Therapeutics - HIV 3

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kyleannkelsey
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288951
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Therapeutics - HIV 3
Updated:
2014-11-11 21:30:39
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Therapeutics HIV
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Therapeutics - HIV
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Therapeutics - HIV
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  1. Cross resistance ___________,___________ and/or ______________is likely after development of resistance to rilpivirine.
    to efavirenz, etravirine, and/or nevirapine
  2. NNRTIs have what effect on Azole antifungals?
    • Decrease in Azole conc.
    • Increase in NNRTI conc.
  3. What NNRTIs affects Clarithromycin and what effect do they have?
    • Rilpivirine
    • Etravirine
    • Increase in both Clarithromycin and NNTRI concentration
  4. What NNRTIs affects PPIs and what effect do they have?
    • Rilpivirine
    • Decrease PPI levels (CI)
  5. What NNRTIs affects Opioids and what effect do they have?
    • Decrease Opioid levels
    • Efavirenz
    • Rilpivirine
  6. Anticonvulsants are CI with what NNRTIs?
    Etravirine
  7. Rifampin/Rifabutin are CI with what NNRTIs?
    • Efavirenz
    • Etravirine
  8. Benzodiazapines are CI with what NNRTIs?
    • Efavirenz
    • Etravirine
  9. What NNRTIs affects Warfarin and what effect do they have?
    • Increase Warfarin levels
    • Efavirenz
    • Etravirine
  10. Enfuvirtide is used at what point in treatment?
    • Usually all other treatments exhausted
    • Low CD4 cells
  11. How is Enfuvirtide used for the treatment of HIV-1?
    In combination with other antiretroviral agents in treatment-experienced patients despite ongoing antiretroviral therapy
  12. What is the MOA of Enfuvirtide?
    Interferes with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes
  13. Maraviroc is a CCR5 co-receptor antagonist, what is the MOA of this drug class?
    Fusion inhibitor
  14. What is Maraviroc indicated for?
    • Combination antiretroviral treatment in adults
    • Only for CCR5-tropic HIV-1 detectable disease
    • Test to determine if you have CCR5-tropic virus
    • For use in patients who have evidence of viral replication
    • HIV-1 strains resistant to other antiretroviral agents
  15. What is the MOA of Maraviroc?
    • Binds to human CCR5 on cell membrane
    • Prevents interaction between HIV-1 gp120 and CCR5
    • Blocks entry of HIV-1 into human cells
  16. Pharmacokinetics:
    23% FF* - 100 mg dose; 33% FF* - 300 mg dose
  17. What are the side effects of Maraviroc?
    Abdominal pain, cough, dizziness, rash, hepatotoxicity, orthostatic hypotension
  18. Should you take a lower or higher dose if you give Maraviroc with a strong CYP3A inhibitor?
    Lower
  19. Should you take a lower or higher dose if you give Maraviroc with a NRTIs, tipranavir/ritonavir, Nevirapine, Enfuvirtide?
    Moderate= normal
  20. Should you take a lower or higher dose if you give Maraviroc with given with CYP3A inducers (efavirenz, rifampin, etc.)?
    Higher
  21. What is the bioavailability of Maraviroc associated with?
    Dose
  22. What are the integrase inhibitors?
    • Raltegravir – Isentress
    • Dolutegravir – Tivicay
    • Dolutegravir abacavir/lamivudine - Triumeq
    • Elvitegravir – Stribild (quad pill)
    • Cobicistat – Tybost
    • Elvitegravir – Vitekta
  23. What is the brand name for Raltegravir?
    Isentress
  24. What is the brand name for Dolutegravir?
    Tivicay
  25. What is the brand name for Dolutegravir abacavir/lamivudine?
    Triumeq
  26. What is the brand name for Elvitegravir?
    Stribild (quad pill)
