Alzepil pills 5mg №28

Indications

- symptomatic treatment of mild, moderate and severe Alzheimer's type dementia.

Dosage and administration

The drug is recommended to be taken in the evening before bedtime.

Treatment begins with taking the drug at a dose of 5 mg 1 time / day and continues for at least 4 weeks to reach C_ss donepezil and evaluate the early clinical effect of therapy.

After 1 month, the dose of Alzepil^® can be increased to 10 mg 1 time / day, which is the maximum recommended daily dose.

Maintenance therapy can continue as long as the therapeutic effect persists, which should be regularly evaluated.

Patients with impaired liver function mild to moderate severity, and with renal impairment do not need to change the treatment regimen, because these conditions do not affect the clearance of donepezil.

Adverse effects

Determination of the frequency of adverse reactions: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, ≤1 / 100), rarely (≥1 / 10 000, ≤1 / 1000), very rarely (≤1 / 10 000).

Cardiovascular: infrequently - bradycardia; rarely - sinoatrial block, AV block.

Nervous system: often - fainting *, fatigue, dizziness, headache, muscle cramps, insomnia, hallucinations, agitation, aggressive behavior; infrequently - convulsive seizures *; rarely extrapyramidal symptoms.

Gastrointestinal: very often - diarrhea, nausea; often - vomiting, dyspepsia, anorexia, gastrointestinal disorders; infrequently - bleeding from the gastrointestinal tract, gastric ulcer and duodenal ulcer.

Urogenital: often - urinary incontinence; rarely - liver dysfunction, incl. hepatitis.

Dermatologic: often - rash, skin itch.

Laboratory research: infrequently, a slight increase in the activity of the muscle isoform of CK in the serum.

Other: pain of different localization, flu-like syndrome.

* When examining patients with fainting or convulsive seizures, the possibility of cardiac blockade should be considered.

Contraindications

- pregnancy;

- lactation period (breastfeeding);

- children's and teenage age up to 18 years (due to the lack of clinical data);

- hypersensitivity to the drug;

- hypersensitivity to piperidine derivatives.

WITH caution the drug should be used for COPD, bronchial asthma, cardiac arrhythmias, general anesthesia, gastric ulcer and duodenal ulcer, while taking NSAIDs, holinoblokatorov or other cholinesterase inhibitors.

Use during pregnancy and lactation

Experience with the use of the drug during pregnancy and lactation is not.

The use of the drug during pregnancy is contraindicated.

It is not known whether the drug is excreted in breast milk.If it is necessary to take the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding.

Application for violations of the liver

Patients with impaired liver function mild to moderate severity do not need to change the treatment regimen, because these conditions do not affect the clearance of donepezil.

Application for violations of kidney function

Patients with impaired renal function do not need to change the treatment regimen, because This condition does not affect the clearance of donepezil.

Use in children

Contraindicated in children and adolescents under 18 years of age.

Special notes

Maintenance therapy can be continued as long as the therapeutic effect persists. In this regard, the effect of donepezil should be regularly evaluated. If the drug ceases to act, it should be canceled.

After cessation of treatment, there is a gradual decrease in the effect of Alzepil, there is no information about withdrawal syndrome in the event of abrupt discontinuation of the drug.

Individual response to donepezil cannot be predicted.

Donepezil can increase the severity of neuromuscular blockade caused by depolarizing muscle relaxants during general anesthesia.

Cholinesterase inhibitors can have a vagotonic effect on heart rate (in particular, cause bradycardia). The potential for such action may be important for patients with SSSS or other disorders of supraventricular conduction, such as sinoatrial or AV blockade.

During treatment, it is necessary to carefully observe patients who have a risk of developing gastric ulcer and duodenal ulcer, for example, patients with a history of gastric ulcer or patients receiving NSAIDs, because cholinomimetics are able to enhance the secretion of hydrochloric acid in the stomach. At the same time, there was no increase in the incidence of peptic ulcer or Gastrointestinal bleeding compared with placebo in clinical studies.

Cholinesterase inhibitors can cause urinary retention, although this effect has not been seen in clinical studies.

It is believed that cholinesterase inhibitors to a certain extent can cause generalized seizures, however, convulsive activity may also be a manifestation of Alzheimer's type dementia.

Given the cholinomimetic effect of cholinesterase inhibitors, they should be prescribed with caution in patients with a history of bronchial asthma or obstructive pulmonary diseases.

Influence on ability to drive motor transport and control mechanisms

Dementia of the Alzheimer's type may itself be accompanied by a violation of the ability to drive and use complex equipment. In addition, the drug, mainly at the beginning of treatment or with an increase in dose, may cause fatigue, dizziness and muscle cramps. The question of the ability of a patient with dementia of the Alzheimer's type while administering donepezil to drive a car or using a complex technique must be decided by the doctor after evaluating the patient's individual response to treatment.

Overdosage

Symptoms: cholinergic crisis (severe nausea, vomiting, drooling, increased sweating, bradycardia, decreased blood pressure, respiratory depression, collapse, convulsions). Possible increasing myasthenia gravis, which can be fatal if respiratory muscles are affected.

Treatment: symptomatic therapy. Atropine IV may be used as an antidote at an initial dose of 1-2 mg, then the dose is selected depending on the effect. It is not known whether donepezil and / or its metabolites are removed from the body during dialysis (hemodialysis, peritoneal dialysis, or hemofiltration).

Drug interaction

Donepezil and / or its metabolic products do not inhibit the metabolism of theophylline, Warfarin, cimetidine, Digoxin, thioridazine, Risperidone, and sertraline. Simultaneous administration of digoxin, cimetidine, thioridazine, risperidone and sertraline does not affect the metabolism of donepezil.

The use of donepezil with levodopa / carbidopa at the same time for 21 days had no effect on the concentration of these drugs in the blood.

CYP3A4 isoenzyme and to a lesser extent CYP2D6 is involved in the metabolism of donepezil. Ketoconazole and quinidine, which are inhibitors of CYP3A4 and CYP2D6, respectively, inhibit donepezil metabolism. Consequently, these and other CYP3A4 inhibitors, such as itraconazole and Erythromycin, and CYP2D6 inhibitors, such as Fluoxetine, can inhibit donepezil metabolism. In healthy volunteers, ketoconazole increased the average concentration of donepezil by about 30%.The simultaneous use of donepezil has no effect on the pharmacokinetics of ketoconazole. Isoenzyme inducers such as rifampicin, phenytoin, Carbamazepine, and ethanol can cause a decrease in plasma plasma level of donepezil. However, the extent of this inhibitory or inducing action is unknown, therefore, such agents should be used in combination with donepezil with caution.

Donepezil has an effect on the action of drugs with anticholinergic activity. In addition, with simultaneous use, donepezil may enhance the action of suxamethonia bromide, other muscle relaxants or cholinergic receptor agonists and beta-blockers that affect cardiac conduction.

With the simultaneous use of donepezil and cholinergic agonists, quaternary anticholinergic drugs such as glycopyrronium bromide, cases of atypical changes in blood pressure and heart rate are described.

Terms and conditions of storage

The drug should be stored out of the reach of children at a temperature not higher than 30 ° C.