Alzheim - instructions for use, doses, side effects, contraindications

Composition of the tablet shell: opada white II YS-30-18056 - 9.0 mg (lactose monohydrate - 40%, hydroxypropylmethylcellulose (hypromellose) - 40%, titanium dioxide - 10%, triacetin - 10%); opadray the transparent II YS-19-19054 1.0 mg (hydroxypropylmethylcellulose (hypromellose) 63%, maltodextrin 27%, triacetin 10%).

Description:

White, round, biconvex tablets, film-coated, with a risk, with the company logo on one side and engraved LUC another.

Pharmacotherapeutic group:Dementia remedy

ATX: & nbsp

N.06.D.X.01 Memantine

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

Pharmacodynamics:

The adamantane derivative, by chemical structure and pharmacological properties, is close to amantadine. Is a non-competitive antagonist Nmethyl-D-aspartate (NMDA) -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 isolation of dopamine. 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 quickly and completely absorbed from the digestive tract, has an absolute bioavailability of about 100%. Time to reach the maximum concentration in the blood plasma (TC_max) - 3-8 hours.

Distribution: when taking a dose of 20 mg, the concentration of memantine in blood plasma is 70-150 ng / ml. The distribution volume 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 of 4- and 6-hydroxymemanthine and 1-nitroso-3,5-dimethyl-adamantane. None of these metabolites has pharmacological activity.

Excretion: is excreted by the kidneys. Elimination occurs single-phase, half-life (T_1/2) is 60-100 hours; clearance is 170 ml / min / 173 m², 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.

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 absorption syndrome, pregnancy, lactation, children under 18 years of age and security is not established).

Carefully:

Epilepsy, thyrotoxicosis, a history of convulsive syndrome, simultaneous use of antagonists NMDA-receptors (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 (III-IV functional class by classification NYHA), uncontrolled arterial hypertension, renal insufficiency, hepatic insufficiency.

Dosing and Administration:

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 of 5 mg (1/2 tablets in the morning);

Second week: daily dose - 10 mg (by 1/2 tablets 2 times a day);

Third week: daily dose of 15 mg (1 tablet in the morning and 1/2 tablets 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): correction of the dose is not required.

Impaired renal function: if the renal function is impaired, the dose of the drug should be reduced. In patients with 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 in a standard manner. In patients with severe renal failure (KK 5-29 ml / min), the use of the drug is not recommended due to insufficient data.

Impaired liver function: in patients with mild and moderate hepatic impairment (class A and B according to the Child-Pugh classification), dosage adjustment is not required.

Side effects:

Dizziness, drowsiness, increased excitability, increased fatigue, anxiety, increased intracranial pressure, nausea, hallucinations, headache, impaired consciousness, hypertonic muscle, gait disturbance, depression, seizures, psychotic reactions, suicidal thoughts, constipation, nausea, pancreatitis, candidamycosis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism, allergic reactions.

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.

Interaction:

It is possible to enhance the effects of memantine when used simultaneously with anticholinergic drugs, levodopa preparations, dopaminergic agonists (for example, 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 antagonists NMDAreceptors. 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 an increase in INR (an international normalized ratio) in patients simultaneously taking oral anticoagulants (warfarin). It is recommended that prothrombin time or INR is monitored regularly.

The excretion of hydrochlorothiazide can increase.

Special instructions:

Memantine should be avoided together with other receptor antagonists NMDA (such as amantadine, ketamine, dextromethorphan), since adverse reactions may occur more often and more intensively, mainly at the CNS level.

Effect on the ability to drive transp. cf. and fur:

Alzheimer's disease has a significant impact on the ability to drive vehicles and work with technical devices that require increased attention; Besides, memantine changes the speed of psychomotor reactions, so you should refrain from driving vehicles and working with complex mechanisms.

Form release / dosage:Tablets, film-coated, 10 mg.

Packaging:

For 15 tablets in a blister of PVC / PVDC and foil aluminum.

For 2 or 4 blisters together with instructions for medical use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000295

Date of registration:17.02.2011

Expiration Date:17.02.2016

The owner of the registration certificate: Laboratorios Bago S.A. Laboratorios Bago S.A. Argentina

Manufacturer: & nbsp

Laboratorios BAGO, S.A. Argentina

Representation: & nbspBBC FARMA BV BBC FARMA BV Netherlands

Information update date: & nbsp06.07.2017

Illustrated instructions

Instructions

Alzheim (Alzeim)