Sedalite
Sedalite: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Sedalit
ATX code: N05AN01
Active ingredient: lithium carbonate (lithium carbonate)
Producer: Pharmstandard-Leksredstva, JSC (Russia)
Description and photo update: 03.10.2019
Prices in pharmacies: from 108 rubles.
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Sedalite is a lithium preparation.
Release form and composition
Sedalit dosage form - film-coated tablets: biconvex, white, round (10 pcs. In blisters, 5 packs in a cardboard box and instructions for use of Sedalit).
Composition of 1 tablet:
- active substance: lithium carbonate - 300 mg;
- auxiliary components: calcium stearate - 4 mg; croscarmellose sodium (primellose) - 20 mg; potato starch - 14.62 mg; talc - 6 mg; povidone (polyvinylpyrrolidone, povidone K-25) - 55.38 mg;
- shell: titanium dioxide - 2.1 mg; talc - 1.65 mg; povidone (polyvinylpyrrolidone, povidone K-25) - 1.837 mg; hydroxypropyl methylcellulose (hypromellose) - 5.87 mg; polysorbate 80 (tween-80) - 0.543 mg.
Pharmacological properties
Pharmacodynamics
Sedalite is one of the normotimal (normalizing mental state and not causing general inhibition) means. It also has antidepressant, anti-manic and sedative effects.
The Sedalite effect is caused by lithium ions (Li +), which displace sodium ions (Na +) from cells, being their antagonists. Due to this, the bioelectrical activity of brain neurons decreases.
Other effects of Sedalite:
- acceleration of the breakdown of biogenic amines (the content of serotonin and norepinephrine in the brain tissues decreases);
- increasing the sensitivity of neurons in the hippocampus and other areas of the brain to the effects of dopamine;
- interaction of lithium carbonate with lipids, which are formed during the metabolism of inositol.
When using lithium carbonate in therapeutic concentrations, the activity of inosyl 1- phosphatase is blocked and the concentration of neuronal inositol, which is involved in the regulation of neuronal sensitivity, decreases.
In migraine, the beneficial effect of lithium preparations may be due to a change in serotonin concentrations, in depression - a decrease in the regulation of beta-adrenergic receptor function and an increase in serotonergic activity.
Pharmacokinetics
The absorption of lithium carbonate is fast (in 6–8 hours) and complete. The substance does not bind to blood proteins. The therapeutic range of blood concentrations is 0.6–1.2 mmol / L. The time to reach C max (maximum concentration of the substance) in the blood is 1–3 hours. A stable serum concentration in the blood is achieved within 4 days.
Lithium carbonate penetrates through the blood-brain (cerebrospinal fluid concentrations are 1/2 of the plasma level) and placental barriers, as well as into breast milk.
The substance does not undergo biological transformation. T 1/2 (half-life) is: adults - 24 hours, adolescents - 18 hours, elderly patients - up to 36 hours. T 1/2 values are determined by the amount of Na + ions in the plasma.
Excretion: 95% - with urine, up to 1% - with feces, 4-5% - with sweat. Excretion by the kidneys depends on the ratios of the concentrations of Li +, K + and Na + ions in the blood.
Indications for use
- migraine;
- manic and hypomanic states of various origins;
- affective psychoses (schizoaffective, manic-depressive);
- sexual disorders;
- Meniere's syndrome;
- some forms of drug dependence;
- alcoholism (affective disorders).
Contraindications
Absolute:
- leukemia;
- heavy surgery;
- diseases of the cardiovascular system associated with heart rhythm disturbances;
- the presence of Brugada syndrome and a burdened history;
- severe renal failure;
- hypothyroidism (uncompensated or untreated);
- low sodium levels in the body, for example, with Addison's disease, dehydration, following a salt-free diet;
- pregnancy and the period of breastfeeding;
- age up to 12 years (the safety profile for this category of patients has not been studied);
- hypersensitivity to the components of the drug, as well as to lithium.
Relative (the appointment of Sedalit requires caution in the presence of such diseases / conditions as):
- hyperparathyroidism;
- thyrotoxicosis;
- retention of urine;
- diseases of the cardiovascular system (including atrioventricular and intraventricular blockade);
- diabetes;
- psoriasis;
- infections;
- diseases of the central nervous system (epilepsy, parkinsonism);
- renal failure.
