Sedalite® (Sedalit®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLithium carbonateLithium carbonate
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  • Sedalite®
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    PHARMSTANDART-FORESTRY, OJSC     Russia
    • Dosage form: & nbspfilm coated tablets
    Composition:

    Composition per one tablet:

    active substance: lithium carbonate - 300 mg;

    auxiliary substances: core: potato starch - 14.62 mg, croscarmellose sodium (impellosis) - 20 mg, povidone (polyvinylpyrrolidone, povidone K-25) - 55.38 mg, talc - 6 mg, calcium stearate-4 mg;

    sheath: hypromellose (hydroxypropyl methylcellulose) 5.87 mg, povidone (polyvinylpyrrolidone, povidone K-25) 1.837 mg, polysorbate 80 (twin 80) 0.543 mg, titanium dioxide 2.1 mg, talc 1.65 mg.

    Description:Round biconvex tablets, covered with a film coating of white color.
    Pharmacotherapeutic group:Normotimicheskoe means
    ATX: & nbsp

    N.05.A.N.01   Lithium

    Pharmacodynamics:

    Normotimicheskoe means (normalizes the mental state without causing general inhibition), also has antidepressant, sedative and antimanic effects. The effect is due to lithium ions (Li+), which, being the antagonists of sodium ions (Na+), expel them from the cells and, thereby, reduce the bioelectrical activity of neurons in the brain. Accelerates the decomposition of biogenic amines (the content 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 plays a role in regulating the sensitivity of neurons.

    The beneficial effect of lithium preparations on migraine may be associated with a change in serotonin concentrations; with depression - with an increase in serotonergic activity and a decrease in the regulation of beta-adrenoreceptor function.

    Pharmacokinetics:

    Suction fast and complete for 6-8 hours. It does not bind to blood proteins. The therapeutic range of concentrations in the blood is in the range from 0.6 to 1.2 mmol / p. Time to reach the maximum concentration in the blood (CmOh) - 1-3 hours. Stable concentration in serum is achieved after 4 days. The drug penetrates the blood-brain barrier (BBB) ​​(concentrations in the cerebrospinal fluid are half of the plasma level), the placental barrier penetrates into breast milk. Biotransformation is not exposed. The half-life period (T1 / 2) in adults is 24 hours, in adolescents - 18 hours, in elderly people - up to 36 hours.Values T1/2 depend on the number of ions Na+ in the plasma. It is excreted by the kidneys - 95%, with feces - less than 1%, with sweat - 4-5%. Kidney excretion is dependent on the ratios of ion concentrations Li+, Na+ and K+ in blood.

    Indications:

    Manic and hypomanic states of various genesis, affective psychoses (manic-depressive, schizoaffective), alcoholism (affective disorders); Migraine, Meniere's syndrome, sexual disorders, drug dependence (some forms).

    Contraindications:

    Hypersensitivity to lithium and other components of the drug; severe surgical interventions; leukemia; pregnancy, the period of breastfeeding; children under 12 years of age (efficacy and safety of use not established); cardiovascular diseases associated with heart rhythm disturbances; presence of Brugada syndrome / family history of Brugada syndrome; severe degree of renal failure; untreated or unrecoverable hypothyroidism; low levels of sodium in the body, for example, in patients with dehydration, patients with a salt-free diet or in patients with Addison's disease.

    Carefully:

    Diseases of the cardiovascular system (incl.atrial-ventricular and intraventricular block), CNS diseases (epilepsy, Parkinson's disease), diabetes, hyperthyroidism, hyperparathyroidism, infection, psoriasis, renal failure, urinary retention.

    Pregnancy and lactation:

    Pregnancy

    The drug Sodalite is contraindicated for use during pregnancy, especially in the first trimester, except for cases when lithium therapy is strictly necessary. Lithium carbonate penetrates the placental barrier. The use of lithium carbonate during pregnancy, especially in the I trimester increases the risk of birth defects, especially the cardiovascular system: especially Ebstein anomaly (hypoplasia of the right ventricle and tricuspid valve).

