Memantine Canon pills 10mg, 90pcs

Composition

1 film-coated tablet,10 mg contains: Active ingredient: memantine hydrochloride 10.00 mg; excipients: calcium hydrophosphate dihydrate 50.40 mg, colloidal silicon dioxide 3.00 mg, croscarmellose sodium 3.00 mg, lactose monohydrate 135.44 mg, magnesium stearate 2.16 mg, povidone K-30 6.00 mg; film coating: Opadry 20 And 205017 blue 6,0000 mg, including: hypromellose (hydroxypropyl methylcellulose) 2,0250 mg hyprolose (hydroxypropyl cellulose) 2,0250 mg, talc 1,2000 mg, titanium dioxide 0,6984 mg, dye brilliant blue 0,0480 mg, dye iron oxide black 0,0036 mg.

Pharmacological action of

Pharmacodynamically potentialability is a non-competitive blocker of NMDA receptors with moderate affinity to them. It modulates the effect of pathologically elevated tonic glutamate content, which can lead to neuronal dysfunction. Pharmacokineticsabsorption: memantine is rapidly and completely absorbed from the gastrointestinal tract( GIT) and has an absolute bioavailability of about 100%. Food intake does not affect absorption. The average time to reach the maximum concentration in blood plasma (Tmax) is from 3 to 8 hours. No accumulation of memantine was observed in normal renal function. Distribution: a daily dose of 20 mg creates a constant concentration of memantine in the blood plasma in the range of 70-150 ng / ml (0.5-1 mmol) with large individual variations. The volume of distribution of memantine is 10 l/kg. About 45% of memantine binds to plasma proteins. Metabolism: about 80% of memantine is excreted unchanged. The main metabolites in humans are N-3,5-dimethylgludantane, a mixture of isomers 4 – and 6-hydroxymemanthine and 1-nitroso-3,5-dimethyl-adamantane. None of these metabolites has pharmacological activity. Cytochrome P-450-catalyzed metabolism was not detected in in vitro studies. In the study, when 14C-memantine was taken orally, an average of 84% of the oral dose was eliminated within 20 days, while more than 99% was excreted by the kidneys. Deduction: memantine is excreted from the body by the kidneys monoexponentially. The half-life (T 1/2) is 60-100 hours. It is excreted by the kidneys. In volunteers with normal renal function, the total clearance is 170 ml / min/1.73 m2, part of the total renal clearance is achieved by tubular secretion. Renal elimination also includes tubular reabsorption, possibly mediated by cationic transport proteins. The rate of renal elimination of memantine under conditions of an alkaline urine reaction can decrease by 7-9 times. Alkalinization of urine can be caused by a sudden change in nutrition, for example, switching from a diet that includes animal products to a vegetarian diet, or due to the intensive use of alkaline gastric buffers. Linearity Studies conducted in volunteers showed linearity of pharmacokinetics in the dose range of 10-40 mg. Pharmacokinetic / pharmacodynamic dependence When using memantine at a dose of 20 mg / day, the level of concentration in the cerebrospinal fluid corresponds to the value of the inhibition constant (ki), which for memantine is 0.5 mmol in the frontal cortex of the brain.

Indications

Moderate to severe Alzheimer’s dementia.

Use during pregnancy and lactation

Use with caution during pregnancy (there is no sufficient experience of use during pregnancy) and breast-feeding (there are no data on penetration into breast milk).

Contraindications

• Hypersensitivity to the Active ingredient or any of the components of the drug;
• Severe hepatic insufficiency (Child-Pugh Class C);
• Congenital galactose intolerance, lactose deficiency, or glucose / galactose malabsorption syndrome;
• Pregnancy;
• Breast-feeding period;
• Children under 18 years of age (efficacy and safety have not been established).

With caution:

• Epilepsy, a history of convulsive syndrome;
• A history of myocardial infarction;
• Heart failure (NYHA grades III-IV);
• Uncontrolled arterial hypertension;
• Concomitant use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan);
• Factors that increase the pH of urine (sudden change of diet (switching from meat to vegetarian), heavy intake of alkaline gastric buffers, renal tubular acidosis or severe urinary tract infections caused by Proteus spp. );
• Kidney failure;
• Liver failure.

