Adult: In moderate to severe cases: As conventional tab: Week 1: Initially, 0.25 mg for 2 days; if tolerated, dose may be increased to 0.5 mg once daily for the rest of the week. Week 2 onwards: 1 mg once daily for 7 days, may be increased by 0.5 mg at weekly intervals up to a dose of 3 mg once daily, followed by a final increase to Max of 4 mg once daily on week 7. Dose titrations must be based on individual response and tolerability. All doses are to be given 1-3 hours before bedtime.
Oral Parkinson's disease
Adult: Alone or as an adjunct to reduce the on-off fluctuations in levodopa response: As conventional tab: Initially, 0.25 mg tid, doses may be increased in increments of 0.75 mg daily at weekly intervals for the 1st 4 weeks according to patient response and tolerability. After 4 weeks, as necessary, dose may be increased by 1.5 mg daily at weekly intervals up to 9 mg daily dose, then by increments of up to 3 mg daily at weekly intervals for the subsequent weeks. Max: 24 mg daily. As prolonged-release tab: Initially, 2 mg once daily for 1 week, then increased to 4 mg once daily from the 2nd week. If sufficient control is not achieved or maintained, daily dose may be increased by 2 mg at weekly or longer intervals according to response up to a dose of 8 mg once daily; if still no response, daily dose may be increased further by 2-4 mg at intervals of at least 2 weeks. Maintain at the lowest effective dose. Max: 24 mg daily. Patients switching from conventional tab to prolonged-release tab: May initiate dose of prolonged-release tab based on the total daily dose of the conventional tab (refer to detailed product guideline for specific dosing).
Special Patient Group
Patient initiated on or withdrawn from concomitant use with CYP1A2 inhibitors or inducers (including cigarette smoking), or estrogen during treatment with ropinirole: Dose adjustment may be required.
Renal Impairment
Parkinson’s disease:
Patient with ESRD on haemodialysis: As conventional tab: 0.25 mg tid. As prolonged-release tab: 2 mg once daily. All doses may be increased according to efficacy and tolerability. Max: 18 mg daily.
Restless legs syndrome:
Patient with ESRD on haemodialysis: As conventional tab: Initially, 0.25 mg once daily, may be increased according to efficacy and tolerability. Max: 3 mg daily.
Administration
tab: May be taken with or without food. extended-release tab: May be taken with or without food. Swallow whole, do not crush/divide/chew.
Special Precautions
Patient with pre-existing dyskinesias, significant CV disease, predisposition to hypotension, cerebrovascular disease. Smokers. Avoid abrupt withdrawal. ESRD (undergoing dialysis) and hepatic impairment. Pregnancy and lactation. Patient receiving estrogen or CYP1A2 inhibitors or inducers. Not recommended for patient with severe renal impairment (CrCl <30 mL/min) without regular dialysis. Avoid use in patient with major psychotic disorder.
Adverse Reactions
Significant: Paradoxical worsening of RLS symptoms (augmentation or early morning rebound), impulse control disorders (e.g. pathological gambling, hypersexuality, compulsive buying, binge eating), dyskinesias, psychotic effects (e.g. hallucinations, paranoid ideation, delusions, confusion, psychotic-like behaviour, mania, disorientation, aggressiveness, agitation, delirium), somnolence and episodes of sudden sleep onset, orthostatic hypotension or hypotension; syncope, sometimes associated with bradycardia; fibrotic complications (e.g. pleural effusion, pleural fibrosis, interstitial lung disease, cardiac valvulopathy), neuroleptic malignant syndrome (abrupt withdrawal or rapid dose reduction), dopamine agonist withdrawal syndrome. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Nausea, vomiting, constipation, abdominal pain, heartburn, dyspepsia. General disorders and administration site conditions: Peripheral oedema, fatigue, pain. Immune system disorders: Hypersensitivity reaction (e.g. urticaria, angioedema, rash, pruritus). Infections and infestations: Viral infection. Injury, poisoning and procedural complications: Fall. Investigations: Increased liver enzymes. Nervous system disorders: Dizziness, headache. Vascular disorders: Hypertension.
This drug may cause excessive daytime somnolence or sudden onset of sleep, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure periodically; daytime alertness, CNS depression, fall risk, and behaviour changes. Perform periodic skin examinations.
Overdosage
Symptoms: Nausea, dizziness, hallucinations, hyperhidrosis, claustrophobia, chorea, palpitations, asthenia, nightmares; fatigue, vomiting, dyskinesia, agitation, somnolence, confusional state, chest pain, syncope, vasovagal syncope, and hypotension. Management: Symptomatic and supportive treatment. Maintain vital signs if necessary. May administer dopamine antagonists (e.g. neuroleptics, metoclopramide).
Drug Interactions
Increased plasma concentration with CYP1A2 inhibitors (e.g. ciprofloxacin, enoxacin, fluvoxamine) and hormone replacement therapy (e.g. estrogen). May diminish therapeutic efficacy with neuroleptics (e.g. phenothiazines, butyrophenones, thioxanthenes) and other centrally active dopamine antagonists (e.g. sulpiride, metoclopramide). May result in INR imbalance in concomitant use with vitamin K antagonists. Concomitant use with CNS depressants may enhance the sedative effect of ropinirole.
Food Interaction
May enhance sedative effect with alcohol. Decreased rate of absorption with high fat meals.
Action
Description: Mechanism of Action: Ropinirole is a non-ergot derivative dopamine receptor agonist that possesses a full intrinsic activity at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 receptor. Its exact mechanism in the treatment of Parkinson’s disease and restless legs syndrome (RLS) has not been fully elucidated, but it is believed to directly stimulate the postsynaptic dopamine receptors in the corpus striatum of the brain. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract (immediate release). Decreased rate of absorption with high fat meals. Bioavailability: Approx 50% (range: 36-57%). Time to peak plasma concentration: Approx 1-2 hours (immediate release); 6-10 hours (prolonged-release). Distribution: Widely distributed throughout the body. Volume of distribution: 7.5 L/kg. Plasma protein binding: 10-40%. Metabolism: Extensively metabolised in the liver by the CYP1A2 isoenzyme via N-despropylation and hydroxylation into inactive metabolites. Undergoes first-pass effect. Excretion: Via urine (<10% as unchanged drug, 60% as metabolites). Elimination half-life: Approx 6 hours.
Chemical Structure
Ropinirole_01 Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5095, Ropinirole. https://pubchem.ncbi.nlm.nih.gov/compound/Ropinirole. Accessed Dec. 21, 2020.
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