Pharmacokinetics of a valpromide isomer,valnoctamide, in healthy subjects |
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Authors: | M. Bialer A. Haj-Yehia N. Barzaghi F. Pisani E. Perucca |
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Affiliation: | (1) Department of Pharmacy, School of Pharmacy, Hebrew University, Jerusalem, Israel;(2) Institute of Medical Pharmacology, University of Pavia, Pavia, Italy;(3) Department of Neurology, University of Messina, Messina, Italy |
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Abstract: | Summary The pharmacokinetics of a single 400 mg oral dose of valnoctamide (VCD) has been investigated in seven healthy, adult, male volunteers. VCD was not biotransformed rapidly to its corresponding acid valnoctic acid (VCA), unlike its isomer valpromide (VPD). It had a mean residence time of 13.2 h and a terminal half-life of 9.3 h. Throughout the study, only low plasma levels of VCA could be detected. Thus, unlike VPD, which is a prodrug of the corresponding acid, (valproic acid, VPA). VCD appears to act as a drug in its own right, and it does not undergo similar hydrolysis. The pharmacokinetic difference may account for the different pharmacological activities of the two isomers. |
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Keywords: | valnoctamide valpromide valproic acid pharmacokinetics healthy subjects tranquiliser |
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