Antiretroviral Agents in HIV-1

Antiretroviral Agents in HIV

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Elimination ▶ Renal excretion 70% ▶ Dosage adjustment in renal insufficiency recommended Serum/Intracellular Half-lives 5-7 hrs/18-22 hrs Adverse Events ▶ Minimal toxicity ▶ Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue 3TC ▶ Renal excretion 50% ▶ Dosage adjustment in renal insufficiency recommended 1.0 hr/7.5 hrs ▶ Peripheral neuropathy ▶ Lipoatrophy ▶ Pancreatitis ▶ Lactic acidosis with hepatic steatosis (rare but potentially life-threatening toxicity) ▶ Hyperlipidemia ▶ Rapidly progressive ascending neuromuscular weakness (rare) ▶ Renal excretion ▶ Dosage adjustment in renal insufficiency recommended 17 hrs/> 60 hrs ▶ Asthenia, headache, diarrhea, nausea, vomiting, and flatulence ▶ Renal insufficiency, Fanconi syndrome ▶ Osteomalacia ▶ Potential for decrease in bone mineral density ▶ Severe acute exacerbation of hepatitis may occur in HBV- coinfected patients who discontinue TDF ▶ Metabolized to AZT glucuronide (GAZT) 1.1 hrs/7 hrs ▶ Renal excretion of GAZT ▶ Dosage adjustment in renal insufficiency recommended ▶ Bone marrow suppression: macrocytic anemia or neutropenia ▶ Gastrointestinal intolerance, headache, insomnia, asthenia ▶ Nail pigmentation ▶ Lactic acidosis with hepatic steatosis (rare but potentially life-threatening toxicity) 11

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