Categories
Uncategorized

Rotigotine

Rotigotine Trade name Neupro

Pregnancy category AU: B3

Routes of administration-Transdermal patch

Bioavailability 37% transdermally

Protein binding 92%

Metabolism Hepatic (CYP-mediated)

Elimination half-life 5–7 hours

Excretion Urine (71%), Fecal (23%)

Rotigotine, is a dopamine agonist of the non-ergoline class of medications indicated for the treatment of Parkinson’s disease and restless legs syndrome.

It is a once-daily transdermal patch which provides a slow and constant supply of the drug over the course of 24 hours.

Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well.

Side effects include  constipation, dyskinesia, nausea, vomiting, dizziness, fatigue, insomnia, somnolence, confusion, and hallucinations.

More serious complications can include psychosis and impulse control disorders like hypersexuality, punding, and pathological gambling.

Mild adverse skin reactions at the patch application site may also occur.[

Rotigotine acts as a non-selective agonist of the dopamine D1, D2, D3, and, to a lesser extent, D4 and D5 receptors,

It has the highest affinity for the D3 receptor.

It has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor.

In functional studies however, rotigotine behaves as a full agonist of D1, D2, and D3 with similar potencies.

At clinical doses rotigotine behaves mostly as a selective D1-like (D1, D5) and D2-like (D2, D3, D4) receptor agonist, with its α2B-adrenergic and 5-HT1A activity also possibly having some minor relevance.

Leave a Reply

Your email address will not be published. Required fields are marked *