Meir Bialer

Summary

Affiliation: The Hebrew University
Country: Israel

Publications

  1. doi request reprint Design and pharmacological activity of glycinamide and N-methoxy amide derivatives of analogs and constitutional isomers of valproic acid
    Neta Pessah
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Behav 22:461-8. 2011
  2. ncbi request reprint Clinical pharmacology of parenteral use of antiepileptic drugs
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 48:46-8. 2007
  3. doi request reprint Evaluation of the enantioselective antiallodynic and pharmacokinetic profile of propylisopropylacetamide, a chiral isomer of valproic acid amide
    Dan Kaufmann
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neuropharmacology 54:699-707. 2008
  4. ncbi request reprint Potent anticonvulsant urea derivatives of constitutional isomers of valproic acid
    Jakob Avi Shimshoni
    Department of Pharmaceutics and Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Faculty of Medicine, and The David R Bloom Centre for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 50:6419-27. 2007
  5. ncbi request reprint Generic products of antiepileptic drugs (AEDs): is it an issue?
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 48:1825-32. 2007
  6. doi request reprint Comparative steady-state pharmacokinetic evaluation of immediate-release topiramate and USL255, a once-daily extended-release topiramate formulation
    Meir Bialer
    Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 54:1444-52. 2013
  7. doi request reprint How did phenobarbital's chemical structure affect the development of subsequent antiepileptic drugs (AEDs)?
    Meir Bialer
    School of Pharmacy, Institute for Drug Research, Faculty of Medicine, and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 53:3-11. 2012
  8. doi request reprint Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI)
    Meir Bialer
    Institute for Drug Research, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, Ein Karem, The Hebrew University of Jerusalem, 91120 Jerusalem, Israel
    Epilepsy Res 103:2-30. 2013
  9. doi request reprint Why are antiepileptic drugs used for nonepileptic conditions?
    Meir Bialer
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 53:26-33. 2012
  10. doi request reprint Chemical properties of antiepileptic drugs (AEDs)
    Meir Bialer
    School of Pharmacy, Institute for Drug Research, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, 91120, Israel
    Adv Drug Deliv Rev 64:887-95. 2012

Collaborators

Detail Information

Publications78

  1. doi request reprint Design and pharmacological activity of glycinamide and N-methoxy amide derivatives of analogs and constitutional isomers of valproic acid
    Neta Pessah
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Behav 22:461-8. 2011
    ..On the basis of these results, N-methoxy-VCD is a good candidate for further evaluation as a new anticonvulsant and central nervous system drug...
  2. ncbi request reprint Clinical pharmacology of parenteral use of antiepileptic drugs
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 48:46-8. 2007
  3. doi request reprint Evaluation of the enantioselective antiallodynic and pharmacokinetic profile of propylisopropylacetamide, a chiral isomer of valproic acid amide
    Dan Kaufmann
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neuropharmacology 54:699-707. 2008
    ..Both of PID's enantiomers, and the racemate, are more potent antiallodynic agents than VPA and have similar potency to gabapentin. Consequently, they have the potential to become new drugs for treating neuropathic pain...
  4. ncbi request reprint Potent anticonvulsant urea derivatives of constitutional isomers of valproic acid
    Jakob Avi Shimshoni
    Department of Pharmaceutics and Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Faculty of Medicine, and The David R Bloom Centre for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 50:6419-27. 2007
    ..The broad spectrum of anticonvulsant activity of the urea derivatives coupled with their wide safety margin make them potential candidates to become new, potent AEDs...
  5. ncbi request reprint Generic products of antiepileptic drugs (AEDs): is it an issue?
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 48:1825-32. 2007
    ....
  6. doi request reprint Comparative steady-state pharmacokinetic evaluation of immediate-release topiramate and USL255, a once-daily extended-release topiramate formulation
    Meir Bialer
    Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 54:1444-52. 2013
    ..Compare the pharmacokinetic (PK) profiles of immediate- and extended-release formulations of topiramate (TPM) in healthy subjects following multiple dosing, and evaluate maintenance of topiramate exposures after switching formulations...
