Thioridazine tablet film 10 mg x60

Chemical properties

Thioridazine is an antipsychotic drug. It has antipsychotic and moderate antidepressant effects. In the form of hydrochloride , it is a white powder that is highly soluble in water and ethyl alcohol, chloroform , methanol , and insoluble in ethers . The drug is produced in the form of film-coated tablets with different dosages. Due to the high incidence of life-threatening arrhythmias and retinopathy , the drug is used strictly according to indications and when other drugs are ineffective. In some countries the medicine has been withdrawn from circulation.

Pharmacodynamics and pharmacokinetics

The mechanism of action of Thioridazine is based on the ability of the drug to disrupt adrenergic and dopaminergic transmission of nerve impulses, especially in the reticular formation of the brain. The substance eliminates the activating effect on the limbic system and cerebral cortex. The drug provides blocking of m-cholinergic receptors , significantly reducing the activity of the autonomic nervous system.

The chemical compound affects various psychomotor functions, reduces general arousal, mobility, eliminates agitation and the degree of affective tension. The medicine also has a sedative effect, but does not lead to general lethargy and lethargy. It has some antidepressant and activating effects, moderate sedative and anticholinergic. Does not have a cataleptogenic effect, reduces blood pressure .

After taking the tablets, their contents are quickly absorbed in the digestive tract. The maximum concentration is observed after 1-4 hours. The drug quickly overcomes the histohematic barriers, the blood-brain and placental barriers, and is excreted in breast milk. The product has a high degree of bioavailability.

Metabolized in the liver with the participation of the cytochrome CYP2D6 to sulforidazine and mesoridazine (active metabolites). The half-life from the body ranges from 6 to 40 hours. The medicine is excreted through the kidneys, with bile. The mesoridazine metabolite is more active than the substance itself; it has a longer elimination time from the body, but a lower degree of binding to blood proteins.

Thioridazine overdose, symptoms and treatment

Xerostomia, nausea, vomiting, drowsiness, disorientation, hyperkinesis, hyperthermia, convulsions, coma, tachycardia, arrhythmia, arterial hypotension, respiratory depression, collapse. Treatment: gastric lavage followed by activated charcoal is recommended. Supportive, symptomatic treatment is carried out under conditions of strict control over the function of the respiratory, cardiovascular and central nervous systems. For hypotension, administration of plasma-substituting solutions is indicated, and in severe cases, careful administration of dopamine. For seizures, the use of benzodiazepines is recommended.

List of pharmacies where you can buy Thioridazine:

• Moscow
• Saint Petersburg

Indications for use

The medicine is prescribed:

• for the treatment of psychotic disorders and schizophrenia , which are accompanied by excessive agitation and hyperactivity ;
• for severe behavioral disorders, aggression, frustration, inability to concentrate, associated with psychotic disorders and neurological diseases;
• patients with severe or moderate depression in adults;
• for neuroses with agitation, anxiety, tension, insomnia , fears;
• for the treatment of Huntington's disease .

Use of the drug Thioridazine

The dose and time of administration are determined individually. As an anxiolytic, adults are prescribed a daily dose of 10-75 mg, children aged 1 year and older - 0.5-2 mg per 1 kg of body weight. As an antipsychotic for psychosis in adults, thioridazine is used in a hospital setting at a daily dose of 100–600 mg, on an outpatient basis - 50–300 mg, for agitated depression and when used in geriatrics - 25–300 mg, for alcohol withdrawal - 100–200 mg, for severe mental disorders of a non-psychotic nature - 25–150 mg. The maximum daily dose for adults is 800 mg, for children aged 1 year and older - 1-4 mg per 1 kg of body weight. When prescribing a dose close to the maximum daily dose, it is divided into 2–4 doses. Treatment of patients with underweight, kidney and liver diseases, as well as elderly patients is recommended to begin with the lowest doses and increase them very slowly. Thioridazine can be used to treat behavioral disorders in patients with epilepsy; in such cases, anticonvulsants should be continued, increasing their doses if necessary.

