Symptomatic treatment of mild to moderately severe Alzheimer's dementia in adults.
Composition:
A 5 cm transdermal patch2 contains 9 mg of rivastigmine (releases 4.6 mg of rivastigmine over 24 h). A 10 cm transdermal patch2 contains 18 mg of rivastigmine (releases 9,5 mg of rivastigmine over 24 h).
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. Absorption of rivastigmine from the transdermal patch is slow. Cmax is reached after 10-16 h. Once the maximum values have been reached, the concentration slowly decreases over the remaining 24 h of the application period. 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 3.4 h after removing the transdermal patch), mainly in the cholinesterase hydrolysis reaction, 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. No differences were found in Cmax and AUC of rivastigmine in patients with Alzheimer's disease and severe renal impairment, compared to patients with normal renal function.
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:
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; with clinically significant liver dysfunction (risk of severity of side effects); with body weight <50 kg (risk of severity of 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. Allergic contact dermatitis should be suspected if an allergic reaction occurs at the site where the patch is applied, larger than the patch size, if there are indications of a greater severity of the local reaction (eg increasing erythema, edema, papules, blisters) and if Within 48 h of removing the patch, there will be no significant alleviation of symptoms - in such cases the treatment should be discontinued. In patients with allergic contact dermatitis after rivastigmine in the form of a patch, oral rivastigmine may be used, only after a negative allergy test result and under strict medical supervision. In the event of extensive cutaneous hypersensitivity reactions, regardless of the route of administration, treatment with rivastigmine should be discontinued. The body weight of the patient should be monitored during treatment with rivastigmine. Rivastigmine may increase or induce extrapyramidal symptoms - patients should be monitored for these side effects. Avoid eye contact when handling the transdermal patch. There is no suitable use in children and adolescents in the treatment of Alzheimer's dementia.
Pregnancy and lactation:
Do not use during pregnancy unless clearly necessary. You should not breast-feed while taking rivastigmine.
Side effects:
Common: urinary tract infections, anorexia, decreased appetite, anxiety, depression, delirium, agitation, headache, dizziness, fainting, nausea, vomiting, diarrhea, dyspepsia, abdominal pain, incontinence, rash, injection site reactions (e.g. erythema, pruritus, edema, dermatitis, irritation), weakness, fatigue, fever, weight loss. Uncommon: dehydration, aggression, psychomotor hyperactivity, bradycardia, peptic ulcer disease, fall. Very rare: extrapyramidal symptoms. Not known: hallucinations, restlessness, Parkinson's disease, epileptic seizure, tremor, atrioventricular block, atrial fibrillation, tachycardia, sick sinus syndrome, hypertension, pancreatitis, hepatitis, increased values of liver function tests, pruritus, erythema, urticaria, vesicles, allergic dermatitis (sclerosis). 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 a transdermal patch: drowsiness, malaise, confusion, severe sweating (often); duodenal ulcer, angina (rare); gastrointestinal haemorrhage (very rare) and some cases of severe vomiting associated with esophageal rupture (frequency unknown).
Dosage:
Adults. 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 dose4.6 mg / 24 h. If tolerable, after at least 4 weeks of treatment, the dose should be increased to 9.5 mg / 24 h.Maintenance dose: 9.5 mg / 24 h. It can be used for as long as it is beneficial to the patient. If the treatment is well tolerated and only after at least 6 months of treatment with a dose of 9.5 mg / 24 h, a dose increase of up to 13.3 mg / 24 h may be considered for patients with significant cognitive impairment (eg, a worse MMSE study) and (or) deterioration of functional status 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 be considered when there is no evidence of therapeutic effects, despite 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 more than a few days. Otherwise, treatment should start at a dose of 4.6 mg / 24 h.Replacement of treatment with capsules or oral solution on the transdermal patch: a patient taking a dose of 3 mg / day oral rivastigmine can be switched to a 4.6 mg / 24 h transdermal patch; a patient taking a dose of 6 mg / day oral rivastigmine can be switched to a transdermal patch 4.6 mg / 24 h; If you take a steady, well-tolerated dose of 9 mg / day oral rivastigmine, you can switch to a transdermal patch at 9.5 mg / 24 h, if the 9 mg / day oral dose is not well tolerated, it is recommended to switch to a transdermal patch at a dose of 4.6 mg / 24 h; a patient receiving a 12 mg / day oral dose of rivastigmine can be switched to a transdermal patch at 9.5 mg / 24 hrs. After conversion to a dose of 4.6 mg / 24 h of rivastigmine in the form of a transdermal patch, if it is well tolerated by At least 4 weeks of treatment, the 4.6 mg / 24 h dose should be increased to 9.5 mg / 24 h, which is the recommended effective dose of the drug. It is recommended to apply the first transdermal patch the day after the last oral dose.Special groups of patients. There is no need to adjust the dose in patients with impaired renal function. In patients with mild to moderate hepatic impairment, the dose should be carefully determined based on individual tolerability due to increased exposure; special care should be taken when titration is increased in these patients. In patients with mc. <50 kg should be taken with extreme caution increasing the dose to above the recommended effective dose of 9.5 mg / 24 h (increased risk of side effects).There is no proper use of the drug in children and adolescents.Way of giving: for use on skin only. The transdermal patch (patch) 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 that is not exposed to abrasion by crimping clothing. Do not attach to the stomach or thigh. Do not attach to the skin red, irritated or dissected. Avoid re-sticking the patch exactly in the same place within 14 days. Every day, before applying a new patch, first remove the patch from the previous day. Only one patch can be used per day. If the patch is peeled off, a new patch should be applied for the rest of the day and then replaced with a new one for the Next day at the usual time. The patch should not be cut into pieces. The patch can be used during everyday activities, including during bathing and in hot weather. Do not expose the patch to direct, prolonged operation of external sources of thermal radiation (such as excessive sunlight, sauna, solarium).
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