Anti HIV

Question 0

Non-nucleoside reverse transcriptase inhibitor (NNRTI)

Answer 0

NNRTIs bind to a site in the reverse transcriptase that results in its non competitive inhibition

Question 1

Nucleoside reverse transcriptase inhibitor (NRTI)

Answer 1

The NRTIs work as competitive inhibitors. They lack a 3’-OH group on the deoxyribose moiety & thus further coupling of the next nucleoside can’t occur in the nascent DNA chain. Thus chain termination occurs.

Question 2

Zidovudine/Azidothymidine (AZT)

Answer 2

A NRTI
For prevention of suspected HIV infection usually needle stick, mom to child transmission
Don’t use as monotherapy
Adverse Effects: headache, nausea, body fat changes, nail discoloration, bm depression & anemia, inhibits liver glucuronidation
Contraindicated w use of aspirin, indomethacin, trimethoprim

Question 3

Emtricitabine, Lamivudine

Answer 3

Sulfur containing NRTIs, cytidine analogs
For HIV
Lamivudine also used for HBV
Adverse Effects: Em - minor GI (nausea), rare hepatotoxicity, rare lactic acidosis

Question 4

Tenofovir

Answer 4

A nucleotide reverse transcriptase inhibitor (NtRTI)
For HIV & HBV
Adverse Effects: GI (nausea, vomiting), rare hepatotoxicity, renal failure

Question 5

Efavirenz, Nevirapine

Answer 5

NNRTIs
Bind to a “pocket” on reverse transcriptase, induces or inhibits CYP3A4
For HIV positive adults Efavirenz is preferred drug w Nevirapine as alternative drug. If pregnant use only Nevirapine
Adverse Effects: Efavirenz - rash, nausea, headache, psychiatric symptoms (memory, confusion, insomnia, psychosis if liver & kidney impairment), teratogenic thus contraindicated in women of child bearing age
Nevirapine - rash may lead to SJS or TEN, Black Box warning liver toxicity

Question 6

Etravirine

Answer 6

NNRTI

Adverse Effects: pregnancy category B

Question 7

Maraviroc

Answer 7

Fusion/Entry Inhibitor

Binds to CCR5 preventing an interaction w gp120

Question 8

Enfuviritide

Answer 8

Fusion/Entry Inhibitor
A peptide that binds to gp41 thus prevents fusion of HIV & T cell membranes
Adverse Effects: injection site prob, peripheral neuropathy, bacterial pneumonia, hypersensitivity rxn, anaphylaxis

Question 9

Raltegravir

Answer 9

Integrase inhibitor

Question 10

Atazanavir, Darunavir, Fosamprenavir, Ritonavir, Lopinavir

Answer 10

Protease inhibitors
Adverse Effects: hyperglycemia, hyperlipidemia, kidney stones, lipodystrophy, liver toxicity
Use Lopinavir in combo w another protease inhibitor such as Ritonavir so to enhance bioavailability

Question 11

Highly Active Anti-Retrovirus Therapy (HAART)

Answer 11

Reduce viral load

1) Lamiduvine & AZT = Combivir
2) Tenofovir, Emtricitabine & Efavirenz = Atripla
3) Abacavir, Lamuvidine & AZT (all NRTIs)
4) Ritonavir boosted Atazanavir, Tenofovir & Emtricitabine
5) Ritonavir boosted Darunavir, Tenofovir & Emtricitabine
6) Raltegravir, Tenofovir & Emtricitabine