(roe TIG oh teen)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Patch 24 Hour, Transdermal:
Neupro: 1 mg/24 hr (30 ea); 2 mg/24 hr (30 ea); 3 mg/24 hr (30 ea); 4 mg/24 hr (30 ea); 6 mg/24 hr (30 ea); 8 mg/24 hr (30 ea) [contains sodium metabisulfite]
Brand Names: U.S.
- Anti-Parkinson's Agent, Dopamine Agonist
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.
Vd: ~84 L/kg
Extensive via conjugation and N-dealkylation; multiple CYP isoenzymes, sulfotransferases, and two UDP-glucuronosyltransferases involved in catalyzing the metabolism
Urine (~71% as inactive conjugates and metabolites, <1% as unchanged drug); feces (~23%)
Time to Peak
15 to 18 hours; can occur 4 to 27 hours post application
After removal of patch: ~5 to 7 hours
Special Populations: Renal Function Impairment
In subjects with severe renal impairment not on dialysis (eg, CrCl 15 to <30 mL/minute), exposure to conjugated rotigotine metabolites was doubled.
Special Populations: Elderly
Although not studied, exposures in older subjects (older than 80 years of age) may be higher because of skin changes with aging.
Use: Labeled Indications
Parkinson disease: For the treatment of Parkinson disease.
Restless legs syndrome: For the treatment of moderate to severe primary restless legs syndrome.
Hypersensitivity to rotigotine or any component of the formulation
Parkinson disease: Topical: Transdermal:
Early-stage: Initial: Apply 2 mg/24 hours patch once daily; may increase by 2 mg/24 hours weekly, based on clinical response and tolerability; lowest effective dose: 4 mg/24 hours (manufacturer recommends a maximum dose of 6 mg/24 hours; higher doses [eg, 8 mg/24 hours] have been studied in clinical trials [Giladi 2007]).
Advanced-stage: Initial: Apply 4 mg/24 hours patch once daily; may increase by 2 mg/24 hours weekly, based on clinical response and tolerability. Recommended dose: 8 mg/24 hours; in clinical trials maximum doses up to 16 mg/24 hours were used.
Discontinuation of treatment in Parkinson’s disease: Decrease by ≤2 mg/24 hours preferably every other day until withdrawal complete
Restless legs syndrome (RLS): Topical: Transdermal: Initial: Apply 1 mg/24 hours patch once daily; may increase by 1 mg/24 hours weekly, based on clinical response and tolerability; lowest effective dose: 1 mg/24 hours (maximum dose: 3 mg/24 hours)
Discontinuation of treatment for RLS: Decrease by 1 mg/24 hours preferably every other day until withdrawal complete
Refer to adult dosing.
Dosing: Renal Impairment
Mild-to-severe impairment (CrCl ≥15 mL/minute): No dosage adjustment necessary.
End-stage renal disease (ESRD) requiring hemodialysis: No dosage adjustment necessary.
Dosing: Hepatic Impairment
Mild-to-moderate hepatic impairment (Child-Pugh class A or B): No dosage adjustment necessary.
Severe hepatic impairment: There are no dosage adjustments provided in manufacturer's labeling (has not been studied).
Transdermal patch: Apply patch to clean, dry, hairless area of intact healthy skin on the front of the abdomen, thigh, hip, flank, shoulder, or upper arm at approximately the same time daily. Remove from pouch immediately before use and press patch firmly in place on skin for 30 seconds. Application sites should be rotated on a daily basis. Do not apply to same application site more than once every 14 days or apply patch to oily, irritated or damaged skin. Avoid exposing patch to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub, direct sunlight). If applied to hairy area, shave ≥3 days prior to applying patch. If patch falls off, immediately apply a new one to a new site.
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.
