ZIAGENCopy

• DRUGBANK - Abacavir
• indication:

  For the treatment of HIV-1 infection, in combination with other antiretroviral agents.

• pharmacology:

• mechanism:

  Abacavir is a carbocyclic synthetic nucleoside analogue. Intracellularly, abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP). Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.

• toxicity:

  Some myocardial degeneration has been noticed in rats and mice

• absorprion:

  Rapid and extensive after oral administration (83% bioavailability)

• halflife:

  1.54 ± 0.63 hours

• roouteelimination:

  Elimination of abacavir was quantified in a mass balance study following administration of a 600-mg dose of 14C-abacavir: 99% of the radioactivity was recovered, 1.2% was excreted in the urine as abacavir, 30% as the 5′-carboxylic acid metabolite, 36% as the 5′-glucuronide metabolite, and 15% as unidentified minor metabolites in the urine. Fecal elimination accounted for 16% of the dose. Fecal elimination accounted for 16% of the dose. Renal excretion of unchanged abacavir is a minor route of elimination in humans.

• volumedistribution:

  * 0.86 ± 0.15 L/kg

• clearance:

  * 0.80 +/- 0.24 L/hr/kg [asymptomatic, HIV-1-infected adult patients receiving single (IV dose of 150 mg]