The use of Sedalit by pregnant women, especially during the first trimester, increases the likelihood of congenital defects, mainly of the cardiovascular system. Taking the drug is possible only for health reasons.
Sedalite, instructions for use: method and dosage
Sedalite tablets are taken orally, preferably after a meal.
The initial daily dose is 600-900 mg (3-4 doses, the last one - in the evening before bedtime). Then it is increased to 1200 mg, then - by 300 mg daily until it reaches 1500–2100 mg. The plasma concentration of lithium during the selection of therapy should be in the range from 0.6 to 1.2-1.6 mmol / l.
The maximum daily dose of Sedalit is 2400 mg.
The duration of treatment when taking Sedalit from 2000 mg per day is 1–2 weeks.
After the disappearance of manic symptoms, the daily dose is gradually reduced to a prophylactic dose of 600–1200 mg. In cases of resumption of symptoms of the disease, the dose is increased.
The therapeutic concentration of lithium ions in the blood in an acute manic state should be in the range of 0.8-1.2 mmol / l, with maintenance therapy - 0.4-0.8 mmol / l. If the concentration exceeds 1.2 mmol / l, the daily dose is reduced.
The positive result of prophylactic monotherapy with Sedalite is manifested while maintaining a stable concentration in the blood:
- adults: in the range of 0.4–0.8 mmol / l for at least 6 months;
- children: in the range of 0.5-1 mmol / l.
Side effects
Adverse reactions, as a rule, depend on the serum concentration of lithium; more rarely, they are observed in patients with a lithium concentration of up to 1 mmol / L.
Disturbances characteristic of the beginning of the use of Sedalit: minor tremor of the hands, thirst, polyuria.
Possible side effects:
- cardiovascular system: bradycardia, ventricular arrhythmia, cardiac arrest, ventricular fibrillation, ventricular tachycardia, pirouette-type tachycardia, hypotension, prolongation of the QT interval, cardiomyopathy, arrhythmia, peripheral circulatory failure, ECG changes, sinus node dysfunction;
- digestive system: dry mouth, gastritis, nausea, vomiting, taste perversion, diarrhea, excessive salivation;
- musculoskeletal system: muscle weakness;
- immune system: an increase in the titer of anti-nuclear antibodies;
- nervous system: encephalopathy, coma, memory disorders, stupor, idiopathic intracranial hypertension, neuroleptic malignant syndrome, irreversible lithium neurotoxicity syndrome (SILENT), convulsions, myasthenia gravis, serotonin syndrome, parkinsonism, symptoms of extrapyramidal disorders, dizziness, dizziness, ataxnitic cases of prolonged therapy), slurred speech, vertigo, nystagmus, revitalization of deep tendon reflexes, minor tremors of the hands, lethargy;
- lymphatic and circulatory system: leukocytosis;
- endocrine system: thyroid dysfunction, including (euthyroid) goiter, hyperthyroidism and hypothyroidism, hyperparathyroidism, parathyroid adenoma;
- reproductive system: sexual dysfunction;
- metabolism and nutrition: hypermagnesemia, anorexia, hypercalcemia, hyperglycemia, weight gain;
- kidneys and urinary tract: polyuria, symptoms of nephrogenic diabetes insipidus, polydipsia, renal failure, irreversible changes in the kidneys, nephrotic syndrome, histological changes in the kidneys with interstitial fibrosis (develop after prolonged treatment);
- skin and subcutaneous tissue: rash, acne-like rash, folliculitis, exacerbation of psoriasis, allergic rash, alopecia, papular rash, acne, itching;
- organ of vision: blurred vision, scotoma;
- general disorders: sudden death, lethargy, edema, asthenia, thirst, malaise and fatigue (disorders may be associated with lithium intoxication).
Overdose
Lithium carbonate has a narrow therapeutic window. Symptoms of lithium intoxication (lithium overdose) can occur due to concomitant diseases, poisoning and iatrogenism.
Any overdose with long-term Sedalite therapy should be considered a potentially serious condition.
Acute overdose is usually a minor risk. It manifests itself with extremely mild symptoms, regardless of the serum concentration of lithium in the blood. However, later, when the rate of lithium excretion is reduced due to renal failure, more severe symptoms may appear. A lethal single dose is likely to be greater than 5 g.
