Linear Pharmacokinetic Behavior of Ropinirole during Multiple Dosing in Patients with Parkinson's Disease

• Published in: Journal of clinical pharmacology 2000-06, Vol.40 (6), p.641-646
• Main Authors: Hubble, Jean, Koller, William C., Atchison, Paul, Taylor, Anne C., Citerone, David R., Zussman, Barry D., Friedman, Carl J., Hawker, Noele
• Format: Article
• Language: English
• Subjects: Adult; Aged; Aged, 80 and over; Anticonvulsants. Antiepileptics. Antiparkinson agents; Antiparkinson Agents - pharmacokinetics; Biological and medical sciences; Female; Humans; Indoles - adverse effects; Indoles - pharmacokinetics; levodopa; Male; Medical sciences; Middle Aged; Neuropharmacology; Parkinson Disease - drug therapy; Parkinson Disease - metabolism; Pharmacology. Drug treatments; ropinirole
• ISSN: 0091-2700; 1552-4604
• DOI: 10.1002/j.1552-4604.2000.tb05990.x

The objectives of this study were to measure the pharmacokinetics of ropinirole at steady state when the drug is used as an adjunct to L‐dopa and evaluate the long‐term tolerability of ropinirole in this indication. Twenty‐four pa tien ts who were taking L‐dopa for Parkinson's disease and experiencing a lack of symptomatic control were recruited. Patients received open‐label adjunctive treatment with ropinirole for up to 2 years. The starting dose was 0.5 mg bid, which could be titrated to a maximum of 6.0 mg tid. Ropinirole demonstrated approximately dose‐linear pharmacokinetics at steady state; corresponding values were higher during tid than bid dosing. A reduction in mean L‐dopa dose was maintained throughout the trial. The combination of L‐dopa and ropinirole was generally well tolerated, with only 1 patient withdrawing from treatment because of adverse events. Thus, ropinirole shows approximately linear steady‐state pharmacokinetics and a good safety profile when administered with L‐dopa.