HIV Agents

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Author:
HUSOP2014
ID:
136649
Filename:
HIV Agents
Updated:
2012-02-24 01:03:49
Tags:
HUSOP DA EXAM2 Anti HIV Drugs
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Description:
Generic, brand, acronym, resistance mutation, combo-therapy side effects.
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  1. Zidovudine
    • Acro: ZDV, AZT (3'-azido-3'-deoxythymidine)
    • Class: Thymidine-NRTI
    • Res-mut: K65R, codon 69
    • Combo: lamivudine
    • Indication: Adult and pediatric HIV, mom/child transmit, post exposure in workers
    • ADE: myelosuppression, minor side effects
    • Activity: in lymphocytes-greater phosphorylation
  2. Stavudine
    • Acro:d4T (2'3'-didehydro-2'3'-dideoxythiymidine)
    • Class: Thymidine- NRTI
    • Res-mut: K65R, codon 69
    • Combo: lamivudine
    • Indication: HIV
    • ADE: peripheral neurophathy, Lactic acidosis, hepatic steatosis
    • Activity: potent in activated cells w/ thymidine kinase in S-phase
  3. Dideoxycytidine (Zalcitabine)
    • Acro: ddC (2'3'-dideoxycytidine )
    • Class: Cytosine- NRTI
    • Res-mut: polymerase mutations,codon 69
    • Combo: ddC, AZT, Saquinavir
    • Indication: HIV-1,2 and HBV
    • ADE: oral ulceration and stomatits, Peripheral neuropathy
    • Activity: best nucleoside in monocyte/macrophages, more potent in resting cells w phosphorylation
  4. Emtricitabine
    • Acro: FTC
    • Class: Cytosine- NRTI
    • Res-mut: M184V, codon 69
    • Combo: w NRTI, NNRTI, Protease-I
    • Indication:HIV-1,2 and HBV
    • ADE: Hyperpigmentation w/UV
  5. Lamivudine
    • Acro: 3TC (2'3'dideoxy3'-thiacytidine)
    • Class: Cytosine- NRTI
    • Res-mut: after 4yrs, M184V, codon 69
    • Combo: AZT
    • Indication: HIV-1,2 and HBV
    • ADE: least toxic profile
  6. Abacavir
    • Acro: ABC
    • Class: Guanosine- NRTI
    • Res-mut: codon 69
    • Combo:
    • Indication: HIV-1,2
    • ADE: fatal-Hypersensitivity reaction(11 day onset, 90% within 6 weeks- HLA-B*5701 and Hsp70-hom)
    • Activity: >300X better
  7. Didanosine
    • Acro: ddl (2'3'-dideoxyinosine)
    • Class: Adenosine- NRTI
    • Res-mut: RT-codon-69
    • Combo:
    • Indication: Adult/Pediatric: HIV1&2 and HTLV-1
    • ADE: peripheral neuropathy, pancreatitis (miochondrial), tingling, lactic acidosis
    • Special: acid labile w antacid buffer, 2 hrs b4 meals,
  8. Tenofovir
    • Acro:TDF
    • Class: Adenosine- NRTI (only nucleotide)
    • Res-mut: single codon K65R
    • Combo:
    • Indication: Adult: HIV-1,2 and HBV
    • ADE: flatulence
  9. Efavirenz
    • Class: NNRT-I bind non-essential HIV RT distant cat site
    • Res-mut: single AA mutation in binding pocket (a must) resistance in days/weeks (alone)
    • Combo: w/zidovudine/lamivudine
    • Indication:Adult/Child HIV-1 (non-naive HIV cells-low tox)
    • ADE: Rash, Disturbing Dreams, teratogen
    • Metabolized: CYPs: 3A4, 2B6/3A4
  10. Nevirapine
    • Class: NNRT-I bind non-essential HIV RT distant cat site
    • Res-mut: single AA mutation in binding pocket (a must)- resistance in days/weeks (alone)
    • Combo: w/ zidovudine/didanosine
    • Indication: Adult/Child HIV-1 in combo only, maternal/child transmission
    • ADE: rash, elevated transaminases, hepatitis
    • Metabolized: CYPs: 3A4, 2B6/3A4
  11. Delavirdine
    • Class: NNRT-I, bind non-essential HIV RT distant cat site
    • Res-mut: Single AA mutation in binding pocket
    • Combo: (A Must)-resistance in days/weeks (alone)
    • Indication: HIV-1
    • ADE:
    • Metabolized: CYPs: 3A4, 2B6/3A4
  12. Saquinavir
    • Class: (aspartyl) Protease-I of Gag/Pol
    • Res-mut: w multiple mutations
    • Combo: w/ritonavir and NRTI
    • Indication: HIV1,2
    • ADE: GI distress
    • Metabolized: CYP 3A4-oxidation
  13. Ritonavir
    • Potent CYP3A4-I used to increase levels of other drugs
    • Class: (aspartyl) Protease-I of Gag/Pol
    • Res-mut: w multiple mutations
    • Combo: not monotherapy due to GI toxicity
    • Indication: HIV-1,2
    • ADE: GI, taste, perioral and peripheral paresthesias, dose depend increase TGs, lipodystrophy
    • Metabolized: CYP 3A4-oxidation
  14. Indinavir
    • Food decreases bioavailability unlike others from class,
    • Class: (aspartyl) Protease-I of Gag/Pol
    • Resistance: w multiple mutations
    • Indication:
    • ADE: crystalluria and nephrolithiasis, insulin-resistance, patient needs to stay hydrated
    • Metabolized: CYP 3A4-oxidation
  15. Nelfinavir
    • Class: (aspartyl) Protease-I of Gag/Pol
    • resistance: w multiple mutations
    • Indication: HIV pregnant women w/ no teratogenesis
    • ADE: Diarrhea (no teratogenesis)
    • Metabolized: CYP 2C19-oxidation(only one in this class)
  16. Amprenavir
    • Prodrug: Fosampernavir, a phosphonooxy
    • Class:(aspartyl) Protease-I of Gag/Pol
    • Resistance: w multiple mutations
    • Indication: HIV-1,2
    • ADE:GI disturbances, hyperglycemia, skin eruptions
    • Metabolized: CYP 3A4-oxidation
  17. Lopinavir
    • Class:(aspartyl) Protease-I of Gag/Pol
    • Resistance: w multiple mutations
    • Indication: HIV-1,2 ( in failed pateints w/ other HIV protease-multidrug combo)
    • ADE: GI distrubances
    • Metabolized: CYP 3A4-oxidation
    • Combo: only use with ritonavir
  18. Atazanavir
    • Metabolite: deamidated c-terminal phenylalanine
    • Class: (aspartyl) Protease-I of Gag/Pol
    • Res-mut: w multiple mutations
    • Indication: HIV-1,2
    • ADE: Hyperbilirubinemia w/o hepatotoxicity, slight rise in cholesterol and TG, no insulin resistance
    • Metabolized: CYP 3A4-oxidation
  19. Enfuvirtide
    • Acro: INN
    • Class: Entry Inhibitor- N36/C34 sequences in gp41
    • Res-mut: gp41 binding domain
    • Combo:
    • Indication: HIV-1 only, Adults with HIV replication despite therapy
    • ADE: Injection site reactions

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