Noodgeron film-coated pills 10mg N60
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Active ingredients
Memantine
Release form
Pills
Composition
Film-coated pills, composition (1 tab.): Active substance: memantine hydrochloride - 10 mg; (equivalent to 8.31 mg of memantine); excipients: MCC - 136.8 mg; calcium phosphate - 84.5 mg; croscarmellose sodium - 4.8 mg; colloidal silicon dioxide - 1.5 mg; magnesium stearate - 2.4 mg; film cover: Opadry II gray 45F27505 (hypromellose 2910/15 cP - 2.5 mg, polydextrose - 2.5 mg, titanium dioxide - 2.48 mg, macrogol / macrogol 4000 - 0.5 mg, iron dye black oxide - 0 , 02 mg) - 8 mg
Pharmacological effect
nootropic, psychometabolic
Pharmacokinetics
Suction. Eating does not affect the absorption of memantine. After ingestion, memantine is rapidly and completely absorbed. Cmax in plasma is from 3 to 8 hours after ingestion. In patients with normal renal function, no accumulation of memantine was observed .; Distribution. With a daily dose of 20 mg / day, Css memantine in the blood plasma is 70–150 ng / ml. The ratio of the average concentration of memantine in the cerebrospinal fluid to plasma concentration when used in a daily dose of 5-30 mg is 0.52. Vd is about 10 l / kg. Approximately 45% of memantine is bound to plasma proteins .; Metabolism. About 80% of ingested memantine is excreted unchanged. The main metabolites: N-3,5-dimethylgludantan, isomeric mixture of 4- and 6-hydroxymemantin and 1-nitroso-3,5-dimethyladamantane do not have their own pharmacological activity. In vitro metabolism carried out by cytochrome P450 isoenzymes was not detected. In the study with the ingestion of 14C-memantine, an average of 84% of the dose ingested was taken for 20 days, with more than 99% being excreted by the kidneys .; Inference. Memantine is displayed monoexponentially with T1 / 2 of the terminal phase is 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, when switching from animal products to a vegetarian diet or due to excessive use of alkaline gastric buffers .; Linearity.In the dose range of 10–40 mg, volunteers showed pharmacokinetic linearity .; Pharmacokinetic / pharmacodynamic relationship. When memantine is taken in a dose of 20 mg / day, the concentration level in the cerebrospinal fluid is equal to the value of ki (inhibition constant), which in the area of the frontal cerebral cortex is 0.5 μmol / l.
Indications
Dementia of Alzheimer's type of moderate and severe.
Contraindications
hypersensitivity to memantine and other components of the drug; ; severe hepatic impairment (Child-Pugh class C); ;pregnancy; ;breast-feeding; ; age up to 18 years (efficacy and safety of the drug have not been established) .; With care: epilepsy; thyrotoxicosis; predisposition to the development of seizures; simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan); factors that increase the pH of urine (abrupt change of diet, for example, the transition to a vegetarian, abundant intake of alkaline gastric buffers); renal tubular acidosis; severe urinary tract infections caused by Proteus spp., myocardial infarction (history), heart failure of the III – IV functional class according to NYHA classification, uncontrolled arterial hypertension, renal failure, hepatic failure.
Use during pregnancy and lactation
It is recommended to be used with caution in patients with epilepsy, 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) 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. Patients with Alzheimer's disease at the stage of moderate or severe dementia usually have impaired ability to drive vehicles and control complex mechanisms. In addition, memantine can cause a change in the reaction rate, so patients should refrain from driving or working with complex mechanisms.
