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).
Top Gene Interactions
Related Pathways
General Information
- 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%). 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
- Uses/Sources: For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
- Symptoms: 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.
- Treatment: 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)
- Route of Exposure: Oral. Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
5-hydroxytryptamine receptor 2A 5-hydroxytryptamine receptor 2C 5-hydroxytryptamine receptor 1A 5-hydroxytryptamine receptor 2B Alpha-2A adrenergic receptor 5-hydroxytryptamine receptor 1B 5-hydroxytryptamine receptor 1D D(1A) dopamine receptor Alpha-1B adrenergic receptor Alpha-1D adrenergic receptor Alpha-2B adrenergic receptor D(1B) dopamine receptor Beta-1 adrenergic receptor 5-hydroxytryptamine receptor 6 Alpha-2C adrenergic receptor |
9057850 18691132 12388666 14978194 |
|
D(2) dopamine receptor D(3) dopamine receptor D(4) dopamine receptor |
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. |
9057850 18393062 1683559 10446316 19324548 11752352 18242171 17573046 |
Ropinirole Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Brain Ischemia | 34.49 |
|
Reperfusion Injury | 23.93 |
|
Radiation Injuries, Experimental | 21.91 |
|
Trigeminal Neuralgia | 20.37 |
|
Diabetes Mellitus, Experimental | 15.44 |
|
Alcoholic liver cirrhosis | 14.75 |
|
Osteoporosis, Postmenopausal | 14.39 |
|
Schizophrenia | 14.33 |
|
Cardiomyopathies | 14.0 |
|
Sepsis | 14.0 |
|
Heat Stroke | 13.56 |
|
Nerve Degeneration | 12.62 |
|
Cocaine dependence | 12.42 |
|
Stomach Neoplasms | 12.36 |
|
Alzheimer's Disease | 12.34 |
|
Myocardial infarction | 12.07 |
|
Anthracosis | 11.97 |
|
Disease Models, Animal | 11.85 |
|
Head and Neck Neoplasms | 11.75 |
|
Lung Neoplasms | 11.67 |
|