title: Pharmacokinetics and bioavailability of dilevalol in normotensive volunteers.
abstract: The bioavailability and pharmacokinetics of dilevalol following oral and intravenous administration were investigated in 12 healthy male volunteers. Dilevalol HCl was administered as a 200-mg oral tablet and a 50-mg intravenous infusion using a randomized cross-over design. Blood and urine samples were collected over 60 hours and analyzed for unchanged and total (unchanged plus Glusulase-released) dilevalol using a high performance liquid chromatography (HPLC) assay. After intravenous administration, total body clearance and volume of distribution of unchanged dilevalol were determined to be 23.2 mL/min/kg and 24.6 L/kg, respectively. After oral administration, a mean maximum concentration of 62 ng/mL was reached at an average peak time of 1.4 hours. Drug was eliminated with a half-life of 8.3 hours after oral administration and 12 hours after intravenous administration. Based on plasma levels and urinary excretion of total dilevalol, the drug was completely absorbed; however, due to first-pass metabolism, the absolute bioavailability of unchanged drug was 11 to 14%.
authors.affiliation: Department of Drug Metabolism/Pharmacokinetics, Schering Research, Bloomfield, New Jersey 07003.
authors.forename: W G
authors.initials: WG
authors.lastname: Kramer
authors.forename: N
authors.initials: N
authors.lastname: Nagabhushan
authors.forename: M B
authors.initials: MB
authors.lastname: Affrime
authors.forename: G P
authors.initials: GP
authors.lastname: Perentesis
authors.forename: S
authors.initials: S
authors.lastname: Symchowicz
authors.forename: J E
authors.initials: JE
authors.lastname: Patrick
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D007741:Labetalol / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male
chemical_list: D007741:Labetalol