    If pregnancy occurs during the use of the drug, the patient should be warned about possible risks to the fetus. As prenatal diagnosis, such patients need an ultrasound, as well as an electrocardiogram of a newborn in the postnatal period.

    In certain cases, when lithium cancellation is characterized by a serious risk to the patient, treatment during pregnancy can be continued.

    In the event that continuation of lithium therapy during pregnancy is necessary, the serum lithium level should be carefully monitored by frequent measurement. This is due to a gradual change in kidney function during pregnancy, and a sudden change in kidney function. The dose should be adjusted. It is recommended to stop lithium intake shortly before birth and resume - a few days after them.

    Newborns with signs of lithium intoxication need to undergo infusion therapy. Newborns with a low concentration of lithium in the blood can have a sluggish appearance that does not require special treatment.

    Women with childbearing potential

    Women receiving lithium carbonate, should use adequate methods of contraception. When planning pregnancy, lithium therapy should be discontinued.

    Breastfeeding period

    It is known that lithium carbonate penetrates into breast milk, so if you need to use the drug during lactation, you should decide whether to quit breastfeeding.

    Dosing and Administration:

    Inside (for 3-4 reception, the last time - before going to bed), after eating,the initial dose is 0,6-0,9 g / day with the subsequent increase to 1,2 g / day, then the dose is daily increased by 0,3 g until a daily dose of 1,5-2,1 g; the maximum daily dose is 2.4 g. During the selection of therapy, the ion concentration Li+ in plasma should not be less than 0.6 and not higher than 1.2-1.6 mmol / l. In doses exceeding 2 g / day, the duration of treatment is 1-2 weeks.

    After the disappearance of manic symptoms, the daily dose is gradually reduced to a preventive dose (0.6-1.2 g). If after a dose reduction, signs of mania appear again, the dose is increased.

    In acute mania, the therapeutic concentration of ions Li+ in blood should be 0,8-1,2 mmol / l, with maintenance treatment - 0,4-0,8 mmol / l; if the concentration of ions Li+ exceeds 1.2 mmol / l, the daily dose should be reduced.

    A positive result of preventive monotherapy is manifested by maintaining a stable concentration in the blood of adults between 0.4-0.8 mmol / l for at least 6 months, children at a dose that allows maintaining therapeutic concentrations in the range of 0.5-1 mmol / l.

    Side effects:

    Side effects are presented depending on the effect on organs and organ systems.

    Side effects usually depend on the concentration of lithium in the serum and are less common in patients with a concentration of lithium below 1.0 mmol / l.

    The beginning of therapy can be accompanied by a small tremor of hands, polyuria and thirst.

    From the blood and lymphatic systems: leukocytosis.

    From the immune system: increase in the titer of antinuclear antibodies.

    From the endocrine system: thyroid disorders, including (euthyroid) goiter, hypothyroidism and hyperthyroidism, hyperparathyroidism, parathyroid adenoma.

    From the side of metabolism and nutrition: hypercalcemia: hypermagnesia; hyperglycemia; anorexia; increase in body weight.

    From the nervous system: coma; idiopathic intracranial hypertension; syndrome of irreversible lithium neurotoxicity (SILENT); encephalopathy; stupor, convulsions; malignant neuroleptic syndrome; myasthenia gravis; serotonin syndrome; Parkinsonism, symptoms of extrapyramidal disorders; ataxia; dizziness; memory disorders, mild cognitive disorder in the case of long-term use; nystagmus; slurred speech; Vertigo: revitalization of deep tendon reflexes; retardation; small tremor of hands.

    From the "side of the organs of vision: scotoma and blurred vision.

    From the heart: heart failure; ventricular fibrillation; ventricular tachycardia; ventricular arrhythmia; tachycardia of the "pirouette" type; interval lengthening QT: cardiomyopathy; arrhythmia; bradycardia; dysfunction of the sinus node; ECG changes.

    From the side of the vessels: insufficiency of peripheral circulation; hypotension.

