Antiretrovirals
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Antiretrovirals
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DrugToxicityCommentsFixed-Dose TherapyResistance
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NRTI (nucleoside reverse transcriptase inhibitors)
Competitive RT inhibitor (chain terminator, ø 3’ OH) (all but TDF require 3x PO4)
M184VQ151MQ151M*TAMsQ151M*: A62V, V75I, F77L, F116Y
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Analog blockingExcision enhancement
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Tzidovudine (AZT), Retrovir+ megaloblastic anemiaused in pregnancyCombivir↑ suscep.+++++TAMs: M41L, D67N, K70R, L210W, T215Y/F, K219E/Q
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Adidanosine (ddI), Videx+ pancreatitis++++
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Tstavudine (d4T), Zeritperipheral neuropathy++++
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Clamivudine (3TC), Epivir+ Tx HBVEpzicomTriumeqDutrebisCombivir+++
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Gabacavir (ABC), ZiagenHLA-B*5701 hypersensitivityEpzicomTriumeq±+++
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Cemtricitabine (FTC), Emtriva+ Tx HBV (similar to 3TC)TruvadaAtriplaCompleraStribild Genvoya+++
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Atenofovir (TDF), Vireadrenal insufficiency, Fanconi, nausea, diarrheaTruvadaAtriplaCompleraStribild Genvoya↑ suscep.
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NNRTI (non-nucleoside reverse transcriptase inhibitors)
Non-competitive inhibitors (ø PO4 required)
L100IK103NK101EY181/8C/LG190EEFV/NVP pressure: L100I, Y181C/I, K103N, V106A/M, V108I, Y188C/H/L and G190A/S
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EntranceEntranceInsideSterics
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efavirenz (EFV), Sustiva+ CNS Sxteratogen (ø pregnancy)Atripla+++++
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nevirapine (NVP), ViramuneStevens-Johnson syndrome, toxic epidermal necrolysis, hepatotoxicity+++++
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delavirdine (DLV), Rescriptorteratogen (ø pregnancy)++++
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etravirine (ETR), Intelence++++
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rilpivirine, EdurantComplera++++
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Protease Inhibitors
Inhibit pol (cleaves polypeptide products)
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saquinavir, Invirase/Fortovasehyperglycemia, HLD, GI intolerance, lipodystrophyP450 (CYP3A4) inhibitor
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ritonavir, NorvirP450 (CYP3A4) inhibitorKaletra
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indinavir (IDV), Crixivancrystal-induced nephropathy
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lopinavirKaletra
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atazanavir, ReyatazEvotaz
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fosamprenavir, Lexiva
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darunavir, PrezistaPrezcobix
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P450 (CYP3A4) inhibitor
No anti-HIV activity
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cobicistat, Tybostelevated Cr, proteinuriaEvotazPrezcobixStribild Genvoya
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Integrase Inhibitors
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raltegravir (RAL), Isentressdecreased hypercholesterolemiaDutrebis
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elviregravir (EVG), VitektaStribild Genvoya
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dolutegravir (DTG), TivicayTriumeq
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Fusion Inhibitors
Blocks gp41 conformational ∆ or binds CCR5 (which binds viral gp120)
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enfuvirtide, Fuzeoninjection site eosinophilia
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maraviroc, Selzentry
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