Anti Virals and Tx of AIDS

Question 1

what does the typical HAART therapy consist of?

Answer 1

2 NRTI (nucleoside reverse transcriptase inhibitors) + 1 NNRTI or 1-2 PIs (protease inhibitors)

Question 2

what is the main reason a 1-2 drug regimen is avoided in treatment of HIV?

Answer 2

HIV easily overcomes therapy through resistance mutations

Question 3

how do NRTI work as an antiviral?

Answer 3

they function as nucleoside analogues that block translation of HIV RNA to DNA by inhibiting the HIV reverse transcriptase enzyme

Question 4

what distinguishes Tenofovir from other reverse transcriptase inhibitors?

Answer 4

it is a nucleoTIDE (has been phosphorylated); note: this drug is also active against hep B

Question 5

to which class of anti-retrovirals do the following drugs belong? efavirenz, nevirapine, and delavirdine.

Answer 5

NNRTI

Question 6

how do protease inhibitors function as anti-retrovirals?

Answer 6

they block release of assembled HIV virus particles from infected cells

Question 7

how are PIs metabolized in the body?

Answer 7

by cytochrome P450

Question 8

what drug can be used to slow the metabolism of PIs and thereby boost their serum levels? What is the MOA?

Answer 8

Ritonavir - it inhibits P450

Question 9

what is a common side effect of NNRTI?

Answer 9

rash

Question 10

pigmentation of the nails is a common side effect of which anti retroviral drug?

Answer 10

AZT