Memantin Kanon

General characteristics. Structure:

Active agent: memantina hydrochloride of 10 mg,
excipients: silicon dioxide colloid (aerosil) of 3 mg; hydrophosphate calcium dihydrate of 50,4 mg; croscarmellose sodium (primelloza) of 3 mg; lactoses monohydrate (sugar milk) 136 mg; magnesium stearate of 1,6 mg; povidone of 6 mg;
structure of a cover: Selekoat of AQ-02003 6 mg, including: gipromelloz (gidroksipropilmetiltsellyuloz) of 3,6 mg; macrogoal-6000 (polyethyleneglycol 6000) of 1,2 mg; titanium dioxide of 1,2 mg.

Description
Tablets, film coated white or almost white color, round, biconvex. On cross section – almost white color.

Pharmacological properties:

Derivative an adamantana, on chemical structure and pharmacological properties it is close to an amantadin. Miemangting blocks glutamate NMDA receptors (including in black substance), thereby reducing the excessive stimulating influence of cortical glutamate neurons on a neostratum developing against the background of insufficient release of dopamine. At the moment there is no evidential base authentically showing ability of drug to slow down or prevent progressive disease of Alzheimer.

Pharmacokinetics. Meal does not influence absorption. After intake it is quickly and completely soaked up (absolute bioavailability about 100%). The maximum concentration in a blood plasma is reached during 3-8 h. Distribution: at reception of a dose of 20 mg concentration of a memantin in a blood plasma of 70-150 ng/ml. The volume of distribution of drug makes 10 l/kg, communication with proteins of plasma – 45%. Drug 60 T1/2 – 80 hours.
Biotransformation: about 80% of a memantin are in a type of initial substance. The main metabolites at the person are N-3,5-dimetilgludantan, mix of isomers 4-and 6-gidroksimemantin and 1-nitrozo-3,5-dimethyl-адамантан. Any of these metabolites has no pharmacological activity.
Elimination proceeds odnofazno, T1/2 makes 60 – 100 hours, the clearance makes 170 ml/min. / 1.73 sq.m. It is removed by kidneys, at alkali reaction of urine removal is slowed down.

Indications to use:

Dementia of altsgeymerovsky type of average and heavy degree of manifestation.

Route of administration and doses:

Inside, during food, without chewing, washing down with enough liquid.
The adult at dementia appoint within 1 week of therapy in a dose 5 mg/days, within the 2nd week - in a dose of 10 mg/days (on 5 mg 2 times in days). Within the 3rd week - in a dose of 15 mg/days (5 mg and 10 mg in days). Maximum daily dose of 20 mg.
Approximate value of a maintenance dose - 10-20 mg/days. The last dose is recommended to accept in the second half of day.
At patients of advanced age: by results of clinical trials, the recommended dose for patients is more senior than 65 years – 20 mg a day.
To children and teenagers 18 years are younger administration of drug is not recommended, owing to lack of data on efficiency and safety for these categories of patients.
To patients with pathology of kidneys:
- With easy degree of a renal failure (clearance of creatinine of 50 - 80 ml/min.) correction of doses is not required.
- With average degree of a renal failure (clearance of creatinine of 30-49 ml/min.) the dose of drug has to be 10 mg a day. In case of good tolerance within at least 7 days of treatment, the dose can be raised to 20 mg a day according to the standard scheme of treatment.
- With a heavy renal failure (clearance of creatinine of 5-29 ml/min.) the dose of drug should not exceed 10 mg a day.
To patients with liver pathology:
With easy degree of a liver failure (classes A and B on a scale of Chayld-Pyyu): correction of a dose of the accepted drug is not required.
With heavy degree of a liver failure: the daily dose should not exceed 10 mg.

Features of use:

At patients with Alzheimer's disease at a stage of moderate and heavy dementia ability to driving of motor transport and control of difficult mechanisms is usually broken.
Miemangting can cause change of speed of response therefore the patients receiving treatment in out-patient conditions should observe extra care during the driving of motor transport or control of mechanisms.

