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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

3

Uses of nystatin

Topical localized infections; too toxic for systemic use

4

Pharmacokinetics of amphotericin B

Given by slow IV infusion, does not enter CNS, slow t1/2 > 2 weeks, hepatic metabolism and renal elimination

5

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

6

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

9

Uses of fluconazole

DOC for esophageal and invasive candidiasis and coccidioidomycoses. Prophylaxis and suppression of cryptococcal meningitis

10

Uses of itraconazole

DOC in blastomycoses and sporotrichoses

11

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

13

Pharmacokinetics of itraconazole

Orally effective; absorption increased by food; metabolized by liver enzymes; inhibits P450

14

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

16

Drugs that block viral penetration and uncoating

Amantadine, enfurvitide

17

Drugs that inhibit viral DNA polymerases

Acyclovir, foscarnet, ganciclovir

18

Drugs that inhibit viral RNA polymerases

Foscarnet, ribavirin

19

Drugs that inhibit viral reverse transcriptase

Zidovudine, didanosine, zalcitabine, lamivudine, stavudine, nevirapine, delavirdine, efavirenz

20

Drugs that inhibt viral aspartate protease

Indinavir, ritonavir, saquinavir, nelfinavir

21

Drugs that inhibit viral neuraminidase

Zanamivir, oseltamivir

22

Drugs used to treat herpes

Acyclovir, ganciclovir, foscarnet

23

Acyclovir

Activated by viral thymidine kinase, inhibitor and chain terminator of DNA polymerase. Use for HSV ans VZV. Side effects: crystalluria, neurotoxicity

24

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

25

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)

26

Zidovudine (ZDV, AZT)

Converted to triphosphate that inhibits reverse transcriptase and causes chain termination. Resistance by mutations of RT gene.

27

Drug interaction of zidovudine (ZDV, AZT)

Increase levels of ZDV: azoles, cimetidine, indomethacin, probenecid, TMP-SMX. Decrease levels of ZDV: rifampin

28

Side effects of ZDV

Neutropenia, anemia, granulocytopenia, headache, myalgias, neuropathy, lactic acidosis

29

MOA enfuvirtide

Binds gp41 and inhibits fusion of HIV-1 to CD4 cells

30

Needle stick HIV prophylaxis

ZDV + 3TC + indinavir