NNRTIs

Question 1

What are the 3 NNRTIs agents?

Answer 1

• Efavirenz
• Nevirapine/Viramune
• Rilpivirine

Question 2

What’s the mode of administration of the NNRTIs?

Answer 2

• Oral administration

*Wellabsorbed with oily foods
*Nevirapine absorption is not impacted by food intake; rilpivirine absorption is increased with food intake

Question 3

What is the metabolic pathway of the NNRTIs?

Answer 3

Cytochrome P450 metabolic pathway

Question 4

What are side effects of using efavirenz?

Answer 4

Neuropsychiatric conditions incl:
- vivid dreams,
- disturbed sleep,
- nightmares,
- hepatitis,
- rash
- gynaecomastia

Question 5

What are the side effects of using Nevirapine?

Answer 5

• Hepatitis,
• Rash (incl Stevens-Johnson Syndrome)

Question 6

What are the side effects of using Rilpivirine?

Answer 6

rash

Question 7

What the mechanism of action of NNRTIs?

Answer 7

• Bind directly and non-competitively to the reverse transcriptase enzyme at a position near to, but distinct from that of the nucleoside there by “slowing the formation of ddDNA”

Question 8

Which is a NNTRI good with CSF penetration?

Answer 8

Nevirapine

Question 9

What drugs does Efavirenz interact with?
What results from these interactions?

Answer 9

• Midazolam: Increases midazolam levels
• Anticonvulsants (phenytoin, phenobarbital, carbamezepine): decreased levels for both efavirenz and anticonvulsants
• Oral contraceptives: reduced efficacy

Question 10

What drugs does nevirapine interact with?
What results from these interactions?

Answer 10

• Oral contraceptives -
  reduced efficacy.
• Rifampicin – decrease NVP
  levels

Question 11

A drug with a lowest volume of distribution due to having 99% protein binding

*It a good drug to use during pregnancy

Answer 11

Efavirenz

Question 12

When is efavirenz and nevirapine contraindicated?

Answer 12

Liver malfunctioning or damage or disease