Ropinirole

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 ) 1.1 Parkinson's Disease Ropinirole tablets are indicated for the treatment of Parkinson’s disease. 1.2 Restless Legs Syndrome Ropinirole tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS).

• Ropinirole tablets can be taken with or without food. • Retitration of ropinirole tablets may be warranted if therapy is interrupted
• Parkinson’s Disease: • The recommended starting dose is 0.25 mg taken three times daily; titrate to a maximum daily dose of 24 mg. • Renal Impairment: The maximum recommended dose is 18 mg/day in patients with end-stage renal disease on hemodialysis
• 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. • Renal Impairment: The maximum recommended dose is 3 mg/day in patients with end-stage renal disease on hemodialysis
• General Dosing Recommendations Ropinirole tablets can be taken with or without food [ see Clinical Pharmacology ]
• If a significant interruption in therapy with ropinirole tablets has occurred, retitration of therapy may be warranted
• Dosing for Parkinson's Disease The recommended starting dose of ropinirole tablets for Parkinson’s disease is 0.25 mg 3 times daily
• Based on individual patient therapeutic response and tolerability, if necessary, the dose should then be titrated with weekly increments as described in Table 1
• After Week 4, if necessary, the daily dose may be increased by 1.5 mg/day on a weekly basis up to a dose of 9 mg/day, and then by up to 3 mg/day weekly up to a maximum recommended total daily dose of 24 mg/day (8 mg 3 times daily)
• Doses greater than 24 mg/day have not been tested in clinical trials
• Table 1. …

• 0.25 mg: white to off-white, circular, beveled edged, biconvex film-coated tablets with ‘2’ over ‘53’ debossed on one side and ‘G’ on the other side • 0.5 mg: pale yellow to yellow, circular, beveled edged, biconvex film-coated tablets with ‘2’ over ‘54’ debossed on one side and ‘G’ on the other side • 1 mg: pale green to green, circular, beveled edged, biconvex film-coated tablets with ‘2’ over …

• Safety and effectiveness
• In pediatric patients have not been established

Dose adjustment is not necessary in elderly (65 years and older) patients, as the dose of ropinirole is individually titrated to clinical therapeutic response and tolerability. Pharmacokinetic trials conducted in patients demonstrated that oral clearance of ropinirole is reduced by 15% in patients older than 65 years compared with younger patients [ see Clinical Pharmacology ( 12.3 )]. …

• Advise the patient to read the FDA-approved patient labeling (Patient Information)
• Dosing Instructions Instruct patients to take ropinirole tablets only as prescribed
• If a dose is missed, advise patients not to double their next dose
• Ropinirole tablets can be taken with or without food [see Dosage and Administration ]
• Ropinirole is the active ingredient in ropinirole tablets (the immediate-release formulation)
• Ask your patients if they are taking another medication containing ropinirole. …

• 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
• History of hypersensitivity/allergic reaction (including urticaria, angioedema, rash, pruritus) to ropinirole or to any of the excipients. ()

• Inhibitors or inducers of CYP1A2: May alter the clearance of ropinirole; dose adjustment of ropinirole may be required. ( 7.1 , 12.3) • Hormone replacement therapy (HRT): Starting or stopping HRT may require dose adjustment of ropinirole. ( 7.2 , 12.3 ) • Dopamine antagonists (e.g., neuroleptics, metoclopramide): May reduce efficacy of ropinirole. ( 7.3 ) 7.1 Cytochrome P450 1A2 Inhibitors and Inducers In vitro metabolism studies showed that cytochrome P450 1A2 (CYP1A2) is the major enzyme responsible for the metabolism of ropinirole. There is thus the potential for inducers or inhibitors of this enzyme to alter the clearance of ropinirole. …

• 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 have reported falling asleep while engaged in activities of daily living, including driving or operating machinery, which sometimes resulted in accidents. …

The following adverse reactions are described in more detail in other sections of the label: • Hypersensitivity [ see Contraindications ( ) ] • 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 Sy …

8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of ropinirole 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 MRHD for Parkinson’s disease. …

The symptoms of overdose with ropinirole are related to its dopaminergic activity. General supportive measures are recommended. Vital signs should be maintained, if necessary. In 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). …

Take it when you remember, unless it is nearly time for the next dose. Then skip the missed one. Never take two doses at once to make up for it. Check your leaflet, as some medicines are different.