Antiretroviral Agents in HIV-1 (trial)

10 Selecting a Treatment Regimen Table 5A. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs) (cont'd) Drug Formulation Dosing Recommendations Elimination Serum/Intracellular Half-lives Adverse Events Lamivudine (3TC) Epivir ® 150, 300 mg tablets or 10 mg/mL oral solution 150 mg bid or 300 mg once daily ▶ Take without regard to meals ▶ Renal excretion 70% ▶ Dosage adjustment in renal insufficiency recommended 5–7 h/18–22 h ▶ Minimal toxicity ▶ Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue 3TC Also available in: 3TC/ZDV Combivir ® 3TC 150 mg + ZDV 300 mg One tablet bid 3TC/ABC Epzicom ® 3TC 300 mg + ABC 600 mg One tablet once daily 3TC/ZDV/ABC Trizivir ® 3TC 150 mg + ZDV 300 mg + ABC 300 mg One tablet bid Stavudine (d4T) Zerit ® Generic 15, 20, 30, 40 mg capsules or 1 mg/mL oral solution Body weight ≥60 kg: 40 mg bid Body weight <60 kg: 30 mg bid b ▶ Take without regard to meals b WHO recommends 30 mg bid dosing regardless of body weight. ▶ Renal excretion 50% ▶ Dosage adjustment in renal insufficiency recommended 1.0 h/7.5 h ▶ Peripheral neuropathy ▶ Lipoatrophy ▶ Pancreatitis ▶ Lactic acidosis with hepatic steatosis (rare but potentially life-threatening toxicity) ▶ Hyperlipidemia ▶ Rapidly progressive ascending neuromuscular weakness (rare) Tenofovir disoproxil fumarate (TDF) Viread ® 150, 200, 250, 300 mg tablets or 40 mg/1 g oral powder Adults: 300 mg once daily Children ≥2 years: ≥17 kg: tablets based on body weight or oral powder a 8 mg/kg once daily. Max: 300 mg/d <17 kg: oral powder a 8 mg/kg once daily. Max: 300 mg/d ▶ Renal excretion ▶ Dosage adjustment in renal insufficiency recommended 17 h/>60 h ▶ 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 Also available in: FTC/TDF/EFV Atripla ® FTC 200 mg + TDF 300 mg + EFV 600 mg One tablet at or before bedtime ▶ Take on an empty stomach to reduce side effects FTC/TDF/RPV Complera ® FTC 200 mg + TDF 300 mg + RPV 25 mg One tablet once daily with meal FTC/TDF Truvada ® FTC 200 mg + TDF 300 mg One tablet once daily FTC/TDF/EVG/ COBI Stribild ® FTC 200 mg + TDF 300 mg + EVG 150 mg + COBI 150 mg One tablet once daily with food Zidovudine (AZT, ZDV) Retrovir ® Generic 100 mg capsules, 300 mg tablets, 10 mg/mL intravenous solution, 10 mg/mL oral solution 300 mg bid or 200 mg tid ▶ Take without regard to meals ▶ Metabolized to AZT glucuronide (GAZT) ▶ Renal excretion of GAZT ▶ Dosage adjustment in renal insufficiency recommended 1.1 h/7 h ▶ 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) Also available in: 3TC/ ZDV Combivir ® 3TC 150 mg + ZVD 300 mg One tablet bid 3TC/ABC/ZDV Trizivir ® 3TC 150 mg + ABC 300 mg + ZDV 300 mg One tablet bid a See full prescribing information for dosing by body weight. Oral powder should be taken with food.

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