【藥品訊息】 理曼提內服液劑 仿單

Alzheimer dementia: Treatment of mild to moderate dementia of the Alzheimer type.
Parkinson disease dementia: Treatment of mild to moderate dementia associated with Parkinson disease.

Acetylcholinesterase Inhibitor (Central)

Duration: Anticholinesterase activity (CSF): ~10 hours (6 mg oral dose).
Absorption: Bioavailability: Oral: 36%.
Distribution: Vd: 1.8 to 2.7 L/kg; penetrates blood-brain barrier (CSF levels are ~40% of plasma levels following oral administration).
Protein binding: 40%.
Metabolism: Extensively via cholinesterase-mediated hydrolysis in the brain; metabolite undergoes N-demethylation and/or sulfate conjugation hepatically; CYP minimally involved; linear kinetics at 3 mg twice daily, but nonlinear at higher doses.
Half-life elimination: Oral: 1.5 hours; Transdermal patch: ~3 hours (after removal).
Excretion: Urine (97% as metabolites); feces (0.4%).

Hypersensitivity to rivastigmine, other carbamate derivatives, or any component of the formulation.

B (FDA)

Infant risk cannot be ruled out.

Common
Endocrine metabolic: Weight loss (26%, female; 18%, male)
Gastrointestinal: Abdominal pain (13%), Diarrhea (7% to 19%), Indigestion (9%), Loss of appetite (6% to 17%), Nausea (29% to 47%), Vomiting (13% to 31%)
Neurologic: Asthenia (4% to 6%), Dizziness (6% to 21%), Headache (4% to 17%), Tremor (4% to 23%)
Serious
Cardiovascular: Atrial fibrillation (1% or more), Atrioventricular block (0.1% to 1%), Myocardial infarction (1% or more), Peripheral ischemia (0.1% to 1%), Sick sinus syndrome (0.1% to 1%)
Endocrine metabolic: Hypokalemia (1% or more), Hyponatremia (0.1% to 1%)
Gastrointestinal: Gastrointestinal hemorrhage (0.1% to 1%
), Hematemesis (0.1% to 1%), Melena (0.1% to 1%), Pancreatitis (0.1% to 1%), Rectal hemorrhage (0.1% to 1%), Rupture of esophagus.
Hepatic: Gamma-glutamyl transferase raised (0.1% to 1%), Hepatitis, Liver function tests abnormal (0.1% to 1%).
Neurologic: Cerebrovascular accident, Intracranial hemorrhage (0.1% to 1%), Seizure (1% or more), Transient ischemic attack (1% or more).
Ophthalmic: Glaucoma (0.1% to 1%).
Psychiatric: Suicidal behavior.
Renal: Acute renal failure (0.1% to 1%).
Respiratory: Bronchospasm (0.1% to 1%).

Alzheimer's disease - Dementia (Mild to Moderate):
Initial, 1.5 mg orally twice daily for 2 weeks.
Titration, if well tolerated, increase in increments of 1.5 mg orally twice daily at minimum of every 2 weeks; MAX 12 mg/day; if intolerable adverse effects (eg, nausea, vomiting, abdominal pain, loss of appetite), interrupt treatment for several doses and restart at same or lower dose.
Dementia (Mild to Moderate) - Parkinson's disease:
Initial, 1.5 mg orally twice daily for 4 weeks.
Titration, if well tolerated, increase in increments of 1.5 mg orally twice daily at minimum of every 4 weeks; MAX 12 mg/day; if intolerable adverse effects (eg, nausea, vomiting, abdominal pain, loss of appetite), interrupt treatment for several doses and restart at same or lower dose.

Renal impairment, moderate to severe (GFR less than 50 mL/min): use lower doses

Hepatic impairment, mild to moderate (Child-Pugh score 5 to 9): use lower doses; severe impairment, no dosing recommendations available