In acute overdose in patients undergoing long-term lithium therapy, severe toxic effects may develop, even in cases of moderate overdose, which is associated with saturation of extravascular tissues with lithium.
With an increased concentration of lithium in the blood, the likelihood of toxic effects increases in the presence of the following diseases / conditions: congestive heart failure, arterial hypertension, diabetes mellitus, chronic renal failure, Addison's disease, schizophrenia.
The onset of symptoms of an overdose of Sedalite can be delayed, their maximum severity can appear after 24 hours. This is especially true for patients who have not received long-term lithium therapy.
Symptoms:
- lungs: dizziness, diarrhea, nausea, blurred vision, polyuria, minor tremor at rest, drowsiness, muscle weakness;
- moderate: myoclonic twitching and muscle contractions, choreoathetoid movements, hypernatremia, fecal or urinary incontinence, loss of consciousness, progressive confusion, fasciculations, revival of deep tendon reflexes, progressive excitement followed by stupor;
- severe: cerebellar symptoms, cardiac arrhythmia (including sinoatrial blockade), nodular and sinus bradycardia, first-degree heart block, arterial hypotension (in rare cases, hypertension), renal and vascular insufficiency, convulsions, coma.
The antidote for Sedalite poisoning is unknown. Activated carbon does not absorb lithium.
With the accumulation of lithium, you need to stop taking Sedalite and evaluate its concentration in the blood every six hours. Particular attention should be paid to maintaining the balance of electrolytes and fluids, as well as the functional state of the kidneys. Forced diuresis and diuretics are categorically contraindicated. Necessary supportive care may include measures to control hypotension and seizures.
The patient's condition must be monitored for at least 24 hours. According to the indications, ECG control is prescribed. It is necessary to take measures to correct hypotension.
In the case of taking Sedalit in a dose of more than 4 g by adults, or in a significant amount by children, gastric lavage is prescribed (no later than an hour later). With chronic lithium accumulation, bowel decontamination is ineffective.
In severe cases, hemodialysis is the therapy of choice. It is indicated for all patients with severe neurological symptoms. This method is recognized as the most effective method for rapidly reducing lithium levels. However, after the cessation of dialysis, a reverse increase in the level of lithium is possible. This may require prolonged or repeated treatment. Also, hemodialysis can be prescribed in case of acute overdose, acute overdose during prolonged therapy, overdose during prolonged therapy in patients with severe symptoms, regardless of the serum concentration of lithium. It should be borne in mind that usually the improvement of the condition, regardless of the method used, takes a longer period of time than the decrease in serum lithium concentration.
special instructions
Lithium carbonate has a narrow therapeutic window. The required dose of Sedalit should be carefully selected and, based on the data on the plasma concentration of lithium, regularly adjusted. It is impossible to start therapy if it is not possible to regularly measure the concentration.
Older patients generally require lower doses to achieve therapeutic concentrations of lithium carbonate. This category of patients is most susceptible to the toxic effects of lithium. Symptoms of toxicity in them can be observed at concentrations of lithium in the blood, which are satisfactorily tolerated by patients of younger age.
A thorough medical examination before / during long-term therapy reduces the likelihood of toxic effects. Examination includes: assessment of the function of the thyroid gland (before the appointment of Sedalit, the patient must be in a euthyroid state), kidneys and the cardiovascular system (in particular, this applies to patients with pathologies of the cardiovascular system).
During the treatment period, it is extremely important for patients to follow a diet that includes adequate fluid intake (2.5 to 3 liters) and table salt (at least during the stabilization period; Sedalite reduces sodium reabsorption in the renal tubules, which can lead to a decrease in sodium concentration). After profuse sweating or diarrhea, a decrease in lithium tolerance is usually noted (additional intake of sodium chloride and liquid under medical supervision is required, as well as, until the condition resolves, a dose reduction or a temporary cessation of therapy).
During the first month of taking Sedalit, the plasma concentration of lithium ions is determined weekly, after reaching a stable concentration - monthly, then - once every 2-3 months.
It is necessary to return to the weekly concentration control in the following cases:
- changing the dosage regimen;
- the presence of an intercurrent infectious or other serious illness;
- combined use with drugs that affect the renal clearance of lithium or electrolyte balance;
- significant changes in the amount of liquid / sodium received.
