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26 Cards in this Set
- Front
- Back
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Beta-lactamase inhibitors
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clavulanic acid, sulbactam, tazobactam
Added to penicillin antibiotics to protect against destruction by beta-lactamase. |
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Pyrazinamide
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Mechanism- Only effective in acidic pH of phagolysosomes where TB engulfed by macrophages is found.
Toxicity- Hepatotoxicity |
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Ethambutol
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Mechanism- Decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
Toxicity- Optic neuropathy |
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Amphotericin B
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Mechanism- Binds ergosterol and forms membrane pores to allow leakage of electrolytes.
Use- Serious systemic mycoses, Crypto, Blasto, Cocci, Aspergillus, Histo, Candida, Mucor. Intrathecally for funal meningitis (does not cross BBB) Toxicity- Fever/chills, hypotension, nephrotoxicity (dec GFR- hydration reduces this), arrhythmias (dec K and Mg), anemia, IV phlebitis. Liposomal Amphotericin B reduces toxicity. can be used with flucytosine for cryptococcal meningitis |
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Nystatin
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Mechanism- Same as Amphotericin B. Used topically because it is too toxic for systemic use. (No-a-statin)
Use- Swish and swallow for oral candidiasis, topical for diaper rash or vaginal candidiasis |
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Fluconazole, ketoconazole, clotrimazole, micronazole, itraconazole, voriconazole
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Azoles
Mechanism- Inhibit fungal sterol synthesis by inhibiting the P450 enzyme that converts lanosterol to ergosterol. Use- Systemic mycoses: fluconazole for crypo meningitis and candidal infections. Ketoconazole for blasto, cocci, histo, candida albicans, HYPERCORTISOLISM (inhibits desmolase). Clotrimazole and miconazole for topical fungal infections. Itraconazole for Sporothrix. Toxicity- Hormone synthesis inhibition (gynecomastia), liver dysfunction (inhibits P450), fever, chills |
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Flucytosine
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Mechanism- inhibits DNA/RNA synthesis by conversion to 5-FU.
Use- Systemic fungal infections (candida, crypto) + amphotericin B Toxicity- N/V/D, BM suppression |
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Caspofungin
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Mechanism- inhibits cell wall synthesis by inhibiting synthesis of beta-glucan
Use- Invasive asperillosis Toxicity- GI, flushing |
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Terbinafine
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Mechanism- Inhibits squalene epoxidase -> squalene toxic to fungi
Use- Determatophytoses (ESP onchomycosis) |
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Griseofulvin
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Mechanism- Interferes with microtubules function to disrupt mitosis. Deposits in keratin containing tissues (nails).
Use- Oral for superficial infections; dermatophytes (tinea, ringworm) - grisely-o-falvin because of toxicity Toxicity- Teratogenic, carcinogenic, confusion , headaches, increases P450 and warfarin metabolism |
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Rimantadine
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Mechanism- Blocks penetration/uncoating (M2) and causes DA release from intact nerve terminals
Use- Prophylaxis and treatment for influenza A ONLY; PD Toxicity- Ataxia, dizziness, slurred speech, anticholinergic Resistance- Mutated M2 protein (% influenza A are resistant) RIMANTIDINE has fewer side effects, but doesnt cross BBB (cant use for PD) |
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Zanamivir, oseltamivir
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Mechanism- Inhibit influenzae neuraminidase to decrease the progeny
Use- Influenza A and B, H1N1, H5N1 |
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Ribavirin
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Mechanism- Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP DH
Use- RSV, chronic hepatitis C Toxicity- Hemolytic anemia, Severe teratogen (inhaled powder concern for people handling on Step) |
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Acyclovir
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Mechanism- Monophosphorylated by HSV/VZV thymidine kinase and acts as a guanosine analog. Cellular enzymes create triphosphate. Inhibits viral DNA polymerase by chain termination
Use- VZV (use famciclovir), HSV, EBV. No effect on latent forms of VZV and HSV Resistance- lack of viral TK Toxicity: rarely nephrotoxicity |
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Ganciclovir
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Mechanism- 5'-monophosphate formed by a CMV viral kinase or HSV/VZV TK. Guanosine analog. Triphosphate formed by cellular kinase. Inhibits viral DNAP.
Use- CMV (esp in IC patients) Toxicity- Leukopenia, neutropenia, thrombocytopenia, renal toxicity. Resistance- Mutated CMV DNAP or lack of viral kinase Valganciclovir is a prodrug of ganciclovir and has better oral bioavailability |
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Foscarnet
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Mechanism- DOES NOT REQUIRE ACTIVATION BY VIRAL KINASE. Inhibits viral DNAP by binding to pyrophosphate site
Use- CMV retinitis when ganciclovir fails. Resistance- mutated DNAP |
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-navir
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HIV Protease inhibitors
Mechanism- Inhibits protease, which cleaves the polypeptide products of HIV mRNA into their functional parts. So maturation of new viruses is halted Toxicity- Hyperglycemia, GI, lipodystrophy, thrombocytopenia (indinavir), inhibits P450, pancreatitis (Ritonavir), nephrolithiasis (indinavir) |
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Zidovudine (ZDV/AZT), Didanosine, Zalcitabine, Stavudine, Lamivudine, Abacavir
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Mechanism- Competitively inhibit nucleotide binding to RT and terminate the DNA chain (lack 3'OH group). Need to be phosphorylated by TK. ZDV for pregnancy
Toxicity- Hypersensitivity (Abacavir), BM suppression (reversed with G-CSF and EPO), peripheral neuropathy (Didanosine, stavudine, zalcitabine), lactic acidosis, megaloblastic anemia (ZDV), GI, hepatic steatosis (didanosine, stavudine) |
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Nevirapine, Efavirenz, Declaviridine
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Mechanism- Bind to RT at a site different from NRTIs. DO NOT REQUIRE P-ATION
Toxicity- BM suppression (reversed with G-CSF and EPO), peripheral neuropathy, rash, GI, false positive for cannabinoids and confusion (efavirenz) |
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Enfuvirtide
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Mechanism- Bind gp41 to inhibition conformational change required for fusion with CD4 cells, blocking entry and replication. Used in patients with persistent viral replication despite antiretroviral therapy.
Toxicity- Hypersensitivity, reactions at subcutaneous injection site, increased risk of bacterial pneumonia |
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Raltegravir
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Integrase inhibitor preventing HIV genome integration
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Cidofovir
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Mech: inhibits viral DNA polymerase- does not require phosphorylation
uses: CMV retinitis toxicity: nephrotoxicity |
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Antibiotics to avoid in pregnancy
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Countless SAFE Momes Take Really Good Care
Clarithromycin -embryotoxic Sulfonamides - kernicterus Aminoglycosides- ototoxicity Fluoroquinolones- caritlage damage Metronidazoles - mutagenic Tetracyclines - discolored teeth, inhibition of bone growth Ribavirin - teratogenic Griseofulvin - teratogenic Chloramphenicol - "gray baby" |
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Interferons
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Glycoproteins to block replication of RNA and DNA
IFN-alpha chronic HepB/C, Kaposi's sarcoma IFN-beta - MS IGN-gamma - NADPH deficiency (chronic granulomatous disease) toxicity is neutropenia |
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Chloroquine
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Blocks plasmodium heme polymerase
toxicity - retinopathy, G6PD hemolysis |
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Antihelminth therapy
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Bendazoles - increase glucose uptake
Pyrantel pamoate - nicotinic receptor agonist paralyzes worm Ivermectin - increases GABA transmission paralyzes wrom Praziquantel - increase Ca influx |
