Requip: Restoring Motor Control in Parkinson's Disease
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Synonyms | |||
Requip (ropinirole hydrochloride) is a non-ergoline dopamine agonist indicated for the treatment of Parkinson’s disease and moderate-to-severe primary Restless Legs Syndrome. As a therapeutic agent targeting dopaminergic pathways, it serves as both monotherapy in early disease stages and adjunctive therapy with levodopa throughout the progression of Parkinsonism. Its mechanism of action involves direct stimulation of dopamine receptors in the striatum, mimicking endogenous dopamine effects to ameliorate motor symptoms. Clinicians value its efficacy in improving motor fluctuations and reducing “off” time in patients experiencing levodopa-related wearing-off phenomena.
Features
- Active pharmaceutical ingredient: Ropinirole hydrochloride
- Available in immediate-release and extended-release (Requip XL) tablet formulations
- Dosage strengths: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg, and 5 mg immediate-release; 2 mg, 4 mg, 6 mg, 8 mg, and 12 mg extended-release
- Selective D2-like receptor agonist with high affinity for D3 receptors
- Extensive hepatic metabolism primarily via CYP1A2 isoenzyme
- Elimination half-life of approximately 6 hours (immediate-release) and 15 hours (extended-release)
- Bioavailability of approximately 50% (immediate-release) with linear pharmacokinetics
Benefits
- Significant improvement in Unified Parkinson’s Disease Rating Scale (UPDRS) scores
- Reduction in “off” time and increased “on” time without troublesome dyskinesias in advanced Parkinson’s disease
- Effective control of sensorimotor symptoms in Restless Legs Syndrome, improving sleep quality
- Lower incidence of fibrosis-related adverse reactions compared to ergot-derived dopamine agonists
- Flexible dosing regimens allowing for individualized titration based on therapeutic response
- Demonstrated efficacy as both monotherapy and adjunctive treatment throughout disease progression
Common use
Requip is primarily prescribed for the management of idiopathic Parkinson’s disease signs and symptoms, including bradykinesia, rigidity, tremor, and postural instability. In clinical practice, it is utilized across various disease stages—as initial monotherapy in early Parkinson’s disease to delay levodopa initiation, and as combination therapy with levodopa in more advanced stages to smooth motor fluctuations. For Restless Legs Syndrome, it is indicated for patients experiencing moderate-to-severe symptoms that significantly impair sleep or daytime functioning. The medication is particularly valuable for patients who develop motor complications with levodopa or those requiring dopamine agonist therapy without the fibrotic risks associated with ergot derivatives.
Dosage and direction
Parkinson’s Disease: Initiate with 0.25 mg three times daily for immediate-release tablets. Based on therapeutic response and tolerability, increase by 0.25 mg/dose every week to achieve 3 mg/day, then by 1.5 mg/day weekly until reaching 9 mg/day, and thereafter by 3 mg/day weekly. Maintenance dose typically ranges between 3-9 mg daily in three divided doses for immediate-release, with maximum recommended dose of 24 mg/day. For extended-release tablets, begin with 2 mg once daily for 1-2 weeks, increasing by 2 mg/day at weekly intervals to effective dose, usually 8-24 mg daily.
Restless Legs Syndrome: Initiate with 0.25 mg once daily 1-3 hours before bedtime. After two days, increase to 0.5 mg daily, then to 1 mg daily by the end of the first week. May further titrate upward by 0.5 mg weekly to maximum of 4 mg daily based on therapeutic response.
All doses should be taken with food to minimize nausea. Dose adjustments require careful monitoring for orthostatic hypotension and sedation. For patients with hepatic impairment, dosage reduction may be necessary.
Precautions
Patients should be cautioned about the potential for sudden sleep onset during activities of daily living, including operation of motor vehicles. Orthostatic hypotension may occur particularly during dose titration; blood pressure monitoring is recommended. Dopamine agonists have been associated with impulse control disorders including pathological gambling, increased libido, hypersexuality, compulsive spending, binge eating, and other intense urges. Patients should be monitored for development of these behaviors. Augmentation of Restless Legs Syndrome symptoms may occur with long-term treatment, characterized by earlier onset of symptoms, increased intensity, or spread to other limbs. Fibrotic complications including pleural effusion, pleural fibrosis, and cardiac valvulopathy have been reported with dopamine agonists; although less common with non-ergot derivatives like ropinirole, monitoring remains advised. Hallucinations and psychotic-like behaviors may emerge, particularly in elderly patients with Parkinson’s disease.
