The effects of a single dose of dilevalol on [3H]-noradrenaline plasma kinetics and plasma lipoprotein cholesterol concentrations.
1. A single oral dose of dilevalol (200 mg or 400 mg) or placebo was administered to 15 normal male volunteers in a double-blind, random order crossover study. 2. Dilevalol had no significant effect on supine blood pressures or heart rates, but caused a significant fall in systolic blood pressure 1 and 30 min following standing, and attenuated the rise in diastolic blood pressure and heart rate that accompanies standing. 3. Dilevalol caused a dose dependent increase in plasma noradrenaline levels from arterialized blood which was due to an increase in noradrenaline spillover with no change in clearance. 4. Dilevalol increased plasma levels of the noradrenaline metabolite 3,4-dihydroxyphenylethylene glycol (DHPG) (which is formed in sympathetic nerves following neuronal uptake of noradrenaline), indicating that the increase in noradrenaline spillover was not due to the blockade of neuronal uptake. 5. Acute dilevalol administration had no effect on total plasma cholesterol, HDL-cholesterol or LDL-cholesterol levels.
Howes
L G
LG
Department of Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Victoria, Australia.
Rowe
P R
PR
Krum
H
H
Louis
W J
WJ
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D002784:Cholesterol / Q000097:blood*; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007741:Labetalol / Q000494:pharmacology*; D008297:Male; D008734:Methoxyhydroxyphenylglycol / Q000031:analogs & derivatives / Q000097:blood; D009638:Norepinephrine / Q000097:blood / Q000493:pharmacokinetics*
D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D008734:Methoxyhydroxyphenylglycol; D002784:Cholesterol; D007741:Labetalol; C010117:3,4-dihydroxyphenylglycol; D009638:Norepinephrine