Arisept - instructions for use, reviews, analogs and formulations (5 mg and 10 mg tablets) drugs for the treatment of Alzheimer's disease, primary degenerative and senile dementia in adults, children and pregnancy. Composition and side effects

In this article, you can read the instructions for using the drug Arisept. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of medical experts on the use of Arisept in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogs of Arisept with the presence of existing structural analogs.Use for the treatment of Alzheimer's disease, primary degenerative and senile dementia in adults, children, as well as in pregnancy and lactation. Composition and side effects of the drug.

Arisept - a selective and reversible inhibitor of the enzyme acetylcholinesterase, which is the predominant type of cholinesterase in the brain. Donepezil (the active substance of the preparation Aricept) inhibits this enzyme more than 1000 times stronger than butyrylcholinesterase, which is contained mainly outside the central nervous system (CNS).

After a single dose of donepezil in doses of 5 mg or 10 mg, the inhibition of acetylcholinesterase activity, measured in erythrocyte membranes, was 63.6% and 77.3%, respectively.

The drug slows the progression of Alzheimer's disease, reduces the severity of cognitive symptoms, in some cases restores the daytime activity of patients and facilitates the care of them. Corrects behavioral disorders, reduces apathy, hallucinations and unreasonable repetitive motions.

Composition

Donepezil + auxiliary substances.

Pharmacokinetics

After oral administration, the maximum concentration of donepezil in blood plasma is reached after about 3-4 hours. Plasma concentrations increase in proportion to the dose.The intake of food does not affect the absorption of donepezil. Binding to plasma proteins is about 95%. It is assumed that donepezil and / or its metabolites can persist in the body for more than 10 days. Arisept is metabolized in the liver and is excreted, like its metabolites, which are formed with the participation of cytochrome P450 isoenzymes, mostly in kidneys in unchanged form: approximately 57% of the administered dose was found in urine and 14.5% in feces. In patients with mild or moderate impairment of liver function, elevated mean concentrations of donepezil in blood plasma can be observed.

Indications

• Alzheimer's disease;
• primary degenerative dementia (dementia);
• dementia of the Alzheimer's type;
• senile (senile) dementia.

Forms of release

Tablets coated with a coating, 5 mg and 10 mg.

Instructions for use and dosing regimen

Adults (including elderly patients) are given an initial dose of 5 mg once a day. Admission in the initial dose is continued for at least 4-6 weeks to reach equilibrium concentrations of donepezil and determine the early clinical effect of therapy. After 1 month, the dose can be increased to 10 mg per day.

The maximum daily dose is 10 mg per day.

Supportive therapy can be continued as long as the therapeutic effect remains, which should be evaluated regularly.

Side effect

• bradycardia (rare pulse);
• sinoatrial blockade, atrioventricular (AV) blockade - on an electrocardiogram (ECG);
• fainting;
• increased fatigue;
• dizziness, headache;
• insomnia;
• hallucinations;
• agitation, aggressive behavior;
• convulsive seizures;
• diarrhea, nausea, vomiting;
• anorexia (eating disorder);
• gastrointestinal disorders;
• bleeding from the gastrointestinal tract (GIT), stomach ulcers and duodenal ulcers;
• urinary incontinence;
• impaired liver function, including hepatitis;
• rash, itching;
• a slight increase in the activity of the muscle fraction of the creatine phosphokinase (CK) enzyme in the blood serum;
• pain of different localization;
• influenza-like syndrome;
• muscle cramps.

Contraindications

• pregnancy, lactation (breastfeeding);
• children and adolescents under 18;
• increased sensitivity to donepezil and piperidine derivatives.

Application in pregnancy and lactation

Contraindicated use of the drug Aricept during pregnancy and lactation (breastfeeding).

Use in children

The safety and efficacy of donepezil in children have not been studied, so the drug is not recommended for this category of patients.

special instructions

Use with caution in patients with obstructive pulmonary disease in history (including bronchial asthma), with heart rhythm disorders, in anesthesia, and in patients with an increased risk of developing an ulcer (for example, patients with a history of peptic ulcer disease or receiving concomitant therapy non-steroidal anti-inflammatory drugs (NSAIDs), concomitantly with NSAIDs, anticholinergic drugs or other cholinesterase inhibitors.

