Index of drugs

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.

1 capsule contains 1.5 mg, 3 mg, 4.5 mg or 6 mg of rivastigmine (as hydrogen tartrate).

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 C_max 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 value_max and increases the AUC by approximately 30%. Rivastigmine is associated with proteins in approximately 40%. 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, 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. The drug is excreted mainly in the urine in the form of metabolites.

Hypersensitivity to the active substance, other carbamates or to any of the excipients. Severe liver dysfunction (no studies).

The drug is not recommended for use in children. Rivastigmine has not been studied in patients with severe 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 patient groups 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, as well as with predisposition to these diseases; with bronchial asthma or obstructive pulmonary disease; with tendencies to urinary tract obstruction and seizures.

Do not use during pregnancy unless clearly necessary. Do not use during breast-feeding.

Patients with Alzheimer's dementia. Very common: dizziness, nausea, vomiting, diarrhea, lack of appetite. Common: agitation, confusion, headache, drowsiness, tremor, abdominal pain, indigestion, increased sweating, fatigue, asthenia, malaise, weight loss. Uncommon: insomnia, depression, fainting, increased values ​​of liver function tests, accidental fall. Rare: convulsions, angina pectoris, peptic ulcer of the stomach and duodenum, rash. Very rare: urinary tract infections, hallucinations, extrapyramidal symptoms (including worsening Parkinson's disease), arrhythmias (eg bradycardia, atrioventricular block, atrial fibrillation, tachycardia), hypertension, gastrointestinal bleeding, pancreatitis. Frequency not known: cases of severe vomiting associated with esophageal rupture, pruritus of the skin. In addition, anxiety, delirium, fever have often been seen in patients using rivastigmine in the transdermal patch.Patients with dementia associated with Parkinson's disease. Very often: tremor, nausea, vomiting.Common: insomnia, anxiety, anxiety, dizziness, drowsiness, headache, worsening Parkinson's disease, slowness of movement, dyskinesia, bradycardia, diarrhea, abdominal pain, indigestion, excessive salivation, increased sweating, muscle stiffness, lack of appetite, dehydration, feeling fatigue, asthenia, gait disturbances. Uncommon: dystonia, atrial fibrillation, atrioventricular block.

Treatment should be initiated and supervised by a physician experienced in the diagnosis and treatment of Alzheimer's dementia or dementia associated with Parkinson's disease. Treatment with rivastigmine can only be undertaken in cases where regular monitoring of the patient's intake is possible. 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 during treatment such as nausea, vomiting, abdominal pain or loss of appetite, weight loss or exacerbation of extrapyramidal symptoms (eg tremor) may disappear 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.
In patients with impaired renal function and mild to moderate hepatic impairment, the dose should be individually adjusted due to the increase in exposure in these patients.
The preparation should be taken twice a day (with morning and evening meals). Swallow the capsules whole.