A blood sample should be taken only in the morning: after taking the last dose at night - after 12 hours; after taking a single dose in the morning - after 24 hours.
If signs of developing toxicity appear against the background of prolonged use of Sedalit, it is necessary to urgently consult a specialist.
The toxic effects of Sedalite are expected at a serum lithium concentration of about 1.5 mmol / L, but in some cases they may appear at lower concentrations. In cases of toxic effects, therapy is immediately discontinued.
At the beginning of the course, depression or manic states may develop.
Taking Sedalite can change the results of laboratory tests, including leukocytosis, a decrease in the concentration of thyroxine and triiodothyronine, a decrease in creatinine clearance, etc.
Before major surgical interventions, therapy should be interrupted 24 hours in advance. For operations in the volume of minor surgery, provided that the level of electrolytes / fluid is properly controlled, therapy can be continued.
Features of the use of Sedalite in renal failure (due to an increased likelihood of toxic reactions):
- mild and moderate: close monitoring of plasma lithium concentration is necessary;
- severe: use is contraindicated.
It is also necessary to monitor kidney function for polyuria and polydipsia.
It should be borne in mind that against the background of taking drugs that reduce the epileptic threshold, and with epilepsy, taking Sedalit increases the likelihood of convulsive conditions.
Due to the risk of encephalopathic syndrome, combined use with antipsychotics is not recommended. The main symptoms of encephalopathic syndrome are weakness, apathy, fever, trembling, confusion, extrapyramidal symptoms, leukocytosis, etc. Sometimes this disorder develops in combination with irreversible brain damage. In order to timely identify neurological toxicity, requiring immediate discontinuation of therapy, careful monitoring of the patient's condition is required. It should be borne in mind that encephalopathic syndrome can proceed similarly to neuroleptic malignant syndrome.
Combined use with antipsychotic drugs is unacceptable.
Long-term use of Sedalit may be associated with a decrease in the concentration of the kidneys, which contributes to the development of nephrogenic diabetes insipidus in combination with polydipsia and polyuria. This category of patients should be carefully monitored for the functional state of the kidneys, as well as the absence of dehydration associated with lithium retention and its toxicity. As a rule, such changes are reversible and go away after you stop taking Sedalit. There is information about the development of hypothyroidism and hyperparathyroidism, which persist even after discontinuation of treatment.
During therapy, the following pathological changes on the electroencephalogram may develop: expansion of the frequency spectrum, diffuse slowing down, disorganization and potentiation of the background rhythm.
Cases of increased intracranial pressure and edema of the optic nerve head (false brain tumor syndrome) have been reported. In case of recurrent visual disturbances and / or headaches, it is necessary to consult a specialist. In cases of development of a false brain tumor syndrome, Sedalite is canceled.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy, when driving vehicles and performing other potentially hazardous work, patients must be careful, which is associated with some adverse reactions of Sedalit, including drowsiness.
Application during pregnancy and lactation
Sedalite is not prescribed during pregnancy / lactation.
In the case of the use of lithium carbonate during pregnancy, especially in the first trimester, the likelihood of congenital defects, mainly defects of the cardiovascular system, increases. First of all, this refers to Ebstein's anomaly (tricuspid valve insufficiency and right ventricular hypoplasia).
If pregnancy occurs during therapy, an ultrasound examination is recommended as a prenatal diagnosis, and an electrocardiogram of the newborn is prescribed in the postnatal period.
In certain cases, if the withdrawal of Sedalit is a serious risk for the patient's condition, the drug is not canceled. This requires careful monitoring of serum lithium levels through frequent measurements. This is due to a gradual change in renal function during pregnancy, and a dramatic change during childbirth. In this regard, the dose of Sedalit requires correction. Reception of lithium is recommended to be canceled shortly before childbirth, in a few days after them treatment can be resumed.
The condition of newborns with signs of lithium intoxication requires infusion therapy. Newborns with a low concentration of lithium in the blood may appear lethargic and do not require special treatment.
When planning a pregnancy, Sedalit should be discontinued. Women receiving lithium carbonate should use adequate contraception.
Pediatric use
Sedalite is not prescribed for patients under 12 years of age.
With impaired renal function
- severe renal failure: therapy is contraindicated;
- renal impairment: Sedalite tablets should be used under medical supervision.
