NNRTIs Flashcards
What are NNRTIs
Highly selective, non-competitive inhibitors of HIV-I RT
Do NNRTIs require phosphorylation
No
NNRTI cross resistance
Between NNRTIs, NOT NRTIs
Main NNRTI AE
Skin Rash - Steven Johnson
Which NNRTI are 3A4 inducers
Nevirapine
Etravirine
Efavirenz
Which NNRTI is a 3A4 inhibitor
Delavirdine
Which NNRTI is a 2C9, 2C19 inhibitor
Etravirine
What metabolizes Nevirapine
3A4
2D6
What are the NNRTIs
Nevirapine
Etravirine
Efavirenz
Delavirdine
Main Nevirapine AE
Hepatotoxicity
When do you not give Nevirapine
Women CD4 > 250
Men CD4 > 400
How does Nevirapine/Delavirdine resistance arise
Mutation at target site
What does non-linear kinetics mean
t1/2 increases with dose
Which NNRTI has non-linear kinetics
Delavirdine
Where is Delavirdine excreted
Kidneys
Delavirdine contraindication
Pregnancy
Delaviradine AE
HA, fever, depression
Who do you give Etravirine to
Treatment-experienced patients
Strains resistant to 1st line NNRTIs
What metabolizes Etravirine
3A4
2C9
2C19
Etravirine AE
N/D Elevated transaminases (esp in hep)
What is the Preferred NNRTI
Efavirenz
What is the most common Efavirenz AE
CNS effects
Vivid Dreams
What happens with Efavirenz in pregnancy
Neural tube defects
When can you give Efavirenz in pregnancy
After 1st trimester
P450 effect of Efavirenz
Induction