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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
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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
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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
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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
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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
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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
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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,
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Tenofovir
- Acro:TDF
- Class: Adenosine- NRTI (only nucleotide)
- Res-mut: single codon K65R
- Combo:
- Indication: Adult: HIV-1,2 and HBV
- ADE: flatulence
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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
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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
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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
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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
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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
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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
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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)
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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
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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
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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
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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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