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- Description en
- DEMANTIN Composition and Dosage Form Coated tablets: 100 pcs. per pack. Memantine hydrochloride . . . . . . 10 mg Clinical-Pharmacological Group Medication for the treatment of dementia (Alzheimer's type). Pharmacological Properties Dysfunction of glutamatergic neurotransmission (especially at the level of N-methyl-D-aspartate (NMDA) receptors) is believed to be involved in the development of symptoms and progression of Alzheimer's disease. Memantine, as an anti-dementia agent, is a potential antagonist of NMDA receptors. Memantine blocks the pathological increase in glutamate levels that leads to neuronal dysfunction. Pharmacokinetics The bioavailability of memantine is approximately 100%. The Tmax of the drug is 3-8 hours. Food intake does not affect the absorption of memantine. Steady-state concentrations of memantine (70-150 ng/mL) are achieved with daily doses of 20 mg, and these levels vary individually. The ratio of active ingredient concentrations in cerebrospinal fluid and blood serum is 0.52, with daily doses ranging from 5-30 mg. The volume of distribution of memantine is 10 L/kg, and the plasma protein binding is 45%. After oral administration, 80% of the absorbed dose is found unchanged in the blood. The main metabolites of memantine are N-3,5-dimethyl-gludantane, mixed isomers of -4 and -6-hydroxy memantine, and 1-nitroso-3,5-dimethyl adamantane. These metabolites have no anti-NMDA activity. In vitro studies have not revealed memantine metabolism reactions catalyzed by the cytochrome P450 system. The terminal half-life of memantine (T1/2) is 60-100 hours. 84% of the absorbed dose is excreted by the kidneys. Renal clearance of memantine is mediated by tubular secretion and tubular reabsorption. In alkaline urine (pH=7-9), memantine excretion may be reduced. Alkalinization of urine can be caused by radical changes in diet (e.g., switching from a meat-rich diet to a vegetable-rich diet, or excessive use of antacids). Special Populations In studies involving elderly volunteers with normal or impaired renal function (creatinine clearance 50-100 mL/min/1.73 m2), no significant correlation was observed between creatinine clearance and total renal clearance of memantine. Memantine undergoes minimal metabolism in the liver, and its metabolites have no anti-NMDA activity. No significant changes in the pharmacokinetics of memantine are expected in patients with mild to moderate hepatic impairment. Pharmacokinetics/Pharmacodynamics Correlation A daily dose of 20 mg of memantine is sufficient to achieve adequate concentrations in the cerebrospinal fluid. Indications DEMANTIN is used for moderate to severe forms of Alzheimer's disease. Dosage Regimen Tablets Adults: The maximum daily dose is 20 mg. The recommended starting dose for the first week is 5 mg once daily (half a tablet every morning) to reduce the risk of side effects. The dose should be increased by 5 mg increments to 10 mg (half a tablet twice daily) during the second week, and to 15 mg/day (1 tablet in the morning and half a tablet in the evening) in the third week. Treatment continues with an increase in dose to 20 mg (1 tablet twice daily) from the fourth week. DEMANTIN can be taken on an empty stomach or after meals. Elderly: The recommended daily dose in patients over 65 years of age is 20 mg (1 tablet twice daily). Children and Adolescents under 18 years of age: The efficacy and safety of memantine have not been studied in children. Renal Impairment: Dose reduction is not necessary in patients with mild renal impairment (serum creatinine level 130 mol/L). The daily dose in patients with moderate renal impairment (creatinine clearance 40-60 mL/min/1.73 m2) is 10 mg. Adequate data are not available regarding the use of the drug in patients with severe renal impairment. Hepatic Impairment: Adequate data are not available regarding the use of the drug in this population. Side Effects In patients with moderate to severe dementia treated with memantine, the incidence of side effects is practically no different from placebo, and the reported side effects are usually mild to moderate in severity. The most common side effects of memantine (>4%) are: Memantine n=299 (%) Memantine n=299 (%) Anxiety 27(9) Urinary incontinence 50(17.4) Injury 20(6.7) 20(6.9) Urinary incontinence 17(5.7) 21(7.3) Diarrhea 16(5.4) 14(4.9) Insomnia 16(5.4) 14(4.9) Dizziness 15(5) 8(2.8) Headache 15(5) 9(3.1) Hallucination 15(5) 6(2.1) Fall 14(4.7) 14(4.9) Constipation 12(4) 13(4.5) Cough 12(4) 17(5.9) The most common side effects observed with memantine (1-10% and more frequent compared to placebo) are: hallucinations, confusion, dizziness, headache, and asthenia. The most uncommon side effects observed with memantine (0.1-1% and more frequent compared to placebo) are: agitation, hypertension, nausea, cystitis, and increased libido. Seizures were mainly observed in patients with a history of convulsions and predisposition to epilepsy. Consult your doctor in case of adverse events. Contraindications DEMANTIN is contraindicated in patients with hypersensitivity to memantine hydrochloride or any other component of the preparation. Pregnancy and Lactation Pregnancy (Category B). Animal studies have shown fetal developmental retardation when memantine was administered at doses equivalent to or slightly higher than human doses. It is not known to what extent this data reflects the risk in humans. Therefore, the use of memantine is not recommended in pregnant women unless there is a clear indication. Breastfeeding is not recommended while taking memantine. Special Instructions In patients with severe renal impairment (creatinine clearance < 20 mL/min/1.73 m2), the drug should be administered with caution. The drug is prescribed with caution in patients with epilepsy due to its pharmacological properties and individual cases. DEMANTIN should not be used concurrently with other NMDA antagonists such as amantadine, ketamine, and dextromethorphan. These substances also act on the same receptors as memantine, which can lead to side effects (especially CNS-related). Patients with increased urine pH (transition from a meat-rich diet to a vegetable-rich diet, or excessive use of antacids, or tubular acidosis or severe urinary tract infection caused by Proteus) may require intensive monitoring. Patients with recent myocardial infarction, or congestive heart failure (NYHA III-IV), or uncontrolled hypertension were not included in memantine studies. Therefore, data on the use of memantine in this population are insufficient. If the drug is used, these patients require intensive monitoring. Pediatric patients: Adequate and controlled clinical trial data on the efficacy and safety of memantine in children are not available. Effect on Ability to Drive and Operate Machinery: During memantine treatment, the patient's reactions may be altered, affecting the ability to drive and operate machinery. Overdose Treatment for overdose is symptomatic. In one case of memantine overdose (400 mg), the patient experienced CNS symptoms (anxiety, psychosis, visual hallucinations, pre-convulsive state, somnolence, stupor, and loss of consciousness). The patient recovered without permanent complications. Interactions with Other Drugs Concomitant administration with memantine may increase the effect of L-DOPA, dopaminergic agonists, and anticholinergic agents. The effect of barbiturates and neuroleptics may be reduced when taken with memantine. Concomitant administration of memantine may increase the effect of antispasmodics, dantrolene, or baclofen, and in such cases, dose adjustment of these agents may be necessary. It is not advisable to prescribe memantine with other NMDA antagonists such as amantadine, ketamine, and dextromethorphan due to the risk of developing pharmacotoxic psychosis. Drugs that use the same renal cationic system (cimetidine, ranitidine, procainamide, quinidine, quinine, and nicotine) interact with memantine and increase its blood levels. Hydrochlorothiazide excretion is reduced when used with memantine. In vitro studies have shown that memantine does not inhibit CYP 1A2, 2A6, 2C9, 2D6, 2E1, 3A, flavin monooxygenase, and epoxide hydrolase enzymes, and the sulfation process. Incompatibility: Not characterized. Shelf Life The preparation should be stored at a temperature not exceeding 25°C, in a dry place, inaccessible to children. Shelf life - 5 years. Conditions of Dispensing from Pharmacy: The preparation is dispensed by prescription only.
