Composition, form of production and packaging
Tablets, film-coated 1 tab.
memantine hydrochloride 10 mg
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
The adamantane derivative, by chemical structure and pharmacological properties, is close to amantadine. It is a noncompetitive antagonist of N-methyl-D-aspartate (NMDA) -receptors (including in black matter), thereby reducing the excessive stimulating effect of cortical glutamate neurons on the neostriatum, which develops against a background of insufficient dopamine excretion. Reducing the intake of calcium ions in neurons, reduces the possibility of their destruction. Has nootropic, cerebrozodilating, antihypoxic and psychostimulating action. Mostly affects the stiffness (rigidity and bradykinesia). Improves weakened memory, concentration of attention, reduces fatigue and symptoms of depression.
PHARMACOKINETICS
Absorption
Memantine is quickly and completely absorbed from the digestive tract, has an absolute bioavailability of about 100%. Time to reach C max in blood plasma - 3-8 h.
Distribution
When taking a dose of 20 mg, the concentration of memantine in blood plasma is 70-150 ng / ml. V d is about 10 l / kg. Connection with blood plasma proteins - 45%.
Biotransformation
About 80% of memantine is in the form of the starting drug. The main metabolites in humans are N-3.5-dimethylgludantan, a mixture of isomers 4- and 6-hydroxymemanthine and 1-nitroso-3,5-dimethyl-adamantane. None of these metabolites has pharmacological activity.
Excretion
It is excreted by the kidneys. Elimination occurs single-phase, T 1/2 is 60-100 h; clearance is 170 ml / min / 173 m 2 , the drug is partially secreted by the renal tubules.With an alkaline reaction of urine, excretion of the drug slows down.
INDICATIONS
Dementia of moderate to severe severity in Alzheimer's disease.
DOSING MODE
Inside. During the meal. The dosage regimen is set individually. It is recommended to begin treatment with the appointment of minimally effective doses.
First week: daily dose - 5 mg (1/2 tablet in the morning);
Second week: daily dose - 10 mg (1/2 tablet 2 times a day);
The third week: a daily dose of 15 mg (1 tablet in the morning and 1/2 tablet in the evening);
Fourth week: daily dose - 20 mg (1 tablet 2 times a day);
The maximum daily dose is 20 mg per day.
Elderly patients (over 65 years of age): dose adjustment is not required.
Impaired renal function: if the kidney function is impaired, the dose of the drug should be reduced. In patients with a creatinine clearance (CK) of 50-80 ml / min, dose adjustment is not required. For patients with moderate renal failure (CK 30-49 ml / min) - 10 mg / day. With good tolerability of the drug for 7 weeks, the dose can be increased to 20 mg / day. by the standard scheme. In patients with severe renal failure (KK 5-29 ml / min), the use of the drug is not recommended due to insufficient data.
Dysfunction of the liver: in patients with mild and moderate liver disorders (class A and B according to the Child-Pugh classification), correction of the dosing regimen is not required.
SIDE EFFECT
Dizziness, drowsiness, increased excitability, increased fatigue, anxiety, increased intracranial pressure, nausea, hallucinations, headache, impaired consciousness, hypertonic muscle, gait disturbance, depression, convulsions, psychotic reactions, suicidal thoughts, constipation, nausea, pancreatitis, candidamycosis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism, allergic reactions.
CONTRAINDICATIONS
Hypersensitivity to any of the components of the drug, severe renal failure (CK 5-29 ml / min), severe hepatic insufficiency, congenital intolerance to galactose, lactase deficiency or glucose / galactose impaired glucose, pregnancy, lactation, children under 18 and security is not established).
Carefully. Epilepsy, thyrotoxicosis, a history of convulsive syndrome, simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan);factors that increase the pH of urine (a sudden change in diet, for example, the transition to vegetarianism, a copious intake of alkaline gastric buffers); severe urinary tract infections, myocardial infarction (history), heart failure (NYHA class III-IV functional class), uncontrolled arterial hypertension, renal failure, hepatic insufficiency.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure (KK 5-29 ml / min).
If the renal function is impaired, the dose of the drug should be reduced.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
Patients with mild to moderate liver disorders (class A and B according to the Child-Pugh classification) do not need to adjust the dosage regimen.
APPLICATION FOR CHILDREN
Contraindicated in children and podraskovom age under 18 years (efficacy and safety not established).
APPLICATION IN ELDERLY PATIENTS
In elderly patients (over 65 years), dose adjustment is not required.
SPECIAL INSTRUCTIONS
Memantine should be avoided together with other NMDA receptor antagonists (such as amantadine, ketamine, dextromethorphan), since adverse reactions may occur more often and more intensively, mainly at the CNS level.
Effect on ability to concentrate
Alzheimer's disease has a significant impact on the ability to drive vehicles and work with technical devices that require increased attention; In addition, memantine changes the speed of psychomotor reactions, in connection with which, it is necessary to refrain from driving vehicles and working with complex mechanisms.
OVERDOSE
Symptoms: dizziness, tremor, agitation, drowsiness, confusion, agitation, stupor, convulsions, psychosis, aggressiveness, hallucinations, gait unsteadiness, vomiting, diarrhea.
Treatment: in case of an overdose, treatment is symptomatic. There is no specific antidote. It is necessary to carry out standard medical measures aimed at removing the active substance from the stomach, for example, gastric lavage, taking activated charcoal, increasing the acidity of urine; it is possible to perform forced diuresis.
DRUG INTERACTION
It is possible to enhance the effects of memantine when used simultaneously with anticholinergic drugs, levodopa preparations, dopaminergic agonists (eg, bromocriptine). Joint use of memantine and amantadine should be avoided in connection with the risk of developing psychosis. Memantine and amantadine belong to the group of NMDA receptor antagonists. The risk of developing psychosis is also possible with the joint use of memantine with phenytoin, ketamine and dextromethorphan.
With simultaneous use with memantine, the effect of barbiturates and neuroleptics is reduced.
Simultaneous administration with antidepressants, selective serotonin reuptake inhibitors and monoamine oxidase inhibitors requires close monitoring of patients.
Simultaneous use of memantine with dantrolene and baclofen, as well as with spasmolytics may be accompanied by a change in their effect, which requires correction of the dose of these drugs.
When used simultaneously with cimetidine, ranitidine, procainamide, quinidine, quinine and nicotine, the risk of increasing memantine concentration in the blood plasma increases.
There are cases of increased MHO (international normalized ratio) in patients taking oral anticoagulants (warfarin) at the same time. It is recommended to monitor prothrombin time or MHO regularly. The excretion of hydrochlorothiazide can increase.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life - 2 years. Do not use the drug after the expiration date.
