Drug information of Rotigotine
Rotigotine transdermal (skin patch) is used to treat symptoms of Parkinson's disease, such as stiffness, tremors, muscle spasms, and poor muscle control.
Rotigotine is also used to treat restless legs syndrome (RLS).
Mechanism of effect
Rotigotine is a nonergot dopamine agonist with specificity for D3-, D2-, and D1-dopamine receptors. Although the precise mechanism of action of rotigotine is unknown, it is believed to be due to stimulation of postsynaptic dopamine D2-type auto receptors within the substantia nigra in the brain, leading to improved dopaminergic transmission in the motor areas of the basal ganglia, notably the caudate nucleus/putamen regions.
Extensive via conjugation and N-dealkylation; multiple CYP isoenzymes, sulfotransferases, and two UDP-glucuronosyltransferases involved in catalyzing the metabolism
Time to reach the peak
15 to 18 hours; can occur 4 to 27 hours post application
Vd: ~84 L/kg
After removal of patch: ~5 to 7 hours
Urine (~71% as inactive conjugates and metabolites, <1% as unchanged drug); feces (~23%)
1-Treatment of Parkinson's disease
2-Treatment of moderate-to-severe primary Restless Legs Syndrome
Usual Adult Dose for Parkinson's Disease:
Early-stage Parkinson's disease: Apply 2 mg topically once a day
Advanced-stage Parkinson's disease: Apply 4 mg topically once a day
Maintenance dose: Increase weekly in 2 mg/24 hours increments if additional therapeutic effect is needed
Lowest effective dose: 4 mg/24 hours
Maximum dose for Early-stage Parkinson's disease: 6 mg/24 hours
Maximum dose for Advanced-stage Parkinson's disease: 8 mg/24 hours
Usual Adult Dose for Restless Legs Syndrome:
Initial dose: Apply 1 mg topically once a day
Maintenance dose: Increase weekly in 1 mg/24 hours increments if additional therapeutic effect is needed
Lowest effective dose: 1 mg/24 hours
Maximum dose: 3 mg/24 hours
1-Safety and efficacy have not been established in patients younger than 18 years.
2-Hypersensitivity to rotigotine or any component of the formulation
Cardiovascular: Systolic hypotension (13% to 32%), orthostatic hypotension (8% to 29%), peripheral edema (3% to 14%)
Central nervous system: Drowsiness (5% to 32%), dizziness (5% to 23%), headache (10% to 21%), fatigue (6% to 18%), malaise (≤14%), sleep disorder (disturbance in initiating/maintaining sleep; 2% to 14%), hallucination (3% to 13%)
Dermatologic: Hyperhidrosis (1% to 11%)
Endocrine & metabolic: Decreased serum glucose (1% to 15%)
Gastrointestinal: Nausea (15% to 48%), vomiting (2% to 20%)
Hematologic & oncologic: Decreased hematocrit (8% to 17%), decreased hemoglobin (8% to 15%)
Local: Application site reaction (21% to 46%)
Neuromuscular & skeletal: Dyskinesia (14% to 17%), asthenia (≤14%), arthralgia (8% to 11%)
1% to 10%:
Cardiovascular: Increased diastolic blood pressure (4% to 8%), systolic hypertension (5%), hypertension (1% to 5%), atrioventricular block (3%), hypoesthesia (3%), abnormal T waves on ECG (2% to 3%)
Central nervous system: Abnormal dreams (1% to 7%), nightmares (3% to 5%), paresthesia (3% to 4%), vertigo (3% to 4%), depression (2% to 3%), equilibrium disturbance (2% to 3%), irritability (1% to 3%), sudden onset of sleep (1% to 2%)
Dermatologic: Pruritus (4% to 9%), erythema (2% to 6%)
Endocrine & metabolic: Weight gain (2% to 9%), change in libido (4% to 6%), hot flash (3% to 4%), low serum ferritin (2%), menstrual disease (1% to 2%)
Gastrointestinal: Constipation (5% to 9%), anorexia (2% to 9%), xerostomia (7%), diarrhea (5% to 7%), dyspepsia (2% to 3%), viral gastroenteritis (1% to 2%)
Hematologic & oncologic: Basal cell carcinoma (3%), leukocyturia (3%)
Infection: Herpes simplex infection (3%), influenza (1% to 3%)
