Typically 3 ARV drugs simultaneously —> antiretroviral therapy (ART)Start ASAP‣Each component administered at optimal dose, frequency‣PT adherence is critical ‣Golden rule: all or nothing ‣ARV drugs available •Nucleoside/nucleotide reverse transcriptase inhibitors Nonnucleoside reverse transcriptase inhibitors Protease inhibitors Integrate inhibitors Entry inhibitors Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)•DrugsZidovudine (Retrovir)‣Lamivudine (epivir)‣Emtricitabine (emtriva)‣Abacavir (ziagen)‣Tenofovir disoproxil fumarate (viread)‣Tenofovir alafenamide (combo tabs only)‣Pharmacology MOA: competitively inhibit reverse transcriptase (RT)‣Must enter cells, be phosphorylated to generate synthetics substances for •RT Block replication by inhibiting incorporation of native nucleotides, •terminating proviral DNA Class Related Properties
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“Backbone” of ART ‣Dosed QD or BID‣Renal elimination, short plasma half-life, longer intracellular half-life •Not major substrates for hepatic CYP enzymes ‣Potential for severe adverse events ‣Toxicities Depends on inhibition of host cell DNA polymerases‣Anemia, granulocytopenia, myopathy, peripheral neuropathy, pancreatitis •BBW: lactic acidosis +/- hepatomegaly and hepatic steatosis (staduvine, •zidovudine, didanosine)Zidovudine (Retrovir)Use diminished in recent years ‣More tolerable, potent NRTIs•BID tablets or capsules, also liquid ‣Renal dose adjustment required •IV formulation —> intrapartum administraiton to prevent mother-to-child ‣transmission Anemia and neutropenia are most frequent dose-limiting adverse effects ‣Lamivudine (Epivir)QD or BID‣Renal dose adjustments required •Active against Hep B virus ‣Lamivudine exhibits extensive cross-resistance with emtricitabine (never ‣together) Generally well tolerated ‣Emtricitabine (emtriva)QD‣Renal dose adjustments required •Active against Hep B virus ‣Extensive cross resistance with lamivudine ‣Generally well tolerated ‣May cause hyperpigmentation of gums and nails (especially in dark-•skinned persons) Abacavir (ziagen)QD or BID‣Hepatic dose adjustments required •Generally well tolerated; hypersensitivity reaction ≤6 weeks of therapy ‣Sign/symptoms: fever, rash, GI, constitutional, respiratory •Prior to initiating screen for HLA-B*5701 •If positive never administer abacavir Tenofovir Disoproxil fumarate ‣QD•Renal adjustments required Active against Hep B virus •
FDA approved for pre-exposure prophylaxis with emtricitabine •Generally well tolerated •Rarely causes acute renal failure Fanconi’s syndrome Proteinuria Tubular necrosis Decreased bone-mineral density Alafenamide ‣QD •Renal dose adjustments required Active against Hep B virus •NOT FDA approved for PrEP•Reduced bone and kidney toxicity compared to other •
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