Donepezil ODT 10 Savi Treatment of Intelligence in Alzheimer's disease (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Donepezil

Ingredient

Composition information	Content
Donepezil	10mg

Uses

indications

Donepezil ODT 10 drug is indicated in symptomatic treatment and temporarily reduced dementia at mild or moderate in Alzheimer's disease.

Pharmacokology

Donepezil Hydrochloride is a special inhibitor and recovery of acetylcholininesterase is a dominant cholinesterase in the brain. In In Vitro test, Donepezil Hydrochloride inhibits this enzyme 1,000 times stronger than butyrylcholininesterase, an enzyme present mainly outside the central nervous system.

Intellect dementia in Alzheimer's disease

In patients with intellectual dementia in Alzheimer's disease participating in the sieve test, the use of Donepezil is only a daily dose of 5mg or 10mg, creating an inhibition of active activity of Acetylcholinesterase in a stable state (measured in erythrocytes) is 63.6% and 77.3% corresponding to the dose measured. The inhibition of acetylcholininesase (Ache) of Donepezil Hydrochloride in red blood cells is related to the Adas-Cog scoring changes, a sensitive scale to check the selective perception. The ability of Donepezil Hydrochloride in changing the process of hidden neuropathy has not been studied. So Donepezil is not considered any effect on the progression of the disease.

The effect of the treatment of intellectual dementia in Alzheimer's disease with Donepezil has been studied in four clinical trials verified by the placebo, 2 6 -month tests and 2 tests that last 1 year.

In a 6-month clinical trial, the effectiveness of Donepezil treatment is based on a combination of three standards: Adas-Cog score (assessment of cognitive ability), clinically based on physician's clinical interviews for changes to the data of the caregivers (assessing the whole function-CIBIC) and the daily assessment of the lifetow of the lifetime of the wisdom in the scaling of the Intelligence Review. Community, family, interests and personal care).

The patients responding to the listed criteria below are considered to be responded to treatment.

Improve = improve the Adas-Coog scale at least 4 points;

improve or not worsen the Cibic+evaluation board; Application

(n = 365)

Population can be evaluated

(n = 352)

10% 10% 10mg 21%* 21%* Treatment.

Pharmacological properties and patient characteristics:

Donepezil hydrochloride is an Ache inhibitor that should inhibit acetylcholin hydrolysis in the central nervous system, so the drug has benefits in therapy. The Ache enzyme appears in the periphery of red blood cells, so the evaluation of the impact of Ache in the red blood cells offers a pharmacological index of Donepezil hydrochloride.

Donepezil Hydrochorid is marked by C14 that has been assessed in a number of trials of pharmacokinetics/pharmacokinetic energy in humans and in clinical trials Pó verified. The concentration of Donepezil hydrochloride measured in plasma on testers and the measurement method of Ache inhibit shows that Donepezil hydrochloride shows pharmacological effects as predicted.

The results from the monitoring of the use of Fri drugs do not show any clear relationship between the concentration of the drug in plasma and the adverse reaction of the drug.

Pharmacokinetics

absorption

The highest concentration in plasma reaches about 3 to 4 hours after drinking. The concentration in plasma and the area under the curve increases proportional to the dose. The half -life is about 70 hours, so the only daily dose will lead to a stable approach. The stable state is achieved within 3 weeks after the beginning of the therapy. Once stable, the concentration of Donepezil Hydrochloride in plasma and the activity of the relevant pharmacies shows that there is very little change throughout the day. Food does not affect the absorption of Donepezil hydrochloride.

Distribution

About 95% Donepezil Hydrochloride is attached to human plasma proteins. The cohesion with plasma proteins of 6-O-Desmethyl Donepezil metabolic works is not well known. The distribution of Donepezil Hydrochloride in different tissues has not been clearly studied. However, in a large -scale study conducted on healthy volunteers, 240 hours after the single dose of 5mg Donepezil Hydrochloride was marked 14C, about 28% of the healed isotopes have not been recovered. This shows that Donepezil Hydrochloride and/or its metabolites can exist in the body for more than 10 days.

Metabolism

Donepezil Hydrochloride is eliminated in urine in both forms of unchanged and metabolic forms by the Cytochrome P450 system into many metabolites, not all of these metabolites are determined. After the single dose of 5mg Donepezil Hydrochloride is marked by 14C, the level of radioactive in plasma, shown by the percentage of the dose percentage, is mainly present in the form of Donepezil Hydrochloride unchanged (30%), 6-O-Desmethyl Donepezil (11%-the only transformation that represents the same activity with Donepezzi Hydrochloride),,,, the only active activity Donepezil-Cis-N-Oxide (9%), 5-O-Desmethyl Donepezil (7%) and Glucuronide Complex of 5-O-Desmethyl Donepezil (3%).

