Maruxa pills 10mg №60

Active ingredient

Dosage Form: film coated tablets

The composition of 1 tablet

Core:

Active substance:

Memantine hydrochloride 10,00 mg

Excipients:

51.45 mg, microcrystalline cellulose 175.00 mg, colloidal silicon dioxide 2.50 mg, talc 9.80 mg, Magnesium stearate 1.25 mg

Shell film: methacrylic acid and ethyl acrylate copolymer (1: 1), 30% aqueous dispersion 0.60 mg, talc 0.27 mg, triacetin 0.12 mg, simethicone 0.01 mg 30% aqueous dispersion contains, in addition to methacrylic acid and ethyl acrylate copolymer, also sodium lauryl sulfate (0.7% calculated on the dry matter in suspension) and polysorbate-80 (2.3% calculated on the dry substance in suspension) as emulsifiers.

It is expressed as the mass of dry matter entering the 30% aqueous dispersion.

Indications for use

• Dementia is moderate to severe in Alzheimer's disease.

Contraindications

• Hypersensitivity to Memantine and other components of the drug.
• Severe hepatic impairment (Child-Pugh class C).

Pregnancy and breastfeeding period

• Age up to 18 years (efficacy and safety have not been established).
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome, because part of the drug Maruxa^® lactose is included.

With care: epilepsy, thyrotoxicosis, predisposition to the development of seizures; simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), urine pH-raising factors (abrupt diet change, for example, switching to vegetarianism, abundant intake of alkaline gastric buffers), renal tubular acidosis, severe urinary tract infections caused by Proteus spp., myocardial infarction (in history), heart failure III-IV functional class according to the NYHA classification, uncontrolled arterial hypertension, renal failure, liver failure.

Use during pregnancy and during breastfeeding

Due to the possible delay in intrauterine development, the drug Maruxa^® not applicable during pregnancy.

There is no information about the allocation of memantine with breast milk. However, given the lipophilicity of memantine, excretion is possible. Therefore, at the time of treatment with the drug Maruxa^® breastfeeding must stop.

Dosage and administration

Therapy should be carried out under the supervision of a physician with expertise in the diagnosis and treatment of dementia in Alzheimer's disease. Therapy should be initiated only if the person who regularly cares for the patient will monitor their drug intake. The diagnosis should be made in accordance with the current recommendations.

It is necessary to regularly assess the tolerability and dose of the drug Maruxa^®preferably within three months after initiation of therapy. Then you should regularly evaluate the clinical efficacy of the drug and the tolerability of therapy in accordance with the current clinical guidelines. Maintenance therapy can be continued indefinitely with a therapeutic effect and good tolerability of Maruxa^®. You should stop using the drug Maruxa^®if the therapeutic effect is no longer observed or if the patient does not tolerate therapy.

Inside, once a day and always at the same time, regardless of the meal.

In order to reduce the risk of side effects, a gradual increase in the dose is recommended: 5 mg per week during the first 3 weeks of therapy. The recommended maintenance dose is 20 mg per day.

The following dosing regimen is recommended:

1st week (1-7 day): daily dose - 5 mg (according to¹And Maroux tablets^® 10 mg every day for 7 days);

2nd week (8-14 day): daily dose - 10 mg (1 Marouks tablet^® 10 mg every day for 7 days);

3rd week (15-21 days): daily dose - 15 mg (according to VA Marux tablets^® 10 mg every day for 7 days);

Starting from the 4th week: daily dose - 20 mg (2 pills of Marux^® 10 mg every day). Elderly patients (over 65)

Dose adjustment is not required.

In patients with creatinine clearance (CK) 50-80 ml / min dose adjustment is not required. Patients with moderate renal insufficiency (CC 3049 ml / min) are recommended

10 mg / day.With good tolerability of the drug for 7 days, the dose can be increased to 20 mg / day according to the standard scheme. In patients with severe renal insufficiency (CC 5-29 ml / min), the daily dose should be 10 mg / day.

In patients with mild and moderate liver dysfunction (Grade A and B on the ChildPup scale), dose adjustment is not required.

Overdose

Symptoms: increased severity of side effects, such as: fatigue, weakness, diarrhea, confusion, drowsiness, dizziness, agitation, hallucinations, gait disturbance, nausea.

In the most severe case of overdose (2000 mg of memantine), the patient survived, with adverse reactions from the nervous system (coma for 10 days, then diplopia and agitation) were observed. The patient received symptomatic treatment and plasmapheresis. The patient recovered without further complications. In another case of severe overdose (400 mg), the patient also survived and recovered. Adverse reactions of the central nervous system are described: anxiety, psychosis, visual hallucinations, convulsive readiness, drowsiness, stupor and loss of consciousness.

Treatment:

In case of overdose, treatment is symptomatic. There is no specific antidote. It is necessary to carry out standard therapeutic measures aimed at removing the active substance from the stomach, for example, washing the stomach, taking activated charcoal, acidifying urine, and possibly conducting forced diuresis.

Interaction with other drugs

The effects of levodopa, dopamine receptor agonists and anticholinergic drugs are potentiated.

The effectiveness of barbiturates, antipsychotic (neuroleptics) drugs decreases with the simultaneous use of memantine.

The simultaneous use of memantine with dantrolene and Baclofen, as well as with antispasmodics may be accompanied by a change in their effect, which requires a dose adjustment of these drugs.

