Index of drugs

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

1 tabl powl. contains 10 mg or 20 mg of Memantine hydrochloride. The tablets contain lactose.

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 is approximately 45% bound to plasma proteins. The volume of distribution is 10 l / kg. In humans, 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 do not show any NMDA receptor 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. Memantine exhibits linear pharmacokinetics in the 10-40 mg dose range.

Hypersensitivity to memantine or to any of the excipients.

Caution is advised in patients with epilepsy, history of seizures or in patients with predisposing factors for epilepsy. The simultaneous administration of N-methyl-D-aspartic acid (NMDA) antagonists such as amantadine, ketamine or dextromethorphan should be avoided because these agents affect the same receptor system as memantine. Their concomitant administration may lead to an increase in frequency and severity of adverse reactions, mainly including o.u.n. Careful monitoring of patients with factors that may lead to an increase in urine pH: drastic changes in diet, eg meat diet to vegetarian or high doses of alkalising gastric agents, and tubular or renal acidosis or severe urinary tract infections caused by bacteria of the genusProteus. Due to limited clinical data, patients should be closely monitored during treatment of patients with recent myocardial infarction, uncompensated congestive heart failure (NYHA III-IV) or uncontrolled hypertension. It is not recommended to use the drug in patients with severe hepatic impairment. The tolerance and dosage of memantine should be regularly evaluated, especially during the first 3 months of treatment. Then, the therapeutic effect of memantine and treatment tolerance should be regularly assessed in accordance with current guidelines. The drug is not recommended for use in children and adolescents under 18 years of age due to the lack of data on safety and efficacy. The drug contains lactose - patients with rare hereditary problems of galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose should not use the drug.

It must not be used during pregnancy unless clearly necessary (no clinical data available). The results of animal studies indicate that there is a risk of suppression of intrauterine fetal growth at exposure levels that are identical or slightly higher than human exposure levels. Women using memantine should not breast-feed.It has not been found whether memantine is excreted in human milk, but this is possible due to the lipophilic properties of the drug.

Common: hypersensitivity to the drug, drowsiness, dizziness, balance disorders, hypertension, dyspnoea, constipation, increased liver enzymes, headaches. 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 thoughts and suicides - such cases have been reported on the market following the introduction of the drug.

Orally. Adults. The maximum daily dose is 20 mg per day. In order to reduce the risk of adverse reactions, the dose should be gradually increased by 5 mg per week during the first 3 weeks of treatment until the maintenance dose is reached, according to the following scheme: 1. week (day 1 - 7): 5 mg once daily for 7 days; 2nd week (day 8 - 14): 10 mg once a day for 7 days; 3rd week (day 15 - 21): 15 mg once daily for 7 days; from the 4th week (from day 22): 20 mg once a day. The maintenance dose is 20 mg once a day. Maintenance treatment can be continued as long as the beneficial therapeutic effect is maintained and the patient tolerates memantine treatment well. Discontinuation of therapy should be considered if there is no evidence of therapeutic effect or if treatment tolerance is poor. In patients with slightly impaired renal function (creatinine clearance 50-80 ml / min) no dosage adjustment is required. In patients with moderate renal impairment (creatinine clearance 30-49 ml / min), the daily dose should be reduced to 10 mg once a day. If the treatment is well tolerated for at least 7 days, the dose may be increased to 20 mg once a 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 as a single dose.
The drug should be administered once a day, at the same time each day, it can be taken with or without food. Table. can be divided into two equal doses.