Ropinirole

Ropinirole is a non-ergoline dopamine agonist. The precise mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, although it is thought to be related to its ability to stimulate dopamine D2 receptors within the caudate-putamen in the brain.

• Ropinirole Tablets are a non-ergoline dopamine agonist indicated for the treatment of Parkinson’s disease (PD) and moderate-to-severe primary Restless Legs Syndrome (RLS). (1.1, 1.2).ICD-10: G25.81

• Ropinirole tablets are contraindicated in patients known to have a hypersensitivity/allergic reaction (including urticaria, angioedema, rash, pruritus) to ropinirole or to any of the excipients.contraindicated

· Ropinirole tablets can be taken with or without food. (2.1) · Retitration of ropinirole tablets may be warranted if therapy is interrupted. (2.1) Parkinson’s Disease: · The recommended starting dose is 0.25 mg taken three times daily; titrate to a maximum daily dose of 24 mg. (2.2) · Renal Impairment: The maximum recommended dose is 18 mg/day in patients with end-stage renal disease on hemodialysis. (2.2) Restless Legs Syndrome: · The recommended starting dose is 0.25 mg once daily, 1 to 3 hours before bedtime, titrate to a maximum recommended dose of 4 mg daily. (2.3) · Renal Impairment: The maximum recommended dose is 3 mg/day in patients with end-stage renal disease on hemodialysis. (2.3) 2.1 General Dosing Recommendations Ropinirole tablets can be taken with or without food [see Clinical Pharmacology (12.3)] . If a significant interruption in therapy with ropinirole tablets have occurred, retitration of therapy may be warranted. 2.2 Dosing for Parkinson's Disease Week Dosage Total Daily Dose 1 0.25 mg 3 times daily 0.75 mg 2 0.5 mg 3 times daily 1.5 mg 3 0.75 mg 3 times daily 2.25 mg 4 1 mg 3 times daily 3 mg Ropinirole tablets should be discontinued gradually over a 7-day period in patients with Parkinson’s disease [see Warnings and Precautions (5.8)]. The frequency of administration should be reduced from three times daily to twice daily for 4 days. For the remaining 3 days, the frequency should be reduced to once daily prior to complete withdrawal of ropinirole tablets.

· Sudden onset of sleep and somnolence may occur (5.1) · Syncope may occur (5.2) · Hypotension, including orthostatic hypotension may occur (5.3) · May cause hallucinations and psychotic-like behaviors (5.4) · May cause or exacerbate dyskinesia (5.5) · May cause problems with impulse control or compulsive behaviors (5.6) 5.1 Falling Asleep during Activities of Daily Living and Somnolence Patients treated with ropinirole tablets have reported falling asleep while engaged in activities of daily living, including driving or operating machinery, which sometimes resulted in accidents. Although many of these patients reported somnolence while on ropinirole tablets, some perceived that they had no warning signs, such as excessive drowsiness, and believed that they were alert immediately prior to the event. Some have reported these events more than 1 year after initiation of treatment. In controlled clinical trials, somnolence was commonly reported in patients receiving ropinirole tablets and was more frequent in Parkinson's disease (up to 40% ropinirole tablets, 6% placebo) than in Restless Legs Syndrome (12% ropinirole tablets, 6% placebo) [see Adverse Reactions (6.1)] . It has been reported that falling asleep while engaged in activities of daily living usually occurs in a setting of pre-existing somnolence, although patients may not give such a history. For this reason, prescribers should reassess patients for drowsiness or sleepiness, especially since some of the events occur well after the start of treatment.

The following adverse reactions are described in more detail in other sections of the label: Hypersensitivity [see Contraindications (4)] Falling asleep during activities of daily living and somnolence [see Warnings and Precautions (5.1)] Syncope [see Warnings and Precautions (5.2)] Hypotension/orthostatic hypotension [see Warnings and Precautions (5.3)] Hallucinations/psychotic-like behavior [see Warnings and Precautions (5.4)] Dyskinesia [see Warnings and Precautions (5.5)] Impulse control/compulsive behaviors [see Warnings and Precautions (5.6)] Withdrawal-emergent hyperpyrexia and confusion [see Warnings and Precautions (5.7)] Withdrawal Symptoms [see Warnings and Precautions (5.8)] Augmentation and early-morning rebound in RLS [see Warnings and Precautions (5.9)] Fibrotic complications [see Warnings and Precautions (5.10)] Retinal pathology [see Warnings and Precautions (5.11)] Most common adverse reactions (incidence with ropinirole tablets at least 5% greater than placebo) in the respective indications were: Early PD: Nausea, somnolence, dizziness, syncope, asthenic condition, viral infection, leg edema, vomiting, and dyspepsia. (6.1) Advanced PD: Dyskinesia, somnolence, nausea, dizziness, confusion, hallucinations, sweating, and headache. (6.1) RLS: Nausea, vomiting, somnolence, dizziness, and asthenic condition. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Alembic Pharmaceuticals Limited at 1-866-210-9797 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Pregnancy: Based on animal data, may cause fetal harm. (8.1) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of ropinirole tablets in pregnant women. In animal studies, ropinirole had adverse effects on development when administered to pregnant rats at doses similar to (neurobehavioral impairment) or greater than (teratogenicity and embryolethality at >36 times) the maximum recommended human dose (MRHD) for Parkinson’s disease. Ropinirole doses associated with teratogenicity and embryolethality in pregnant rats were associated with maternal toxicity. In pregnant rabbits, ropinirole potentiated the teratogenic effects of L-dopa when these drugs were administered in combination [see Data] . In the U.S. general population, the estimated background risk of major birth defects and of miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. The background risk of major birth defects and miscarriage in the indicated populations is unknown. Data Animal Data : Oral administration of ropinirole (0, 20, 60, 90, 120, or 150 mg/kg/day) to pregnant rats during organogenesis resulted in embryolethality, increased incidence of fetal malformations (digit, cardiovascular, and neural tube defects) and variations, and decreased fetal weight at the two highest doses.