    From the gastrointestinal tract: gastritis; nausea; diarrhea; vomiting; dry mouth; excessive salivation. Lithium salts can cause a taste perversion.

    From the skin and subcutaneous tissue: an allergic rash; exacerbation of psoriasis; an ugly rash; alopecia; acne; papular rashes; folliculitis; itching; rash.

    From the osteomuscular system and connective tissue: muscle weakness.

    From the side of the kidneys and urinary tract: symptoms of insipid nephrogenic diabetes; kidney failure; irreversible changes in the kidneys; nephrotic syndrome; histological changes in the kidneys with interstitial fibrosis after long-term administration; polyuria; polydipsia.

    From the reproductive system and the breast: sexual dysfunction.

    General disorders and reactions at the injection site: sudden death; edema; asthenia; lethargy; thirst; fatigue and malaise can be a consequence of lithium intoxication.

    Some side effects are noted with an increase in the level of lithium in the blood - see the symptoms in the section "Overdose".

    Overdose:

    Lithium carbonate has a narrow "therapeutic window". Symptoms of lithium overdose (lithium intoxication) can be a consequence of concomitant diseases, iatrogenic and poisoning.

    Any overdose in a patient on long-term lithium therapy should be considered a potentially serious condition.

    Acute overdose

    Acute overdose usually carries a slight risk; patients have exceptionally mild symptoms, regardless of the concentration of lithium in the blood serum. However, later, with a decrease in the rate of lithium excretion due to the presence of renal insufficiency, more severe symptoms may appear. The lethal dose for a single dose is likely to exceed 5 g.

    Acute overdose the patients who are on long-term lithium therapy

    Acute overdose in a patient who is on long-term lithium therapy can lead to severe toxic effects, even with a moderate overdose, as extravascular tissues are already saturated with lithium.

    In patients with elevated lithium concentration in the blood, the risk of toxic effects is higher in the presence of the following pathological conditions: arterial hypertension, diabetes mellitus, congestive heart failure, chronic renal failure, schizophrenia, Addison's disease.

    Symptoms

    The onset of symptoms can be delayed; their maximum severity can reach no earlier than 24 hours; especially in patients who do not receive lithium therapy for a long time.

    Mild symptoms: nausea; diarrhea; blurred vision; polyuria; dizziness; a small tremor of rest; muscle weakness and drowsiness.

    Moderate symptoms: progressive confusion; loss of consciousness; fasciculation; revitalization of deep tendon reflexes; myoclonic muscle contractions and twitchings; choreoathetoid movements; incontinence of urine or feces; progressive agitation with a subsequent stupor; hypernatremia.

    Severe symptoms: coma; convulsions; cerebellar symptoms; cardiac arrhythmia, including sinoatrial block; sinus and nodal bradycardia; heart block of the first degree; arterial hypotension or, rarely, hypertension; vascular insufficiency; renal insufficiency.

    Tactics

    Antidote for poisoning with lithium is not known.

    In the case of accumulation of lithium, it is necessary to stop taking it and assess its concentration in the blood every six hours. Particular attention should be paid to maintaining a balance of fluid and electrolytes, as well as kidney function. Forced diuresis and diuretics should not be used under any circumstances. The necessary supportive therapy may include measures to control hypotension and seizures.

    All patients should be monitored for a minimum of 24 hours. If symptoms are present, ECG monitoring is necessary. Measures should be taken to correct hypotension.

    When taking the drug at a dose of more than 4 g adults or in a large number of children need to wash the stomach - no later than an hour later. With chronic accumulation, decontamination of the intestine is not effective.

    Note: Activated carbon does not absorb lithium.

    With severe poisoning, the therapy of choice is hemodialysis. It should be administered to all patients with severe neurologic symptoms. This method is most effective for rapid reduction of lithium level. However, after the termination of dialysis, it may be reversed. This may require prolonged or repeated treatment. Hemodialysis, also, can be prescribed with acute overdose, acute overdose against long-term therapy, overdose with prolonged therapy to patients with severe symptoms, regardless of the concentration of lithium in the serum. Note: Improvement of the condition usually takes longer than a decrease in serum lithium concentration, regardless of the method used.