The simultaneous use of memantine and amantadine due to the risk of psychosis should be avoided. Memantine and amantadine belong to the group of NMDA receptor antagonists. The risk of developing psychosis is also increased with simultaneous use of memantine with phenytoin, ketamine and dextromethorphan.

With simultaneous use with cimetidine, Ranitidine, procainamide, quinidine, quinine and nicotine increases the risk of increasing the concentration of memantine in the blood plasma.

When taken simultaneously with hydrochlorothiazide, it is possible to decrease the concentration of hydrochlorothiazide in the blood plasma by increasing its elimination from the body. An increase in the International Normalized Relationship (INR) is possible in patients who are simultaneously taking oral indirect anticoagulants (warfarin). It is recommended to regularly monitor prothrombin time or INR. Simultaneous use with antidepressants, selective serotonin reuptake inhibitors and monoamine oxidase inhibitors requires careful monitoring of patients.

No drug interactions were observed with a single simultaneous use of memantine with glibenclamide / Metformin or donepezil in healthy volunteers.

When applied simultaneously with memantine, no change in the pharmacokinetics of galantamine in healthy volunteers was observed.

In vitro, memantine does not inhibit isoenzymes CYP 1A2, 2A6, 2C9, 2D6, 2E1, FOR, monooxygenase, containing flavin, epoxyhydrolase or sulfation.

special instructions

It is recommended to be used with caution in patients with epilepsy, a history of convulsions, or in patients with a predisposition to epilepsy.

The simultaneous use of memantine and antagonists of NMDA receptors, such as amantadine, ketamine or dextromethorphan, should be avoided. These compounds act on the same receptor system as memantine, therefore undesirable reactions (mainly associated with the central nervous system) can occur more often and be more pronounced.

The patient has factors that influence the increase in urine pH (abrupt changes in nutrition, such as switching from diets that include animal products, to a vegetarian diet, or intensive consumption of alkaline gastric buffers), as well as renal tubular acidosis or severe urinary tract infections Proteus spp., Require careful monitoring of the patient's condition.

From the majority of clinical studies, patients with a history of myocardial infarction, decompensated chronic heart failure (NYHA class III-IV functional class) or uncontrolled arterial hypertension were excluded.Therefore, data on the use of memantine in these patients is limited, the drug should be taken under the careful supervision of a physician.

Impact on the ability to perform potentially hazardous activities that require special attention and quick reactions (for example, driving, working with moving machinery)

In patients with Alzheimer's disease at the stage of moderate and severe dementia, the ability to drive vehicles and manage complex mechanisms is usually impaired. In addition, memantine may cause a change in the reaction rate, so patients should refrain from driving or working with complex mechanisms.

Pharmacological properties

Pharmacotherapeutic group: dementia remedy Code

Pharmacological properties

Pharmacodynamics

Derived adamantane. It is a noncompetitive antagonist of M-methyl-B-aspartate (YMBA) receptors, has a modulating effect on the glutamatergic system. It regulates the transport of ions, blocks Calcium channels, normalizes the membrane potential, improves the transmission of nerve impulses. Improves cognitive processes, increases daily activity.

Pharmacokinetics

Suction

Quickly and completely absorbed after ingestion. Maximum concentration in plasma (С_thatx) is achieved within 3-8 hours after ingestion. In patients with normal renal function, there is no accumulation of memantine.

Distribution

When taken daily at a dose of 20 mg per day, the equilibrium concentration of memantine in the blood plasma is 70-150 ng / ml. When using a daily dose of 5-30 mg, the ratio of the average concentration in the cerebrospinal fluid to the plasma concentration was calculated to be 0.52. The volume of distribution is about 10 l / kg. About 45% of memantine is bound to plasma proteins .

Metabolism

About 80% of ingested memantine is excreted unchanged. The major metabolites of N-3,5-dimethylgludantan, an isomeric mixture of 4- and 6-hydroxy-memantine and

1-nitroso-3-5-dimethyl-adamantane does not have its own pharmacological activity. In vitro metabolism carried out by cytochrome P450 isoenzymes was not detected. In the study by ingestion ¹⁴On average, C-memantine 84% of the ingested dose was eliminated within 20 days, with more than 99% eliminated by the kidneys.

Removal

Excreted mono-exponentially. Half-life (Tu₂a) the terminal phase is from 60 to 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 due to canalicular secretion. Renal excretion also includes tubular reabsorption, possibly mediated by cationic transport proteins. The rate of renal elimination of memantine in alkaline conditions of urine can be reduced by 7-9 times. Alkalization of urine can be caused by a drastic change in diet, for example, a transition from a diet that includes animal products to a vegetarian diet, or due to the intensive use of alkaline gastric buffers.

Linearity

Studies in volunteers showed pharmacokinetics linearity in the dose range of 10-40 mg.

Pharmacokinetic / pharmacodynamic dependence

When memantine is used in a dose of 20 mg / day, the concentration level in the cerebrospinal fluid corresponds to the inhibition constant (kj), which for memantine is 0.5 μmol in the region of the frontal cortex.

Storage conditions

At a temperature not higher than 25 ° С, in the original package.

Keep out of the reach of children.

Shelf life

Do not use the drug after the expiration date.

Vacation conditions

Prescription.