Rotigotine: transdermal dopamine agonist treatment of Parkinson's disease and restless legs syndrome.
OBJECTIVE
To evaluate the pharmacology, pharmacokinetics, clinical efficacy, and tolerability of rotigotine, a nonergoline D(3)/D(2)/D(1) dopamine receptor agonist in the treatment of Parkinson's disease and restless legs syndrome (RLS).


METHODS
A literature search was conducted using MEDLINE (1996-December 2006) and International Pharmaceutical Abstracts, using the search terms rotigotine and dopamine agonist. References cited in the articles were reviewed for additional information. Information was also obtained from Schwarz Pharma. Abstracts for posters at scientific conferences were accessed from conference Web sites.


METHODS
English-language literature reporting controlled animal and human clinical studies was reviewed to evaluate the pharmacology, pharmacokinetics, therapeutic use, and adverse effects of rotigotine. Clinical trials selected for inclusion were limited to those with human subjects; data from animal studies were included if human data were not available.


RESULTS
Rotigotine has been investigated in early Parkinson's disease, as adjuvant therapy to levodopa in advanced Parkinson's disease, and in RLS. It is administered transdermally, which provides the convenience of once-daily dosing, constant drug delivery, and sustained stable plasma concentrations. In clinical trials of patients with early Parkinson's disease, rotigotine has decreased combined scores on the motor and activities of daily living sections of the Unified Parkinson's Disease Rating Scale up to 85 weeks. In patients with advanced Parkinson's disease, rotigotine reduced mean off-time when used as an adjuvant to levodopa. Rotigotine has decreased the severity of RLS in Phase III trials. Acute adverse events are similar to those of other dopamine agonists and are most common during the titration phase. Mild-to-moderate application site reactions are common.


CONCLUSIONS
Longer trials are required to determine whether transdermal rotigotine will reduce development of dyskinesias and motor fluctuations in Parkinson's disease and augmentation and rebound in RLS by preventing pulsatile dopamine stimulation associated with levodopa and other dopamine agonists.
Splinter
Michele Y
MY
Department of Pharmacy: Clinical and Administrative Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, PO Box 26901, Oklahoma City, OK 73190, USA. michele-splinter@ouhsc.edu
D000279:Administration, Cutaneous; D002986:Clinical Trials as Topic; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000627:therapeutic use*; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy*; D012148:Restless Legs Syndrome / Q000188:drug therapy*; D013764:Tetrahydronaphthalenes / Q000008:administration & dosage / Q000627:therapeutic use*; D013876:Thiophenes / Q000008:administration & dosage / Q000627:therapeutic use*; D016896:Treatment Outcome
D018491:Dopamine Agonists; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; C047508:rotigotine