英文药名: Requip XL (Ropinirole XL Tablets)

中文药名: 罗匹尼罗缓释片

生产厂家: Glaxo Smith Kline

药品简介

葛兰素史克公司（GSK）近日宣布，罗匹尼罗缓释片（ropinirole，Requip XL）用于治疗先天性帕金森病已在美国获得批准，本品由此成为首个一日1次口服治疗帕金森病的非麦角多巴胺激动剂。
帕金森病患者用药，当药物作用减弱时会出现症状复发的情况，III期临床研究结果显示在患者已使用的左旋多巴疗法基础上联用本品可减少患者症状不受控制的时间，研究中显示每天平均可减少2.1小时的症状不受控制时间。 　　
GSK公司表示，许多患者使用抗帕金森病药物时，每天需要多次服用，而在正确的时间服药对患者来说是个挑战，而且有的患者行动受限不方便自己服用。每天用药1次的Requip XL可使有效成分平稳释放，给患者带来方便。

Important Safety Information About REQUIP XL

Prescription REQUIP XL is not for everyone. REQUIP XL may cause you to fall asleep or feel very sleepy during normal activities such as driving; or to faint or feel dizzy, nauseated, or sweaty when you stand up. Tell your doctor if you experience these or the following problems, or if you drink alcohol or are taking other medicines that make you drowsy. Side effects may include nausea, dizziness, drowsiness or sleepiness, headache, and sudden uncontrolled movements (dyskinesia). Increase or decrease in blood pressure and heart rate may occur. Hallucinations may occur at any time during treatment. Also tell your doctor if you experience new or increased gambling, sexual, or other intense urges while taking REQUIP XL. REQUIP XL may increase the side effects of L-dopa. Most patients were not bothered enough to stop taking REQUIP XL.
DRUG DESCRIPTION
REQUIP (ropinirole) is an orally administered non-ergoline dopamine agonist. It is supplied as the hydrochloride salt of ropinirole 4-[2-(dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one and has an empirical formula of C16H24N2O?HCl. The molecular weight is 296.84 (260.38 as the free base).
Ropinirole hydrochloride is a white to yellow solid with a melting range of 243° to 250°C and a solubility of 133 mg/mL in water. REQUIP XL Extended-Release Tablets are formulated as a three-layered tablet with a central, active-containing, slow-release layer, and 2 placebo outer layers acting as barrier layers which control the surface area available for drug release. Each biconvex, capsule-shaped tablet contains 2.28 mg, 4.56 mg, 6.84 mg, 9.12 mg, or 13.68 mg ropinirole hydrochloride equivalent to ropinirole 2 mg, 4 mg, 6 mg, 8 mg, or 12 mg, respectively. Inactive ingredients consist of carboxymethylcellulose sodium, colloidal silicon dioxide, glyceryl behenate, hydrogenated castor oil, hypromellose, lactose monohydrate, magnesium stearate, maltodextrin, mannitol, povidone, and one or more of the following: FD&C Yellow No. 6 aluminum lake, FD&C Blue No. 2 aluminum lake, ferric oxides (black, red, yellow), polyethylene glycol 400, titanium dioxide.

INDICATIONS
Parkinson's Disease
REQUIP XL (ropinirole extended-release tablets) is indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease.
DOSAGE AND ADMINISTRATION
General Dosing Considerations
REQUIP XL Extended-Release Tablets are taken once daily, with or without food. Taking REQUIP XL with food may reduce the occurrence of nausea; this has not been established in controlled clinical trials [see CLINICAL PHARMACOLOGY].
Tablets must be swallowed whole and must not be chewed, crushed, or divided.
If a significant interruption in therapy with REQUIP XL has occurred, retitration of therapy may be warranted.
Dosing for Parkinson's Disease
The starting dose is 2 mg taken once daily for 1 to 2 weeks, followed by increases of 2 mg/day at 1-week or longer intervals as appropriate, depending on therapeutic response and tolerability, up to a maximally recommended dose of 24 mg/day.

In clinical trials, dosage was initiated at 2 mg/day and gradually titrated based on individual therapeutic response and tolerability. Doses greater than 24 mg/day have not been studied in clinical trials. Patients should be assessed for therapeutic response and tolerability at a minimal interval of 1 week or longer after each dose increment. Caution should be exercised during dose titration because too rapid a rate of titration may lead to dose selection that may not provide additional benefit, but that may increase the risk of adverse reactions [see Clinical Studies]. Due to the flexible dosing design used in clinical studies, specific dose response information could not be determined.

When REQUIP XL is administered as adjunct therapy to L-dopa, the concurrent dose of L-dopa may be decreased gradually as tolerated. In the placebo-controlled advanced Parkinson's disease study, the L-dopa dose was reduced once patients reached a dose of REQUIP XL of 8 mg/day. Overall, L-dopa dose reduction was sustained in 93% of patients treated with REQUIP XL and in 72% of patients on placebo. On average the L-dopa dose was reduced by 34% in patients treated with REQUIP XL [see Clinical Studies]. REQUIP XL should be discontinued gradually over a 7–day period.
Following conversion to REQUIP XL, the dose may be adjusted depending on therapeutic response and tolerability [see DOSAGE AND ADMINISTRATION].
HOW SUPPLIED
Dosage Forms And Strengths
2 mg, pink, biconvex, capsule-shaped, film-coated, tablets debossed with “GS” and “3V2”
4 mg, light brown, biconvex, capsule-shaped, film-coated, tablets debossed with “GS” and “WXG”
6 mg, white, biconvex, capsule-shaped, film-coated, tablets debossed with "GS" and "11F"
8 mg, red, biconvex, capsule-shaped, film-coated, tablets debossed with “GS” and “5CC”
12 mg, green, biconvex, capsule-shaped, film-coated, tablets debossed with "GS" and "YX7"
Each biconvex, capsule-shaped, film-coated tablet contains ropinirole hydrochloride equivalent to the labeled amount of ropinirole as follows:

2 mg: pink tablets debossed with “GS” and “3V2”, in bottles of 30 (NDC 0007–4885–13) and 90 (NDC 0007-4885-59).
4 mg: light brown tablets debossed with “GS” and “WXG”, in bottles of 30 (NDC 0007–4887–13) and 90 (NDC 0007-4887-59).
6 mg: white tablets debossed with "GS" and "11F", in bottles of 30 (NDC 0007-4883-13) and 90 (NDC 0007-4883-59).
8 mg: red tablets debossed with “GS” and “5CC”, in bottles of 30 (NDC 0007-4888-13) and 90 (NDC 0007-4888-59).
12 mg: green tablets debossed with "GS" and "YX7", in bottle of 30 (NDC 0007-4882-13).
Storage
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].

SIDE EFFECTS
The following adverse reactions are described in more detail in the WARNINGS AND PRECAUTIONS section of the label:

Falling asleep during activities of daily living
Syncope
Symptomatic hypotension, hypotension, postural/orthostatic hypotension
Elevation of blood pressure and changes in heart rate
Hallucination
Dyskinesia
Major psychotic disorders
Events with dopaminergic therapy
Retinal pathology
Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug (or of another development program of a different formulation of the same drug) and may not reflect the rates observed in practice.

During the premarketing development of REQUIP XL, patients with advanced Parkinson's disease received REQUIP XL or placebo as adjunctive therapy in 1 clinical trial. In a second trial, patients with early Parkinson's disease were treated with REQUIP XL or the immediate-release formulation of REQUIP without L-dopa.

于2011-01-20更新