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.

One capsule contains 1.5 mg, 3 mg, 4.5 mg or 6 mg of rivastigmine in the form of 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 increased 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%). researchin vitro and animal studies have shown that the main cytochrome P450 isoenzymes play only a minor role in rivastigmine metabolism. 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. Severe hepatic impairment (due to lack of research in this group of patients).

The drug is not recommended for use in children and adolescents (under 18 years of age). Rivastigmine has not been studied in patients with very advanced dementia in Alzheimer's disease or in Parkinson's disease, other types of dementia or other types of memory impairment (eg age-related cognitive impairment), and therefore rivastigmine is not recommended in this patient group. Use with caution in patients with sinus node syndrome or conduction disorders (sinoatrial block, atrioventricular block); in patients with active gastric or duodenal ulcer disease, as well as in patients with predisposition to these diseases; in patients with a history of bronchial asthma or obstructive pulmonary disease; in patients with tendencies to urinary tract obstruction and seizures. Like other cholinomimetics, rivastigmine may exacerbate or induce extrapyramidal symptoms (including motor retardation, dyskinesias, gait disturbances, tremor), especially in patients with dementia associated with Parkinson's disease - patients should be monitored for these side effects.

Do not use 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 common: dizziness; nausea, vomiting, diarrhea; lack of appetite.Common: agitation, confusion; headache, drowsiness, tremor; abdominal pain and dyspepsia; excessive sweating; tiredness, asthenia; bad mood; weight loss. Uncommon: insomnia, depression; swoon; increased values ​​of liver function tests; casual fall. Rare: convulsions; angina pectoris; peptic ulcer of the stomach and duodenum; rash. Very rare: urinary tract infections; hallucinations; extrapyramidal symptoms (including worsening of patients with Parkinson's disease); cardiac arrhythmias (e.g. bradycardia, atrioventricular block, atrial fibrillation, tachycardia), arterial hypertension; gastrointestinal bleeding, pancreatitis. Frequency unknown: cases of severe vomiting associated with esophageal rupture.Patients with dementia associated with Parkinson's disease. Very often: tremor; nausea, vomiting, lack of appetite. Common: insomnia, anxiety, anxiety; dizziness, drowsiness, headache, worsening of Parkinson's disease, slowness of movement, dyskinesia; bradycardia; diarrhea, abdominal pain, indigestion, excessive salivation; excessive sweating; muscle stiffness; tiredness, asthenia, dehydration; gait disturbances. Uncommon: dystonia, atrial fibrillation, atrioventricular block. Side effects (eg hypertension, hallucinations in patients with dementia found in Alzheimer's disease and exacerbation of extrapyramidal symptoms, especially tremor in patients with dementia associated with Parkinson's disease) have been observed shortly after increasing the dose. These effects may resolve after dose reduction; in the remaining cases, rivastigmine was discontinued.

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 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 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 after at least 2 weeks 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 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 moderate renal impairment and mild to moderate hepatic impairment, the dose should be carefully adjusted according to individual tolerability.
The preparation in the form of capsules should be taken with the morning and evening meals. Swallow the capsules whole.