Typically 3 arv drugs simultaneously antiretroviral

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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) Drugs Zidovudine (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
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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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  • Fall '19
  • Tetracycline, UTI, Ceftriaxone

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