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Antibiotics
First AID Antibiotics MOAs and Toxicity only
| Question | Answer |
|---|---|
| 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
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