pharmachologic effect
Normotimic agent (normalizes the mental state without causing general inhibition).
It also has antidepressant, sedative and antimanic effects. The effect is caused by lithium ions, which, being antagonists of sodium ions, displace them from cells and thereby reduce the bioelectrical activity of brain neurons. Accelerates the breakdown of biogenic amines (the concentration of norepinephrine and serotonin in brain tissue decreases). Increases the sensitivity of neurons in the hippocampus and other areas of the brain to the action of dopamine. Interacts with lipids formed during the metabolism of inositol. At therapeutic concentrations, it blocks the activity of inosyl-1-phosphatase and reduces the concentration of neuronal inositol, which is involved in the regulation of neuronal sensitivity.
The beneficial effects of lithium in migraine may be due to changes in platelet serotonin and histamine concentrations. The antidepressant effect may be due to increased serotonergic activity and decreased regulation of β-adrenergic receptor function.
Side effects
From the central nervous system and peripheral nervous system:
muscle weakness, hand tremors, adynamia, drowsiness; with prolonged use, articulation disorders and hyperreflexia are possible.
From the cardiovascular system:
heart rhythm disturbances.
From the digestive system:
dyspepsia.
From the endocrine system:
rarely - thyroid dysfunction.
Other:
increased thirst, impaired hematopoiesis, leukocytosis, increased body weight.
Drug interactions
When used simultaneously with thiazide diuretics and indapamide, a rapid increase in the concentration of lithium in the blood plasma and the development of toxic effects are possible.
When used simultaneously with ACE inhibitors, it is possible to increase the concentration of lithium in the blood plasma and develop toxic effects; with NSAIDs - the toxic effects of lithium may be enhanced; with iodine preparations - there may be an increased risk of thyroid dysfunction; with xanthine derivatives - it is possible to increase the excretion of lithium in the urine, which can lead to a decrease in its effectiveness.
When used simultaneously with alprazolam, a clinically significant increase in the concentration of lithium in the blood plasma is possible; with acyclovir - a case of increased toxic effects of lithium has been described; with baclofen - cases of increased hyperkinetic symptoms in patients with Huntington's chorea have been described.
When lithium carbonate is used simultaneously with verapamil, drug interactions are unpredictable. With the simultaneous use of lithium carbonate with diltiazem, a case of the development of psychosis has been described.
When used simultaneously with haloperidol, extrapyramidal symptoms may increase; with carbamazepine, clonazepam - neurotoxicity may develop.
When used simultaneously with methyldopa, lithium toxicity may develop; with metronidazole - it is possible to increase the concentration of lithium in the blood plasma.
When used simultaneously with sodium chloride, sodium bicarbonate, high sodium intake increases the excretion of lithium, which may lead to a decrease in its effectiveness.
When used simultaneously with norepinephrine, the vasoconstrictor effect of norepinephrine may be reduced; with phenytoin - cases of the development of symptoms of lithium toxicity have been described; with fluoxetine - it is possible to increase the concentration of lithium in the blood plasma and develop toxic effects; with furosemide and bumetanide, cases of increased toxic effects of lithium have been described.
When used simultaneously with chlorpromazine and other phenothiazines, it is possible to reduce the absorption of phenothiazines from the gastrointestinal tract and reduce their concentration in the blood plasma by 40%, increase the intracellular concentration of lithium and the rate of its excretion in the urine, increase the risk of developing extrapyramidal reactions, delirium, cerebellar dysfunction (especially in elderly people).
