Side effects typical of lithium salts are. Lithium preparations - instructions for use, indications, composition and price

25.05.2020

Drugs that affect kidney function can affect serum lithium concentration, and even a small increase in its concentration can be dangerous, since the therapeutic range of lithium is narrow.
Lithium ions do not affect the activity of liver enzymes and do not undergo biotransformation themselves; they are excreted from the body unchanged.
Interaction with certain classes of drugs:
Antipsychotics. Lithium, if necessary, can be administered concurrently with antipsychotics. There is evidence that, when combined with antipsychotics, reversible neurotoxicity sometimes occurs in middle-aged and elderly people. However, this drug combination is quite safe and effective if antipsychotics and lithium are used in moderate doses and the patient is closely monitored; however, the use of this combination of drugs should be discontinued as soon as the therapeutic effect of lithium is achieved. With a combination of neuroleptics and lithium, tremor can become generalized; some patients also have a peculiar deterioration in their mental state, internal tension, agitation, irritability, explosiveness, emotional lability, impulsivity, impaired memory for current events. Extrapyramidal side effects and hyperkinesias are possible; there have been cases of a clinical picture resembling neuroleptic malignant syndrome. Severe neuroxic reactions occur extremely rarely: for example, acute toxic encephalopathy with deep dullness, cerebral, cerebellar and brainstem neurological symptoms, signs of cerebral edema can develop. Most often, encephalopathy was observed when lithium was combined with haloperidol, but it has also been described when combined with thioridazine, perphenazine and thiothixene. Such factors as high doses of drugs, organic pathology of the central nervous system, the presence of infection, fever, and dehydration predispose to neurotoxic reactions with this combination of drugs. The use of lithium in conjunction with antipsychotics can also lead to an increase in body weight.
Carbamazepine (Finlepsin). The combination of lithium with carbamazepine is used for persistent MDP, however, according to some reports, carbamazepine can increase the side effects of lithium.
In most cases, the combination of carbamazepine and lithium is well tolerated, but in patients at risk (with signs of the neurotoxic effect of lithium or with a history of neurological diseases), symptoms of a neurotoxic effect are possible even with moderate concentrations of drugs in the blood. Both drugs cause hypothyroidism, so thyroid function must be monitored during therapy. Lithium can reduce leukopenia and neutropenia caused by carbamazepine, but lithium is not a prophylactic agent for inhibiting hematopoiesis. It can also reduce carbamazepine-induced hyponatremia.
Valproic acid. Sometimes it can increase the efficiency of lithium in case of permanent TIR
Tricyclic antidepressants (amitriptyline). Lithium can enhance the therapeutic effect of antidepressants, but the risk of intoxication also increases. There are rare cases of seizures when combined with a high dose of amitriptyline and lithium, as well as cardiovascular complications and hypothyroidism while taking lithium and tricyclic antidepressants for more than six months. There is evidence of the appearance of signs of a neurotoxic effect in the form of tremor, memory impairment, distraction, disorganization of thinking even with normal blood lithium concentration and moderate doses of amitriptyline. Serotonin syndrome was diagnosed in a number of patients against the background of a combination of lithium and clomipramine.
Antidepressants are selective serotonin reuptake inhibitors (fluoxetine). The combination of lithium with antidepressants of this group, as a rule, is well tolerated, but it can also cause adverse consequences: intoxication of the central nervous system and arterial hypertension or hypotension. In general, lithium can enhance the serotonergic effect of SSRIs, thereby causing characteristic neurological and gastrointestinal side effects. Cases of serotonin syndrome have sometimes been reported. Antidepressants in this group can increase the side effects of lithium.
Antidepressants are monoamine oxidase inhibitors. The combination of lithium with drugs in this group can cause serotonin syndrome.
Dopaminergic drugs. Against the background of a combination of lithium and levodopa, the development of dyskinesias and hallucinations is possible; when combined with methyldopa, neurotoxic side effects may develop out of proportion to the concentration of lithium in the blood plasma.
Verapamil. The appearance of cardiotoxic and other side effects is possible in patients with neoplastic processes complicated by cardiovascular diseases.
Thyroid hormones. When lithium is combined with thyroxine or liothyronine, the release of thyroid hormone decreases.
Iodine preparations. The combination is not recommended due to the pronounced side effects on the function of the thyroid gland.
Antihypertensive drugs. ACE inhibitors and angiotensin 1 receptor antagonists can increase serum lithium concentration, resulting in lithium intoxication; therefore, it is better to prescribe antihypertensive drugs of other groups (beta-blockers, prazosin) to patients taking lithium. Methyldopa in combination with lithium can cause confusion, tremors, dysarthria, blurred vision, lethargy, and dysphoria. Lithium reduces the hypotensive effect of clonidine.
Diuretics ("diuretics"). When combined with thiazide diuretics (for example, hydrochlorothiazide), lithium excretion decreases and its serum concentration increases, which can lead to lithium intoxication. Potassium-sparing diuretics are safer; data on the combination of lithium with loop diuretics and carbonic anhydrase inhibitors are contradictory. Sometimes lithium is combined with a potassium-sparing or thiazide diuretic to reduce lithium-induced polyuria or nephrogenic diabetes insipidus. Osmotic diuretics decrease the concentration of lithium in the blood, which can lead to a decrease in the effectiveness of therapy and the emergence of "breakthrough" mania or depression.
Some non-steroidal anti-inflammatory drugs (indomethacin, phenylbutazone) increase the reabsorption of lithium in the kidneys and, as a result, its concentration in the blood, which can lead to intoxication. Ketorolac is incompatible with lithium preparations.
Metronidazole, tetracyclines. Serum lithium concentration increases. Cases of severe renal intoxication with the combined use of lithium and metronidazole have been described.
Theophylline, aminophylline. The serum concentration of lithium decreases, which may lead to a decrease in the effectiveness of therapy, the occurrence of mania or depression.
Cardiac glycosides (digitoxin). This combination is not recommended due to the increased toxic effects of lithium and the development of arrhythmias.
Muscle relaxants. Lithium can potentiate their action. If surgical treatment with the use of muscle relaxants is necessary, it is necessary to warn the anesthesiologist about lithium intake and stop taking it 48-72 hours before the operation.
Inhalation anesthetics. It is necessary to discontinue the lithium preparation 1-2 days before the operation.
Caffeine. Lithium-induced tremors may increase.
Ethanol. Lithium relieves alcohol euphoria, reduces alcohol cravings and cognitive impairments caused by alcoholism. Lithium is ineffective for alcohol withdrawal. Like other CNS depressants, ethanol interacts with lithium and can cause sedation or confusion.