  7. doi request reprint How did phenobarbital's chemical structure affect the development of subsequent antiepileptic drugs (AEDs)?
    Meir Bialer
    School of Pharmacy, Institute for Drug Research, Faculty of Medicine, and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 53:3-11. 2012
    ..In contrast, phenobarbital is still used worldwide in epilepsy. Nevertheless, the development of nonsedating phenobarbital derivatives will answer a clinical unmet need and might make this old AED more attractive...
  8. doi request reprint Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI)
    Meir Bialer
    Institute for Drug Research, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, Ein Karem, The Hebrew University of Jerusalem, 91120 Jerusalem, Israel
    Epilepsy Res 103:2-30. 2013
    ..Since the previous Eilat conference, retigabine (ezogabine) has been marketed and four newer AEDs in development (NAX 810-2, SPD, tonabersat and VX-765) are included in this manuscript...
  9. doi request reprint Why are antiepileptic drugs used for nonepileptic conditions?
    Meir Bialer
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 53:26-33. 2012
    ..Therefore, a new AED with additional approved indications in bipolar disorder and neuropathic pain might have a potential market size three times larger than that of epilepsy alone...
  10. doi request reprint Chemical properties of antiepileptic drugs (AEDs)
    Meir Bialer
    School of Pharmacy, Institute for Drug Research, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, 91120, Israel
    Adv Drug Deliv Rev 64:887-95. 2012
    ....
  11. doi request reprint Pharmacokinetics and drug interactions of eslicarbazepine acetate
    Meir Bialer
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 53:935-46. 2012
    ..Eslicarbazepine clearance is induced by phenobarbital, phenytoin, and CBZ and it dose-dependently decreases plasma exposure of oral contraceptive and simvastatin...
  12. doi request reprint Generic products of antiepileptic drugs: a perspective on bioequivalence and interchangeability
    Meir Bialer
    Faculty of Medicine, Institute of Drug Research, School of Pharmacy and David R Bloom Center for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 51:941-50. 2010
    ....
  13. ncbi request reprint Correlation analysis between anticonvulsant ED50 values of antiepileptic drugs in mice and rats and their therapeutic doses and plasma levels
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Behav 5:866-72. 2004
    ..Consequently, the aim of this work was to perform a correlation analysis between therapeutic daily doses (D) and average steady-state plasma concentrations (Css,av) of AEDs and their activity in common anticonvulsant animal models...
  14. ncbi request reprint Progress report on new antiepileptic drugs: a summary of the Seventh Eilat Conference (EILAT VII)
    Meir Bialer
    Department of Pharmaceutics, Faculty of Medicine, School of Pharmacy and David R Bloom Center for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Res 61:1-48. 2004
    ....
  15. ncbi request reprint New antiepileptic drugs currently in clinical trials: is there a strategy in their development?
    Meir Bialer
    Department of Pharmaceutics and David R Bloom Center, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Israel
    Ther Drug Monit 24:85-90. 2002
    ..This is particularly true for new AEDs that are second-generation or follow-up compounds of existing AEDs...
  16. ncbi request reprint Pharmacokinetic interactions of topiramate
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9120, Israel
    Clin Pharmacokinet 43:763-80. 2004
    ..The results of many of these drug interaction studies with topiramate have not been published before, and are presented and discussed for the first time in this article...
  17. ncbi request reprint Extended-release formulations for the treatment of epilepsy
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    CNS Drugs 21:765-74. 2007
    ..Weighing up the advantages and disadvantages for once- versus twice-daily administration of ER formulations in epilepsy leads to a conclusion in favour of twice-daily administration...
  18. ncbi request reprint Valproic Acid: second generation
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neurotherapeutics 4:130-7. 2007
    ....
