Overview
11 DESCRIPTION Ropinirole tablets contain ropinirole, a non-ergoline dopamine agonist, as the hydrochloride salt. The chemical name of ropinirole hydrochloride is 4-[2-(dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one and the empirical formula is C 16 H 24 N 2 O•HCl. The molecular weight is 296.84 (260.38 as the free base).
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Ropinirole is a non-ergoline dopamine agonist. The precise mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, although it is thought to be related to its ability to stimulate dopamine D2 receptors within the caudate-putamen in the brain. The precise mechanism of action of ropinirole as a treatment for Restless Legs Syndrome is unknown, although it is thought to be related to its ability to stimulate dopamine receptors. 12.2 Pharmacodynamics Clinical experience with dopamine agonists, including ropinirole, suggests an association with impaired ability to regulate blood pressure resulting in orthostatic hypotension, especially during dose escalation.
Indications
- 1 INDICATIONS AND USAGE Ropinirole Tablets are a non-ergoline dopamine agonist indicated for the treatment of Parkinson’s disease (PD) and moderate-to-severe primary Restless Legs Syndrome (RLS). (1.1, 1.2). 1.1 Parkinson's Disease Ropinirole tablets are indicated for the treatment of Parkinson’s disease. 1.2 Restless Legs Syndrome Ropinirole tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS).
Common Doses
- 0.25 mg
- 24 mg
- 18 mg
- 4 mg
Dosage
2 DOSAGE AND ADMINISTRATION · Ropinirole tablets can be taken with or without food. (2.1) · Retitration of ropinirole tablets may be warranted if therapy is interrupted. (2.1) Parkinson’s Disease: · The recommended starting dose is 0.25 mg taken three times daily; titrate to a maximum daily dose of 24 mg. (2.2) · Renal Impairment: The maximum recommended dose is 18 mg/day in patients with end-stage renal disease on hemodialysis. (2.2) Restless Legs Syndrome: · The recommended starting dose is 0.25 mg once daily, 1 to 3 hours before bedtime, titrate to a maximum recommended dose of 4 mg daily.
Contraindications
- 4 CONTRAINDICATIONS Ropinirole tablets are contraindicated in patients known to have a hypersensitivity/allergic reaction (including urticaria, angioedema, rash, pruritus) to ropinirole or to any of the excipients. History of hypersensitivity/allergic reaction (including urticaria, angioedema, rash, pruritus) to ropinirole or to any of the excipients (4)
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are described in more detail in other sections of the label: Hypersensitivity [see Contraindications (4)] Falling asleep during activities of daily living and somnolence [see Warnings and Precautions (5.1)] Syncope [see Warnings and Precautions (5.2)] Hypotension/orthostatic hypotension [see Warnings and Precautions (5.3)] Hallucinations/psychotic-like behavior [see Warnings and Precautions (5.4)] Dyskinesia [see Warnings and Precautions (5.5)] Impulse control/compulsive behaviors [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS · Inhibitors or inducers of CYP1A2: May alter the clearance of ropinirole tablets; dose adjustment of ropinirole tablets may be required (7.1, 12.3) · Hormone replacement therapy(HRT): Starting or stopping HRT may require dose adjustment of ropinirole tablets (7.2, 12.3) · Dopamine antagonists (e.g., neuroleptics, metoclopramide): May reduce efficacy of ropinirole tablets (7.3) 7.1 Cytochrome P450 1A2 Inhibitors and Inducers In vitro metabolism studies showed that CYP1A2 is the major enzyme responsible for the metabolism of ropinirole.