Literature DB >> 2111246

Pharmacokinetics of a valpromide isomer, valnoctamide, in healthy subjects.

M Bialer1, A Haj-Yehia, N Barzaghi, F Pisani, E Perucca.   

Abstract

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 pro-drug 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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Year:  1990        PMID: 2111246     DOI: 10.1007/bf00315032

Source DB:  PubMed          Journal:  Eur J Clin Pharmacol        ISSN: 0031-6970            Impact factor:   2.953


  10 in total

1.  Commentary: a physiological approach to hepatic drug clearance.

Authors:  G R Wilkinson; D G Shand
Journal:  Clin Pharmacol Ther       Date:  1975-10       Impact factor: 6.875

2.  A clinical study in the use of valmethamide, an anxiety-reducing drug.

Authors:  W STEPANSKY
Journal:  Curr Ther Res Clin Exp       Date:  1960-05

3.  Rapid gas chromatographic assay for monitoring valnoctamide in plasma.

Authors:  M Bialer; B Hoch
Journal:  J Chromatogr       Date:  1985-02-08

4.  Variability in level-dose ratio of valproate: monotherapy versus polytherapy.

Authors:  R H Levy
Journal:  Epilepsia       Date:  1984       Impact factor: 5.864

5.  Structure-pharmacokinetic relationships in a series of valpromide derivatives with antiepileptic activity.

Authors:  A Haj-Yehia; M Bialer
Journal:  Pharm Res       Date:  1989-08       Impact factor: 4.200

6.  [Use of valpromide in psychiatric therapeutics].

Authors:  P A Lambert; G Venaud
Journal:  Encephale       Date:  1987 Nov-Dec       Impact factor: 1.291

7.  Dipropylacetic acid plasma levels; diurnal fluctuations during chronic treatment with dipropylacetamide.

Authors:  F Pisani; A Fazio; G Oteri; R Di Perri
Journal:  Ther Drug Monit       Date:  1981       Impact factor: 3.681

8.  Pharmacokinetics of valpromide after oral administration of a solution and a tablet to healthy volunteers.

Authors:  M Bialer; A Rubinstein; I Raz; O Abramsky
Journal:  Eur J Clin Pharmacol       Date:  1984       Impact factor: 2.953

9.  Pharmacokinetics of a valpromide isomer, valnoctamide, in dogs.

Authors:  A Haj-Yehia; M Bialer
Journal:  J Pharm Sci       Date:  1988-10       Impact factor: 3.534

10.  Some clinical pharmacological aspects of n-dipropylacetamide.

Authors:  F Pisani; R Di Perri
Journal:  Ital J Neurol Sci       Date:  1980-10
  10 in total
  14 in total

1.  Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities.

Authors:  Sara Ornaghi; Lawrence S Hsieh; Angélique Bordey; Patrizia Vergani; Michael J Paidas; Anthony N van den Pol
Journal:  J Neurosci       Date:  2017-06-19       Impact factor: 6.167

Review 2.  Diverse mechanisms of antiepileptic drugs in the development pipeline.

Authors:  Michael A Rogawski
Journal:  Epilepsy Res       Date:  2006-04-18       Impact factor: 3.045

3.  Valnoctamide, a non-teratogenic amide derivative of valproic acid, inhibits arachidonic acid activation in vitro by recombinant acyl-CoA synthetase-4.

Authors:  Hiren R Modi; Mireille Basselin; Stanley I Rapoport
Journal:  Bipolar Disord       Date:  2014-07-08       Impact factor: 6.744

4.  sec-Butylpropylacetamide (SPD), a new amide derivative of valproic acid for the treatment of neuropathic and inflammatory pain.

Authors:  Dan Kaufmann; Peter J West; Misty D Smith; Boris Yagen; Meir Bialer; Marshall Devor; H Steve White; K C Brennan
Journal:  Pharmacol Res       Date:  2016-11-24       Impact factor: 7.658

5.  Stereoselective anticonvulsant and pharmacokinetic analysis of valnoctamide, a CNS-active derivative of valproic acid with low teratogenic potential.

Authors:  Tawfeeq Shekh-Ahmad; Naama Hen; Boris Yagen; John H McDonough; Richard H Finnell; Bogdan J Wlodarczyk; Meir Bialer
Journal:  Epilepsia       Date:  2013-12-06       Impact factor: 5.864

6.  Structure activity relationship of human microsomal epoxide hydrolase inhibition by amide and acid analogues of valproic acid.

Authors:  O Spiegelstein; D L Kroetz; R H Levy; B Yagen; S I Hurst; M Levi; A Haj-Yehia; M Bialer
Journal:  Pharm Res       Date:  2000-02       Impact factor: 4.200

7.  Impairment of carbamazepine-10, 11-epoxide elimination by valnoctamide, a valpromide isomer, in healthy subjects.

Authors:  F Pisani; A Fazio; C Artesi; G Oteri; E Spina; T Tomson; E Perucca
Journal:  Br J Clin Pharmacol       Date:  1992-07       Impact factor: 4.335

8.  Mood stabilizers inhibit cytomegalovirus infection.

Authors:  Sara Ornaghi; John N Davis; Kelly L Gorres; George Miller; Michael J Paidas; Anthony N van den Pol
Journal:  Virology       Date:  2016-09-19       Impact factor: 3.616

9.  Pharmacokinetic analysis of the structural requirements for forming "stable" analogues of valpromide.

Authors:  A Haj-Yehia; S Hadad; M Bialer
Journal:  Pharm Res       Date:  1992-08       Impact factor: 4.200

Review 10.  Can we develop improved derivatives of valproic acid?

Authors:  M Bialer; A Haj-Yehia; K Badir; S Hadad
Journal:  Pharm World Sci       Date:  1994-02-18
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