Contraindications
Requip is contraindicated in patients with known hypersensitivity to ropinirole or any component of the formulation. Concomitant use with antipsychotics that are dopamine antagonists (such as phenothiazines, butyrophenones, thioxanthenes) is contraindicated due to mutual antagonism of therapeutic effects. Severe hepatic impairment necessitates avoidance or extreme caution due to significantly reduced clearance. The medication is contraindicated in patients with a history of syncope associated with dopaminergic therapy. Patients with major psychotic disorders should not receive Requip due to risk of exacerbating psychiatric symptoms.
Possible side effect
Very common (≥10%): Nausea, dizziness, somnolence, sudden sleep attacks, syncope Common (1-10%): Vomiting, fatigue, peripheral edema, abdominal pain, constipation, orthostatic hypotension, hallucinations, confusion, impulse control disorders, dyskinesias, headache Uncommon (0.1-1%): Hypertension, atrial fibrillation, palpitations, visual disturbances, nightmares, amnesia, hyperhidrosis, elevated liver enzymes, weight changes Rare (<0.1%): Allergic reactions, bronchospasm, angioedema, fibrotic complications, neuroleptic malignant syndrome (upon abrupt withdrawal), pathological gambling, hypersexuality Post-marketing reports: Psychotic symptoms, compulsive behaviors, increased libido, binge eating, priapism
Drug interaction
Strong CYP1A2 inhibitors (fluvoxamine, ciprofloxacin) may significantly increase ropinirole exposure, requiring dose reduction. Estrogens may decrease ropinirole clearance by approximately 30%; dose adjustment may be needed when initiating or discontinuing estrogen therapy. Dopamine antagonists (metoclopramide, antipsychotics) may diminish efficacy of ropinirole. CNS depressants (alcohol, benzodiazepines, opioids) may potentiate sedative effects. Drugs affecting blood pressure may exacerbate orthostatic hypotension. Levodopa/carbidopa coadministration may increase the incidence of dyskinesias and hallucinations. Smoking may increase ropinirole clearance due to CYP1A2 induction.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed dose. For the extended-release formulation, if missed within 12 hours of the usual dosing time, the dose should be taken immediately. If beyond 12 hours, the missed dose should be skipped and the next dose taken at the regular time.
Overdose
Symptoms may include nausea, vomiting, dizziness, visual hallucinations, hyperhidrosis, claustrophobia, choreiform dyskinesias, palpitations, arrhythmias, sedation, and orthostatic hypotension. Cases of syncope and convulsions have been reported. General supportive measures should be implemented along with cardiac monitoring. Gastrointestinal decontamination may be considered if presented early. Dopamine antagonists such as neuroleptics should be avoided as they may exacerbate Parkinsonian symptoms. Hemodialysis is unlikely to be beneficial due to extensive protein binding and large volume of distribution.
Storage
Store at 20-25°C (68-77°F) with excursions permitted between 15-30°C (59-86°F). Protect from light and moisture. Keep in original container with lid tightly closed. Do not remove desiccant from bottle. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Do not transfer tablets to other containers as this may affect stability.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Individual patient responses to medication may vary. Treatment decisions should be made in consultation with a qualified healthcare professional who can consider the patient’s complete medical history, current medications, and specific clinical circumstances. The prescribing physician should be familiar with the complete prescribing information and latest clinical guidelines. Patients should not discontinue or adjust medication without medical supervision due to risk of withdrawal symptoms or disease exacerbation.
Reviews
Clinical studies demonstrate that approximately 60-70% of Parkinson’s disease patients experience significant improvement in motor symptoms with ropinirole therapy. In randomized controlled trials, adjunctive ropinirole reduced “off” time by 1.5-2.1 hours daily compared to placebo. For Restless Legs Syndrome, over 75% of patients report meaningful symptom improvement based on validated rating scales. Long-term extension studies show maintained efficacy for up to 5 years in Parkinson’s disease, though some patients may require additional levodopa over time. Patient satisfaction surveys indicate improved quality of life measures particularly regarding mobility and sleep parameters. The extended-release formulation receives higher adherence ratings due to once-daily dosing convenience while maintaining therapeutic efficacy comparable to the immediate-release formulation administered three times daily.