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Antibiotics

First AID Antibiotics MOAs and Toxicity only

QuestionAnswer
Penicillin MOA: Bind transpeptidases (PBPs), block crosslinking of cell wall, activate autolytic enzymes. Toxicity: hypersensitivity rxns, hemolytic anemia
Methicillin, nafcillin, dicloxacillin MOA: same as penicillin, (penicillinase resisitant) Toxicity: Hypersensitivity rxns, Methicillin-interstitial nephritis
Ampicillin, amoxicillin (aminopenicillins) MOA: same as penicillin but combined with penicillinase-inhibitor (clavulanic acid) Toxicity: hypersensitivity rxn, ampcillin rash, pseudomembranous colitis
Ticarcillin, carbenicillin piperacillin MOA: same as penicillin --> Anti-pseudomonal (should use with clavulanic acid) Toxicity: hypersensitivity rxn
Cephalosporins MOA: same as penicillin but less susceptible to penicillinases. Increasing generations have increasing activity against gram neg and decreased against gram positive Toxicity: cross-hypersensitivity with pen, nephro (w/ aminos), disulfram like effects
Aztreonam MOA: binds to PBP3 (no effect on gram + or anaerobes) Toxicity: Usually non-toxic, maybe GI upset
Imipenem/cilastin, meropenem MOA: beta-lactamase reistant carbapenem (cilastin decreases renal metabolism of imipenem) Toxicity: GI, skin, SEIZURES (reduced with Meropenem)
Vancomycin MOA: binds D-Ala, D-Ala to inibit cell wall synthesis Toxicity: Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing ("red man syndrome")
Aminoglycosides (gentamicin, neomycin, amikacin, tobramycin, streptomycin) MOA: Bind 30S to inhibit initiation complex (require O2) Toxicity: Nephrotoxicity (w/ cephalosporins), Ototoxicity (w/loop diuretics), Teratogenicity
Tetracylcines (tetracyline, doxycycline, demococlycine, minocycline) MOA: bind 30S and prevent attachment of aminoacyl-tRNA. Toxicity: Dont take with milk or iron as this decreases intestinal abs, GI distress, photosensitivity, bone probs in children
Macrolides (erythromycin, azithromycin, clarithromycin) MOA: bind 23S rRNA of 50S subunit, blocking translocation Toxicity: GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes, increased serum conc of theophyllines, ora anticoags, prolonged QT
Chloramphenicol MOA: Inhibit 50S peptidyltransferase activity Toxicity: Anemia (dose dependant), Aplastic anemia (dose independent), gray baby syndrome
Clindamycin MOA: blocks peptide bond formation at 50S Toxicity: Pseudomembranous colitis, fever, diarrhea
Sulfonamides (SMX, sulfisoxazole, triple sulfas, sulfadiazine) MOA: PABA antimetabolites that inhibit dihyropterate synthease) Toxicity: Hypersensitivity rxns, hemolysis in G6PD-D, nephrotoxicity, photosens, kernicterus in kids, displace other drugs from albumin
Trimethoprim MOA: Inibits bacterial dihydrofolate reductase Toxicity: Megalobastic anemia, leukopenia, granulocytopenia (may alleviate with folinic acid)
Fluoroquinolones (Cipro-, nor-, spar-, mos-, gati- floxacin) MOA: Inhibits DNA gyrase (topoisomerase II) Toxicity: GI, superinfections, skin rashes, dizziness, contraindicated in preg, tendonitis and tendon rupture in adults, leg cramps in kids
Metronidazole MOA: forms toxic metabolites in the bacteria cell that damage DNA Toxicity: Disulfiram-like reaction, headache, metallic taste, contraindicated in pregnancy
Polymyxins MOA: bind to cell membranes of bacteria and disrupt their osmotic properties Toxicity: Neurotoxicity, renal tubular necrosis
