Symptomatic treatment of mild to moderately severe Alzheimer's dementia. Symptomatic treatment of mild to moderately severe dementia in patients with idiopathic Parkinson's disease.
Composition:
One capsule contains 1.5 mg, 3 mg, 4.5 mg or 6 mg of rivastigmine in the form of hydrogen tartrate. 1 ml of oral solution contains 2 mg of rivastigmine in the form of hydrogen tartrate.
Action:
An inhibitor of acetyl and butyrylcholinesterases from the group of carbamates. Rivastigmine improves cholinergic neurosynaptic transmission by slowing down the process of acetylcholine decomposition released by functionally efficient cholinergic neurons. Thus, rivastigmine may have a positive effect on cognitive deficits related to cognitive processes in patients with dementia associated with Alzheimer's disease and Parkinson's disease. Rivastigmine is absorbed quickly and completely from the gastrointestinal tract, reaching Cmax after about 1 hour. Due to the effect of rivastigmine on its target enzyme, the increase in bioavailability is about 1.5 times higher than it would result from the increase in the dose. The absolute bioavailability at 3 mg is approximately 36% ± 13%. Administration of rivastigmine with food delays the absorption of the drug by 90 minutes, decreases the C valuemax and increases the AUC by approximately 30%. Rivastigmine is approximately 40% bound to plasma proteins. It easily penetrates the blood-brain barrier. It is rapidly and extensively metabolised (T.0,5 in the blood is about 1 hour), mainly in the hydrolysis reaction, by means of cholinesterase, to the decarbamylated metabolite. The resulting metabolite showsin vitro only a small inhibitory activity against acetylcholinesterase (<10%). Cytochrome P450 enzymes play only a minor role in the metabolism of rivastigmine. It is excreted mainly in the urine in the form of metabolites.
Contraindications:
Hypersensitivity to rivastigmine, other carbamates or to any of the excipients. Allergic contact dermatitis after previous use of rivastigmine in the form of a patch.
Precautions:
Rivastigmine has not been studied in patients with very advanced dementia in Alzheimer's disease or in the course of Parkinson's disease, other types of dementia or other types of memory impairment (eg age-related cognitive impairment) - the use of rivastigmine in these patients is not recommended. Use with caution in patients with sinus node syndrome or conduction disorders (sinoatrial block, atrioventricular block); with active peptic ulcer of the stomach or duodenum and with tendencies to these diseases; with bronchial asthma or obstructive pulmonary disease; with tendencies to urinary tract obstruction and seizures. No studies have been performed in patients with severe hepatic impairment - close monitoring is required when using this medicine in this patient population. Patients with a body weight <50 kg and patients with clinically significant problems with their liver or kidneys may experience more side effects. In women, stomach and intestinal disorders are more common. If you experience side effects that do not improve with rivastigmine, you may need to stop treatment. Treatment with rivastigmine should be discontinued in the event of extensive cutaneous hypersensitivity reactions, regardless of the route of administration. In patients with allergic contact dermatitis rivastigmine in the form of a patch may be treated with oral rivastigmine only after a negative allergy test result and under close medical supervision. The body weight of the patient should be monitored during treatment with rivastigmine. Rivastigmine may increase or induce extrapyramidal symptoms, especially in patients with dementia associated with Parkinson's disease - patients should be monitored for these side effects. There is no suitable use in children and adolescents in the treatment of Alzheimer's dementia. The oral solution contains sodium benzoate, which has a slight irritating effect on the skin, eyes and mucous membranes.
Pregnancy and lactation:
Do not use during pregnancy unless clearly necessary. You should not breast-feed while taking rivastigmine.
