Antiretroviral Agents in HIV-1 (trial)

9 Continued on next page Table 5A. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs) Drug Formulation Dosing Recommendations Elimination Serum/Intracellular Half-lives Adverse Events Abacavir (ABC) Ziagen ® 300 mg tablets or 20 mg/mL oral solution 300 mg bid or 600 mg once daily ▶ Take without regard to meals ▶ Metabolized by alcohol dehydrogenase and glucuronyl transferase ▶ Renal excretion of metabolites 82% ▶ Dosage adjustment for ABC is recommended in patients with hepatic insufficiency 1.5 h/12–26 h ▶ 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 Also available in: ABC/ZDV/3TC Trizivir ® ABC 300 mg + ZDV 300 mg + 3TC 150 mg One tablet bid ABC/3TC Epzicom ® ABC 600 mg + 3TC 300 mg One tablet once daily Didanosine (ddI) Videx EC ® Generic ddI EC Videx EC ® 125, 200, 250, 400 mg capsules ▶ Buffered tablets (non-EC) no longer available Videx ® 10 mg/mL oral solution Body weight ≥60 kg: 400 mg once daily a ▶ With TDF, 250 mg once daily Body weight <60 kg: 250 mg once daily a ▶ With TDF, 200 mg once daily ▶ Take 1/2 hour before or 2 hours aer a meal a Preferred dosing with oral solution is bid (total daily dose divided into 2 doses) ▶ Renal excretion 50% ▶ Dosage adjustment in renal insufficiency recommended 1.5 h/>20 h ▶ 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 Emtricitabine (FTC) Emtriva ® 200 mg hard gelatin capsule or 10 mg/mL oral solution 200 mg capsule once daily or 240 mg (24 mL) oral solution once daily ▶ Take without regard to meals ▶ Renal excretion 86% ▶ Dosage adjustment in renal insufficiency recommended 10 h/>20 h ▶ Minimal toxicity ▶ Hyperpigmentation/skin discoloration ▶ Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue FTC 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

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