Ropinirole

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Requip, Rolipexa, Ropinirol; Belgium: Requip, Ropinirole; Bulgaria: Requiver, Requip, Ropinirole, Ropinstad; Cyprus: Adartrel, Requip; Czech Republic: Adartrel, Aropilo, Aropix, Lirona, Requip, Ropinirol, Ropinirole, Ropinstad; Denmark: Adartrel, Requip, Ropinirol; Estonia: Requip, Ropinirole; Finland: Adartrel, Requip, Ropinirol; France: Requip, Ropinirole; Germany: Adartrel, Lesparol, Requip, Roparless, Ropi-Torr, RopiCare, Ropimed, Ropinal, Ropinirol, Ropipark, Ropiran, Ropiril, Ropirol, Tifirol, Yrolmed; Greece: Adartrel, Reparkin, Requip, Ropinirol, Ropinirole; Hungary: Adartrel, Aropilo, Nirolensan, Parkirol, Requip, Romyl, Ropidopin, Ropinirol; Ireland: Adartrel, Eironil, Requip, Roni, Ropinirole, Ropirade; Italy: Requip, Ropinirolo; Latvia: Requip, Ropinirol, Ropinirole; Lithuania: Adartrel, Requip, Ropinirol, Ropinirole; Luxembourg: Requip; Malta: Adartrel, Requip, Ropinir; Netherlands: Adartrel, Requip, Ropinirol, Sonirol; Poland: Adartrel, Aparxon, Aropilo, Aropix, Ceuronex, Lirona, Requip, Ropinir, Ropinirole, Ropinstad; Portugal: Adartrel, Dopil, Requip, Ropimed, Ropinirol; Romania: Aleta, Requip, Ropinirol; Slovakia: Adartrel, Aropix, Lirona, Requip, Ropinirol, Ropinstad; Slovenia: Requip, Ropinirol; Spain: Adartrel, Requip, Ropigen, Ropinirol; Sweden: Adartrel, Requip, Ropinirol; UK: Adartrel, Requip, Ropinirole.

North America

Canada: Requip, Ropinirole; USA: Requip, Ropinirole.

Latin America

Argentina: Requip; Mexico: Requip.

Asia

Japan: Requip.

Drug combinations

Chemistry

Ropinirole Hydrochloride: C~16~H~24~N~2~O HCl. Mw: 296.84. (1) 2H-Indol-2-one, 4-[2-(dipropylamino)ethyl]-1,3-dihydro-, monohydrochloride; (2) 4-[2-(Dipropylamino)ethyl]-2-indolinone monohydrochloride. CAS-91374-20-8; CAS-91374-21-9 (ropinirole)(1993).

Pharmacologic Category

Antiparkinsonian Agents; Non-Ergot-Derivative Dopamine Receptor Agonists. (ATC-Code: N04BC04).

Mechanism of action

Has high relative in vitro specificity and full intrinsic activity at D~2~ and D~3~ dopamine receptor subtypes, binding with higher affinity to D~3~ than to D~2~ or D~4~ receptor subtypes. Although precise mechanism of action unknown, it is believed to be due to stimulation of postsynaptic dopamine D~2~-type receptors within caudate putamen in brain. Mechanism of ropinirole-induced postural hypotension believed to be due to D~2~-mediated blunting of noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.

Therapeutic use

Treatment of idiopathic Parkinson’s disease in patients with early Parkinson’s disease and not receiving concomitant levodopa therapy; also in patients with advanced disease on concomitant levodopa. Treatment of moderate-to-severe primary restless legs syndrome (RLS).

Pregnancy and lactiation implications

There are no adequate, well-controlled studies in pregnant women. Use only if potential benefit outweighs risk to fetus. Use not recommended in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to ropinirole or any component of the formulation.

Warnings and precautions

May cause hallucinations (risk may be increased in the elderly). Dopamine agonists used for Parkinson’s disease or restless legs syndrome associated with compulsive behaviors and/or loss of impulse control, manifested as pathological gambling, libido increases (hypersexuality), and/or binge eating (causality not established). Risk for melanoma development increased in Parkinson’s disease patients. May cause orthostatic hypotension. Use with caution in risk of hypotension or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Syncope, sometimes associated with bradycardia, observed in association with ropinirole in both early Parkinson’s disease (without levodopa) and advanced Parkinson’s disease (with levodopa). Risk of fibrotic complications (e.g. pleural effusion/fibrosis, interstitial lung disease) reported in patients receiving ropinirole (drug causation not established). Pathologic degenerative changes observed in retinas of albino rats during studies with this agent, but not observed in retinas of albino mice or other species (significance of these data for humans remains uncertain). Somnolence might occur (caution with concomitant sedating medication). Use with caution in patients receiving other CNS depressants or psychoactive agents (effects with other sedative drugs or ethanol may be potentiated), in pre-existing dyskinesias (may be exacerbated), and in severe hepatic or renal impairment. Avoid use in major psychotic disorder (may exacerbate psychosis). Augmentation (earlier onset of symptoms in evening/afternoon, increase and/or spread of symptoms to other extremities) or rebound (shifting of symptoms to early morning hours) may occur in some RLS patients. Dopaminergic agents associated with syndrome resembling neuroleptic malignant syndrome on abrupt withdrawal or significant dosage reduction after long-term use.

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