HIV Treatment

Question 0

Protease inhibitors

Answer 0

Lopinavir, Atazanavir, Darunavir, Fosamprenavir, Saquinavir, Indinavir, Ritonavir

*-Navir ending (Navir tease a protease)

Question 1

Overall HIV treatment

Answer 1

HAART (highly active antiretroviral therapy)
Regimen of 3 drugs to prevent resistance:
1) 2 NRTIs
2) 1 NNRTI or 2) 1 protease inhibitor or 2) 1 integrase inhibitor

Question 2

Mechanism of protease inhibitors

Answer 2

Prevent maturation of new viruses.

Assembly of the Virions depends on HIV-1 protease (pol gene)
Which cleaves the polypeptide products of HIV mRNA into their functional parts

Question 3

Extra MOA of ritonavir

Answer 3

Boosts other drug concentrations by inhibiting cytochrome p450

Question 4

Protease inhibitor toxicity

Answer 4

Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy, nephropathy.
Hematuria in indinavir

Question 5

NRTIs (nucleoside reverse transcriptase inhibitors)

Answer 5

Tenofovir (TDF), Lamivudine (3TC), Zidovudine (AZT/ZDV), Didanosine (ddl), Stavudine (d4T), Emtricitabine (FTC)

Question 6

Mech of NRTIs

Answer 6

Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH)
Tenofovir is nucleotide analog and does not have to be activated
Others are nucleoside analogs and do need activation (phosphorylation)
ZDV - prophylaxis and pregnancy (dec fetal transmission)

Question 7

Toxicity of NRTIs

Answer 7

BM suppression (can be reversed with G-CSF and EPO)
Peripheral neuropathy
Lactic acidosis (nucleosides)
Rash (tenofovir/ non-nucleosides)
Anemia (ZDV)

Question 8

NNRTIs

Answer 8

Neviparine
Efavirenz
Delavirdine

Question 9

Mech of NNRTI

Answer 9

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

Question 10

Toxicity of NNRTIs

Answer 10

Same as NRTIs:
BM suppression (can be reversed with G-CSF and EPO)
Peripheral neuropathy
Lactic acidosis (nucleosides)
Rash (non-nucleosides)

Question 11

Integrase inhibitors

Answer 11

Raltegravir

Question 12

Mech of integrase inhibitors

Answer 12

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

Question 13

Toxicity of integrase inhibitors

Answer 13

Hypercholesterolemia