Rotigotine
Rotigotine Uses, Dosage, Side Effects, Food Interaction and all others data.
Rotigotine (Neupro) is a non-ergoline dopamine agonist indicated for the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS) in Europe and the United States. It is formulated as 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.
Rotigotine was developed by Aderis Pharmaceuticals. In 1998 Aderis licensed worldwide development and commercialization rights to Schwarz Pharma of Germany. It was approved by the European Medicines Agency in 2006 and by the FDA in 2007. However, all Neupro patches in the United States and some of Europe were recalled in 2008 due to delivery mechanism issues. Rotigotine has been authorized as a treatment for RLS since August 2008.
| Trade Name | Rotigotine |
| Availability | Prescription only |
| Generic | Rotigotine |
| Rotigotine Other Names | Rotigotina, Rotigotine |
| Related Drugs | Neupro, Azilect, Duopa, Apokyn, Xadago, Ongentys, Gocovri, Rytary, Sinemet, Sinemet CR |
| Weight | 1mg/24hr, 2mg/24hr, 3mg/24hr, 4mg/24hr, 6mg/24hr, 8mg/24hr |
| Type | Transdermal film, extended release, transdermal |
| Formula | C19H25NOS |
| Weight | Average: 315.48 Monoisotopic: 315.165685603 |
| Protein binding | 92% in vitro and 89.5% in vivo. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rotigotine is a non-selective dopamine agonist used for the treatment of Parkinson's Disease and Restless Leg Syndrome.
For use/treatment in neurologic disorders and parkinson's disease as well as moderate-to-severe primary Restless Legs Syndrome.
Rotigotine is also used to associated treatment for these conditions: Parkinson's Disease (PD), Severe restless legs syndrome (RLS), Moderate restless leg syndrome
How Rotigotine works
Rotigotine, a member of the dopamine agonist class of drugs, is delivered continuously through the skin (transdermal) using a silicone-based patch that is replaced every 24 hours. A dopamine agonist works by activating dopamine receptors in the body, mimicking the effect of the neurotransmitter dopamine. The precise mechanism of action of rotigotine as a treatment for Restless Legs Syndrome is unknown but is thought to be related to its ability to stimulate dopamine
Toxicity
The most likely symptoms of overdose would be those related to the pharmacodynamic profile of a dopamine agonist, including nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions, and other signs of excessive dopaminergic stimulation.
Food Interaction
No interactions found.[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Rotigotine Drug Interaction
Moderate: rasagiline, diphenhydramine, duloxetine, escitalopram, pregabalin, carbidopa / entacapone / levodopaUnknown: amphetamine / dextroamphetamine, amoxicillin / clavulanate, celecoxib, heparin, atorvastatin, mirabegron, acetaminophen, vitamin a topical, bioflavonoids, carbidopa / levodopa, sotalol, cyanocobalamin, ascorbic acid, cholecalciferol
Rotigotine Disease Interaction
Major: hypotension, psychosisModerate: asthma, cardiovascular disease, fluid retention
Volume of Distribution
The weight normalized apparent volume of distribution, (Vd/F), in humans is approximately 84 L/kg after repeated dose administration.
Elimination Route
Bioavailability varies depending on the application site. Differences in bioavailability were very small between the abdomen and hip (<1%). In contrast, the shoulder and thigh had a very large different in measured bioavailability (46%), with the shoulder showing the higher value. Tmax, 8 mg dose = 15 - 18 hours (it take approximately 3 hours until rotigotine reaches detectable levels in the plasma). The peak concentration cannot be observered. Steady state is reached in 2-3 days.
Half Life
After removal of the patch, plasma levels decreased with a terminal half-life of 5 to 7 hours. The pharmacokinetic profile showed a biphasic elimination with an initial half-life of 3 hours.
Elimination Route
Urine (71%), Fecal (23%). Most of rotigotine that is excreted in the urine is in the form of inactive conjugates. Unchanged drug made up less <1%.
Innovators Monograph
You find simplified version here Rotigotine
