Maruxa coated pills 10mg N30
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Active ingredients
Memantine
Release form
Pills
Composition
The core of the active substance: rabeprazole sodium 10 mg (which corresponds to rabeprazole 9.42 mg) excipients: mannitol (E421) - 18.5 mg; magnesium oxide light - 30 mg; hyprolosis, 2.625 mg; low substituted hyprolosis - 12.75 mg; magnesium stearate - 1.125 mg shell (binding layer): ethyl cellulose - 0.44 mg; magnesium oxide light - 0.61 / mg shell (enteric): hypromellose phthalate - 6.3 mg; monoglycerides, diacetylated - 0.64 mg; talc - 0.59 mg; titanium dioxide (E171) - 0.32 mg; iron dye red oxide (E172) - 0,017 mg
Pharmacological effect
Nootropic, neurometabolic
Pharmacokinetics
Suction. Quickly and completely absorbed after ingestion. Tmax in blood plasma - 3–8 hours after ingestion. In patients with normal renal function, accumulation of memantine was not observed. Distribution. With a daily dose of 20 mg / day, Css 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. Vd is equal to 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 do not possess their own pharmacological activity. In vitro, metabolism carried out by cytochrome P450 isoenzymes was not detected. Inference. Excreted mono-exponentially. T1 / 2 of the terminal phase ranges from 60 to 100 hours. It is excreted by the kidneys. In volunteers with normal renal function, 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 may decrease by a factor of 7–9. Alkalization of urine can be caused by a drastic change in nutrition, 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 (ki), which for memantine is 0.5 μmol in the area of the frontal cortex of the brain
Indications
Dementia moderate to severe with Alzheimer's disease
Contraindications
Classification of the incidence of side effects WHO: very often - ≥1 / 10; often from ≥1 / 100 to <1/10; infrequently - from ≥1 / 1000 to <1/100; rarely from ≥1 / 10000 to <1/1000; very rarely - <1/10000; frequency unknown - cannot be estimated based on available data. In clinical studies, the overall incidence of adverse reactions did not differ when memantine and placebo were taken. They were generally mild to moderate in severity. The most frequent adverse reactions in the memantine group compared with placebo were: dizziness (6.3 versus 5.6%, respectively), headache (5.2 versus 3.9%), constipation (4.6 versus 2.6%) , drowsiness (3.4 versus 2.2%) and arterial hypertension (4.1 versus 2.8%). Side effects are classified by MedDRA. Infectious and parasitic diseases: rarely - fungal infections. On the part of the immune system: often - hypersensitivity to the components of the drug. Psychiatric disorders: often - drowsiness; infrequently - confusion, hallucinations *; frequency unknown - psychotic reactions. On the part of the nervous system: often - dizziness, imbalance; infrequently - gait disturbance; very rarely - seizures. From the side of the heart: infrequently - heart failure. On the part of the vessels: often - increased blood pressure; infrequently - venous thrombosis / thromboembolism. The respiratory system, organs of the chest and mediastinum: often - shortness of breath. On the part of the digestive tract: often - constipation; infrequently - nausea, vomiting; frequency is unknown - pancreatitis. On the part of the liver and biliary tract: often - increased activity of liver enzymes; frequency unknown - hepatitis. General disorders and disorders at the injection site: often - headache; infrequently - fatigue. * Hallucinations have been observed mainly in patients with Alzheimer's disease at the stage of severe dementia. In post-registration use, the following adverse reactions were reported: dizziness, drowsiness, irritability, fatigue, anxiety, increased ICP, nausea, hallucinations, headache, impaired consciousness, muscle tone,gait disturbance, depression, convulsions, psychotic reactions, suicidal thoughts, constipation, nausea, pancreatitis, candidiasis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism and allergic reactions.
Use during pregnancy and lactation
Due to the possible delay in intrauterine development, Maroux's drug is not used 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 Maruxa, breastfeeding should be stopped.
