Memantine pills 20mg №90

Tradename:

Memantine canon

International non-proprietary name:

memantine

Dosage Form:

film coated tablets

Pharmacotherapeutic group:

dementia treatment tool.

Pharmachologic effect:

Adamantane derivative, by chemical structure and pharmacological properties similar to amantadine. Memantine blocks glutamate NMDA receptors (including in the substantia nigra), thereby reducing the excessive stimulatory effect of cortical glutamate neurons on neostratum, which develops against the background of insufficient release of dopamine. At the moment there is no evidence base reliably showing the ability of the drug to slow down or prevent the progressive course of Alzheimer's disease.
Pharmacokinetics
Food intake does not affect absorption. After ingestion, it is quickly and completely absorbed (absolute bioavailability of about 100%). The maximum plasma concentration is reached within 3-8 hours. Distribution: when taking a dose of 20 mg, the concentration of memantine in the blood plasma is 70-150 ng / ml. The volume of distribution of the drug is 10 l / kg, the relationship with plasma proteins - 45%. T1 / 2 of the drug 60 - 80 hours.
Biotransformation: approximately 80% of memantine is in the form of the original substance.The main metabolites in humans are N-3,5-dimethylgludantan, a mixture of 4- and 6-hydroxymemantine isomers and 1-nitroso-3,5-dimethyl-adamantane. None of these metabolites has pharmacological activity.
Elimination proceeds in single phase, T1 / 2 is 60 - 100 hours, clearance is 170 ml / min / 1.73 m2. Excreted by the kidneys, with alkaline urine excretion slows down.

Indications for use:

- Dementia of Alzheimer's type of moderate and severe severity.

Contraindications:

Hypersensitivity, severe renal failure, severe liver failure, congenital intolerance to galactose, lactase deficiency or glucose impaired glucose / galactose absorption syndrome, pregnancy, lactation, children under 18 years of age (efficacy and safety not established).

Use during pregnancy and lactation:

Acceptance of memantine is contraindicated during pregnancy and lactation.

Carefully:

It is used with caution in patients with thyrotoxicosis, epilepsy, myocardial infarction, heart failure, convulsive syndrome in history, factors that increase the pH of urine, simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), factors that increase the pH of urine (abrupt diet changes). plentiful reception of gastric buffers), severe urinary tract infections, myocardial infarction (in history), heart failure III-IV functional class NYHA, uncontrolled arterial hypertension, renal insufficiency Th, hepatic failure.

Dosage and administration:

Inside, during a meal, without chewing, drinking plenty of liquid.
Adults with dementia are prescribed during the 1st week of therapy at a dose of 5 mg / day, during the 2nd week at a dose of 10 mg / day (5 mg 2 times a day). During the 3rd week - at a dose of 15 mg / day (5 mg and 10 mg per day). The maximum daily dose of 20 mg.
The approximate value of the maintenance dose is 10-20 mg / day. The last dose is recommended to take in the afternoon.
In elderly patients: according to the results of clinical studies, the recommended dose for patients older than 65 years is 20 mg per day.
Children and adolescents under 18 years of age are not recommended to take the drug, due to the lack of data on efficacy and safety for these categories of patients.
Patients with kidney disease:
- With mild renal insufficiency (creatinine clearance 50–80 ml / min), dosage adjustment is not required.
- With an average degree of renal failure (creatinine clearance 30-49 ml / min), the dose should be 10 mg per day. In the case of good tolerability for at least 7 days of treatment, the dose may be increased to 20 mg per day according to the standard treatment regimen.
- With severe renal insufficiency (creatinine clearance 5-29 ml / min), the dose of the drug should not exceed 10 mg per day.
Patients with liver disease:
With a mild degree of liver failure (Child-Pugh grades A and B): no dose adjustment is required.
With severe liver failure: the daily dose should not exceed 10 mg.

Side effect:

From the central and peripheral nervous system
Often: headache, dizziness, gait disturbance, cramps, drowsiness, increased intracranial pressure.
Very rarely: epileptic seizures. Infrequently: increased fatigue.
Mental disorders
Infrequently: depression, irritability, sleep disturbance, confusion, hallucinations, psychotic reactions.
Since the cardiovascular system
Often: hypertension. Infrequently: venous thrombosis / thromboembolism, heart defects.
From the digestive system
Often: constipation. Infrequently: nausea, vomiting, pancreatitis.
On the part of the respiratory system
Upper respiratory tract infections, bronchitis, flu-like syndrome, dyspnea.
On the part of the urinary system
Urinary Tract Infections
From the skin:
Rarely: fungal diseases.
On the part of the immune system:
Often: hypersensitivity to the drug
General reactions: General weakness

Overdose:

In the course of ongoing clinical studies and post-marketing research of memantine drugs, a limited amount of information about overdose was obtained.
Symptoms: With sufficiently large overdose (200 mg once or more than 100 mg per day for 3 days), the following symptoms were identified: weakness, fatigue, diarrhea, or absence of symptoms. With an overdose of less than 140 mg or with an unknown overdose, the following adverse events from the nervous system were identified: confusion, drowsiness, dizziness, agitation, aggression, hallucinations and gait disturbance from the gastrointestinal tract: vomiting and diarrhea.
In the most serious cases of overdose, the patient survived after taking more than 2000 mg of memantine with adverse events from the nervous system (coma for 10 days, diplopia, agitation). The patient received symptomatic therapy and plasmapheresis and recovered without any consequences.
Another described case of a serious overdose is 400 mg once. The patient recovered without consequences. There were reactions from the nervous system: anxiety, psychosis, visual hallucinations, stupor, drowsiness, unconsciousness.
Treatment: in case of overdose, symptomatic treatment is necessary. There is no specific antidote for intoxication with memantine. Conduct standard procedures for the evacuation of the drug by washing, the use of activated charcoal, forced diuresis, means alkalizing urine.
In the event of symptoms of over-irritation of the central nervous system, symptomatic therapy should be chosen very carefully.

Interaction with other drugs:

-In case of simultaneous use with levodopa preparations, dopamine receptor agonists, m-cholinoblockers, the action of the latter can be enhanced.
-When used simultaneously with barbiturates, neuroleptics, the effect of the latter may decrease.
-When used together, it can change (increase or decrease) the effect of dantrolene or Baclofen, so the doses of drugs should be selected individually.
- Avoid concurrent use with phenytoin, amantadine, ketamine and dextramethorphan.
- Possible increase in plasma concentrations of cimetidine, procainamide, quinidine, kinin and nicotine while taking it with memantine.
- It is possible to reduce the concentration of hydrochlorothiazide while taking it with memantine.
- According to the post-marketing experience of using memantine, there were isolated cases of reduced INR in patients simultaneously taking Warfarin .
- In pharmacokinetic studies in healthy young volunteers, once taking memantine with Metformin or donepezil, no interaction effects were recorded.
-Also in similar studies no interaction with galantamine was found.

Special instructions:

In patients with Alzheimer's disease at the stage of moderate and severe dementia, the ability to drive vehicles and manage complex mechanisms is usually impaired.
Memantine can cause a change in the reaction rate, therefore, patients receiving outpatient treatment should take special care when driving vehicles or operating machinery.

Storage conditions:

In a dry, dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.