Aricept
Instructions for use:
- 1. Release form and composition
- 2. Indications for use
- 3. Contraindications
- 4. Method of application and dosage
- 5. Side effects
- 6. Special instructions
- 7. Drug interactions
- 8. Analogs
- 9. Terms and conditions of storage
- 10. Terms of dispensing from pharmacies
Arisept is a selective reversible acetylcholinesterase inhibitor.
Release form and composition
Dosage form - film-coated tablets: round, biconvex:
- 5 mg each: white film shell, engraving "Aricept" on one side and "5" on the other; on a cross section - one layer, the core is white;
- 10 mg each: white film shell, "Aricept" engraving on one side and "10" on the other; on a cross section - two layers, the core is white.
In blisters: 7 pcs. - 1 blister in a cardboard box; 14 pcs. - 2 or 7 blisters in a cardboard box; 15 pcs. - in a cardboard box 2, 4 or 8 blisters.
1 tablet contains:
- active substance: donepezil hydrochloride - 5 or 10 mg;
- auxiliary components: hyprolose, corn starch, lactose monohydrate, microcrystalline cellulose, magnesium stearate;
- film sheath: white opadry YS-1R-18134-A (macrogol, hypromellose, titanium dioxide (E 171), talc; additionally in the yellow sheath - iron oxide yellow dye).
Indications for use
The use of Arisept is indicated for the symptomatic treatment of mild, moderate and severe dementia of the Alzheimer's type.
Contraindications
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- simultaneous use with other acetylcholinesterase inhibitors, antagonists or agonists of the cholinergic system;
- children and adolescents up to 18 years old;
- hypersensitivity to piperidine derivatives;
- individual intolerance to the components of the drug.
It is recommended to prescribe Arisept with caution in case of cardiac arrhythmias (due to the risk of vagotonic effect on the heart rate, including bradycardia), a history of obstructive pulmonary pathologies (including bronchial asthma), patients with an increased risk of peptic ulcer formation (for example, if data are available a history of peptic ulcer disease or when used together with non-steroidal anti-inflammatory drugs), as well as with anesthesia.
In pregnant women, adequate controlled studies of the efficacy and safety of the drug have not been carried out, therefore, therapy is permissible only if the intended benefits of treatment for the mother are significantly exceeded over the potential risk for the fetus.
Since there is no data on the release of donepezil during lactation in lactating women, breastfeeding should be discontinued during treatment.
Method of administration and dosage
The tablets are taken orally, 1 time per day before bedtime, regardless of the meal.
Recommended dosage: the initial dose is 5 mg, to achieve equilibrium concentrations of donepezil, the administration is continued for 4-6 weeks. After evaluating the early clinical effect of therapy, the daily dose can be increased to a maximum of 10 mg. Supportive therapy can be continued until the therapeutic effect persists, which must be regularly evaluated.
No dose adjustment is required in patients with impaired liver function (mild to moderate severity) and kidney function.
The effect on clearance of donepezil has not been studied in patients with severe hepatic impairment.
