Memantine Canon

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Memantine Canon: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Memantin-Canon

ATX code: N06DX01

Active ingredient: memantine (Memantin)

Producer: CJSC "Kanonfarma production" (Russia)

Description and photo update: 2019-08-07

Prices in pharmacies: from 450 rubles.

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Memantine Canon is a drug for the treatment of moderate to severe Alzheimer's dementia.

Release form and composition

Dosage form - film-coated tablets: round, biconvex, the color of the shell is white or almost white (dosage 5, 15 and 20 mg) or blue (dosage 10 mg); the color of the core in the cross section is almost white (in blisters made of printed aluminum lacquered foil and polyvinyl chloride film: dosage 5, 15, 20 mg - in a cardboard box 1, 3, 6 or 9 packs of 10 pcs. or 1-3 packs 30 pcs.; dosage 10 mg - in a cardboard box 1, 3, 6, 9, 10 or 12 packs of 10 pcs., or 3, 5 or 6 packs of 20 pcs., or 1-4 packs of 30 pcs..; a set of tablets with a dosage of 5, 10, 15 and 20 mg - in a pack of cardboard 4 packs (1 pack of tablets of each dosage) 7 pcs. (7 tablets 5 mg + 7 tablets 10 mg + 7 tablets 15 mg + 7 tablets of 20 mg. Each pack also contains instructions for using Memantine Canon).

1 film-coated tablet contains (for a dosage of 5/10/15/20 mg, respectively):

active substance: memantine hydrochloride - 5, 10, 15 or 20 mg;
additional components: colloidal silicon dioxide - 2/3 / 4.2 / 5.2 mg; lactose monohydrate - 61.6 / 136 / 130.3 / 161.1 mg; povidone K-30 - 3.6 / 6 / 7.5 / 9.4 mg; calcium hydrogen phosphate dihydrate - 24.3 / 50.4 / 45.5 / 55 mg; croscarmellose sodium - 2.8 / 3/6 / 7.5 mg; magnesium stearate - 0.7 / 1.6 / 1.5 / 1.8 mg;
film shell: Opadray [hydroxypropyl cellulose (hyprolose) - 1.012 5 / 2.025 / 2.025 / 2.7 mg; titanium dioxide - 0.375 / 0.698 4 / 0.75 / 1 mg; hydroxypropyl methylcellulose (hypromellose) - 1.012 5 / 2.025 / 2.025 / 2.7 mg; talc - 0.6 / 1.2 / 1.2 / 1.6 mg; additionally for a dosage of 10 mg: black iron oxide dye - 0.003 6 mg; brilliant blue - 0.048 mg] –3/6/9/8 mg.

Pharmacological properties

Pharmacodynamics

The active component of Memantine Canon is memantine, a potential-dependent non-competitive blocker of NMDA receptors with moderate affinity for them. The substance blocks the effects of glutamate, which can lead to neuronal dysfunction in a pathologically increased concentration.

Pharmacokinetics

The main pharmacokinetic characteristics of memantine:

absorption: memantine is rapidly and fully absorbed from the gastrointestinal tract (gastrointestinal tract), its absolute bioavailability is ~ 100%. The absorption of the substance does not depend on the time of the meal. T _Cmax (time to reach the maximum concentration in blood plasma) is 3–8 hours. In patients without renal impairment, accumulation of memantine is not observed;
distribution: a constant concentration of memantine in blood plasma in the range of 70-150 ng / ml (0.5-1 mmol) with large individual variations is maintained when taking 20 mg per day. V _d (volume of distribution) memantine - 10 l / kg. ~ 45% of the substance binds to blood plasma proteins;
metabolism: the amount of memantine excreted unchanged is ~ 80%. This process proceeds with the formation of pharmacologically inactive metabolites - N-3,5-dimethylgludantane, a mixture of isomers of 4- and 6-hydroxymemantine and 1-nitroso-3,5-dimethyl-adamantane. In vitro studies catalyzed by cytochrome P ₄₅₀ metabolism was not detected;
excretion: in studies in which patients took ¹⁴ C- labeled memantine orally, it was found that, on average, 84% of the oral dose taken was excreted within 20 days; moreover, most (over 99%) was excreted in the urine. Memantine is excreted from the body by the kidneys monoexponentially. T _1/2 (half-life) - from 60 to 100 hours. The total clearance in patients without pathologies of renal function is 170 ml / min / 1.73 m ², part of the total renal clearance is achieved through tubular secretion. Renal excretion also includes tubular reabsorption, possibly mediated by cationic transport proteins. Under conditions of an alkaline urine reaction, the rate of renal elimination of the active substance Memantine Canon can decrease by 7-9 times. It is possible that urine alkalization due to a sharp change in nutrition, for example, a transition to a vegetarian diet from a diet that includes products of animal origin, or due to the intensive use of alkaline gastric buffers.

