Research Topics
| Meir BialerSummaryAffiliation: The Hebrew University Country: Israel Publications
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Detail Information
Publications
Design and pharmacological activity of glycinamide and N-methoxy amide derivatives of analogs and constitutional isomers of valproic acidNeta 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...
Clinical pharmacology of parenteral use of antiepileptic drugsMeir Bialer
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 48:46-8. 2007- Evaluation of the enantioselective antiallodynic and pharmacokinetic profile of propylisopropylacetamide, a chiral isomer of valproic acid amideDan 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... - Potent anticonvulsant urea derivatives of constitutional isomers of valproic acidJakob 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... - 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.... - 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... - 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... - 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... - 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.... - Pharmacokinetics and drug interactions of eslicarbazepine acetateMeir 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... - Valproic Acid: second generationMeir Bialer
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Neurotherapeutics 4:130-7. 2007.... - 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.... - New antiepileptic drugs that are second generation to existing antiepileptic drugsMeir 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.... - Pharmacokinetic interactions of topiramateMeir 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... - The pharmacokinetics and interactions of new antiepileptic drugs: an overviewMeir 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... - 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.... - Correlation analysis between anticonvulsant ED50 values of antiepileptic drugs in mice and rats and their therapeutic doses and plasma levelsMeir 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... - 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... - 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... - Generic products of antiepileptic drugs: a perspective on bioequivalence and interchangeabilityMeir 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.... - Extended-release formulations for the treatment of epilepsyMeir 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... - 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... - Key factors in the discovery and development of new antiepileptic drugsMeir 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... - Evaluation of stereoselective anticonvulsant, teratogenic, and pharmacokinetic profile of valnoctylurea (capuride): a chiral stereoisomer of valproic acid urea derivativeJakob A Shimshoni
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 51:323-32. 2010.... - Comparative pharmacodynamic and pharmacokinetic analysis of two anticonvulsant halo derivatives of 2,2,3,3-tetramethylcyclopropanecarboxamide, an amide of a cyclic analog of valproic acidNeta 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 α-F-TMCD as an antiallodynic and antinociceptive compound was also evaluated... - Evaluation of the antiallodynic, teratogenic and pharmacokinetic profile of stereoisomers of valnoctamide, an amide derivative of a chiral isomer of valproic acidDan 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... - 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 epilepsyDorit Mimrod
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Epilepsia 46:1046-54. 2005..VPA was not found to have any clinically significant influence on TPM pharmacokinetic and metabolic profiles... - Pharmacokinetic and metabolic investigation of topiramate disposition in healthy subjects in the absence and in the presence of enzyme induction by carbamazepineMalka Britzi
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 46:378-84. 2005..Although 2,3-diol-TPM and 10-OH-TPM were measured in unconjugated form, the significant increases in their AUC and urinary excretion are consistent with the twofold increase in TPM clearance... - Synthesis and evaluation of antiallodynic and anticonvulsant activity of novel amide and urea derivatives of valproic acid analoguesDan 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... 