Treatment should be prescribed and conducted by a physician with experience in managing patients with Alzheimer's disease.

Supportive therapy can be continued as long as the therapeutic effect remains. If the therapeutic effect disappears, then donepezil should be discarded. After discontinuation of treatment, there is a gradual decrease in donepezil, there is no information on withdrawal syndrome in the event of a sudden discontinuation.It is impossible to predict an individual reaction to donepezil therapy.

The efficacy of donepezil in patients with severe dementia of the Alzheimer's type, other types of dementia, or other types of memory impairment (eg, age-related deterioration of cognitive function) has not been studied.

Arisept, being an inhibitor of cholinesterase, can enhance muscle relaxation of succinylcholine type during anesthesia.

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

It is believed that cholinomimetics are capable of causing generalized convulsions. However, the appearance of seizures during treatment with donepezil can also be a manifestation of Alzheimer's disease.

Influence on the ability to manage motor vehicles and work with mechanisms

Dementia Alzheimer's type itself can be accompanied by a disruption in the ability to drive and use sophisticated technology.In addition, donepezil, mainly at the beginning of treatment or with increasing doses, can cause fatigue, dizziness and muscle cramps. The question of the ability of a patient with Alzheimer's dementia during the use of donepezil to drive a car or use complicated equipment should be decided by the doctor after assessing the patient's individual response to treatment.

Drug Interactions

The clinical experience of using donepezil is limited, therefore, when taking into account the risk of unknown to the present moment, the manifestations of interaction with other drugs.

Donepezil metabolized with the participation of the isoenzyme CYP3A4 and to a lesser extent - CYP2D6. Ketoconazole and quinidine, which are inhibitors of CYP3A4 and CYP2D6, respectively, suppress the metabolism of donepezil. 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 mean concentrations of donepezil by approximately 30%. However, this action was not comparable with the action of ketoconazole on other substances metabolized with the participation of CYP3A4, so it is unlikely to be of clinical significance.

Inducers of enzymes such as rifampicin, phenytoin, Carbamazepine and ethanol can cause a decrease in donepezil activity. However, the degree of such inhibitory or inducing action is unknown (caution is required when using simultaneously).

Arisept can influence the effect of drugs that have anticholinergic activity. In addition, with concurrent use, donepezil can enhance the action of succinylcholine, other muscle relaxants or cholinergic receptor agonists and beta-blockers that affect conduction of the heart, although in vitro studies have shown that donepezil has minimal effect on the hydrolysis of succinylcholine.

With simultaneous use of donepezil with other cholinomimetics and quaternary anticholinergic drugs, such as glycopyrrolate, cases of atypical changes in blood pressure (BP) and heart rate are described.

Analogues of Arisept

Structural analogs for the active substance:

• Alzepil;
• Dementis;
• Donepezil hydrochloride;
• Donepezil hydrochloride monohydrate;
• Jasnal.

Analogues on the pharmacological group (M- and H-cholinomimetics, including anticholinesterase agents):

• Aksamon;
• Alzepil;
• Alzenorm;
• Aminostigmine injection 0.1%;
• Amiridin;
• Galantamine;
• Galanthamine hydrobromide;
• Glenor SR;
• Dementis;
• Donepezil hydrochloride;
• Donepezil hydrochloride monohydrate;
• Ipigrix;
• Ipidacrin;
• Kalimin 60 N;
• Carbachol;
• Mio-Hall;
• Neuromidine;
• Nivalin;
• Pyridostigmine bromide;
• Proserin;
• Prozerin injection 0.05%;
• Proserin tablets 0.015 g;
• Reminil;
• Ubretid;
• Exelon;
• Jasnal.

Response of a therapist

My mom's Alzheimer's disease began to develop suddenly and very quickly. After consulting my psychiatrist colleague, I began giving her Aricept one 5 mg tablet once a day. But after almost a month of treatment, there was no positive dynamics. A month later, I twice increased the daily dose. But after about a week my mother complained of headaches and insomnia, twice she had vomiting. Therefore Arisept had to be canceled and again to seek help from a psychiatrist to prescribe another drug from Alzheimer's dementia. Now I'm giving my mom to Dementis. From the very beginning of treatment, very little has passed, so it's too early to say anything about its effectiveness.

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