Memorial - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate - 192.5 mg, siliconized microcrystalline cellulose (microcrystalline cellulose - 36.75 mg, colloidal silicon dioxide - 0.75 mg) - 37.50 mg, talc - 2.50 mg, magnesium stearate -2.50 mg;

film jacket: Opadry OY-S-28959 (white): hypromellose (hydroxypropylmethylcellulose) - 3,1250 mg, titanium dioxide - 1,5625 mg, triacetin - 0,3125 mg.

Description:Biconvex capsular tablets covered with a white film membrane, with a risk on both sides. Color on the cut: from white to almost white.

Pharmacotherapeutic group:Dementia remedy

ATX: & nbsp

N.06.D.X.01 Memantine

N.06.D.X Other drugs for the treatment of dementia

Pharmacodynamics:Has nootropic, cerebrozodilating, antihypoxic and psychostimulating action. The adamantane derivative, by chemical structure and pharmacological properties, is close to amantadine. It blocks glutamate N-methyl-D-aspartate (NIMOA) -receptors (including in black matter), thereby reducing the excessive stimulating effect of cortical glutamate neurons on the neostriatum, which develops against the background of insufficient dopamine release. Reducing the flow of ionized calcium into neurons, reduces the possibility of their destruction. Mostly affects the stiffness (rigidity and bradykinesia). In addition to the action on the central nervous system memantine affects the efferent innervation. It improves weakened memory, concentration of attention, reduces fatigue and symptoms of depression, reduces the spasticity of skeletal muscles caused by diseases and brain damage, increases daily activity.

Pharmacokinetics:

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract. The maximum concentration is achieved in 3-8 hours.Food does not affect the absorption of the drug. A daily dose of 20 mg results in an equilibrium plasma concentration of 70 to 150 ng / ml. The distribution volume is about 10 l / kg. Connection with plasma proteins - 45%. With normal renal function, no cumulation of memantine was observed. 80% of memantine circulating in the blood is unchanged substance. Metabolism occurs without the involvement of cytochrome P450. The main metabolites are K-3,5-dimethylgludantan, an isomeric mixture of 4- and 6-hydroxymemanthine and 1-nitroso-3,5-dimethyladamantane. None of the metabolites has antagonistic activity with respect to NMDA receptors.

It is excreted mainly by the kidneys. Excretion occurs single-phase, the half-life is 60-100 h; clearance is 170 ml / min / 1.73 m², partially secreted by the renal tubules. With an alkaline urine reaction, excretion of the drug slows down (on average by 80% at a pH of urine of 8).

Indications:Dementia of moderate to severe severity in Alzheimer's disease.

Contraindications:Hypersensitivity, to the components of the drug; severe hepatic impairment; lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (the preparation contains lactose); pregnancy, breastfeeding, age under 18 years.

Carefully:Be wary appoint patients with thyrotoxicosis, epilepsy, convulsions (including in the anamnesis); simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), the presence of factors that increase the pH of urine (a dramatic diet change, a copious intake of alkaline gastric buffers), severe urinary tract infections, myocardial infarction (history), heart failure III-IV functional class (NYHA classification), uncontrolled hypertension , renal insufficiency, hepatic insufficiency.

Pregnancy and lactation:Memantine has the ability to slow the development of the fetus. For the time of treatment with memantine, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake.

During the first week, the daily dose is 5 mg (in the morning). In the second week, the daily dose is 10 mg (5 mg twice a day). During the third week, the daily dose is 15 mg per day (10 mg in the morning and 5 mg in the evening). From the fourth week, the daily dose is 20 mg per day. The maximum daily dose of 20 mg per day.

Dose adjustments in elderly patients (over 65 years) are not required.

With moderate renal failure (creatinine clearance 50-80 ml / min), dose adjustment is usually not required; with a creatinine clearance of 30-49 ml / min, the daily dose initially does not exceed 10 mg, then after 7 days, with good tolerability, the dose can be increased up to 20 mg. In severe renal failure (creatinine clearance 5-29 ml / min) daily dose should not exceed 10 mg.

With mild and moderate hepatic insufficiency (class A and B according to the Child-Pugh classification), dose adjustment is not required.

Side effects:

From the nervous system: dizziness, headache, drowsiness, gait disturbance, imbalance, confusion, hallucinations, convulsions, psychosis, increased excitability.

From the gastrointestinal tract: constipation, vomiting, pancreatitis, nausea.

Infections and infestations: fungal infections.

From the cardiovascular system: increased blood pressure, venous thrombosis, thromboembolism, congestive heart failure, dyspnea.

On the part of the body as a whole: general weakness, increased

fatigue, allergic reactions.

From the side of the blood and lymphatic system: Agranulocytosis, leukopenia (including neutropenia), pancytopenia, thrombocytopenia, thrombocytopenic purpura.

From the liver and bile ducts: hepatitis, increased laboratory parameters of liver function. Disorders of the psyche: suicidal thoughts, psychotic reactions.

From the side of the kidneys and urinary tract: acute renal failure,

From the skin: Stevens-Jones syndrome.

In Alzheimer's disease, depression, suicidal ideation and suicide attempts may occur.

Overdose:

Symptoms: dizziness, tremor, agitation, drowsiness, dullness of consciousness, agitation, stupor, convulsions, aggressiveness, hallucinations, gait unsteadiness, vomiting, diarrhea.

Treatment: gastric lavage, the appointment of activated charcoal; symptomatic therapy. There is no specific antidote. Removal of the drug can be accelerated by acidification of urine.

Interaction:

At simultaneous application it can weaken the effect of barbiturates and neuroleptics. The effects of baclofen and dantrolene may change under the influence of memantine, so their dosage may need to be corrected.

With the simultaneous use of memantine with preparations of levodopa, dopamine agonists, anticholinergic agents, the effect of the latter may be enhanced.

Due to memantine and amantadine antagonists of NMDA receptors should avoid simultaneous use because of the risk of developing toxic effects. Potentially toxic are also combinations of memantine with ketamine, dextromethorphan and phenytoin.

For the transport of amantadine, cimetidine, ranitidine, hindindine, procainamide, quinine and nicotine, the same renal cation system is used in the body, which may cause the interaction of these drugs with memantine, leading to an increase in its concentration in the blood plasma.

With simultaneous application memantine can cause a decrease in the concentration of hydrochlorothiazide in the blood serum.

When used simultaneously with warfarin and other indirect anticoagulants, careful monitoring of prothrombin time and the international normalized relationship is required.

Special instructions:An alkaline urine reaction requires a more careful observation of such patients because of the slower release of memantine.

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving a vehicle and performing work that requires a high concentration of attention.

Form release / dosage:The tablets covered with a film membrane, 10 mg.

Packaging:10 tablets in a planar cell package (blister) from a polyvinylchloride film and aluminum foil. 3, 6 or 9 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000758

Date of registration:29.09.2011 / 30.09.2016

Expiration Date:Unlimited

The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia

Manufacturer: & nbsp

BILIM ILAC SANAYI VE TICARET, A.S. Turkey

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp28.04.2018

Illustrated instructions

Instructions

Memorel® (Memorel)