2773 Ropinirole Ropinirole is a non-ergoline dopamine agonist, manufactured by GlaxoSmithKline. It is used in the treatment of Parkinson's disease, and is also one of two medications in the United States with an FDA-approved indication for the treatment of restless legs syndrome (the other being Pramipexole). 91374-21-9 5095 C16H24N2O 260.188860 White powder. 243-250°C 133 mg/mL Oral. Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption. 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. 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 No indication of carcinogenicity to humans (not listed by IARC). For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome. 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. General supportive measures are recommended. Vital signs should be maintained, if necessary. Removal of any unabsorbed material (e.g., by gastric lavage) should be considered. (L1712) 2009-07-21T20:26:26Z 2014-12-24T20:25:50Z Ropinirole C07564 8888 Ropinirole DB00268 true CCCN(CCC)CCC1=C2CC(O)=NC2=CC=C1 C16H24N2O InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19) InChIKey=UHSKFQJFRQCDBE-UHFFFAOYSA-N 260.3746 260.1888634 Exogenous Solid 2.7 HMDB14413 CHEMBL589 4916 <p><a href="http://www.drugsyn.org/Ropinirole.htm">DrugSyn.org</a></p>