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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 |
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Main Authors: | , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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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 |
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ISSN: | 0022-3549 1520-6017 |
DOI: | 10.1002/jps.10054 |