5 mg tablet 10 mg tablet 7-14-21-28 mg cap,sprinkle,ER 24hr dose pack 2 mg/mL solution
Trade names in Russia
Akatinol Memantine, Noodzheron, Maruxa, Memantinol, Memantal, Memantine, Memantine Canon, Memaneurin, Memantine-Richter, Memantine hydrochloride, Memikar, Alzeim, Memantine-TL
Release form
- Tablets: 10 mg, 20 mg
- Oral drops 10 mg/ml
- Oral dispersible tablets: 10 mg, 20 mg
Indications
◊ Recommendations of the Russian Ministry of Health
F00.0 Dementia in early onset Alzheimer's disease
F00.1 Late-onset dementia in Alzheimer's disease
F00.2 Dementia in Alzheimer's disease, atypical or mixed type
F00.9 Dementia in Alzheimer's disease, unspecified
◊ FDA recommendations
G.30 Alzheimer's disease
◊ EMA recommendations
G.30 Alzheimer's disease
◊ Using Off-label
- Vascular dementia
- Dementia with Lewy bodies
- Frontotemporal dementia
- HIV-associated dementia
- Multiple sclerosis
Mechanism of action and pharmacokinetics
Memantine acts as a non-competitive antagonist of NMDA receptors, preferentially binding to cation channels gated by NMDA receptors. Long-term increases in glutamate levels in the brains of patients with dementia counteract the voltage-gated block of NMDA receptors by Mg2+ ions and promote a continuous influx of Ca2+ ions into cells, which ultimately leads to neuronal degeneration. Studies show that memantine binds to NMDA receptors more effectively than Mg2+ ions, and thereby effectively blocks the long-term influx of Ca2+ ions through the NMDA channel, maintaining transient physiological activation of the channels with higher concentrations of glutamate released into the synapses. Thus, memantine protects against chronically elevated glutamate concentrations. Memantine also exhibits serotonin (5-HT3) receptor antagonistic activity with potential similar to that of the NMDA receptor, and reduced nicotinic acetylcholine receptor antagonistic activity. This drug does not bind to γ-aminobutyric acid (GABA), benzodiazepine, dopamine, adrenergic, histamine, glycine, or voltage-gated calcium, sodium, or potassium receptors.
- Little metabolized;
- It is excreted almost unchanged in the urine;
- The half-life is approximately 60-100 hours; peak plasma concentrations after 3-7 hours [3].
- Minimal inhibition of CYP450 enzymes.
Akatinol Memantine (tab.p.pl/vol.20mg No. 98)
A country
Germany
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Memantine
Compound
1 film-coated tablet contains Active substance: memantine hydrochloride 20 mg Excipients: Microcrystalline cellulose: 263.5 mg Croscarmellose sodium: 13.5 mg Colloidal silicon dioxide: 1.5 mg Magnesium stearate: 1.5 mg Coating: Opadry pink: 12 mg consisting of: - Hypromellose: 7.5 mg - Titanium dioxide E171: 3.3984 mg - Macrogol 400: 0.75 mg - Red iron oxide E172: 0.2004 mg - Yellow iron oxide E172: 0.1512 mg Description Pink to light brown, oval-shaped tablets engraved with “20” on one side and “MEM” on the other side and film-coated. Release form: Film-coated tablets, 20 mg. 14 tablets with a dosage of 20 mg in a blister made of polyvinyl chloride film and aluminum foil. 2, 4 or 7 blisters along with instructions for use are placed in a cardboard box.
Pharmacological properties
Pharmacodynamics: Adamantane derivative. Being a non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors, it reduces the excessive stimulatory effect of cortical glutamate neurons on the neostriatum. 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. The maximum concentration in blood plasma is achieved within 2-6 hours. With normal renal function, no accumulation of the drug was observed. Excretion occurs in two phases. The half-life is 4-9 hours in the first phase, 40-65 hours in the second phase. About 80% of memantine is excreted unchanged. Metabolites do not have their own pharmacological activity. Excreted in urine. When urine is alkaline, excretion slows down.
Indications for use
Moderate to severe dementia in Alzheimer's disease.
Contraindications
Individual hypersensitivity to the drug, severe renal failure (creatinine clearance 5-29 ml/min), severe liver failure, pregnancy, breastfeeding, children under 18 years of age (due to insufficient data). With caution Prescribe with caution to patients with thyrotoxicosis, epilepsy, convulsions (including a history), simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), the presence of factors that increase urine pH (sudden change of diet, for example, switching to vegetarianism, heavy intake alkaline gastric buffers), severe urinary tract infections, myocardial infarction (history), heart failure functional class III-IV (NYHA classification), uncontrolled arterial hypertension, renal failure, liver failure.
