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QuickView for Ropinirole (compound)

Name: ropinirole
PubChem Compound ID: 5095
Molecular formula: C16H24N2O
Molecular weight: 260.375 g/mol
Ropinirole; Ropinirolum [INN-Latin]; Lopac-R-4152; 91374-21-9; 2H-Indol-2-one, 4-(2-(dipropylamino)ethyl)-1,3-dihydro-; NCGC00015893-01; C07564; 91374-20-8; ReQuip; Ropinirol [INN-Spanish]
Name: ropinirole
Name (isomeric): DB00268
Drug Type: small molecule
Ropinirolum [INN-Latin]; Ropinirole hydrochloride; Ropinirole HCl; Ropinirol [INN-Spanish]
Brand: ReQuip CR, Requip, ReQuip XL
Category: Antidyskinetics, Antiparkinson Agents, Dopamine Agonists, Central Nervous System Agents
CAS number: 91374-21-9
Indication: For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is u...
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Mechanism of Action:
Ropinirole binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have d...
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Absorption: Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
Protein binding: 40% bound to plasma proteins with a blood-to-plasma ratio of 1:1.
Biotransformation: Hepatic. Ropinirole is extensively metabolized to inactive metabolites via N -despropylation and hydroxylation pathways, largely by the P450 isoenzyme CYP1A2. N-despropyl ropinirole is the predominant metabolite found in urine (40%), followed by the carboxylic acid metabolite (10%), and the glucuronide of the hydroxy metabolite (10%).
Route of elimination: Ropinirole is extensively metabolized by the liver to inactive metabolites, and less than 10% of the administered dose is excreted as unchanged drug in urine.
Half Life: 6 hours
Clearance: 47 L/hr [after oral administration to Parkinson's disease patients and patients with Restless Legs Syndrome]
Toxicity: Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting.
Affected organisms: Humans and other mammals
Drug interaction:
FluvoxamineIncreases the effect and toxicity of ropinirole
CiprofloxacinCiprofloxacin may increase the effect and toxicity of ropinirole.
PaliperidoneThe atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, ropinirole. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
ThiothixeneThiothixene may antaonize the effects of the anti-Parkinsonian agent, Ropinirole. Consider alternate therapy or monitor for decreased effects of both agents.
ZuclopenthixolAntagonism may occur between zuclopenthixol, a dopamine D2 receptor antagonist, and ropinirole, a dopamine agonist. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concurrent therapy is initiated, discontinued or dose(s) changed.
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