Contraindications

Thioridazine is not recommended for use:

• for acute depression ;
• patients in a coma , with severe depression of the central nervous system;
• for severe diseases of the heart and blood vessels, blood diseases ( arterial hypertension , chronic heart failure, arterial hypotension , arrhythmia );
• children under one year old;
• if you are allergic to a substance;
• patients with traumatic brain injury;
• in combination with drugs that prolong the QT interval, with CYP2D6 ;
• for porphyria , pregnancy and breastfeeding.

There are also some restrictions when treating the following groups of patients:

• alcoholics;
• patients with hematopoietic disorders;
• breast cancer patients ;
• patients with angle-closure glaucoma , prostatic hyperplasia ;
• patients with renal and liver failure, epilepsy , myxedema ;
• ulcers, especially during exacerbation;
• patients with chronic diseases that are accompanied by impaired respiratory function;
• patients with Reye's syndrome and the elderly.

Thioridazine

During the treatment period, it is necessary to monitor the morphological composition of the blood.

Elderly patients with dementia

In randomized clinical trials comparing some atypical antipsychotics with placebo in elderly patients with dementia, a threefold increase in the risk of cerebrovascular events was observed. The mechanism by which the risk of cerebrovascular complications increases is unknown. An increase in this risk cannot be excluded when taking other antipsychotics or when taking antipsychotics in patients of other groups, therefore thioridazine should be used with caution in patients with risk factors for stroke. In elderly patients with dementia-related psychosis, an increased risk of death was observed when treated with antipsychotic drugs. In placebo-controlled studies, most patients treated with atypical antipsychotics had a 1.6 to 1.7 times greater risk of death than patients treated with placebo. In a placebo-controlled clinical trial, patients receiving the active drug (an antipsychotic) had a mortality rate of 4.5% at the end of a 10-week course of treatment versus 2.6% in patients receiving placebo. Although causes of death varied in clinical studies with atypical antipsychotics, most causes of death were either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia). Observational studies have confirmed that, like treatment with atypical antipsychotics, treatment with typical antipsychotics may also increase mortality. The extent to which the increase in mortality may be attributable to antipsychotic drug use rather than to certain patient characteristics is unclear.

QT prolongation

In elderly patients using phenothiazines, including thioridazine, changes in the terminal segment of the ECG were observed, including prolongation of the QT interval, depression and T wave inversion, and the appearance of U waves. To date, the appearance of these changes is associated with changes in repolarization, which is not associated with myocardial damage and is reversible. However, significant prolongation of the QT interval can cause ventricular arrhythmias leading to sudden death.

Tardive dyskinesia

Long-term use of antipsychotic drugs may be associated with the development of tardive dyskinesia, the severity of which varies significantly among patients.

Neuroleptic malignant syndrome

When taking thioridazine, like other antipsychotic drugs, cases of the development of neuroleptic malignant syndrome have been reported, the clinical manifestations of which are: hyperpyrexia, muscle rigidity, changes in mental status, autonomic disorders (irregular pulse and blood pressure, tachycardia, arrhythmia, sweating, shortness of breath) , impaired consciousness up to coma.

If neuroleptic malignant syndrome occurs, it is necessary to immediately stop taking thioridazine and other drugs necessary for concomitant therapy, prescribe symptomatic therapy and monitor vital functions.

If a patient requires antipsychotic treatment after a history of neuroleptic malignant syndrome, the possibility of repeat drug therapy with thioridazine should be carefully assessed. Such patients must be closely monitored medically.

Fractures, injuries

Thioridazine may cause drowsiness, postural hypotension, and motor and sensory instability, which may lead to falls and subsequent fractures and other injuries.

Patients with epilepsy

Due to the ability of thioridazine to lower the seizure threshold, when treating patients with epilepsy, their condition should be carefully monitored and, if possible, electroencephalography should be performed.

Patients with Parkinson's disease

Except in special cases, thioridazine should not be used in patients with Parkinson's disease.

Venous thromboembolic complications

When using antipsychotic drugs, cases of venous thromboembolic complications, sometimes fatal, have been observed. Therefore, thioridazine should be used with caution in patients with risk factors for the development of venous thromboembolic complications.