  27. What is the brand name for Cobicistat?
    Tybost
  28. What is the brand name for Elvitegravir?
    Vitekta
  29. What is the generic name for Isentress ?
    Raltegravir –
  30. What is the generic name for Tivicay?
    Dolutegravir
  31. What is the generic name for Triumeq?
    Dolutegravir abacavir/lamivudine
  32. What is the generic name for Stribild (quad pill)?
    Elvitegravir
  33. What is the generic name for Tybost ?
    Cobicistat
  34. What is the generic name for Vitekta?
    Elvitegravir
  35. What is the MOA of Raltegravir?
    • Integrase inhibitor – prevent insertion of HIV DNA into the human DNA genome
    • Block the formation of HIV-1 provirus
  36. What group of patients is Raltegravir used in?
    Treatment of HIV for tx-naïve and drug resistant pts with HAART
  37. Should Raltegravir be administered without regard to food?
    Either
  38. How long does it take to reach steady-state after beginning Raltegravir?
    Achieved within 2 days of dosing
  39. How is Raltegravir metabolized?
    By UGT1A1 via glucuronidation
  40. What are the side effects of Raltegravir?
    • Skin rash evolve to Stevens-Johnsons syndrome
    • Elevated CPKs
  41. What is the dose of Dolutegravir (Tivicay)?
    • 50 mg QD
    • Take BID if using enzyme inducers like: efavirenz, boosted fosamprenavir, tipranavir, or rifampin
    • Treatment-experienced patient – 50 mg BID
  42. Should you give Dolutegravir (Tivicay) with or without food?
    Can be administered without regard to food
  43. What should patients on Dolutegravir (Tivicay) avoid?
    • Avoid cation containing meds: mg, Ca supplements, iron, sucralfate, antacids
    • Anticonvulsants: phenytoin, phenobarbital, carbamazepine,
  44. What are the Side effects of Dolutegravir (Tivicay)?
    • Insomnia, headache
    • Hypersensitivity reactions (rash)
    • Worsening or elevated LFTs
  45. What does Stribild contain?
    • Tenofovir, emtricitabine – NRTIs
    • Elvitegravir – integrase inhibitor
    • Cobicistat – novel P450 inhibitor (no activity against HIV)
  46. What patients are eligible to receive Stribild (Tenofovir, emtricitabine, Eltegravir and Cobicistat)?
    • Used for tx-naïve patients
    • Only in patients with CrCl > 70 ml/min
  47. What is the dose of Stribild (Tenofovir, emtricitabine, Eltegravir and Cobicistat)?
    1 tab QD
  48. Cobicistat is FDA approved to be given with what other drugs?
    FDA approved to be given with atazanavir or darunavir
  49. What type of drug is Cobicistat?
    P450 inhibitor
  50. Elvitegravir comes in what dosage sizes?
    85 & 150 mg tablets
  51. How is Elvitegravir used?
    With boosted PI + another drug (NRTI)
  52. What is the most common side effect of Elvitegravir?
    Diarrhea (7%)
  53. What is EC90?
    Concentration of drug that are needed to inhibit 90% of the viral growth
  54. A resistant virus EC90 compared to a wild-type virus is many times lower or higher?
    Higher
  55. Phenotypic resistance is the consequence of____________________________________.
    Specific mutations in target genes
  56. Combination regimens with enhanced antiviral potency suggests that the emergence of resistance is reduced when____________________________.
    viral replication is effectively suppressed
  57. What is the most common reason for resistance to develop to HIV drugs?
    • Non-adherence
    • (Make regimens doable)
  58. What is “Viral load”?
    • Number of RNA copies in the serum
    • Indirect reflection of the number productively infected cells
    • associated with the rate of disease progression and time of death
  59. HIV RNA viral load or CD4 counts are more predictive of disease progression?
    RNA viral load
  60. Typically ____________ virions are produced daily.
    10^9 to 10^10
  61. When What is HIV RNA assay used for?
    • Assessing baseline status in newly diagnosed
    • Assessing response to therapy
    • Assessing development of resistance to current therapy
  62. What are the benefits of Combination therapy for HIV?
    Reduced toxicity and emergence of resistance
  63. The minimal change in viral load considered to be statistically significant is:
    A threefold or 0.5 log copies/mL change
  64. Optimal viral suppression is generally defied as a viral load below the level of detection, what is the level of detection?
    < 200 copies/mL
  65. How long does it take for an antiviral regimen to produce viral suppression?
    Achieved in 12-24 weeks

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