新多巴胺受体激动剂甲磺酸培高利特  

PERGOLIDE MESYLATE——A NEW DOPAMINE RECEPTOR AGONIST

作　　者：唐怡勤[1] 魏月芳[1] 曹立文 

机构地区：[1]国家医药管理局天津药物研究院

出　　处：《中国新药杂志》1998年第5期348-350,共3页Chinese Journal of New Drugs

摘　　要：目的：简述甲磺酸培高利特的药理活性和临床疗效。方法：临床前药理研究主要与溴隐亭进行比较。Ⅰ期临床：对１７例健康自愿受试者耐受性和血催乳素作用进行研究。临床试验：２６２例帕金森患者合并美多巴用药６周；１３５例高催乳素患者用药３周与溴隐亭比较。结果：药理评价显示甲磺酸培高利特是一典型Ｄ受体激动剂。帕金森病治疗，随机双盲临床试验显示合用美多巴比安慰剂合用美多巴更为有效（Ｐ＜０．０１）；治疗高催乳素血症显示０．０５～０．１５ｍｇ／ｄ与溴隐亭２．５～１０ｍｇ／ｄ作用相等（Ｐ＞０．０５）。OBJECTIVE:Briefly reviewing the pharmacological action and clinical effect of pergolide mesylate,a DA receptor agonist.METHODS:Preclinical pharmacological studies were performed mainly in comparison with Bromocriptine.Phase I clinical study was carried out on 17 healthy volunturs to assess tolerability and effect on flasma prolactin.Clinical trials were carried out on 262 cases of Parkinsons disease in combination with madopar for 6 weeks,and 135 cases of hyperprolactrinemia in comparison with bromocriptine for 3 months.RESULTS:Pharmacological evaluation showed that Pergolide mesylate is a specific dopminergic DA receptor agonist.Randomized double blind clinical trial on Parkinsons disease in combination with madopar showed highly significant more potent therapeutic effect(P<0.01)as compared with placedo+madopar.Effect on hyperprolactinemia showed that a dose of 0.05～0.15 mg/d of pergolide mesylate is equivalent to 2.5～10 mg/d of bromocriptine (P>0.05).CONCLUSION:Pergolide mesylate proved to be an effective drug for the treatment of Parkinsons disease and hyperprolactinemia,with less adverse side effects.

关 键 词：甲磺酸培高利特 帕金森病 多巴胺受体 激动剂 

分 类 号：R971.9[医药卫生—药品]