Depressant effect on the central nervous system

Like other phenothiazines, thioridazine can enhance the inhibitory effect of various depressants (alcohol, anesthetics, barbiturates, narcotics, other psychoactive drugs, insecticides atropine and phosphorus, and others) on the central nervous system.

A case of respiratory arrest has been reported with the combined use of a phenothiazine and a large dose of barbiturates.

Withdrawal syndrome

Due to the possibility of developing withdrawal syndrome, three abrupt cessation. treatment with high doses of thioridazine, discontinuation of the drug should be carried out gradually.

Photosensitivity

Due to the possibility of photosensitivity, patients receiving thioridazine should be advised to avoid exposure to direct sunlight.

Ethanol-containing substances

During treatment with thioridazine, the intake of ethanol-containing substances is prohibited.

Side effects

During treatment with the drug, the following may occur:

• drowsiness , confusion , fainting, agitation , severe central nervous system agitation, hallucinations , sleep disturbances, convulsions , dystonia and parkinsonian extrapyramidal disorders;
• photophobia , vomiting, blurred vision, problems with thermoregulation, hyposalivation , indigestion , diarrhea or constipation , cholestatic hepatitis ;
• amenorrhea , gynecomastia , galactorrhea , dysmenorrhea , weight gain, swelling of the mammary glands;
• tachycardia , drop in blood pressure, changes in the electrocardiogram, leukopenia , agranulocytosis , thrombocytopenia ;
• pancytopenia , nasal congestion, dysuria , bronchospastic syndrome, urinary retention, priapism , sexual dysfunction, changes in libido ;
• skin rashes, dermatitis , Quincke's edema , swelling, melanosis of the skin.

Cases of sudden death of patients caused by disturbances in the functioning of the heart have been reported.

Side effects of the drug Thioridazine

Common side effects, especially when using a high dose and early in treatment, include drowsiness, sedation, dizziness, nasal congestion, and dry mouth. Dose-dependent orthostatic hypotension is sometimes observed, especially in elderly patients. Other dose-related effects associated with the anticholinergic activity of thioridazine include disturbances of accommodation, tachycardia, constipation, and urinary retention or incontinence. In some patients, thioridazine, even in low doses, can cause a feeling of mental depression, nausea, dizziness, headache, or, conversely, paradoxical effects of agitation, agitation or insomnia. In some cases, neuroleptic malignant syndrome (muscle rigidity, hyperthermia, mental status disorders, autonomic lability) was observed, requiring immediate discontinuation of thioridazine. When used in high doses, as with other phenothiazines, ECG changes of the repolarization type are described (lengthening of the Q-T , flattening of the T and appearance of the U ). These changes are most likely due to a decrease in potassium concentration in the blood. Like all phenothiazines, thioridazine can in rare cases provoke arrhythmias. Cases of sudden unexplained death, possibly due to arrhythmia or cardiac arrest, have been reported among patients receiving tricyclic antipsychotics, including thioridazine. When prescribing high (neuroleptic) doses of thioridazine, extrapyramidal symptoms are possible; when using low (anxiolytic) doses they are practically not observed. There have been reports of cases of pigmentary retinopathy during long-term treatment with thioridazine, mainly when taking more than 800 mg of thioridazine per day. Antipsychotic drugs such as thioridazine can cause hyperprolactinemia, leading to galactorrhea, menstrual irregularities, erectile dysfunction (weakness of erection or priapism) and ejaculation, and sometimes weight gain and edema. These effects can be prevented by reducing the dose of thioridazine. Rare cases of leukopenia and agranulocytosis, especially in the first months of treatment, photosensitivity, allergic rash, jaundice, hepatitis and liver dysfunction have been described.

Thioridazine, instructions for use (Method and dosage)

The medicine has an individual dosage regimen. The treatment regimen is determined by the attending physician, depending on many factors.

On average, adults over the age of 12 years are prescribed from 20 to 800 mg of the drug per day, 3 times a day. High dosages of medication can be prescribed for no more than 5 weeks.

