HIV Therapy

Question 1

What are the protease inhibitors?

Answer 1

Lopinavir
Atazanavir
Darunavir

“navir”

Question 2

What is the mechanism of the protease inhibitors?

Answer 2

Assembly of visions depends on HIV-1 protease, which cleaves the polypeptide products of HIV mRNA into their functional parts. Thus, protease inhibitors prevent maturation of new viruses. Ritonavir can “boost” other drug concentrations by inhibiting cup 450.

All protease inhibitors end in -navir.

“Navir tease a protease.”

Question 3

What are the NRTIs?

Answer 3

Tenofovir
Emtricitabine
Abacavir
Lamivudine
Zidovudine (AZT)
Didanosine
Stavudine

Question 4

What is the mechanism of the NRTIs?

Answer 4

Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack a ‘OH group). Tenofovir is a nucleotide analog and does not have to be activated ; the others are nucleoside analogs and do need to be phosphorylated to be active. ZDV is used for general prophylaxis and during pregnancy and reduce risk of fetal transmission.

Question 5

What are the NNRTIs?

Answer 5

Nevirapine
Efavirenz
Delavirdine

Question 6

What is the mechanism of the NNRTIs?

Answer 6

Bind to reverse transcriptase at site different from NRTIs. Do not require phosphorylation to be active or compete with nucleotides.

Question 7

What is the mechanism of Raltegravir?

Answer 7

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase.