AntiAIDS

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Author:
ljmtf3
ID:
61008
Filename:
AntiAIDS
Updated:
2011-01-26 12:32:19
Tags:
Pharmacology AntiAIDS
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Description:
Pharmacology, AntiAids
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  1. Abacavir
    • NRTI
    • Guanosine analog
    • good oral bioavalibility 83%
    • Elimination T1/2 1.5 h
    • Intracellular T1/2 12-26 h
    • CSF con 1/3 of plasma
    • Requires 2 mutations of HIV to be resistant to this drug.
    • Side effects: hypersensitivity, fever, malaise, n/v, diarrhea, skin rashes, pancreatitis(rare)
  2. Didanosine
    • NRTI
    • deoxyadenosine analog
    • oral bio 30-40% on empty stomach
    • Buffer (packaged with pills) interferes with: indinavir (PI), antivirals, and fluoroquinolones
    • Levels increase with: tenofovir ganciclovir
    • Levels decrease with: antivirals tipranavir, atazanavir
    • Side effects: dose dependent pancretitis(augmentited by alcoholism), peripheral neuropathy, diarrhea, hepatitis, CNS toxicity, optic neuritis
  3. Emtricitabine
    • NRTI
    • Fluorinated analog of Lamivudine
    • Oral bioavailability 93%
    • T1/2 >39 h
    • CSF conc is low
    • improvement on lamivudine cuz of longer T1/2
    • side effects: HA, diarrhea, Nausea, hyperpigmentation (3%)(more frequent in African americans
  4. Lamivudine
    • NRTI
    • Cytosine analog
    • active against AZT resistant strains
    • low dose effective against HBV
    • Oral bio: >80%
    • T1/2: 10.5-15.5 hr
    • CSF conc: 20% better than emtricitabine
    • side effects: HA, insomnia, fatigue, GI discomfort
  5. Tenofovir
    • NRTI
    • adenosine analog
    • Atripla: tenofovir, emtricitabine, efavirenz
    • Oral bio: 25% in fasting, 39% with high fat meal
    • T1/2: 60 h
    • CSF conc 55% of plasma
    • Used in place of stavudine in cases of dyslipidemia
    • renal secretion
    • Side effects: HA, n/v, diarreha, asthma, renal toxicity (rare)
    • Bone toxicity in animals only
  6. Zalcitabine (ddC)
    • NRTI
    • cytosine analog
    • Oral bio: 80%
    • T1/2: 10 h
    • CSF conc 20% of plasma
    • renal secretion
    • Side effects: Dose-dep peripheral neuropathy in 10-20%, drug withdrawl nullify, oral and esophageal ulcerations, self limiting HA, nausea, rash, Pancreatitis(rare)
  7. Zidovudine (AZT)
    • NRTI
    • deoxythymidine analog
    • Okay in pregnacy and after birth
    • t1/2: 3-7h
    • CSF conc 60-65% of plasma
    • renal secretion
    • Side effects: dyslipidemia and insulin resistance, myelosuppresion, anemia, neutropenia, thrombocytopenia, depigmentation(rare), self limiting HA, GI intolerance, insomnia
  8. Nevirapine (general info)
    • NNRTI
    • lipophilic noncompetitive inhibitor
    • Oral bio: 90% NOT FOOD DEPENDENT
    • 60% plasma bound
    • CSF conc 45% of plasma
    • Metabolized by P450 excreted by urine
    • Therapeutic use: monotherapy and used in combo with other antiretrovirals
  9. Nevirapine (drug interactions)
    • Inducers of CYP, including CYP3A4: ketoconazole, oral contraceptives, methadone
    • Conc of Nivirapine increase with: cimetidine or macrolide agents
    • Drugs metabolized by CYP3A4 or CYP2B6: rifampin, rifabutin (problem with treating TB and HIV people)
  10. Nevirapine (Side effects)
    • Common: skin rash (17%), sometimes toxic epidermal necrolysis, hepatic toxicity
    • Rare: abnormal liver function tests, chlils, fever, sore throat, pain in arm legs or feet, sleepiness, sores in mouth