For children, it is necessary to adjust the dosage depending on weight and age.

The maximum daily dosage for an adult (from 12 years old) is 0.8 g.

Thioridazine tablet film 10 mg x60

Clinical and pharmacological group: Antipsychotic drug (neuroleptic) Pharmacotherapeutic group: Antipsychotic drug (neuroleptic)

pharmachologic effect

Antipsychotic drug (neuroleptic), piperidine derivative of phenothiazine. It has an antipsychotic, moderate sedative (without severe inhibition), as well as antidyskinetic effect, antihistamine effect and antiemetic effect are weakly expressed. It has anticholinergic activity and causes a hypotensive effect. The intensity of action is inferior to pericyazine.

The mechanism of antipsychotic action is associated with blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain. It also has an alpha-adrenergic blocking effect and suppresses the release of pituitary and hypothalamic hormones. However, blockade of dopamine receptors increases the release of prolactin by the pituitary gland.

The central antiemetic effect is due to inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, the peripheral effect is due to blockade of the vagus nerve in the gastrointestinal tract.

Pharmacokinetics

Clinical data on the pharmacokinetics of thioridazine are limited.

Phenothiazines are highly bound to plasma proteins. They are excreted mainly by the kidneys and partly with bile.

Indications of the active substances of the drug Thioridazine Schizophrenia, psychotic disorders accompanied by hyperactivity and agitation, severe behavioral disorders associated with psychotic disorders or neurological diseases, accompanied by aggressiveness, inability to concentrate for a long time, reduced resistance to the development of frustration. Moderate and severe depression in adults, neuroses accompanied by anxiety, agitation, depressed mood, tension, sleep disorders, fears, Huntington's disease. ICD-10 codes

Dosage regimen The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.

Individual. When taken orally, the daily dose for adults and children over 12 years of age is 20-800 mg/day, the frequency of use is 2-4 times/day. The course of treatment with high doses is continued for no more than 5 weeks.

For children 1-5 years old - 1 mg/kg/day, over 5 years old - 75-100 mg/day, in severe cases - 300 mg/day, frequency of administration - 2-4 times/day.

The maximum daily dose for adults and children over 12 years of age is 800 mg.

Side effect

From the side of the central nervous system: possible drowsiness, confusion, anxiety, excessive motor excitability, headaches, postural hypotension (especially in elderly patients), visual impairment, and in isolated cases - NMS. With prolonged use, extrapyramidal disorders are possible. In high doses, it causes pigmentary retinopathy more often than other phenothiazines.

From the digestive system: possible dry mouth, nausea, vomiting, diarrhea, rarely - cholestatic jaundice.

From the cardiovascular system: postural hypotension (especially in elderly patients), heart rhythm disturbances are possible. In high doses, like other phenothiazines, especially with concomitant hypokalemia, it can cause ECG changes - prolongation of the QT interval, flattening of the T wave, appearance of the U wave.

From the hematopoietic system: in isolated cases - leukopenia, agranulocytosis.

From the endocrine system: swelling of the nipples of the mammary glands, menstrual irregularities, inhibition of ejaculation are possible.

Metabolism: swelling is possible. With long-term use in high doses, melanosis may develop.

From the respiratory system: nasal congestion.

Allergic reactions: possible skin rash, itching.

Contraindications for use Acute depressive states, comatose states, severe depression of the central nervous system, severe diseases of the cardiovascular system, a history of blood diseases, children under 1 year of age, hypersensitivity to thioridazine.

Use during pregnancy and breastfeeding During pregnancy, the use of thioridazine is possible only under strict indications. Adequate and well-controlled studies of the safety of thioridazine during pregnancy have not been conducted. It should be borne in mind that newborns whose mothers received thioridazine at the end of pregnancy may experience symptoms of intoxication: excessive drowsiness, tremor, hyperactivity. If it is necessary to use thioridazine during lactation, the issue of stopping breastfeeding should be decided.

Use for liver dysfunction

Patients with liver disease require regular monitoring of liver function.

