Oxcarbazepine - CAS 28721-07-5
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Not Intended for Therapeutic Use. For research use only.
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Sodium Channel
Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM. Oxcarbazepine is marketed as Trileptal by Novartis and available in some countries as a generic drug.
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1.Efficacy and acceptability of oxcarbazepine vs. carbamazepine with betahistine mesilate tablets in treating vestibular paroxysmia: a retrospective review.
Yi C1, Wenping X1, Hui X1, Xin H1, Xiue L1, Jun Z1, Shangyong G1. Postgrad Med. 2016 Apr 8. [Epub ahead of print]
OBJECTIVES: Vestibular paroxysmia (VP) is a rare episodic peripheral vestibular disorder that can cause acute short attacks of vertigo. This study aimed to compare the efficacy and acceptability of carbamazepine (CBZ), CBZ plus betahistine mesilate tablets (BMT) and oxcarbazepine (OXC) plus BMT in treating VP within 12 weeks.
2.The Curse of the Dolphins: Cognitive Decline and Psychosis.
Phelps R1, Tsai A, Hagen A, Pinter J, Smith R, Stein MT. J Dev Behav Pediatr. 2016 Apr 18. [Epub ahead of print]
CASE: Isela is an 11-year-old Mexican-American girl with mild intellectual disability. During a vacation with her family, she went swimming with dolphins. A few days later, Isela awoke at night with laughing spells; during the day, she was pacing, aggressive, and had a decline in self-care and communication skills. Her parents attributed the symptoms to the dolphins. She was evaluated by a pediatric neurologist. The sleep-deprived electroencephalogram, brain magnetic resonance imaging, lumbar puncture, and thyroid function tests were normal. A genomic microarray was sent. The neurologist initiated empirical therapy for seizures with lamotrigine, which caused a rash. It was discontinued. She was then treated with oxcarbazepine followed by topiramate for several months without any change in symptoms. Comparative genomic hybridization revealed a small deletion at 14q13.1, which includes the NPAS3 gene. Psychiatry was consulted after several months of persistent symptoms.
3.Development and validation of an enantioselective SFC-MS/MS method for simultaneous separation and quantification of oxcarbazepine and its chiral metabolites in beagle dog plasma.
Yang Z1, Xu X1, Sun L1, Zhao X1, Wang H1, Fawcett JP2, Yang Y3, Gu J4. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 May 1;1020:36-42. doi: 10.1016/j.jchromb.2016.03.013. Epub 2016 Mar 15.
A rapid and sensitive assay based on supercritical fluid chromatography-tandem mass spectrometry (SFC-MS/MS) has been developed and validated for the determination of oxcarbazepine (OXC) and its chiral metabolite licarbazine (Lic) in beagle dog plasma using carbamazepine as internal standard. Chiral analysis in a run time of only 3min was performed on an ACQUITY UPC(2) ™ Trefoil™ CEL2 column (3.0×150mm, 2.5μm) at 50°C by isocratic elution with a mobile phase of supercritical carbon dioxide (purity≥99.99%) and methanol (60:40, v/v) at a flow rate of 2.3mL/min. The assay was linear over the concentration ranges 5-1000ng/mL for OXC and 0.5-100ng/mL for the enantiomers of Lic with corresponding lower limits of quantitation of 5ng/mL and 0.5ng/mL. Intra- and inter-day precisions were in the range 0.78-14.14% with accuracies in the range -10.80% to 0.42%. The method was successfully applied to a pharmacokinetic study involving a single oral administration of 16mg/kg OXC as Trileptal(@) tablets to beagle dogs.
4.Pain phenotype as a predictor for drug response in painful polyneuropathy A retrospective analysis of data from controlled clinical trials.
Holbech JV1, Bach FW, Finnerup NB, Jensen TS, Sindrup SH. Pain. 2016 Mar 22. [Epub ahead of print]
The drugs available for treatment of neuropathic pain have a somewhat disappointing efficacy with many patients left with limited or no effect. Individualized treatment based on phenotype according to presumed underlying pain mechanism(s) has been proposed to improve outcome. We report a retrospective analysis of phenotype-specific effects of several neuropathic pain drugs, which were studied in a series of cross-over, placebo-controlled, clinical trials. The data originate from 7 trials with similar design and outcome recordings, which all had a thorough baseline registration of symptoms, signs and quantitative sensory testing. The latter was used to phenotype patients into subgroups reflecting presumed pain mechanisms. There were a total of 361 patient records distributed over treatments with 4 antidepressants and 4 anticonvulsants. Five of the drugs reduced total pain significantly compared to placebo. Only a few phenotype-specific differences in total pain reduction were found within the investigated drugs.
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CAS 28721-07-5 Oxcarbazepine

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