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Antibiotics

Anti-infective agents
Drugs that are designed to act on selectively on foreign organisms or cells

Anti-infective agents
Classifications of anti-infective agents according to the organisms they are designed to kill antibacterial or antibiotics antifungals antiprotozoals antihelmintics antivirals

1. 2. 3. 4. 5.

Anti-infective agents
Classifications of anti-infective agents according to their mechanism of action 1. inhibit of cell wall synthesis 2. inactivate certain microbial enzymes 3. inhibit protein synthesis by destroying ribosomes 4. interfere with DNA synthesis 5. alter cell membrane permeability

Anti-infective agents

Anti-infective spectrum of activity


Refers to its effectiveness against different types of microorganisms Narrow-spectrum anti-infectives are effective against a few or specific species of pathogens Broad-spectrum anti-infectives are effective against a wide array of microorganisms

Anti-infective spectrum of activity


The main goal of anti-infective therapy is to reduce the population of the invading microorganisms to a level at which the immune system can take care of the infection Anti-infective treatment in an immune compromised host is useless

Anti-microbial resistance
Microorganisms may develop resistance in a number of ways including the following 1. producing enzymes that can deactivate the drug 2. changing cellular permeability 3. altering binding sites on ribosomal membranes 4. producing chemicals that can antagonize the drug

Anti-microbial resistance
To prevent emergence of resistant strains of microorganisms 1. drugs should be given at the recommended dose 2. duration of therapy should be long enough to eradicate the population of invaders 3. doses should be spread at even intervals to insure that critical concentrations are maintained. 4. anti-infectives should only be used when indicated

Adverse reactions to antibiotics


Most common adverse reactions to antiinfective therapy 1. kidney damage (oliguria, anuria, edema) 2. gastrointestinal toxicity (nausea and vomiting, diarrhea) 3. neurotoxicity (CN VIII damage vertigo, loss of hearing) 4. hypersensitivity reactions 5. superinfections

Antibiotics
anti-bacterial drugs Two basic types of antibiotics according to their effects on cells 1. bacteriostatic agents prevent bacterial growth 2. bactericidal agents kill bacterial cells

Antibiotics
Two types of bacterial cells according to cell wall composition 1. gram positives skin, respiratory tract 2. gram negatives gastrointestinal (GI) and genitourinary (GU) tract

Antibiotics
Major groups of antibiotics according to their chemical structure and mechanism of action 1. aminoglycoside 2. cephalosporin 3. fluoroquinolone 4. macrolide 5. lincosamide

Antibiotics
Major groups of antibiotics according to their chemical structure and mechanism of action 6. monobactam 7. penicillin 8. penicillinase resistant 9. sulfonamide 10. Tetracycline 11. anti-mycobacterial (anti-TB and antileprotic)

Aminoglycoside antibiotics
Drugs under this class: amikacin, gentamicin, kanamycin, neomycin, streptomycin and tobramycin Mechanism of action (MOA): Bactericidal, inhibit protein synthesis Spectrum: gram negatives (P.aeruginosa, E.coli, Proteus, Klebsiella-EnterobacterSerratia, Citrobacter), gram positive (S.aureus)

Aminoglycoside antibiotics
Pharmacodynamics: poorly absorbed via GIT, parenteral administration is preferred Adverse effects: CNS (ototoxicity) renal, hepatic toxicity Contraindications: known allergy to this drug, patients with documented renal or hepatic disease, with active mycobacterial or herpetic infection, CNS disorders like parkinsonism and myasthenia gravis

Aminoglycoside antibiotics
Drug-drug interaction: toxic effects are increased by CNS drugs, diuretics Synergistic bactericidal effect with cephalosporins, penicillins and penicillinase resistant pens

Cephalosporins
4 generations of drugs under this class 1st gen: cefadroxil, cefazolin, cephalexin largely effective against gram pos and some gram negs 2nd gen: cefaclor, cefoxitin, cefuroxime less effective against gram pos but with extended gram neg coverage