Use for renal impairment

Use with caution in patients with renal failure.

Use in children Contraindicated in children under 1 year of age.

special instructions

Use with caution in patients with cardiac arrhythmias, heart disease, severe respiratory diseases, renal failure, Parkinson's disease, a history of closed-angle glaucoma, prostatic hypertrophy, myasthenia gravis, epilepsy, pheochromocytoma, hypersensitivity to other phenothiazines.

Patients with liver disease require regular monitoring of liver function.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, you should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug interactions

When used simultaneously with drugs that have a depressant effect on the central nervous system, with ethanol or ethanol-containing drugs, the depressant effect on the central nervous system may be enhanced.

With simultaneous use, the effect of anticonvulsants and cimetidine is reduced.

With the simultaneous use of drugs that have an anticholinergic effect, the anticholinergic effect may be enhanced.

When used simultaneously with sympathomimetics, the arrhythmogenic effect is enhanced.

With simultaneous use, the effect of antihypertensive drugs is enhanced and the risk of developing orthostatic hypotension increases.

With simultaneous use, the effectiveness of drugs to suppress appetite decreases (with the exception of fenfluramine).

When used simultaneously with antithyroid drugs, there is a risk of developing agranulocytosis; with anticoagulants, the effectiveness of anticoagulants decreases; with beta-blockers, the hypotensive effect may be enhanced, and the risk of developing irreversible retinopathy, arrhythmia and tardive dyskinesia may increase.

When used simultaneously with hypoglycemic drugs, a slight decrease in their effectiveness is possible; with amphetamine, an antagonistic interaction appears; with apomorphine, the emetic effect of apomorphine decreases, and its inhibitory effect on the central nervous system increases.

With simultaneous use, thioridazine increases the concentration of prolactin in the blood plasma and reduces the effect of bromocriptine.

With simultaneous use, it is possible to reduce the effects of guanethidine and clonidine and reduce the antiparkinsonian effect of levodopa.

With the simultaneous use of probucol, astemizole, cisapride, disopyramide, erythromycin, pimozide, procainamide, the QT interval may be prolonged and the risk of developing ventricular tachycardia may increase.

When used simultaneously with lithium salts, the absorption of lithium from the gastrointestinal tract decreases, the rate of excretion of lithium ions by the kidneys increases, and extrapyramidal disorders increase. Early signs of lithium toxicity (nausea and vomiting) may be masked by the antiemetic effect of thioridazine.

With simultaneous use of thiazide diuretics, hyponatremia may increase.

When used simultaneously with trazodone, it is possible to increase the concentration of trazodone in the blood plasma; with phenobarbital, it is possible to decrease the concentration of phenobarbital in the blood plasma.

When used simultaneously with quinidine, the cardiodepressive effect is potentiated. Possible prolongation of the QT interval and increased risk of developing ventricular tachycardia.

When used simultaneously with epinephrine, a sharp and pronounced decrease in blood pressure is possible.

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On prescription.

Interaction

Simultaneous use with drugs that depress the central nervous system and ethyl alcohol leads to increased sedative properties of the drug.

The medicine reduces the effectiveness of anticonvulsants and cimetidine .

Thioridazine enhances the effect of anticholinergics and sympathomimetics.

The combined use of the drug with drugs that lower blood pressure leads to an even greater decrease in blood pressure and the development of orthostatic hypotension .

When combined with appetite suppressants other than fenfluramine , this substance significantly reduces their effectiveness.

Simultaneous use of the drug with anticoagulants leads to a decrease in their effectiveness; with antithyroid drugs – to the development of agranulocytosis ; with beta-blockers - leads to increased hypotensive effect. The drug increases the risk of arrhythmias , tardive dyskinesia , and retinopathy .

Hypoglycemic agents lose their effectiveness when used with Thioridazine.

The combined use of the drug with amphetamine leads to a mutual weakening of the properties of both drugs.

With the simultaneous use of this substance and apomorphine , the emetic effect of the latter is reduced and the sedative effect is enhanced.

