Rotigotine CDS® (constant delivery system), (-)-5,6,7,8-tetrahydro-6 [propyl-2-(2-thienyl-ethyl) amino]-1-naphthalenolis (Neupro®, Schwarz Pharma) is a silicone-based lipophilic nonergotamine D2 agonist patch designed to deliver constant drug levels over a 24-hour period (7). Detectable serum levels are achieved two to three hours after initial application and a serum steady state is achieved after approximately 24 hours. In the current formulation, the 9 mg (20 cm2) patch delivered approximately 4 mg of drug over a 24-hour period. Similarly, the 40 cm2 patch has 18 mg of the drug and delivers 8 mg over a period of 24 hours and the 60 cm2 patch has 27 mg of rotigotine and delivers 12 mg over 24 hours. Increased dermal sizes appear to proportionally increase serum drug levels. Pharmacokinetic studies demonstrate that the drug has a T1/2 of about five to seven hours, but maintains steady-state levels while the patch is worn. The current design is formulated to be worn for 24 hours. There were no measurable metabolites.
Rotigotine has been compared with placebo and other dopamine agonists in both early and advanced PD (8-13). In general, the studies have shown efficacy and an AE profile similar to that of other dopamine agonists. Phase Ila dose finding studies showed a linear dose-response curve, as measured by the Unified Parkinson's Disease Rating Scale (UPDRS), between 4.5 and 54 mg/day (120 cm2). A multicenter, double-blind study of rotigotine in early PD demonstrated significant benefit in UPDRS scores compared with placebo. The majority of patients (90%) reached a dose level of 13.5 mg/day (12). A multicenter, double-blind study of advanced PD compared rotigotine 40 cm2 (n = 111), rotigotine 60 cm2 (n = 120), and placebo (n = 120) and reported a decrease in off time of 2.7, 2.1, and 0.9 hours, respectively (13). The most common adverse events have been application site reactions, somnolence, nausea, vomiting, dizziness, dyskinesia, and edema.
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