Studies carried out with the help of volunteers have demonstrated the linearity of pharmacokinetics in the dose range from 10 to 40 mg.

The level of concentration in the cerebrospinal fluid corresponds to the value of the inhibition constant (Ki) when taking Memantine Canon at a daily dose of 20 mg, which for memantine is 0.5 μmol in the frontal cortex.

Indications for use

Memantine Canon is indicated for the treatment of moderate to severe Alzheimer's dementia.

Contraindications

Absolute:

severe liver failure (class C on the Child-Pugh scale);
lactose deficiency or glucose / galactose malabsorption syndrome, congenital galactose intolerance;
period of pregnancy and lactation;
age up to 18 years (there is no information on the effectiveness and safety of use);
hypersensitivity to the active substance or any other component of the drug.

Relative (use Memantine Canon tablets with caution):

epilepsy, a history of convulsive syndrome;
CHF (chronic heart failure) (NYHA classes III – IV);
uncontrolled arterial hypertension;
a history of myocardial infarction;
impaired renal / hepatic function;
factors that increase urine pH, such as heavy intake of alkaline gastric buffers, sudden diet changes (switching from meat to vegetarian), renal tubular acidosis, or severe urinary tract infections caused by Proteus spp.;
joint administration of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan).

Memantine Canon, instructions for use: method and dosage

Treatment with Memantine Canon is carried out under the supervision of a physician who is experienced in the diagnosis and treatment of dementia in patients with Alzheimer's disease.

It is recommended to start therapy only when the patient (or a person constantly caring for him) is ready to regularly monitor the intake of pills. The diagnosis should be made in accordance with current guidelines. It is necessary to constantly assess the tolerance of the drug and the effectiveness of the prescribed dose, preferably within 3 months after the start of treatment. After that, it is required to regularly evaluate the clinical efficacy of the drug and the tolerability of treatment in accordance with the current clinical guidelines. The duration of maintenance therapy is not limited in time, provided that Memantine Canon is well tolerated and has a positive effect. In the absence of the latter or if the patient is intolerant of therapy, it is necessary to interrupt taking the pills.

Memantine Canon is administered orally, at the same time, 1 pc. per day. The tablets are not chewed, washed down with a sufficient amount of liquid. Food intake does not affect the effectiveness of the drug. Maximum per day, you can take no more than 20 mg of memantine.

The doctor sets the dosage regimen individually. At the beginning of therapy, it is recommended to prescribe the minimum effective dose. To reduce the risk of undesirable side effects, a constant dose is selected by titration with an increase of 5 mg every 7 days for the first 3 weeks, according to the following scheme:

first week (days 1 to 7): 1 tablet 5 mg daily for a week;
second week (days 8 to 14): 1 tablet of 10 mg daily for a week;
third week (days 15 to 21): 1 tablet 15 mg daily for a week;
from the fourth week: 1 tablet of 20 mg daily.

Application of Memantine Canon in selected patient groups:

advanced age (over 65 years): the recommended daily dose is 20 mg;
renal dysfunction: mild disorders [creatinine clearance (CC) from 50 to 80 ml / min] - no dose adjustment is required; moderate disturbances (CC from 30 to 49 ml / min) - the daily dose of Memantine Canon is 10 mg (provided that it is well tolerated for at least a week of treatment, the daily dose can be increased to 20 mg in accordance with the standard dosing regimen); severe disorders (CC from 5 to 29 ml / min) - the daily dose of the drug should not exceed 10 mg;
liver disorders: with mild or moderate severity (classes A and B according to the Child-Pugh classification), dose adjustment is not required; in severe cases (class C on the Child - Pugh scale), Memantine Canon is prohibited.

Side effects

The incidence of adverse reactions is classified as follows: very often - ≥ 1/10 appointments (> 10%); often - from ≥ 1/100 to 1% and <10%); infrequently - from ≥ 1/1000 to 0.1% and <1%); rarely - from ≥ 1/10 000 to, 01% and <0.1%); extremely rare - <1/10 000 appointments (<0.01%); with an unknown frequency - it is impossible to establish the frequency of occurrence of adverse reactions from the available data.