REGULATORY AGENTS (LITHIUM SALTS)

Lithium salts for the treatment of manic conditions began to be used since 1949. Only by 1970 was convincing evidence of their high therapeutic efficacy obtained and methods for preventing numerous side effects were developed. An alternative to lithium salts for manic-depressive psychosis can be antipsychotics and antiepileptic drugs - carbamazepine, clonazepam and valproate.

In the 19th century, lithium salts were prescribed for patients with gout, since lithium urate dissolves well in water. In the early 20th century, lithium bromide gained fame as a sedative and anticonvulsant. Among the indications for its use was mania. In the 1940s. cardiologists have suggested replacing part of the table salt of lithium with chloride in the diet of patients with arterial hypertension and heart failure. This has led many patients to severe intoxication, even fatal.

Australian scientist Cade, having isolated toxic nitroso compounds from the urine of mental patients. studied their effect in an experiment on guinea pigs. Simultaneously, the animals received lithium salts to increase the solubility of urates. Lithium carbonate caused lethargy in guinea pigs. In 1949, lithium carbonate was successfully used to treat several patients with mania.

Lithium is the lightest alkali metal (group la). Its chemical properties are the same as sodium and potassium. In biological fluids, the concentration of lithium is determined by flame photometry or atomic absorption spectrophotometry. Traces of lithium are found in mammalian tissues, although its physiological role has not been established.

Lithium ion in therapeutic concentration does not have a psychotropic effect in healthy people (does not cause sedation, depression or euphoria). In patients with manic-depressive psychosis, lithium exhibits anti-manic and normotimic properties (normalizes mood in case of mania and depression).

Lithium ions, penetrating into neurons through fast sodium channels, can cause a single action potential. However, lithium is not cleared from cells. Na/TO-ATP-ase. The lithium gradient between the extracellular environment and the cell cytoplasm is smoothed out. Long retention of lithium in cells alters the transmembrane transport of sodium and potassium ions. This disrupts the electrical processes in the membrane.

