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).

Rivastigmine is an inhibitor of acetyl- and butyrylcholinesterase from the group of carbamates, which improves cholinergic neurotransmission, by slowing down the process of acetylcholine decomposition released by functionally functional 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 exerts an inhibitory action against cholinesterases, forming a complex with them by means of a covalent linkage, which causes their inactivation temporarily. After oral administration, rivastigmine is absorbed quickly and completely, reaching a maximum blood concentration 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 would result from the increase in 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 plasma 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%). No unchanged rivastigmine was found in the urine. Excretion of metabolites in urine is the main route of elimination. Fewer than 1% of the administered dose is excreted in the faeces.

Hypersensitivity to the active substance, other carbamates or to any of the excipients. Previous reactions at the site of administration, indicative of allergic contact dermatitis after application of a rivastigmine patch.

If there is a suspicion of contact dermatitis after using a rivastigmine patch (if the reactions at the patch site spread to the area of ​​the skin larger than the patch, if there are indications of a greater severity of the local reaction and if within 48 h of the patch removal there is no significant alleviation of symptoms) treatment should be discontinued. Patients with reactions at the patch site indicating allergic contact dermatitis as a result of rivastigmine patch, who still need treatment with rivastigmine, can be switched to oral rivastigmine only after a negative allergy test result and under close medical supervision. It is possible that some patients who are allergic to rivastigmine by contact with rivastigmine-containing patches will not be able to take rivastigmine in any form. If extensive cutaneous hypersensitivity reactions occur after rivastigmine administration, irrespective of the route of administration (oral, transdermal), treatment should be discontinued. Patients with signs and symptoms of dehydration as a result of long-term vomiting or diarrhea may be treated with intravenous fluids and dose reduction or discontinuation of treatment, if the diagnosis and initiation of treatment occur quickly. Dehydration can have serious consequences. Weight loss may occur during treatment - body weight should be monitored. Rivastigmine should be used with caution in patients with a diseased sinus node or with conduction disorders (sinoatrial block, atrioventricular block). The drug should be used with caution in patients with active gastric or duodenal ulcer disease, as well as in patients who are predisposed to these diseases.Cholinesterase inhibitors should be used with caution in patients with a history of bronchial asthma or obstructive pulmonary disease. Cholinomimetics may cause or exacerbate urinary tract obstruction and seizures - the drug should be used with caution in patients who are predisposed to these diseases. 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), and therefore it is not recommended for use in this group of patients. Rivastigmine may increase or induce extrapyramidal symptoms. Intensity (including slowness of movement, dyskinesias, gait disturbances) and an increased incidence or severity of tremor have been observed in patients with dementia associated with Parkinson's disease. Clinical control is recommended for these side effects. Patients with clinically significant renal or hepatic impairment may have more side effects. No studies have been performed in patients with severe hepatic impairment - close monitoring is required in this group of patients. Patients with a body weight below 50 kg may experience more side effects and the risk of stopping treatment due to these activities may be higher. There is no justification for the use of rivastigmine in children and adolescents in the treatment of Alzheimer's dementia.

It must not be used during pregnancy unless clearly necessary. Patients taking rivastigmine should not breast-feed.

The frequency and severity of side effects increase with increasing dose. Nausea and vomiting occur especially in the initial period of treatment and / or during the dose escalation period and are more frequent in women.Patients with Alzheimer's dementia. Very often: lack of appetite, dizziness, nausea, vomiting, diarrhea. Common: agitation, confusion, anxiety, headache, drowsiness, tremor, abdominal pain, dyspepsia, excessive sweating, fatigue, asthenia, malaise, weight loss. Uncommon: insomnia, depression, fainting, increased values ​​of liver function tests, accidental 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), arrhythmias (eg bradycardia, atrioventricular block, atrial fibrillation, tachycardia), hypertension, gastrointestinal bleeding, inflammation of the pancreas. Not known: aggression, restlessness, sick sinus syndrome, cases of severe vomiting associated with esophageal rupture, hepatitis, pruritus, disseminated hypersensitivity reactions. In addition, following the use of the transdermal patch preparation the following side effects were observed: 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: reduced appetite, dehydration, insomnia, anxiety, anxiety, visual hallucinations, depression, dizziness, drowsiness, headache, worsening of Parkinson's disease, slowness of movement, dyskinesia, hypokinesis, "toothed" stiffness, bradycardia, hypertension, diarrhea, abdominal pain, indigestion, excessive salivation, excessive sweating, fatigue, asthenia, gait disturbances. Parkinson walk. Uncommon: dystonia, atrial fibrillation, atrioventricular block, hypotension. Not known: aggression, sick sinus syndrome, hepatitis, disseminated hypersensitivity reactions. In addition, agitation (often) was observed after applying the preparation in the form of a transdermal patch.

Orally. Adults. 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. The diagnosis should be made on the basis of current guidelines. 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 by the patient, after at least 2 weeks of treatment, it can be increased to 3 mg 2 times a day. Subsequent titration up to 4.5 mg, and then up to 6 mg twice daily, is possible with good tolerability of the current dose and may be considered for at least 2 weeks. duration of treatment 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 therapeutic dose is 3-6 mg 2 times a day; in order to achieve maximum therapeutic effect, patients should continue treatment taking the drug at the highest, well-tolerated dose. The recommended maximum daily dose is 6 mg 5 times a day. Maintenance treatment can be continued as long as the therapeutic effect persists. Therefore, the therapeutic effects of rivastigmine should be reassessed regularly, 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. Individual patient response to rivastigmine treatment is unpredictable. However, better treatment outcomes have been seen in patients with Parkinson's disease and moderate dementia and in patients with Parkinson's disease and visual hallucinations. Therapy was not investigated in placebo-controlled clinical trials lasting longer than 6 months. If treatment 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. No dose adjustment is required in patients with mild to moderate renal or hepatic impairment - the dose should be carefully determined in this patient group depending on individual tolerability. Close monitoring is necessary in patients with severe hepatic impairment (no study). The preparation should be taken twice a day, with morning and evening meals. The capsule should be swallowed whole.