Index of drugs

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

1 tabl contains 10 mg Memantine hydrochloride equivalent to 8.31 mg memantine. Each press of the dispenser pump (one dose) delivers 0.5 ml of solution that contains 5 mg memantine hydrochloride equivalent to 4.16 mg memantine.

Memantine is a voltage-dependent, medium-affinity, non-competitive NMDA receptor antagonist (N-methyl-D-aspartic acid). It modifies the effects of pathologically increased glutamate concentration, which can lead to neuronal dysfunction. The results of clinical trials involving a population of patients with moderate to severe Alzheimer's disease indicate a beneficial effect of memantine compared to placebo. The use of memantine leads to improved parameters of general clinical assessment, cognitive functions and daily functioning. The results of the analysis of patients who experienced deterioration of the disease showed a statistically significant better therapeutic effect of memantine in the prevention of deterioration, compared with placebo. Following oral administration, the absolute bioavailability of the drug is approximately 100%. The maximum concentration in the blood occurs after 3-8 hours after taking the drug. Memantine binds to approximately 45% of plasma proteins. In man about 80% of the drug occurs in the circulation in unchanged form. The major metabolites are N-3,5-dimethyl-gludantane, a mixture of 4- and 6-hydroxy-memantine isomers and 1-nitroso-3,5-dimethyl-adamantane. These metabolites have no NMDA antagonistic activity. The drug is mainly excreted in the urine. T_0,5 is 60-100 h. In the kidneys there is also the process of reabsorption from the tubules, probably with the participation of proteins involved in the transport of cations. In the case of alkalinisation of urine, the rate of excretion of memantine by the kidneys may be slowed down by 7-9 times.

Hypersensitivity to memantine or other ingredients.

There are no data on the use of the drug in patients with severe hepatic impairment - use in this group of patients is not recommended. It is not recommended for children under 18 years of age, as the safety and efficacy of the medicine have not been established. Caution should be exercised in patients with epilepsy, with history of seizures or in patients with predisposing factors for epilepsy. The simultaneous use of N-methyl-D-aspartic acid (NMDA) antagonists such as amantadine, ketamine, dextromethorphan should be avoided. Caution in patients with factors that may increase urine pH (eg drastic changes in diet, high doses of alkalising gastric drugs, renal tubular acidosis, severe urinary tract infections caused by bacteria of the genusProteus). There are limited data on the use of memantine in patients with recent myocardial infarction, uncompensated congestive heart failure (NYHA III-IV) and poorly controlled hypertension - the drug should be used with caution.

The drug should not be used during pregnancy unless it is absolutely necessary. Women taking memantine should not breast-feed.

Common: hypersensitivity to the drug, drowsiness, pain and dizziness, balance disorders, hypertension, dyspnoea, constipation, increased liver enzymes. Uncommon: fungal infections, confusion, hallucinations, abnormal gait, heart failure, venous thrombosis / embolism, vomiting, fatigue. Very rare: epileptic seizures. Frequency unknown: psychotic reactions, pancreatitis, hepatitis. Alzheimer's disease is associated with depression, suicidal ideation and suicide - post-marketing experience has been reported in patients treated with the preparation.

Treatment should be started and supervised by a doctor who has experience in the diagnosis and therapy of Alzheimer's disease. Treatment can only be started if the caregiver provides constant supervision over the patient's taking the medicine. Diagnosis should be made in accordance with the current guidelines.The tolerance and dosage of memantine should be regularly reviewed, with current clinical guidelines, especially within 3 months after starting treatment. Maintenance treatment can be continued as long as the beneficial therapeutic effect is maintained and the patient tolerates memantine 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. In order to reduce the risk of side effects, the dosage should be increased gradually, by 5 mg every week, according to the following scheme: in the first week 5 mg once a day (1/2 tabl or 1 push of the pump); in the second week 10 mg once a day (1 table or 2 pump pressures); in the third week 15 mg once a day (1 1/2 tables or 3 pump pressures); from the fourth week, the recommended dose is 20 mg once a day (2 tables or 4 pump pressures).
No dosage adjustment is necessary for patients with mild or moderate hepatic impairment. In patients with slightly impaired renal function (creatinine concentration 50-80 ml / min) dose modification is not necessary; for patients with moderate renal impairment (creatinine clearance 30-49 ml / min), the daily dose should be reduced to 10 mg, for good tolerance for at least 7 days, the dose can be increased to 20 mg per day according to the schedule. In patients with severe renal impairment (creatinine clearance 5-29 ml / min) the dose should be reduced to 10 mg. In the elderly: the recommended daily dose is 20 mg.
The drug should be taken once a day, at the same time, regardless of meals. The solution must not be poured or pumped into the mouth directly from the bottle or dosing pump; it should be dosed on a spoon or into a glass of water.