In the central nervous system, lithium inhibits the release of dopamine and norepinephrine caused by depolarization and calcium ions, increases neuronal uptake and presynaptic deposition of these neurotransmitters, does not affect dopamine receptors and adrenergic receptors; in the hippocampus increases the release of serotonin; stimulates the synthesis of acetylcholine. It is possible that lithium inhibits the catalytic activity of inositol monophosphatase, which reduces the formation of phosphatidylinositol diphosphate as a substrate of phospholipase C. Lithium also reduces the activity of adenylate cyclase and guanylate cyclase. The enzyme blockade disrupts the production of secondary messengers - diacylglycerol, inositol triphosphate, cAMP and cGMP.

Lithium is rapidly and completely absorbed from the gastrointestinal tract, creating a peak blood concentration 2-4 hours after ingestion. Does not bind to plasma proteins. Slowly penetrates the blood-brain barrier. The concentration of lithium in the brain is 40-50% of the concentration in the blood. Selectively accumulates in the striatum, hypothalamus and pituitary gland.

Approximately 95% of a single dose of lithium is eliminated in the urine (1 / 3-2 / 3 in 6-12 hours, the rest within 10-14 days); 80% is reabsorbed in the proximal convoluted tubule. The half-life is 20-24 hours. With repeated administration, the excretion of lithium accelerates in the first 5-6 days, then a balanced state occurs, when the intake into the body is equal to elimination. In the elderly, lithium excretion slows down.

About 1% of lithium is excreted in feces, 4-5% in sweat. With increased sweating, the elimination of lithium ions prevails over the elimination of sodium ions. The concentration of lithium in saliva is twice that in blood plasma; in tears, it is the same as in blood. Lithium passes into breast milk.

The volume of distribution and clearance of lithium change with hyponatremia (concomitant diseases, a decrease in the amount of water and electrolytes in the body). Lithium retention is caused by butadione, indomethacin and thiazide diuretics. The renal excretion of lithium is accelerated by aminophylline, diacarb. osmotic diuretics, triamterene.

Indications for the appointment of lithium salts are relief of acute mania and prevention of relapse of manic-depressive psychosis. Therapy is carried out only with a sufficient content of sodium ions and normal function of the cardiovascular system and kidneys. In an acute attack of mania, lithium salts reduce expansive euphoric mood disorders and excessive urges. The therapeutic effect comes slowly - after 8-10 days. The preventive action is aimed at lengthening the intervals between the phases of manic-depressive psychosis, suppressing both manic and depressive phases. Only 60-80% of patients are sensitive to lithium salt therapy.

Lithium has a small latitude of therapeutic action, therefore, monitoring of its concentration in the blood is necessary (the analysis is carried out 8-10 hours after ingestion). For effective and safe treatment of acute mania, it is necessary to create a lithium concentration of 0.9-1.1 meq / l, for the prevention of relapse of manic-depressive psychosis - 0.6-1 meq / l. Intoxication can occur when the therapeutic concentration is exceeded by 2-3 times.

The first time the concentration of lithium is determined on the 5th day after the start of treatment, since during this period it becomes stable. With an increase in the lithium dose, the concentration study is repeated after another 5 days. After establishing the optimal therapeutic dose, analyzes are performed less frequently.

Withdrawal of lithium maintenance therapy may be accompanied by a relapse of mania with suicidal attempts.

Lithium salts are used for repeated exacerbations of endogenous depression, schizoaffective disorders, chronic alcoholism,

Lithium preparations are taken orally in tablets and capsules. The most popular was LITHIUM CARBONATE (in tablets with slow release - CONTEMNOL). This salt is characterized by low hygroscopicity and slight irritant effect on the intestines.

LITHIUM OXIBUTIRATE injected into the muscles. Anion GHB gives the drug anti-aggressive. nootropic and antihypoxic properties.

Side effects of lithium are nausea, vomiting, diarrhea, drowsiness, peripheral edema, acne-like rash, allergic reactions (dermatitis, vasculitis). In rare cases, benign diffuse hyperplasia of the thyroid gland develops without significant disruption of hormonal function. The secretion of thyroid-stimulating hormone increases, absorption Y 131 the thyroid gland, the content of iodine-binding protein and thyroxine in the blood decreases moderately. Lithium is thought to interfere with tyrosine iodination. Lithium can cause symptoms of hyperfunction of the parathyroid glands and nephrogenic diabetes insipidus (the sensitivity of kidney adenylate cyclase to the action of vasopressin decreases, thirst, polyuria appear).

Long-term lithium therapy causes chronic interstitial nephritis (renal failure, as a rule, does not develop), insulin-like effects, tooth flattening T on the ECG? leukocytosis, men may develop sexual dysfunction.

