Metabolic complications increase total cholesterol

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Metabolic complications: increase total cholesterol, increase TGs, insulin resistance Fat redistribution GI adverse effects Lopinavir (w/ ritonavir (Kaletra)) Only boosted PI coformulated with Ritonavir BID Liquid formulation contains 42% ethanol 3A4 inhibitor and substrate Diarrhea, nausea, hyperlipidemia Atazanavir (reyetaz) QD Increase BA with acid medium Boosted with ritonavir or cobicistat Biliary elimation (inhibits UGT1A1 glucorinidation) 3A4 and 2C9 inhibitor Associated with increased risk of kidney stones, gallstones, unconjugated hyperbilirubinemia Darunavir (Prezista) QD (BID if PI resistance) Boosted with ritonavir or cobicistat Can be administered with H2RAs, PPIs 3A4 substrate and inhibitor Limited GI or lipid abnormalities Contains sulfonamide moiety Integrate Strand Transfer Inhibitors (INSTIs) Drugs Raltegravir (isentress) Elvitegravir (vitekta) Dolutegravir (tivicay) Bictegravir (biktarvy) Pharmacology MOA: blocks the catalytic activity of HIV encoded integrase Prevents integration of viral DNA into host chromosome Properties and Toxicities Do not require boosting Except elvitegravir
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Minimal drug interactions Except elvitegravir high genetic barrier to resistance Generally well tolerated; HA and GI effects most commonly reported Rare: neuropsychiatric ADEs, HSR, rhabdomyolysis Raltegravir (isentress, isentress HD) BID HD version —> QD no food requirements chewable formulation, phenylalanine Chelation of divalent cations May occur 6 hrs before or 2 hrs after dosing UGT1A1 substrate HA, nausea, asthenia, fatigue, CK elevations, rhabdomyolysis Elvitegravir Must be administered with food only available boosted with cobicistat 3A4, UGT1A1/3 substrate Inhibits tubular secretion of SCr w/o affecting actual GFR Nausea, diarrhea, depression Dolutegravir (trivicay) QD (BID if resistant) W/ or w/o food Chelation of divalent cations may occur 6 hrs before or 2 hours after UGT1A1, 3A4 substrate Inhibits renal organic cation transporter (OCT) 2 Doubles metformin concentrations inhibits tubular secretion of SCr w/o affecting GFR Insomnia, HA, HSR, rash, organ dysfunction Bictegravir Biktarvy Bictegravir/emtricitabine/tenofovir alafenamide QD No food requirements No booster required diarrhea, nausea, headache chelation of divalent cations May occur 6 hrs before or 2 hrs after UGT1A1, 3A4 metabolism Inhibits renal OCT2 Doubles metformin conc. Inhibit tubular secretion of SCr Doesn’t affect GFR Entry Inhibitors Pharmacology MOA: chemokine receptor antagonist, binds to host cell CCR5 receptor, blocks, binding of viral gp120 on host CD4 cell Question about chelation
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Maraviroc (selzentry) BID No food requirements Requires tropism assay before use CCR5-tropic HIV-1 virus only
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  • Fall '19
  • Tetracycline, UTI, Ceftriaxone

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