Dosage and administration
Inside, regardless of the meal, 1 time per day, at the same time every day .; The tolerability and dose of Noodzheron should be regularly assessed, mainly within 3 months after the start 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 Noodgeron. Noodzheron should be discontinued if the therapeutic effect is no longer observed or the patient does not tolerate treatment .; 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 of therapy .; The maximum daily dose is 20 mg / day. The recommended maintenance dose of Noodzheron is 20 mg / day; The following dosing regimen is recommended: 1st week (1st-7th day): daily dose - 5 mg (1/2 table. 10 mg) .; 2nd week (8–14th day): daily dose - 10 mg (1 tab. 10 mg) .; 3rd week (15–21st day): daily dose - 15 mg (1.5 pills. 10 mg) .; Starting from the 4th week: daily dose - 20 mg (2 tab. 10 mg) .; Elderly patients (over 65). Dose adjustment is not required .; Impaired renal function. Patients with Cl creatinine 50–80 ml / min dose adjustment is not required. Patients with moderate renal insufficiency (Cl creatinine 30–49 ml / min) 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 (Cl creatinine 5–29 ml / min), the daily dose should not exceed 10 mg / day; Liver dysfunction.In patients with mild and moderate liver dysfunction (class A and B on the Child-Pugh scale) dose adjustment is not required .; Patients with severe hepatic impairment (class C on the Child-Pugh scale) drug Noodzheron contraindicated.
Side effects
With simultaneous use with levodopa preparations, dopamine receptor antagonists, m-cholinoblockers, the effects of the latter can be enhanced. With simultaneous use with barbiturates, neuroleptics, the effect of the latter may be reduced .; With simultaneous use, it can change (strengthen or reduce) the effect of dantrolene or baclofen, so the doses of drugs should be selected individually. Concurrent administration with amantadine, ketamine, phenytoin and dextromethorphan should be avoided due to the increased risk of developing psychosis .; Possible increase in plasma concentrations of cimetidine, ranitidine, procainamide, quinidine, quinine and nicotine while taking with memantine .; May decrease the level of hydrochlorothiazide while taking with memantine. Perhaps an increase in MHO in patients taking oral anticoagulants (warfarin) .; Memantine may increase the excretion of hydrochlorothiazide .; Concurrent use with antidepressants, SSRIs and MAO inhibitors requires careful monitoring of patients .; Pharmacokinetic interaction of memantine with glibenclamide, metformin, donepezil, galantamine is absent. In vitro, memantine does not inhibit isoenzymes CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A, flavin-containing monoxidase, epoxyhydrolase, or sulfation.
Overdose
Adverse effects are classified according to the frequency of their development: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), unknown frequency - the available data is not enough to estimate the frequency of side effects .; Infectious and parasitic diseases: infrequently - fungal infections .; On the part of the immune system: often - hypersensitivity to the components of the drug .; Psychiatric disorders: often - drowsiness; infrequently - confusion, hallucinations *; unknown frequency - psychotic reactions .; On the part of the nervous system: often - dizziness, imbalance; infrequently - gait disturbance; seizures very rarely .; Heart part: Infrequent - heart failure .; On the part of the vessels: often - increased blood pressure; infrequently - venous thrombosis and / or thromboembolism .; On the part of the digestive tract: often - constipation; infrequently - vomiting,nausea; unknown frequency - pancreatitis .; On the part of the liver and biliary tract: often - elevated liver enzymes; unknown frequency - hepatitis .; The respiratory system, organs of the chest and mediastinum: often - shortness of breath .; General disorders and disorders at the injection site: often - headache; infrequently - fatigue .; * Hallucinations were mainly observed in patients with Alzheimer's disease at the stage of severe dementia .; In the post-marketing period, the following adverse reactions were reported: agranulocytosis, leukopenia (including neutropenia), pancytopenia, thrombocytopenia, thrombocytopenic purpura, hepatitis, acute renal failure, Stevens-Johnson syndrome.
Interaction with other drugs
Precautionary measures
special instructions
Symptoms: with relatively large overdose (200 mg once and 105 mg / day for 3 days) - fatigue, weakness and / or diarrhea or symptoms were absent. In the case of overdose in a dose of 140 mg once or receiving an unknown dose, the patients had adverse reactions from the central nervous system: confusion, hypersomnia, drowsiness, dizziness, agitation, aggression, hallucinations, gait disturbance and / or from the digestive system: vomiting, diarrhea ; 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 therapy. You should use the standard therapeutic measures to remove the active substance from the stomach, such as washing the stomach, taking activated carbon, acidifying the urine, it is possible to conduct forced diuresis. There is no specific antidote.