A mild degree of lithium intoxication, which occurs at the peak of the therapeutic concentration in the blood, is manifested by a sedative effect, tremors, nausea, vomiting, abdominal pain, and diarrhea. For severe poisoning, confusion, hyperreflexia, gross tremor, dysarthria, ataxia, convulsions, focal neurological signs, arrhythmia, arterial hypotension, albuminuria, indomitable vomiting, and profuse diarrhea are characteristic. A fatal coma develops. The most effective way to treat lithium intoxication is hemodialysis.

Taking lithium salts during pregnancy is dangerous for the mother and the fetus, especially with concomitant therapy with diuretics and a salt-free diet. In newborns, reversible disorders are diagnosed - depression of the central nervous system, muscle hypotension, heart murmur. Lithium treatment for women in the early period of pregnancy is accompanied by Ebstein's cardiovascular anomaly (deformation of the tricuspid valve) in newborns. The incidence of this anomaly in the population is 1 in 20,000 live newborns, with lithium salt therapy - 1 in 5,000. The diagnosis can be made perinatally using ultrasonography. The anomaly is amenable to surgical correction. Carbamazepine and valproate have more fetotoxic effects than lithium salts.

Lithium salts are contraindicated in diseases of the cardiovascular system, kidneys, liver, peptic ulcer disease, cholecystitis, thyroid dysfunction, cataract, hypersensitivity, pregnancy. For the period of treatment, breastfeeding is stopped

Pharmacotherapeutic group N05AN01 - antipsychotic drugs.

Main Pharmacological action: blocks sodium transport to neurons, in turn suppresses depolarization-dependent (i.e. calcium-dependent) release of norepinephrine and dopamine (without affecting serotonin release); the mechanism of action of lithium is not fully understood; lithium inhibits the reuptake of these catecholamines; in patients with bipolar or unipolar affective disorders, lithium contributes to the disappearance of the symptoms of mania and prevents their development, and also prevents the phase of depression or reduces its symptoms in both types of affective disorders, stabilizing the patient's mood; in healthy people, lithium does not lead psychotropic action. Lithium salts inhibit ADH (vasopressin) and the effect of thyroid-stimulating hormone (TSH) on the thyroid gland, which can lead to certain side effects; in the kidneys and thyroid gland, lithium salts inhibit ADH and thyroid-stimulating hormone by adenylate cyclase.

INDICATIONS: treatment of the manic phase of bipolar disorder by the WHO (recommendation for the use of drugs in the Basic Formulary of the World Health Organization "I, 2008), BNF (recommendation for the use of drugs in the British National Formulary, 60th edition), prevention of recurrence of episodes of bipolar disorder WHO ( recommendation for the use of drugs in the Basic Formulary of the World Health Organization "i", 2008), BNF (recommendation for the use of drugs in the British National Formulary, 60th issue), as well as to reduce the intensity and frequency of subsequent episodes of BNF mania (recommendation for the use of drugs in British National Formulary, Issue 60) in patients with a history of manic episodes, prevention of the WHO depression phase (recommendation for the use of drugs in the Basic Formulary of the World Health Organization "I, 2008), BNF (recommendation for the use of drugs in the British National Formulary, 60th edition) in patients with unipolar affective disorder.

Method of administration and dosage: through a narrow therapeutic range of lithium concentrations, doses should be selected individually, based on the concentration of lithium in the blood serum and clinical effect, the total daily dose is usually 0.5 - 1.25 g of lithium carbonate (in several doses) WHO (recommendation for use Medicines in the Basic Formulary of the World Health Organization "" I, 2008), treatment should be started with a low daily dose, and then gradually increased; during the initial period of treatment, the concentration of lithium in serum should be monitored at least once a week; the optimal concentration of lithium is from 0.5 to 0.8 mmol / l BNF (recommendation for the use of drugs in the British National Formulary, issue 60), after reaching the desired concentration, control tests can be performed less often - once a month with BNF or once every two months, during the period of remission, the concentration of lithium in the serum can be determined every 2-3 months with BNF; in severe manic disorders, the recommended dose is 1.5 BNF-2, 0 g / day, while the concentration of lithium in the serum should be within 0.6-1 , 2 mmol / L, after relief of severe symptoms, the dose of lithium carbonate should be immediately reduced; the daily dose of lithium carbonate should be taken in at least three doses, if one dose has been missed, the next dose should not be doubled.

