title: Pharmacokinetics of dilevalol in normotensive and hypertensive volunteers.
abstract: Dilevalol is a novel antihypertensive agent combining vasodilation due to selective beta 2-adrenergic receptor agonism with nonspecific antagonism of beta 1- and beta 2-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.
authors.affiliation: Department of Drug Metabolism, Schering-Plough Corporation, Bloomfield, New Jersey 07003.
authors.forename: W G
authors.initials: WG
authors.lastname: Kramer
authors.forename: G
authors.initials: G
authors.lastname: Perentesis
authors.forename: M B
authors.initials: MB
authors.lastname: Affrime
authors.forename: J E
authors.initials: JE
authors.lastname: Patrick
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D004334:Drug Administration Schedule; D005215:Fasting; D005502:Food; D006207:Half-Life; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism; D007262:Infusions, Intravenous; D007741:Labetalol / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011897:Random Allocation
chemical_list: D007741:Labetalol