    Interaction:

    Interactions can arise as a result of increasing or decreasing the concentration of lithium, or, through other mechanisms, the most important of which is the neurotoxicity that can occur with therapeutic concentrations of lithium in the case of co-administration with other drugs that are centrally acting on CNS.

    Interactions leading to increased serum lithium concentrations

    Co-administration of the following drugs may increase the concentration of lithium and the risk of toxic effects:

    Any drug that is capable of causing kidney failure can potentially increase the concentration of lithium, thus causing toxic effects. In case the use of the drug is strictly necessary, requires careful monitoring of the level of lithium in the blood and dose adjustment if necessary.

    - Antibiotics (metronidazole, tetracycline, co-trimoxazole, trimethoprim). N.B. Symptoms of toxic effects can occur with low or normal lithium concentrations when co-trimoxazole or trimethoprim are co-administered. The toxic effect of lithium has been noted in individual cases in patients taking spectinomycin.

    - Non-steroidal anti-inflammatory drugs (including selective inhibitors of COX-2); in the case of initiation or discontinuation of therapy with non-steroidal anti-inflammatory drugs, more frequent monitoring of the serum lithium concentration is necessary.

    - Medications that affect the renin-angiotensin system (ACE inhibitors, angiotensin II receptor antagonists).

    Diuretics (including herbal remedies). In addition to the above-mentioned types of exposure, thiazide diuretics demonstrate a paradoxical antidiuretic effect, as a result of which water retention and lithiation intoxication are possible. Loop diuretics (furosemide and bumeganid, ethacrynic acid) are less likely to cause lithium delay, however, care must be taken.

    - Other drugs that affect the electrolyte balance, for example, steroids, can change the rate of lithium removal, and therefore it is necessary to avoid their joint application.


    Interactions leading to a decrease in serum lithium concentration:


    Co-administration of the following drugs may lead to a decrease in lithium concentration and a risk of decreased efficacy:

    - The xanthine derivatives (for example, theophylline, caffeine);

    - Preparations containing large amounts of sodium, for example bicarbonate sodium;

    - Inhibitors of carbonic anhydrase;

    - Urea.

    Interactions that can be not associated with an increase or decrease in the concentration of lithium:

    The joint administration of the following drugs may accelerate the appearance of symptoms of toxic effects at a lithium concentration within the normal range:

    - Antipsychotic drugs, including atypical antipsychotics: high doses of olanzapine, clozapine, and haloperidol;

    - Carbamazepine;

    - Phenytoin;

    - Methyldopa;

    - Clonazepam;

    - Tricyclic and tetracyclic antidepressants;

    - Calcium channel blockers; These drugs can cause neurotoxic reactions in therapeutic doses;

    - Neuromuscular blockers; Lithium can cause neurotoxic reactions in therapeutic doses.

    Selective serotonin reuptake inhibitors: co-administration with lithium can exacerbate serotonin syndrome. Non-steroidal anti-inflammatory drugs, including selective inhibitors of COX-2: at the beginning or discontinuation of treatment with non-steroidal anti-inflammatory drugs, more frequent monitoring of serum lithium concentration is necessary.

    Triptans: toxic effects of lithium,resembling a serotonin syndrome.

    Neuromuscular blockers: lithium can prolong the action of neuromuscular blockers.

    Drugs that reduce the convulsive threshold

    It is advisable to use caution when co-prescribing lithium and drugs that reduce the convulsive threshold, such as antidepressants, antipsychotics, anesthetics and theophylline.

    Drugs that extend the interval QT

    Lithium can lengthen the interval QT, especially, with its increased concentration in the blood. Thus, it is necessary to avoid co-administration of drugs with a potential risk of lengthening the interval QT. and also take into account other potential risk factors, such as: old age, female sex. congenital elongated interval syndrome QT, diseases of the heart and thyroid and metabolic disorders such as hypokalemia, hypocalcemia and hypomagnesemia.

