OBJECTIVE: To evaluate the pharmacology, pharmacokinetics, clinical efficacy,
and tolerability of rotigotine, a nonergoline D3/D2/D1 dopamine receptor agonist in
the treatment of Parkinson’s disease and restless legs syndrome (RLS).
DATA SOURCES: 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.
STUDY SELECTION AND DATA EXTRACTION: 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.
DATA SYNTHESIS: 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.
Key Words: dopamine agonist, rotigotine.
Ann Pharmacother 2007;41:285-95.
Published Online, 9 Jan 2007, www.theannals.com, DOI 10.1345/aph.1H113
THIS ARTICLE IS APPROVED FOR CONTINUING EDUCATION CREDIT
ACPE UNIVERSAL PROGRAM NUMBER: 407-000-07-009-H01 |