- Active
- memantine
What is it?
DEMANTIN Composition and Dosage Form Coated tablets: 100 pcs. per pack. Memantine hydrochloride . . . . . . 10 mg Clinical-Pharmacological Group Medication for the treatment of dementia (Alzheimer's type). Pharmacological Properties Dysfunction of glutamatergic neurotransmission (especially at the level of N-methyl-D-aspartate (NMDA) receptors) is believed to be involved in the development of symptoms and progression of Alzheimer's disease. Memantine, as an anti-dementia agent, is a potential antagonist of NMDA receptors. Memantine blocks the pathological increase in glutamate levels that leads to neuronal dysfunction. Pharmacokinetics The bioavailability of memantine is approximately 100%. The Tmax of the drug is 3-8 hours. Food intake does not affect the absorption of memantine. Steady-state concentrations of memantine (70-150 ng/mL) are achieved with daily doses of 20 mg, and these levels vary individually. The ratio of active ingredient concentrations in cerebrospinal fluid and blood serum is 0.52, with daily doses ranging from 5-30 mg. The volume of distribution of memantine is 10 L/kg, and the plasma protein binding is 45%. After oral administration, 80% of the absorbed dose is found unchanged in the blood. The main metabolites of memantine are N-3,5-dimethyl-gludantane, mixed isomers of -4 and -6-hydroxy memantine, and 1-nitroso-3,5-dimethyl adamantane. These metabolites have no anti-NMDA activity. In vitro studies have not revealed memantine metabolism reactions catalyzed by the cytochrome P450 system. The terminal half-life of memantine (T1/2) is 60-100 hours. 84% of the absorbed dose is excreted by the kidneys. Renal clearance of memantine is mediated by tubular secretion and tubular reabsorption. In alkaline urine (pH=7-9), memantine excretion may be reduced. Alkalinization of urine can be caused by radical changes in diet (e.g., switching from a meat-rich diet to a vegetable-rich diet, or excessive use of antacids). Special Populations In studies involving elderly volunteers with normal or impaired renal function (creatinine clearance 50-100 mL/min/1.73 m2), no significant correlation was observed between creatinine clearance and total renal clearance of memantine. Memantine undergoes minimal metabolism in the liver, and its metabolites have no anti-NMDA activity. No significant changes in the pharmacokinetics of memantine are expected in patients with mild to moderate hepatic impairment. Pharmacokinetics/Pharmacodynamics Correlation A daily dose of 20 mg of memantine is sufficient to achieve adequate concentrations in the cerebrospinal fluid. Indications DEMANTIN is used for moderate to severe forms of Alzheimer's disease. Dosage Regimen Tablets Adults: The maximum daily dose is 20 mg. The recommended starting dose for the first week is 5 mg once daily (half a tablet every morning) to reduce the risk of side effects. The dose should be increased by 5 mg increments to 10 mg (half a tablet twice daily) during the second week, and to 15 mg/day (1 tablet in the morning and half a tablet in the evening) in the third week. Treatment continues with an increase in dose to 20 mg (1 tablet twice daily) from the fourth week. DEMANTIN can be taken on an empty stomach or after meals. Elderly: The recommended daily dose in patients over 65 years of age is 20 mg (1 tablet twice daily). Children and Adolescents under 18 years of age: The efficacy and safety of memantine have not been studied in children. Renal Impairment: Dose reduction is not necessary in patients with mild renal impairment (serum creatinine level 130 mol/L). The daily dose in patients with moderate renal impairment (creatinine clearance 40-60 mL/min/1.73 m2) is 10 mg. Adequate data are not available regarding the use of the drug in patients with severe renal impairment. Hepatic Impairment: Adequate data are not available regarding the use of the drug in this population. Side Effects In patients with moderate to severe dementia treated with memantine, the incidence of side effects is practically no different from placebo, and the reported side effects are usually mild to moderate in severity. The most common side effects of memantine (>4%) are: Memantine n=299 (%) Memantine n=299 (%) Anxiety 27(9) Urinary