Integrase inhibitors & Fusion inhibitor Flashcards
What are the agent drugs under integrase inhibitors??
- Raltegravir
- Dolutegravir
*rapid decrease in viral load
How are the integrase inhibitors administered?
Orally
*Well absorbed with food
CSF penetration?
Yeah, good levels in CSF
What’s the metabolic pathway of the integrase inhibitors?
- Metabolized by the UGT 1A1 pathway in the liver.
What are the common side effects from using integrase inhibitors?
- Diarrhea
- nausea
- headaches
What drug agent is found under fusion inhibitors?
- Enfuvirtide
What’s the administration route of enfuvirtide?
- Subcutaneous administration
Which antiretroviral therapy agent, is used as salvage therapy?
- Enfuvirtide
What’s the metabolic pathway of fusion inhibitors?
- Proteolytic hydrolysis, (not cytochrome P450)
What are the toxicities or side effects from enfuvirtide?
- Injection site reaction
Raltegravir, an integrase interacts with Rifampicin. What outcome is seen from this?
Reduced Raltegravir plasma levels
Adverse effects: myopathy, rhabdomyolysis
What drugs does dolutegravir, interacts with? And what outcomes are seen with such?
- Antacids & iron supplements ↓ DTG plasma conc. Dose spacing
- Anticonvulsants (carbamazepine, phenobarbital, phenytoin) ↓ DTG
plasma conc. Avoid co-admin if possible - Metformin ↑Metformin plasma conc. Limit metformin dose to max
500 mg 12-hourly
When is the right weight and age to use Dolutegravir as an ART regimen?
- Weight (>/= 3kg)
- Age (>/=4 weeks) but less than 10 years
Why is dolutegravir’s use feared on infants younger than 4 weeks?
- It increases the risk of neural tube tube defect
A drug to avoid at periconception and on first 6 weeks of pregnancy
Dolutegravir