Side effects
Moderate to mild Alzheimer's disease:
- the body as a whole: often - toothache, chest pain, flu; infrequently - apathy, facial edema, fever, chills, periorbital edema, phlegmon, hiatal hernia, general chills, abscess, head fullness;
- nervous system: often - aggression, delirium, increased excitability, irritability, anxiety, tremor, paresthesia, vertigo, increased libido, aphasia, ataxia, pathological cry; infrequently - emotional lability, intracranial hemorrhage, hostility, increased muscle tone, muscle spasm, pathological gait, stroke, transient ischemic attack, chills (local), neuralgia, dysphoria, hypokinesia, numbness (local), neurodermatitis, paranoia, dysphasia decreased libido, emotional isolation, melancholy, long strides, nystagmus;
- cardiovascular system: often - increased blood pressure (BP), hot flushes, vasodilatation, decreased blood pressure, atrial fibrillation; infrequently - bradycardia, angina pectoris, peripheral vascular disease, postural hypotension, atrioventricular block I degree, myocardial infarction, chronic heart failure, supraventricular tachycardia, arteritis, deep vein thrombosis;
- lymphatic system and blood system: infrequently - thrombocytopenia, anemia, thrombocytosis, eosinophilia, erythropenia;
- digestive system: often - epigastric pain, fecal incontinence, bloating, gastrointestinal bleeding; infrequently - dry mouth, increased appetite, belching, intense thirst, flatulence, gingivitis, cholelithiasis, periodontal abscess, salivation, diverticulitis, herpes simplex, irritable bowel syndrome, gastritis, tongue edema, gastroenteritis, gastric discomfort, melena, increased transaminase activity, intestinal obstruction, hemorrhoids, jaundice, stomach ulcer, duodenal ulcer, polydipsia;
- metabolism and nutrition: often - dehydration; infrequently - increased body weight, gout, hyperglycemia, hypokalemia, increased activity of creatine phosphokinase and / or lactate dehydrogenase;
- endocrine system: infrequently - goiter, diabetes mellitus;
- musculoskeletal system: often - bone fractures; infrequently - myofasculation, muscle weakness;
- sense organs: often - blurred vision, eye irritation, cataracts; infrequently - an unpleasant taste in the mouth, flashing "flies" before the eyes, dryness of the mucous membrane of the eyes, hemorrhage in the retina, glaucoma, hemorrhage in the conjunctiva, ringing in the ears, hearing loss, ear pain, blepharitis, otitis media, kinetosis, otitis externa, noise in ears;
- respiratory system: often - sore throat, shortness of breath, bronchitis; infrequently - runoff of mucus from the nasopharynx, vomiting, pneumonia, congestion in the lungs, hyperventilation, wheezing, pharyngitis, hypoxia, pleurisy, snoring, sleep apnea, lung collapse;
- genitourinary system: often - nocturia, urinary incontinence; infrequently - urge to urinate, dysuria, metrorrhagia, hematuria, cystitis, prostatic hyperplasia, enuresis, pyelonephritis, mastitis, fibroadenosis of the mammary glands, inability to empty the bladder, fibrocystic mastopathy, vaginitis, pyuria, renal failure;
- dermatological reactions: often - pruritus, profuse sweating, urticaria; infrequently - night sweats, dermatitis, discoloration of the skin, erythema, hyperkeratosis, fungal dermatitis, alopecia, shingles, skin striae, hirsutism, skin ulcers.
Severe Alzheimer's disease:
- the body as a whole: often - abdominal pain, asthenia, fungal infection, flu-like syndrome; infrequently - facial edema, malaise, allergic reaction, hernia, phlegmon, sepsis;
- nervous system: often - anxiety, tremor, agitation, convulsions, pathological gait, vagrancy; infrequently - delirium, apathy, increased salivation, vertigo, euphoria, pathological dreams, ataxia, increased muscle tone, vasodilatation, dementia, cerebral ischemia, major seizure, extrapyramidal syndrome, hemiplegia, cerebral hemorrhage, hypokinesia, cerebral artery disease, cerebral hemorrhage stroke;
- cardiovascular system: often - pathological deviation of electrocardiographic parameters, bradycardia, decreased blood pressure, heart failure; infrequently - angina pectoris, cardiomegaly, myocardial infarction, peripheral vascular disease, atrial fibrillation, supraventricular extrasystoles, chronic heart failure, ventricular extrasystoles;
- metabolism and nutrition: often - weight loss, peripheral edema, increased activity of alkaline phosphatase and / or lactate dehydrogenase; infrequently - increased body weight, hypercholesterolemia, hypoglycemia, hypokalemia, hyperbilirubinemia, cachexia, increased blood urea nitrogen, gout, B 12 deficiency anemia, increased creatinine concentration, hypoproteinemia, hyponatremia, increased activity of alanine aminotransferase (ALT) A, Iron-deficiency anemia;
