Buy Akatinol Memantine film-coated tablets 10 mg No. 30 in pharmacies
Buy Akatinol Memantine in pharmacies Akatinol Memantine in the medicine directory DOSAGE FORMS film-coated tablets 10 mg
MANUFACTURERS Merz Pharma GmbH and Co. KGaA (Germany)
GROUP Nootropic drugs
COMPOSITION Active substance: memantine hydrochloride.
INTERNATIONAL NON-PROPENTED NAME Memantine
SYNONYMS Memantine Canon, Memantine-TL, Memikar, Memorel, Noodzheron
PHARMACOLOGICAL ACTION Pharmacodynamics. Being a non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors, it has a modulating effect on the glutamatergic system. 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. It is excreted in the urine.
INDICATIONS FOR USE Dementia of the Alzheimer's type, vascular dementia, mixed dementia of all degrees of severity.
CONTRAINDICATIONS Individual hypersensitivity to the drug, severe renal dysfunction, pregnancy, breastfeeding, children under 18 years of age (due to insufficient data).
SIDE EFFECTS For the body as a whole - general side effects. Often: headache; rarely: fatigue. Infections. Rarely: fungal infections. Mental disorders. Often: drowsiness; rarely: confusion, hallucinations; frequency not established: psychotic reactions. Disorders of the cardiovascular system. Rarely: hypertension, venous thrombosis/thromboembolism; uncommon: heart failure. Respiratory system disorders. Common: shortness of breath. Gastrointestinal disorders. Common: constipation; rarely: nausea, vomiting; frequency not established: pancreatitis. Disorders of the central and peripheral nervous system. Common: dizziness; rarely: gait disturbance; very rarely: convulsions. Hallucinations have been observed mainly in patients with Alzheimer's disease at the stage of severe dementia.
INTERACTION When used simultaneously with L-dopa drugs, dopamine agonists, and anticholinergics, 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 and dexamethophan should be avoided. Plasma levels of cimetidine, procainamide, kinidine, kinin and nicotine may increase when taken simultaneously with memantine. A decrease in hydrochlorothiazide levels may occur when taken concomitantly with memantine.
METHOD OF APPLICATION AND DOSAGE Orally, during meals. The dosage regimen is set individually. It is recommended to begin treatment with the administration of minimally effective doses. Adults with dementia 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. The optimal dose is achieved gradually, with the dose increasing every week.
OVERDOSE Symptoms: increased severity of side effects. Treatment: gastric lavage, taking activated carbon, symptomatic therapy.
SPECIAL INSTRUCTIONS Prescribe with caution to patients with thyrotoxicosis, epilepsy, seizures (including a history), myocardial infarction, heart failure. 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 changes in the reaction rate; therefore, in patients receiving treatment on an outpatient basis, special care should be taken when driving or operating machinery.
STORAGE CONDITIONS Store out of the reach of children at a temperature not exceeding 25 C.
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.
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
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]
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 (tab.p.pl/vol.10mg No. 90)
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 10 mg Excipients: lactose – 174.75 mg; microcrystalline cellulose – 52.1 mg; colloidal silicon dioxide – 1.25 mg; talc – 11.15 mg; magnesium stearate – 0.75 mg. Shell: methacrylic acid copolymer, type C – 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. Description Film-coated tablets are white, oblong, biconvex, scored on each side. Release form: Film-coated tablets, 10 mg. 10 tablets in a blister made of polyvinyl chloride film and aluminum foil. 3 or 9 blisters along with instructions for use are placed in a cardboard box.
Pharmacological properties
Pharmacodynamics: Being a non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors, it has a modulating effect on the glutamatergic system.
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. It is excreted in the urine.
Indications for use
Dementia of Alzheimer's type, vascular dementia, mixed dementia of all degrees of severity.
Contraindications
Individual hypersensitivity to the drug, severe renal dysfunction, pregnancy, breastfeeding, children under 18 years of age (due to insufficient data). Prescribe with caution to patients with thyrotoxicosis, epilepsy, seizures (including a history), myocardial infarction, and heart failure.
Mode of application
Inside, during meals. The dosage regimen is set individually. It is recommended to begin treatment with the administration of minimally effective doses. Adults with dementia 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. The optimal dose is achieved gradually, with the dose increasing every week.
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 Hallucinations1 Frequency not established Psychotic reactions2 Cardiovascular disorders Rarely Hypertension Rarely Venous thrombosis/thromboembolism Uncommon Heart failure Respiratory system disorders Common Dyspnea Gastrointestinal disorders Common Constipation Rarely Nausea, vomiting Frequency not established Pancreatitis2 Disorders of the central and peripheral nervous system Common Dizziness Rare Gait disturbance Very rare Seizures 1 Hallucinations have been observed mainly in patients with Alzheimer's disease at the stage of severe dementia. 2 There are isolated reports of the occurrence of these adverse reactions when using the drug in clinical practice practice (data obtained after the drug went on sale).
Overdose
Symptoms: increased severity of side effects. Treatment: gastric lavage, taking activated carbon, symptomatic therapy.
Interaction
When used simultaneously with L-dopa drugs, dopamine agonists, and anticholinergics, 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 and dexamethophan should be avoided. Plasma levels of cimetidine, procainamide, kinidine, kinin and nicotine may increase when taken simultaneously with memantine. A decrease in hydrochlorothiazide levels may occur when taken concomitantly with memantine.
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, therefore, in patients receiving treatment on an outpatient basis, special care should be taken when driving or operating machinery.
Dispensing conditions in pharmacies
On prescription
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.
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].
