Carbamazepine suppresses synchronized afterdischarging in disinhibited immature rat hippocampus in vitro

Bath application of therapeutic concentrations of the anticonvulsant carbamazepine suppressed penicillin-induced synchronized afterdischarging in immature rat CA₃ hippocampal pyramidal cells. Afterdischarging was completely abolished in all preparations at a concentration of 30 μM (IC₅₀ = 8.5 ± 1.4 μM; mean ± S.E.M.). The duration of the preceding epilptiform burst was not altered at this concentration and was diminished by only 24.4 ± 1.2% at a supratherapeutic concentration of 100 μM. These results suggest that a carbamazepine-sensitive neurophysiological mechanism distinct from those responsible for epileptiform burst generation plays a key role in the generation of afterdischarges in developing hippocampus.     

Central Hypotensive Effects of Nicardipine in Conscious Freely Moving Spontaneously Hypertensive Rat

The central cardiovascular effects of the calcium channel blocker nicardipine was studied in conscious freely moving normotensive Wistar Kyoto rats (WKY) and spontaneously hypertensive rats (SHR). Nicardipine was administered in a 1.5 μ1 volume into the lateral ventricle of the brain (i.c.v.) or intravenously (i.v.). The injection of vehicle alone did not significantly change mean arterial pressure (MAP) or heart rate (HR). Nicardipine (10,30,100 and 300 μg/kg), intravenously administered, dose-dependently decreased MAP and increased HR in WKY and SHR. However, when administered i.c.v., nicardipine (10 μg/kg) increased MAP and HR in WKY and decreased MAP without any significant change in HR in SHR. These results are consistent with previous work reporting an exaggerated hypotensive response to i.c.v. administration of dihydropyridine calcium channel blockers in anesthetized SHR as compared to WKY. They suggest that a 1,4–dihydropyridine-sensitive pressor system is present in the SHR but not in the WKY.     

血脉通胶囊与卡马西平联用对癫痫模型小鼠的保护作用

目的：研究血脉通胶囊与卡马西平（CBZ）联用对癫痫模型小鼠的保护作用。方法：第1、3、5、8、10天腹腔注射戊四唑（PTZ,45mg／kg）,第12天腹腔注射PTZ（75mg／kg）以复制小鼠癫痫模型。实验分为模型（等容生理盐水）组、CBZ（120mg／kg）组、联合用药（CBZ120mg／kg＋血脉通胶囊500mg／kg）组。除第12天外,每次腹腔注射PTZ前30min灌胃给药。计算小鼠轻、重度发作率和死亡率,记录小鼠癫痫轻度发作潜伏期、重度发作持续时间、发作等级,并观察脑组织病理切片。结果：与模型组比较,CBZ组与联合用药组小鼠重度发生率、死亡率显著降低,轻度发作潜伏期显著延长,重度发作持续时间显著缩短,发作等级显著降低（P〈0．01）,小鼠脑组织的损伤明显减轻。与CBZ组比较,联合用药组以上指标均显著改善（P〈0．05）。结论：血脉通胶囊和CBZ联用对小鼠PTZ慢性点燃有明显的抑制作用。     

Amelioration of erectile dysfunction following a switch from carbamazepine to oxcarbazepine: recent clinical experience

ABSTRACT

Oxcarbazepine is an antiepileptic drug (AED) indicated for use as monotherapy and add-on therapy in adults and children 4 years of age and older. Despite being structurally related to carbamazepine, oxcarbazepine differs substantially in its pharmacokinetic and safety profile; oxcarbazepine has a much lower risk of pharmacokinetic drug–drug interactions than carbamazepine. Carbamazepine has also been shown to induce the hepatic synthesis of sex hormone-binding globulin, thus reducing free serum testosterone levels and possibly causing erectile dysfunction (ED) in some men; these effects have not been observed with oxcarbazepine. This paper provides a discussion of recent clinical experience with men who presented in private clinical practice with complaints of ED while being treated with carbamazepine for seizure disorders. The four illustrative case studies presented in this report suggest that switching AED treatment from carbamazepine to oxcarbazepine in men with epilepsy can reduce the ED side effects observed with carbamazepine.     

高效液相法同时测定血清中卡马西平、苯妥英钠、苯巴比妥的实验方法学研究

【摘要】目的建立高效液相色谱／二极管阵列同时测定血清中卡马西平、苯妥英钠、苯巴比妥含量的检测法。方法以600μl乙酸乙酯为萃取溶剂;样品用量0．2ml血清,萃取时间3min,以3500r／min速度离心4min,取400txl萃取剂于75℃水浴中挥发至干;用1．0ml流动相溶解残留物,10000r／min离心20min后进样分析。分析条件：柱温30℃,流动相（甲醇：水=60：40）,波长254nm,实现了3种药物的有效分离。结果在优化条件下,3种待测组分在1．52～120mg／L范围内呈线性,相关系数（r）≥0．999,检出限（S／N=3）为0．4—1．5mg／L,样品的平均加标回收率为91．3％～111％,相对标准偏差（RSD）〈5％。结论该方法确定了最佳样品预处理条件,优化了色谱分离及检测条件,灵敏、准确,能够满足血清中抗癫痫药物浓度的监测要求。     

卡马西平过量致偏瘫和偏身感觉障碍

1例51岁女性三叉神经痛患者I：3服卡马西平（0．2g,3次／d）治疗约1年,因疼痛加重1d内累积服用卡马西平2g,第2天在口服卡马西平0．4g之后出现头晕、视物模糊和右侧肢体麻木、无力,遂入院。人院后体格检查：右侧中枢性面舌瘫,咽反射消失,右侧肢体肌力为Ⅳ级,右侧面部及肢体痛觉减退。头部磁共振成像和弥散加权磁共振成像检查未见异常。停用卡马西平,同时给予改善循环药物治疗。4d后患者完全恢复正常。     

Effects of Anticonvulsants on Cell Growth and Enzymatic and Receptor Binding Activity in a Neuroblastoma X Glioma Hybrid Cell Culture

Summary: : The effects of anticonvulsants on markers of growth, intracellular enzymes, and synaptic functions were evaluated using a rapidly dividing cholinergic neuroblastoma x glioma hybrid cell-line (NG108-15). Cell cultures were exposed for 4 days to phenobarbital, phenytoin, carbamazepine, or valproic acid. Anticonvulsant concentrations added to the media were selected to produce free levels in the cell media that were equivalent to free levels in humans ranging from therapeutic to very toxic. Free levels of anticonvulsants in the toxic range affected cell number, protein content, and neurochemical markers. However, only valproic acid and phenytoin reduced cell growth at therapeutic free drug concentrations. Valproic acid was the only medication to act as a differentiating agent, significantly increasing the activity of choline acetyl transferase, (3-galactosidase, and muscarinic cholinergic receptor binding. These results emphasize the importance of performing drug studies at appropriate free drug concentrations and suggest that valproic acid differs from other commonly prescribed anticonvulsants by having both a growth-suppressing and a differentiating effect.     

Using cold plasma to treat warts in children: A case series

Treatment of warts is especially challenging in the pediatric patient population because of the pain associated with many of available treatments. Cold atmospheric pressure plasma is a novel treatment with expanding clinical uses for a variety of skin conditions. In this case series, we present five pediatric patients who achieved full clearance of warts with cold plasma treatment. While further studies are needed, these results are promising because of the efficacy and entirely painless nature of this treatment modality.