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Pharmacokinetics of dilevalol in normotensive and hypertensive volunteers

1989; Elsevier BV; Volume: 63; Issue: 19 Linguagem: Inglês

10.1016/0002-9149(89)90121-5

1879-1913

William G. Kramer, George Perentesis, Melton B. Affrime, James E. Patrick,

Analytical Methods in Pharmaceuticals

Dilevalol is a novel antihypertensive agent combining vasodilation due to selective β2-adrenergic receptor agonism with nonspecific antagonism of β1-and β2-adrenergic receptors. Studies of dilevalol's pharmacokinetics in normotensive and hypertensive volunteers have demonstrated that (1) it is rapidly and well absorbed; (2) because of extensive first-pass metabolism its absolute oral bioavailability is about 12%; (3) its mean elimination half-life is 8 to 12 hours after administration of single oral or intravenous doses to normal volunteers, a value consistent with once-daily dosing; and (4) food does not appear to alter its bioavailability or pharmacokinetics.