Elimination

Donepezil Hydrochloride is eliminated in urine in both forms of unchanged and metabolic forms. In 10 days, about 57% of the total amount of radioactive used were recovered from urine (17% in the form of unchanged Donepezil), and 14.5% were recovered from feces, showing the biological change and the excretion of urine were mainly excreted. There are no signs that Donepezil Hydrochloride and/or any of its metabolites participate in the intestinal cycle. Donepezil concentration in plasma decreases over 70 hours of sale.

Sex, race and history of smoking have no clinical significant effect on the concentration of Donepezil Hydrochloride in plasma. Donepezil's pharmacokinetics have not been officially studied in healthy elderly people or in patients with dementia in Alzheimer's disease or patients with dementia due to blood vessels. However, the average concentration in the plasma of patients is almost equivalent to healthy volunteers.

Patients with mild to medium-sized liver failure have an increase in Donepezil concentration in a stable state, the area under the average concentration curve is about 48% and the highest concentration in plasma (CMAX) is about 39%.

Before taking Donepezil ODT 10 Savi Treatment of Intelligence in Alzheimer's disease (3 blisters x 10 tablets)

How to use

oral medication. Regardless of the meal. Put the medicine on the tongue for the tongue to disintegrate and swallow without water or drink with water.

Dosage

Adults and the elderly:

The treatment begins at a dose of 5 mg/day (1 -dose per day).

The dose of 5 mg/day should be maintained for at least a month to be able to assess the earliest clinical response to the treatment as well as help achieve Donepezil concentration in a stable state.

After one month of clinical evaluation in the treatment at 5 mg/day, the dose can be increased to 10 mg/day (1 -day dose per day). The maximum daily dose proposed is 10 mg. Doses greater than 10 mg/day have not been studied in clinical trials.

When stopping treatment, it is possible to see a decrease in the beneficial effects of Donepezil. There is no evidence of feedback effect after sudden treatment.

Note: For a dose of 5 mg/time, it is advisable to use the appropriate content (Donepezil ODT 5)

kidney and liver failure:

A similar dose regimen can be used for patients with renal failure or liver failure mild or moderate because these conditions do not affect the clearance of Donepezil.

Children:

Donepezil is not used for children.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?

Symptoms

Overdose from cholinesterase inhibitors can lead to acetylcholine secretions characterized by nausea, severe vomiting, salivation, sweating, slow heart rate, low blood pressure, respiratory loss, stroke and convulsions. It is likely to increase myasthenia gravis and can lead to death if the respiratory muscles are affected.

Handling

In any case of overdose, the body support should be used. The third -level anti -secretion like atropine can be used as an antidote in the case of donepezil hydrochloride overdose.

Atropin sulfate intravenously: The starting dose from 1 to 2 mg intravenously, the next dose is based on clinical response. Non -typical response to blood pressure and heart rate have been reported with other cholin -like effects when used to mix with four -level anti -cholin secretion like glycopyrrolate. It is unknown Donepezil hydrochloride and/or its metabolic flooring may be except for the separation of the jurisdiction (hemorrhage, peritoneal or dialysis).

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

The most common side effects are diarrhea, muscle spasms, fatigue, nausea, vomiting and insomnia.

The side effects are recorded more than each individual case listed below, by the system group and frequency. The frequency is defined as follows: Very common (≥ 1/10), common (> 1/100, 1/1,000, 1/10,000,

Systemic agencies group Often Heavy behavior, nightmares Heart

Slow heart rate Sinus blockers, atrial - ventricular blockers Foam Itchy

bedwetting Experiment increases the concentration of muscle creatin kinase in the blood

* When investigating the study of patients who fainted or epilepsy, should pay attention to the possibility of a cardiac transmission or prolonged sinus stop.

Cases of hallucinations, agitation and aggressive behaviors have been adjusted by reducing the dose or stopping treatment.

In cases of unexplained liver dysfunction, Donepezil Odt 10.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Donepezil ODT 10 is contraindicated in the following cases:

Hypersensitivity to Donepezil, Piperidin derivatives or any ingredients of the drug.

Contraindicated in children under 18 years old.

