- 期刊
羅匹尼羅氯化氫（力必平）：第二代抗柏金森疾病之非麥角鹼多巴胺接受體促進劑
Ropinirole Hydrochloride (Requip): The Second Generation of nonergot-derivative Dopamine Receptor Agonist against Parkinsonism
摘要
為了藥品安全和增加治療效果，非麥角鹼類在柏金森疾病和其他運動障礙被廣泛研究，在第二代非麥角鹼類多巴胺接受體促進劑中，目前在臺灣已經上市，以羅匹尼羅氯化氫（力必平）為代表，其主要藥理機轉為活化基底核處突觸後多巴胺D2接受體。目前，力必平在臺灣是被核准使用在柏金森疾病和腳不寧靜症候羣病人，其他報告有頑固性憂鬱、纖維肌肉疼痛、注意力缺乏過動兒、週期性肢體運動、Gilles de la Tourette等。力必平在服用後二天即達到藥物濃度，在血中之半衰期為6小時，主要在肝經由細胞色素CYP1A2代謝，其88%代謝物經由尿液排出。腎肌酐清除率至30毫升／分鐘對時力必平之代謝沒有影響。力必平對早期柏金森疾病之正面貢獻為可當作單一治療劑、延後使用左多巴之時間、較少出現不良運動事件、和取代低量左多巴治療。其對後期柏金森疾病合併治療之正面貢獻為增加抗柏金森疾病運動效果、改善其他神經精神症狀、降低對左多巴之需求、和減少異動症事件發生。雖然力必平比較麥角鹼類藥物少有嚴重副作用，但偶有脚水腫、昏厥、噁心、嘔吐、頭暈、疲倦、多睡和視幻覺之情形出現。力必平生產甘胱谷，故被認為擁有神經保護作用。在老年患者由於藥品廓清率可能減少15-30%，劑量頇視臨床藥效調整。在人類並沒有傳出胎兒畸形事件和對母乳有明顯影響，但是衛生單位基於安全，仍然奉勸小心使用。直至目前，並沒有關於力必平之偽藥報告或藥害救濟申請案例。
並列摘要
Because of drug safety and efficiency, non-ergoline derivatives are extensively investigated in Parkinson's disease and related movement disorders. Ropinirole hydrochloride (Requip) is the most common second generation of non-ergoline dopamine agonist marketed in Taiwan. Its pharmacological action is to activate the postsynaptic dopamine-2 receptor in striatum. Currently, requip is licensed for Parkinson’s disease and restless leg syndrome in Taiwan, but it also shows benefit for refractory depression, fibromyalgia, attention-deficient hyperactivity, periodic leg movement and Gilles de la Tourette syndrome. Its steady state concentration is obtained two days after treatment and biological half-life in blood is 6 hours. It is metabolized in liver by the cytochrome CYP1A2 and about 88% of metabolites are excreted via urine. Its metabolism does not change when creatinine clearance is above 30 ml/min. The benefit of requip in early Parkinson’s disease includes a monotherapy agent, a delay use of L-dopa, a less frequent onset of dyskinesia and a replacement of low-dose L-dopa. A combined use with L-dopa in advanced Parkinson’s disease enhances the motor improvement, corrects a few neuropsychiatric symptoms, reduces the dose of L-dopa, and decreases the frequency of dyskinesia. Although the frequency of side effect of requip is less than ergot-derivative dopamine agonists, leg edema, syncope, nausea, vomiting, dizziness, asthenia, somnolence and halluicnosis sometimes occur. Neuroprotection is considered due to an activation of glutathione. In elderly, a scheduled dose is suggested as drug clearance decreases 15-30%. In human, fetal deformity or adverse breastfeeding event has not been reported. In so far, there is no fake medicine or drug relief reported in Taiwan.