Sedalite (lithium carbonate) (table 300 mg No. 50)
A country
Russia
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Active substance
Lithium carbonate
Compound
10 pieces. — contour cell packaging 5 pcs. Film-coated tablets. For 1 tab. lithium carbonate 300 mg.
pharmachologic effect
Normotimic agent (normalizes the mental state without causing general inhibition). It also has antidepressant, sedative and antimanic effects. The effect is caused by lithium ions, which, being antagonists of sodium ions, displace them from cells and thereby reduce the bioelectrical activity of brain neurons. Accelerates the breakdown of biogenic amines (the concentration of norepinephrine and serotonin in brain tissue decreases). Increases the sensitivity of neurons in the hippocampus and other areas of the brain to the action of dopamine. Interacts with lipids formed during the metabolism of inositol. At therapeutic concentrations, it blocks the activity of inosyl-1-phosphatase and reduces the concentration of neuronal inositol, which is involved in the regulation of neuronal sensitivity. The beneficial effect of lithium in migraine may be associated with changes in the concentrations of serotonin and histamine in platelets. The antidepressant effect may be associated with increased serotonergic activity and decreased regulation of β-adrenergic receptor function.
Indications for use
Manic and hypomanic states of various origins, prevention and treatment of affective psychoses, prevention and treatment of affective disorders in patients with chronic alcoholism. Migraine, Meniere's syndrome, sexual disorders, drug addiction.
Mode of application
The dose is determined by the level of lithium concentration in the blood plasma. Taken orally. For adults, the dose is 300-600 mg 3-4 times a day. The therapeutic concentration of lithium in plasma is 0.6-1 mmol/l. For children under 12 years of age - 15-20 mg 2-3 times a day. The maximum daily dose for adults when taken orally is 2.4 g.
Interaction
When used simultaneously with thiazide diuretics and indapamide, a rapid increase in the concentration of lithium in the blood plasma and the development of toxic effects is possible. When used simultaneously with ACE inhibitors, an increase in the concentration of lithium in the blood plasma and the development of toxic effects is possible; with NSAIDs - the toxic effects of lithium may be enhanced; with iodine preparations - there may be an increased risk of thyroid dysfunction; with xanthine derivatives - it is possible to increase the excretion of lithium in the urine, which can lead to a decrease in its effectiveness. When used simultaneously with alprazolam, a clinically significant increase in the concentration of lithium in the blood plasma is possible; with acyclovir - a case of increased toxic effects of lithium has been described; with baclofen - cases of increased hyperkinetic symptoms in patients with Huntington's chorea have been described. When lithium carbonate is used simultaneously with verapamil, the drug interaction is unpredictable. With the simultaneous use of lithium carbonate with diltiazem, a case of the development of psychosis has been described. With simultaneous use with haloperidol, extrapyramidal symptoms may increase; with carbamazepine, clonazepam - the development of neurotoxicity is possible. When used simultaneously with methyldopa, the toxic effect of lithium may develop; with metronidazole - it is possible to increase the concentration of lithium in the blood plasma. When used simultaneously with sodium chloride, sodium bicarbonate, high sodium intake increases the excretion of lithium, which can lead to a decrease in its effectiveness. When used simultaneously with norepinephrine, the vasoconstrictor effect of norepinephrine may decrease; with phenytoin - cases of the development of symptoms of lithium toxicity have been described; with fluoxetine - it is possible to increase the concentration of lithium in the blood plasma and develop toxic effects; with furosemide, bumetanide, cases of increased toxic effects of lithium have been described. When used simultaneously with chlorpromazine and other phenothiazines, it is possible to reduce the absorption of phenothiazines from the gastrointestinal tract and reduce their concentration in the blood plasma by 40%, increase the intracellular concentration of lithium and the rate of its excretion in the urine, increasing the risk of developing extrapyramidal reactions, delirium, cerebellar dysfunction (especially in the elderly).
Side effect
From the central nervous system and peripheral nervous system: muscle weakness, hand tremors, adynamia, drowsiness, with prolonged use, articulation disorders, hyperreflexia are possible. From the cardiovascular system: heart rhythm disturbances. From the digestive system: dyspepsia. From the endocrine system: rarely - dysfunction of the thyroid gland. Other: increased thirst, impaired hematopoiesis, leukocytosis, weight gain.
