Index of drugs

Treatment of patients with moderate to severe Alzheimer's disease.

tablets. 1 tabl powl. contains 10 mg (20 mg) of Memantine hydrochloride equivalent to 8.31 mg (16.62 mg) of memantine. The tablets contain lactose.Solution. 1 g of the solution contains 10 mg of memantine hydrochloride equivalent to 8.31 mg of memantine. One push of the dosing pump (1 dose) provides 0.5 ml of a solution containing 5 mg of memantine hydrochloride equivalent to 4.16 mg memantine. The solution contains sorbitol and potassium.

Memantine is a potential-dependent, medium-affinity, non-competitive NMDA receptor antagonist. It modifies the effects of pathologically increased concentrations of glutamate, which can lead to neuronal dysfunction. The absolute bioavailability of memantine is approximately 100%. The maximum plasma concentration occurs between 3 and 8 hours after taking the drug. Memantine is approximately 45% bound to plasma proteins. Approx. 80% of the drug occurs in the circulation unchanged. The main metabolites are: N-3,5-dimethylglutantane, a mixture of 4- and 6-hydroxymemantyne isomers and 1-nitroso-3,5-dimethyladamantane. These metabolites have no NMDA antagonistic activity. In researchin vitro no cytochrome P-450 enzymatic system was observed in metabolic processes. The drug is excreted through the kidneys in more than 99%. Final T_0,5 60-100 h. In the case of alkalinisation of urine, the rate of excretion of memantine by the kidneys may be reduced by 7-9 times.

Hypersensitivity to the active substance or to any of the excipients.

Caution is advised in patients with epilepsy, history of seizures or patients with predisposing factors for epilepsy. The simultaneous use of NMDA antagonists (amantadine, ketamine, dextromethorphan) should be avoided. Careful monitoring of patients with agents that may lead to an increase in urine pH (eg drastic changes in diet, high doses of stomach alkalising preparations, renal tubular acidosis, severe urinary tract infections caused by bacteria of the genus) should be carefully monitored.Proteus). Patients with recent myocardial infarction, uncompensated congestive heart failure (NYHA III-IV) or uncontrolled hypertension should be carefully monitored (limited data are available for the administration of memantine to these patients). It is not recommended for use in children and adolescents under 18 years due to a lack of data on safety and efficacy. It is not recommended for patients with severe hepatic impairment (no data). The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Memantine must not be used during pregnancy unless clearly necessary. The results of animal studies indicate a risk of suppression of intrauterine fetal growth, with exposure levels identical or slightly higher than the human exposure levels. The risk for people is unknown. It is not known whether memantine is excreted in human milk. However, this is possible due to the lipophilic properties of the drug. Women taking memantine should not breast-feed.

Common: drowsiness, dizziness, balance disorders, hypertension, shortness of breath, constipation, increased liver enzymes, headaches. Uncommon: fungal infections, hypersensitivity to the drug, confusion, hallucinations, abnormal gait, heart failure, venous thrombosis / embolism, hepatitis, fatigue. Very rare: epileptic seizures. Frequency unknown: psychotic reactions, pancreatitis. After the introduction of the drug, cases of depression, suicidal thoughts and suicides were also reported.

Orally. Treatment should be initiated by a doctor who has experience in the diagnosis and therapy of Alzheimer's disease.Treatment can only be started if the carer provides constant supervision over the patient's use of the medicine. Diagnosis should be made in accordance with the current guidelines. The tolerance and dosage of memantine should be regularly evaluated, especially during the first 3 months of treatment. Then, the therapeutic effect of memantine should be regularly evaluated and the patient should be tolerated according to the current guidelines. Maintenance treatment can be carried out as long as a beneficial therapeutic effect is maintained and the patient tolerates the treatment well. Discontinuation of treatment should be considered if there is no evidence of therapeutic effect or if treatment tolerance is poor. Adults. The maximum daily dose is 20 mg per day. In order to reduce the risk of adverse reactions, the dose should be increased gradually, by 5 mg every week, until the maintenance dose is reached, according to the following schedule: 1. week (day 1-7): 5 mg, during the first 3 weeks of treatment. once a day for 7 days; 2nd week (day 8-14): 10 mg once a day for 7 days; 3rd week (day 15-21): 15 mg daily for 7 days; starting from 4 weeks: 20 mg once a day. The recommended maintenance dose is 20 mg per day. In patients over 65 years, the recommended daily dose is 20 mg per day according to the diagram described above. In patients with slightly impaired renal function (creatinine clearance 50-80 ml / min) dose modification is not required. In patients with moderate renal impairment (creatinine clearance 30-49 ml / min) the daily dose should be 10 mg. If treatment is well tolerated for at least 7 days, the dose can be increased to 20 mg per day according to the standard schedule. In patients with severe renal impairment (creatinine clearance 5-29 ml / min), the daily dose should be 10 mg. In patients with mild or moderate hepatic impairment (Child-Pugh A and B), no dose adjustment is required. It is not recommended for patients with severe hepatic impairment. The preparation should be administered once a day, at the same time each day, regardless of meals. The solution should be dosed on a spoon or into a glass of water.