    The following drugs may cause lengthening of the interval QT and tachycardia such as "pirouette":

    - Antiarrhythmic drugs class Ia (aymalin, cibenzoline, disopyramide, hydroquinidine, procainamide, quinidine);

    - Antiarrhythmic drugs class III (amiodarone, azimilide, cibenzoline, dofetilidem, ibutilide. sotalol);

    - Antipsychotic drugs (amisulpride, haloperidol, droperidol. mesoridazine, pimozide, sertindole, thioridazine and clozaril);

    - Antibiotics (erythromycin, sparfloxacin with intravenous administration);

    - Antagonists of serotonin receptors (kstapserin, dolasetron mesylate);

    - Antihistamines (ascemisol, terfenadine);

    - Antimalarial drugs (artemisinin derivatives, mefloquine, halofantrine);

    - Other: arsenic trioxide, cisapride and ranolazine.

    ECG monitoring should be performed after initiation of treatment; when the patient develops symptoms or changes in the course of the disease or therapy associated with an increased risk of interaction or arrhythmia.

    Non-drug interactions:

    - A diet low in sodium. Rapid reduction in sodium intake may cause an increase in lithium levels.

    - Concomitant disease can cause lithium toxicity.

    Special instructions:

    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 blood plasma.If there is no possibility of regular measurement of the concentration of lithium in blood plasma, therapy should begin.

    Elderly patients often require lower doses of lithium to achieve a therapeutic drug concentration. They are most susceptible to the toxic action of lithium; the excretion of lithium can also be reduced. Symptoms of toxicity in elderly patients can develop at lithium concentrations in the blood, which are transferred satisfactorily to young patients.

    Since information on the safety and efficacy of lithium carbonate in children under the age of 12 years is not available, its use in this category of patients is contraindicated.

    Prior to the appointment of long-term therapy with lithium drugs, in order to avoid the development of toxic effects, a thorough medical examination before and during treatment is necessary. Before the appointment of the drug should evaluate the function of the kidneys, thyroid (before the initiation of lithium therapy the patient must be in the euthyroid state) and the cardiovascular system, especially in patients with diseases of the cardiovascular system.Against the background of treatment, a periodic evaluation of the function of the kidneys, the thyroid gland and the cardiovascular system is required.

    It is known that lithium carbonate reduces the reabsorption of sodium in the renal tubules, which can lead to a decrease in the concentration of sodium. Thus, it is extremely important for patients to follow a diet, including adequate fluid intake (2500-3000 ml) and table salt, at least during the stabilization period. There was a decrease in tolerance to lithium after profuse sweating or diarrhea. In such cases, an additional the intake of liquid and table salt under medical supervision, as well as a reduced dose or temporary discontinuation of the drug until the condition is resolved.

    During the first month of therapy, the concentration of ions Li+ in blood plasma is determined weekly, then, after reaching a stable concentration, the control is carried out monthly, then in 2-3 months. Return to weekly monitoring is required when changing the dosage of lithium carbonate; presence of an intercurrent infectious or other serious disease; significant changes in the amount of sodium and / or liquid produced; taking medications that alter the renal clearance of lithium; taking drugs that affect the 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 the symptoms of developing toxicity, and also recommend the immediate recourse to medical care in the event of such symptoms.

    Effects of toxic effects are expected at a concentration of lithium in the blood serum of about 1.5 mmol / l, however, it is possible their manifestation even at lower concentrations. When toxic effects occur, treatment should be immediately discontinued and always takes this very seriously.

    At the beginning of treatment, it can provoke depression or a manic condition.

    Against the background of therapy with the drug, it is possible to change the results of laboratory tests (including leukocytosis, a decrease in the concentration of thyroxin and triiodothyronine, a decrease in creatinine clearance, albuminuria, etc.)

    The intake of lithium carbonate should be discontinued 24 hours before a large surgical intervention.During surgery in the volume of small surgery, treatment can be continued provided that the level of fluid and electrolytes is properly monitored.

