HIV Pharmacotherapy

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What is the life cycle of HIV?
- Binding
- Fusion
- Reverse transcription
- Nuclear localization/uncoating
- Integration
- Transcription
- Splicing
- Translation +/- modification
- Assembly/budding
- Maturation
What agents are used to target budding in HIV?

Miraviroc
What are the characteristics of Maraviroc?
- Blocks CCR5 receptor (need a Tropism test before using this agent)
- Acceptable for tx naive pts (not DOC or even alternative)
- 3A4 substrate
- Myopathy
What agents are used to target fusion in HIV?

Enfuvirtide
What are the characteristics of Enfuvirtide?
- Last line, salvage tx
- Difficult to get into solution
- Must be refridgerated
- Skin nodules
What agents are used to target reverse transcriptase conversion of viral RNA to DNA in HIV?
- NRTIs
- NNRTIs
What are the NRTIs used for HIV?
- Abacavir
- Didanosine
- Emtricitabine
- Lamivudine
- Stavudine
- Tenofovir disaproxil fumarate
- Zidovudine
What are the NNRTIs used for HIV?
- Delavirdine
- Efavirenz
- Etravirine
- Nevirapine
What are the characteristics of Abacavir?
- Tremendously effective NRTI
- No food effect
- Alcohol increases levels
- life-threatening hypersensitivity (need a HLA-B*5701 test to use)
What are the characteristics of Didanosine?
- Good secondary drug
- Take on empty stomach
- Pancreatitis (common)
- Peripheral neuropathy
What are the characteristics of Emtricitabine?
- Similar to Lamivudine
- V. long half-life (39h)
- Good tolerance and compliance
What are the characteristics of Lamivudine?
- Great combo drug
- Can resensitize to Zidovudine
- Caution discontinuing in Hep B pts (rebound hepatitis)
- Very little SE
What are the characteristics of Stavudine?
- Falling out of favor as 2nd line
- Pancreatitis
- Peripheral neuropathy
- Metabolic syndrome
- Lipodystrophy
What are the characteristics of Tenofovir?
- V. effective
- a nucleotide (requires 1 less phosphorylation than other NRTIs)
- Give with food
- Big DI with Didanosine
- Nephrotoxic
- Hepatotoxic
- HA
- NVD
What are the characteristics of Zidovudine?

Bone marrow suppression (neutropenia and anemia)
What are the class side effects of NRTIs?
- Lactic acidosis
- Peripheral neuropathy ("D" drugs)
- Watch dosing in renal dysfunction
What are the class effects of NNRTIs?
- Rash
- Hepatotoxicity
- Complete cross-resistance (except Etravirine)
- multiple DI
What are the characteristics of Delavirdine?
- Least effective NNRTI
- 3A4 inhibitor
What are the characteristics of Efavirenz?
- Most used/effective NNRTI
- Take on an empty stomach
- Mixed 3A4 inhibition/induction
- CNS SE (give at night)
What are the characteristics of Etravirine?
- Newest approved
- Take after a meal
- No cross-resistance
What are the characteristics of Nevirapine?
- 2nd most used NNRTI
- 3A4 inducer (self-induces)
- Most hepatotoxic NNRTI (don't use if CD4 >250 in females and >400 in males)
- Avoid in severe liver dysfunction
- Least metabolic SE
What agents are used to inhibit integration of viral DNA into cellular DNA in HIV?

Raltegravir
What are the characteristics of Raltegravir?
- Recently moved to 1st line
- Myopathy (worse than Maraviroc - check CPK routinely)
- HA
- NVD
What agents are used to inhibit protease assembly and maturation in HIV?
- Atazanavir
- Darunavir
- Fosamprenavir
- Indinavir
- Lopinavir/Ritonavir
- Nelfinavir
- Ritonavir
- Saquinavir
- Tipranavir
What are the class effects of the PIs?
- Generally accepted as most effective
- Kind of work like vaccines because they make the live virus non-virulent
- 3A4 inhibition
- Lipodystrophy
- Dyslipidemia
- Hyperglycemia
- Elevation of transaminases
What are the characteristics of Atazanavir?
- Most used PI
- Boost with Efavirenz and Tenofovir
- Take with food
- Big interaction with PPIs and H2 blockers
- Hyperbilirubinemia (usually not problematic)
- maybe less metabolic effects than other PIs
What are the characteristics of Darunavir?
- 1st line PI
- Boost with Ritonavir
- Take with food
- Sulfonamide moiety
What are the characteristics of Fosamprenavir?
- Alternative PI
- Rash
What are the characteristics of Indinavir?
- Take on empty stomach (unless boosted)
- V. labile to humdity
- Great distribution to various tissues
- Nephrolithiasis (drink 6 additional 8oz glass of water/d)
What are the characteristics of Lopinavir/Ritonavir?
- 1st line or salvage
- Take with food (42% alcohol)
- Refrigerate to extend shelf-life
- DOC in pregnancy
What are the characteristics of Nelfinavir?

Take with food
What are the characteristics of Ritonavir?
- Used as a booster, not as a PI
- Refrigeration extends shelf-life (capsules only)
- Greatest 3A4 inhibition
- Most metabolic effects?
What are the characteristics of Saquinavir?
- Salvage tx
- ECG abnormalities (QT prolongation)
- NVD
What are the characteristics of Tipranavir?
- Salvage tx
- Unique resistance profile
- Refrigeration extends shelf-life
- Sulfonamide moiety
- Intracranial hemorrhage (v. rare)
What are the combination products used in HIV?
- Atripla (Efavirenz + Emtricitabine + Tenofovir)
- Trizivir (Abacavir + Lamivudine + Zidovudine)
- Kaletra (Lopinavir + Ritonavir)
- Combivir (Lamivudine + Zidovudine)
- Truvada (Emtricitabine + Tenofovir)
- Epzicom (Abacavir + Lamivudine)
What is the preferred NNRTI-based regimen for HIV in therapy naive pts?

Atripla (Efavirenz + Emtricitabine + Tenofovir)
What is the alternative NNRTI-based regimen for HIV in therapy-naive pts?
- Efavirenz + Epzicom (Abacavir + Lamivudine) or Combivir (Zidovudine + Lamivudine)
- Navirapine + Combivir
What is the preferred PI-based regimen for HIV in therapy-naive pts?
- Atazanavir + Ritonavir + Truvada (Emtricitabine + Tenofovir)
- Darunavir + Ritonavir + Truvada
What is the alternative PI-based regimen for HIV in therapy-naive pts?
- Atazanavir + Ritonavir + Epzicom (Abacavir + Lamivudine) or Combivir (Zidovudine + Lamivudine)
- Fosamprenavir + Ritonavir + Epzicom or Combivir or Truvada
- Kaletra (Lopinavir + Ritonavir) + Epzicom or Combivir or Truvada
What is the preferred INSTI-based regimen for HIV in therapy-naive pts?

Raltegravir + Truvada (Tenofovir + Emtricitabine)
What is the preferred regimen for HIV in pregnant women?

Kaletra (Lopinavir + Ritonavir) + Combivir (Zidovudine + Lamivudine)
What is the procedure for Post Exposure Prophylaxis?
- Determine HIV status of source
- Begin 2-3 drug regimen ASAP (<2h)
- Consult with ID physician to determine risk of transmission and duration of tx

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giddyupp

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HIV Pharmacotherapy

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HIV Pharmacotherapy

Updated

2011-02-04T16:48:55Z

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