What is rotigotine


RotigotineDrug groupsDopamine agonists Rotigotine is an active ingredient from the group of dopamine agonists with dopaminergic properties in the central nervous system. It is used in the form of a transdermal patch to treat Parkinson's disease and restless legs syndrome. The patch is applied once a day at the same time of day for 24 hours and continuously releases the active ingredient through the skin into the bloodstream. The job should be changed daily. The most common possible adverse effects include nausea, vomiting, application site reactions, drowsiness, dizziness, and headache.

synonymous: Rotigotinum, N-0437, N-0923

Products

Rotigotine is commercially available as a transdermal patch in various strengths (Neupro®). It was approved in Switzerland in 2006 as the first TTS for Parkinson's therapy.

Structure and properties

Rotigotine (C.19H25NOS, Mr = 315.5 g / mol) is an aminotetralin and thiophene derivative that is structurally related to dopamine. It has a non-ergoline structure and lies as pure S.-Enantiomer before. Rotigotine is lipophilic, has a low molecular weight and is therefore suitable for transdermal administration. It has high first pass metabolism and low oral bioavailability. Therefore, no oral dosage forms are available.

Effects

Rotigotine (ATC N04BC09) has dopaminergic properties. The effects are based on binding to various dopamine receptors in the central nervous system. Rotigotine has the highest binding affinity for the D3 receptor. The active ingredient is continuously released from the patch through the skin into the bloodstream over 24 hours.

Indications

For the treatment of Parkinson's disease and restless legs syndrome.

dosage

According to the specialist information. The patch is applied once a day, regardless of meals, at the same time of day and remains on the skin for 24 hours. The job should be changed daily. The patch should be placed on clean, dry and uninjured skin. Possible application sites are, for example, the abdomen, thighs, hips or upper arm.

See also → Transdermal patches.

Contraindications
  • Hypersensitivity
  • Magnetic resonance imaging (MRI)
  • Cardioversion
  • Severe hepatic insufficiency

The complete precautionary measures can be found in the product information sheet.

Interactions

Rotigotine is metabolized by various CYP isoenzymes. Drug interactions have been reported with dopamine antagonists, levodopa, central depressant drugs, and alcohol.

unwanted effects

The most common possible adverse effects include nausea, vomiting, application site reactions, drowsiness, dizziness, and headache.

see also

Dopamine agonists, restless legs syndrome, transdermal patches, anti-parkinsonian drugs

literature
  • Pharmaceutical product information (CH, D, USA)
  • Chen J.J., Swope D.M., Dashtipour K., Lyons K.E. Transdermal rotigotine: a clinically innovative dopamine-receptor agonist for the management of Parkinson's disease. Pharmacotherapy, 2009, 29 (12), 1452-67 Pubmed
  • Reading P. Treating restless legs syndrome with rotigotine. Br J Hosp Med (Lond), 2010, 71 (4), 216-9 Pubmed
  • Sanford M., Scott L.J. Rotigotine transdermal patch: a review of its use in the treatment of Parkinson's disease. CNS Drugs, 2011, 25 (8), 699-719 Pubmed
  • Sixel-Döring F., Trenkwalder C. Rotigotine transdermal delivery for the treatment of restless legs syndrome. Expert Opin Pharmacother, 2010, 11 (4), 649-56 Pubmed
author

Conflicts of Interest: None / Independent. The author has no relationships with the manufacturers and is not involved in the sale of the products mentioned.

additional Information
Support PharmaWiki with a donation!

© PharmaWiki 2007-2021 - PharmaWiki provides independent and reliable information about medication and health.
This article was last changed on April 12th, 2020.
Imprint and data protection declaration
Show products for this page