverse effects:
• Mild, infrequent and transitory GI disturbances
• Alcohol consumption should be avoided
• Not indicated in children under 2 years of age
or pregnancy.
 Diethylcarbamazine
 The drug of choice for the treatment of filariasis,
loiasis and tropical eosinophilia.
Pharmacokinetics:
 It is a synthetic derivative of piperazine
 Rapidly absorbed from the gut
 It has a half life of 2-3 hours which increases in
alkaline urine up to 10 hours.
 Equilibrates with all tissues except fat
 It is excreted in urine unchanged.
 Dosage is reduced in urinary alkalosis and renal
impairment.
 DIETHYLCARBAMAZINE con’d
 Mechanism of action:
 It immobilizes microfilariae in tissues and alters its surface
structure, making them more susceptible to destruction by
host defense mechanism

 Unknown mechanism against adult worms

 It also possesses an immunosuppressive effects

 It has no teratogenic effects on experiment animals

 DIETHYLCARBAMAZINE
con’d
 It is a drug of choice for the treatment tissue cestodes,
W. bancrofti, B. malayi, B. timori, and Loa loa.

 Microfiliariae are rapidly killed. Adult worms are killed

slowly requiring several courses of treatment. Adult worms
are either killed or sterilized.

 It is highly effective against L. loa.

 DIETHYLCARBAMAZINE con’d

 Anti histamines and corticosteroids are given in allergic

manifestations.

Complete Cure may be require several courses of treatment over 1-2

years.

 The drug may be used in prophylaxis for loiasis, bancroftian, and

Malayan filariasis
 Tropical (pulmonary) eosinophilia
Mansonella streptocerca
 DIETHYLCARBAMAZINE con’d
Drug induced/ Reactions induced by Dying
parasites:
Fever , malaise, papular rash, headache, GI
disturbance, cough, chest, muscle, joint pain
Leukocytosis, proteinurea, ↑ eosinophilia
 Retinal hemorrhage
 Encephalopathy
 Lymphangitis and lymphadenopathy.
 DIETHYLCARBAMAZINE con’d
 Contraindications and cautions
1. Hypertension
2. Renal disease
3. Patient suspected of having malaria
4. Patients with lymphangitis
 IVERMECTIN
• It is the drug of choice for treatment of
strongyloidasis and onchocerciasis
• It is used orally and is rapidly absorbed,
• It has a half-life of 16 hrs
• It is exclusively excreted in feces
 IVERMECTIN cont’d
• Mechanism of action:
• It intensifies GABA –mediated transmission
of signals in peripheral nerves  paralyzing the
worm.
• In onchocerciasis it is microfilaricidal. It does
not kill the adult worm
 IVERMECTIN cont’d
• Clinical uses:
• Onchocerciasis: with the 1st treatment,
patients with microfilariae in the cornea or
anterior chamber may be treated with
corticosteroid.
 IVERMECTIN cont’d
• Strongyloidiasis: in immunosuppresed patient,
repeated treatment is often needed.
• Bancrofti filaricidal: as it is mirofilaricidal
• It is also used for scabies, lice, and cutaneous
larva migrans.
• Eliminates adcarid worms
• Reduces microfilariae in Brugia malayi and M
ozzardi.
 IVERMECTIN cont’d
 Adverse effects:
1. Fatigue
2. dizziness,
3. GI disturbance
 In Onchocerciasis:
1. Mazotti reaction: fever, headache, dizziness,
somnolence (state of being drowsy), weekness,
rash ,diarrhea, arthralagia, hypotension,
lymphadenitis, peripheral edema due to killing of
microfiliariae, for this steroids may be necessary
for several days
2. Swelling and abscess at site of adult worm
3. Punctuate corneal opacities.
 IVERMECTIN con’d
 Contraindication:
1. other drugs that enhance GABA activity e.g
Barbiturates, bnezodiazepines, valproic acid.
2. pregnancy
3. Impaired blood brain barrier
4. Children under 5 years of age.
 BITHIONOL
 It is the drug of choice for the treatment of
fascioliasis (sheep liver fluke)

It is also used as an alternative for praziquantel in

treating pulmonary paragonimiasis
Repeat doses in case of cerebral paragonimiasis.

