Composition, form of production and packaging
A set of tablets (5 mg, 10 mg, 15 mg, 20 mg)
Tablets covered with a film shell from white to grayish-white, oval in shape, engraved "5" on one side and "MEM" on the other side.
1 tab.
memantine hydrochloride 5 mg
Excipients: microcrystalline cellulose - 65.875 mg, croscarmellose sodium - 3.375 mg, silicon dioxide colloid - 0.375 mg, magnesium stearate - 0.375 mg.
The composition of the shell: opadray white - 3 mg (hypromellose - 1.875 mg, titanium dioxide (E171) - 0.9375 mg, macrogol 400 - 0.1875 mg).
The tablets covered with a film membrane from white to grayish-white color, oblong form, biconcave, with a risk on each side.
1 tab.
memantine hydrochloride 10 mg
Excipients: lactose monohydrate - 174.75 mg, microcrystalline cellulose - 52.1 mg, silicon dioxide colloid - 1.25 mg, talc - 11.15 mg, magnesium stearate - 0.75 mg.
The composition of the shell: a copolymer of methacrylic acid and ethylcrylate (1: 1) - 1.449 mg, sodium lauryl sulfate - 0.01 mg, polysorbate 80 - 0.034 mg, triacetin 0.15 mg, simethicone emulsion 0.007 mg, talc 0.35 mg.
Tablets, covered with a film shell from beige to orange, oval; with engraving "15" on the one hand and "MEM" on the other hand.
1 tab.
memantine hydrochloride 15 mg
Excipients: microcrystalline cellulose - 197.625 mg, croscarmellose sodium - 10.125 mg, silicon dioxide colloid - 1.125 mg, magnesium stearate - 1.125 mg.
The composition of the shell: opadray orange - 9 mg (hypromellose - 5.625 mg, titanium dioxide (E171) - 2.2275 mg, macrogol 400 - 0.5625 mg, iron oxide yellow (E172) - 0.549 mg iron oxide red (E172) - 0.036 mg).
Tablets covered with a film membrane from pink to light brown in color, oval in shape; with engraving "20" on the one hand and "MEM" on the other side.
1 tab.
memantine hydrochloride 20 mg
Excipients: microcrystalline cellulose - 263.5 mg, croscarmellose sodium - 13.5 mg, silicon dioxide colloid - 1.5 mg, magnesium stearate - 1.5.
The composition of the shell: opadray pink - 12 mg (hypromellose - 7.5 mg, titanium dioxide (E171) - 3.3984 mg, macrogol 400 - 0.75 mg, iron oxide red (E172) - 0.1512 mg iron oxide yellow (E172) - 0.2004 mg).
7 pcs. - Blisters (4) with each dosage - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
The adamantane derivative. Being a non-competitive agent of N-Menm-D-acnapra (NMDA) -receptors, it has a modulating effect on the glutamatergic system. It regulates ion transport, blocks calcium channels, normalizes membrane potential, improves the process of nerve impulse transmission. Improves cognitive processes, increases daily activity.
PHARMACOKINETICS
After oral administration, it is quickly and completely absorbed. C max in blood plasma is achieved within 3-8 hours. With normal renal function cumulation memantine is not observed. Distribution: daily doses of 20 mg / day lead to a stable concentration of memantine in plasma 70 -150 ng / ml.
Metabolism
About 80% of memantine is excreted unchanged. In experiments in vitro metabolism, carried out by cytochrome P450, was not revealed. Metabolites do not have their own pharmacological activity. It is excreted from the body monoexponentially, with T 1/2 terminal phase 60-100 h. It is excreted in the urine. With an alkaline urine reaction, excretion slows down,
INDICATIONS
- dementia of moderate to severe severity in Alzheimer's disease.
DOSING MODE
The drug should be taken orally 1 time / day and always at the same time. Can be taken regardless of food intake.
Assign:
- Week 1 (days 1-7): 1 tablet with a dosage of 5 mg every day for seven days;
- 2nd week (days 8-14): 1 tablet with a dosage of 10 mg every day for seven days;
- Week 3 (days 15-21): 1 tablet with a dosage of 15 mg every day for seven days.
Starting with the 4th week: one tablet with a dosage of 20 mg every day.