  19. ncbi request reprint The pharmacokinetics and interactions of new antiepileptic drugs: an overview
    Meir Bialer
    Department of Pharmaceutics and David R Bloom Center for Pharmacy, The Hebrew University of Jerusalem, Israel
    Ther Drug Monit 27:722-6. 2005
    ..However, in spite of the large therapeutic arsenal of old and new AEDs, about 30% of epileptic patients are still not seizure-free, and thus, there is a substantial need to develop new AEDs...
  20. doi request reprint Key factors in the discovery and development of new antiepileptic drugs
    Meir Bialer
    Institute of Drug Research, School of Pharmacy, Faculty of Medicine, and The David R Bloom Centre for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Nat Rev Drug Discov 9:68-82. 2010
    ..We also discuss the current approach to AED discovery and highlight some of the unique features of newer models of pharmacoresistance and epileptogenesis that have emerged in recent years...
  21. doi request reprint Progress report on new antiepileptic drugs: a summary of the Tenth Eilat Conference (EILAT X)
    Meir Bialer
    Institute for Drug Research, School of Pharmacy and David R Bloom Center for Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Res 92:89-124. 2010
    ..The CNS efficacy of these compounds in anticonvulsant animal models as well as other disease model systems are presented in Tables 1 and 2 and their proposed mechanism of action at summarized in Table 3...
  22. ncbi request reprint New antiepileptic drugs that are second generation to existing antiepileptic drugs
    Meir Bialer
    The Hebrew University of Jerusalem, Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, P O Box 12065, Ein Karem, Jerusalem 91120, Israel
    Expert Opin Investig Drugs 15:637-47. 2006
    ....
  23. ncbi request reprint Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII)
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy, David R Bloom Center for Pharmacy, The Hebrew University of Jerusalem, 91120 Jerusalem, Israel
    Epilepsy Res 73:1-52. 2007
    ....
  24. doi request reprint Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX)
    Meir Bialer
    Department of Pharmaceutics, School of Pharmacy and David R Bloom Centre for Pharmacy, Faculty of Medicine, Ein Karem, The Hebrew University of Jerusalem, 91120 Jerusalem, Israel
    Epilepsy Res 83:1-43. 2009
    ..The CNS efficacy of these compounds in anticonvulsant animal models as well as other disease model systems are presented in first and second tables and their proposed mechanisms of action are summarized in the third table...
  25. doi request reprint Evaluation of stereoselective anticonvulsant, teratogenic, and pharmacokinetic profile of valnoctylurea (capuride): a chiral stereoisomer of valproic acid urea derivative
    Jakob A Shimshoni
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 51:323-32. 2010
    ....
  26. doi request reprint Comparative pharmacodynamic and pharmacokinetic analysis of two anticonvulsant halo derivatives of 2,2,3,3-tetramethylcyclopropanecarboxamide, an amide of a cyclic analog of valproic acid
    Neta Pessah
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 51:1944-53. 2010
    ..The potential of ╬▒-F-TMCD as an antiallodynic and antinociceptive compound was also evaluated...
  27. ncbi request reprint Pharmacokinetic and metabolic investigation of topiramate disposition in healthy subjects in the absence and in the presence of enzyme induction by carbamazepine
    Malka Britzi
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 46:378-84. 2005
    ..To characterize the metabolic profile of topiramate (TPM) in humans and to assess the influence of enzyme induction by carbamazepine (CBZ) on the pharmacokinetics and metabolic profile of TPM...
  28. doi request reprint Evaluation of the antiallodynic, teratogenic and pharmacokinetic profile of stereoisomers of valnoctamide, an amide derivative of a chiral isomer of valproic acid
    Dan Kaufmann
    Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Israel
    Neuropharmacology 58:1228-36. 2010
    ..2S,3S)-VCD is more potent and less embryotoxic than (2R,3S)-VCD and thus, has a potential to become a candidate for development as a new drug for treating neuropathic pain...
  29. ncbi request reprint Preclinical evaluation of 2,2,3,3-tetramethylcyclopropanecarbonyl-urea, a novel, second generation to valproic acid, antiepileptic drug
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neuropharmacology 51:933-46. 2006
    ..In the hepatotoxicity study the blood levels of TMCU were evaluated at day 1 and day 7 of the treatment. TMCU mutagenicity was evaluated in the Ames test...
