Index of drugs

Symptomatic treatment of mild to moderately severe Alzheimer's dementia.

4.6 cm transdermal patch² contains 6.9 mg of rivastigmine - releases 4.6 mg of rivastigmine for 24 h. 9.2 cm transdermal patch² contains 13.8 mg of rivastigmine - releases 9,5 mg of rivastigmine for 24 hours.

Rivastigmine is an inhibitor of acetyl- and butyrylcholinesterase from the group of carbamates, facilitating cholinergic neurotransmission, 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. Absorption of rivastigmine from the transdermal patch is slow. The maximum concentration occurs after 10-16 h. Once the maximum values ​​have been reached, the plasma concentration slowly decreases over the remaining 24-hour period of use. In the case of multiple doses of the drug (as at steady-state), after changing the transdermal patch into a new one, the plasma rivastigmine concentration initially slowly decreases on average for about 40 min, until absorption of the substance from the newly-applied transdermal patch will be faster than it would be. excretion, after which the concentration in the plasma begins to increase again reaching the Next peak after approx. 8 hours. At steady-state, the smallest concentrations constitute approx. 50% of the maximum concentrations, contrary to oral administration, when the concentrations between doses decrease to practically zero. Rivastigmine is poorly bound to plasma proteins (approximately 40%). It easily penetrates the blood-brain barrier. It is rapidly and extensively metabolised; T_0,5 plasma elimination is about 3.4 h after removing the transdermal patch. Metabolism occurs mainly as a result of cholinesterase hydrolysis. Renal excretion of metabolites is the main route of elimination.

Hypersensitivity to rivastigmine, to 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.

Patients with signs and symptoms of dehydration as a result of prolonged vomiting or diarrhea may be treated with intravenous fluids and dose reduction or discontinuation of treatment if the diagnosis is resolved quickly and treatment is started. Weight loss may occur during treatment - body weight should be monitored. Caution should be exercised when prescribing: patients with sick sinus syndrome or conduction disorders (sinoatrial block, atrioventricular block); patients with active peptic ulcer of the stomach or duodenum or patients prone to these diseases, because rivastigmine may increase the secretion of gastric juice; patients prone to obstruction of the urinary tract and seizures, because cholinomimetics may cause or exacerbate these diseases; patients with a history of asthma or obstructive pulmonary disease. After application of the patch with rivastigmine skin reactions may occur at the patching site and their intensity is usually mild to moderate - these reactions do not in themselves indicate sensitization. However, the use of patches with rivastigmine may lead to the development of allergic contact dermatitis. Its occurrence should be suspected if the reactions at the patch site spread to the area of ​​the skin larger than the size of the patch, if there are indications of a greater severity of the local reaction (eg growing erythema, edema, papules, blisters) and if within 48 h of the image the patch will not significantly alleviate symptoms. In such cases, the treatment should be discontinued. Patients with reactions where the patch is sticking to 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 due to contact with patches containing this substance 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.Rivastigmine may increase or induce extrapyramidal symptoms. Avoid contact with the eyes. Incorrect use of the preparation and errors in the dosage of rivastigmine in the form of patches were the cause of serious side effects (some cases required hospitalization and even, though rarely, led to death). In most cases, the mistakes consisted of applying a new patch without removing the previous one and applying multiple patches simultaneously. Patients with mc. less than 50 kg may experience more side effects and the risk of stopping treatment due to these effects may be higher. Patients with clinically significant hepatic impairment and patients with clinically significant renal impairment may have more side effects. There is no justification for the use of rivastigmine in children and adolescents in the treatment of Alzheimer's dementia.

Rivastigmine should not be used during pregnancy unless clearly necessary. Women using rivastigmine should not breast-feed.

Common: urinary tract infections, anorexia, decreased appetite, anxiety, depression, delirium, agitation, headache and dizziness, fainting, nausea, vomiting, diarrhea, indigestion, abdominal pain, rash, incontinence, reactions at the site of hypersecretion (eg erythema , pruritus, edema, dermatitis, irritation at the site of grafting), weakness (eg fatigue, weakness), fever, weight loss. Uncommon: dehydration, aggression, psychomotor hyperactivity, bradycardia, gastric ulcer. Rare: fall. Very rare: extrapyramidal symptoms. Frequency unknown: hallucinations, restlessness, Parkinson's disease, epileptic seizure, atrioventricular block, atrial fibrillation, tachycardia, sick sinus syndrome, arterial hypertension, pancreatitis, hepatitis, increased values ​​of liver function tests, pruritus, erythema, urticaria, blisters, allergic dermatitis, disseminated skin hypersensitivity reactions. The following adverse reactions were observed only after administration of rivastigmine capsules or oral solution, and were not observed in clinical studies with rivastigmine in the form of transdermal patches: drowsiness, malaise, tremor, confusion, severe sweating (common); duodenal ulcers, angina (rare); gastrointestinal haemorrhage (very rare) and cases of severe vomiting associated with esophageal rupture (frequency unknown).

