Antiretroviral drugs

Question 1

Receptors for HIV entry

Answer 1

CD4 and CCR5/CXCR4

Question 2

Prototype nucleoside reverse transcriptase inhibitor (NRTIs)

Answer 2

Emtricitabine

Question 3

NNRTIs prototype

Answer 3

Efavirenz

Question 4

Prototype protease inhibitor

Answer 4

Atazanavir

Question 5

MOA of NRTIs

Answer 5

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

Question 6

Emtricitabine adverse effects

Answer 6

diarrhea, headache, nausea, rash

severe: hepatotoxicity, lactic acidosis

Question 7

Pharmacokinetics of emtricitabine

Answer 7

oral or IV, metabolized by the kidney

Question 8

Drug interactions with emtircitabine

Answer 8

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

Question 9

Side effects of Efavirenz

Answer 9

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

Question 10

Drug interactions with efavirenz

Answer 10

rifampin, dilantin, methadone

Question 11

MOA of NNRTIs

Answer 11

allosteric inhibition

Question 12

Pharmcokinetics of NNRTIs

Answer 12

good oral absorption, metabolized by CYP3A4, long half life

Question 13

Atazanavir MOA

Answer 13

binds reversibly to active site of protease

Question 14

Pharmacokinetics of atazanavir

Answer 14

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

Question 15

Adverse effects of atazanavir

Answer 15

GI, metabolic effects

Question 16

Drug interactions with atazanvir

Answer 16

rifampin, statins, amiodarone, oral contraceptives

Question 17

Integrase inhibitor prototype

Answer 17

dolutegravir