Abacavir
Abacavir. NRTI — guanosine analog, phosphorylated to carbovir-TP, a chain-terminator for HIV reverse transcriptase. HLA-B*5701 carriers (~5% of… Oral half-life 1.5 h.
NRTI — guanosine analog, phosphorylated to carbovir-TP, a chain-terminator for HIV reverse transcriptase. HLA-B*5701 carriers (~5% of populations of European descent) develop life-threatening hypersensitivity → mandatory pre-treatment genotyping.
PK: half-life 1.5 h and F 0.83 are both verbatim and stand, and V 60 L is the review 0.86 L/kg scaled to 70 kg — measured after intravenous dosing, so a TRUE volume that pairs safely with a bioavailability. F is now cited to the primary that measured it (PMID:10453964, six HIV-infected men, oral versus a 60-minute intravenous infusion) rather than to the review quoting it. ka 1.5 /h dropped as a DIGIT COLLISION with the half-life; the cited paper only absorption figure is a peak at 0.63-1 hour. ANALYTE CAVEAT: 1.5 h is the PLASMA PARENT half-life, but the drug is dosed once daily on the strength of an intracellular carbovir-triphosphate half-life above 20 hours — right analyte for a plasma model, wrong one for an effect model.
Pharmacokinetics
- Oral — t½ 1.5 h · F 83% · Vd 60 L
Sources: PMID:18479171, PMID:10453964