Treatment should be initiated and supervised by a physician experienced in the diagnosis and treatment of Alzheimer's dementia. The diagnosis should be made on the basis of current guidelines. Treatment with rivastigmine can only be started if the patient has a carer who can administer the medicine and monitor the course of treatment. Treatment starts with a dose of 4.6 mg / 24 h. After at least 4 weeks of treatment and if in the opinion of the treating physician it is well tolerated, a dose of 4.6 mg / 24 h should be increased to 9.5 mg / 24 h , which is the recommended effective daily dose, which should be continued for as long as the patient can see the benefits of treatment. If the treatment is well tolerated and only after at least 6 months of treatment with a dose of 9.5 mg / 24 h, the treating physician may consider increasing the dose to 13.3 mg / 24 h in patients with significant cognitive impairment (eg worse MMSE ) and / or deterioration of the functional status (based on the doctor's assessment) during treatment with the recommended effective daily dose of 9.5 mg / 24 h. Clinical benefits of rivastigmine should be regularly evaluated. Discontinuation of treatment should also be considered when there is no evidence of therapeutic effects, despite the use of the optimal dose. Treatment should be temporarily discontinued if gastrointestinal side effects are found until resolution. You can resume treatment with the same dose using the transdermal patch, if the interruption of use lasted no longer than 3 days. Otherwise, start treatment with 4.6 mg / 24 h.Replacement of treatment with capsules or oral solution for patches of the transdermal patch. Due to the comparable exposure in patients treated with rivastigmine capsules or oral solution, the treatment can be changed into a transdermal patch according to the following procedure. A patient receiving a 3 mg / day oral dose may be switched to a 4.6 mg / 24 h transdermal patch. A patient receiving a 6 mg / day oral dose may be switched to a 4.6 mg / 24 transdermal patch. h. A patient receiving a stable, well-tolerated dose of 9 mg / day in oral form can be switched to a transdermal patch at 9.5 mg / 24 h. If the oral dose of 9 mg / day is not stable and well tolerated, it is recommended to change the treatment 4.6 mg / 24 h transdermal patch. Patients taking a 12 mg / day oral dose can be switched to a transdermal patch system at a dose of 9.5 mg / 24 h. After switching to a transdermal patch 4, 6 mg / 24 h, if it is well tolerated for at least 4 weeks of treatment, the dose should be increased to 9.5 mg / 24 h. It is recommended that the first patch be applied the day after the last oral dose. In patients with mc. less than 50 kg should be carefully increased dose and patients should be monitored - if adverse reactions occur, consideration should be given to reducing the maintenance dose to 4.6 mg / 24 h; special care should be taken when increasing the dose to above the recommended effective dose of 9.5 mg / 24 h. No dose adjustment is necessary in patients with impaired hepatic function or in patients with impaired renal function. In these patients, the dose should be carefully determined depending on the individual tolerance. In patients with clinically significant renal or hepatic impairment, a 4.6 mg / 24 h patch should be considered as both the initial dose and the maximum dose. No studies have been performed in patients with severe hepatic impairment. The patches should be applied once a day to clean, dry, hairless and undamaged, healthy skin of the upper or lower back, upper arm or chest, in a place not exposed to abrasion by crimping clothing. It is not recommended to stick the patch on the thigh or stomach due to the reduced bioavailability of rivastigmine observed after applying the transdermal patch to these sites. Do not stick the patch on your skin red, irritated or split. Avoid re-sticking the patch exactly in the same place within 14 days. After removing the patch, wash your hands with soap and water. Every day, before applying a new patch, first remove the patch from the previous day. The patch should be replaced after 24 hours. Only one patch should be used at a time. The patch should be pressed firmly on the inside of the hand and held for at least 30 seconds until the edges of the patch adhere well to the skin. If the patch peels off, apply a new patch for the rest of the day and then replace it with the next day at the usual time. The patch can be used in everyday situations, including during bathing and in hot weather. Do not expose the patch to direct, prolonged exposure to external heat sources (such as excessive sunlight, sauna, solarium). The patch should not be cut into pieces.