Alcohol (Ethyl): May enhance the sedative effect of Rotigotine. Monitor therapy
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification
Amisulpride: Anti-Parkinson Agents (Dopamine Agonist) may diminish the therapeutic effect of Amisulpride. Amisulpride may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Avoid combination
Antipsychotic Agents (First Generation [Typical]): Anti-Parkinson Agents (Dopamine Agonist) may diminish the therapeutic effect of Antipsychotic Agents (First Generation [Typical]). Antipsychotic Agents (First Generation [Typical]) may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Management: Avoid concomitant therapy if possible and monitor for decreased effects of both agents when these combinations cannot be avoided. Atypical antipsychotics such as clozapine and quetiapine may be less likely to reduce the effects of anti-Parkinson agents. Consider therapy modification
Antipsychotic Agents (Second Generation [Atypical]): May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Management: Consider using an alternative antipsychotic agent when possible in patients with Parkinson disease. If an atypical antipsychotic is necessary, consider using clozapine or quetiapine, which may convey the lowest interaction risk. Consider therapy modification
Blood Pressure Lowering Agents: May enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
BuPROPion: Anti-Parkinson Agents (Dopamine Agonist) may enhance the adverse/toxic effect of BuPROPion. Monitor therapy
CNS Depressants: May enhance the sedative effect of Rotigotine. Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy
Levodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa. Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Methylphenidate: May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist). Monitor therapy
Metoclopramide: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Sulpiride: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Avoid combination
Cardiovascular: Systolic hypotension (13% to 32%), peripheral edema (dose related; 3% to 14%)
Central nervous system: Drowsiness (dose related; 5% to 32%), orthostatic hypotension (8% to 29%), dizziness (5% to 23%), headache (10% to 21%), fatigue (6% to 18%), sleep disorder (disturbance in initiating/maintaining sleep; dose related; 2% to 14%), malaise (≤14%), hallucination (dose related; 3% to 13%), insomnia (7% to 11%)
Dermatologic: Hyperhidrosis (dose related; 1% to 11%)
Endocrine & metabolic: Decreased serum glucose (1% to 15%)
Gastrointestinal: Nausea (dose related; 15% to 48%), vomiting (dose related; 2% to 20%)
Hematologic & oncologic: Decreased hematocrit (8% to 17%), decreased hemoglobin (8% to 15%)
Local: Application site reaction (dose related; 21% to 46%)
Neuromuscular & skeletal: Dyskinesia (dose related; 14% to 17%), weakness (≤14%), arthralgia (8% to 11%)
1% to 10%:
Cardiovascular: Increased diastolic blood pressure (4% to 8%), systolic hypertension (5%), hypertension (dose related; 1% to 5%), atrioventricular block (3%), abnormal T waves on ECG (≤3%), syncope
Central nervous system: Abnormal dreams (dose related; 1% to 7%), nightmares (dose related; 3% to 5%), depression (2% to 5%), paresthesia (dose related; 4%), vertigo (3% to 4%), equilibrium disturbance (2% to 3%), irritability (1% to 3%), sleep attacks (dose related; 1% to 2%)
Dermatologic: Pruritus (4% to 9%), erythema (dose related; 2% to 6%)
Endocrine & metabolic: Weight gain (2% to 9%), change in libido (4% to 6%), hot flash (3% to 4%), low serum ferritin (dose related; 2%), menstrual disorder (1% to 2%)
Gastrointestinal: Constipation (5% to 9%), anorexia (2% to 9%), xerostomia (dose related; 7%), diarrhea (5% to 7%), dyspepsia (dose related; 2% to 3%), viral gastroenteritis (1% to 2%)
Genitourinary: Change in WBC count (urine, ≤3%)
Hematologic & oncologic: Basal cell carcinoma (3%), leukocyturia (3%)
Infection: Herpes simplex infection (3%)
Neuromuscular & skeletal: Tremor (4%), muscle spasm (dose related; 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%), sinus congestion (2% to 3%), sinusitis (dose related; 2% to 3%)
Miscellaneous: Hiccups (dose related; 2% to 3%)
<1% (Limited to important or life-threatening): Confusion, delirium, delusions, impulse control disorder, increased creatine phosphokinase, neuroleptic malignant syndrome, paranoia, psychotic symptoms
Concerns related to adverse effects:
• Application site reactions: Dose-dependent application site reactions, potentially severe, have been observed; daily rotation of application sites has been shown to decrease incidence of reactions. If a generalized (nonapplication site) skin reaction occurs; discontinue therapy.
• Fibrosis: Rare cases of pleural effusion, pleural thickening, pulmonary infiltrates, retroperitoneal fibrosis, pericarditis and/or cardiac valvulopathy have been reported in patients treated with ergot-derived dopamine agonists. The potential of rotigotine, a nonergot derived dopamine agonist, to cause similar fibrotic complications is unknown. Discontinuation of therapy may resolve complications, but not in all cases.
• Fluid retention: Weight gain and fluid retention have been reported, primarily associated with development of peripheral edema in Parkinson disease patients; use caution and monitor for weight gain in patients with concomitant illnesses (eg, heart failure or renal insufficiency).
• Hallucinations/psychotic-like behavior: May cause hallucinations (dose-related) and other psychotic-like behaviors (eg, agitation, delirium, delusions, aggression). In general, avoid use in patients with preexisting major psychotic disorders.
• Impulse control disorders: Dopamine agonists used for Parkinson disease or restless legs syndrome have been associated with compulsive behaviors and/or loss of impulse control, which has manifested as pathological gambling, libido increases (hypersexuality), and/or binge eating. Causality has not been established, and controversy exists as to whether this phenomenon is related to the underlying disease, prior behaviors/addictions and/or drug therapy. Dose reduction or discontinuation of therapy has been reported to reverse these behaviors in some, but not all cases.
• Melanoma: Risk for melanoma development is increased in Parkinson’s disease patients; drug causation or factors contributing to risk have not been established. Patients receiving therapy for any indication should be monitored closely and periodic skin examinations should be performed.
• Orthostatic hypotension: Dopamine agonists may cause orthostatic hypotension and syncope; Parkinson’s disease patients appear to have an impaired capacity to respond to a postural challenge. Use with caution in patients at risk of hypotension (such as those receiving antihypertensive drugs) or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Parkinson’s and RLS patients being treated with dopaminergic agonists ordinarily require careful monitoring for signs and symptoms of postural hypotension, especially during dose escalation, and should be informed of this risk.
• Somnolence: Use is commonly associated with somnolence. In addition, falling asleep during activities of daily living, including while driving, has also been reported and may occur without significant warning signs. Monitor for daytime somnolence or pre-existing sleep disorder. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive agents; discontinue if significant daytime sleepiness or episodes of falling asleep occur. Effects with other sedative drugs or ethanol may be potentiated.
• Cardiovascular disease: Use with caution in patients with pre-existing cardiovascular disease; therapy has been associated with increases in blood pressure (as well as orthostatic hypotension), which may be significant (>40 mm Hg or ≥20 mm Hg increase in systolic or diastolic measurements, respectively), increased heart rate, syncope, and weight gain/fluid retention.
• Dyskinesia: Use with caution in patients with preexisting dyskinesia; therapy may cause or exacerbate dyskinesia.
• Restless legs syndrome (RLS): Augmentation (earlier onset of symptoms each day and/or an overall increase in symptom severity) or rebound (considered to be an end of dose effect) may occur in some patients with RLS.
Dosage form specific issues:
• Aluminum: Patch contains aluminum; remove patch prior to magnetic resonance imaging or cardioversion to avoid skin burns.
• Heat application: Avoid exposure of application site to any direct external heat sources (eg, hair dryers, heating pads, electric blankets, saunas, hot tubs, direct sunlight); heat exposure has not been studied with the rotigotine patch, but an increase in the rate and extent of absorption has been observed with other transdermal products.
• Sulfites: Patch contains sodium metabisulfite which may cause allergic reaction in susceptible individuals.
• Discontinuation of therapy: Taper treatment when discontinuing therapy; do not stop abruptly. Other dopaminergic agents have been associated with a syndrome resembling neuroleptic malignant syndrome on withdrawal and/or significant dosage reduction.
Blood pressure (including orthostatic); daytime alertness; periodic skin evaluations (melanoma development)
Pregnancy Risk Factor
Adverse events have been observed in animal reproduction studies.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience nausea, vomiting, constipation, lack of appetite, nightmares, diarrhea, fatigue, dry mouth, sweating a lot, loss of strength and energy, insomnia, application site irritation, or joint pain. Have patient report immediately to prescriber uncontrollable urges, severe dizziness, passing out, confusion, skin growths, mole changes, severe headache, angina, tachycardia, abnormal heartbeat, mood changes, hallucinations, behavioral changes, muscle pain, muscle rigidity, abnormal movements, decreased libido, severe skin irritation, weight gain, swelling of arms or legs, vision changes, or narcolepsy (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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