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Abacavir

Brand and Other Names: Abacavir
Mechanism of Action:

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.

Indications:

Indicated for HIV-1 infection in combination with other antiretroviral agents.

Route: oral
Dose:

600 mg daily: either 300 mg twice daily or 600 mg once daily.

Adverse Reactions:

Nausea, headache, fatigue, vomiting, and sleep disturbances.

Contraindication:

Positive for HLA-B*5701 allele.

Prior hypersensitivity reaction to abacavir.

Moderate or severe hepatic impairment.

Warnings and Precautions:

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.

See package insert for full prescribing information.