ABACAVIR

Antiviral Activity

Used in the treatment of HIV-1 infection in combination with at least two additional antiretroviral agents
Active against susceptible HIV strains

Pregnancy Risk Factor

Category C

Contraindication/Precaution

Hypersensitivity to abacavir or any component
HIV-infected mothers should not breast-feed in order to avoid transmission to a non-infected newborn
Use caution in the presence of impaired liver function
The safety and effectiveness of abacavir sulfate have not been established in pediatric patients <3 years old. Mechanism of Action Carbocyclic synthetic nucleoside analogue, intracellularly converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP) Inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA Prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Pharmacodynamics/Kinetics Metabolism:  Liver, (not significantly metabolized by cytochrome P450) Half-life:  1.5 h Elimination:  excreted in urine and some in feces  Dosage Children:  >3 years old:
8 mg/kg PO bid (ad maximum of 300 mg PO dib)

Adults:  

300 mg PO bid

Dosage In Renal Failure

Cr. clearance (ml/min):
none
Dialysis
Hemo: N/A
CAPD:  N/A