Antiretroviral drugs Flashcards Preview

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Flashcards in Antiretroviral drugs Deck (17):
1

Receptors for HIV entry

CD4 and CCR5/CXCR4

2

Prototype nucleoside reverse transcriptase inhibitor (NRTIs)

Emtricitabine

3

NNRTIs prototype

Efavirenz

4

Prototype protease inhibitor

Atazanavir

5

MOA of NRTIs

activated by host enzymes, substrates of RTase and inhibit viral RTase, chain terminators

6

Emtricitabine adverse effects

diarrhea, headache, nausea, rash
severe: hepatotoxicity, lactic acidosis

7

Pharmacokinetics of emtricitabine

oral or IV, metabolized by the kidney

8

Drug interactions with emtircitabine

bone marrow toxic drugs, rifampin, fluconazole and TMP-SMX

9

Side effects of Efavirenz

CNS: vivid dreams, poor concentration
hepatitis, rash
false positive cannabis test
teratogenic

10

Drug interactions with efavirenz

rifampin, dilantin, methadone

11

MOA of NNRTIs

allosteric inhibition

12

Pharmcokinetics of NNRTIs

good oral absorption, metabolized by CYP3A4, long half life

13

Atazanavir MOA

binds reversibly to active site of protease

14

Pharmacokinetics of atazanavir

poor oral bioavailbility, metabolized by CYPs, Ritonavir taken to boost plasma levels

15

Adverse effects of atazanavir

GI, metabolic effects

16

Drug interactions with atazanvir

rifampin, statins, amiodarone, oral contraceptives

17

Integrase inhibitor prototype

dolutegravir