Mode of application
The drug should be taken orally once a day and always at the same time, regardless of meals. Prescribed during the 1st week of therapy (days 1-7) at a dose of 5 mg/day, during the 2nd week (days 8-14) at a dose of 10 mg/day, during the 3rd week (days 15 -21) - at a dose of 15 mg/day, during the 4th week (days 22-28) - at a dose of 20 mg/day. The maximum daily dose is 20 mg. In patients over 65 years of age, as well as patients with a creatinine clearance of 50-80 ml/min, no dose adjustment is required. For patients with moderate renal failure (creatinine clearance 30-49 ml/min), the daily dose is 10 mg. Subsequently, if the drug is well tolerated for 7 weeks, the dose can be increased to 20 mg according to the standard regimen.
Side effect
Adverse reactions are classified according to clinical manifestations (according to damage to certain organ systems) and frequency of occurrence: very often (≥ 1/10), often (≥ 1/100 to From the body as a whole - general adverse reactions Often Headache Rarely Fatigue Infections Rarely Fungal infections Mental disorders Often Drowsiness Rarely Confusion Rarely Hallucinations* Frequency not established Psychotic reactions Cardiovascular system disorders Rare Increased blood pressure Rarely Venous thrombosis/thromboembolism Gastrointestinal disorders Common Constipation Rarely Nausea, vomiting Frequency not established Pancreatitis Disorders from the central and peripheral nervous system Often Dizziness Rarely Gait disturbance Very rarely Seizures *Hallucinations have been observed mainly in patients with Alzheimer's disease at the stage of severe dementia.There are isolated reports of the occurrence of these adverse reactions when using the drug in clinical practice (data obtained after the drug went on sale): Dizziness, drowsiness, increased excitability, increased fatigue, anxiety, increased intracranial pressure, nausea, hallucinations, headache, impaired consciousness, muscle hypertonicity, gait disturbances, depression, convulsions, psychotic reactions, suicidal thoughts, constipation , nausea, pancreatitis, candidiasis, increased blood pressure, vomiting, cystitis, increased libido, venous thrombosis, thromboembolism, allergic reactions.
Overdose
Symptoms: dizziness, tremor, agitation, drowsiness, confusion, agitation, stupor, convulsions, psychosis, aggressiveness, hallucinations, unsteadiness of gait, vomiting, diarrhea. Treatment: gastric lavage, taking activated carbon, symptomatic therapy. There is no specific antidote.
Interaction
When used simultaneously with levodopa drugs, dopamine receptor antagonists, and m-anticholinergic blockers, the effect of the latter may be enhanced. When used simultaneously with barbiturates and neuroleptics, the effect of the latter may decrease. When used together, it may change (increase or decrease) the effect of dantrolene or baclofen, so the doses of the drugs should be selected individually. Concomitant use with amantadine, ketamine, phenytoin and dextromethophan should be avoided due to an increased risk of developing psychosis. Plasma concentrations of cimetidine, ranitidine, procainamide, quinidine, quinine and nicotine may increase when taken simultaneously with memantine. It is possible that hydrochlorothiazide levels may decrease when taken concomitantly with memantine. It is possible that the INR (international normalized ratio) may increase in patients taking oral anticoagulants (warfarin). Memantine may increase the excretion rate of hydrochlorothiazide. Concomitant use with antidepressants, selective serotonin reuptake inhibitors and monoamine oxidase inhibitors requires careful monitoring of patients.
special instructions
Patients with Alzheimer's disease in the stages of moderate to severe dementia usually have impaired ability to drive vehicles and operate complex machinery. In addition, memantine may cause a change in the reaction rate, so patients should refrain from driving vehicles or operating complex machinery. Prescribe with caution to patients with thyrotoxicosis, epilepsy, convulsions (including a history), simultaneous use of NMDA receptor antagonists (amantadine, ketamine, dextromethorphan), the presence of factors that increase urine pH (sudden change of diet, for example, switching to vegetarianism, copious intake of alkaline gastric buffers), severe urinary tract infections, myocardial infarction (history), heart failure functional class III-IV (NYHA classification), uncontrolled arterial hypertension, renal failure, liver failure.
Dispensing conditions in pharmacies
On prescription
Treatment regimen
◊ Dosage and dose selection
- 10 mg twice daily
- 28 mg once daily (long-acting)
- Initially 5 mg/day, increase by 5 mg every week; a dose greater than 5 mg should be divided into parts; the maximum dose is 10 mg twice a day [1].
- Long-acting: initially 7 mg once daily, can be increased by 7 mg weekly, maximum dose 28 mg once daily [1].
◊ How quickly it works
Memory improvement is not expected, and it will take months for the condition to stabilize [1].
◊ Expected result
Slows down the development of the disease, but does not stop the degenerative process.
