Antiretroviral Agents in HIV-1 (2014)

DHHS Adult HIV 2014

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17 Elimination Serum/ Intracellular Half-Lives Adverse Events b • Metabolized by alcohol dehydrogenase and glucuronyl transferase • Renal excretion of metabolites: 82% • Dosage adjustment for ABC is recommended in patients with hepatic insufficiency (Table 4). 1.5 hours/12-26 hours • Hypersensitivity reaction (HSR): Patients who test positive for HLA-B*5701 are at highest risk. HLA screening should be done before initiation of ABC. Do not rechallenge after possible HSR. • Symptoms of HSR may include fever, rash, nausea, vomiting, diarrhea, abdominal pain, malaise, or fatigue or respiratory symptoms such as sore throat, cough, or shortness of breath. • Some cohort studies suggest increased risk of MI with recent or current use of ABC, but this risk has not been observed in all. • Renal excretion: 86% • Dosage adjustment in patients with renal insufficiency is recommended (Table 4). 10 hours/ >20 hours • Minimal toxicity • Hyperpigmentation/skin discoloration • Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue FTC. • Renal excretion: 70% Dosage adjustment in patients with renal insufficiency is recommended (Table 4). 5-7 hours/18-22 hours • Minimal toxicity • Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue 3TC. • Renal excretion - primary route of elimination • Dosage adjustment in patients with renal insufficiency is recommended (Table 4). 17 hours/ >60 hours • Renal insufficiency, Fanconi syndrome, proximal tubulopathy • Osteomalacia, decrease in bone mineral density • Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue TDF. • Asthenia, headache, diarrhea, nausea, vomiting, and flatulence

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