Side effects when using drugs: pseudotumor of the brain, tremor (large-scale tremor and fibrillation), ataxia, athetosis, increased tendon reflexes, extrapyramidal symptoms, urinary and fecal incontinence, convulsions, drowsiness, disorientation, memory impairment, coma, visual disturbances, speech disorders, hypotension, a fainting, bradycardia, dysfunction of the sinus node, vascular insufficiency, peripheral edema, nausea, vomiting, diarrhea, abdominal pain, anorexia, edema of the salivary glands, glucosuria, decreased creatinine clearance, albuminuria, oliguria, diabetes symptoms (diabetes mellitus) (polypuria ) hair loss, acne, psoriasis, itching, rash, covering with ulcers, hyperkeratosis, folliculitis; dry mouth, impotence; Graves' disease, hypothyroidism, hyperthyroidism, weight loss, hyperglycemia, hypercalcemia, allergic vasculitis, anemia, leukopenia, leukocytosis, edema, taste disorders, caries, side effects caused by lithium are more pronounced in elderly patients than in young people, despite the same serum lithium concentration.

Contraindications to the use of drugs: hypersensitivity to the active substance or auxiliary ingredients, severe renal failure, recent MI (myocardial infarction), organic brain pathology, leukemia, pregnancy (due to embryotoxic effects in the first trimester) and breastfeeding (lithium is excreted in milk), the drug is contraindicated in children.

Drug release forms: caps. (Capsules) 300 mg tab. (Tablets) prolonged action 400 mg

Visualization with other drugs

Diuretics, especially thiazides and amiloride, a low sodium diet and increased sodium loss (due to excessive sweating), delay lithium excretion and increase the risk of lithium accumulation. NSAIDs (non-steroidal anti-inflammatory drugs) (indomethacin, ibuprofen), tetracyclines, methyldopa and ACE inhibitors (ACE) - inhibition of lithium excretion in the urine. With haloperidol - leads to encephalopathy, with leukocytosis, increased levels and activity of plasma enzymes, increased levels of urea and blood nitrogen and morning hyperglycemia. A similar interaction is possible with other neuroleptics. Strengthens and prolongs the action of muscle relaxants, regardless of their mechanism of action, as non-depolarizing (pancuronium) and depolarizing (succinylcholine) drugs. Lithium enhances the inhibitory effect of high doses of iodide on the thyroid gland. Suppresses the action of amphetamines. Fluoxetine, methyldopa and metronidazole - an increase in the concentration of lithium in the blood - the risk of side and toxic effects of lithium. Chlorpromazine and other phenothiazine derivatives - exacerbation of extrapyramidal symptoms, potentiation of the neurotoxic effect of lithium. With tricyclic antidepressants - provokes manic or manic-depressive states. Xanthines (aminophylline, caffeine, theophylline) and others with an alkaline reaction (sodium carbonate) and urea - accelerate the excretion of lithium, reducing its concentration in serum. May increase the concentration of glucose, parathyroid hormone and calcium in plasma.

Features of use in women during pregnancy and lactation

Pregnancy Contraindicated.
Lactation: Contraindicated.

Features of use in case of insufficiency of internal organs

Dysfunction of the cervical-vascular system: Contraindicated in CHF, cardiac arrhythmias and conduction disorders.
Dysfunction of the pechinka: No specific recommendations
Impaired renal function Contraindicated in violation of the excretory function.
Respiratory dysfunction: No special recommendations

Features of use in children and the elderly

children under 12 years old Contraindicated.
Elderly and senile persons: A proportional dose reduction is necessary.

Application measures

Information for the doctor: Use with caution in patients with Parkinson's disease, hypothyroidism, sinus node and AV (atrioventricular) conduction dysfunction, epilepsy, psoriasis, congenital muscle weakness, diabetes mellitus and schizophrenia. Since lithium blocks sodium reabsorption in the renal tubules, ensure adequate intake of sodium and water during treatment. In case of diarrhea or excessive sweating (for infectious diseases), a dose reduction or temporary discontinuation of treatment may be required.
Information for the patient: During the treatment of severe exacerbations of the disease, driving and other mechanisms are contraindicated.

Many of us were moistened by a wave of interest in “biohacking” performed by the entrepreneur Sergei Fage (whose criticism we are), Sergei recently released the second series about his adventures in life. We must admit that we were interested in some of the details of "phage hacking" and we decided to understand, for example, what science says about lithium intake.