Side effects

Below are the adverse reactions obtained both in the course of the conducted studies and from spontaneous reports. WHO classification of adverse reactions: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (Infectious and parasitic diseases often: fungal infections. Frequency unknown: candidiasis. Immune system disorders Often: hypersensitivity to the components of the drug. Frequency unknown: allergic reactions, Stevens-Johnson syndrome. Psychiatric disorders Often: hallucinations (observed mainly in patients with severe Alzheimer’s disease). Frequency unknown: psychotic reactions, increased excitability, depression, anxiety, suicidal thoughts. Nervous system disorders often: headache, dizziness, drowsiness, balance disorders. Infrequently: gait disorder, confusion. Very rare: convulsions. Frequency unknown: impaired consciousness, increased intracranial pressure, muscle hypertonicity. Disorders of the heart often: heart failure. Vascular disorders are common: increased blood pressure. Infrequently: venous thrombosis and / or thromboembolism. Respiratory, thoracic, and mediastinal disorders often: shortness of breath. Disorders of the gastrointestinal tract often: constipation. Infrequently: nausea, vomiting. Frequency unknown: pancreatitis. Liver and biliary tract disorders: Frequency unknown: hepatitis. Skin and subcutaneous tissue disorders Frequency unknown: thrombocytopenic purpura. Disorders of the genitourinary system Frequency not known: acute renal failure, cystitis, increased libido. Common disorders are often: fatigue, general weakness. Laboratory and instrumental data: Often: increased activity of liver enzymes. Frequency unknown: agranulocytosis, leukopenia (including neutropenia), pancytopenia, thrombocytopenia.

Interaction

Levodopa, dopamine receptor agonists, and m-holinoblockers. When memantine is co-administered with levodopa preparations, dopamine receptor antagonists, and m-holinoblockers, the effect of the latter may be enhanced, as with co-use with other NMDA receptor antagonists. Barbiturates and antipsychotics. When used concomitantly 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 dosage of drugs should be selected individually. Amantadine, ketamine, dextromethorphan. Concomitant use with amantadine, ketamine, phenytoin and dextromethorphan should be avoided?because of the increased risk of developing psychosis. These drugs are chemically bound NMDA receptor antagonists. Phenytoin. Co-use of memantine with phenytoin should be avoided. Cimetidine, ranitidine, procainamide, quinidine, quinine, nicotine. Plasma concentrations of cimetidine, ranitidine, procainamide, quinidine, quinine, and nicotine may increase when co-administered with memantine due to the use of the same renal cationic transport system. Hydrochlorothiazide. It is possible to reduce the concentration of hydrochlorothiazide or any combination with hydrochlorothiazide when taken simultaneously with memantine. Indirect anticoagulants. It is possible to increase the international normalized ratio (MHO) in patients taking indirect anticoagulants (warfarin). Although there is no causal relationship, careful monitoring of prothrombin time and INR is recommended in patients taking warfarin and memantine concomitantly. Antidepressants. Concomitant use with antidepressants, selective serotonin reuptake inhibitors, and monoamine oxidase inhibitors requires careful monitoring of patients. No interactions. In pharmacokinetic studies after a single dose of memantine, no interactions of memantine with glibenclamide, metformin, donepezil or galantamine were detected. Memantine does not inhibit the isoenzymes CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, CYP3A, flavin-containing monooxydase, epoxidhydrolase, or sulfation in vitro.