Dosage and administration
Inside, 1 time per day and always at the same time, regardless of the meal. 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. You should regularly assess the tolerability and dose of the drug Maruxa, preferably within 3 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 in the presence of a therapeutic effect and good tolerability of the drug Marux. The use of Maruxa should be discontinued if the therapeutic effect is no longer observed or the patient does not tolerate therapy. In order to reduce the risk of side effects, a gradual increase in the dose is recommended: 5 mg / week. during the first 3 weeks. therapy. The recommended maintenance dose is 20 mg / day. The following dosing regimen is recommended: 1st week. (1–7th day): daily dose - 5 mg (1⁄2 pills. Maroux 10 mg every day for 7 days); 2nd week (8–14th day): daily dose - 10 mg (1 tab. Maruxa 10 mg every day for 7 days); 3rd week (15–21st day): daily dose - 15 mg (11⁄2 pills. Maroux 10 mg every day for 7 days); Starting from the 4th week: daily dose - 20 mg (2 pills. Marux 10 mg each day).
Side effects
Classification of the incidence of side effects of the World Health Organization (WHO): very often> 1/10 often from> 1/100 to <1/10 rarely from> 1/1000 to <1/100 rarely from> 1/10000 to <1 / 1000 very rarely <1/10000 frequency unknown cannot be estimated based on available data. In clinical studies, the overall incidence of adverse reactions did not differ when memantine and placebo were taken. They were generally mild to moderate in severity. The most frequent adverse reactions in the memantine group compared with placebo were: dizziness (6.3% versus 5.6%, respectively), headache (5.2% versus 3.9%), constipation (4.6% versus 2 , 6%), drowsiness (3.4% versus 2.2%, respectively) and arterial hypertension (4.1% versus 2.8%, respectively). Infectious and parasitic diseases: rarely - fungal infections. Violations of the blood and lymphatic system: the frequency is unknown - agranulocytosis, leukopenia (including neutropenia), pancytopenia, thrombocytopenia, thrombocytopenic purpura. Immune system disorders: often - hypersensitivity to the components of the drug. Psychiatric disorders: often - drowsiness; infrequently - confusion, hallucinations; frequency unknown - psychotic reactions. Nervous system disorders: often - dizziness, imbalance; infrequently - gait disturbance; very rarely - seizures. Heart disorders: Infrequently - heart failure. Disturbances from vessels: often - increase in arterial pressure; infrequently - venous thrombosis / thromboembolism. Disturbances from the respiratory system, organs of the chest and mediastinum: often - shortness of breath. Disorders of the gastrointestinal tract: the frequency is unknown - pancreatitis. Disorders of the liver and biliary tract: often - increased activity of hepatic transaminases; frequency unknown - hepatitis. Kidney and urinary tract disorders: frequency unknown - acute renal failure. Violations of the skin and subcutaneous tissues: the frequency is unknown - Stevens-Johnson syndrome. General disorders and disorders at the injection site: often - headache; infrequently - fatigue. Hallucinations have been observed mainly in patients with Alzheimer's disease at the stage of severe dementia. In post-registration use of Maruxa, the following adverse reactions were reported: dizziness, drowsiness, anxiety, fatigue, anxiety, increased intracranial pressure, nausea, hallucinations, headache, impaired consciousness, muscle tone, impaired gait, depression, convulsions, psychotic reactions, suicidal thoughts, constipation, nausea, pancreatitis, candidiasis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism and allergies cal reactions.
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. The side reactions of the central nervous system are described: anxiety, psychosis, visual hallucinations, convulsive readiness, drowsiness, stupor and loss of consciousness. Treatment: symptomatic. The specific antidote of the drug does not exist. It is necessary to carry out standard therapeutic measures aimed at removing the active substance from the stomach, such as washing the stomach, taking activated carbon, acidifying the urine, it is possible to conduct 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. Perhaps an increase in MHO in patients simultaneously taking oral indirect anticoagulants (warfarin). It is recommended to regularly monitor the PV or MHO. Simultaneous use with antidepressants, SSRIs and MAO inhibitors requires careful monitoring of patients. No drug interaction was 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 CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A, monooxygenase containing flavin, epoxyhydrolase or sulfation.
special instructions
It is recommended to be used with caution in patients with epilepsy, history of convulsions, or with a predisposition to epilepsy. The simultaneous use of memantine and other NMDA receptor antagonists, 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) may 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 canalicular 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 myocardial infarction with a history of decompensated CHF (III – IV functional class according to the NYHA classification) 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. Influence on ability to drive vehicles and work with mechanisms. 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 can cause a change in the reaction rate, so patients should refrain from driving or working with complex mechanisms.