Contraindications
Leukemia, severe surgical interventions, pregnancy, lactation.
special instructions
Use with caution for cardiovascular diseases (including AV block, intraventricular block), central nervous system diseases (including epilepsy, parkinsonism, organic lesions, schizophrenia), severe dehydration, infectious diseases, urinary retention, renal deficiency, as well as in diabetes mellitus, hyperparathyroidism, thyrotoxicosis, psoriasis, in debilitated patients and with hyponatremia of any etiology. Elderly and debilitated patients require adjustment of the dosage regimen. Nausea and vomiting, as early signs of lithium toxicity, can be masked by the antiemetic effect of some phenothiazines During the first month of therapy, the concentration of lithium in the blood plasma should be monitored weekly. When a stable concentration is achieved, control is carried out monthly, then once every 2-3 months. Avoid drinking alcohol during the treatment period. Long-acting dosage forms should not be used in children under 12 years of age, do not alternate with other dosage forms. Effect on the ability to driving vehicles and operating machinery. During treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Storage conditions
Room temperature
Dispensing conditions in pharmacies
On prescription
special instructions
Use with caution for cardiovascular diseases (including AV block, intraventricular block), central nervous system diseases (including epilepsy, parkinsonism, organic lesions, schizophrenia), severe dehydration, infectious diseases, urinary retention, renal deficiency, as well as in diabetes mellitus, hyperparathyroidism, thyrotoxicosis, psoriasis, in weakened patients and in hyponatremia of any etiology.
Elderly and debilitated patients require dosage adjustment.
Nausea and vomiting, early signs of lithium toxicity, may be masked by the antiemetic effect of some phenothiazines.
During the first month of therapy, the concentration of lithium in the blood plasma should be monitored weekly. When a stable concentration is achieved, monitoring is carried out monthly, then once every 2-3 months.
During the treatment period, avoid drinking alcohol.
Long-acting dosage forms should not be used in children under 12 years of age and should not be alternated with other dosage forms.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Sedalit®
Lithium carbonate has a narrow “therapeutic window”. The required dose of the drug should be carefully selected and regularly adjusted, based on data on the concentration of lithium in the blood plasma. If it is not possible to regularly measure the concentration of lithium in the blood plasma, therapy should not be started.
Elderly patients often require lower doses of lithium to achieve therapeutic drug concentrations. They are most susceptible to the toxic effects of lithium; lithium excretion may also be reduced. Symptoms of toxicity in elderly patients may develop at lithium blood concentrations that are tolerated satisfactorily in younger patients.
Since there is no information on the safety and effectiveness of lithium carbonate in children under 12 years of age, its use in this category of patients is contraindicated.
Before prescribing long-term therapy with lithium preparations, in order to avoid the development of toxic effects, it is necessary to conduct a thorough medical examination before and during treatment. Before prescribing the drug, the function of the kidneys, thyroid gland (the patient must be in a euthyroid state before starting lithium therapy) and the cardiovascular system should be assessed, especially in patients with diseases of the cardiovascular system. During treatment, periodic assessment of renal, thyroid and cardiovascular function is required.
Lithium carbonate is known to reduce sodium reabsorption in the renal tubules, which may lead to decreased sodium concentrations. Thus, it is extremely important for patients to follow a diet, including adequate fluid intake (2500-3000 ml) and sodium chloride, at least during the stabilization period. Decreased tolerance to lithium has been noted following excessive sweating or diarrhea. In such cases, it is necessary to take additional fluids and table salt under medical supervision, as well as reduce the dose or temporarily stop taking the drug until the condition resolves.
During the first month of therapy, the concentration of Li+ ions in the blood plasma is determined weekly, then, once a stable concentration is achieved, monitoring is carried out monthly, then every 2-3 months. Return to weekly monitoring is required when lithium carbonate dosage changes; the presence of an intercurrent infectious or other serious disease; significant changes in the amount of sodium and/or fluid received; taking drugs that alter the renal clearance of lithium; taking medications that affect electrolyte balance.
Blood samples are always taken in the morning, i.e. 12 hours after taking the last dose at night or 24 hours after taking a single dose in the morning.
