Critical appraisal of rotigotine transdermal system in management of Parkinson’s disease and restless legs syndrome – patient considerations

Abstract

Rotigotine (RTG) is a dopamine agonist that is used as mono and adjunct therapy to treat Parkinson's disease, and as therapy for moderate-to-severe restless legs syndrome. RTG is the only dopamine agonist currently available as a 24-hour/day transdermal system, providing once-a-day dosing. As a transdermal patch, RTG bypasses the gastrointestinal tract, making it a treatment option for patients with dysphagia. The use of RTG also avoids the need to schedule administration of medication around meals. This review provides a critical appraisal of RTG as treatment of Parkinson's disease and RLS. PharmacologyRTG is a non-ergot DA at D1-D5 receptors, as well as 5-HT1A serotonergic, and α-2adrenergic receptors. [1][2][3][4] Binding and functional assessments of RTG with recombinant receptors demonstrate a high affinity for D3 and D2 receptors, and is best described as a D3/D2/D1 receptor agonist. 1,4 RTG, (6S)-6-(propyl[2-{2-thienyl}ethyl]amino)-5,6,7,8-tetrahydro-1-naphthalenol, has a molecular weight of 315.48 Da and its empirical formula is C 19 H 25 NOS. 1,5 Figure 1 shows the structural representation of RTG. It is available only in a transdermal patch form, which is composed of a backing film made of an aluminized polyester film with a pigment coat. A self-adhesive drug matrix layer contains the active ingredient along with ascorbyl palmitate, povidone, silicone adhesive, sodium metabisulfite, and dl-α-tocopherol as inactive ingredients. 5 RTG is formulated in a transdermal system, with a terminal half-life of 5-7 hours. 6

Clinical Evaluation of Sleep Disorders in Parkinson’s Disease

“…In a randomized controlled study of over 300 patients, the efficacy of levodopa and cabergoline in the treatment of RLS was compared; the study showed a greater efficacy on symptoms for the cabergoline treatment, while patients in the levodopa treatment group reported better tolerability [ 103 ]. Pramipexole, rotigotine, and ropinirole have also shown good efficacy in controlling RLS symptoms [ 104 , 105 , 106 ]. Finally, both immediate-release and extended-release ropinirole have been shown to have a significant effect in mitigating daytime sleepiness episodes in EDS [ 107 ].…”