Side effects:
Patients with Alzheimer's dementia. Very often: lack of appetite, dizziness, nausea, vomiting, diarrhea. Common: decreased appetite, agitation, confusion, anxiety, headache, drowsiness, tremor, abdominal pain, indigestion, excessive sweating, fatigue, weakness, malaise, weight loss. Uncommon: insomnia, depression, fainting, increased values of liver function tests, fall. Rare: convulsions, angina, gastric and duodenal ulcer, rash. Very rare: urinary tract infections, hallucinations, extrapyramidal symptoms (including deterioration in patients with Parkinson's disease), arrhythmia (eg bradycardia, atrioventricular block, atrial fibrillation, tachycardia), hypertension, gastrointestinal bleeding, pancreatitis . Not known: dehydration, aggression, restlessness, sick sinus syndrome, cases of severe vomiting associated with esophageal rupture, hepatitis, pruritus, allergic dermatitis (sclerosis). Additional side effects were seen after using rivastigmine in the form of a transdermal patch: delirium, fever, decreased appetite, incontinence (common), psychomotor hyperactivity (uncommon), erythema, urticaria, blisters, allergic dermatitis (frequency unknown).Patients with dementia associated with Parkinson's disease. Very often: tremor, nausea, vomiting, fall. Common: decreased appetite, dehydration, insomnia, anxiety, anxiety, visual hallucinations, depression, dizziness, drowsiness, headache, worsening of Parkinson's disease, slowness of movement, dyskinesia, hypokinesis, stiffness of the "gear", bradycardia, hypertension, diarrhea, abdominal pain, indigestion, excessive salivation, sweating, fatigue, weakness, gait disturbance, parkinsonian gait. Uncommon: dystonia, atrial fibrillation, atrioventricular block, hypotension. Not known: aggression, sick sinus syndrome, hepatitis, allergic dermatitis (sclerosis).
Dosage:
Orally. Treatment with rivastigmine can only be started if it is possible to take care of the person responsible for the patient's regular intake of medicine. The starting dose is 1.5 mg 2 times a day. If the dose is well tolerated, it can be increased to 3 mg 2 times a day after at least 2 weeks of treatment. Subsequent titration to 4.5 mg, followed by up to 6 mg twice daily, is possible with good tolerability of the current dose and may be considered after at least a 2-week treatment period with the previous dose. Adverse reactions (eg nausea, vomiting, abdominal pain or loss of appetite), weight loss or exacerbation of extrapyramidal symptoms (eg tremor) in patients with dementia associated with Parkinson's disease, occurring during treatment, may resolve if one or several doses are missed . If side effects persist, the daily dose should be temporarily reduced to the previous well-tolerated dose or treatment should be discontinued. The maintenance dose is 3-6 mg twice daily; for maximum therapeutic effect, patients should continue treatment using the highest, well-tolerated dose. The recommended maximum daily dose is 6 mg 2 times a day. Maintenance treatment can be continued as long as the therapeutic effect persists. Therefore, the therapeutic effect of the medicine should be regularly reassessed, particularly in patients treated with doses lower than 3 mg twice daily. If there is no beneficial change in the relief of dementia after 3 months of treatment, treatment should be discontinued. Discontinuation of treatment should also be considered in the absence of signs of therapeutic effect. Therapy was not investigated in placebo-controlled clinical trials lasting more than 6 months. If rivastigmine was discontinued for more than a few days, treatment should be resumed at 1.5 mg twice daily. Determination of the optimal dose should then take place as described above.Special groups of patients. No dose adjustment is required in patients with mild to moderate renal or hepatic impairment, however, due to increased exposure in these populations, the dose should be carefully determined based on individual tolerability. There have been no studies in patients with severe hepatic impairment, however, the drug can be used in this patient population under strict monitoring. The use of the drug in children and adolescents is not appropriate for the treatment of Alzheimer's dementia.Way of giving. The drug should be taken twice a day (with morning and evening meals). Swallow the capsules whole. The prescribed amount of oral solution should be withdrawn from the bottle using the supplied dosing syringe; the oral solution can be taken directly from the syringe. The oral solution and capsules can be used interchangeably in equal doses.
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