Pharmacokinetics and Bioavailability of Pinacidil Capsules in Human Volunteers

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Abstract
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 (t½ and volume of distribution (Vd) of pinacidil were 204 ± 0·40 h and 1·4 ± 0·4 l/kg respectively, while the elimination rate constant (k el) was 0·34 ± 0·07 h1 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.