A specific and reversible inhibitor of acetylcholinesterase - the main cholinesterase in the brain. In patients with Alzheimer's disease, the drug administered in therapeutic doses inhibits the enzyme activity in about 64-77%. The inhibition of acetylcholinesterase in red blood cells by donepezil correlates with changes in the ADAS-Cog scale in which selected cognitive aspects are measured. The effect of donepezil on the change in the course of the neuropathological basis has not been studied, therefore, no effect on the progression of the disease can be attributed to the drug. Cmaxin the blood occurs 3-4 h after oral administration. The food does not affect absorption. Steady state is achieved within 3 weeks. Donepezil binds to plasma proteins in 95%. It is metabolised in the liver with the participation of cytochrome P450 to many metabolites (one of the metabolites - 6-O-demethyldonepezil is pharmacologically active). The drug is excreted in the urine (in about 57%) and faeces (in about 15%). T0,5 is about 70 hours.
Contraindications:
Hypersensitivity to donepezil hydrochloride, piperidine derivatives or other ingredients of the preparation. In addition, tabl. coated - pregnancy.
Precautions:
Do not use in children and adolescents <18 years. The use of donepezil in patients with severe dementia in Alzheimer's disease, other types of dementia or other types of memory impairment (e.g., age related cognitive impairment) has not been studied. Particularly cautiously use in patients with sinus node syndrome or other supraventricular conduction disorders, i.e. embolic-atrial block or atrioventricular block (the drug may exert a vagotonic effect on the heart rate); in patients with bronchial asthma or obstructive pulmonary disease; in patients with an increased risk of peptic ulcer disease (with a history of peptic ulcer disease or taking NSAIDs, these patients should be monitored for symptoms of peptic ulcer). The preparation of donepezil together with other acetylcholinesterase inhibitors, agonists or cholinergic antagonists should be avoided. Donepezil may increase muscle relaxation caused by succinylcholine derivatives during anesthesia. During treatment, fainting or fits may occur; the possibility of blocking the heart or sinus arrest should be considered. Donepezil as a cholinomimetic can inhibit urinary outflow from the bladder and exacerbate or cause extrapyramidal symptoms. During the treatment with donepezil very rarely and especially in patients receiving concomitant antipsychotics, the occurrence of neuroleptic malignant syndrome (NMS) has been observed. If you have symptoms of RH or high fever with an unexplained reason, without other clinical symptoms of RH, donepezil should be discontinued. Consideration should be given to discontinuation of donepezil in the case of unexplained liver dysfunction. Due to the lactose content in the table in area, should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. Due to the content of sucrose, Glucose and sorbitol in the tabl. Q-Tab, should not be used in patients with fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency; Table. Q-Tab, may be harmful for patients with phenylketonuria, as they contain aspartame.
Pregnancy and lactation:
Women taking donepezil should not breastfeed. Table. coated: use of the drug in pregnancy is contraindicated if it is not absolutely necessary. Table. disintegrating in the mouth (Q-Tab): do not be used during pregnancy unless clearly necessary.
Side effects:
Very common: diarrhea, nausea, headache.Common: colds, anorexia, hallucinations, agitation, unusual dreams, nightmares, fainting, dizziness, insomnia, vomiting, stomach disorders, rash, pruritus, muscle cramps, urinary incontinence, fatigue, pain, accidents. Uncommon: convulsions, bradycardia, gastrointestinal haemorrhage, peptic ulcer of the stomach and duodenum, slight increase in muscle creatine kinase activity. Rare: extrapyramidal symptoms, atrioventricular block, sinoatrial block, liver dysfunction (including hepatitis). Very rare: a neuroleptic malignant syndrome.
Dosage:
Orally. Adults / elderly patients: initially 5 mg once daily for at least one month. After a clinical evaluation of the efficacy of the initial dose, the dose can be increased to 10 mg once a day. The maximum recommended daily dose is 10 mg. Treatment should be initiated and supervised by a physician experienced in the diagnosis and treatment of dementia in Alzheimer's disease. The diagnosis should be made in accordance with the approved guidelines (eg DSM IV, ICD 10). Treatment should only be started if the patient has a carer who will regularly monitor the use of the product. Maintenance treatment should be continued for as long as the beneficial effect of the preparation is found; Regular clinical evaluation of the medicine's action is necessary. Discontinuation of the drug should be considered when there is no longer any therapeutic effect.Special flu patients. No dosage adjustment is necessary for patients with renal insufficiency. Due to the possible increased drug exposure in patients with mild to moderate hepatic insufficiency, the dose should be adjusted to the patient's individual tolerability. There are no data on use in patients with severe hepatic impairment. The preparation should be taken in the evening, at bedtime. Put the Q-Tab tablet on the tongue and wait for it to disintegrate and then swallow; you can drink with water.
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