So you don't have to click too much, here's a quote from Fage's column:

Lithium... We get about 1-3 mg of lithium from water per day. It is prescribed for patients with bipolar disorder in dosages ranging from 800 to 2000 mg per day. I take 100 mg per day, which is 10 to 20 times less than what is considered safe for human use.

There are two reasons. Firstly, lithium has been proven to improve neurogenesis and in many ways have a positive effect on the body - here is a list of more than 50 studies that support this. Second, from a subjective point of view, lithium makes me more stress-resistant.

There is simply no reason not to take lithium in such small doses. All this reasoning after the last article on the topic that lithium is harmful shows that critics do not understand a damn about medicine and cannot read.

We provide additional data on lithium so that the inquisitive minds of readers can continue to deepen their knowledge that not everything is as unambiguous and binary as the avant-garde of "biohacking" presents it.

Lithium - the history of discovery and prohibition

Lithium has long been used to treat mental disorders. Ancient, Roman, medieval physicians used water from special sources to treat manias, affective disorders, patients in a state of "agitation" and "euphoria". Modern scientists have found that these waters had a high concentration of this alkali metal.

In 1949, the Australian scientist John Cade, through experiments on guinea pigs, noticed that lithium salts have a calming effect. After that, having tested the drugs on himself, he began to use them in patients with mania, schizophrenia and depression.

The use of lithium salts in patients with mania had such a strong calming effect that Cade began to associate mania with a lack of lithium in the body.

Unfortunately, the side effects made themselves felt. Lithium salts, which began to be used as a substitute for common table salt in the diet of hypertensive patients, led to deaths, and in the United States the FDA banned the use of lithium preparations until 1970.

Types of lithium preparations

In modern medicine, lithium preparations belong to the group of normotimics - medicines designed to stabilize mood in people with mental illness.

They are used in the form of salts - mainly carbonate. Citrate, orotate, succinate, chloride, sulfate and other compounds are also used.

The most common lithium preparations are:

Lithium carbonate... Known under trade names: Contemnol, Litarex, Sedalit, Litosan-SR, Lithium carbonate and others.
Lithium Oxybutyrate - is used in lower concentrations than lithium carbonate preparations, but it has high activity and less pronounced side effects.
Nicotinate (Litonit) - used in the complex therapy of chronic alcoholism.

In Russia, it is mainly used only lithium carbonate.

The mechanism of action of lithium

Lithium has multifaceted effects on the nervous system. One of the main effects is the stimulation of the reuptake of norepinephrine and serotonin by adrenergic endings. This inhibits noradrenergic activity, which forms the development of affective states.

Lithium also acts as an antagonist of sodium ions in nerve and muscle cells - this slows down the conduction of nerve impulses.

Lithium ions also increase the sensitivity of certain parts of the brain to dopamine.

According to some reports, lithium preparations block the activity of enzymes involved in the synthesis of inositol, a substance involved in the regulation of neuronal sensitivity.

Lithium in therapeutic doses

Nowadays, drugs based on lithium salts used for the treatment of mental illnesses: manic and hypomanic states, for the prevention of affective bipolar and schizoaffective disorders... Can also be used with treatment of chronic alcoholism, as part of complex therapy for depression... Prescribed by a doctor.

Additionally, you can highlight the external use of lithium succinate in the treatment of certain skin diseases, such as seborrheic dermatitis, mycoses and others.

Lithium dosage

The minimum therapeutic concentration of lithium in the blood is 0.6 mmol / L, and the maximum allowable concentration is 1.6 mmol / L. In practice, it is not recommended to exceed the concentration of 1.2 mmol / l.

Preventive concentrations can be lower: 0.2-0.4 mmol / L, however, they can also cause unpleasant side effects.

In psychotic disorders, usually starting with 0.6-0.9 g of lithium carbonate. With good tolerance, 1.2 g is prescribed on the second day, and the dose is increased daily by 0.3 g to a daily dose of 1.5-2.1 g. If necessary, the dosage can be increased to 2.4 g / day (with mandatory control blood). In doses over 2 g per day, the drug is not recommended for more than 1-2 weeks. Older patients should be given lower doses of lithium than younger patients.

After the disappearance of psychotic symptoms, the dosage is gradually reduced to 1.2-0.6 g per day. In case of recurrence of psychotic phenomena, the dosage is again increased to the effective level. 7-10 days after the re-achievement of the full therapeutic effect, the dose is gradually reduced again.