Neuromuscular & skeletal: Tremor (4%), muscle spasm (3% to 4%)
Ophthalmic: Visual disturbance (3% to 5%)
Otic: Tinnitus (2% to 3%)
Renal: Increased blood urea nitrogen (3% to 11%)
Respiratory: Nasopharyngitis (8% to 10%), cough (3%), nasal congestion (3%), paranasal sinus congestion (2% to 3%), sinusitis (2% to 3%)
InteractionsNitroprusside sodium , Sodium Oxybate , Butalbital and Acetaminophen , Ramelteon , Brimonidine , Bupropion , pentoxifylline , Duloxetine , Diazoxide , Metoclopramide , Pholcodine , Quinagolide , Solriamfetol , Sulpiride , Alizapride , Lormetazepam , Molsidomine , Naftopidil , Nicergoline , Obinutuzumab , Nicorandil , Amifostine , Dexmethylphenidate , Alfuzosin , Amisulpride , Bromperidol , Secobarbital , Tolcapone , Clorazepate , Quazepam , Opium , Bromopride , ethotoin
Alcohol (Ethyl), Alfuzosin, Alizapride, Amifostin,Amisulpride, Antipsychotic Agents (First Generation [Typical]), Antipsychotic Agents (Second Generation [Atypical]), Blood Pressure Lowering Agents, Brimonidine (Topical), Bromopride, Bromperidol, BuPROPion, CNS Depressants, Diazoxide, DULoxetine, Herbs (Hypotensive Properties), Hypotension-Associated Agents, Levodopa-Containing Products, Lormetazepam, Methylphenidate, Metoclopramide, Molsidomine, Naftopidil, Nicergoline, Nicorandil, Nitroprusside, Obinutuzumab, Pentoxifylline,Pholcodine, Phosphodiesterase 5 Inhibitors, Prostacyclin Analogues, Quinagolide, Solriamfetol,Sulpiride
1-Drinking alcohol with rotigotine can increase side effects.
2-Avoid applying a patch to skin that is irritated, or to skin where you have applied lotion, oil, cream, ointment, or powder.
3-Do not expose the skin patch to heat while you are wearing it. This includes a hot tub, heating pad, sauna, or heated water bed. Heat can increase the amount of drug absorbed through your skin and may cause harmful effects.
Points of recommendation
1-Tell your doctor if you have ever had:
-asthma or a sulfite allergy
-high or low blood pressure
-schizophrenia, bipolar disorder, or psychosis
-narcolepsy or other sleep disorder
-if you feel light-headed or nauseated when you stand up
2-Apply the patch to clean, dry, and hairless skin. Avoid placing the patch where it will be rubbed by a waistband or tight clothing. Press the patch firmly into place for about 30 seconds. You may leave the patch on while bathing, showering, or swimming.
3-Remove the skin patch after 24 hours and replace it with a new one. Choose a different place on your body to wear the patch each time you put on a new one. Do not use the same skin area twice within 14 days.
4-If a patch falls off, put a new patch on a different place on your body and wear it the rest of the day. Then replace the patch the next day at your regular time.
5-The rotigotine patch may burn your skin if you wear the patch during an MRI (magnetic resonance imaging). Remove the patch before undergoing such a test.
6-Do not stop using rotigotine suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using rotigotine.
7-Upon discontinuation, reduce the daily dose by a maximum of 2 mg every 24 hours, if possible; reduce the dose every other day until withdrawal is complete.
Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15ºC and 30ºC (59ºF and 86ºF). Store in original pouch until application.
Pregnancy levelHAVE NOT BEEN ESTABLISHED
There are no adequate data on developmental risk associated with use in pregnant women
Breast feeding warning
There are no data on presence of drug in human milk, effects on the breastfed infant, or on milk production; however, inhibition of lactation may occur because drug decreases secretion of prolactin in humans; studies have shown that rotigotine and/or its metabolite(s) are excreted in rat milk.