Buy Alzepil pills 5 mg 28 pcs
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Alzepil® [Donepezil]

Egis
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2019-09-19
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Clinical Pharmacology

Alzepil is a specific and reversible acetylcholinesterase inhibitor that is the predominant type of cholinesterase in the brain. The drug inhibits this enzyme more than 1000 times stronger than butyrylcholinesterase, which is contained mainly outside the central nervous system. After a single dose of the drug in doses of 5 mg or 10 mg, the degree of inhibition of acetylcholinesterase activity, measured in erythrocyte membranes, was 63.6% and 77.3%, respectively. Inhibition of acetylcholinesterase in erythrocytes under the action of donepezil correlates with changes in the ADAS-cog scale (cognitive function assessment scale in Alzheimer's disease). The ability of Alzepil to alter the course of concomitant neurological diseases has not been studied. Thus, the drug cannot be considered to affect the progression of such diseases.

Pharmacokinetics

Suction. Cmax Donepezil in plasma after oral administration is reached in about 3-4 hours. Concentration in plasma and AUC increase in proportion to the dose. T1/2 is approximately 70 hours and the systematic use of single doses leads to the achievement of an equilibrium state, which is achieved within 2-3 weeks after the start of therapy. In equilibrium, the concentration of donepezil in plasma and the corresponding pharmacodynamic activity vary slightly during the day. Eating does not affect the absorption of donepezil.

Distribution. Plasma protein binding - 95%. The binding of plasma proteins of the active metabolite, 6-O-desmethyldoneepesil, is unknown. Distribution has not been studied. Donepezil and / or its metabolites may persist in the body for more than 10 days.

Metabolism and excretion. Donepezil is metabolized in the liver by the cytochrome P450 system and is excreted mainly by the kidneys: approximately 57% of the administered dose is found in the urine (17% in unchanged form) and 14.5% in the faecal masses.

After a single dose of 5 mg, the concentration of unchanged donepezil in plasma is 30% of the dose taken, 6-O-desmethyldonepestyl - 11% (the only metabolite with similar activity with donepezil hydrochloride), donepezil-cis-N-oxide - 9%, 5-O-desmethyldonepesyl - 7% and the glucuronic conjugate 5-O-desmethyldoneepesyl - 3%.

Gender, race and smoking do not have a significant effect on plasma plasma level of donepezil.

Increased C may be observed in patients with mild or moderate hepatic impairment.ss donepezil in blood plasma.

Indications

Symptomatic treatment of mild or moderate Alzheimer's disease

Composition

1 tablet contains:
active substance: donepezil hydrochloride monohydrate (corresponds to donepezil hydrochloride - 5 mg)
Excipients: MCC; low substitution hydroxypropylcellulose (L-HPC B1); magnesium stearate; Opadry Y-1-7000 white (hypromellose; titanium dioxide; macrogol 400)

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Alzepil® [Donepezil]

Dosage and Administration

Alzepil is used strictly as prescribed by a 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. Reception in the initial dose of 5 mg should be continued for 1 month to assess the early clinical effect of therapy and to reach the equilibrium concentration of donepezil. After a month, if necessary, you can increase to 10 mg per day (in 1 reception). The recommended maximum daily dose of 10 mg. Clinical studies with a dosage of more than 10 mg / day has not been conducted.
At dysfunction of a liver and kidneys adjustment of doses is not required.
Due to the possible increase in exposure with mild or moderate liver dysfunction, the dose increase should be carried out taking into account individual tolerance.

Adverse reactions

Nausea, diarrhea, headache, fainting, dizziness, insomnia, fatigue, hallucinations, agitation, aggressive behavior (which stop after reducing the dose or discontinuation of the drug), vomiting, indigestion, urinary incontinence, rash, skin itch, muscle cramps, anorexia, colds, pain of different localization, a slight increase in serum concentration of muscle cretinophosphokinase, bradycardia, seizures, gastrointestinal bleeding, gastric and duodenal ulcers, sinoatrial and a trioventricular block, extrapyramidal symptoms, abnormal liver function, including hepatitis.

Contraindications

Carefully: chronic obstructive pulmonary disease, bronchial asthma, cardiac arrhythmias, general anesthesia, peptic ulcer and duodenal ulcer, simultaneous intake of NSAIDs, holinoblokatorov or other cholinesterase inhibitors.

Drug interactions

Alzepil and / or its metabolites do not inhibit the metabolism of theophylline, warfarin, cimetidine or digoxin.
When used simultaneously with digoxin or cimetidine, the metabolism of donepezil hydrochloride 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 the average concentration of donepezil by about 30%.
Enzyme inducers (rifampicin, phenytoin, carbamazepine, and ethanol) can reduce donepezil levels. However, the extent of such an inhibitory or inducing action is not known, so such combinations of drugs should be used with caution. Alzepil can interact with drugs that have anticholinergic activity.
Also, Alzepil has a synergistic effect when taken simultaneously with succinylcholine, other muscle relaxants or antagonists of cholinergic receptors and beta-blockers that affect the conductivity of the heart.
With simultaneous use of Alzepil with other cholinomimetics and quaternary anticholinergic drugs such as glycopyrrolate, cases of abnormal changes in blood pressure and heart rate are described.