For reference: Sergei Fage, with whom we began this text, takes micro doses of lithium (they will be discussed below): he writes that he takes a dosage “10-20 times lower than the therapeutic one: 0.1 g / day”.

Contraindications and side effects

Lithium preparations are very toxic, their use should be under the supervision of a physician.Common side effects are tremor of the hands, exacerbation of diseases of the gastrointestinal tract, thirst, the development of cardiac arrhythmias, muscle weakness and frequent urge to urinate, impaired renal function.

An increase in the concentration of lithium in the blood above 1.5-2.0 mmol / l can cause acute poisoning, the manifestations of which can be constant nausea, increased tremor of the hands, muscle twitching, vomiting, diarrhea, drowsiness, confusion appear.

In the future, an increase in symptoms is possible - the manifestation of seizures, focal neurological symptoms, a decrease in arterial pressure, oliguria, the development of stupor and coma. Toxic concentrations of lithium can lead to irreversible damage to the central nervous system, up to and including death.

Contraindications for use: impaired renal excretory function, pregnancy and lactation, cardiac conduction disorders, type 1 and 2 diabetes, thyroid disease, age up to 15 years or old age, general depletion of the body, taking during a salt-free diet , exacerbation of inflammatory diseases of the gastrointestinal tract, hyponatremia, taking diuretic drugs or ACE inhibitors, individual drug intolerance, cataracts, osteoporosis, leukemia, chronic diarrhea, which can cause changes in electrolyte balance, dehydration.

Application of lithium salts in microdoses

A separate point is the interest of scientists in mini-doses of lithium. According to numerous studies, they have a lot of versatile effects on the body in the absence of pronounced side effects that can occur when using lithium salts in therapeutic doses.

Here are some of the research-backed effects of mini-doses of lithium.

Neuroprotective effect of microdoses of lithium preparations

According to numerous studies, lithium preparations have pronounced neuroregenerative properties, can be used for the treatment and prevention of cerebrovascular diseases: strokes, thromboembolisms, traumatic injuries of the cranial nerves. There is a decrease in the risk of developing Alzheimer's disease, Parkinson's, dementia, memory improves, and the volume and density of the gray matter of the brain increases.

Research and scientific articles:

Microdoses of lithium increase bone formation andcan become drugs for the treatment of osteoporosis

Research and articles:

Microdoses of lithium preparations reduce the risk of certain types of cancer, and also inhibit the spread of metastases of rectal cancer and glioma (brain tumor) as part of complex therapy.

Research and articles:

Melanoma prevention, leukemia and prostate cancer therapy with lithium

There are also studies showing the effectiveness of lithium salts for the prevention of melanoma and in the treatment of leukemia, prostate cancer.

Lithium preparations inhibit the development of vascular atherosclerosis, lower blood glucose levels and prevent the development of type 2 diabetes.

Small doses of lithium preparations inhibit the development of renal failure, while high doses can cause it:

Research:

It is also worth knowing that the statement about a slowdown in the progression of amyotrophic lateral sclerosis during therapy with lithium preparations was refuted:Clinical Trial Testing Lithium in ALS Terminates Early for Futility. 2010.

Lithium and telomeres

Research shows that microdoses of lithium salts protect telomeres - special areas at the ends of chromosomes, the length of which decreases with each cell division.

When telomeres run out, the cell loses its ability to divide. This phenomenon limits the maximum human life span, which is 110-120 years.

Lithium preparations have a wide range of effects, from well-studied to speculated. But due to the large number of side effects, contraindications and, in general, the topic of interaction with the human body is not fully understood, it is not recommended to use these drugs to prevent a disease, improve memory and other effects without consulting a doctor. Take care of yourself.

Text: Alexey Kalik

Lithium carbonate

Chemical properties

Salt formed alkali metal lithium and carbonic acid ... Substance - colorless powder or crystals, odorless. The product is poorly soluble in water (especially in hot water), practically insoluble in alcohols. His molecular mass \u003d 73.9 grams per mole. The melting point is about 618 degrees Celsius.

Lithium Carbonate is used in the production of plastics, pyrotechnics, porcelain, sitalls , in the desulfurization of steel, in the glass industry.

For medical purposes, lithium salts began to be used by ancient physicians. They used alkaline mineral waters rich in lithium compounds to treat patients with agitation and other mental disorders accompanied by euphoria.

