Glyburide
Glyburide. Second-generation sulfonylurea — K-ATP channel closure → insulin release. Hepatically metabolized (CYP3A4); active M1 metabolite… Oral half-life 9.7 h.
Second-generation sulfonylurea — K-ATP channel closure → insulin release. Hepatically metabolized (CYP3A4); active M1 metabolite contributes to hypoglycemia in renal impairment. Beers-list problematic in elderly.
PK: half-life 9.7 h is verbatim but is the TERMINAL phase of a two-compartment fit — the same paper gives an initial phase of 3.3 h, so a one-compartment curve on 9.7 h overstates persistence. V 14 L matched nothing: both human intravenous determinations give 7.3-7.4 L (PMID:8576296 "7.44 +/- 1.53 litres" intravenously), and the larger 15.5 and 20.8 L figures in that same abstract belong to the METABOLITES M1 and M2, a wrong-analyte trap. F is re-cited to Neugebauer 1985 (PMID:3932228), the only true absolute determination, verbatim "an absolute bioavailability of 102% for HB 420" — formulation-specific, since the older form is 73% of it. ka 0.7 /h dropped, unstated anywhere.
Pharmacokinetics
- Oral — t½ 9.7 h · F 100% · Vd 7.44 L
Sources: PMID:24374443, PMID:3932228, PMID:8576296