When prescribing long-term lithium therapy, the physician should give patients clear instructions regarding symptoms of developing toxicity, and also recommend urgent medical attention if such symptoms occur.
Toxic effects are expected at serum lithium concentrations of about 1.5 mmol/L; however, they may also occur at lower concentrations. If toxic effects occur, treatment should be discontinued immediately and should always be taken very seriously.
At the beginning of treatment, it can provoke depression or mania.
During drug therapy, laboratory test results may change (including leukocytosis, decreased concentrations of thyroxine and triiodothyronine, decreased creatinine clearance, albuminuria, etc.)
Lithium carbonate should be stopped 24 hours before major surgery. During minor surgery, treatment can be continued provided that fluid and electrolyte levels are properly monitored.
In renal failure, lithium excretion is reduced, which increases the risk of toxic reactions. Lithium is contraindicated in severe renal failure. In case of mild to moderate renal failure, careful monitoring of the concentration of lithium in the blood plasma is required. Monitoring of renal function is also required in patients with polyuria and polydipsia.
In patients on long-term lithium therapy, morphological changes in the kidneys were noted in the form of glomerular interstitial fibrosis and nephron atrophy. Morphological changes were also observed in patients with manic-depressive states who were never prescribed lithium. The relationship between renal function, morphological changes and lithium therapy has not been proven. In patients taking medications that lower the epileptic threshold and in patients with epilepsy when prescribed lithium carbonate, the risk of developing convulsive conditions increases.
It is not recommended to prescribe lithium carbonate together with antipsychotics. Some patients taking lithium together with antipsychotics developed an encephalopathic syndrome (characterized by weakness, apathy, fever, trembling, confusion, extrapyramidal symptoms, leukocytosis, etc.). In some cases, this syndrome was accompanied by irreversible brain damage. Due to the existence of a possible cause-and-effect relationship between the development of encephalopathic syndrome and the combined use of lithium and antipsychotics, it is necessary to carefully monitor patients undergoing combination treatment for early detection of neurological toxicity, requiring immediate cessation of treatment. Encephalopathic syndrome may have a similar or similar course to neuroleptic malignant syndrome.
Co-prescription with antipsychotic drugs is not allowed.
Lithium carbonate should be avoided in patients with congenital QT prolongation. as well as patients taking medications that can prolong the QT interval. Caution must be exercised in patients with risk factors for prolongation of the QT interval, which primarily include heart disease, bradycardia, thyroid disease, hypokalemia, hypomagnesemia, hypocalcemia. female gender and old age.
Lithium therapy may manifest or aggravate Brugada syndrome, an inherited sodium channel disorder of the heart with characteristic ECG changes (right bundle branch block and ST segment elevation in the right precordial leads), which can lead to cardiac arrest or sudden death. Lithium carbonate should not be used in patients with Brugada syndrome or a family history of Brugada syndrome. Use with caution in patients with a family history of cardiac arrest or sudden death.
Long-term drug therapy may be associated with a decrease in the concentrating ability of the kidneys, which contributes to the development of nephrogenic diabetes insipidus, with polyuria and polydipsia. These patients should be closely monitored for renal function and for dehydration due to lithium retention and toxicity. As a rule, these changes are reversible and regress after discontinuation of drug therapy. There is evidence of the occurrence of hyperparathyroidism and hypothyroidism, which persist even after discontinuation of the drug.
There are reported cases of increased intracranial pressure and papilledema (false brain tumor syndrome). If this syndrome develops, drug therapy should be discontinued. Patients should be warned to report recurrent headaches and/or visual disturbances to their physician.
Patients prescribed long-term therapy with lithium carbonate should be counseled regarding symptoms of toxicity and instructed to seek immediate medical attention at the first sign of such symptoms.
During drug therapy, the following pathological changes in the electroencephalogram may be recorded: diffuse slowing, expansion of the frequency spectrum, potentiation and disorganization of the background rhythm.
