Jasnal - instructions for use, doses, side effects, contraindications

Active substanceDonepezilDonepezil

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Jasnal®

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KRKA, dd, Novo mesto, AO

Dosage form: & nbspfilm-coated tablets

Composition:

1 A film coated tablet contains:

Active substance: donepezil hydrochloride monohydrate 5.22 mg or 10.43 mg (corresponding to 5 mg or 10 mg of donepezil hydrochloride).

Excipients: lactose monohydrate, microcrystalline cellulose, corn starch, giprolase, magnesium stearate.

Shell:

Tablet 5 mg: fall off Y-1-7000 (a mixture of titanium dioxide, hypromellose and macrogol).

Tablet 10 mg: opada yellow 02B22462 (a mixture of titanium dioxide, hypromellose, macrogol and iron oxide of yellow oxide).

Description:

Tablets 5 mg: round, biconvex tablets, covered with a film shell of white or almost white color.

Tablets 10 mg: round, biconvex tablets, covered with a film coating of a yellowish brown color.

Pharmacotherapeutic group:cholinesterase inhibitor

ATX: & nbsp

N.06.D.A.02 Donepezil

Pharmacodynamics:Donepezil is a selective, reversible inhibitor of the enzyme acetylcholinesterase (AChE), which is the predominant type of cholinesterase in the brain. Donepezil blocks the disintegration of acetylcholine, which transfers excitation to the central nervous system. In this way, donepezil increases the content of acetylcholine in the synapses and enhances the cholinergic activity. After a single dose of donepezil in doses of 5 mg and 10 mg, the activity of acetylcholinesterase was inhibited by 63.6 and 77.3%, respectively (estimated in erythrocyte membranes). Suppression of cholinesterase activity in erythrocytes was accompanied by changes in the scales ADAS (ADAS-cog: cognitive scale of Alzheimer's disease assessment). Slows down 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 and unreasonable repetitive motions.

Pharmacokinetics:

When taken orally donepezil quickly absorbed and reaches maximum plasma concentrations after 3-4 hours. Plasma concentrations and area under the concentration-time curve (AUC) increase in proportion to the dose. Stable concentrations in the plasma are achieved after 3 weeks. Food and time do not affect the absorption of the drug.

95% of donepezil bind to plasma proteins. On the connection with plasma proteins of the active metabolite - 6-O-desmethyldone peroxide is unknown. The distribution was not studied. Donepezil and / or its metabolites can persist in the body for more than 10 days. The volume of distribution is approximately 12 l / kg body weight.

Donepezil is metabolized in the liver by the cytochrome P450 system. The total clearance of donepezil is up to 0.13 l / kg / h or 10 l / h. After a single administration of 5 mg, the concentration of unmodified donepezil in plasma was 30% of the administered dose, 6-O-desmethyldone peroxide - 11% (the only metabolite having similar activity with donepezil hydrochloride), donepezil-cis-N-oxide 9%, 5-O-desmethyldonepezil-7%, and glucuronic conjugate 5-O-desmethyldonepezil - 3%.

Approximately 57% of donepezil is excreted by the kidneys (17% - unchanged) and up to 15% - through the liver. The elimination half-life is 70 hours.

Repeated use of the drug once a day gradually leads to the creation of Css (equilibrium concentration), which is achieved within 3 weeks after initiation of therapy. In the equilibrium state, the donepezil concentration in the plasma and the corresponding pharmacodynamic activity vary slightly during the day.

Indications:

Jasnal® It is used for symptomatic treatment of dementia of the Alzheimer's type of mild and moderate severity.

Contraindications:Hypersensitivity to donepezil, piperidine derivatives and other components of the drug.

Carefully:

Syndrome of sinus node weakness (SSSU), severe arrhythmia, conduction disorders, general anesthesia, patients with a history of ulcer (history of peptic ulcer disease, non-steroidal anti-inflammatory drugs (NSAIDs)), chronic obstructive pulmonary disease (COPD), bronchial asthma, simultaneous use with acetylcholinesterase inducers, agonists and / or antagonists of the cholinergic system, patients with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome, pregnancy and period lactation.

Pregnancy and lactation:

Data on use during pregnancy and lactation are absent. The drug should be given to pregnant women only if the expected benefit of treatment exceeds the possible risk to the fetus.

Dosing and Administration:

Inside.

The initial dose is 5 mg donepezil per day (at one time) in the evening, at night.

A dose of 5 mg / day should be taken at least 1 month before reaching equilibrium concentrations of donepezil in plasma and assessing the clinical effect of treatment. A month later, if necessary, you can increase to 10 mg / day (at one time).

The maximum recommended daily dose is 10 mg.

The duration of therapy is determined by the doctor.

Side effects:

- From the cardiovascular system: rarely fainting, increased blood pressure, vasodilatation, atrial fibrillation, stress angina, myocardial infarction, sinoatrial and AV block (I degree), congestive heart failure, arteritis, bradycardia, peripheral vascular disease, supraventricular tachycardia, deep vein thrombosis;

- from the central nervous system: often (more than 5%) - fatigue, weakness, insomnia, headache, dizziness, muscle cramps; hallucinations, tremor, depression, agitation, paresthesia, aggressiveness, vertigo, ataxia, anxiety, nervousness, aphasia, unusual dreams, convulsions;

- from the digestive system: very often (> 5%) - diarrhea, nausea, vomiting; often (1 to 5%) - loss of appetite and digestive disorders, weight loss; less than 1% - stool incontinence, abdominal pain, stomach ulcers and 12- intestines, gastrointestinal bleeding, liver function disorders, hepatitis (with idiopathic liver damage, the question of discontinuing treatment with donepezil);

- from the urinary system: frequent urination, nocturnal urination, incontinence;

- from the senses: cataract, visual acuity reduction;

- from the respiratory system: shortness of breath, laryngitis, bronchitis;

- from the skin: skin rash, skin itching, urticaria, ecchymosis, a feeling of "tides" of blood to the skin of the face, sweating, purpura;

- Other: rarely - a slight increase in the concentration of muscle CKK in the serum, anemia, thrombocytopenia, erythrocytopenia and eosinophilia, pain of different localization, cold.