Metabolism

Ropinirole displayed linear kinetics over the dosing range of 1 to 8 mg three times daily. Steady-state concentrations are expected to be achieved within 2 days of dosing.

The symptoms of overdose with ropinirole tablets are related to its dopaminergic activity. General supportive measures are recommended. Vital signs should be maintained, if necessary. In the clinical trials, there have been patients who accidentally or intentionally took more than their prescribed dose of ropinirole. The largest overdose reported with ropinirole in clinical trials was 435 mg taken over a 7-day period (62.1 mg/day). Of patients who received a dose greater than 24 mg/day, reported symptoms included adverse events commonly reported during dopaminergic therapy (nausea, dizziness), as well as visual hallucinations, hyperhidrosis, claustrophobia, chorea, palpitations, asthenia, and nightmares. Additional symptoms reported in cases of overdose included vomiting, increased coughing, fatigue, syncope, vasovagal syncope, dyskinesia, agitation, chest pain, orthostatic hypotension, somnolence, and confusional state.

• May 5, 2008ANDAANDA078110Prinston Inc
• Feb 25, 2010ANDAANDA090135Glenmark Pharms Ltd
• Mar 24, 2010ANDAANDA090429Alembic Ltd
• Feb 7, 2012ANDAANDA079165Mlv
• May 17, 2012ANDAANDA090869Actavis Elizabeth
• Jun 6, 2012ANDAANDA201576Dr Reddys Labs Ltd
• Nov 28, 2012ANDAANDA079229Orbion Pharms
• Apr 22, 2013ANDAANDA202786Alembic

1. 1Drug Ineffective1,3967.7%
2. 2Fall1,2216.7%
3. 3Fatigue1,1716.4%
4. 4Nausea1,1166.1%
5. 5Dizziness8834.8%
6. 6Hallucination8694.8%
7. 7Pain7824.3%
8. 8Dyspnoea7694.2%
9. 9Diarrhoea7494.1%
10. 10Death7374.0%
11. 11Asthenia7324.0%
12. 12Headache6823.7%
13. 13Off Label Use6673.7%
14. 14Insomnia6623.6%
15. 15Somnolence6263.4%

The 10 most recently updated of 80 ClinicalTrials.gov registrations naming Ropinirole as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Infusion of Apomorphine: Long-term Safety Study
  Active not recruiting · Phase 3 · Interventional · 99 enrolled · MDD US Operations, LLC a subsidiary of Supernus Pharmaceuticals
  NCT02339064updated 2025-06-19
• Gait Analysis in Neurological Disease
  Recruiting · Observational · 120 enrolled · Beth Israel Deaconess Medical Center
  NCT02994719updated 2025-06-08
• Impact of Switching to Continuous Release Dopamine Agonists
  Completed · Phase 3 · Interventional · 11 enrolled · University of Toledo
  NCT00465452updated 2025-05-16
• Exercise Training Versus Ropinirole in Treating Restless Legs Syndrome Among Hemodialysis Patients
  Completed · Interventional · 84 enrolled · Lahore General Hospital
  NCT06468371updated 2024-06-21
• Treatment of Hyperprolactinemia With the Non-ergoline Dopamine Agonist Ropinirole
  Completed · Phase 1 · Phase 2 · Interventional · 16 enrolled · Columbia University
  NCT03038308updated 2024-06-04
• Butrans for Treatment of Restless Legs Syndrome
  Withdrawn · Phase 4 · Interventional · 0 enrolled · Massachusetts General Hospital
  NCT02138357updated 2023-10-25
• Relative Bioavailability Study of Ropinirole Implants in Parkinson's Patients on L-Dopa Switched From Oral Ropinirole
  Terminated · Phase 1 · Phase 2 · Interventional · 6 enrolled · Titan Pharmaceuticals
  NCT03250117updated 2023-05-06
• Ropinirole for the Treatment of Muscle Cramps in Patients With Cirrhosis
  Completed · Phase 4 · Interventional · 31 enrolled · Vanderbilt University Medical Center
  NCT03176966updated 2022-10-31
• DIalysis Symptom COntrol-Restless Legs Syndrome Trial
  Completed · Phase 3 · Interventional · 52 enrolled · Population Health Research Institute
  NCT03806530updated 2022-09-21
• Effectiveness of Ropinirole and Gabapentin for the Treatment of RLS in Patients on Maintenance HD
  Terminated · Phase 2 · Interventional · 3 enrolled · University of Alberta
  NCT03708237updated 2022-07-12

Frequently asked questions

How does Ropinirole work?

Ropinirole is a non-ergoline dopamine agonist. The precise mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, although it is thought to be related to its ability to stimulate dopamine D2 receptors within the caudate-putamen in the brain.

What is Ropinirole used for?

According to FDA labeling, Ropinirole carries indications including: Ropinirole Tablets are a non-ergoline dopamine agonist indicated for the treatment of Parkinson’s disease (PD) and moderate-to-severe primary Restless Legs Syndrome (RLS). (1.1, 1.2).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ropinirole?

Ropinirole is classified as Dopamine agonists, Nonergot Dopamine Agonist, Dopamine Agonists, Increased Central Nervous System Dopamine Activity.

What are the contraindications for Ropinirole?

Ropinirole labeling lists contraindications including: Ropinirole tablets are contraindicated in patients known to have a hypersensitivity/allergic reaction (including urticaria, angioedema, rash, pruritus) to ropinirole or to any of the excipients.. Always consult the full prescribing information and a clinician.