◊ If it doesn't work
- Change the dose, switch to a cholinesterase inhibitor (galantamine, donepezil, rivastigmine) or add a cholinesterase inhibitor.
- Reconsider the diagnosis to rule out depression or non-Alzheimer's dementia [1].
◊ How to stop taking it
- There were no cases of withdrawal syndrome.
- Theoretically, discontinuation of dosage may cause memory impairment and changes in behavior that may remain uncorrected after resumption or initiation of dosage [1].
◊ Treatment combinations
- Atypical antipsychotics for behavior correction;
- Antidepressants for depression, apathy, loss of interest;
- Can be combined with cholinesterase inhibitors;
- Carbamazepine, oxcarbamazepine for behavioral disorders;
Akatinol Memantine, 90 pcs., 10 mg, film-coated tablets
INSTRUCTIONS for medical use of the drug Akatinol Memantine
I APPROVED
Head of the Department of State Control of Medicines and Medical Equipment of the Ministry of Health of the Russian Federation
Approved by the Pharmacological Committee of the Ministry of Health of Russia
Chemical name:
1-amino−3,5-dimethyl-adamantane hydrochloride 3,5-dimethyl-tricyclo-(3,3,1,137)-decane−1-aminohydrochloride
Description
Film-coated tablets, cream-colored, oblong, biconvex, scored on each side. Covered with a film shell. Tablet length 12.6±0.1 mm; width 5.6±0.1 mm; height 3.7±0.1 mm.
Drops are a colorless transparent solution.
Compound
1 film-coated tablet contains: active substance - memantine hydrochloride 10 mg, excipients: lactose 174.75 mg, MCC 52.100 mg, colloidal silicon dioxide 1.25 mg, talc 11.15 mg, magnesium stearate 0.75 mg; film coating: methacrylic acid copolymer 1.446 mg, sodium lauryl sulfate 0.010 mg, polysorbate 80 0.034 mg, triacetin 0.150 mg, SE 0.01 mg, talc 0.35 mg.
1 ml of drops contains: active substance - memantine hydrochloride 10 mg, excipients: potassium sorbate 2 g, sorbitol solution 100 ml, purified water 888 ml.
Pharmacological properties
Pharmacodynamics
Memantine has a modulating effect on the glutamatergic system, being a non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. It has a pathogenetic effect on degenerative processes in the central and peripheral nervous system. Regulates ion transport - blocks calcium channels. Has a neuroprotective effect. Normalizes membrane potential. Improves the process of nerve impulse transmission. Improves cognitive processes, memory and learning ability, increases daily activity.
Pharmacokinetics
After oral administration, Akatinol Memantine is quickly and completely absorbed. Cmax in blood plasma is achieved within 2–6 hours. With normal renal function, no accumulation of the drug was observed. Elimination occurs in two phases. T1/2 is, on average, in the first phase - 4-9 hours, in the second - 40-65 hours. It is excreted mainly by the kidneys (75-90%).
Indications
Degenerative dementia (Alzheimer's type), vascular dementia, mixed dementia of all degrees of severity. Weakening of memory, ability to concentrate, ability to learn. Cerebral and spinal spastic syndrome due to traumatic brain injury, multiple sclerosis, stroke.
Contraindications
— Individual hypersensitivity to the drug.
— Severe renal dysfunction.
- Pregnancy.
- Breast-feeding.
Prescribe with caution to patients with thyretoxicosis and epilepsy.
Side effects
Dizziness, feeling tired, anxiety, increased excitability, nausea.
Interaction
With simultaneous use of Akatinol Memantine with barbiturates, neuroleptics, and anticholinergics, the effect of the latter may be enhanced. When used together, Akatinol Memantine may change the effect of dantrolene or baclofen, so the doses of the drugs should be selected individually.
Overdose
The manifestations of the described side effects may increase.
Directions for use and doses
The dosage regimen is set individually. It is recommended to begin treatment with the administration of minimally effective doses.
Adults with dementia syndrome are prescribed a dose of 5 mg/day during the 1st week of therapy, and a dose of 10 mg/day during the 2nd week. During the 3rd week - at a dose of 15–20 mg/day. If necessary, it is possible to further increase the dose weekly by 10 mg until a daily dose of 30 mg is reached. For movement disorders caused by pathology of the central nervous system, a daily dose of 10 mg is prescribed during the 1st week of treatment, a dose of up to 10 mg/day during the 2nd week, and 20–30 mg during the 3rd week. . If necessary, it is possible to further increase the dose by 10 mg weekly until a daily dose of 60 mg is reached.
The approximate maintenance dose is 10–20 mg/day.
The daily dose is evenly divided into several doses throughout the day, the drug should be taken with meals, the last dose is recommended to be taken before dinner.
For patients with impaired renal function, the dosage regimen is set individually, depending on clinical effectiveness, under the control of renal function during treatment.
