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.