incontinence 50(17.4) Injury 20(6.7) 20(6.9) Urinary incontinence 17(5.7) 21(7.3) Diarrhea 16(5.4) 14(4.9) Insomnia 16(5.4) 14(4.9) Dizziness 15(5) 8(2.8) Headache 15(5) 9(3.1) Hallucination 15(5) 6(2.1) Fall 14(4.7) 14(4.9) Constipation 12(4) 13(4.5) Cough 12(4) 17(5.9) The most common side effects observed with memantine (1-10% and more frequent compared to placebo) are: hallucinations, confusion, dizziness, headache, and asthenia. The most uncommon side effects observed with memantine (0.1-1% and more frequent compared to placebo) are: agitation, hypertension, nausea, cystitis, and increased libido. Seizures were mainly observed in patients with a history of convulsions and predisposition to epilepsy. Consult your doctor in case of adverse events. Contraindications DEMANTIN is contraindicated in patients with hypersensitivity to memantine hydrochloride or any other component of the preparation. Pregnancy and Lactation Pregnancy (Category B). Animal studies have shown fetal developmental retardation when memantine was administered at doses equivalent to or slightly higher than human doses. It is not known to what extent this data reflects the risk in humans. Therefore, the use of memantine is not recommended in pregnant women unless there is a clear indication. Breastfeeding is not recommended while taking memantine. Special Instructions In patients with severe renal impairment (creatinine clearance < 20 mL/min/1.73 m2), the drug should be administered with caution. The drug is prescribed with caution in patients with epilepsy due to its pharmacological properties and individual cases. DEMANTIN should not be used concurrently with other NMDA antagonists such as amantadine, ketamine, and dextromethorphan. These substances also act on the same receptors as memantine, which can lead to side effects (especially CNS-related). Patients with increased urine pH (transition from a meat-rich diet to a vegetable-rich diet, or excessive use of antacids, or tubular acidosis or severe urinary tract infection caused by Proteus) may require intensive monitoring. Patients with recent myocardial infarction, or congestive heart failure (NYHA III-IV), or uncontrolled hypertension were not included in memantine studies. Therefore, data on the use of memantine in this population are insufficient. If the drug is used, these patients require intensive monitoring. Pediatric patients: Adequate and controlled clinical trial data on the efficacy and safety of memantine in children are not available. Effect on Ability to Drive and Operate Machinery: During memantine treatment, the patient's reactions may be altered, affecting the ability to drive and operate machinery. Overdose Treatment for overdose is symptomatic. In one case of memantine overdose (400 mg), the patient experienced CNS symptoms (anxiety, psychosis, visual hallucinations, pre-convulsive state, somnolence, stupor, and loss of consciousness). The patient recovered without permanent complications. Interactions with Other Drugs Concomitant administration with memantine may increase the effect of L-DOPA, dopaminergic agonists, and anticholinergic agents. The effect of barbiturates and neuroleptics may be reduced when taken with memantine. Concomitant administration of memantine may increase the effect of antispasmodics, dantrolene, or baclofen, and in such cases, dose adjustment of these agents may be necessary. It is not advisable to prescribe memantine with other NMDA antagonists such as amantadine, ketamine, and dextromethorphan due to the risk of developing pharmacotoxic psychosis. Drugs that use the same renal cationic system (cimetidine, ranitidine, procainamide, quinidine, quinine, and nicotine) interact with memantine and increase its blood levels. Hydrochlorothiazide excretion is reduced when used with memantine. In vitro studies have shown that memantine does not inhibit CYP 1A2, 2A6, 2C9, 2D6, 2E1, 3A, flavin monooxygenase, and epoxide hydrolase enzymes, and the sulfation process. Incompatibility: Not characterized. Shelf Life The preparation should be stored at a temperature not exceeding 25°C, in a dry place, inaccessible to children. Shelf life - 5 years. Conditions of Dispensing from Pharmacy: The preparation is dispensed by prescription only.