Antiretroviral Drugs

Question 1

Reverse Transcriptase Inhibitors

Answer 1

Nucleoside analogs that are activated in host cell by kinases and then inhibit viral transcriptase
All oral, mainly renal

Question 2

Reverse Transcriptase Inhibitors SE

Answer 2

Rare mitochondrial tox

Lactic acidosis & hepatic steatosis

Question 3

Emtricitabine

Answer 3

NRTI
HIV & hepB
Among best tolerated

Question 4

Tenofovir

Answer 4

NucleoTide RTI
HIV & hep B
Potential for renal impairment

Question 5

Nonnucleoside RTIs

Answer 5

Bind to noncatalytic site to inhibit reverse transcriptase
Oral Daily
Always used w/NRTIs because high likelihood for resistance for entire class

Question 6

Abacavir

Answer 6

NRTI

Severe hypersensitivity rxn

Question 7

Efavirenz

Answer 7

NNRTI
Induces P450 and CYP34A (decreases methadone levels)
Least likely to develop resistance
Preg category D

Question 8

NNRTI SE

Answer 8

CYP450 DDIs
Rash, hepatox,
Low barrier to resistance

Question 9

Protease Inhibitors

Answer 9

Inhibits viral protease
Oral
P450 = DDI
Base w/2NRTIs

Question 10

Atazanavir

Answer 10

PI

SE: rash, bilirubinemia/jaundice

Question 11

PI SE

Answer 11

increase LDL = risk of CAD
P450 DDIs
glucose intolerance
fat redistribution

Question 12

Darunavir

Answer 12

PI

SE: severe rash –> SJS

Question 13

Ritonavir

Answer 13

PI
most potent P450 inhibitor
SE: GI & hepatotox

Question 14

Integrase Inhibitors

Answer 14

Inhibits viral enzyme that inserts genome into DNA
Oral
Hepatic glucuronidation
Base w/2 NRTIs

Question 15

II SE

Answer 15

Well tolerated
Increased HR, sweating, liver enzymes
DDI w/ glucuronidaiton inducers (rifampin)

Question 16

Dolutegravir

Answer 16

II

Question 17

Enfuvirtide

Answer 17

Fusion inhibitor = prevents HIV fusion w/ gp41 & cell entry
Twice daily SC
Option in drug resistance

Question 18

Maraviroc

Answer 18

CCR5 Receptor Antagonist
Block CCR5-tropic HIV into CD4
Oral CYP3A4 = ddis
Fecal and renal
Option if resistance but must be R5-tropic HIV-1