Children are prescribed a dose of 500 mcg/kg/day.
special instructions
For elderly patients, it is preferable to prescribe the drug in the form of drops. The optimal dose is achieved gradually, with the dose increasing every week.
Release form
Film-coated tablets: packs of 30 and 90 pcs.
Drops for oral administration: in bottles of 50 and 100 ml.
Storage conditions
List B.
Store at a temperature not exceeding 25°C out of the reach of children.
Best before date
Tablets - 3 years, drops - 5 years.
Conditions for dispensing from pharmacies
On prescription.
Enterprise - 60318, Germany, Frankfurt am Main
Special patient groups
◊ Patients with kidney problems
- No special dose selection is required.
- In severe renal failure, reduce the dose.
◊ Patients with liver disease
No special dose selection is required.
◊ Patients with heart disease
No special dose selection is required.
◊ Elderly patients
The same pharmacokinetics as in young patients.
◊ Children and teenagers
The use of memantine has not been studied.
◊ Pregnant women
- Risk Category B – animal studies have not shown any risk of adverse effects on the fetus, and there have been no adequate studies in pregnant women;
- Not recommended for pregnant women or those preparing to conceive [1].
◊ Breastfeeding
Memantine is not known to pass into breast milk, but all psychotropic drugs pass into breast milk. It is recommended that you stop taking memantine or stop breastfeeding [1].
Akatinol Memantine
Treatment should be initiated and supervised by a physician experienced in diagnosing and treating Alzheimer's dementia.
Therapy should only be started with a caregiver who will regularly monitor the patient's medication intake.
Diagnosis of the disease should be carried out in accordance with current recommendations.
The tolerability and dosage of memantine should be reviewed on a regular basis, preferably within three months of starting treatment. Thereafter, the clinical benefit of memantine and the patient's tolerance to treatment should be reassessed on a regular basis in accordance with current clinical guidelines.
Maintenance treatment can be continued indefinitely as long as the therapeutic effect is favorable and as long as the patient tolerates memantine treatment.
If there is no evidence of therapeutic efficacy or if the patient is intolerant to treatment, discontinuation of memantine should be considered.
The drug should be taken orally once a day at the same time, regardless of meals.
The maximum daily dose is 20 mg.
To reduce the risk of adverse reactions, increase the initial dose to a maintenance dose by titrating 5 mg per week over the first 3 weeks as follows:
1st week (days 1-7): prescribed 5 mg per day.
Week 2 (days 8-14): 10 mg per day is prescribed.
Week 3 (days 15-21): 15 mg per day is prescribed.
4th week and beyond: prescribed 20 mg per day.
The recommended maintenance dose is 20 mg per day.
Tablets with other dosages are available for titration with increasing doses.
Elderly patients
According to clinical studies, the recommended dose for patients over 65 years of age is 20 mg per day.
Kidney failure
In patients with mild renal impairment (creatinine clearance 50-80 ml/min), no dose adjustment is required.
In patients with moderate renal failure (creatinine clearance 30-49 ml/min), the daily dose is 10 mg. If the drug is well tolerated for at least 7 days of treatment, the dose can be increased to 20 mg/day according to the standard titration scheme.
In patients with severe renal failure (creatinine clearance 5-29 ml/min), the daily dose is 10 mg.
Liver failure
In patients with mild or moderate hepatic impairment (Child-Pugh class A and B), no dose adjustment is required.
There are no data on the use of memantine in patients with severe hepatic impairment. Not recommended for use in patients with severe liver failure.
Side effects and other risks
◊ Mechanism of side effects
Presumably due to excessive effects on NMDA receptors.
◊ Side effects
- Dizziness, headache;
- Constipation;
- Dangerous side effects: seizures;
- Weight gain: no;
- Sedation: no, but weakness may occur [1].
◊ What to do about side effects
Wait; Reduce the dose, switch to another drug.
◊ Long-term use
After 6 months, treatment may no longer slow the progression of Alzheimer's disease [1].
◊Addiction
No.
◊ Overdose
- There were no deaths.
- Anxiety, psychosis, visual hallucinations, drowsiness, stupor, loss of consciousness.
Expert advice
- One of two medications recommended for severe Alzheimer's disease;
- The action of memantine is similar to the natural inhibition of NDMA receptors by magnesium, so memantine is a kind of “artificial magnesium.”
- Theoretically, memantine's NMDA antagonism is strong enough to reduce the excitation of glutamate receptors characteristic of Alzheimer's disease, but not strong enough to affect the use of glutamate for plasticity, learning and memory.
- Has a related structure to amantadine, which is also a weak NMDA antagonist
- Memantadine is well tolerated and rarely causes side effects
- The consequences of 5-HT3 receptor antagonist activity have not been studied, but this may be why so few gastrointestinal side effects are observed [1]
