Ropinirole

Indications

Ropinirole is used for: Parkinson's disease, Restless leg syndrome

Adult Dose

Oral As monotherapy in Parkinson's disease Adult: Initially, 250 mcg tid, may increase by 750 mcg at wkly intervals for the first 4 wk. Subsequent increments can be made in steps of 1.5 mg at wkly intervals up to 9 mg/day, then in steps of 3 mg at wkly intervals. Usual dose ranges from 3-9 mg daily. Max: 24 mg/day. Higher dose may be necessary if used in conjunction with levodopa. Gradual withdrawal is recommended. Restless leg syndrome Adult: Initially, 250 mcg daily for 2 days, taken 1-3 hr before bedtime. May increase to 500 mcg daily for the next few days. Subsequent increments may be made in steps of 500 mcg at wkly intervals until 3 mg daily is reached. Max: 4 mg daily. Hepatic impairment: Dosing adjustments may be required.

Child Dose

Renal Dose

Administration

May be taken with or without food. May be taken w/ meals to reduce occurrence of nausea.

Contra Indications

Lactation.

Precautions

Pregnancy. May impair ability to drive or operate machinery. Withdrawal should be gradual. Hepatic or renal impairment. May cause daytime sleepiness or episodes of falling asleep during activities. May cause or worsen pre-existing dyskinesia.

Pregnancy-Lactation

Pregnancy There are no adequate data on developmental risk associated with use 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) maximum recommended human dose (MRHD) for Parkinson’s disease Lactation There are no data on presence of ropinirole in human milk, the effects of ropinirole on breastfed infant, or effects of ropinirole on milk production; however, inhibition of lactation is expected because ropinirole inhibits secretion of prolactin in humans; ropinirole or metabolites, or both, are present in rat milk Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from ropinirole or from the underlying maternal condition

Interactions

Inhibitors of CYP1A2 e.g. cimetidine, ciprofloxacin, erythromycin, fluvoxamine, isoniazid, ritonavir and zileuton may increase serum concentrations of ropinirole. Oestrogens and tobacco smoking may decrease clearance of ropinirole. Efficacy may be reduced by dopamine antagonists such as phenothiazines and metoclopramide.

Adverse Effects

Side effects of Ropinirole : >10% Nausea (40-60%), Dizziness (6-40%), Somnolence (11-40%), Syncope (1-12%), Vomiting (12%), Fatigue (8-11%), Viral infection (11%), Dyspepsia (10%) 1-10% Hypertension (5%), Flushing (3%), Orthostasis (1-6%), Chest pain (4%), Palpitation (3%), Extrasystoles (2%), Tachycardia (2%), Hyperhidrosis (3%), Abnormal pain (3-7%), Anorexia (4%), Flatulence (3%), Malaise (3%), Hypoesthesia (4%), Urinary tract infection (5%), Impotence (3%), Alkaline phosphatase (3%), Abnormal vision (6%), Xerophthalmia (2%), Increased diaphoresis (3-6%) <1% Agitation, Aneurysm, Aphasia, Bradycardia, Cardiac arrest, Valvulopathy, Cellulitis, Colitis, Delusion, Delirium, Diaphoresis, Dyspnea, Ulceration, Glaucoma, Psychotic-like behavior, Impulse control/compulsive behavior, Withdrawal-emergent hyperpyrexia and confusion, Melanoma, Fibrotic complications

Mechanism of Action

Ropinirole is a non-ergot dopamine D2-agonist with similar actions to those of bromocriptine. It is used in the management of Parkinson's disease, either alone or as an adjunct to levodopa.