Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Normotimicheskoe means (normalizes the mental state, without causing general inhibition). It also has antidepressant, sedative and antimanic effects. The effect is due to lithium ions, which, being antagonists of sodium ions, push them out of cells and thereby reduce the bioelectrical activity of brain neurons. Accelerates the disintegration of biogenic amines (the concentration of norepinephrine and serotonin in the brain tissues decreases). Increases the sensitivity of the neurons of the hippocampus and other areas of the brain to the action of dopamine. It interacts with lipids formed in the metabolism of inositol.
In therapeutic concentrations, 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 on migraine may be associated with a change in the concentrations of serotonin and histamine in platelets. Antidepressant effect may be associated with increased serotonergic activity and decreased regulation of the ОІ-adrenoreceptor function.
PHARMACOKINETICS
When ingested absorbed from the gastrointestinal tract. C max of the active substance in plasma is reached after approximately 9 hours. It does not bind to plasma proteins. Penetrates through the placental barrier, excreted in breast milk. It is not metabolized.
It is excreted by the kidneys - 95%, with feces - less than 1%, with sweating - 4-5%.
INDICATIONS
Manic and hypomanic conditions of various genesis, prevention and treatment of affective psychoses, prevention and treatment of affective disorders in patients with chronic alcoholism. Migraine, Meniere's syndrome, sexual disorders, drug dependence.
DOSING MODE
The dose is determined by the level of lithium concentration in the blood plasma. Is taken internally. For adults, the dose is 300-600 mg 3-4 times / 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 / day.
The maximum daily intake for adults with oral intake is 2.4 g.
SIDE EFFECT
From the side of the central nervous system and the peripheral nervous system: muscle weakness, hand tremor, adynamia, drowsiness, with prolonged use, there may be a violation of articulation, hyperreflexia.
From the cardiovascular system: heart rhythm disturbances.
From the digestive system: indigestion.
From the endocrine system: rarely - thyroid dysfunction.
Other: increased thirst, hematopoiesis, leukocytosis, weight gain.
CONTRAINDICATIONS
Leukemia, severe surgery, pregnancy, lactation.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in renal failure.
APPLICATION FOR CHILDREN
Medicinal forms of prolonged action should not be used in children under 12 years of age.
APPLICATION IN ELDERLY PATIENTS
Older patients need a correction of the dosing regimen.
SPECIAL INSTRUCTIONS
They are used with caution in cardiovascular diseases (including AV blockade, intraventricular blockade), CNS diseases (including epilepsy, parkinsonism, organic lesions, schizophrenia), severe dehydration, infectious diseases, urinary retention, renal disease insufficiency, as well as diabetes mellitus, hyperparathyroidism, thyrotoxicosis, psoriasis, weakened patients and hyponatremia of any etiology.
Patients of the elderly and weakened patients need a correction of the dosing regimen.
Nausea and vomiting, like 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, the control is carried out monthly, then once every 2-3 months.
During the treatment period, do not drink alcohol.
Medicinal forms of prolonged action should not be used in children under 12 years old, do not alternate with other dosage forms.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
DRUG INTERACTION
With simultaneous use with thiazide diuretics, indapamide, a rapid increase in the concentration of lithium in the blood plasma and the development of toxic effects are possible.
With simultaneous use with ACE inhibitors, an increase in the concentration of lithium in the blood plasma and the development of toxic effects are possible; with NSAIDs - may increase the toxic effects of lithium; with iodine preparations - there may be an increased risk of thyroid dysfunction; with derivatives of xanthine - it is possible to increase the excretion of lithium in the urine, which can lead to a decrease in its effectiveness.
With simultaneous use with alprazolam, a clinically significant increase in the concentration of lithium in the blood plasma is possible; with acyclovir - a case of enhancing the toxic effect of lithium has been described; with baclofen - cases of hyperkinetic symptoms in patients with Huntington's chorea are described.
With the simultaneous use of lithium carbonate with verapamil, drug interaction is unpredictable. With the simultaneous use of lithium carbonate with diltiazem, the case of the development of psychosis is described.
With simultaneous use with haloperidol, it is possible to increase extrapyramidal symptoms; with carbamazepine, clonazepam - neurotoxicity may develop.
With the simultaneous use of methyldopa, the development of toxic effects of lithium is possible; with metronidazole - it is possible to increase the concentration of lithium in blood plasma.
When used simultaneously with sodium chloride, sodium bicarbonate, a high sodium intake enhances the excretion of lithium, which can lead to a decrease in its effectiveness.
With simultaneous application with norepinephrine, a decrease in the vasoconstrictive effect of norepinephrine is possible; with phenytoin - cases of development of symptoms of toxic action of lithium are described; with fluoxetine - an increase in the concentration of lithium in the blood plasma and the development of toxic effects; with furosemide, bumetanide, cases of enhancement of the toxic effect of lithium have been described.
With simultaneous application 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 its rate of excretion in the urine, increase the risk of extrapyramidal reactions, delirium, impaired cerebellar function (especially in elderly people).