  30. ncbi request reprint Metabolism of a new antiepileptic drug, N-methyl-tetramethylcyclopropanecarboxamide, and anticonvulsant activity of its metabolites
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Res 58:1-12. 2004
    ..As OH-MTMCD was also present at lower concentrations than MTMCD in mouse brain, it is likely that MTMCD itself and not one of its metabolites is responsible for its activity in therapy-resistant epilepsy...
  31. doi request reprint Synthesis and evaluation of antiallodynic and anticonvulsant activity of novel amide and urea derivatives of valproic acid analogues
    Dan Kaufmann
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Israel
    J Med Chem 52:7236-48. 2009
    ..These data indicate strong potential for the above-mentioned novel compounds as candidates for future drug development for the treatment of neuropathic pain...
  32. ncbi request reprint A comparative study of the effect of carbamazepine and valproic acid on the pharmacokinetics and metabolic profile of topiramate at steady state in patients with epilepsy
    Dorit Mimrod
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
    Epilepsia 46:1046-54. 2005
    ..To compare the influence of enzyme-inducing comedication and valproic acid (VPA) on topiramate (TPM) pharmacokinetics and metabolism at steady state...
  33. pmc Anticonvulsant activity, teratogenicity and pharmacokinetics of novel valproyltaurinamide derivatives in mice
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Israel
    Br J Pharmacol 139:755-64. 2003
    ....
  34. ncbi request reprint Efficacy of antiepileptic tetramethylcyclopropyl analogues of valproic acid amides in a rat model of neuropathic pain
    Ilan Winkler
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neuropharmacology 49:1110-20. 2005
    ..Tetramethylcyclopropyl analogues of VPA amides have potential to become a new series of drugs for neuropathic pain treatment...
  35. ncbi request reprint Pharmacokinetics and metabolism of a new potent antiepileptic drug, 2,2,3,3-tetramethycyclopropanecarbonylurea, in rats
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P O B 12065 Ein Karem, Jerusalem 91120, Israel
    Drug Metab Dispos 33:1538-46. 2005
    ..p. administration of 5 and 20 mg/kg TMCU, the drug was excreted in the urine as OH-TMCU at an extent of 28.3 +/- 2.6% and 42.1 +/- 3.8%, respectively. A portion of OH-TMCU was excreted in the urine as TMCU sulfate and TMCU glucuronide...
  36. doi request reprint Anticonvulsant profile and teratogenicity of 3,3-dimethylbutanoylurea: a potential for a second generation drug to valproic acid
    Jakob Avi Shimshoni
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 49:1202-12. 2008
    ....
  37. ncbi request reprint Pharmacokinetic-pharmacodynamic relationships of (2S,3S)-valnoctamide and its stereoisomer (2R,3S)-valnoctamide in rodent models of epilepsy
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
    Pharm Res 20:1293-301. 2003
    ..The purpose of this study was to evaluate the anticonvulsant activity of two VCD stereoisomers in comparison with VCD (racemate), valpromide (VPD), and valproic acid (VPA) and to study their pharmacokinetic-pharmacodynamic relationships...
  38. pmc Characterization of the anticonvulsant profile and enantioselective pharmacokinetics of the chiral valproylamide propylisopropyl acetamide in rodents
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Jerusalem, Israel
    Br J Pharmacol 138:602-13. 2003
    ..This study also showed the importance of studying the pharmacokinetics and pharmacodynamics of chiral drugs following administration of the individual enantiomers as well as the racemic mixture...
  39. doi request reprint Synthesis and anticonvulsant activity of aromatic tetramethylcyclopropanecarboxamide derivatives
    Jakob Avi Shimshoni
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Bioorg Med Chem 16:6297-305. 2008
    ..The better anticonvulsant potency of compound 21 and its wider safety margin compared to valproic acid (VPA) and zonisamide make it a potential candidate to become a new AED second-generation to VPA...
