Alzepil (Donepezil) 10 mg, 28 pcs.

Aegis, Hungary

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$95
Alzepil (Donepezil) 10 mg, 28 pcs.
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Product Overview

Composition

1 tablet contains:


Active substance:

donepezil hydrochloride monohydrate - 10.42 mg (corresponding to donepezil hydrochloride - 10 mg)      

Excipients:

microcrystalline cellulose - 192 mg,

low substituted hydroxypropyl cellulose (L-HPC B1) - 48 mg,

magnesium stearate - 2 mg.

The composition of the film shell:

 Opadry Y-1-7000 white (hypromellose - 3.75 mg, titanium dioxide - 1.875 mg, macrogol 400 - 0.375 mg) - 6 mg.


 



pharmachologic effect

A selective and reversible inhibitor of acetylcholinesterase, which is the main predominant type of cholinesterase in the brain. In vitro donepezil inhibits this enzyme more than 1000 times stronger than butyrylcholinesterase - an enzyme that is located mainly outside the central nervous system.

A single dose of 5 mg or 10 mg in equilibrium is accompanied by inhibition of cholinesterase activity (evaluated on the model of erythrocyte membranes) by 63.6% and 77.3%, respectively. The ability of donepezil hydrochloride to inhibit erythrocyte cholinesterase activity correlates with changes in results on the ADAS-cog scale, which is a sensitive tool for assessing changes in cognitive function. The ability of donepezil hydrochloride to change the course of concomitant neurological changes has not been investigated. Thus, it cannot be considered that donepezil affects the progression of the disease.

The effectiveness of donepezil was investigated in four placebo-controlled studies, two six-month and two one-year.

In a six-month clinical trial, the analysis was performed using three performance criteria after completion of the administration of donepezil. Used the ADAS-Cog scale (indicator of cognitive function); the scale of impressions of the clinician about changes based on interviews and data obtained from persons caring for the patient (an indicator of the general level of function); subscale of daily activity of the clinical scale for assessing dementia (an indicator of the patient’s ability to participate in society, to perform household chores, favorite things, to serve himself).

Patients who met the following criteria were considered responding to treatment.

Answer = ADAS-Cog improvement of at least 4 points, no CIBIC deterioration, no deterioration in the subscale of daily activity of the clinical dementia assessment scale.

  % Response
  Patients who were prescribed treatment ("ITT - Intent to treat"), n = 365 The population, the analysis of which was possible, n = 352
Placebo group ten% ten%
The group receiving donepezil hydrochloride in a dose of 5 mg 18%* 18%*
The group receiving donepezil hydrochloride at a dose of 10 mg 21% * 22% **

* p <0.05, ** p <0.01

Donepezil hydrochloride caused a dose-dependent, statistically significant increase in the percentage of patients who were recognized as responding to treatment.

Indications

Symptomatic treatment of mild to moderate Alzheimer's disease 

Contraindications

  • hypersensitivity (including piperidine derivatives);
  • pregnancy (see. "Use during pregnancy and lactation");
  • lactation period (see. "Use during pregnancy and lactation");
  • children under 18 years of age (due to lack of clinical data).

Precautions: chronic obstructive pulmonary disease, bronchial asthma, cardiac arrhythmias, general anesthesia, gastric and duodenal ulcer, concomitant use of NSAIDs, anticholinergics, or other cholinesterase inhibitors.

Side effects

Nausea, diarrhea, headache, fainting, dizziness, insomnia, fatigue, hallucinations, agitation, aggressive behavior (which stop after a dose reduction or drug withdrawal), vomiting, upset stomach, urinary incontinence, rash, skin itching, muscle cramps, anorexia, colds, pain of various localization, a slight increase in the concentration of muscle cretinine phosphokinase in the blood serum, bradycardia, seizures, gastrointestinal bleeding, gastric and duodenal ulcers, sinoatrial and atrioventricular block, extrapyramidal symptoms, impaired liver function, including hepatitis.

Interaction

Alzepil and / or its metabolites do not inhibit the metabolism of theophylline, warfarin, cimetidine or digoxin.
 
With simultaneous use with digoxin or cimetidine, donepezil hydrochloride metabolism does not change.
 
Ketoconazole and quinidine, inhibitors of CYP3A4 (itraconazole, erythromycin) and 2D6 (fluoxetine), inhibit donepezil metabolism. In a study in healthy volunteers, ketoconazole increased average donepezil concentrations by about 30%.
 
