Antiretrovirals

Question 1

ENTRY/ FUSION INHIBITORS

Answer 1

Maraviroc and enfuvirtide

Question 2

Binds specifically and selectively to CCR5.

Prevents viral fusion and entry

Answer 2

Maraviroc

Metabolized by CYP 3A4
dose must be reduced when given with PIs
• Given orally
AE: Well tolerated (risk for hepatotoxicity)

Question 3

Structurally similar to gp41. Prevents viral fusion and entry

Answer 3

Enfuvirtide
- approved for treatment-experienced adults
NO activity against HIV-2
• Given parenterally
AE: Injection-related

Question 4

These drugs end in INE except for Tenofovir and Abacavir

Answer 4

NUCLEOSIDE/TIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)

STAVUDINE
TENOFOVIR
ZIDOVUDINE
EMTRICITABINE
LAMIVUDINE
DIDANOSINE
ABACAVIR

Question 5

Competitive inhibitors of reverse transcriptase
Need to be phosphorylated to be activated
Lacks 3’OH —> termination of DNA elongation
Used for both HIV 1 and 2

Answer 5

NRTIs

Question 6

AE: peripheral neuropathy, myopathy, lipoatrophy & lactic acidosis
inhibition of mitochondrial DNA polymerase
•Pancreatitis, myelosuppression & cardiomyopathy

Answer 6

NRTI

Question 7

particularly associated with dyslipidemia & insulin resistance

Answer 7

Zidovudine & Stavudine

Question 8

Thymidine analog
• Strong inhibitor of b and g DNA polymerases
• AE: Peripheral neuropathy & pancreatitis
Cannot be given with Didanosine

Answer 8

Stavudine

Question 9

Adenosine analog
Causes GI upset in lactose intolerant patients
Increases Didanosine concentration (dosage reduction is usually required)
Decreases Atazanavir concentration (should be boosted with Ritonavir)

Answer 9

Tenofovir

Question 10

Thymidine analog
Recommended for pregnancy, labor,
postpartum and post-exposure prophylaxis of infants
AE: neutropenia, macrocytic anemia and lipoatrophy

Answer 10

ZIDOVUDINE