The general profile of undesirable adverse reactions of Memantine Canon, data on which were obtained both in the course of planned studies and from spontaneous reports:

mental disorders: infrequently - confusion, hallucinations (observed mainly in patients with severe Alzheimer's disease); with an unknown frequency - psychotic reactions;
CNS (central nervous system): often - dizziness, headache, imbalance, drowsiness; infrequently - gait disturbance; extremely rare - epileptic seizures, convulsions;
CVS (cardiovascular system): often - increased blood pressure (blood pressure); infrequently - thromboembolism and / or venous thrombosis, heart failure, heart defects;
respiratory system, organs of the chest and mediastinum: often - shortness of breath;
immune system: often - hypersensitivity to the constituents of the drug;
skin and subcutaneous tissue: with an unknown frequency - Stevens-Johnson syndrome;
Gastrointestinal tract: often - constipation; infrequently - nausea / vomiting; with an unknown frequency - pancreatitis;
liver and biliary tract: often - violation of liver function tests; with an unknown frequency - hepatitis;
kidneys and urinary tract: with unknown frequency - acute renal failure;
hematopoietic organs: with an unknown frequency - leukopenia (including neutropenia), agranulocytosis, thrombocytopenia, thrombocytopenic purpura, pancytopenia;
parasitic diseases and infections: infrequently - fungal infections;
general disorders: infrequently - general weakness, fatigue.

In post-registration studies in patients with Alzheimer's disease, depression, thoughts of suicide and attempts to commit it were also recorded.

Overdose

With a single dose of Memantine Canon in a dose not exceeding 140 mg, or in the case of an unknown dose, the following side reactions were noted: from the central nervous system - hypersomnia, confusion, dizziness, drowsiness, agitation, aggression, gait disturbance, hallucinations; from the digestive tract - vomiting, diarrhea.

With a single dose of a large dose (200 mg) or taking 105 mg per day for 3 days, diarrhea, weakness, fatigue were noted. In some cases, no symptoms were observed.

A case of severe overdose was described (2000 mg of memantine was taken), when the patient developed side reactions from the central nervous system (for 10 days the patient was in a coma, then diplopia and agitation followed). As a therapy, symptomatic treatment and plasmapheresis were prescribed. The patient recovered completely, no further complications were observed.

In another case, a severe overdose of memantine was noted after a single dose of Memantine Canon at a dose of 400 mg. CNS side effects such as visual hallucinations, drowsiness, decreased seizure threshold, anxiety, psychosis, stupor, and loss of consciousness have been reported. The patient also survived and fully recovered.

For the treatment of an overdose, it is recommended to carry out standard measures to remove memantine from the body, namely: rinse the stomach, take activated charcoal, carry out forced diuresis and take measures to increase the acidity of urine.

There is no specific antidote.

special instructions

Patients with epilepsy or with a predisposition to it, as well as patients with a history of seizures, should be careful during therapy with Memantine Canon.

Since the simultaneous administration of memantine with other antagonists of NMDA receptors (amantadine, ketamine, dextromethorphan) can cause undesirable reactions more often, and they can be of greater intensity, mainly at the level of the central nervous system, their combined use should be avoided.

Careful monitoring of the patient's condition is required if he has factors that affect the increase in urine pH:

Sudden changes in nutrition (switching to a vegetarian diet from a diet that includes foods of animal origin, or intensive consumption of alkaline gastric buffers);
severe urinary tract infections caused by Proteus spp., renal tubular acidosis.

Since patients with decompensated CHF (classes III – IV according to the NYHA classification), a history of myocardial infarction or uncontrolled arterial hypertension did not participate in most of the clinical studies conducted, they have insufficient data on the use of memantine. In this regard, therapy with Memantine Canon in patients of this category should be carried out under the close supervision of a physician.

Influence on the ability to drive vehicles and complex mechanisms

Alzheimer's disease at the stage of moderate to severe dementia is often associated with impaired ability to drive vehicles and complex mechanisms. In addition, the use of Memantine Canon can influence the reaction rate. In this connection, such patients should refrain from driving and working with complex and moving mechanisms.

Application during pregnancy and lactation

Since there are no clinical data on the effects of memantine on the course of pregnancy, the use of Memantine Canon for women carrying a child is contraindicated. In the course of scientific studies carried out in animals, it was found that memantine can cause intrauterine growth retardation of the fetus when exposed to identical or slightly higher concentrations of the active substance in comparison with those in humans. The potential risk to humans is not known.

There is no information on the elimination of memantine in breast milk. It is assumed that, due to its lipophilic structure, memantine is able to penetrate into breast milk, and therefore it is contraindicated to take the drug for women who are breastfeeding. If the reception of Memantine Canon is justified by the patient's condition, breastfeeding should be discontinued.

