Symptomatic treatment of mild to moderately severe Alzheimer's dementia.
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). A 15 cm transdermal patch2 contains 27 mg of rivastigmine (releases 13.3 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 and Parkinson'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.
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 impairment of liver or kidney function (due to the increased exposure to rivastigmine in these populations and the risk of increased side effects, the dose should be carefully determined depending on the individual tolerance); with a body weight <50 kg (these patients should be monitored to detect side effects, and if such occur, a reduction in the maintenance dose to 4.6 mg / 24 h should be considered). 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. Patients and their carers should be provided with important instructions on the use of patches as incorrect use and errors in dosing may lead to serious side effects (some cases required hospitalization and rarely lead to death, most consisted of applying a new patch without removing the previous one and applying multiple patches at the same time). 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. 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, lack of appetite, decreased appetite, anxiety, depression, delirium, agitation, headache, fainting, dizziness, nausea, vomiting, diarrhea, indigestion, abdominal pain, incontinence, rash, reactions at the site of erythema, pruritus, edema, dermatitis, irritation at the site of attrition), 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.
Dosage:
Outwardly.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, start treatment with 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 stable and well-tolerated, it is recommended to change treatment to transdermal system 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: For 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.Usage: transdermal 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 that is not exposed to abrasion by crumple 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 peels off, apply a new patch for the rest of the day and then replace it with the Next day at the usual time.Do not expose the patch to direct, prolonged operation of external sources of thermal radiation (such as excessive sunlight, sauna, solarium). The patch should not be cut into pieces. The patch can be used during everyday activities, including during bathing and in hot weather.