    • Uncommon: aching joints and muscles, sore lips, dark urine, little appetite, N/V, yellow skin or eyes
  11. Delavirdine
    • NNRTI
    • 400mg tid
    • INHIBITOR OF CYP450
    • Oral bio: 85%
    • 98% protein bound
    • Side effects: HA, N/D, fatigue, skin rash (18%), steven-johnson syndrome (rare)
  12. Efavirnez
    • NNRTI
    • 600mg qd
    • T1/2: 40-55h
    • INHIBITOR OF CYP450
    • Oral bio: 85%
    • 99% protein bound
    • Side effects: HA, insomnia, confusion
    • Increased LFT
    • Congenital anamolies
  13. Indinavir (general info)
    • PI: inhibit HIV1(more potent for this one) and HIV2 proteases
    • Oral bio: 65% MUST TAKE ON EMPTY STOMACH
    • 60% protein bound
    • CSF conc 75% (highest among PI)
    • Metabolized in liver (CYP3A4), excreted in feces
    • Resistance due to multiple codon substitutions
  14. Indinavir (side effects)
    • Common: blood in urine (crystalluria and nephrolithiasis, sharp back pain below ribs
    • Uncommon: hyperbilirubinemia, GI upset, ab pain, HA, fatigue, insomnia
    • Rare: confusion, dehydration, dry skin, fatigue, n/v, weightloss
  15. Saquinavir
    • PI
    • high protein bound
    • poor CNS penetration
    • excreted in feces
  16. Ritonavir
    • PI
    • bind to active site on HIV protease
    • metabolized extensively eliminated mainly in feces
    • 98-99% protein bound
    • Side effects: Dose dependent GI upset
    • (only prescribed now to boost other drugs, inhibits CYP3A4)
  17. Lopinavir/Ritonavir
    • PI
    • More potent against HIV-1 than ritonavir (boosts lopinavir by P450)
    • only in co-form with ritonavir
    • Fast Absorption INcreased by HIGH FAT MEAL
    • highly protein bound
    • low CNS penetration
    • Side effects: GI upset
  18. Nelfinavir
    • PI
    • Slow Absorption INcreased by HIGH FAT MEAL
    • highly protein bound
    • M8 is active metabolite
    • Side effects: diarrhea, flatulence
  19. Amprenavir
    • PI
    • active site inhibitor of HIV protease
    • Fast absorption DEcreased by high fat meal
    • highly protein bound
    • Side effect: GI intolerance
  20. Fosamprenavir
    • PI
    • Phosphonooxy prodrug of amprenavire
    • increased water solubility
    • improved oral bioavailability over amprenavir
  21. Darunavir
    • New PI
    • well tolerated reduced side effects
    • combo with ritonavir cuz CYP3a4
    • ONCE A DAY DOSING (800mg)
    • Take with FOOD
  22. Atazanavir
    • New PI
    • ONCE A DAY DOSING (300mg)
    • combo with ritonavir
    • less likely to cause lipodystrophy
    • DONT use with PPI
    • DONT use with INDANAVIR cuz both inhibit UGt1a1
  23. Enfuvirtide
    • Fusion/entry inhibitor
    • Binds to gp41 subunit of viral envelope to prevent the conformational changes required for fusion of viral and cellular membranes
    • no cross resistance with other classes of antiretrovirals
    • subcutaneous injection
    • Side effects: location reaction, hypersensitivity
    • high cost; reserved for people who fail other regimesn
  24. Maraviroc
    • CCR5 inhibitor
    • combo with other antiretroviral
    • 150-300 mg oral
    • Side effects: hepatotoxicity, cardiovascular events, immune reconstitution syndrome, potential risk of infection, potential risk of malignancy
  25. Raltegravir
    • Integrase inhibitor (binds to integrase to inhibit strand transfer)
    • no interaction with P450
    • metabolized by glucoronidation
    • combo therapy only cuz resistance requires only a single point mutation
    • Drug interactions: through UGT1a1, rifampin, efavirenz, tipranavir, ritonavir, atanzanavir

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