Indication: For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
Pharmacology: 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 unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.
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 demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.
Drug Category: Dopamine Agonists; Antiparkinson Agents; Antidyskinetics; Central Nervous System Agents; ATC:N04BC04
Absorption: Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
Interactions:
DrugBank: Interactions for Ropinirole
Interactions for Ropinirole:
P 450 Interaction:In vitro metabolism studies showed that CYP1A2 was
the major enzyme responsible for the metabolism of ropinirole. There is thus the potential for substrates or
inhibitors of this enzyme when coadministered with ropinirole to alter its clearance. Therefore, if therapy with a
drug known to be a potent inhibitor of CYP1A2 is stopped or started during treatment with Requip , adjustment
of the Requip dose may be required.
L-dopa: Co-administration of carbidopa + L-dopa (Sinemet® 10/100 mg b.i.d.) with
ropinirole (2.0 mg t.i.d.) had no effect on the steady-state pharmacokinetics of ropinirole (n=28 patients). Oral
administration of Requip 2.0 mg t.i.d. increased mean steady state C max of L-dopa by 20% but its
AUC was unaffected (n=23 patients).
Digoxin: Co-administration of Requip (2.0 mg t.i.d.) with digoxin (0.125-0.25 mg
q.d.) did not alter the steady-state pharmacokinetics of digoxin in 10 patients.
Theophylline: Administration of theophylline (300 mg b.i.d., a substrate of CYP1A2) did
not alter the steady-state pharmacokinetics of ropinirole (2 mg t.i.d.) in 12 patients with Parkinson's disease.
Ropinirole (2 mg t.i.d.) did not alter the pharmacokinetics of theophylline (5 mg/kg i.v.) in 12 patients with
Parkinson's disease.
Ciprofloxacin: Co-administration of ciprofloxacin (500 mg b.i.d.), an inhibitor of
CYP1A2, with ropinirole (2 mg t.i.d.) increased ropinirole AUC by 84% on average, and C max by 60% (n=12
patients).
Estrogens: Population pharmacokinetic analysis revealed that estrogens (mainly
ethinylestradiol: intake 0.6-3 mg over 4-month to 23-year period) reduced the oral clearance of ropinirole by 36% in
16 patients. Dosage adjustment may not be needed for Requip in patients on estrogen therapy because patients
must be carefully titrated with ropinirole to tolerance or adequate effect. However, if estrogen therapy is stopped
or started during treatment with Requip , then adjustment of the Requip (ropinirole hydrochloride) dose may be
required.
Dopamine Antagonists: Since ropinirole is a dopamine agonist, it is possible that
dopamine antagonists, such as neuroleptics (phenothiazines, butyrophenones, thioxanthenes) or metoclopramide, may
diminish the effectiveness of Requip . Patients with major psychotic disorders, treated with neuroleptics,
should only be treated with dopamine agonists if the potential benefits outweigh the risks.
Population analysis showed that commonly administered drugs, e.g., selegiline, amantadine, tricyclic
antidepressants, benzodiazepines, ibuprofen, thiazides, antihistamines, and anticholinergics did not affect the oral
clearance of ropinirole.
Chemical IUPAC Name: 4-(2-dipropylaminoethyl)-1,3-dihydroindol-2-one
Chemical Formula: C16H24N2O
Half Life: 6 hours
Drug Type: Approved Drug
# Accession No: APRD00302
CAS Registry Number: 91374-21-9
Ropinirole News (When available)
Those restless legs16 Jan 2006 Pittsburgh Tribune-Review, Now, she said, symptoms occur about twice a week. "My doctor prescribed Requip, but I don't take it because it can cause sleepiness," said Brunot, who works as ...
Requip (ropinirole HCl) Tablets Significantly Improve Symptoms of ...Jan 3, 2006 PharmaLive.com (press release), RESEARCH TRIANGLE PARK, NC, January 03, 2006 /PRNewswire/ -- Data published in the January issue of Mayo Clinic Proceedings show that Requip(R) (ropinirole HCl ...
Exact cause of restless legs is unknownJan 9, 2006 Newark Star Ledger, In more severe cases, medications may be necessary. RLS often is treated with medications known as nonergotamine agonists (such as Requip). ...
GSK drug soothes restless legs syndromeJan 3, 2006 Pharmaceutical Business Review GlaxoSmithKline's Requip tablets have been shown to significantly improve symptoms of restless legs syndrome in a large-scale trial. ...
Drug Approved To Treat Restless Leg SyndromeJan 4, 2006 cbs4denver.com, ...(CBS4) DENVER New research released Tuesday shows a drug called Requip can alleviate the symptoms of restless legs syndrome (RLS). ...
Restless legs symptoms come and goJan 2, 2006 Charleston Post Courier (subscription), And for the first week, they did, so I figured I'd surely scored the real thing, a new extended-release version of Requip, a Parkinson's disease drug approved ...