Clinical pharmacology and efficacy of rotigotine (Neupro® patch) in the treatment of restless leg syndrome

Expert Opin Drug Metab Toxicol. 2016 Aug;12(8):967-75. doi: 10.1080/17425255.2016.1194393. Epub 2016 Jun 16.

Abstract

Introduction: Restless legs syndrome/Willis Ekbom disease (RLS/WED) is a sensorimotor disorder characterized by unpleasant sensations in the legs accompanied by an urge to move them, that typically occurs and tend to worsen in the evening/night or during period of inactivity. Standard medications for RLS/WED are dopamine agonists and calcium channel α-2-δ ligands. The clinical spectrum of RLS/WED is very broad, ranging from individuals suffering from the disease during limited periods up to those severely affected, with daily symptoms. In such cases a long-acting drug like rotigotine should be considered.

Areas covered: The clinical pharmacology and efficacy of rotigotine was examined to evaluate the evidence supporting its use in RLS/WED.

Expert opinion: The rotigotine transdermal patch provides constant delivery of the drug, maintaining a stable plasma concentration over 24 hours by means of a single daily application. Several randomized, double-blind, placebo-controlled trials have demonstrated the efficacy of rotigotine in improving moderate-to-severe RLS/WED symptoms. Rotigotine is generally well tolerated. The most common adverse effects were application-site reactions, dose-dependent, more frequently reported in the first period of treatment. Incidence of augmentation in RLS/WED patients treated with oral dopamine agonists is higher when compared with the use of transdermal rotigotine.

Keywords: Rotigotine; adverse events; augmentation; dopamine agonists; restless leg syndrome.

Publication types

  • Review

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Dopamine Agonists / administration & dosage
  • Dopamine Agonists / pharmacology
  • Dopamine Agonists / therapeutic use*
  • Drug Delivery Systems
  • Humans
  • Randomized Controlled Trials as Topic
  • Restless Legs Syndrome / drug therapy*
  • Restless Legs Syndrome / physiopathology
  • Tetrahydronaphthalenes / administration & dosage
  • Tetrahydronaphthalenes / pharmacology
  • Tetrahydronaphthalenes / therapeutic use*
  • Thiophenes / administration & dosage
  • Thiophenes / pharmacology
  • Thiophenes / therapeutic use*
  • Time Factors
  • Transdermal Patch

Substances

  • Dopamine Agonists
  • Tetrahydronaphthalenes
  • Thiophenes
  • rotigotine