Anticonvulsant activity, teratogenicity and pharmacokinetics of novel valproyltaurinamide derivatives in miceNina Isoherranen
Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Israel
Br J Pharmacol 139:755-64. 2003....- Preclinical evaluation of 2,2,3,3-tetramethylcyclopropanecarbonyl-urea, a novel, second generation to valproic acid, antiepileptic drugEyal 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... - Metabolism of a new antiepileptic drug, N-methyl-tetramethylcyclopropanecarboxamide, and anticonvulsant activity of its metabolitesNina 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... - Anticonvulsant profile and teratogenicity of 3,3-dimethylbutanoylurea: a potential for a second generation drug to valproic acidJakob Avi Shimshoni
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 49:1202-12. 2008.... - Pharmacokinetic-pharmacodynamic relationships of (2S,3S)-valnoctamide and its stereoisomer (2R,3S)-valnoctamide in rodent models of epilepsyNina Isoherranen
Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
Pharm Res 20:1293-301. 2003..The more favorable brain penetration of (2S,3S)-VCD and its lower EC50 value in the 6Hz test provides one advantage over (2R,3S)-VCD as a new antiepileptic drug... - Efficacy of antiepileptic tetramethylcyclopropyl analogues of valproic acid amides in a rat model of neuropathic painIlan 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... - Pharmacokinetics and metabolism of a new potent antiepileptic drug, 2,2,3,3-tetramethycyclopropanecarbonylurea, in ratsEyal 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... - Synthesis and anticonvulsant activity of aromatic tetramethylcyclopropanecarboxamide derivativesJakob 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... - Syntheses and evaluation of anticonvulsant profile and teratogenicity of novel amide derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamideNaama 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... - Anticonvulsant activity, neural tube defect induction, mutagenicity and pharmacokinetics of a new potent antiepileptic drug, N-methoxy-2,2,3,3-tetramethylcyclopropane carboxamideEyal 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... - 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 teratogenicityNina Isoherranen
Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 44:1280-8. 2003.... - The activity of antiepileptic drugs as histone deacetylase inhibitorsSara Eyal
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Ein Karem, Hebrew University of Jerusalem, Israel
Epilepsia 45:737-44. 2004..25 mM and 1 mM, respectively. CONCLUSIONS: We found that in addition to VPA, the newer AED TPM and the major metabolite of LEV, PBA, are able to induce histone hyperacetylation in human cells, although with lower potencies than VPA... - Tetramethylcyclopropyl analogue of a leading antiepileptic drug, valproic acid. Synthesis and evaluation of anticonvulsant activity of its amide derivativesEyal 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... - Alpha-fluoro-2,2,3,3-tetramethylcyclopropanecarboxamide, a novel potent anticonvulsant derivative of a cyclic analogue of valproic acidNeta 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... - Characterization of the anticonvulsant profile and enantioselective pharmacokinetics of the chiral valproylamide propylisopropyl acetamide in rodentsNina 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... - Critical analysis of the discrepancy between V(beta) and V(ss) for drugs exhibiting different two-compartment disposition profilesEyal 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)... - Synthesis and anticonvulsant evaluation of dimethylethanolamine analogues of valproic acid and its tetramethylcyclopropyl analogueTawfeeq 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... - 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... - Efficacy of antiepileptic isomers of valproic acid and valpromide in a rat model of neuropathic painIlan 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... - Histone deacetylases inhibition and tumor cells cytotoxicity by CNS-active VPA constitutional isomers and derivativesSara 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... - Gas chromatographic determination of novel valproyl taurinamide derivatives in mouse and dog plasmaNina 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... - Anticonvulsant profile and teratogenicity of N-methyl-tetramethylcyclopropyl carboxamide: a new antiepileptic drugNina Isoherranen
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Epilepsia 43:115-26. 2002..CONCLUSIONS: The results obtained in this study show that M-TMCD is a broad-spectrum anticonvulsant drug that does not induce NTDs and support additional studies to evaluate its full therapeutic potential... - 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 assayMalka 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... - Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIVNaama 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... - Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamatesNaama 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... - Evaluation of the effects of propylisopropylacetic acid (PIA) on neuronal growth cone morphologyJakob 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... - The relationships between half-life (t1/2) and mean residence time (MRT) in the two-compartment open body modelEyal Sobol
