Noodgeron film-coated pills 10mg N30
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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 of the membrane: 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, accumulation of memantine is not 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 removed by the kidneys. Excretion. 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 in volunteers, pharmacokinetic linearity was revealed. 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 liver failure (class C on the Child-Pugh scale), pregnancy, breastfeeding, age up to 18 years (the efficacy and safety of the drug have not been established) .With caution: 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. Avoid the simultaneous use of memantine and antagonists of NMDA-receptors, such as amantadine, ketamine or dextromethorphan. 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 most clinical studies, patients with a history of myocardial infarction, decompensated CHF (III – IV functional class according to NYHA) or uncontrolled hypertension was excluded.Therefore, data on the use of memantine in these patients is limited, the drug should be taken under the close supervision of a physician. The effect on the ability to drive 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 tolerance and dose of Noodgeron 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. 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 tab. 10 mg) . Starting from the 4th week: daily dose - 20 mg (2 pills. 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. Violation of the liver.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 insufficiency (class C on the Child-Pugh scale) are not allowed to use Noodgeron.
Side effects
With simultaneous use with levodopa preparations, dopamine receptor antagonists, m-cholinoblockers, the action of the latter can be enhanced. When used simultaneously with barbiturates, neuroleptics, the action of the latter can be reduced. When used simultaneously, it can change (increase or decrease) the effect of dantrolene or baclofen, so the doses should be select individually. Concurrent administration with amantadine, ketamine, phenytoin, and dextromethorphan should be avoided due to an increased risk of psychosis. Plasma concentrations of cimetidine, ranitidine, procainamide, quinidine, quinine, and nicotine may be increased while co-administered with memantine. Concurrent administration of hydrochlorothiazide is possible. memantine. Perhaps an increase in MHO in patients taking oral anticoagulants (warfarin). Memantine may increase the excretion of hydrochlorothiazide. Simultaneous use with antidepressants, SSRIs and MAO inhibitors requires careful monitoring of patients. Memantine interacts with glibenclamide, metformin, and it will need to be monitored carefully for patients with glibenclamide, metformin, and it should be monitored for treatment of memantine with glibenclamide, metformin, and for example, if it is used to treat patients with oral antioxidants. 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 are not enough to assess the frequency of side effects. Infectious and parasitic diseases: infrequently - fungal infections. From the immune system: often - hypersensitivity to the components of the drug. Psychiatric disorders: often - drowsiness; infrequently - confusion, hallucinations *; unknown frequency - psychotic reactions. From the nervous system: often - dizziness, imbalance; infrequently - gait disturbance; very seldom - convulsions. From the heart: infrequently - heart failure. From the vessels: often - increase in blood pressure; infrequently - venous thrombosis and / or thromboembolism. On the side of the gastrointestinal tract: often - constipation; infrequently - vomiting,nausea; unknown frequency - pancreatitis. From the side of the liver and biliary ducts: often - elevated liver enzymes; unknown frequency — hepatitis. For the respiratory system, organs of the chest and mediastinum: often - shortness of breath. Common disorders and disorders at the injection site: often - headache; infrequently - fatigability. * Hallucinations were mainly observed in patients with Alzheimer's disease in the severe dementia stage. Stevens Johnson.
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.