Jasna

Manufacturer:
KRKA, d.d

Latin name:
YASNAL

Group affiliation:
Selective inhibitor of brain acetylcholinesterase. Drug for the treatment of dementia

Active substance Ath:
N06DA02 Donepezil

Pharmaceutical form:
Pills, Film-coated

Application:
After consultation with the doctor

Pharmacological action

Selective and reversible inhibitor acetylcholinersterase, which is the predominant type of cholinesterase in the brain. Dniepezu inhibits this enzyme in more than 1000 times stronger, than Butyrholinsterase, contained, primarily, Outside the central nervous system.
After a single reception, dnopted in doses 5 mg or 10 MG degree of suppression of activity of acetylcholinersterase, measured in the membranes of red blood cells, are, respectively, 63.6 and 77.3%.
Inhibiting acetylcholinersterase in red blood cells under the influence of a dimensional correlates with changes in the ADAS-COG scale (Assessment scale for cognitive functions in Alzheimer's disease).

Testimony

Symptomatic treatment of the dementia of the Alzheimer type of mild or moderate severity.

Contraindications

Increased sensitivity to prenipezil and pyperidine derivatives.

Side effects

From the digestive system: often – diarrhea, nausea, vomiting; dyspepsia are possible, hepatitis, stomach ulcers and duodenum and bleeding from the gastrointestinal tract, anorexia.

From the central and peripheral nervous system: often – fatiguability, insomnia, muscle cramps; possible headache, dizziness, hallucinations, anxiety, violent behavior, seizures.

Cardio-vascular system: rarely – fainting, bradycardia, sinoatrialnaya and AV-blokada.

Other: rarely – A slight increase in the concentration of muscle CFC in serum; pain of various localization is possible, accidents, cold, muscle cramps.

Dosing and Administration

Adults (incl. elderly patients) administered in an initial dose of 5 mg 1 time / Reception in the initial dose continues for at least 4-6 weeks, To achieve equilibrium concentrations of dimensional and determine the early clinical effect of therapy. Through 1 month, the dose can be increased to 10 mg /

The maximum daily dose is 10 mg /

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

Cautions

With caution in patients with obstructive diseases of the lungs in an anamnesis (incl. asthmatic), with heart rhythm disturbances, during anesthesia, as well as patients with an increased risk of ulcer development (eg, patients with a history of peptic ulcer or receiving concomitant NSAID therapy).

It is necessary to avoid simultaneous use with other inhibitors of acetylcholinerase, agonists or antagonists of the holinergic system.

The treatment must be prescribed and conducted by the doctor, having experience of patients with Alzheimer's disease.

Supportive therapy can be continued until, As long as the therapeutic effect. If the therapeutic effect disappears, then dineps should be canceled. After the cessation of treatment, there is a gradual reduction in the action of preneps, There are no messages about the syndrome in the case of a sharp cessation of administration. An individual reaction to the therapy with a dimensional cannot be predicted.

The efficiency of dimensional in patients with a severe form of alzheimer type dementia, other types of dementia or other types of memory impairment (eg, age -related deterioration of cognitive function) I have not been studied.

Donepezil, It is a cholinesterase inhibitor, can enhance muscle relaxation suktsinilholinovogo type during anesthesia.

Cholinesterase inhibitors (incl. donepezil) may have vagotonic effects on heart rate (in particular, Call bradycardia). The potential possibility of such an action can be important for patients with SSU or other violations of the supraventricular conductivity, such as syno).

It is believed, that holinomimetics are able to cause generalized convulsions. However, the appearance of convulsions during the treatment with a dimensile may also be a manifestation of Alzheimer's disease.

The safety and efficiency of the use of preneps in children was not studied, Therefore, the drug is not recommended to prescribe this category of patients.

Effects on ability to drive vehicles and operate machinery

The dementia of the Alzheimer type itself may be accompanied by a violation of the ability to drive a car and the use of complex equipment. Besides, donepezil, mainly at the beginning of treatment or with an increase in the dose, may cause fatigue, dizziness and muscle cramps. The question of the patient’s ability with the dementia of the Alzheimer type during the use of the dimensill to drive a car or use complex equipment should be decided by the doctor after assessing the patient’s individual reaction to treatment.

Cooperation

Clinical experience in the use of dimensional is limited, Therefore, when applied, the risk of unknown to the present moment of manifestations of interaction with other drugs should be taken into account.

Doneps is metabolized with the participation of the CYP3A4 isoenzyme and to a lesser extent – CYP2D6. Ketoconazole and quinidine, which are CYP3A4 and CYP2D6 inhibitors, respectively, Suppress the metabolism of dimensional. Hence, These and other CYP3A4 inhibitors, such as itraconazole and erythromycin, and CYP2D6 inhibitors, Such as fluoxetine, can inhibit metabolism dimensional. In healthy volunteers, ketoconazole increased the average concentration of dimensional 30%. However, this action was not comparable to the action of ketoconazole on other substances, metabolized with the participation of CYP3A4, Therefore, it is unlikely to have a clinical value.

Enzymes inducers, such as rifampicin, phenytoin, Karbamazepine and ethanol can cause a decrease in dimensional. However, the degree of such an inhibitory or inducing action is unknown (With simultaneous use, caution is required).

Donpezil can influence the effect of drugs, having anticholinergic activity. Besides, while applying, Doneps could strengthen the action, other muscle relaxants or agonists of holinergic receptors and beta-blockers, influencing the conductivity of the heart, although the study in vitro showed, that the hydrochloride dance has a minimum effect on the hydrolysis of succinylcholine.

With the simultaneous use of dimensile with other cholinomimetics and quarterly anticholinergic drugs, Such as glycopyrrolate, Cases of atypical changes in blood pressure and heart rate are described.

Shelf life

3 year