Flashcards in FA pharma Deck (161)
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1
MOA of polyenes
Formation of artificial pores in the ergosterol membranes disrupts membrane permeability
2
Uses of amphotericin B
Severe infections by Aspergillus, Candida, Cryptococcus, Histoplasma, Mucor, Sporothrix
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Uses of nystatin
Topical localized infections; too toxic for systemic use
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Pharmacokinetics of amphotericin B
Given by slow IV infusion, does not enter CNS, slow t1/2 > 2 weeks, hepatic metabolism and renal elimination
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Side effects of amphotericin B
Infusion-related: fever chills, muscle rigor, hypotension alleviated by NSAIDs, antihistamines, meperidine, steroids. Dose-dependant: nephrotoxicity, decreased GFR, tubular acidosis, anemia
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Azole drugs
Ketoconazole, fluconazole, itraconazole, clotrimazole
7
MOA of azoles
Fungicidal by inhibiting 14-alpha-demethylase which converts lanosterol to ergosterol
8
Uses of ketoconazole
DOC for Paracoccidioides; backup for Blastomyces, Histoplasma; Oral use in mucocutaneous candidiasis or dermatophytoses
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Uses of fluconazole
DOC for esophageal and invasive candidiasis and coccidioidomycoses. Prophylaxis and suppression of cryptococcal meningitis
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Uses of itraconazole
DOC in blastomycoses and sporotrichoses
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Uses of clotrimazole
Used topically for candidal and dermatophytic infections
12
Pharmacokinetics of ketoconazole
Orally effective; absorption decreased by antacids; metabolized by liver enzymes; inhibits P450
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Pharmacokinetics of itraconazole
Orally effective; absorption increased by food; metabolized by liver enzymes; inhibits P450
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Pharmacokinetics of fluconazole
Orally effective; enters CSF; eliminated in the urine in unchanged form
15
Side effects of azoles
Decreased synthesis of cortisol and testosterone --> decreased libido, gynecomastia, menstrual irregularities; Increased liver function tests and rare hepatotoxicity
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Drugs that block viral penetration and uncoating
Amantadine, enfurvitide
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Drugs that inhibit viral DNA polymerases
Acyclovir, foscarnet, ganciclovir
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Drugs that inhibit viral RNA polymerases
Foscarnet, ribavirin
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Drugs that inhibit viral reverse transcriptase
Zidovudine, didanosine, zalcitabine, lamivudine, stavudine, nevirapine, delavirdine, efavirenz
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Drugs that inhibt viral aspartate protease
Indinavir, ritonavir, saquinavir, nelfinavir
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Drugs that inhibit viral neuraminidase
Zanamivir, oseltamivir
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Drugs used to treat herpes
Acyclovir, ganciclovir, foscarnet
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Acyclovir
Activated by viral thymidine kinase, inhibitor and chain terminator of DNA polymerase. Use for HSV ans VZV. Side effects: crystalluria, neurotoxicity
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Ganciclovir
Activated by viral thymidine kinase, inhibitor and chain terminator of DNA polymerase. Use for HSV, VZV, CMV, AIDS retinitis and transplant patients. Side effects: hematotoxicity, crystalluria, rash
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Foscarnet
Inhibits viral DNA and RNA polymerases. Use for HSV, VZV, CMV, AIDS retinitis, transplant patients. Side effects: nephrotoxic acute tubular necrosis, hypocalcemia (tremors, seizures)
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Zidovudine (ZDV, AZT)
Converted to triphosphate that inhibits reverse transcriptase and causes chain termination. Resistance by mutations of RT gene.
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Drug interaction of zidovudine (ZDV, AZT)
Increase levels of ZDV: azoles, cimetidine, indomethacin, probenecid, TMP-SMX. Decrease levels of ZDV: rifampin
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Side effects of ZDV
Neutropenia, anemia, granulocytopenia, headache, myalgias, neuropathy, lactic acidosis
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MOA enfuvirtide
Binds gp41 and inhibits fusion of HIV-1 to CD4 cells
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