Antiretroviral Drugs- Non-Nucleoside Reverse Transcriptase Inhibitors NNRTI's)

Question 1

What drugs are NNRTI’s?

Answer 1

1) Nevirapine
2) Delaviridine
3) Efavirenz
4) Etravirine

Question 2

NNRTI’s MOA:

Answer 2

NON-COMPETITIVE INHIBITORS that bind the viral reverse transcriptase at a site other than the active catalytic site to inhibit enzyme activity

Question 3

NNRTI’s do not require what to be active?

Answer 3

phosphorylation

Question 4

NNRTI’s do not compete with…

Answer 4

nucleoside analogs bc they are non comp inhibitors- so there is NO CROSS RESISTANCE WITH NRTIs

Question 5

NNRTI’s do not have cross resistance with what classes of drugs?

Answer 5

NRTI’s and Protease Inhibitors

Question 6

Nevirapine is metabolized by what enzyme and to what?

Answer 6

CYP3A to hydroxy-lated metabolite and elim in urine

Question 7

What drugs should not be co-admin’d with Nevirapine?

Answer 7

Ketoconazole
Drugs that modulate CYP3A: 
Cimetidine 
Macrolides
Rifabutin
Rifampin

Question 8

Delarvirdine is what % plasma bound?

Answer 8

98%

Question 9

Delarviridine should be avoided in what population?

Answer 9

Pregnancy

Question 10

How is delarviridine metabolized?

Answer 10

by CYP3A and CYP2D6, but also INHIBITS CYP3A- so may cause DDIs with drugs metab’d by the above

Question 11

Delarviridine may cause DDIs with drugs that are…

Answer 11

highly plasma protein bound

Question 12

Efavirenz is metabolized by…

Answer 12

CYP3A and CYP2B6

Question 13

Efavirenz is what % plasma bound?

Answer 13

99%

Question 14

*Efavirenz side effects are:

Answer 14

1) dizziness
2) drowsiness
3) insomnia
4) crystal urea
5) confusion
6) amnesia
7) agitation
8) delusion
9) depression
10) nightmares
11) euphoria
12) skin rash
13) n/v/d HA
14) elevated liver enzymes
15) increased serum cholesterol

Question 15

Efavirenz is CI’d in what population?

Answer 15

pregnancy

Question 16

Efavirenz has DDI’s with what drugs?

Answer 16

thos that are modulated by CYP3A4 function