| Autor: |
Hallén, Bengt, Gabrielsson, Johan, Palmér, Lena, Ekström, Björn |
| Zdroj: |
Pharmacology & Toxicology; 1993, Vol. 73 Issue 3, p153-158, 6p |
| Abstrakt: |
(+)-Terodiline was given orally (25 mg) and intravenously (12.5 mg) to eight healthy volunteers. The pharmacokinetics of (+)-terodiline could be described by a one compartment model. The lag time of absorption was 0.6 ± 0.5 hr (mean ± S.D.), the absorption half-life 0.9 ± 0.5 hr, the time to maximum serum concentration 5.6 ± 2.2 hr and the corresponding maximum serum concentration 62 ± 22 μg/1. The volume of distribution was found to be 372 ± 84 1, the systemic clearance 86 ± 29 ml/min., the mean residence time 81 ± 38 hr and the observed terminal half-life of elimination 56 ± 26 hr. The urinary excretion of the intravenous dose was 12 ± 6% and the renal clearance 10 ± 5 ml/min. The bioavailability of (+)-terodiline was 93 ± 19%. The present results indicate that (+)-terodiline as well as the racemate can be characterized as low clearance long half-life drugs. One subject was a poor hydroxylator of debrisoquine and exhibited a 3-fold decrease in clearance and increase in half-life of (+)-terodiline relative to extensive metabolizers. Observed pharmacological effects were mild accomodation disturbances and dry mouth, i.e. the same effects as those that may be seen at a corresponding dose of terodiline given as a racemic mixture. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
Plný text