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel
Biopharm Drug Dispos 25:157-62. 2004..g) Following zero and first order input MRT increases compared with i.v. bolus and so does CV and thus, the chances of MRT>t(1/2) are growing... - Pros and cons for the development of new antiepileptic drugsMeir 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)... - Mathematical comparison between volume of distribution (V) and volume of distribution at steady-state (Vss) utilizing model-independent approachEyal 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... - Topiramate and phenytoin pharmacokinetics during repetitive monotherapy and combination therapy to epileptic patientsR C Sachdeo
The University of Medicine and Dentistry of New Jersey, New Brunswick, NJ, USA
Epilepsia 43:691-6. 2002..TPM may affect PHT concentrations in a few patients because of inhibition by TPM of the CYP2C19-mediated minor metabolic pathway of PHT... - Development of new antiepileptic drugs: challenges, incentives, and recent advancesEmilio Perucca
Institute of Neurology, IRCCS C Mondino Foundation, Pavia, Italy
Lancet Neurol 6:793-804. 2007.... - Effect of topiramate or carbamazepine on the pharmacokinetics of an oral contraceptive containing norethindrone and ethinyl estradiol in healthy obese and nonobese female subjectsDennis R Doose
Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, New Jersey, USA
Epilepsia 44:540-9. 2003.... - Therapeutic drug monitoring of the newer antiepileptic drugsSvein 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... - Amidic modification of valproic acid reduces skeletal teratogenicity in miceAkinobu Okada
Safety Research Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co, Ltd, Tokyo, Japan
Birth Defects Res B Dev Reprod Toxicol 71:47-53. 2004..A structure-teratogenicity relationship of VPA on the skeleton is suspected... - Topiramate and lamotrigine pharmacokinetics during repetitive monotherapy and combination therapy in epilepsy patientsDennis R Doose
Johnson and Johnson Pharmaceutical Research and Development L L C, Raritan, New Jersey, U S A
Epilepsia 44:917-22. 2003.... - An interaction study between the new antiepileptic and CNS drug carisbamate (RWJ-333369) and lamotrigine and valproic acidShuchean 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... - Pharmacokinetics of the new antiepileptic and CNS drug RWJ-333369 following single and multiple dosing to humansCaiping Yao
Johnson and Johnson Pharmaceutical Research and Development, L.L.C, Raritan and Titusville, NJ, USA
Epilepsia 47:1822-9. 2006..Thus, orally administered RWJ-333369 has no hepatic first-pass effect. The 12-h half-life will enable bid dosing with an immediate-release oral formulation... - Pharmacokinetic interaction study between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine in healthy adultsSuchean Chien
Johnson and Johnson Pharmaceutical Research and Development, L.L.C, Raritan and Titusville, New Jersey, USA
Epilepsia 47:1830-40. 2006..CBZ induced RWJ-333369 clearance, resulting in shortened half-life and decreased exposure (AUCss) and C(max). Concomitant administration of RWJ-333369 with CBZ was generally safe and tolerated... - Teratology study of derivatives of tetramethylcyclopropyl amide analogues of valproic acid in miceAkinobu Okada
Drug Safety Research Laboratories, Astellas Pharma, Inc, Osaka, Japan
Birth Defects Res B Dev Reprod Toxicol 77:227-33. 2006..CONCLUSIONS: In addition to their more potent antiepileptic activity, these findings clearly indicate that N-methoxy-TMCD and TMC-urea are distinctly less teratogenic than VPA in NMRI mice... - Eslicarbazepine acetate: a double-blind, add-on, placebo-controlled exploratory trial in adult patients with partial-onset seizuresChristian 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... - Valproate decreases inositol biosynthesisGalit 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..CONCLUSIONS: The rate-limiting step of inositol biosynthesis, catalyzed by MIP synthase, is inhibited by VPA; inositol depletion is a first event shown to be common to lithium and VPA... - Identification of early-responsive genes correlated to valproic acid-induced neural tube defects in miceAkinobu 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... - Plasma and whole blood pharmacokinetics of topiramate: the role of carbonic anhydraseRichard 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)... - Polycomb homologs are involved in teratogenicity of valproic acid in miceAkinobu Okada
Safety Research Laboratories, Yamanouchi Pharmaceutical Co, Ltd, Tokyo, Japan
Birth Defects Res A Clin Mol Teratol 70:870-9. 2004..CONCLUSIONS: We propose that, during embryonic development, VPA may affect the gene silencing pathway mediated by the Polycomb group complex. The epigenetic mechanism of VPA teratogenicity on anteroposterior patterning is suspected... - Interlaboratory variability in the quantification of new generation antiepileptic drugs based on external quality assessment dataJohn 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)...