• Title/Summary/Keyword: Ethosuximide

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HPLC Determination and Pharmacokinetic Profile of Ethosuximide in Korean Subjects (에토석시미드의 HPLC 분석법 및 한국인에서의 약동학적 특징)

  • 배정우;김지홍;양상인;김현경;장춘곤;한혜원;박영서;손의동;이석용
    • YAKHAK HOEJI
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    • v.47 no.6
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    • pp.444-459
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    • 2003
  • Ethosuximide is an oral anticonvulsantic agent used in the first choice anti-absence seizure drug. The purpose of this study was to assess the pharmacokinetic profile of the ethosuximide in healthy Korean volunteers and to develop the efficient assay method of ethosuximide in human plasma. The pharmacokinetics of ethosuximide administered orally was evaluated after a dose of 500 mg. Ethosuximide was assayed from plasma by a specific HPLC method reading absorbance at 195 nm. AUC was 1222$\pm$160 $\mu\textrm{g}$/$m\ell$$.$hr, $C_{max}$ 14.2l$\pm$1.74 $\mu\textrm{g}$/$m\ell$, $T_{max}$ 1.06$\pm$0.62 hr and half-life 77.83$\pm$12.46 hr. The half-life in Korean was longer than, in Caucasian (53∼56 hr).).).

Antihyperalgesic Effects of Ethosuximide and Mibefradil, T-type Voltage Activated Calcium Channel Blockers, in a Rat Model of Postoperative Pain (흰쥐의 술 후 통증 모델에서 T형 칼슘 통로 차단제인 Ethosuximide와 Mibefradil의 항통각과민 효과)

  • Shinn, Helen Ki;Cha, Young Deog;Han, Jeong Uk;Yoon, Jeong Won;Kim, Boo Seong;Song, Jang Ho
    • The Korean Journal of Pain
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    • v.20 no.2
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    • pp.92-99
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    • 2007
  • Background: A correlation between a T-type voltage activated calcium channel (VACC) and pain mechanism has not yet been established. The purpose of this study is to find out the effect of ethosuximide and mibefradil, representative selective T-type VACC blockers on postoperative pain using an incisional pain model of rats. Methods: After performing a plantar incision, rats were stabilized on plastic mesh for 2 hours. Then, the rats were injected with ethosuximide or mibefradil, intraperitoneally and intrathecally. The level of withdrawal threshold to the von Frey filament near the incision site was determined and the dose response curves were obtained. Results: After an intraperitoneal ethosuximide or mibefradil injection, the dose-response curve showed a dose-dependent increase of the threshold in a withdrawal reaction. After an intrathecal injection of ethosuximide, the threshold of a withdrawal reaction to mechanical stimulation increased and the increase was dose-dependent. After an intrathecal injection of mibefradil, no change occurred in either the threshold of a withdrawal reaction to mechanical stimulation or a dose-response curve. Conclusions: The T-type VACC blockers in a rat model of postoperative pain showed the antihyperalgesic effect. This effect might be due to blockade of T-type VACC, which was distributed in the peripheral nociceptors or at the supraspinal level. Further studies of the effect of T-type VACC on a pain transmission mechanism at the spinal cord level would be needed.

Effects of Ethosuximide on the Pilocarpine Induced Seizure in Rat Model of Neuronal Migration Disorder

  • Kim, Byung-Kon;Choi, In-Sun;Cho, Jin-Hwa;Jang, Il-Sung;Lee, Maan-Gee;Choi, Byung-Ju
    • The Korean Journal of Physiology and Pharmacology
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    • v.10 no.5
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    • pp.235-242
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    • 2006
  • Cortical malformation-associated epileptic seizures are resistant to conventional anticonvulsant drugs. Relatively little research has been conducted on the effects of antiepileptic drugs (AEDs) on seizure activity in a rat model of dysplasia. We have used rats exposed to methylazoxymethanol acetate (MAM) in utero, an animal model featuring nodular heterotopia, to investigate the effects of ethosuximide (ETX) in the dysplastic brain. Pilocarpine was used to induce acute seizure in MAM-exposed and age-matched vehicle-injected control animals. Field potential recordings were used to monitor the amplitude and number of population spikes, and paired pulse inhibition in response to stimulation of the commissural pathway. Pharmaco-resistance was tested by measuring seizure latencies after pilocarpine administration (320 mg/kg, Lp.) with and without pre-treatment with ETX. Pre-treatment with 300 mg of ETX significantly prolonged the latency to the status epilepticus (SE) in both control and MAM-treated groups. Pre-treatment with ETX 100mg and ETX 200 mg had little effect in MAMexposed rats. However, ETX 200 mg prolonged the latency to the SE in control groups. Spontaneous field potential and secondary after-discharges were higher for MAM-treated rat in comparison with control rats injects with ETX. The main findings of this study are that acute seizures initiated in MAM-exposed rats are relatively resistant to standard ETX assessed in vivo. These data suggest that ETX do not prolong seizure latencies in MAM-rats exposed to pilocarpine.