Antiretroviral Agents in HIV-1

Antiretroviral Agents in HIV

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Elimination ▶ Metabolized by alcohol dehydrogenase and glucuronyl transferase ▶ Renal excretion of metabolites 82% ▶ Dosage adjustment for ABC is recommended in patients with hepatic insufficiency Serum/Intracellular Half-lives 1.5 hrs/12-26 hrs Adverse Events ▶ Hypersensitivity reaction symptoms may include fever, rash, nausea, vomiting, 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 is not substantiated in other studies ▶ Renal excretion 50% ▶ Dosage adjustment in renal insufficiency recommended 1.5 hrs/> 20 hrs ▶ Pancreatitis ▶ Peripheral neuropathy ▶ Lactic acidosis with hepatic steatosis (rare but potentially life-threatening toxicity) ▶ Potential association with noncirrhotic portal hypertension, some cases presented with esophageal varices ▶ One cohort study suggested increased risk of MI with recent or current use of ddI, but this risk is not substantiated in other studies ▶ Renal excretion 86% ▶ Dosage adjustment in renal insufficiency recommended 10 hrs/> 20 hrs ▶ Minimal toxicity ▶ Hyperpigmentation/skin discoloration ▶ Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue FTC Continued on next page. 9

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