Clinical Pharmacology Details


ROPINIROLE


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Indications & Dose:

Parkinson’s disease, either used alone or as adjunct to cobeneldopa or co-careldopa



Adult: Initially 750 micrograms daily in 3 divided doses, then increased in steps of 750 micrograms daily, dose to be increased at weekly intervals, increased to 3 mg daily in 3 divided doses, then increased in steps of 1.5–3 mg daily, adjusted according to response, dose to be increased at weekly intervals; usual dose 9–16 mg daily in 3 divided doses, higher doses may be required if used with levodopa, when administered as adjunct to levodopa, concurrent dose of levodopa may be reduced by approx. 20%, daily maximum dose to be given in 3 divided doses; maximum 24 mg per day



Adult: Initially 2 mg once daily for 1 week, then 4 mg once daily, increased in steps of 2 mg at intervals of at least 1 week, adjusted according to response, increased to up to 8 mg once daily, dose to be increased further if still no response; increased in steps of 2–4 mg at intervals of at least 2 weeks if required; maximum 24 mg per day


Parkinson’s disease in patients transferring from ropinirole immediate-release tablets



Adult: Initially ropinirole modified-release once daily substituted for total daily dose equivalent of ropinirole immediate-release tablets; if control not maintained after switching, titrate dose, consider slower titration in patients over 75 years, when administered as adjunct to levodopa, concurrent dose of levodopa may gradually be reduced by approx. 30%, if treatment interrupted for 1 day or more, consider re-initiation with immediate-release tablets


Moderate to severe restless legs syndrome



Adult: Initially 250 micrograms once daily for 2 days, increased if tolerated to 500 micrograms once daily for 5 days, then increased if tolerated to 1 mg once daily for 7 days, then increased in steps of 500 micrograms daily, adjusted according to response, dose to be increased at weekly intervals; usual dose 2 mg once daily, doses to be taken at night, repeat dose titration if restarting after interval of more than a few days; maximum 4 mg per day


Elderly:The clearance of ropinirole is decreased in patients over 65 years of age. but the dose of ropinirole for elderly patients can be titrated in the normal manner.


Children and Adolescents: There are no data available on the use of ropinirole in patients under 18 years of age therefore, ropinirole is not recommended for use in patients within this age group


RENAL AND HEPATIC IMPAIRMENT


In patients with mid to moderate renal impairment (creatinine clearance 30 - 50 ml/min) no change in the clearance of ropinirole was observed, indicating that fie dosage adjustment is necessary in this population


The rise of ropinirole in patients with severe renal (creatinine clearance 30 ml/min) or hepatic impairment has not been studied Administration of ropinirole to such patients is riot recommended

Contraindications:

Side Effects:

CNS: Drowsiness, euphoria, somnolence


CV: Bradycardia, postural hypotension, supraventricular ectopy (rare)


GI: Nausea 

Cautions:

Precautions:

 Cardiovascular disease, breast feeding, pregnancy 

Interaction:

 Drugs


• Ciprofloxacin, enoxac in, pefoxacin: Addition increases ropinirole concentrations


• Dopamine antagonists: Diminished anti-Parkinson’s effect


• Estrogens: Reduced ropinirole clearance, may need to decrease ripinirole if estrogen stopped 

Warnings:

Adverse Effects:

Lactations:

Pregnancy category D; inhibits lactation 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: