Treatment of the signs and symptoms of idiopathic Parkinson's disease (early-stage to advanced-stage disease).
#仿單變更2021
藥理
Rotigotine is a nonergot dopamine agonist with specificity for D3, D2, and D1dopamine 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.
藥動學
Approximately 45% of the active substance within the patch is released to the skin in 24 hours. Protein binding: ~90%, Excretion: Urine (~71% as inactive conjugates and metabolites, <1% as unchanged drug); feces (~23%). Half-life elimination: After removal of patch: ~5-7 hours.
禁忌症
Hypersensitivity to the active substance or to any of the excipients. Patients receive magnetic resonance imaging or cardioversion.
懷孕分類
C
哺乳分類
Excretion in breast milk unknown/use caution.
副作用
Common:
Cardiovascular: Orthostatic hypotension (Parkinson disease, 16% to 32%; restless legs syndrome, 8% to 13% ), Peripheral edema (2% to 9% )
Dermatologic: Application site reaction (19% to 43% ), Diaphoresis (1% to 11% )
Gastrointestinal: Loss of appetite (2% to 9% ), Nausea (Parkinson disease, 28% to 48%; restless legs syndrome, 15% to 23% ), Vomiting (Parkinson disease, 10% to 20%; restless legs syndrome, 2% to 4% ), Xerostomia (3% to 7% )
Neurologic: Dizziness (Parkinson disease, 14% to 23%; restless legs syndrome, 5% to 9% ), Dyskinesia (14% ), Headache (10% to 21% ), Sleep disorder (2% to 14% ), Somnolence (5% to 32%; sudden onset of sleep, up to 2% )
Serious:
Cardiovascular: Atrioventricular block, First degree (3% ), Syncope
Psychiatric: Compulsive behavior, Hallucinations (Up to 7% ), Impulse control disorder.
Postmarketing: increased creatine phosphokinase in blood specimen <2021/4/19>
劑量和給藥方法
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; the maximal dose is 8 mg/24 hours.
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; up to a maximal dose of 16 mg/24 hours.