Ropinirole Er (ropinirole HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ropinirole hydrochloride is a nonergot-derivative dopamine receptor agonist.
Ropinirole, a dipropylaminoethyl indolone derivative, is a nonergot-derivative dopamine receptor agonist. In in vitro binding studies, ropinirole demonstrated high binding specificity for and intrinsic activity at dopamine D2 receptors compared with other dopamine receptor agonists (e.g., bromocriptine, pergolide), having a higher affinity for the D3 subtype than for the D2 or D4 subtypes. Ropinirole binds with moderate affinity to opiate receptors but has little or no affinity for alpha1-, alpha2-, or beta-adrenergic; dopamine D1; benzodiazepine; gamma-aminobutyric acid (GABA); serotonin type 1 (5-hydroxytryptamine (5-HT1)); serotonin type 2 (5-HT2); or muscarinic receptors.
The exact mechanism of action of ropinirole in the management of parkinson disease has not been fully elucidated. There is considerable evidence that manifestations of parkinson disease, regardless of the cause of the syndrome, are related to depletion of dopamine in the corpus striatum. While levodopa is believed to act principally by increasing dopamine concentrations in the brain, ropinirole appears to act by directly stimulating postsynaptic dopamine receptors in the corpus striatum.
The exact mechanism of action of ropinirole in the management of restless legs syndrome (RLS) is not known, but is thought to be related to its ability to stimulate dopamine receptors.
USES: This medication is used alone or with other medications to treat Parkinson's disease. It can improve your ability to move and decrease shakiness (tremor), stiffness, slowed movement, and unsteadiness. It may also decrease the number of episodes of not being able to move ("on-off syndrome").
Ropinirole works by helping to restore the balance of a certain natural substance (dopamine) in the brain.
Generic name: ropinirole HCl
Pronunciation: (row-PIN-uh-roll)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Ropinirole Er
Indications
The following indications are listed for Ropinirole Er:
- Idiopathic Parkinsonism
Also known as: Paralysis Agitans, Primary Parkinson's Disease.
Dosing
Dosage of ropinirole hydrochloride is expressed in terms of ropinirole.
Therapy should be initiated with a low dosage and titrated slowly until the maximum therapeutic response is achieved.
If ropinirole therapy is interrupted for a substantial period of time, retitration may be warranted.
Because dosage of ropinirole is titrated to clinical response, routine dosage adjustment based solely on age is not necessary in geriatric patients.
Ropinirole is administered orally as conventional (immediate-release) tablets or extended-release tablets. The extended-release tablets are FDA-labeled for use only in the treatment of parkinson disease.
For the management of parkinson disease, ropinirole is administered as immediate-release tablets in 3 equally divided doses daily or as extended-release tablets once daily. For the management of restless legs syndrome (RLS), ropinirole is administered as immediate-release tablets once daily, 1-3 hours before bedtime. Both formulations of the drug may be administered without regard to food.
The extended-release tablets should be swallowed whole, and not chewed, crushed, or divided. The tablet is designed to slowly release ropinirole over a 24-hour period; if rapid GI transit occurs, incomplete release of the drug may occur, causing some tablet residue to appear in the stool.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to ropinirole hydrochloride or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects of immediate-release ropinirole in patients with early parkinson disease include nausea, somnolence, dizziness, syncope, asthenic condition, viral infection, leg edema, vomiting, and dyspepsia.
Common adverse effects of the extended-release tablets in patients with early parkinson disease include nausea, somnolence, sudden onset of sleep, hypertension, headache, abdominal pain/discomfort, dizziness, and constipation.
Common adverse effects of immediate-release ropinirole in patients with advanced parkinson disease receiving concomitant levodopa include dyskinesia, somnolence, nausea, dizziness, confusion, hallucinations, sweating, and headache.
Common adverse effects with the extended-release ropinirole tablets in patients with advanced parkinson disease include nausea, dyskinesia, dizziness, and hallucinations.
Common adverse effects of immediate-release ropinirole in patients with RLS include nausea, somnolence, vomiting, dizziness, and fatigue.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of ropinirole have not been established in pediatric patients.
There are no adequate data on the developmental risks associated with the use of ropinirole in pregnant women. In animal studies, adverse developmental effects (e.g., teratogenicity, embyrolethality) were observed when the drug was administered to pregnant rats at dosages similar to or greater than the recommended maximum human dosage; these dosages also were associated with maternal toxicity. In pregnant rabbits, oral administration of ropinirole had no effect on embryofetal development, but when administered in combination with levodopa, an increased incidence of fetal malformations was observed.
It is not known whether ropinirole is distributed into human milk; however, the drug is distributed into milk in rats. The effects of ropinirole on the breast-fed infant or on milk production are not known. The known benefits of breast-feeding should be considered along with the mother's clinical need for ropinirole and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.
Because ropinirole inhibits prolactin secretion, the drug is expected to inhibit lactation.
Oral clearance of ropinirole is reduced by 15% in geriatric patients older than 65 years of age compared with younger patients. In clinical studies of ropinirole in patients with parkinson disease, some adverse effects were more frequent in geriatric patients (e.g., hallucinations, vomiting, nausea) than in younger patients receiving the drug.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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