Enzyme inducers (rifampicin, phenytoin, carbamazepine, and ethanol) can lower donepezil levels. However, the extent of such inhibitory or inducing action is not known, therefore, such combinations of drugs should be used with caution. Alzepil may interact with drugs with anticholinergic activity.
 
Also, Alzepil has a synergistic effect when taken simultaneously with succinylcholine, other muscle relaxants or antagonists of cholinergic receptors and beta-blockers, which affect the conductivity of the heart.
 
With the simultaneous use of Alzepil with other cholinomimetics and quaternary anticholinergics, such as glycopyrrolate, cases of atypical changes in blood pressure and heart rate have been described.

How to take, course of administration and dosage

Alzepil is used strictly as prescribed by the doctor!
 
The drug should be taken orally in the evening before bedtime. For adults and elderly patients, the drug is prescribed in an initial dose of 5 mg 1 time per day.
 
Admission in an initial dose of 5 mg should be continued for 1 month in order to assess the early clinical effect of therapy and achieve an equilibrium concentration of donepezil. After a month, if necessary, you can increase up to 10 mg per day (in 1 dose). The recommended maximum daily dose is 10 mg. Clinical studies with a dosage of more than 10 mg / day have not been conducted.
 
In case of impaired liver and kidney function, dose adjustment is not required.
 
Due to the possible increase in exposure with mild or moderate impairment of liver function, an increase in dose should be performed taking into account individual tolerance.

Overdose

Symptoms:  cholinergic crisis (severe nausea, vomiting, salivation, sweating, bradycardia, arterial hypotension, respiratory depression, collapse and convulsions). It is possible to increase muscle weakness, which, with damage to the respiratory muscles, can lead to death.
 
Treatment:  General supportive treatment should be prescribed. As an antidote, tertiary anticholinergics are used, for example, atropine in an initial dose of 1-2 mg intravenously, then the dose is selected depending on the clinical effect. There is no data on the removal of donepezil hydrochloride and / or its metabolites by dialysis (hemodialysis, peritoneal dialysis or hemofiltration).

Special instructions

Treatment should be prescribed and performed by a specialist doctor with experience in managing patients with Alzheimer's type dementia. The diagnosis of the disease must be made in accordance with generally accepted criteria (e.g. DSM IV, ICD 10). Treatment can only be carried out if there is a person who can control the administration of drugs. Treatment is carried out until there is a therapeutic effect, which should be regularly evaluated.
 
In the absence of a therapeutic effect, the drug should be discontinued. An individual response to Alzepil therapy cannot be predicted. After discontinuation of the drug, its effect gradually and slowly disappears. There is no information about the withdrawal syndrome in case of a sharp cessation of the drug.
 
The effectiveness of Alzepil has not been established in patients with severe Alzheimer's type of dementia, other types of dementia, or impaired memory (for example, with an age-related decrease in cognitive function).
 
Being an inhibitor of cholinesterase, Alzepil can enhance the succinylcholine type of muscle relaxation during general anesthesia. It can also have a vagotonic effect on heart rate (cause bradycardia). The possibility of such an action should be taken into account with weak sinus node or other disorders of supraventricular conduction, such as sinoatrial or atrioventricular block.
 
Cases of fainting and seizures have been reported. When examining such patients, it is necessary to take into account the possibility of a blockade or prolonged sinus stop.
 
Caution should be exercised in patients with an increased risk of developing an ulcer (for example, patients with a history of peptic ulcer or taking non-steroidal anti-inflammatory drugs (NSAIDs)).
 
However, clinical studies of donepezil compared with placebo did not reveal an increase in the incidence of peptic ulcers or gastrointestinal bleeding.
 
Cholinomimetics can cause obstruction of the mouth of the bladder, although clinical studies using donepezil hydrochloride do not have this information.
 
It is believed that cholinomimetics can cause generalized seizures, but seizures can also be a manifestation of Alzheimer's disease. Cholinomimetics can aggravate or reduce extrapyramidal disorders.
 
Particular care should be taken when prescribing the drug to patients with asthma or obstructive pulmonary diseases in the anamnesis.
 
Alzepil should not be taken concurrently with other acetylcholinesterase inhibitors, agonists or antagonists of the cholinergic system.
 
There is no data on the use of the drug in patients with severe impaired liver function. In case of impaired liver function of an unknown etiology, the possibility of discontinuing the drug Alzepil should be considered.
 
Pediatric Use
 
The safety and effectiveness of Alzepil in children has not been studied, therefore, the drug is not recommended for this category of patients.

Storage conditions

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

Shelf life

5 years

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