Pharmacokinetics and pharmacodynamics of a new transdermal delivery system for bopindolol.
1. In two separate studies, each with 12 healthy male volunteers, the pharmacokinetic and dynamic properties of a transdermal delivery system for bopindolol were evaluated. 2. In study I it was shown that bopindolol absorption from a 14 mg patch occurred over the whole 7-day application period. No signs of a significant skin depot were found. 3. In study II, a linear pharmacokinetic behaviour but a non-linear kinetic/dynamic relationship was established for the patches over a dose range from 7 to 21 mg. Comparable peak effects of reduction in exercise-induced tachycardia were observed after different patch doses and an i.v. injection. However, the effect was significantly prolonged with the patches compared with the injection and was maintained over 7 days. 4. The patches showed a good local and systemic tolerability in both studies over a dosing interval of up to 7 days.
Department of Anaesthesia, University of Basel/Kantonsspital, Switzerland.
J
J
Drewe
R
R
Meier
U
U
Timonen
M
M
Thumshirn
J
J
Munzer
T
T
Kissel
K
K
Gyr
D000279:Administration, Cutaneous; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D000328:Adult; D000704:Analysis of Variance; D005080:Exercise Test; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D010869:Pindolol / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D011897:Random Allocation; D012016:Reference Values
D000319:Adrenergic beta-Antagonists; D010869:Pindolol; C036007:bopindolol