Cephalosporins
4 generations of drugs under this class 3rd gen: cefoperazone, ceftazidime, cefotaxime, ceftriaxone weak against gram pos, potent against gram neg 4th gen: cefepime, cefixime broad spectrum with good gram pos and neg coverage

Cephalosporins
MOA: Bacteriostatic at low dose, Bactericidal, inhibit bacterial cell wall synthesis Pharmacodynamics: well absorbed via GIT

Cephalosporins
Adverse effects: relatively safe with nonspecific side effects, Pseudomembranous colitis (GI mucosal inflammation with hemorrhage) is a rare but severe complication Contraindications: known allergy to this drug Drug-drug interaction: alcohol (disulfiram-like reaction), anticoagulants

Fluoroquinolones
Ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, norfloxacin, ofloxacin, sparfloxacin MOA: inhibit DNA synthesis

Fluoroquinolones
Spectrum: Broad spectrum, for treatment of GUT and atypical RTI Pharmacodynamics: well absorbed in GIT Adverse effects: photosensitivity, suppression of bone marrow activity

Fluoroquinolones
Contraindications: allergy, pregnant and lactating women, infants, children and adolescents Drug-drug interaction: potentiate the effect of cardiac drugs and theophylline, absorbed poorly if given with sucralfate, iron salts, mineral supplements and antacids

Macrolides
Erythromycin, azithromycin, clarithromycin MOA: Bacteriostatic, bactericidal, interferes with protein function Spectrum: broad, treatment of RT, GUT, GIT infections, used for patients who are allergic to penicillin

Macrolides
Contraindications: fungal and viral infections, pregnancy and lactation Adverse effects: non specific and relatively rare Drug-drug interaction: increases serum levels of digoxin, anticoagulants and theophylline, should be given on empty stomach

Lincosamides
Clindamycin, lincomycin MOA: similar with macrolides For treatment of severe skin, GUT, GIT infections More toxic than macrolides Adverse effects: Pseudomembranous colitis, bone marrow depression

Monobactam antibiotics
Aztreonam MOA: interferes with cell wall synthesis Spectrum: mostly for gram pos but is effective against some gram neg infections as well, used among patients who are allergic to penicillins and cephalosporins

Monobactam antibiotics
Contraindications: allergies, pregnancy and lactation Adverse effects: rare, mild and non specific

Penicillin and Penicillinase resistant antibiotics


Penicillinase: enzyme produced by penicillin resistant gram pos bacteria which can inactivate the drug Penicillins G, V Extended spectrum penicillins: Amoxicillin, ampicillin, carbenicillin, ticarcillin Penicillinase resistant antibiotics: dicloxacillin, nafcillin and oxacillin

Penicillin and Penicillinase resistant antibiotics


MOA: interferes with cell wall synthesis Spectrum: for treatment of most gram pos infections

Penicillin and Penicillinase resistant antibiotics


Contraindications: allergy Adverse effects: Hypersensitivity and anaphylaxis, GIT symptoms

Sulfonamides
Cotrimoxazole (trimethoprimsulfamethoxazole), sulfadiazine, sulfasalazine MOA: inhibit folic acid synthesis by blocking PABA Pharmacodynamics: well absorbed in GIT

Sulfonamides
Spectrum: for treatment of susceptible GUT including trachoma and RT infections Contraindications: pregnancy and lactation, TERATOGENIC!

Sulfonamides
Adverse effects: GI disturbance, Renal and hepatotoxicity, Dermatological including Stevens Johnson syndrome (SJS) Drug-drug interaction: increases hypoglycemic effect of antidiabetic drugs

Tetracyclines
Tetracycline, doxycycline, minocycline, oxytetracycline MOA: inhibits protein synthesis Spectrum: broad, treatment of Ricketssiae, Vibrio cholerae

Tetracyclines
Pharmacodynamics: adequately absorbed in GIT Contraindications: children, pregnancy and lactation

Tetracyclines
Adverse effects: direct irritation of GIT, fatal hepatotoxicity, weakening of bones and teeth (Grey baby syndrome) Drug-drug interaction: interferes with absorption of insulin, calcium containing drugs/food products, bone marrow suppression, decreases absorption of oral contraceptives