Abacavir
Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5′-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.
Indicated for HIV-1 infection in combination with other antiretroviral agents.
600 mg daily: either 300 mg twice daily or 600 mg once daily.
Nausea, headache, fatigue, vomiting, and sleep disturbances.
Positive for HLA-B*5701 allele.
Prior hypersensitivity reaction to abacavir.
Moderate or severe hepatic impairment.
Lactic acidosis and hepatomegaly with steatosis: Rare but potentially fatal.
Immune reconstitution syndrome: Can unmask latent infections.
Myocardial infarction (MI): Inconclusive evidence for increased risk; consider cardiovascular history when prescribing.