SIDE EFFECT
Adverse reactions are classified according to the clinical manifestations (according to the damage of certain organ systems) and the frequency of occurrence: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to < 1/100), rarely (> 1/10000 to <1/1000), very rarely (<1/10000), the frequency is not established (there is currently no data on the incidence of adverse reactions).
From the body as a whole - general adverse reactions Often Infrequent Headache Fatigability
Immune system Often Hypersensitivity to drug components
Infections Rarely Fungal infections
Mental disturbances Often Infrequent infrequently Frequency not established Drowsiness Confusion of consciousness Hallucinations * Psychotic reactions
Cardiovascular Disorders Often Infrequent Infrequently Increased Blood Pressure Venous Thrombosis / Thromboembolism Heart Failure
Respiratory system Often Shortness of breath
Gastrointestinal disorders Often infrequent Frequency not established Constipation Nausea, vomiting Pancreatitis
Disturbances from the central and peripheral nervous system Often Infrequently Very rarely Dizziness Disturbance of gait Cramps
* Hallucinations were observed, mainly, in patients with Alzheimer's disease at the stage of severe dementia.
There are some reports of these adverse reactions in the use of the drug in clinical practice (data obtained after the appearance of the drug on sale): dizziness, drowsiness, increased excitability, increased fatigue, anxiety, increased intracranial pressure, nausea, hallucinations, headache, impaired consciousness , muscle hypertension, gait disorders, depression, seizures, psychotic reactions, suicidal thoughts, constipation, nausea, pancreatitis, candidiasis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism, allergic reactions.
CONTRAINDICATIONS
hypersensitivity to the drug;
- severe renal failure (QA 5-29 ml / min);
severe hepatic impairment;
- Pregnancy;
- the period of breastfeeding;
- age under 18 years (due to insufficient data).
With caution appoint a patient with thyrotoxicosis, epilepsy; predisposition to the development of seizures, the simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), the presence of factors that increase the pH of the urine (a dramatic diet change, for example, the transition to vegetarianism, a copious intake of alkaline buffer solutions), severe urinary tract infections (caused by Proteus bacteria), myocardial infarction (history), heart failure III-IV functional class (according to NYHA classification), uncontrolled arterial hypertension, renal insufficiency, hepatic insufficiency.
PREGNANCY AND LACTATION
It is forbidden to use the drug during pregnancy and during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution in case of moderate renal insufficiency.
It is forbidden to use the drug in severe kidney failure (QA 5-29 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution in moderate hepatic impairment.
Prohibited the use of the drug in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in patients under the age of 18 years.
SPECIAL INSTRUCTIONS
In patients with Alzheimer's disease, the ability to drive vehicles and manage complex mechanisms is usually impaired in the stage of moderate and severe dementia.In addition, memantine can cause a change in the reaction rate, so patients need to refrain from managing motor vehicles or working with complex mechanisms.
OVERDOSE
Symptoms: increased severity of side effects, such as: fatigue, weakness, diarrhea, confusion, drowsiness, dizziness, agitation, hallucinations, gait disturbance, nausea.
In the worst case of overdose (2000 mg memantine), the patient survived, with adverse reactions from the nervous system (coma 10 days, then diplopia and agitation). The patient received symptomatic treatment and nlazmopheresis. The patient recovered without further complications.
Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy, urine acidification, forced diuresis.
DRUG INTERACTION
With the simultaneous use with preparations of levodopa, dopamine receptor antagonists, m-cholinoblocators, the effect of the latter can be enhanced.
With simultaneous use with barbiturates, neuroleptics, the effect of the latter may decrease.
When combined, the effect of dantrolene or baclofen can be altered (enhanced or decreased), so the doses of the drugs should be selected individually.
Simultaneous application with amantadine, ketamine, phenytoin and dextromethorphan should be avoided because of the increased risk of developing psychosis.
Possible increase in plasma concentrations of cimetidine, ranitidine, procainamide, quinidine, quinine and nicotine while taking with memantine.
It is possible to reduce the concentration of hydrochlorothiazide when taken concomitantly with memantine.
Possible an increase in MHO in patients taking indirect anticoagulants (warfarin).
Memantium can increase the excretion of hydrochlorothiazide.
Simultaneous use with antidepressants, selective serotonin reuptake inhibitors and monoamine oxidase inhibitors requires close monitoring of patients.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 4 years. Do not use after the expiration date.
