Non-Nucleoside Reverse Transcriptase Inhibitors

Question 1

Efavirenz
MOA

Answer 1

Binds to hydrophobic pocket for p66 subunit of HIV reductase transcriptase. This allosteric binding causes a conformational change in HIV reductase transcriptase that inhibits DNA transcript elongation

Question 2

Efavirenz
Abs/Distrb/Elim

Answer 2

Given orally; the concentration in the CSF is 45% of the plasma level.

Question 3

Efavirenz
Clinical use

Answer 3

HIV-1 infection in combination with other antiretrovirals. Can reduce mother-to-foetus
transmission of the virus by ~50%.