  40. doi request reprint Syntheses and evaluation of anticonvulsant profile and teratogenicity of novel amide derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide
    Naama Hen
    Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 53:4177-86. 2010
    ..The anticonvulsant properties of these compounds make them potential candidates for further development as new, potent, and safe AEDs...
  41. ncbi request reprint Anticonvulsant activity, neural tube defect induction, mutagenicity and pharmacokinetics of a new potent antiepileptic drug, N-methoxy-2,2,3,3-tetramethylcyclopropane carboxamide
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsy Res 73:75-84. 2007
    ..These results support further studies to fully characterize the therapeutic potential of OM-TMCD...
  42. doi request reprint Stereoselective pharmacodynamic and pharmacokinetic analysis of sec-Butylpropylacetamide (SPD), a new CNS-active derivative of valproic acid with unique activity against status epilepticus
    Naama Hen
    Institute for Drug Research, Faculty of Medicine, School of Pharmacy, The Hebrew University of Jerusalem, Israel
    J Med Chem 56:6467-77. 2013
    ....
  43. ncbi request reprint Tetramethylcyclopropyl analogue of a leading antiepileptic drug, valproic acid. Synthesis and evaluation of anticonvulsant activity of its amide derivatives
    Eyal Sobol
    Department of Pharmaceutics, Faculty of Medicine, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 47:4316-26. 2004
    ..5 in the MES test, which is about 12 times greater than that of VPA. Compounds 21 and 25 have the potential for development as novel potent and safe central nervous system active drugs with a broad spectrum of antiepileptic activity...
  44. ncbi request reprint Developmental outcome of levetiracetam, its major metabolite in humans, 2-pyrrolidinone N-butyric acid, and its enantiomer (R)-alpha-ethyl-oxo-pyrrolidine acetamide in a mouse model of teratogenicity
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 44:1280-8. 2003
    ....
  45. ncbi request reprint The activity of antiepileptic drugs as histone deacetylase inhibitors
    Sara Eyal
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Ein Karem, Hebrew University of Jerusalem, Israel
    Epilepsia 45:737-44. 2004
    ..The aim of this study was to assess comparatively the activity of traditional and newer AEDs as HDAC inhibitors...
  46. doi request reprint Alpha-fluoro-2,2,3,3-tetramethylcyclopropanecarboxamide, a novel potent anticonvulsant derivative of a cyclic analogue of valproic acid
    Neta Pessah
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, and The David R Bloom Centre for Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 52:2233-42. 2009
    ..Unlike 1, 11 was nonteratogenic in mice. This novel compound has the potential to become a candidate for development as a new potent and safe antiepileptic and CNS drug...
  47. doi request reprint Valnoctamide and sec-butyl-propylacetamide (SPD) for acute seizures and status epilepticus
    Tawfeeq Shekh-Ahmad
    School of Pharmacy, Faculty of Medicine, Institute for Drug Research, The Hebrew University of Jerusalem, Ein Karem, Jerusalem, Israel
    Epilepsia 54:99-102. 2013
    ..SPD activity in the pilocarpine and soman-induced SE models when administered 20-60 min after seizure onset, differentiates SPD from benzodiazepines and all other antiepileptic drugs . ..
  48. doi request reprint Synthesis and anticonvulsant evaluation of dimethylethanolamine analogues of valproic acid and its tetramethylcyclopropyl analogue
    Tawfeeq Shekh-Ahmad
    Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Israel
    Epilepsy Res 98:238-46. 2012
    ..2,2,3,3-Tetramethylcyclopropanecarboxylic acid (TMCA) is an inactive cyclopropyl analogue of VPA that serves as a starting material for the synthesis of CNS-active compounds...
  49. ncbi request reprint Critical analysis of the discrepancy between V(beta) and V(ss) for drugs exhibiting different two-compartment disposition profiles
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Biopharm Drug Dispos 26:51-8. 2005
    ..The newly derived equations along with their graphical presentation may serve as an excellent predictive tool for checking the accuracy of the experimentally obtained values of V(beta) and V(ss)...