 Pharmacokinetics:
 It is orally administered and excreted in urine.
 BITHIONOL
 Adverse effects:
1. GI disturbance
2. Dizziness,headache
3. Pruriuts ,urticaria,Leucopenia
 Contraindications and precautions:
1. hepatitis,
2. leucopenia
3. Used with caution under 8 years of age.
 ANTISEPTICS AND
DISINFECTANTS
They have specific use and their selectivity
is very low.
 General information
• Disinfectants are strong chemical agents that inhibit or kill
microorganisms

• Antiseptics are disinfecting agents with sufficiently low

toxicity for host cells→can be used directly on skin, mucous
membranes, or wounds

• Sterilants kill both vegetative cells and spores when applied to

materials for appropriate times and temperatures
 IDEAL DISINFECTANT
• effective at room temperature,
• noncorrosive and nontoxic,
• inexpensive,
• capable of killing the vegetative form of all
pathogenic organisms,
• require limited time of exposure
 antiseptic
• The ideal antiseptic has to have similar properties as
an ideal disinfectant. But the primary importance for
antiseptics is the selective toxicity which means
toxicity to microorganisms but not to human cells.
The degree of selectivity of the antiseptic agents can
change depending on the tissues they contact.
 Indications
Antiseptic drugs are used in:
• The treatment of skin infections
• Prevention of infections in cuts and wounds
• Cleaning the skin area of surgery from
microorganisms
• Prophylaxis and treatment of infections in mucosal
areas such as mouth, nose and vagina that are open
to environment
• As a scrub for surgeans and the medical personnel
 STERILANTS
Sterilants kill both vegetative cells and spores when
applied to materials for appropriate times and
temperatures.
Handwashing is the most important means of
preventing transmission of infectious agents from
person to person or from regions of high microbial
load such as mouth, nose, or gut to potential sites of
infection.
REGULAR HANDWASHING IS BEST DONE WITHOUT
DISINFECTANTS TO MINIMIZE DRYING, IRRITATION
OR SENSITIZATION OF SKIN.
 CLASSIFICATIONS OF ANTISEPTICS
AND DISINFECTANTS
1. Those that denature proteins,
2. Those that cause osmotic disruption of the cell,
3. Those that interfere with specific metabolic
processes.

• The first and second classifications are tend to kill the organisms.
• The third one affects cell growth and reproduction without killing the
cell.
 MECHANISM OF ACTION
Phenols, iodine, alcohols, aldehydes and metallic
compounds denature proteins and DNA bases.

Cationic detergents interfere with plasma membrane’s

permeability and cause leakage of enzyme,
coenzyme and metabolites.

Oxidizing compouns oxidize functional molecules in the

microorganisms.
 HALOGENS
• The halogens and halogen – releasing compounds
include some of the most effective antimicrobial
compounds used for disinfection and antisepsis.
• Iodine and chlorine are the most effective halogens
with bromine and fluorine being less active.
• Because of the irritating nature of the products of
sodium hypochlorite, it is currently used primarily as
a disinfectant.
 IODINE
Tincture of iodine (2g I, 2.5 g NaI and 50%
ethanol to 100 mL).
Powerful antiseptic for intact skin, should avoid
contact with mucosas. Can cause serious
hypersensitivity reactions, staining of skin and
dressing can happen and this limits its use.
 .
Iodophores less irritating less hypersensitivity compared with
tincture of iodine.
Povidon iodine (A complex of I with polivinyl pyrrolidone-surface
active agent-). Can be used as antiseptics or disinfectants.
Kill vegetative bacteria, mycobacteria, fungi, lipid containing
viruses. They kill spores as well on prolonged use
 CHLORINE
Chlorine is a strong oxidizing agent. Hypochloric acid
and sodium hypochlorite (household bleach 5.25%)
are bactericidal and effective disinfectants
1:10dilutions it provides 5000 ppm of chlorine. This is
the concentration recommended for disinfection of
blood spills. Dilutions are made with tap water and
when the opaque bottle is tightly closed it preserves
its activity.
 ALDEHYDES
2-8% of formaldehyde can be used as a sterilizing agent for
surgical instruments. Not corrosive for metal, plastic or
rubber. Broad spectrum of activity against microorganisms
and viruses. Alkylate chemical groups in proteins and nucleic
acids. It is especially useful for instruments that can not be
autoclaved. (hemodialyzers, dental handpieces, respiratory
therapy equipment). 3% solution is useful topically on hands
and feet in treatment of hyperhidrosis. Presence of organic
material, low concentration, and perfusion inefficiency can
cause failure.
Formaldehyde is marketed as the 34-38% solution and is called
formol and contains methyl alcohol in order to prevent
polymerization and precipitation of formaldehyde.
Formaldehyde has a pungent odor and is highly
irritating to repiratory mucous membranes and eyes
at concentration of 2-5 ppm is rarely used because of
its toxicity and tendency to cause sensitization with
repeated contact. The relative risk of formaldehyde
as a human carcinogen when used as a disinfectant is
significant.
Glutaraldehyde 2% w/v pH7.4-8.5 is not significantly
affected by the presence of organic material and is
relatively nonirritating, nonallergenic and
noncorrosive when proper safeguards are employed.
Activated solutions are bactericidal, sporicidal,
fungicidal and virucidal. Exposure of skin and mucus
membranes can cause sensitization, irritation and
damage. Protection of health care workers from
exposure to glutaraldehyde conc>0.2 ppm is advised It
is important to use it only in well – ventilated areas
and never using it as a surface disinfectant.
 OXIDIZING AGENTS
Hydrogen peroxide is the most common of a number of
oxidizing compounds that have been used as
antiseptics. It is also effective in injured skin due to its
bubbling effect. 3% solution is effective
Concentrations potentially useful for antisepsis are
effective against vegetative bacteria, higher
concentrations are sporicidal
Disinfection of respirators, acrylic resin implants, plastic
eating utensils, soft contact lenses, cartons for milk or
juice
10-25% conc is sporicidal
 PHENOLS
Phenol is the oldest surgical antiseptic but is no longer
used even as a disinfectant because of its corrosive
effect on tissues and its carcinogenic effects.
Phenolic derivatives (o-phenylphenol-coal tar
distillates- etc) can be used. Skin absorption and skin
irritation still occurs with these derivatives.
Detergents are added to formulations to clean and
remove organic material that may decrease the
activity of these compounds.
• They are bactericidal , fungicidal and inactivate
lipophilic viruses. Not sporicidal. Used on floors,
beds, countertops and benchtops
• Disrupt cell walls and membranes, precipitate
proteins and inactivate enzymes