Be cautious when using

General: The treatment should be started and monitored by the doctor who has experience in the treatment of intellectual dementia. The diagnosis should be based on recognized instructions (such as DSM IV - Diagnostic and Statistical Manual of Mental Disorder, ICD 10 - International Classification of Diseases). The treatment with Donepezil should start when the patient's care is taken care of, responsible for monitoring the patient to take the drug steadily. Maintenance treatment may continue when the drug is still effective for patients. Therefore, the clinical effect of Donepezil should be re -evaluated on a regular basis. Should consider stopping treatment when the treatment effect is no longer available. The response of each individual for Donepezil cannot predict. Using Donepezil for patients with severe dementia, other types of intelligence or other types of memory decline (such as reducing age -related cognitive function) has not been studied.

Anesthesia: Donepezil is a cholininusterase inhibitor that has the ability to enhance the muscle relaxation of Succinylcholin during anesthesia.

Cardiovascular: Due to the pharmacological effect of this drug, the cholinesterase inhibitors may have sympathetic effects on the heart rate (such as slow heart rate). This tolerance can be especially important for patients with "pathological sinus syndrome" or the pathogens on the ventricle of the heart, such as atrial or atrial sinus transmission.

Digestive: Patients with high risk of gastrointestinal ulcer, such as patients with a history of ulcer or patients who are taking simultaneously non -steroidal anti -inflammatory drugs (NSAID) Degal Antiinflammatory; NSAID) should be monitored with digestive symptoms. However, the clinical studies on Donepezil showed no increase in the rate of digestive ulcers or gastrointestinal hemorrhage compared to placebo.

Genitals and organs: Although it has not been recorded in the clinical trials of Donepezil, drugs that have the same effect as cholin can cause urinary retention.

neuropathy:

Epilepsy: The drugs have a cholin -like effect that is thought to have a body convulsions. However, seizures can also be a symbol of Alzheimer's disease. Drugs that are like cholin can worsen or cause foreign symptoms.

Neuroleptic Malignant Syndrome: NMS): is a death syndrome, characterized by symptoms such as hyperthermia, muscle hardness, cognitive change, creatin phosphokinase plasma, reported occurring when using Donepezil (dangerous), mainly in patients stopping in combination with psychotic drugs. Other signs include muscle pattern, acute renal failure. In the patient, there are signs and symptoms of NMS or high fever for unknown reasons, it should be stopped.

Respiratory: Due to the effects of cholin of the drug, be careful when prescribing cholinesterase inhibitors for patients with a history of asthma or obstructive pulmonary disease. Do not use in combination with other acetylcholinininininiserase inhibitors, motorbike owners or antagonists of the cholinergic system.

Severe liver failure: There is no data for patients with severe liver failure.

Colonel: The Manitol ingredient in the preparation can cause light laxative. Aspartam ingredients in preparations are a source of phenylalanin, so be cautious when used for people with phenylketon dollar.

The effect of the drug on the ability to drive and operate machinery

dizziness, sleep, fatigue, fatigue and muscle spasms may occur, especially when starting treatment or when increasing the dose of Donepezil hydrochloride should be cautious when driving or operating machinery.

Use drugs for women during pregnancy and lactation

pregnancy:

There is no clinical data on the use of Donepezil hydrochloride for pregnant women.

The studies on streaks show that Donepezil hydrochloride does not cause teratogenicity but have found toxicity during and after birth. The potential risk to people is still unknown.

Therefore, this drug should therefore be used for women during pregnancy unless the effect is superior to the risk

breastfeeding period:

Donepezil secretes mouse milk. It is unclear whether Donepezil hydrochloride is secreted into breast milk or not and no research in women who are breastfeeding. Therefore, women who are using Donepezil should not breastfeed.

Drug interaction

In vitro studies show that isenzyme 3A4 and a small part of isenzyme 2D6, in the Cytochrom P450 system, it affects the metabolism of Donepezil. CYP3A4 inhibitors such as ketoconazole, otraconazole, erythromycin and CYP2D6 inhibitors such as quinidine, fluoxetin increase the concentration of donepezil in plasma. In a study in healthy volunteers, Ketoconazole increased the average concentration of Donepezil by about 30%. The concentration/effect of Donepezil can also increase due to Conivaptan, corticosteroid (body).

In contrast, enzyme induction drugs such as rifampicin, phenytoin, carbamazepin and alcohol reduce the concentration of donepezil in plasma. The concentration/effect of Donepezil can also be reduced by anti -cholinergic drugs, Peginterferon alpha 2b, tocilizumab.

Donepezil can increase the concentration of anti -psychotic drugs, beta blockers, cholinergic agreements, sucinylcholin. Donepezil can reduce the concentration of anti -cholinergic drugs, nerve -muscles (no reducing).

Storage

Refer to the drug user manual.

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