  50. ncbi request reprint New CNS-active drugs which are second-generation valproic acid: can they lead to the development of a magic bullet?
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, POB 12065, Ein Karem, Jerusalem 91120, Israel
    Curr Opin Neurol 16:203-11. 2003
    ..These characteristics would give such a drug the potential to be utilized in epilepsy and other CNS disorders...
  51. doi request reprint Stereoselective anticonvulsant and pharmacokinetic analysis of valnoctamide, a CNS-active derivative of valproic acid with low teratogenic potential
    Tawfeeq Shekh-Ahmad
    Faculty of Medicine, School of Pharmacy, Institute for Drug Research, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 55:353-61. 2014
    ..VCD exhibits stereoselective pharmacokinetics (PK) in animals and humans. The current study comparatively evaluated the pharmacodynamics (PD; anticonvulsant activity and teratogenicity) and PK of the four individual stereoisomers of VCD...
  52. ncbi request reprint Analysis of topiramate and its metabolites in plasma and urine of healthy subjects and patients with epilepsy by use of a novel liquid chromatography-mass spectrometry assay
    Malka Britzi
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Ther Drug Monit 25:314-22. 2003
    ..Two quantitatively significant TPM metabolites (10-OH-TPM and 2,3-diol-TPM) and two quantitatively minor metabolites (9-OH-TPM and 4,5-diol-TPM) were detected and quantified in urine samples from patients with epilepsy...
  53. ncbi request reprint Histone deacetylases inhibition and tumor cells cytotoxicity by CNS-active VPA constitutional isomers and derivatives
    Sara Eyal
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Ein Kerem, The Hebrew University of Jerusalem, Jerusalem, Israel
    Biochem Pharmacol 69:1501-8. 2005
    ..In conclusion, in comparison to the VPA derivatives and constitutional isomers tested in this study, VPA had the optimal chemical structure in terms of HDACs inhibition and tumor cells cytotoxicity...
  54. pmc Efficacy of antiepileptic isomers of valproic acid and valpromide in a rat model of neuropathic pain
    Ilan Winkler
    Department of Pharmaceutics, The Hebrew University of Jerusalem, Jerusalem, Israel
    Br J Pharmacol 146:198-208. 2005
    ..Consequently, VCD and DID have potential to become new drugs for the treatment of neuropathic pain...
  55. doi request reprint Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV
    Naama Hen
    Institute for Drug Research, The Hebrew University of Jerusalem, Jerusalem, Israel
    J Med Chem 54:3977-81. 2011
    ..Compounds 9, 14, and 19 inhibited CA II, while 10 and 12 inhibited all isoforms. Structural studies suggest that differences in the active sites' hydrophobicity modulate the affinity of the inhibitors...
  56. ncbi request reprint Anticonvulsant profile and teratogenicity of N-methyl-tetramethylcyclopropyl carboxamide: a new antiepileptic drug
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Epilepsia 43:115-26. 2002
    ....
  57. ncbi request reprint Gas chromatographic determination of novel valproyl taurinamide derivatives in mouse and dog plasma
    Nina Isoherranen
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, P O Box 12065 Ein Karem, Israel
    J Chromatogr B Analyt Technol Biomed Life Sci 788:125-36. 2003
    ..The developed method was suitable for quantification of a series of CNS-active valproyl taurineamide derivatives in biological samples at relevant in vivo concentrations...
  58. doi request reprint Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamates
    Naama Hen
    Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
    J Med Chem 55:2835-45. 2012
    ..Compounds 34, 38, 40, and 47 offer the optimal efficacy-safety profile and, consequently, are promising candidates for development as new antiepileptics...
  59. pmc Evaluation of the effects of propylisopropylacetic acid (PIA) on neuronal growth cone morphology
    Jakob A Shimshoni
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Neuropharmacology 56:831-7. 2009
    ..These results demonstrate an effect of (R,S)-PIA on the neuronal actin cytoskeleton shared in common with other mood stabilizers, and suggest a potential to induce structural changes within the CNS...