    With renal failure, lithium excretion decreases, which increases the risk of developing toxic reactions. Lithium is contraindicated in patients with severe renal insufficiency. With renal insufficiency of mild and moderate severity, careful monitoring of lithium concentration in blood plasma is required. Control of kidney function is also required for patients with polyuria and polydipsia.

    Patients on long-term lithium therapy were noted to have morphological changes in the kidney in the form of glomerular interstitial fibrosis and nephron atrophy. Morphological changes were also noted in patients with manic-depressive conditions, who were never prescribed lithium. The relationship between kidney function, morphological changes and lithium therapy has not been proven. In patients taking medications that reduce the epileptic threshold and in patients with epilepsy in the appointment of lithium carbonate, the risk of developing convulsive conditions increases.

    It is not recommended to prescribe lithium carbonate together with neuroleptics. Some patients taking lithium together with neuroleptics 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. In connection with the existence of a possible causal relationship between the development of encephalopathic syndrome and the joint use of lithium and neuroleptics, it is necessary to carefully monitor patients on combined treatment for the early detection of neurological toxicity requiring immediate cessation of treatment. Encephalopathic syndrome may occur similarly or similarly to a malignant neuroleptic syndrome.

    Do not share with antipsychotic drugs.

    Avoid prescribing lithium carbonate to patients with congenital lengthening of the interval QT. as well as patients taking medications that can increase the interval QT. Caution should be exercised in patients with risk factors for lengthening the interval QT, which, above all, include heart disease, bradycardia, thyroid disease, hypokalemia, hypomagnesemia, hypocalcemia. female sex and advanced age.

    Lithium therapy may exert or aggravate the course of Brugada syndrome, a hereditary disease associated with the sodium channels of the heart with characteristic changes on the ECG (right bundle branch blockade and segment elevation ST in the right thoracic leads), which can lead to cardiac arrest or sudden death. Lithium carbonate should not be used in patients with Brugada syndrome, or with a family history of Brugada syndrome. Patients with cardiac arrest or sudden death in a family history should be administered with caution.

    Long-term therapy with the drug may be associated with a decrease in the concentration ability of the kidneys, which contributes to the development of nephrogenic diabetes insipidus, with polyuria and polydipsia. Such patients need to be closely monitored kidney function, and lack of dehydration due to lithium retention and toxicity.As a rule, these changes are reversible and regress after termination of therapy with the drug. There are data on the occurrence of hyperparathyroidism and hypothyroidism, which persist even after the drug is discontinued.

    There are data on reported cases of increased intracranial pressure and edema of the optic nerve disk (false brain tumor syndrome). With the development of this syndrome, therapy with the drug should be discontinued. Patients should be warned about the need to report to a doctor about cases of intermittent headache and / or visual disturbances.

    Patients who are prescribed long-term lithium carbonate therapy should be instructed in relation to symptoms of toxicity and should be instructed to consult a doctor immediately if the first signs of such symptoms appear.

    On the background of drug therapy, the following pathological changes can be recorded on the electroencephalogram: diffuse deceleration, expansion of the frequency spectrum, potentiation and disorganization of the background rhythm.

    Effect on the ability to drive transp. cf. and fur:

    Care should be taken when driving vehicles and other potentiallyhazardous activities, as some side effects of lithium carbonate on the central nervous system, such as drowsiness, can adversely affect the ability to drive and perform potentially dangerous activities requiring increased concentration and speed of psychomotor reactions.

    Form release / dosage:Film coated tablets 300 mg.
    Packaging:

    For 10 tablets in a contour mesh box made of PVC film and aluminum foil printed lacquered.

    For 5 contour mesh packages together with the instruction is placed in a pack of cardboard.
    Storage conditions:Store at a temperature not exceeding 25 ° C.
    Keep out of the reach of children.
    Shelf life:

    3 years. At the end of the expiration date the drug should not be used.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001453/07
    Date of registration:09.07.2007
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.09.2015
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