Stereoselective disposition of talinolol in man

The disposition of the β‐blocking drug talinolol is controlled by P‐glycoprotein in man. Because talinolol is marketed as a racemate, we reevaluated the serum‐concentration time profiles of talinolol of a previously published study with single intravenous (30 mg) and repeated oral talinolol (100 mg...

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Published in:Journal of pharmaceutical sciences 2002-02, Vol.91 (2), p.303-311
Main Authors: Zschiesche, Michael, Lemma, Girum Lakew, Klebingat, Klaus‐Jürgen, Franke, Gerd, Terhaag, Bernd, Hoffmann, Anna, Gramatté, Thomas, Kroemer, Heyo K., Siegmund, Werner
Format: Article
Language:English
Subjects:
Adrenergic beta-Antagonists - blood
Adrenergic beta-Antagonists - chemistry
Adrenergic beta-Antagonists - pharmacokinetics
Adult
Antihypertensive agents
Area Under Curve
ATP Binding Cassette Transporter, Subfamily B, Member 1 - biosynthesis
Biological and medical sciences
Cardiovascular system
Drug Interactions
Enzyme Inhibitors - pharmacokinetics
Humans
Male
man
Medical sciences
Microsomes, Liver - metabolism
Molecular Conformation
P-glycoprotein
Pharmacology. Drug treatments
Propanolamines - blood
Propanolamines - chemistry
Propanolamines - pharmacokinetics
racemate
Rifampin - pharmacokinetics
Statistics, Nonparametric
talinolol
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Summary:The disposition of the β‐blocking drug talinolol is controlled by P‐glycoprotein in man. Because talinolol is marketed as a racemate, we reevaluated the serum‐concentration time profiles of talinolol of a previously published study with single intravenous (30 mg) and repeated oral talinolol (100 mg for 14 days) before and after comedication of rifampicin (600 mg per day for 9 days) in eight male healthy volunteers (age 22–26 years, body weight 67–84 kg) with respect to differences in the kinetic profiles of the two enantiomers S(−) talinolol and R(+) talinolol. Additionally, the metabolism of talinolol in human liver microsomes was examined. After oral administration, S(−) talinolol was slightly less absorbed and faster eliminated than R(+) talinolol. The absolute bioavailabilty of the R(+) enantiomer of talinolol was slightly but significantly higher than of its S(−) enantiomer. Coadministration of rifampicin further intensified this difference in the disposition of R(+) and S(−) talinolol (p 
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.10054