Drug interactions
Interactions of Sedalite can occur due to a change (decrease or increase) in the concentration of lithium or through other mechanisms, the most important of which is neurotoxicity, which can occur at therapeutic concentrations of lithium in the case of combined use with other drugs that centrally affect the central nervous system.
Concomitant use leading to an increase in serum lithium concentration and the likelihood of toxic effects:
- non-steroidal anti-inflammatory drugs, including selective COX-2 inhibitors (in the case of starting or ending therapy with these drugs, more frequent monitoring of serum lithium concentration is required);
- any medicinal products that may result in renal failure (if combination therapy is necessary, the level of lithium in the blood should be carefully monitored; dose adjustment may be required);
- antibiotic drugs (metronidazole, co-trimoxazole, tetracycline, trimethoprim);
- diuretics, including herbal preparations (thiazide diuretics - a paradoxical antidiuretic effect is likely to develop, as a result of which lithium intoxication and water retention are possible; loop diuretics (bumetanide, furosemide, ethacrynic acid) - lithium retention is less common, but combined use requires caution);
- drugs that affect the renin-angiotensin system (angiotensin II receptor antagonists, ACE inhibitors);
- other medicines that affect electrolyte balance (for example, steroids).
Combined use leading to a decrease in serum lithium concentration and the likelihood of a decrease in efficacy:
- xanthine derivatives (eg caffeine, theophylline);
- Medicines with high sodium content (such as sodium bicarbonate)
- urea;
- carbonic anhydrase inhibitors.
Combined use, leading to an acceleration of the onset of symptoms of toxic effects at concentrations of lithium that are in the normal range:
- tetracyclic / tricyclic antidepressants;
- antipsychotic drugs, including atypical antipsychotics, high doses of haloperidol, clozapine, olanzapine;
- phenytoin;
- carbamazepine;
- clonazepam;
- methyldopa;
- calcium channel blockers (the likelihood of developing neurotoxic reactions);
- selective serotonin reuptake inhibitors: (the likelihood of exacerbation of serotonin syndrome);
- neuromuscular blockers (the likelihood of prolonging their action, as well as the development of neurotoxic reactions);
- triptans (the likelihood of developing toxic effects of lithium, resembling serotonin syndrome).
Also, caution is required when using Sedalit in combination with any drugs that lower the seizure threshold (for example, antidepressants, antipsychotics, theophylline, anesthetics).
Combined use, leading to a prolongation of the QT interval and the development of tachycardia such as pirouette (Sedalite can prolong the QT interval, especially with an increased concentration of lithium in the blood; combined use with drugs that have a potential risk of prolongation of the QT interval should be avoided; other potential risk factors: female gender, old age, congenital long QT syndrome, heart and thyroid diseases, and metabolic disorders such as hypocalcemia, hypokalemia and hypomagnesemia):
- antagonists of serotonin receptors (dolasetron mesylate, kstapserin);
- class Ia antiarrhythmic drugs (cybenzoline, aymalin, disopyramide, procainamide, hydroquinidine, quinidine);
- class III antiarrhythmic drugs (dofetilide, amiodarone, cybenzoline, azimilide, ibutilide, sotalol);
- antibiotics (erythromycin, intravenous sparfloxacin);
- antipsychotics (sertindole, amisulpride, haloperidol, mesoridazine, droperidol, pimozide, clozaril, thioridazine);
- antimalarial drugs (mefloquine, artemisinin derivatives, halofantrine);
- antihistamines (terfenadine, astemizole);
- others: arsenic trioxide, ranolazine, cisapride.
Sedalite non-drug interactions:
- concomitant diseases that can cause lithium toxicity;
- a low sodium diet (chances of increased lithium levels).
Analogs
Sedalit's analogues are: Contemnol, Litosan-SR, Mikalit, Kvilonum.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Sedalite
Reviews about Sedalite are different. With a properly selected dosage, the drug has the claimed therapeutic effect. At the same time, they often indicate the development of side effects, the severity of which has wide individual variability.
Price for Sedalite in pharmacies
The approximate price for Sedalite (50 tablets) is 106–129 rubles.
Sedalite: prices in online pharmacies
Drug name Price Pharmacy |
Sedalite 300 mg film-coated tablets 50 pcs. 108 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!