Overdose:

Symptoms: cholinergic crisis (severe nausea, vomiting, increased salivation, sweating, bradycardia, arterial hypotension, respiratory depression, collapse and convulsions). Muscle weakness can develop with inhibition of respiratory muscle function, which can cause death.

Treatment: symptomatic therapy. As an antidote, it is possible to use tertiary anticholinergics, incl. slow intravenous administration of atropine: the initial dose from 1,0 before 2,0 mg IV, maintenance doses - depending on the effect. Monitoring of vital functions. It is not known whether donepezil and / or its metabolites in dialysis (hemodialysis, peritoneal dialysis or hemofiltration).

Interaction:

Donepezil hydrochloride and / or its metabolites do not inhibit metabolism theophylline, warfarin, thioridazine, risperidone, sertraline, cimetidine, or digoxin. The simultaneous use of donepezil and digoxin, thioridazine, risperidone, sertraline, cimetidine Do not change metabolism donepezil.

Inhibitors of cytochrome P isoenzyme450 3A4 (itraconazole, erythromycin) and 2D6 (fluoxetine) or inhibitors CYP3A4 and CYP2D6 (ketoconazole, quinidine) Suppress metabolism donepezil.

Inductors CYP3A4 and CYP2D6 (rifampicin, phenytoin, carbamazepine and ethanol) reduce the concentration of donepezil in the blood.

Donepezil can reduce the activity of drugs with anticholinergic activity (atropine, scopolamine, benzatropin, diphenhydramine).

Donepezil acts as a synergist when combined with suksametazonium chloride, other neuromuscular blockers and β-blockers, affecting the conduction system of the heart.

With simultaneous application to other cholinomimetics and quaternary anticholinergics such as glycopyrronium bromide, cases of atypical changes in arterial administration (BP) and heart rate (HR) are described.

Special instructions:

Treatment should be prescribed and conducted by a specialist doctor who has experience in managing patients with dementia such as Alzheimer's. The diagnosis of the disease should be made in accordance with generally accepted criteria (for example, DSM IV - Diagnostic and Statistical Manual on Mental Disorders of the Fourth Revision, ICD 10 - International Classification of Diseases of the Tenth Revision). Treatment can be carried out only if there is a person able to control the intake of medicines.

Treatment is carried out as long as there is a therapeutic effect that should be regularly evaluated. If there is no curative effect, the drug should be stopped.After the drug is discontinued, its effect gradually and slowly disappears. Information about the syndrome of "cancellation" in the event of a sudden discontinuation of donepezil is not.

Individual response to therapy donepezil oh, it's impossible to predict.

Being an inhibitor of cholinesterase donepezil can enhance succinylcholine type of muscle relaxation during general anesthesia. It can also have a vagotonic effect on the heart rate (cause bradycardia). Therefore, it should be used with caution in patients with sinus node weakness syndrome (SSSU), severe arrhythmia, supraventricular conduction disorders (sinoatrial and atrioventricular blockade).

Patients at risk for developing ulcers (for example, in patients with a history of peptic ulcer disease or receiving non-steroidal anti-inflammatory drugs (NSAIDs)) should be carefully monitored. Cholinomimetics can increase the secretion of acid in the stomach. At the same time, placebo-controlled clinical trials showed no increase in the incidence of peptic ulcers or gastrointestinal bleeding compared with placebo.

Being a holinomimetic, donepezil can cause generalized convulsive seizures, although they may be a manifestation of Alzheimer's disease.

Particular care should be taken when prescribing a patient with bronchial asthma or obstructive pulmonary disease in an anamnesis.

Donepezil can not be administered simultaneously with acetylcholinesterase inhibitors, holinomimetics and holinoblokatorami.

One Yasnala® 5 mg tablet contains 84 mg of lactose, and a 10 mg tablet contains 168 mg of lactose. At recommended doses with each dose, the patient receives 84 mg or 168 mg of lactose. Therefore, the drug is not recommended for persons suffering from lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.

Effect on the ability to drive transp. cf. and fur:

The drug has an effect on psychophysical abilities. Dementia Alzheimer's type itself can affect the ability to drive and work with machinery. In addition, the drug can cause fatigue, dizziness, muscle cramps (especially at the beginning of treatment or with increasing doses). The ability of the patient to drive a car should be evaluated by a doctor.

Form release / dosage:

Tablets, film-coated, 5 mg and 10 mg.

Packaging:

For 7 or 10 tablets in a blister pack.

For 1, 4, 8 or 14 blisters (a blister for 7 tablets) in a pack of cardboard along with instructions for use.

For 3, 6 or 12 blisters (blister for 10 tablets) in a pack of cardboard along with instructions for use.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008113/08

Date of registration:14.10.2008

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp19.01.2016

Illustrated instructions

Instructions

Jasnal® (Yasnal®)