葛兰素史克公司近日宣布，美国FDA已批准Requip XL(ropinirole)长效片剂用于原发性帕金森病症状及体征的治疗。这也是FDA目前批准的唯一一种口服用药一日一次治疗帕金森病的非麦角碱类药物。
当使用的药物疗效退去，帕金森病患者通常会经历一种症状复发的所谓“关期(off)”，运动迟缓、震颤、僵直使这些患者即使完成简单的活动和运动都变得很难。一项重要的疗效及安全性评价试验结果显示，与基线状态相比，将长效ropinirole加入病人正在使用的多巴胺疗法中能够将患者的“关期”平均减少2.1小时。如果与安慰剂对照组相比，多巴胺+长效ropinirole治疗组病人关期的减少更具显著性差异，平均达到1.7小时。
FDA对该药的批准主要以一项名为EASE-PD（治疗帕金森的疗效及安全）的辅助研究结果为基础。这项多中心双盲安慰剂对照研究对于多巴胺无法有效控制的原发性帕金森病患者进行了研究。结果如上文所述，患者的关期显著减短。
Generic Name for REQUIP XL
Ropinirole 2mg, 4mg, 6mg, 8mg, 12mg; ext-rel tabs.
Legal Classification:
Rx
Pharmacological Class for REQUIP XL
Dopamine agonist (non-ergot).
Manufacturer of REQUIP XL
GlaxoSmithKline Pharmaceuticals
Indications for REQUIP XL
Idiopathic Parkinson's disease.
Adult dose for REQUIP XL
Titrate gradually. Swallow whole. Taking with food may reduce nausea. Initially 2mg once daily for 1–2 weeks, then increase by 2mg/day at ≥1-week intervals to max 24mg/day. Switching from immediate-release ropinirole: give initial dose to closely match total daily dose of immediate-release form.
Children's dosing for REQUIP XL
Not recommended.
Also:
REQUIP
Warnings/Precautions for REQUIP XL
See literature. Consider discontinuing if excessive daytime sleepiness or if sudden onset of sleep during daily activities occurs. Monitor for drowsiness or sleepiness, and for orthostatic hypotension. Dyskinesia. Sleep disorders. Severe renal or hepatic impairment. Severe cardiovascular disease. Hypertension. Changes in heart rate. Psychotic disorders. Avoid abrupt cessation (withdraw over 1 week). Elderly may have higher risk of hallucinations. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interactions for REQUIP XL
Consider reducing concomitant levodopa dose. Alcohol, other CNS depressants may be potentiated. Potentiated by ciprofloxacin, possibly other CYP1A2 inhibitors. May be antagonized by dopamine antagonists (eg, phenothiazines, butyrophenones, metoclopramide). Adjust ropinirole dose if estrogens are added or discontinued. Monitor with drugs that induce CYP1A2 (eg, cigarette smoke).
Adverse Reactions for REQUIP XL
Early parkinsonism (without levodopa): Nausea, somnolence (including sudden sleep onset), abdominal pain/discomfort, dizziness, headache, constipation; dyskinesia, vomiting, syncope, fatigue, dyspepsia, infections, pain, sweating, asthenia, edema, postural hypotension, hypertension, changes in heart rate, pharyngitis, confusion, hallucinations, abnormal vision, aggravated parkinsonism. Advanced disease (with levodopa): also arthralgia, tremor, anxiety, dry mouth, hypokinesia, paresthesia.
How is REQUIP XL supplied?
Tabs—100; XL tabs (2mg, 4mg, 8mg)—30, 90; XL tabs (6mg, 12mg)—30
Related Disease:
Parkinsonism