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Table 309-21. Antiretroviral Drugs Used in the Treatment of HIV Infection

Drug Status IndicationDose asMonotherapy

Dose inCombination Supporting Data Toxicity

REVERSE TRANSCRIPTASE INHIBITORSZidovudine (AZT,

azidothymidine, Retrovir,

3 azido-3 -deoxythymidine)

Licensed Treatment of HIVinfection whenantiretroviraltherapy isindicated

Not indicated 200 mg q8h or 300mg bid

19 vs 1 death in original placebo-controlled trial in 281 patients withAIDS or ARC. Decreasedprogression to AIDS in patients with

CD4+ T cell counts

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increased by a mean of 22/LLamivudine

(Epivir, 2 3 -dideoxy-3 -thiacytidine,3TC)

Licensed In combination withother antiretroviralagents for thetreatment of HIVinfection

Not indicated 150 mg bid Superior to AZT alone with respect tochanges in CD4 counts in 495patients who were zidovudine-naiveand 477 patients who werezidovudine-experienced. OverallCD4+ T cell counts for thezidovudine group were at baselineby 24 wk, while in the group treatedwith zidovudine plus lamivudine,

they were 10-50 cells/L abovebaseline. 54% decrease inprogression to AIDS/deathcompared to AZT alone

Abacavir(Ziagen)

Licensed For treatment of HIVinfection incombination withother antiretroviralagents

Not indicated 300 mg bid Abacavir + AZT + 3TC equivalent toindinavir + AZT + 3TC with regard toviral load suppression (~60% in

each group with

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warranted AIDS-defining event or death incombination with ddC compared toeither agent alone

abnormalities

(Fortovase softgel capsule)

Licensed For use incombination withother antiretroviralagents whentreatment iswarranted

Not indicated 1200 mg tid Reduction in the mortality rate andAIDS-defining events for patientswho received hard-gel formulationin combination with ddC

Diarrhea, nausea,abdominal pain,headaches,hyperglycemia, fatredistribution, lipidabnormalities

Ritonavir (Norvir) Licensed In combination withnucleosideanalogues fortreatment of HIVinfection whentreatment iswarranted

Not indicated 600 mg bid Reduction in the cumulative incidenceof clinical progression or death from34 to 17% in patients with CD4+ T

cell count

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(79% vs 64% with