Pharmacokinetics and bioavailability of pinacidil capsules in human volunteers.
Pinacidil is a new and potent vasodilator, which has recently been used in the treatment of various forms of hypertension. In this study pharmacokinetic parameters were determined following administration of intravenous (0.2 mg/kg) and capsule (12.5 mg) formulations of pinacidil to twelve healthy volunteers. The serum half-life (t1/2) and volume of distribution (Vd) of pinacidil were 2.04 +/- 0.40 h and 1.4 +/- 0.4 l/kg respectively, while the elimination rate constant (k el) was 0.34 +/- 0.07 h-1. The mean bioavailability of pinacidil (capsule formulation) was 57% +/- 16 S.D. Mild side-effects such as dizziness, headache and fatigue were noted in two volunteers following intravenous administration of pinacidil, while no side-effects were reported with the oral formulation.
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D002214:Capsules; D005260:Female; D006146:Guanidines / Q000008:administration & dosage / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D020110:Pinacidil; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000378:metabolism*
D002214:Capsules; D006146:Guanidines; D014665:Vasodilator Agents; D020110:Pinacidil