By 1949 Australian scientist John Cade is injecting TOlithium arbonate to heal, and various manias ... Then, due to the high toxicity of such compounds, a ban was introduced on their use until 1970. Today, Lithium Carbonate is actively used in medicine as normotimics and an antipsychotic agent.

pharmachologic effect

Sedative, antipsychotic, normotimic.

Pharmacodynamics and pharmacokinetics

The substance acts as an antagonist sodium ions in nerve and muscle cells. Thus, muscle weakness develops, it becomes difficult to conduct nerve impulse ... Lithium affects transport and other monoamines , in some areas of the brain, sensitivity to.

Salts also inhibit enzyme activity , kinase 3 glycogen synthetase , protein kinase C ... Substance stimulates shear intraneuronal metabolism of catecholamines .

After penetration into the stomach, the agent is quickly and completely absorbed. It reaches its maximum concentration within 6-12 hours. The half-life is from one day to 2.5 days (after a year of daily intake). The medicine overcomes blood-brain barrier , passes into breast milk.

Lithium salts are excreted through the kidneys, depending on the level of sodium and potassium, lithium, or is reabsorbed in the renal tubules or retains its equilibrium concentration in the blood.

Indications for use

The tool is used:

for treatment manic and hypomanic states of various origins;
as a prophylactic agent or as a medicine for affective psychoses ;
with chronic;
for treatment, meniere's syndrome , sexual deviations;
with some forms of drug dependence.

Contraindications

Lithium carbonate should not be prescribed:

with hypersensitivity to the substance;
after major operations;
patients with severe cardiovascular disease;
at and;
breastfeeding women;
if the patient has, including a history;
with renal failure;
persons with severe dehydration and imbalance electrolytes ;
pregnant women.

Side effects

After taking the medicine, you may experience:

, nausea , dryness of the oral mucosa, vomiting,;
, decreased muscle tone,;
leukocytosis , heart rhythm disturbance, slowing down hematopoiesis ;
renal failure polyuria ;
feeling thirsty, weight gain, myasthenia gravis , ;
and allergic rashes,.

Lithium Carbonate, application instruction (Way and dosage)

The dosage is determined by the attending physician depending on the initial concentration of lithium in the blood plasma.

Lithium Carbonate preparations are taken orally.

The average daily dosage for an adult is about 900-2400 mg, divided into 3-4 doses.

The dosage should be selected so that the equilibrium concentration of the agent in the blood is from 0.6 to 1.2 mmol per liter.

As a rule, when taking 1 gram of substance per day, the optimal equilibrium concentration is reached within 10-14 days.

If during the treatment there are marked improvements in the patient's condition, then it is highly discouraged to interrupt therapy in order to avoid relapse.

For children, the optimal concentration of lithium is 0.5-1 mmol per liter.

Overdose

In case of drug overdose, the following develop: hyperreflexia , speech disorders, epileptic seizures and tonic convulsions , oliguria , loss of consciousness, collapse ... Treatment is according to the symptoms that appear.

Interaction

The combination of a drug with thiazide diuretics , methyldopa , or can lead to a rapid increase in the plasma concentration of lithium in the blood and the development of toxic effects.

ACE inhibitors , nonsteroidal anti-inflammatory drugs increase the concentration of lithium in the blood, increase the risk of adverse reactions.

The combined intake of the substance leads to an increase in the level of lithium in the blood.

Derivatives enhance the excretion of lithium from the body in the urine, this can lead to a decrease in the effectiveness of the drug.

When this compound is combined with, the toxic effect of the drug is enhanced.

Better not to combine with the drug, drug interactions are unpredictable.

With the combined use of the drug and isolated cases of amplification were described hyperkinetic symptoms in patients sick chorea of \u200b\u200bHuntington ., disorders in the work of the cerebellum.

Terms of sale

We need a recipe.

Storage conditions

The tablets are stored in a dark, dry place, away from children.

Shelf life

special instructions

Some phenothiazines may mask symptoms of lithium toxicity.

After a month of continuous medication, it is recommended to perform weekly monitoring of the concentration of lithium in the blood plasma. Then this indicator can be checked once a month, then - once every 2-3 months.

During therapy, do not drive a car or perform potentially hazardous activities.

Elderly

The elderly and debilitated patients need dosage adjustments.

With alcohol

Alcohol should not be taken during treatment.

Preparations that contain (Analogues)

Matching ATX level 4 code:

The substance is included in the composition of medicines: Contemnol, Lithium Carbonate, Liosan-SR, Coated Tablets Lithium Carbonate .