- digestive system: often - fecal incontinence, constipation, dyspepsia, gastroenteritis; infrequently - vomiting, dysphagia, increased activity of gamma-glutamyl transpeptidase, flatulence, gastritis, periodontitis, periodontal abscess, pathological deviation of indicators of functional liver function tests, rectal bleeding, esophagitis, stomach ulcer;
- lymphatic system and blood system: often - anemia; infrequently - leukocytosis;
- endocrine system: infrequently - diabetes mellitus;
- musculoskeletal system: often - arthritis; infrequently - bone fractures, arthrosis, cramps of the lower extremities, arthralgia, myalgia, osteoporosis;
- respiratory system: often - pneumonia, bronchitis, pharyngitis, increased cough; infrequently - bronchospasm, shortness of breath, rhinitis;
- sense organs: infrequently - visual impairment, conjunctivitis, lacrimation disorder, glaucoma, ear pain;
- dermatological reactions: often - itchy skin, rash, skin ulcers; infrequently - dry skin, urticaria, vesicular-bullous rash, sweating, psoriasis, shingles, discoloration of the skin;
- genitourinary system: often - glucosuria, urinary tract infection, hematuria, cystitis; infrequently - frequent urination, vaginitis, dysuria, albuminuria.
In addition, the following side effects have been reported in post-marketing studies: hallucinations, convulsions, aggressive behavior, hepatitis, duodenal ulcer, gastrointestinal bleeding, stomach ulcer.
special instructions
The diagnosis and prescription of Aricept should be carried out by a physician with experience in the treatment of Alzheimer's disease.
If there is no clinical effect of the drug, it is canceled. Abrupt withdrawal of donepezil after prolonged therapy does not cause withdrawal in the patient.
Taking the drug requires special care in patients with violations of supraventricular conduction with sick sinus syndrome, sinoatrial or atrioventricular block.
The appearance of seizures in a patient may be a manifestation of Alzheimer's disease, and not a side effect of the drug.
Reception of donepezil under anesthesia may cause increased muscle relaxation against the background of simultaneously used depolarizing muscle relaxants.
Mental and physical disorders in a patient with dementia of the Alzheimer's type limit his ability to drive vehicles and mechanisms. In addition, due to the possible appearance of dizziness, fatigue and muscle cramps at the beginning of treatment with donepezil or when its dose is increased, the attending physician should advise the patient about his ability to drive a car or other complex equipment during treatment.
Drug interactions
Due to the limited clinical experience of using Aricept, the physician should consider the risk of interaction when prescribing the drug in unexplored combinations with other agents.
The metabolism of donepezil is not affected by the simultaneous administration of cimetidine, digoxin, thioridazine, sertraline, risperidone.
The drug does not inhibit the metabolism of warfarin, theophylline, cimetidine, thioridazine, risperidone, digoxin, sertraline.
Ketoconazole, itraconazole, quinidine, erythromycin (inhibitors of the CYP3A4 isoenzyme) and fluoxetine (an inhibitor of the isoenzyme CYP2D6) slightly suppress donepezil metabolism.
Donepezil has no effect on the pharmacokinetics of ketoconazole.
Phenytoin, rifampicin, carbamazepine, ethanol (inducers of liver microsomal enzymes) can reduce the concentration of donepezil, but the degree of their inhibitory or inducing effect has not been established.
Arisept can reduce the effect of drugs with anticholinergic activity.
With concomitant therapy, donepezil can enhance the effect of muscle relaxants, cholinergic receptor agonists, beta-blockers acting on cardiac conduction.
When combined with glycopyrronium bromide and other quaternary anticholinergics, cholinomimetics, an atypical change in blood pressure and heart rate is possible.
Taking the drug for 21 days simultaneously with the combination therapy with levodopa and carbidopa does not affect the patient's motor activity and the blood content of each drug.
Analogs
Arisept's analogs are: Divare, Alzepil, Yasnal, Alzamed, Aripezil, Donerum, Servonex, Dementis.
Terms and conditions of storage
Keep out of the reach of children. Store at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
