Pharmacology Exam 1

Card Set Information

Author:
Rx2013
ID:
61318
Filename:
Pharmacology Exam 1
Updated:
2011-01-22 15:38:28
Tags:
Treatment AIDS
Folders:

Description:
Treatment of AIDS
Show Answers:

Home > Flashcards > Print Preview

The flashcards below were created by user Rx2013 on FreezingBlue Flashcards. What would you like to do?


  1. Retroviruses
    • RNA as thier genetic material
    • enveloped
  2. HIV replication requires
    chemokine receptor on Tcells and macrophages
  3. HIV binds to this receptor
    • CCR5 co-receptor
    • chemokine receptor
  4. HIV RT has ______ fidelity _____ mutation rate.
    • low fidelity
    • high mutation rate
  5. Problems encountered with anti-HIV therapy
    • virus hides in deep tissues
    • virus hides in brain
    • virus integrates into cellular genome
    • can cause mutation in target genes unlike DNA virus
  6. Six classes of antiretroviral agents
    • Nucleoside/Nucleotide RT inhibitor
    • Non-nucleoside/tide RT inhibitor
    • Protease inhibitor
    • fusion inhibitor
    • integrase inhibitor
    • CCR5 antagonist
  7. Nucleoside/tide RT inhibitors (8 DRUGS)
    • Abacavir
    • Didanosine
    • Emtricitabine
    • Lamivudine
    • Stavudine
    • Tenefovir
    • Zalcitabine
    • Zidovudine
  8. Nucleoside/tide RT inhibitors MoA
    • require intracellular activation (phosphorylation)
    • competitive inhibition of HIV RT
    • termination of DNA elongation
  9. Abacavir
    • NRTI
    • guanosine analog
    • good OB, short HL
    • skin rashes in 50%
  10. Didanosine
    • NRTI
    • deoxyadenosine analog
    • 30% OB
  11. increases Didanosine serum levels
    • ganciclovir
    • tenofovir
  12. decreases serum levels of Didanosine
    • tipranavir
    • atazanavir
  13. Side effects of Didanovir
    • pancreatitis
    • peripheral neuropathy
  14. Emtricitabine
    • fluorinated analog of Lamivudine
    • NRTI
    • 93% OB 39hr HL
  15. Lamivudine
    • cytosine analog
    • NRTI
    • active against AZT resistant strains
    • 80% OB 10-15 hr HL
    • 20% CSF
  16. Problems with low dose ARV therapy
    • creates resistance
    • some are used in low doses to treat HBV and these patients could also have HIV
  17. Stavudine
    • Thymidine analog
    • NRTI
    • OB 86% not dependant on food
    • 3.5 hr HL
    • 55% CSF
  18. Side effects of Stavudine
    • dyslipidemia (buffalo hump)
    • insulin resistance
    • peripheral neuropathy
  19. Drug Drug interaction with stavudine
    isoniazid
  20. Tenofovir
    • NRTI
    • adenosine analog
    • increased OB after fatty meal
    • 60hr intracellular HL
  21. indications for Tenofovir
    used in place of stavudine in cases of dyslipidemia
  22. Zalcitabine
    • cytosine analog
    • NRTI
    • 80% OB on empty stomach
    • 10hr intracellular HL
    • peripheral neuropathy 10-20%
  23. Zidovudine
    • Deoxythymidine analog
    • NRTI
    • used in pregnancy
    • 3-7 hr HL
    • 60% CSF
    • dyslipidemia and insulin resistance
  24. Non-nucleoside RT inhibitors
    • directly interact with RT inducing a conf. change
    • specific for HIV 1 RT
    • must be used in combo to avoid resistance
    • no-cross resistance with NRTIs or PIs
  25. NNRTIs (3 drugs)
    • Delavirdine
    • Efavirnez
    • Nevirapine
  26. Action of NNRTIs
    • no phosphorylation required
    • CYP450 interactions
    • Allosteric inhibition of RT
  27. Nevirapine
    • NNRTI
    • highly lipophilic
    • not food dependant 90% OB
    • 60% protein bound
  28. Drug interactions with Nevirapine
    • moderate induction of CYP3A4
    • Rifampin
    • Rifabutin
    • Cimetidine or macrolides increase concentrations
  29. Side effects with Nevirapine
    • 17% skin rash
    • epidermal necrolysis
    • hepatic toxicity
  30. Delaviridine
    • NNRTI
    • 98% protein bound
    • 18% skin rash
    • inhibits CYP450
  31. Efavirnez
    • NNRTI
    • 99% protein bound
    • increased LFT
    • Congenital abnormalities
    • inhibits CYP450
  32. Protease inhibitors
    • acts on late stages of HIV replication
    • prevents new waves of infection
    • substrate and inhibitor of CYP3A4
    • only ARV to act after viral integration into host genome
  33. PI strongest inhbitor of CYP3A4
    ritonavir
  34. weakest PI that inhibits CYP3A4
    saquinavir
  35. PIs that induce CYP
    • amprenavir
    • ritanovir
  36. Only ARV to act after viral integration into the host genome
    PIs
  37. Indinavir
    • PI 10x more potent for HIV1 vs 2
    • must be taken on an empty stomach
    • highest [CSF] among PIs
  38. Common side effects of indinavir
    blood in urine due to crystalluria and nephrolitiasis
  39. Protese Inhibitors (6 drugs)
    • saquinavir
    • ritonavir
    • lopinavir/ritonavir
    • nelfinavir
    • amprenavir
    • fosamprenavir
  40. Lopinavir/ritonavir combo
    • ritonavir inhibits metabolism of lopinavir
    • increased absorption with high fat meals
  41. Nelfinavir
    • PI
    • increased absorption with high fat meal
  42. Amprenavir
    decreased absorption with high fat meal
  43. Fosamprenavir
    prodrug for amprenavir with improved OB
  44. 2 new PIs
    • Darunavir
    • Atazanavir
    • dosed once daily
    • used in combo with ritonavir
    • recommended for ARV naive pt
  45. Atazanacir should not be used with
    PPIs
  46. Fusion/Entry inhibitors
    • bind GP41 of viral envelope preventing conf change
    • no cross resistance
    • administered by injection
    • high cost reserved for failed treatments
    • Enfuvirtide
  47. Maraviroc
    • CCR5 inhibitor
    • hepatotoxicity
    • cardiovascular risk
  48. Raltegravir
    integrase inhibitor
  49. Raltegravir drug interactions through UGT1A1
    • Rifampin
    • Efavirenz
    • Tipranavir
    • Ritonavir
    • Atazanavir
  50. NRTI recommended in pregnancy
    • Zidovudine
    • lamivudine
  51. NNRTIs recommended in pregnancy
    Nevirapine
  52. PIs recommended in pregnancy
    • Nelfinavir
    • Saquinavir
  53. Alternate NRTIs that may be used in pregnancy
    • Didanosine
    • Emtricitabine
    • Abacavir
    • Stavudine
  54. Alternate PIs that may be used in pregnancy
    • Indinavir
    • Lopinavir/Ritonavir
    • Ritonavir
  55. HAART means taking
    a combination of 3 or more ARVs from at least 2 classes
  56. HAART treatment is modified according to
    • CD4+ Tcell count
    • Viral load
    • tolerance
  57. Drugs under investigation for prophylaxis
    tenofovir with or without emtricitabine

What would you like to do?

Home > Flashcards > Print Preview