Steady state pharmacokinetics of hydrolysed bopindolol in young and elderly men.
Steady-state pharmacokinetic parameters of the new, long-acting beta-adrenoceptor blocker bopindolol have been measured in 17 young and 20 elderly healthy men. The t 1/2 beta and the AUC(0----24 h) of hydrolysed bopindolol (the active metabolite) were both increased (40% and 26%, respectively) in the elderly subjects but tmax, Cmax and CL/f were not altered. However, after adjusting the parameters to allow for the different average body weights of the two groups, Cmax and CL/f became significantly different (+29% and -30%, respectively). AUC(0----24 h) was increased by 41%. The changes of up to 41% in pharmacokinetic parameters were smaller than the alterations of 50-100% usually seen when titrating doses of antihypertensive drugs. The clinical relevance of the effects was not examined, but similar changes have been reported for other beta-blockers which did not appear to be clinically relevant and did not affect the dosage required to treat hypertension.
Holmes
D
D
Clinical Research Department, Sandoz Pharma Ltd., Basel, Switzerland.
Nuesch
E
E
Houle
J M
JM
Rosenthaler
J
J
D000293:Adolescent; D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics*; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000375:Aging / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D006868:Hydrolysis; D008297:Male; D008875:Middle Aged; D010869:Pindolol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D011869:Radioligand Assay
D000319:Adrenergic beta-Antagonists; D010869:Pindolol; C036007:bopindolol