The medicine causes an increase in the concentration of prolactin in the blood and reduces the effectiveness of bromocriptine .

The drug can reduce the effectiveness of levodopa and guanethidine .

The combined use of the drug with probucol , cisapride , astemizole , disopyramide , pimozide , erythromycin , procainamide leads to prolongation of the QT interval and the development of ventricular tachycardia .

Thioridazine reduces the rate of absorption of lithium salts from the digestive tract and increases the rate of excretion of lithium ions from the body. The drug is also able to mask some signs of acute lithium intoxication, vomiting, and nausea.

hyponatremia increases ; with trazodone – its concentration in the blood increases.

The drug reduces the plasma concentration of phenobarbital .

The combined use of the drug and quinidine increases the load on the heart and can lead to prolongation of the QT interval and tachycardia .

Concomitant use with epinephrine causes a sharp decrease in blood pressure .

Drug interactions Thioridazine

Thioridazine, like other phenothiazines, can enhance the inhibitory effect on the central nervous system of alcohol, central nervous system depressants and antihistamines, the M-anticholinergic effect of anticholinergics and the inhibitory effect of quinidine derivatives on the myocardium. Thioridazine can reduce the severity of the antiparkinsonian effect of levodopa, reduce the seizure threshold in patients with epilepsy (which may require changing the dose of anticonvulsants), and reduce the pressor effect of adrenergic vasoconstrictors. MAO inhibitors may enhance or prolong the sedative and antimuscarinic effects of phenothiazines. Concomitant use of lithium preparations contributes to the development of extrapyramidal symptoms and increased neurotoxic properties of thioridazine. Taking beta-adrenergic receptor blockers may cause an increase in the concentration of thioridazine in the blood plasma. The absorption of thioridazine may be impaired by antacids and antidiarrheal drugs.

special instructions

During treatment, it is recommended to monitor liver function, peripheral blood composition, heart function, and the general condition of the patient.

During therapy, you should not drive a car or perform potentially dangerous actions that require high reaction speed.

Thioridazine, more often than other representatives of a number of phenothiazines , causes visual impairment, pigmentary retinopathy , and hemeralopia .

When treated with this substance, tardive dyskinesia . The risk is higher in women and during treatment with high doses of the drug. In some cases, these types of symptoms are irreversible. If adverse reactions develop, the drug is discontinued and symptomatic treatment is carried out.

Special instructions for the use of the drug Thioridazine

Caution is required when using thioridazine for narrow-angle glaucoma, prostatic hypertrophy and cardiovascular diseases. Thioridazine causes leukopenia or agranulocytosis relatively rarely, however, in the first months of treatment it is recommended to regularly count blood cells, and if clinical signs of pathological changes in blood composition appear, do so immediately. In case of liver diseases, regular monitoring of its functional state is necessary. Persons taking thioridazine should be careful when driving or operating potentially dangerous machinery. During pregnancy, thioridazine is prescribed only for absolute indications. Breastfeeding should be interrupted during treatment with thioridazine.

Drugs containing (Thioridazine analogues)

Level 4 ATC code matches:
Thiodazine

Thioril

Neuleptil

Sonapax

There is a large selection of structural analogues (synonyms) of this drug. The most common synonyms of Thioridazine: Ridazine , Melleril , Thioril , Sonapax , Thiodazine , Tison .

Reviews

Reviews of Thioridazine drugs are mostly positive; it is often prescribed to children and used as a sedative or antidepressant . Some prefer, in order to avoid adverse reactions, to take glycine .

Some reviews about the drug:

• “... The drug was prescribed for insomnia, neurosis and anxiety. The medicine seemed quite effective to me, I went through everything fine with it, and stood firm through everything. There were no adverse reactions at all”;
• “... My son was prescribed medication for hyperactivity. So the drug seemed to help, but the side effects were very strong: dizziness, vomiting, the child turned into a vegetable. In short, they stopped taking pills, changed the doctor, and at the same time the treatment tactics”;
• “... I took this remedy, it seemed to help me, but severe drowsiness and visual disturbances forced me to stop the course of treatment.”