Side effects:

From the central and peripheral nervous system
Often: headache, dizziness, disturbance of gait, spasm, drowsiness, increase in intracranial pressure.
Very seldom: epileptic seizures. Infrequently: increased fatigue.
Mental disturbances
Infrequently: depression, hyperexcitability, sleep disorder, confusion of consciousness, hallucination, psychotic reactions.
From cardiovascular system
Often: hypertensia. Infrequently: venous thrombosis / thromboembolism, heart diseases.
From the alimentary system
Often: lock. Infrequently: nausea, vomiting, pancreatitis.
From respiratory system
Upper respiratory tract infections, bronchitis, grippopodobny syndrome, диспноэ.
From an urinary system
Infections of an uric path
From integuments:
Seldom: fungus diseases.
From immune system:
Often: hypersensitivity to drug
General reactions: General weakness.

Interaction with other medicines:

- At simultaneous use with levodopa drugs, agonists of dopamine receptors, m-holinoblokatorami action of the last can amplify.
- At simultaneous use with barbiturates, neuroleptics action of the last can decrease.
- At combined use can change (to strengthen or reduce) action of a dantrolen or Baclofenum therefore doses of drugs should be selected individually.
- It is necessary to avoid simultaneous use with Phenytoinum, amantadiny, ketamine and dextromethorphan.
- Increase in plasma of concentration of Cimetidinum, procaineamide, quinidine, a kinin and nicotine at a concomitant use is possible with memantiny.
- Decrease in concentration of a hydrochlorothiazide at a concomitant use is possible with memantiny.
- By experience of post-marketing use of a memantin separate cases of decrease in MNO at the patients who are at the same time accepting Warfarin were registered.
- In pharmacokinetic researches at healthy young volunteers at a single dose of a memantin with metformin or donepezil no effects of interaction were recorded.
- Also in similar researches interaction with Galantaminum is not revealed.

Contraindications:

Hypersensitivity, heavy renal failure, heavy liver failure, inborn intolerance of a galactose, deficit of lactase or syndrome of the broken absorption of a glucose/galactose, pregnancy, the lactation period, children's age up to 18 years (efficiency and safety are not established).

Use at pregnancy and in the period of a lactation:
Reception of a memantin is contraindicated at pregnancy and in the period of a lactation.

With care:
With care apply at patients with a thyrotoxicosis, epilepsy, at a myocardial infarction, heart failure, a convulsive syndrome in the anamnesis, factors the raising urine pH, simultaneous use of antagonists of NMDA receptors (амантадин, ketamine, dextromethorphan), factors the raising urine pH (sharp change of a diet, plentiful reception of gastric buffers), heavy infections of urinary tract, a myocardial infarction (in the anamnesis), heart failure the III-IV functional class NYHA, uncontrollable arterial hypertension, a renal failure, a liver failure.

Overdose:

In the course of the conducted clinical researches and a post-market research of drugs of a memantin the limited amount of information about overdoses was received.
Symptoms: At rather big overdoses (200 mg once or more than 100 mg a day within 3 days) the following symptoms were revealed: weakness, fatigue, diarrhea or lack of symptoms. At overdose less than 140 mg or at unknown overdose were revealed the following undesirable phenomena from a nervous system: confusion of consciousness, drowsiness, dizziness, agitation, aggression, hallucinations and disturbance of gait and from digestive tract: vomiting and diarrhea.
In the most serious cases of overdose the patient survived after reception of more than 2000 mg of a memantin with the undesirable phenomena from a nervous system (a lump within 10 days, a diplopia, agitation). The patient received symptomatic therapy and a plasma exchange and was recovered without any effects.
Other described case of serious overdose – 400 mg once. The patient recovered without effects. Reactions from a nervous system were noted: concern, psychosis, visual hallucinations, stupor, drowsiness, unconsciousness.
Treatment: in case of overdose it is necessary to carry out a symptomatic treatment. The specific antidote at intoxication memantiny does not exist. To carry out standard procedures for evacuation of drug by washing, use of absorbent carbon, the artificial diuresis, means alkalinizing urine.
In case of symptoms of superirritation of the central nervous system, symptomatic therapy has to be picked up extremely accurately.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 10 mg.
On 10, 20 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 1, 3, 6, 9, 10, 12 blister strip packagings on 10 tablets or on 3, 5, 6 blister strip packagings on 20 tablets, or on 1, 2, 3, 4 blister strip packagings on 30 tablets together with the application instruction place in a pack from a cardboard.