Appendix D: Adult Dosing Guidelines for Selected Antiretroviral Drugs
| Drug | Adult dosing | Important side effects; comments |
|---|---|---|
| Nucleoside reverse transcriptase inhibitors (NRTIs) | ||
| Abacavir (ABC) | 300 mg 2x/day |
• Hypersensitivity in 2-5% of patients • Alcohol increases ABC levels by 40% |
| Didanosine (ddI) |
<60 kg, 125 mg 2x/day or 250 mg/day; 100 mg 2x/day if combined with TDF ≥60 kg, 200 mg 2x/day; 125 mg 2x/day if combined with TDF |
• Chills or fever, headache, nausea, vomiting, peripheral neuropathy, pancreatitis, lipodystrophy, weakness, abdominal pain, diarrhea, retinal changes, optic neuritis, fat redistribution/ accumulation, rash, lactic acidosis, severe hepatomegaly with steatosis • Take on empty stomach • Increased toxicity with d4T • Avoid during pregnancy • Alcohol increases risk of pancreatitis • Adjust dose with renal failure |
| Emtricitabine (FTC) | 200 mg/day |
• Generally well-tolerated • Headache, decreased appetite, nausea, vomiting, rash, lactic acidosis, hepatomegaly, skin hyperpigmentation • Related chemically to 3TC, but more potent |
| Lamivudine (3TC) | 150 mg 2x/day or 300 mg/day |
• Generally well-tolerated • Headache, decreased appetite, nausea, diarrhea, vomiting, lactic acidosis, hepatomegaly, pancreatitis (especially in children) |
| Stavudine (d4T) |
Immediate-release: <60 kg, 30 mg 2x/day; ≥60 kg, 40 mg 2x/day Extended-release: <60 kg, 75 mg/day; ≥60 kg, 100 mg/day |
• Peripheral neuropathy, lipodystrophy, lactic acidosis, hepatomegaly with steatosis, pancreatitis, hyperlipidemia • Fatal pancreatitis has been reported when used with ddI • Avoid during pregnancy • Do not use with AZT |
| Zidovudine (AZT) |
300 mg 2x/day Perinatal HIV transmission prevention: • For mother: 100 mg 5x/ day or 200 mg 3x/day or 300 mg 2x/day starting at the 14th week of gestation until labor, then 2 mg/kg IV over 1 hour followed by 1 mg/kg/hour IV until umbilical cord clamping • Alternative: 2 mg/kg IV over 1 hour followed by 1 mg/kg/hour until delivery + single-dose NVP 200 mg orally at onset of labor |
• Anemia, headache, insomnia, malaise, anorexia, constipation, nausea, vomiting, lactic acidosis, hepatomegaly with steatosis, leukopenia, myopathy, neuropathy • Do not use with d4T • See Protocol 2.4 for appropriate management of infants born to mothers treated with this regimen |
| Nucleotide reverse transcriptase inhibitor (NRTI) | ||
| Tenofovir (TDF) | 300 mg/day |
• Nephrotoxicity, including Fanconi syndrome • Take with food |
| Nonnucleoside reverse transcriptase inhibitors (NNRTIs) | ||
| Efavirenz (EFV) |
600 mg/day If used concurrently with R, 800 mg/day |
• Dizziness, agitation, vivid dreams, hepatitis, lipodystrophy, depression, hallucinations, impaired concentration, insomnia, somnolence, rash (very common, especially in children), hyperglycemia, hyperlipidemia and fat redistribution (less common) • Administer at bedtime without food (at least 2 hours after a meal) • Avoid during pregnancy. • Decreases effectiveness of oral contraceptives |
| Nevirapine (NVP) |
200 mg/day for 14 days, then 200 mg 2x/day Perinatal HIV transmission prevention: for women with no prior ART, single-dose NVP 200 mg orally at onset of labor, followed by 4 mg/kg administered to the newborn within 48-72 hours of birth |
• Headache, fatigue, diarrhea, nausea, rash (most common), fat redistribution (less common), hepatitis (generally within 12 weeks of initiation), hepatic failure (severe, life-threatening hepatotoxicity, some fatal cases), severe skin reactions (Stevens-Johnson syndrome) • Women with CD4 >250 cells/mm3, including pregnant women, are especially vulnerable for fatal hepatotoxicity |
| Protease inhibitors (PIs) | ||
| Amprenavir (APV) |
1200 mg 2x/day If with RTV: 600 mg 2x/day + 100 mg RTV 2x/day |
• Nausea, vomiting, diarrhea, rash, Stevens-Johnson syndrome, lipodystrophy • Avoid taking with high-fat meal • Decrease dose in liver failure to 300 mg • Decreases effectiveness of oral contraceptives • Avoid during pregnancy |
| Atazanavir (AZV) | 400 mg/day |
• Take with food |
| Indinavir (IDV) | 800 mg 3x/day |
• Abdominal pain, nausea, vomiting, asymptomatic hyperbilirubinemia, back pain, acute hemolytic anemia, hyperglycemia (including cases of new onset diabetes mellitus), hepatitis (rare), nephrolithiasis, lipodystrophy • Take with plenty of water to avoid nephrolithiasis • Take on empty stomach • If boosted with RTV 100 mg, can be dosed 800 mg 2x/day and taken with food |
| Lopinavir/ Ritonavir (LPV/ RTV) |
400/100 mg 2x/day 533/133 mg 2x/day when combined with EFV, APV, NFV, or NVP |
• Diarrhea, lipodystrophy, nausea • Refrigeration required • Take with food |
| Nelfinavir (NFV) | 1250 mg 2x/day |
• Secretory diarrhea, nausea, vomiting, lipodystrophy • Take with food |
| Ritonavir (RTV) | Start at 300 mg 2x/day and escalate to 600 mg 2x/day over 2 weeks |
• Hepatitis, lipodystrophy • Refrigeration required • Poorly tolerated when used alone at 600 mg 2x/day; best used to boost levels of other PIs |
Source: Bartlett JG, Gallant JE. Medical management of HIV infection. Baltimore, MD: Johns Hopkins University, 2005.
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