Product Information
Registration Status: ActiveREQUIP TABLET 0.25mg is approved to be sold in Singapore with effective from 1999-11-06. It is marketed by GLAXOSMITHKLINE PTE LTD, with the registration number of SIN10976P.
This product contains Ropinirole 0.25mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Catalent UK Packaging Limited (Primary and Secondary Packager) in SPAIN, andGlaxo Wellcome S.A. in UNITED KINGDOM.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
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).
Indication
For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
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.
Pharmacokinetics
- Absorption
- Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
- Distribution
- * 7.5 L/kg * 525 L
- Metabolism
- 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%).
- Elimination
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.
Active Ingredient/Synonyms
Ropinirol | Ropinirolum | Ropinirole |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.