Pediatric use

Children and adolescents under 18 years of age are prohibited from using Memantine Canon, since there is no reliable data on its efficacy and safety in the treatment of patients of this age category.

With impaired renal function

Patients with impaired renal function Memantine Canon should be taken with caution.

Correction of the daily dose depending on QC:

QC from 50 to 80 ml / min: dose adjustment is not required;
CC from 30 to 49 ml / min: the daily dose is reduced to 10 mg (provided that it is well tolerated during the week of therapy, it can be increased to 20 mg according to the standard dosing regimen);
CC from 5 to 29 ml / min: the daily dose is not more than 10 mg.

For violations of liver function

Patients with severe hepatic impairment (class C on the Child-Pugh scale) are not prescribed Memantine Canon tablets.

In case of mild and moderate liver dysfunctions, the drug is taken with caution. There is no need to adjust the dose.

Use in the elderly

For patients over 65 years of age, the recommended daily dose of Memantine Canon is 20 mg.

Drug interactions

levodopa, m-anticholinergic agents and dopamine receptor agonists: their effect can be enhanced, as when taken together with other NMDA receptor antagonists;
barbiturates and antipsychotics: their effect may be reduced;
anticonvulsants (dantrolene, baclofen): memantine influences their effectiveness (enhances or weakens), and therefore the doses of drugs are selected individually;
ketamine, amantadine, dextromethorphan (chemically related NMDA receptor antagonists): increased risk of psychosis;
phenytoin: combined use with memantine is not recommended;
ranitidine, cimetidine, quinidine, quinine, procainamide, nicotine: their concentration in plasma may increase, since these substances use the same renal cationic transport system as memantine;
hydrochlorothiazide (or any combination with hydrochlorothiazide): may decrease the concentration of hydrochlorothiazide;
indirect anticoagulants (warfarin): an increase in MHO (international normalized ratio) is possible. Although a causal relationship has not been identified, it is recommended to establish monitoring of prothrombin time and INR in patients who take memantine along with warfarin;
antidepressants, monoamine oxidase inhibitors and selective serotonin reuptake inhibitors: requires careful monitoring of the patient's condition;
glibenclamide, metformin, donepezil, galantamine: in pharmacokinetic studies with a single dose of memantine, no interactions were found.

According to the results of in vitro studies, memantine does not inhibit isoenzymes CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2E1, CYP3A, epoxide hydrolase, flavin-containing monoxidase and sulfation processes.

Analogs

The analogues of Memantine Canon are Akatinol Memantine, Alzeym, Maruksa, Memantal, Memantine, Memantine Sandoz, Memantin-Alvogen, Memantin-Richter, Memantin-TL, Memantinol, Memikar, Noodzheron, Noodzheron-Teva, Tingrex, etc.

Terms and conditions of storage

Store in the manufacturer's packaging, observing the temperature regime not exceeding 25 ºС.

Keep out of the reach of children.

Shelf life is 3 years. After the expiration date, it is prohibited to take the medicinal product.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Memantine Canon

Reviews of Memantine Canon indicate the effectiveness of the drug when used in patients with Alzheimer's disease. At the same time, the effectiveness of the remedy is not assessed by the patients themselves, but by the people caring for patients with this diagnosis. In the reviews it is noted that Memantine Canon has a good effect on the patient's condition with constant use: aggressiveness disappears, cases of psychosis decrease, and interest in life increases. Users also pay attention to the fact that this drug can only be purchased with a doctor's prescription.

The price of Memantine Canon in pharmacies

The price for Memantine Canon film-coated tablets is:

dosage of 10 mg: 552–793 rubles. (pack of 30), RUB 1349–1886 (90 pcs in the package);
dosage 15 mg: 750 rubles. (in the package 30 pcs.);
dosage 20 mg: 1586-1952 rubles. (30 pcs in the package), 4450–5598 rubles. (90 pcs in the package).

Memantine Canon: prices in online pharmacies

Drug name

Price

Pharmacy

Memantine Canon 10 mg film-coated tablets 30 pcs.

450 RUB

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Memantine Canon tablets p.p. 10mg 30 pcs.

576 r

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Memantine Canon 20 mg film-coated tablets 30 pcs.

956 r

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Memantine Canon 10 mg film-coated tablets 90 pcs.

1169 RUB

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Memantine Canon tablets p.p. 20mg 30 pcs.

1372 RUB

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Memantine Canon tablets p.p. 10mg 90 pcs.

1680 RUB

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Memantine Canon 20 mg film-coated tablets 90 pcs.

3430 RUB

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Memantine Canon tablets p.p. 20mg 90 pcs.

RUB 4936

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!