Pharmacokinetics of the enantiomers of tertatolol in the rat after oral and intravenous administration.
1. Plasma concentrations of the two enantiomers of tertatolol were determined by gc/ms. Deuterium labelling of one of the tertatolol enantiomers was used for chiral discrimination. 2. No isotope effects were observed following simultaneous oral administration of tertatolol and [2H9]tertatolol. 3. After intravenous administration of the pseudoracemate or of each enantiomer separately, (+)-tertatolol showed a lower total clearance and volume of distribution, compared to the (-) enantiomer. 4. After oral administration of the pseudoracemate or of each enantiomer separately, no substantial difference in bioavailability were observed between the enantiomers.
Département de Chimie Thérapeutique, Faculté de Pharmacie, Illkirch-Graffenstaden, France.
T
T
Lave
C
C
Efthymiopoulos
B
B
Van Overloop
A
A
Gairard
O
O
Crambes
J C
JC
Koffel
L
L
Jung
D000284:Administration, Oral; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D008401:Gas Chromatography-Mass Spectrometry; D007275:Injections, Intravenous; D008297:Male; D011412:Propanolamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013876:Thiophenes
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D013876:Thiophenes; C005632:tertatolol