AgentsPreferred dosingDosage formsAdvantagesDisadvantages
Basic regimens (preferred)
Zidovudine (Retrovir) plus lamivudine (Epivir)Zidovudine: 300 mg twice daily or 200 mg three times daily, with foodZidovudine: 100-mg capsules and 300-mg tabletsZidovudine associated with decreased risk of HIV transmission; serious toxicity is rare when used for postexposure prophylaxis; side effects are predictable and manageable with antimotility and antiemetic agents; can be used during pregnancy; can be given as a single tablet twice daily.Side effects are common (especially nausea and fatigue) and may result in low adherence; potential source virus resistance; potential for delayed toxicity unknown.
Lamivudine: 300 mg daily or 150 mg twice dailyLamivudine: 150- and 300-mg tablets
Combination therapy available(Combivir)Combivir: one tablet twice dailyCombivir: tablets containing 300 mg zidovudine and 150 mg lamivudine
Zidovudine plus emtricitabine (Emtriva)Zidovudine: 300 mg twice daily or 200 mg three times daily, with foodZidovudine: see aboveZidovudine: see aboveZidovudine: see above
Emtricitabine: 200 mg dailyEmtricitabine: 200-mg capsulesEmtricitabine: once-daily dosing; well tolerated; long intracellular half-life (40 hours); tolerability and virologic response rates appear better than regimens containing didanosine (Videx) plus stavudine (Zerit).Emtricitabine: rash may be more common than with lamivudine; cross-resistance with lamivudine; hyperpigmentation possible with long-term use in nonwhites.
Tenofovir (Viread) plus lamivudineTenofovir: 300 mg daily*Tenofovir: 300-mg tabletsTenofovir: once-daily dosing; resistance profile activity against certain thymidine analogue mutations; well toleratedTenofovir: same class warnings as nucleoside reverse transcriptase inhibitors; drug interactions; increased drug concentrations in persons taking atazanavir (Reyataz) and lopinavir/ritonavir (Kaletra); must monitor patients for toxicity.
Lamivudine: 300 mg daily or 150 mg twice dailyLamivudine: see aboveLamivudine: see above
Tenofovir plus emtricitabineTenofovir: 300 mg daily*Tenofovir: see aboveTenofovir: see aboveTenofovir: see above
Emtricitabine: 200 mg dailyEmtricitabine: see aboveEmtricitabine: see aboveEmtricitabine: see above
Combination therapy available (Truvada)Truvada: one tablet daily*Truvada: tablets containing 300 mg tenofovir and 200 mg emtricitabine
Basic regimens (alternate)
Lamivudine plus stavudineLamivudine: 300 mg daily or 150 mg twice dailyLamivudine: see aboveLamivudine: see abovePotential source virus resistance; potential for delayed toxicity unknown.
Stavudine: 40 mg twice daily†; 30 mg twice daily in patients weighing less than 60 kg (132 lb)Stavudine: 15-, 20-, 30-, and 40-mg tabletsStavudine: GI side effects are rare
Emtricitabine plus stavudineEmtricitabine: 200 mg dailyEmtricitabine: see aboveEmtricitabine: see abovePotential source virus resistance; potential for delayed toxicity unknown.
Stavudine: 40 mg twice daily†; 30 mg twice daily in patients weighing less than 60 kgStavudine: see aboveStavudine: see above
Lamivudine plus didanosineLamivudine: 300 mg daily or 150 mg twice dailyLamivudine: see aboveLamivudine: see aboveDiarrhea more common with buffered preparation; associated with toxicity (i.e., peripheral neuropathy, pancreatitis, and lactic acidosis); must be taken on an empty stomach except when taken with tenofovir; drug interactions.
Didanosine: 400 mg daily or 200 mg twice daily‡; 125 mg twice daily or 250 mg daily in patients weighing less than 60 kgDidanosine: 25-, 50-, 100-, 150-, and 200-mg buffered tabletsDidanosine: once daily dosing
Emtricitabine plus didanosineEmtricitabine: 200 mg dailyEmtricitabine: see aboveEmtricitabine: see aboveEmtricitabine: see above
Didanosine: 400 mg daily or 200 mg twice daily‡; 125 mg twice daily or 250 mg daily in patients weighing less than 60 kgDidanosine: see aboveDidanosine: see aboveDidanosine: see above
Expanded regimen (preferred)
Basic regimen plus lopinavir/ritonavirThree capsules twice dailyCapsules containing 133 mg lopinavir and 33 mg ritonavirPotent HIV protease inhibitor; generally well toleratedPotential for serious or life-threatening drug interactions; may accelerate clearance of certain drugs, including OCPs (requiring additional or alternate contraceptive methods); may cause severe hyperlipidemia, especially hypertriglyceridemia; GI side effects common.
Expanded regimens (alternate)
Basic regimen plus one of the following drugs:
Atazanavir with or without ritonavir (Norvir)Atazanavir alone: 400 mg daily*Atazanavir: 100-, 150-, and 200-mg capsulesPotent HIV protease inhibitor; once-daily dosing; generally well toleratedHyperbilirubinemia and jaundice common; potential for serious or life- threatening drug interactions; must avoid coadministration with proton pump inhibitors; administration of antacids and buffered medications must be separated by two hours and histamine H2 antagonists by 12 hours to avoid decreasing atazanavir levels; caution must be used with products known to cause PR prolongation (e.g., diltiazem [Cardizem]).
Ritonavir: 100-mg capsules
Fosamprenavir (Lexiva) with or without ritonavirFosamprenavir alone: 1,400 mg twice dailyFosamprenavir: 700-mg capsulesOnce-daily dosing when taken with ritonavirGI side effects common; multiple drug interactions; OCPs decrease fosamprenavir concentrations; incidence of rash in healthy volunteers, especially when used with low doses of ritonavir; differentiating between early drug-associated rash and acute seroconversion may be difficult.
With ritonavir: 1,400 mg fosamprenavir daily plus 200 mg ritonavir daily, or 700 mg fosamprenavir twice daily plus 100 mg ritonavir twice dailyRitonavir: see above
Indinavir (Crixivan) with or without ritonavirIndinavir: 800 mg twice dailyIndinavir: 200-, 333-, and 400-mg capsulesPotent HIV inhibitorPotential for serious or life-threatening drug interactions; serious toxicity possible; consumption of eight glasses of water daily is required; hyperbilirubinemia is common; requires acid for absorption and cannot be taken simultaneously with didanosine.
Ritonavir: 100 mg twice dailyRitonavir: see above
Saquinavir (Invirase) plus ritonavirSaquinavir: 1,000 mg twice dailySaquinavir: 200-mg capsulesGenerally well tolerated, although GI events are common.Potential for serious or life-threatening drug interactions; substantial pill burden
Ritonavir: 100 mg twice dailyRitonavir: see above
Nelfinavir (Viracept)1,250 mg twice daily with meals250- and 625-mg tabletsGenerally well toleratedDiarrhea and other GI side effects common; potential for serious or life-threatening drug interactions; substantial pill burden
Efavirenz (Sustiva)600 mg daily at bedtime50-, 100-, and 200-mg capsules and 600-mg tabletsOnce-daily dosing; does not require phosphorylation before activation; may be active earlier than other agentsAssociated with rash that may progress to Stevens-Johnson syndrome; differentiating between early drug-associated rash and acute seroconversion can be difficult; CNS side effects; teratogenic; potential for serious or life-threatening drug interactions.