Antiretrovirals

  1. What class of drugs do not undergo CYP metabolism?
    NRTIs
  2. What NRTI has the best placental penetration?
    ZDV
  3. How are NRTIs cleared?
    Renally except abacavir and ZDV
  4. What NNRTI has to be taken on an empty stomach due to increased absorption with high fat meals?
    Efavirenz
  5. What NNRTI needs to be taken with a meal with greater than 500 calories for adequate absorption?
    Rilpivirine
  6. What is the 1/2 life of NNRTIs?
    30-50 hrs
  7. Are NNRTIs cleared renally?
    no
  8. Are protease inhibitors substrates for P-gp or CYP 3A4?
    Both
  9. What drugs have high 1st past metabolism and low bioavailability?
    PIs
  10. Which protease inhibitor is a P-gp inhibitor?
    Ritonavir
  11. What is special about atazanavir?
    Needs acid to be absorbed
  12. How is enfuvirtide given?
    SC
  13. Maraviroc
    Substrate of P-gp and CYP 450
  14. What drug/drug class is metabolized via glucuronidation?
    Integrase inhibitors (raltegravir)
  15. What is the interation between Tenofovir(TDF) and atazanavir?
    • Decreated [ATV]
    • Always boost with ritonavir
  16. EFV/NVP + Rifampin
    • Decreased [EFV/NVP]
    • Increase EFV dose
  17. EFV/NVP + statins
    • Decreased concentration of statins
    • Monitor cholesterol, may need to be more agressive
  18. What drug is contraindicated with rilpivirine?
    Proton Pump inhibitors
  19. List the drugs that are contraindicated with protease inhibitors
    • Rifampin
    • Midazolam/triazolam
    • Ergot derivatives
    • Cisapride
    • St. John's wort
    • Lovastatin/simvastatin
    • Pimozide
  20. ATV + PPI
    • Decreased ATV
    • MAX dose of omeprazole 20 mg
    • boost with ritonavir if naieve
  21. PIs+ amiodarone, lidocaine, quinidine, bepridil
    • Increased concentration of antiarrhthmics
    • Avoid if possible
  22. PIs + trazodone
    • Increased [trazodone]
    • start with lowest dose or cut current dose initially
  23. PIs + immunosuppressants
    • increased immunnosuppressants
    • TDM
  24. PIs + statins
    • Increased statin
    • Use pravastatin or atorvastatin
  25. Maraviroc (MVC) + inducers
    • decrease MVC
    • double dose of MVC
  26. MVC + inhibitors
    • Increase MVC
    • Give 1/2 of usual MVC dose
  27. Raltegravir + rifampin
    • Decrease raltegravir
    • Double usual dose
  28. Raltegravir + phenytoin/phenobarb
    Use caution
Author
rclee06
ID
144713
Card Set
Antiretrovirals
Description
PK
Updated