  60. ncbi request reprint The relationships between half-life (t1/2) and mean residence time (MRT) in the two-compartment open body model
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
    Biopharm Drug Dispos 25:157-62. 2004
    ..The relationships between t(1/2) and MRT in the two-compartment model have not been explored and it is not clear whether in this model too MRT is always greater than t(1/2)...
  61. ncbi request reprint Pros and cons for the development of new antiepileptic drugs
    Meir Bialer
    Department of Pharmaceutics and David R Bloom Centre for Pharmacy, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Israel
    CNS Drugs 16:285-9. 2002
    ..This is especially true for developing countries where resources would be much better spent on prevention and closing the treatment gap (the difference between those who can be treated and those who are treated)...
  62. ncbi request reprint Mathematical comparison between volume of distribution (V) and volume of distribution at steady-state (Vss) utilizing model-independent approach
    Eyal Sobol
    Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Jerusalem, Israel
    Biopharm Drug Dispos 25:99-101. 2004
    ..This new method does not require any knowledge of microscopical rate constants and is based solely on an exponentially decreasing function, which is the common way to describe drug disposition following i.v. bolus...
  63. ncbi request reprint Topiramate and phenytoin pharmacokinetics during repetitive monotherapy and combination therapy to epileptic patients
    R C Sachdeo
    The University of Medicine and Dentistry of New Jersey, New Brunswick, NJ, USA
    Epilepsia 43:691-6. 2002
    ..To evaluate the potential pharmacokinetic interactions between topiramate (TPM) and phenytoin (PHT) in patients with epilepsy by studying their pharmacokinetics (PK) after monotherapy and concomitant TPM/PHT treatment...
  64. ncbi request reprint Effect of topiramate or carbamazepine on the pharmacokinetics of an oral contraceptive containing norethindrone and ethinyl estradiol in healthy obese and nonobese female subjects
    Dennis R Doose
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, New Jersey, USA
    Epilepsia 44:540-9. 2003
    ....
  65. ncbi request reprint Therapeutic drug monitoring of the newer antiepileptic drugs
    Svein I Johannessen
    The National Center for Epilepsy, Sandvika, Norway, Carlo Besta, Milan, Italy
    Ther Drug Monit 25:347-63. 2003
    ..Although routine monitoring in general cannot be recommended at present, measurements of some of the drugs is undoubtedly of help with individualization of treatment in selected cases in a particular clinical setting...
  66. ncbi request reprint Pharmacokinetic interaction study between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine in healthy adults
    Suchean Chien
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan and Titusville, New Jersey, USA
    Epilepsia 47:1830-40. 2006
    ..To characterize the possible pharmacokinetic interaction between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine (CBZ) following multiple dosing in healthy subjects...
  67. ncbi request reprint An interaction study between the new antiepileptic and CNS drug carisbamate (RWJ-333369) and lamotrigine and valproic acid
    Shuchean Chien
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan and Titusville, NJ, USA
    Epilepsia 48:1328-38. 2007
    ..To characterize possible pharmacokinetic interactions between the new antiepileptic drug carisbamate (RWJ-333369) and valproic acid (VPA) or lamotrigine (LTG) following multiple dosing in healthy subjects...
  68. ncbi request reprint Pharmacokinetics of the new antiepileptic and CNS drug RWJ-333369 following single and multiple dosing to humans
    Caiping Yao
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan and Titusville, NJ, USA
    Epilepsia 47:1822-9. 2006
    ..To characterize the pharmacokinetics of the new antiepileptic and CNS drug RWJ-333369 following single and multiple oral doses to healthy subjects, including the effect of food on bioavailability...
  69. ncbi request reprint Development of new antiepileptic drugs: challenges, incentives, and recent advances
    Emilio Perucca
    Institute of Neurology, IRCCS C Mondino Foundation, Pavia, Italy
    Lancet Neurol 6:793-804. 2007
    ....
