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利舒脲经皮应用于普通狨猴中由1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)诱导的帕金森病以及帕金森病患者病例

[Dermal application of lisuride on parkinsonism induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in the common marmoset and on cases with Parkinson's disease].

作者信息

Nomoto M, Iwata S, Irifune M, Kaseda S, Osame M, Fukuda T

机构信息

Department of Pharmacology, Kagoshima University School of Medicine, Japan.

出版信息

Nihon Shinkei Seishin Yakurigaku Zasshi. 1998 Jun;18(3):81-7.

PMID:9800199
Abstract

Dermal administration is a nonoral drug delivery system that can keep the concentration of a drug in the body at a proper level for a long time. This is suitable especially in patients in the advanced stages of Parkinson's disease with a wearing-off phenomenon (short duration of effects on antiparkinsonian drugs), or in postoperative patients who cannot be treated with oral administration. We studied the effects of lisuride, a dopamine receptor agonist, in the dermal application on MPTP-treated common marmosets and on 5 patients with Parkinson's disease. Lisuride was applied to 4 x 5 cm of skin of the abdomen of monkeys. In patients with Parkinson's disease, lisuride was applied to the skin of the chest. The agent reversed akinesia of MPTP-treated animals within 30 min following the application and relieved the animal of parkinsonism for 5 days at a dose of 2 mg/kg. In patients, the dermal application of lisuride increased the duration of the ON period at doses of 1 to 2 mg/kg. These results suggest that the dermal application of lisuride is a useful treatment in parkinsonism.

摘要

皮肤给药是一种非口服给药系统,它能使药物在体内的浓度长时间维持在适当水平。这尤其适用于处于帕金森病晚期且出现疗效减退现象(抗帕金森病药物的作用持续时间短)的患者,或无法进行口服给药治疗的术后患者。我们研究了多巴胺受体激动剂利苏瑞得经皮肤给药对用MPTP处理的普通狨猴以及5例帕金森病患者的影响。将利苏瑞得涂于猴子腹部4×5平方厘米的皮肤上。对于帕金森病患者,将利苏瑞得涂于胸部皮肤。给药后30分钟内,该药物使经MPTP处理的动物的运动不能得到逆转,并且以2毫克/千克的剂量可使动物的帕金森症状缓解5天。在患者中,利苏瑞得经皮肤给药,剂量为1至2毫克/千克时,可延长“开”期的持续时间。这些结果表明,利苏瑞得经皮肤给药对帕金森病是一种有效的治疗方法。

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