Anti-TB drugs (general toxicities) Ethambutol - optic neropathy (red-green color blindness) Others - hepatotoxicity
Isoniazid (INH) MOA: decrease synthesis of mycolic acids Toxicity: Hemolysis if G6PD deficient, neurotoxicity (preventable with B6), hepatotoxicity, SLE-like syndrome (reversible)
Rifampin MOA: inhibits DNA-dependent RNA polymerase Toxicity: minor hepatotoxicity and drug interactions (p450 inducer), orange bodily fluids (non-toxic)
Amphotericin B MOA: binds ergosterol, forms membrane pores that allow leakage of electrolytes Toxicity: Fever/chills, hypotension, nephrotoxicity (DEC w/ hydration), arrhythmias (altered renal tubule permeability-K/Mg2), anemia, IV phlebitis, azotemia (dose dependant)
Nystatin MOA: Binds ergosterol, disrupts fungal membranes Toxicity: Too toxic for systemic use (topical only)
Azoles (fluconazole, ketoconazole, clotrimazole, miconazole, itraconalze, voriconazole) MOA: Inhibit ergosterol synthesis Toxicity: hormone synthesis inhibition (gynecomastia), liver dysfunction (inhibits p-450), fever, chills
Flucytosine MOA: inhibits DNA synthesis by conversion to fluorouracil (competes with uracil) Toxicity: Nausea, vomiting, diarrhea, bone marrow suppression, cannot be used alone because of rapid resistance
Caspofungin MOA: Inhibits cell wall synthesis Toxicity: GI upset, flushing
Terbinafine MOA: Inhibits fungal enzyme squalene epoxidase (step in ergosterol synthesis) Toxicity: Rash, reversible agranulocytosis
Griseofulvin MOA: Interferes with microtubule function, disrupts mitosis Toxicity: Teratogenic, carcinogeneic, confusion, headaches, induced p450
Amantadine MOA: blocks viral penetration/uncoating (M2 protein), may buffer pH of endosome, also causes release of DA (Parkinson treatment) Toxicity: Ataxia, dizziness, slurred speech Note: 90% of all flu strains resistant (mutated M2)
Zanamivir, oseltamivir MOA: inhibit influenza neuraminidase
Ribavirin MOA: inhibits synthesis of guanine nucleotides by inibiting IMP dehydrogenase Toxicity: Hemolytic anemia, severe teratogen
Acyclovir MOA: Inhibits viral DNA polymerase (must be phosphorylated in cell by HSV/VZV thymidine kinase) Toxicity: Generally well tolerated
Ganciclovir MOA: Inhibits viral DNA polyermase (must be phosphorylated by CMV or HSV/VZV thymidine kinase) Toxicity: Leukopenia, neutropenia, thrombocytopenia, renal toxicity
Foscarnet MOA: inhibits viral DNA polyermase (does NOT require activation by viral kinase), it is a pyrophosphate analog Toxicity: Nephrotoxicity
Protease Inhibitors (-navir) MOA: inhibit assembly of new virus by blocking protease in progeny Toxicity: GI intolerance, hyperglycemia, lipodystrophy, thrombocytopenia (indinavir)
Nucleoside RTI (zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir) MOA: Preferentiall inhibit reverse transcriptase of HIV Toxicity: Bone marrow suppression, peripheral neuropathy, lactic acidosis, megaloblastic anemia (ZDV)
Non-nucleoside RTI (nevirapine, efavirenz, delavirdine) MOA: preferentially inhibit reverese transcriptase in HIV Toxicity: Bone marrow suppression, peripheral neuropathy, rash
Fusion Inhibitors (Enfuvirtide) MOA: bind viral gp41 subunit, inhibit conformation change required for fusion with CD4 cells Toxicity: Hypersensitivity reactions, increase risk of bacterial pneuomonia
IFN MOA: Glycoprotines from human luekocytes that block various stages of viral RNA and DNA synthesis alpha - Hep B/C, Kaposis. Beta - MS. Gamma - NADPH oxidase def. Toxicity: Neutropenia
Created by: thearson