Pregnancy and Lactation

Experience of the drug during pregnancy and lactation is not. It is not known whether the drug is excreted in breast milk. Therefore, the use during pregnancy is contraindicated, if necessary, taking the drug during lactation is necessary to solve the issue of stopping breastfeeding.

Special instructions

Treatment should be prescribed and carried out by a specialist doctor who has experience in managing patients with dementia of the Alzheimer's type. The diagnosis of the disease must be made in accordance with generally accepted criteria (for example, DSM IV, ICD 10). Treatment can be carried out only if there is a person who is able to control the medication. Treatment is carried out as long as there is a therapeutic effect, which should be regularly evaluated.In the absence of a therapeutic effect, the drug should be stopped. The individual response to Alzepil therapy cannot be predicted. After discontinuation of the drug, its effect gradually and slowly disappears. There is no information about withdrawal syndrome in case of abrupt discontinuation of the drug.
The effectiveness of Alzepil has not been established in patients with severe Alzheimer's-type dementia, other types of dementia, or memory impairment (for example, with age-related cognitive decline).
As an inhibitor of cholinesterase, Alzepil can enhance the succinylcholine type of muscle relaxation during general anesthesia. It may also have a vagotonic effect on heart rate (cause bradycardia). The possibility of such an action should be considered in case of weak sinus node or other disorders of supraventricular conduction, such as sinoatrial or atrioventricular block.
Cases of fainting and convulsions have been reported. When examining such patients, it is necessary to take into account the possibility of blockade or prolonged sinus arrest.
Caution should be exercised in patients with an increased risk of developing an ulcer (for example, patients with a history of peptic ulcer disease or taking nonsteroidal 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 in clinical studies conducted using donepezil hydrochloride, such information is not available.
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.
Special care should be taken when prescribing the drug to patients with bronchial asthma or obstructive pulmonary diseases in history.
Alzepil should not be taken concurrently with other acetylcholinesterase inhibitors, agonists or antagonists of the cholinergic system.
There are no data on the use of the drug in patients with severely impaired liver function. In case of impaired liver function of 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, so the drug is not recommended to prescribe this category of patients.

Overdosage

Symptoms: cholinergic crisis (severe nausea, vomiting, drooling, sweating, bradycardia, arterial hypotension, respiratory depression, collapse and seizures). May increase muscle weakness, which, if the respiratory muscles are damaged, can be fatal.
Treatment: general supportive treatment should be prescribed. As an antidote, tertiary anticholinergic drugs are used, for example, atropine in the 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).

  • Brand name: Alzepil
  • Active ingredient: Donapezil
  • Dosage form: Pills
  • Manufacturer: Egis
  • Country of Origin: Hungary

Studies and clinical trials of Donepezil (Click to expand)
  1. Pharmacotherapy for people with Alzheimer's disease: a Markov-cycle evaluation of five years' therapy using donepezil
  2. Donepezil for dementia with Lewy bodies: a case study
  3. Sustained cognitive improvement following treatment of Alzheimer's disease with donepezil
  4. Donepezil for the treatment of psychosis in dementia with Lewy bodies
  5. Donepezil for behavioural disorders associated with Lewy bodies: a case series
  6. Did knowledge, opinions, background, and health authority advice influence early prescribing of the novel Alzheimer's disease drug donepezil in general practice?—National postal survey
  7. Donepezil in Alzheimer's disease: eighteen month results from Southampton Memory Clinic
  8. Better cognitive and psychopathologic response to donepezil in patients prospectively diagnosed as dementia with Lewy bodies: a preliminary study
  9. Use of donepezil for the treatment of mild – moderate Alzheimer's disease: an audit of the assessment and treatment of patients in routine clinical practice
  10. Improvement in sundowning in dementia with Lewy bodies after treatment with donepezil
  11. Carers' assessment of patients on donepezil—how reliable?
  12. Donepezil hydrochloride: A treatment drug for Alzheimer’s disease
  13. Limited donepezil inhibition of acetylcholinesterase measured with positron emission tomography in living Alzheimer cerebral cortex
  14. Donepezil for Huntington's disease
  15. Donepezil for the treatment of language deficits in adults with Down syndrome: A preliminary 24-week open trial
  16. Donepezil effects on language in children with Down syndrome: Results of the first 22-week pilot clinical trial
  17. Preliminary study of the safety and efficacy of donepezil hydrochloride in children with Down syndrome: A clinical report series
  18. The efficacy, safety, and tolerability of donepezil for the treatment of young adults with Down syndrome
  19. Donepezil for treatment of cognitive dysfunction in children with Down syndrome aged 10–17
  20. Variability of AChE, BChE, and ChAT genes in the late-onset form of Alzheimer's disease and relationships with response to treatment with Donepezil and Rivastigmine
  21. A rapid and specific approach for direct measurement of donepezil concentration in human plasma by LC-MS/MS employing solid-phase extraction
  22. A rapid and specific approach for direct measurement of donepezil concentration in human plasma by LC-MS/MS employing solid-phase extraction
  23. A rapid and sensitive LC-MS/MS method for quantification of donepezil and its active metabolite, 6-o-desmethyl donepezil in human plasma and its pharmacokinetic application
  24. Interaction study of aspirin or clopidogrel on pharmacokinetics of donepezil hydrochloride in rats by HPLC-fluorescence detection

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