  70. ncbi request reprint Amidic modification of valproic acid reduces skeletal teratogenicity in mice
    Akinobu Okada
    Safety Research Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co, Ltd, Tokyo, Japan
    Birth Defects Res B Dev Reprod Toxicol 71:47-53. 2004
    ..The objective of this study was to investigate the teratogenic effects of VPA, VPD, and VCD on the skeleton of NMRI mice...
  71. ncbi request reprint Topiramate and lamotrigine pharmacokinetics during repetitive monotherapy and combination therapy in epilepsy patients
    Dennis R Doose
    Johnson and Johnson Pharmaceutical Research and Development L L C, Raritan, New Jersey, U S A
    Epilepsia 44:917-22. 2003
    ....
  72. ncbi request reprint Plasma and whole blood pharmacokinetics of topiramate: the role of carbonic anhydrase
    Richard P Shank
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ 08869 0602, USA
    Epilepsy Res 63:103-12. 2005
    ..The difference between TPM blood and plasma pharmacokinetics was more profound at low doses (< or = 100 mg/day)...
  73. ncbi request reprint Valproate decreases inositol biosynthesis
    Galit Shaltiel
    Stanley Research Center and Zlotowski Center for Neuroscience, Ben Gurion University of the Negev, Mental Health Center, Beersheva, Israel
    Biol Psychiatry 56:868-74. 2004
    ..Valproate also depletes inositol in yeast, Dictyostelium, and rat neurons. This raised the possibility that the effect is the result of myo-inositol-1-phosphate (MIP) synthase inhibition...
  74. ncbi request reprint Polycomb homologs are involved in teratogenicity of valproic acid in mice
    Akinobu Okada
    Safety Research Laboratories, Yamanouchi Pharmaceutical Co, Ltd, Tokyo, Japan
    Birth Defects Res A Clin Mol Teratol 70:870-9. 2004
    ..We have attempted to describe a fundamental role of the Polycomb group (Pc-G) in VPA-induced transformations of the axial skeleton...
  75. ncbi request reprint Identification of early-responsive genes correlated to valproic acid-induced neural tube defects in mice
    Akinobu Okada
    Drug Safety Research Laboratories, Astellas Pharma Inc, 2 1 6 Kashima, Yodogawa ku, Osaka 532 8514, Japan
    Birth Defects Res A Clin Mol Teratol 73:229-38. 2005
    ..However, the molecular mechanism of its teratogenesis is unknown. This study was conducted to investigate the genomewide effects of VPA disruption of normal neural tube development in mice...
  76. ncbi request reprint Eslicarbazepine acetate: a double-blind, add-on, placebo-controlled exploratory trial in adult patients with partial-onset seizures
    Christian Elger
    Department of Epileptology, University of Bonn, Bonn, Germany
    Epilepsia 48:497-504. 2007
    ..To explore the efficacy and safety of eslicarbazepine acetate (BIA 2-093), a new antiepileptic drug, as adjunctive therapy in adult patients with partial epilepsy...
  77. ncbi request reprint Teratology study of derivatives of tetramethylcyclopropyl amide analogues of valproic acid in mice
    Akinobu Okada
    Drug Safety Research Laboratories, Astellas Pharma, Inc, Osaka, Japan
    Birth Defects Res B Dev Reprod Toxicol 77:227-33. 2006
    ..The objective of this study was to investigate the teratogenic effects of these compounds in NMRI mice...
  78. ncbi request reprint Interlaboratory variability in the quantification of new generation antiepileptic drugs based on external quality assessment data
    John Williams
    Subcommission on Therapeutic Drug Monitoring and Pharmacokinetics, ILAE Commission on Therapeutic Strategies, Department of Pharmacology, Therapeutics and Toxicology, University of Wales College of Medicine, Heath Park, Cardiff, Wales
    Epilepsia 44:40-5. 2003
    ..To assess interlaboratory variability in the determination of serum levels of new antiepileptic drugs (AEDs)...