Pharm_Antibiotics Flashcards
Aminoglycosides: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Mechanism: Bactericidal; inhibit formation of initiation complex and cause misreading of mRNA. Requite O2 for uptakel therefore ineffective against anaerobes. Clinical use: Severe gram-negative rod infections. Synergistic with β-lactam antibiotics. Neomycin for bowel surgery. Toxicity: Nephrotoxicity (+ cephalosporins), Ototoxicity (+ loop diuretics). Teratogen.
Ampicillin, amoxicillin (aminopenicillins)
Mechanism: Same as penicillin. Wider spectrum; penicillinase sensitive. Also combine with clavulanic acid to enhance spectrum. Amoxicillin has greater oral bioavailability than ampicillin. Clinical use: Extended-spectrum penicillin - certain gram-positive bacteria (Listeria monocytogenes, Enterococci) and gram-negative rods (Haemophilus influenza, E.coli, Proteus mirabilis, Salmonella) Toxicity: Hypersensitivity reactions; ampicillin rash; pseudomembranous colitis
Anti-TB drugs (5)
1st line - Streptomycin, Pyrazinamide, Isoniazid (INH), Rifampin, Ethambutol 2nd line - Cycloserine Important side effect of ethambutol is optic neuropathy (red-green color blindness). For other drugs, hepatotoxicity.
Antimycobacterial drugs
M.tuberculosis Prophylaxis: Isoniazid; Treatment: Rifampin, Isoniazid, Pyrazinamide, Ethambutol M.avium-intracellulare Prophylaxis: Azithromycin; Treatment: Azithromycin, rifampin, ethambutol, streptomycin M.leprae Prophylaxis: N/A; Treatment: Dapsone, rifampin, clofazimine
Aztreonam
Mechanism: A monobactam resistant to β-lactamases. Inhibits cell wall synthesis (binds to PBP3). Synergistic with aminoglycosides. No cross-allergenicity with penicillins. Clinical use: Gram-negative rods only - No activity against gram-positive anaerobes. For penicillin-allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides. Toxicity: Usually nontoxic; occasional GI upset. No cross-sensitivity with penicillin or cephalosporins
Bactericidal antibiotics (6)
Vancomycin, Fluoroquinolones, Penicillin, Aminoglycosides, Cephalosporins, Metronidazole
Bacteriostatic antibiotics (6)
Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol
Cephalosporins: 1st generation (cefazolin, cephalexin)
Mechanism: β-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. Clinical use: gram-positive cocci, Proteus mirabilis, E.coli, Klebsiella pneumoniae Toxicity: Hypersensitivity reactions, vitamin K deficiency. Cross-hypersensitivity with penicillins occurs in 5-10% of patients. ↑nephrotoxicity of aminoglycosides; disulfiram-like reaction with ethanol (in cephalosporins with a methylthiotetrazole group, e.g., cefamandole)
Cephalosporins: 2nd generation (cefoxitin, cefaclor, cefuroxime)
Mechanism: β-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. Clinical use: gram-positive cocci, Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E.coli, Klebsiella pneumoniae, Serratia marcescens Toxicity: Hypersensitivity reactions, vitamin K deficiency. Cross-hypersensitivity with penicillins occurs in 5-10% of patients. ↑nephrotoxicity of aminoglycosides; disulfiram-like reaction with ethanol (in cephalosporins with a methylthiotetrazole group, e.g., cefamandole)
Cephalosporins: 3rd generation (ceftriaxone, cefotaxime, ceftazidime)
Mechanism: β-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. Clinical use: serious gram-negative infections resistant to other β-lactams Toxicity: Hypersensitivity reactions, vitamin K deficiency. Cross-hypersensitivity with penicillins occurs in 5-10% of patients. ↑nephrotoxicity of aminoglycosides; disulfiram-like reaction with ethanol (in cephalosporins with a methylthiotetrazole group, e.g., cefamandole)
Cephalosporins: 4th generation (cefepime)
Mechanism: β-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. Clinical use: ↑ activity against Pseudomonas and gram-positive organisms Toxicity: Hypersensitivity reactions, vitamin K deficiency. Cross-hypersensitivity with penicillins occurs in 5-10% of patients. ↑nephrotoxicity of aminoglycosides; disulfiram-like reaction with ethanol (in cephalosporins with a methylthiotetrazole group, e.g., cefamandole)
Chloramphenicol
Mechanism: Inhibits 50S peptidyltransferase activity. Bacteriostatic. Clinical use: Meningitis (Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae). Conservative use owing to toxicities but often still used in developing countries due to low cost. Toxicity: Anemia (dose dependent), aplastic anemia (dose dependent), gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase)
Clavulanic acid
β-lactamase inhibitors
Clindamycin
Mechanism: Blocks peptide bond formation at 50S ribosomal subunit. Bacteriostatic. Clinical use: Anaerobic infections (e.g., Bacterioides fragilis, Clostridium perfrigens) in aspiration pneumonia or lung abscesses. Toxicity: Pseudomembranous colitis (C. difficile overgrowth), fever, diarrhea PS: Treats anaerobes above the diaphragm vs. metronidazole (anaerobic infections below the diaphragm)
Contraindication: Tetracyclines
in pregnancy
Contraindications: Fluoroquinolones
in pregnant women and in children because animal studies show damage to cartilage
Demeclocycline
ADH antagonist; acts as a diuretic in SIADH
DOC: Candida albicans
Nystatin for superficial infection; amphotericin B for serious systemic infection
DOC: Chlamydiae
azithromycin or doxycycline
DOC: Gardnerella vaginalis
metronidazole
DOC: Haemophilus influenzae
Treat meningitis with ceftriaxone. Rifampin prophylaxis in close contacts.
DOC: Helicobacter pylori (3)
Triple therapy: (1) metronidazole, bismuth, tetracycline / amoxicillin; (2) metronidazole, omeprazole, clarithromycin (3) PPI, clarithromycin, amoxicillin / metronidazole
DOC: Legionella pneumophila
erythromycin
DOC: Leprosy (Hansen’s disease)
Long-term oral dapsone; toxicity is hemolysis and methomoglobinemia. Alternate treatments include rifampin and combination of clofazimine and dapsone.
DOC: Lyme disease - Borrelia burgdorferi
doxycycline, ceftriaxone
DOC: Mycoplasma pneumoniae
tetracycline or erythromycin
DOC: Neonatal Chlamydia trachomatis
azithromycin
DOC: Pneumocystis jiroveci (formerly carinii)
TMP-SMX, pentamidine, dapsone
DOC: Pseudomembranous colitis - Clostridia difficile
Metronidazole
DOC: Pseudomonas aeruginosa
Aminoglycoside + extended-spectrum penicillin (e.g., piperacillin, ticarcillin)
DOC: Rickettsiae
Doxycycline
DOC: Sporothrix schenckii
Itraconazole or potassium iodide
DOC: Syphilis
penicillin G
DOC: Systemic mycoses (Histoplasmosis, Blastomycosis, Coccidioidomycosis, Paracoccidioidomycosis)
fluconazole or ketoconazole for local infection; amphotericin B for systemic infection