How to take it, course of use and dosage

Therapy should be conducted under the supervision of a doctor who has experience in the diagnosis and treatment of dementia in Alzheimer’s disease. Therapy should be initiated if the patient (or a person who constantly cares for the patient) is ready to regularly monitor the intake of the drug. The diagnosis should be made in accordance with the current guidelines. The tolerability and dose of Memantine Canon should be evaluated regularly, preferably within three months of starting therapy. Then, the clinical efficacy of the drug and the tolerability of therapy should be regularly evaluated in accordance with current clinical guidelines. Maintenance therapy can be continued indefinitely if there is a positive effect and the drug Memantine Canon is well tolerated.Discontinue the use of the drug if the positive therapeutic effect is no longer observed or if the patient does not tolerate therapy. The drug should be used orally, once a day, at the same time, without chewing, with a sufficient amount of liquid, regardless of food intake. The maximum daily dose is 20 mg. The dosage regimen is set individually. It is recommended to start treatment with the minimum effective dose. To reduce the risk of undesirable side effects, a constant dose is selected by increasing titration of 5 mg per week for the first three weeks according to the following scheme:Week 1 (days 1-7): 5 mg daily for seven days. Week 2 (days 8-14):  10 mg every day for seven days. Week 3 (days 15-21): 15 mg daily for seven days. Starting from the 4th week: 20 mg every day. Use in selected patient groups Elderly patients For patients over 65 years of age, the recommended dose is -20 mg per day. Patients with impaired renal function in patients with mild renal impairment (creatinine clearance 50-80 ml / min), no dose adjustment is required. In patients with moderate renal impairment (creatinine clearance 30-49 ml / min), the dose of the drug should be 10 mg per day. If this dose is well tolerated for at least 7 days of treatment, then it can be increased to 20 mg per day in accordance with the standard dosage regimen. In patients with severe renal impairment (creatinine clearance 5-29 ml / min), the dose of the drug should not exceed 10 mg per day. Patients with hepatic impairment Patients with mild or moderate hepatic impairment (Child-Pugh class A and B) do not need to adjust the dose. In patients with severe hepatic insufficiency (Child-Pugh class C), the use of Memantine Canon is contraindicated.

Overdose

Symptoms:In cases of overdose at a dose of less than 140 mg once or in the case of taking an unknown dose, patients experienced adverse reactions from the central nervous system: confusion, hypersomnia, drowsiness, dizziness, agitation, aggression, hallucinations, gait disorders; as well as gastrointestinal disorders: vomiting, diarrhea. With relatively large overdoses (200 mg once and 105 mg / day for 3 days), the following symptoms were observed: fatigue, weakness and/or diarrhea, or there were no symptoms. In the most severe case of overdose, the patient survived after taking a dose of 2000 mg of memantine, he had adverse reactions from the central nervous system (coma for 10 days, then diplopia and agitation). The patient received symptomatic treatment and plasmapheresis. The patient recovered without further complications. In another case of severe overdose, the patient survived and recovered after taking memantine 400 mg once. The patient experienced adverse reactions from the central nervous system: anxiety, psychosis, visual hallucinations, a decrease in the threshold of convulsive readiness, drowsiness, stupor and loss of consciousness. Treatment:There is no specific antidote for memantine intoxication. It is necessary to carry out standard measures aimed at removing the drug from the body: gastric lavage, taking activated charcoal, conducting forced diuresis, increasing the acidity of urine.

Special instructions

It is recommended to use with caution in patients with epilepsy, a history of seizures, or in patients with a predisposition to epilepsy. Memantine should be avoided along with other NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), as adverse reactions may occur more frequently and of greater intensity, mainly at the level of the central nervous system. The presence of factors affecting the increase in urine pH (sudden changes in diet, for example, switching from a diet that includes animal products to a vegetarian diet, or intensive consumption of alkaline gastric buffers), as well as renal tubular acidosis or severe urinary tract infections caused by Proteus spp., require careful monitoring of the patient’s condition. Patients with a history of myocardial infarction, decompensated chronic heart failure (NYHA functional class III-IV), or uncontrolled hypertension were excluded from most clinical trials. Therefore, data on the use of memantine in such patients are limited, and the drug should be taken under the careful supervision of a doctor. Effects on the ability to drive vehicles and engage in other potentially dangerous activities In patients with moderate to severe Alzheimer’s disease, the ability to drive vehicles and manage complex mechanisms is usually impaired. In addition, memantine can cause changes in the reaction rate, so patients should refrain from driving vehicles and working with complex mechanisms.

Composition

Tablet Form of production

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Memantine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Consequences of stroke, Alzheimer’s disease, Concussion and other traumatic brain injuries, Acquired dementia, Alcoholism