Products
Rotigotine is commercially available as a transdermal patch in various potencies (Neupro). It was approved in many countries in 2006 as the first TTS for Parkinson’s disease therapy.
Structure and properties
Rotigotine (C19H25NOS, Mr = 315.5 g/mol) is an aminotetralin and thiophene derivative structurally related to dopamine. It has a non-ergoline structure and exists as a pure -enantiomer. Rotigotine is lipophilic, has a low molecular mass, 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 due to binding to various dopamine receptors in the central nervous system. Rotigotine has the highest binding affinity to 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 SmPC. The patch is applied once daily at the same time of day, regardless of meals, and remains on the skin for 24 hours. The site should be changed daily. The patch should be applied to clean, dry and uninjured skin. Possible application sites include the abdomen, thighs, hips, or upper arm. See also under transdermal patches.
Contraindications
- Hypersensitivity
- Magnetic resonance imaging (MRI)
- Cardioversion
- Severe hepatic insufficiency
Full precautions can be found in the drug label.
Interactions
Rotigotine is metabolized by several CYP isozymes. Drug-drug interactions have been described with dopamine antagonists, levodopa, central depressant drugs, and alcohol.
Adverse effects
The most common potential adverse effects include nausea, vomiting, application site reactions, drowsiness, dizziness, and headache.