• Hexachlorophen as skin disinfectant has no longer

been used because of its neurotoxic effects
 Chlorhexidine
Chlorhexidine was approved for use in surgical scrubs
It is highly effective against gram-positive organisms,
vegetative bacteria, mycobacteria, moderately active
against fungi and viruses, spore germination is also
inhibited. Strongly adsorbs to bacterial membranes
and causes leakage of small molecules and
precipitation of cytoplasmic proteins.
Water soluble chlorhexidine digluconate is used as an antiseptic.
Most effective against gram- positive cocci and less active
against gram-positive and gram-negative rods, spore
germination is also inhibited.It strongly adsorbs to bacterial
membranes and causes leakage of small molecules and
precipitation of cytoplasmic proteins. It is resistant to
inhibition by blood or organic material. Anionic or nonanionic
agents in moisturizers, soaps,surfactants neutralize its action.
Used in oral rinses, should not be used during surgery of the
middle ear, causes sensorineural deafness.
 SURFACE ACTIVE AGENTS
These are compounds that produce a detergent effect. They are
quaternary ammonium compounds.
Cationic agents were used as cold sterilization solutions. But they
are ineffective against bacterial spores, tubercle bacilli, fungi,
viruses and many gram-negative bacteria. The bactericidal
action of these compounds is due to inactivation of energy-
producing enzymes, denaturation of proteins and disruption
of cell membrane.

Cetylpyridinium chloride, benzethonium chloride and similar

cationic agents are used in mouth rinses and sore throat
remedies.
They bind to the surface of colloidal protein in blood,
serum, milk and to fibers in cotton, mops, cloths and
paper towels (inactivation). Anionic detergents also
inactivate them.
They are also used for sanitation of floors and bench
tops. Since their toxicity is low they are used as
sanitizers in food production facilities.
Polyhexamethylene biguanide used in drop form for
acanthamoeba keratitis.
 HEAVY METALS
Mercury and silver compounds were used as
antimicrobial agents. Silver nitrate was commonly
used in dentistry to treat oral ulcers but is no longer
used because it delays healing and alters cellular
morphology. In medicine, silver nitrate eyedrops
remain useful in the prophylaxis of gonococcal
infection in the newborn.
Mercury is an environmental hazard, however,
thiomersal (0.001-0.004%) is still used as a
preservative of vaccines, antitoxins and immune sera
Benzoic acid and salts, parabens
-alkyl esters of p-hydroxybenzoic acid
Sorbic acid and salts, phenolic compounds
Quaternary ammonium compounds, alcohols also used
 Sterilization
• It is the killing of all forms of microorganisms.

• Dry heat
• Steam
• Chemical vapor
• Ethylene oxide gases
• Formaldehyde gases
• Ultraviolet radiation
• Gamma radiation
• Filtration
ACTIVITIES OF DISINFECTANTS
READ CAREFULLY THE PROVIDED BOOKS:
KARCH, A. M. (2013). FOCUS ON
NURSING PHARMACOLOGY.
PHILADELPHIA: LIPPINCOTT
WILLIAMS & WILKINS.
JONES & BARTLETT LEARNING., &
JONES & BARTLETT PUBLISHERS.
(2000). NURSE'S DRUG HANDBOOK.
SUDBURY, MA: JONES AND
BARTLETT PUBLISHERS.

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