Thiodazine
Thiodazin: 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. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Thiodazine
ATX code: N05AC02
Active ingredient: thioridazine (thioridazine)
Manufacturer: San Pharmaceutical Industries Limited (India)
Description and photo update: 2018-21-11
Thiodazine is an antipsychotic (neuroleptic) drug.
Release form and composition
The dosage form of Thiodazine is film-coated tablets: round, on one side for dosages of 10, 25 and 50 mg there is a dividing line; in a dosage of 10 mg - light orange or light orange with a pink tinge, in a dosage of 25 mg - blue, in a dosage of 50 mg - yellow, in a dosage of 100 mg - blue (in a strip of aluminum foil 10 pcs., 10 strips in a cardboard box).
Composition of one tablet:
- active substance: thioridazine hydrochloride - 10, 25, 50 or 100 mg;
- auxiliary components (core): microcrystalline cellulose, starch, lactose, polyvinylpyrrolidone K30 (povidone K30), magnesium stearate, sodium methylparaben (sodium methylparahydroxybenzoate), colloidal silicon dioxide, purified talc;
- shell: Eudragit E100 (copolymer of methyl methacrylate, dimethylaminoethyl methacrylate and butyl methacrylate) or E5 premium (hypromellose), polyethylene glycol 6000 (macrogol 6000), dyes (depending on the dosage) titanium dioxide, sunset yellow, indigo carmine or quinoline yellow.
Pharmacological properties
Pharmacodynamics
The active substance of Thiodazine is thioridazine, a phenothiazine derivative belonging to the piperidine group. The substance has properties that are inherent in other phenothiazines, but the clinical spectrum of its pharmacological actions also differs significantly from the spectrum of other phenothiazine derivatives. The distinctive properties of thioridazine include its pronounced anxiolytic and sedative activity, as well as its low ability to lead to extrapyramidal disorders.
Thioridazine has a moderate alpha-adrenergic blocking and m-anticholinergic effect, has an antihypertensive and antiemetic effect. The active substance can help prolong the QT interval.
When thioridazine is used in low doses, it has an anxiolytic effect: it reduces feelings of anxiety, anxiety, fear, and reduces emotional tension. In patients taking Thiodazine, there is an improvement in adaptation to the surrounding reality. The drug is also effective in cases of mild depressive disorders.
When high doses of thioridazine are used, it has an antipsychotic effect.
Thiodazine has a wide therapeutic range. As a rule, the drug is well tolerated by patients in compliance with the recommended dosage regimen.
Pharmacokinetics
- absorption: rapidly absorbed in the gastrointestinal tract, C max (maximum concentration) in blood plasma is achieved 2–4 hours after administration. The bioavailability index is subject to interindividual variability, on average it is 60%;
- distribution and metabolism: more than 95% of thioridazine hydrochloride binds to blood plasma proteins. The substance has the property of penetrating the placental barrier and excreted in breast milk. Thioridazine and its main metabolites (mesoridazine and sulforidazine) cross the BBB (blood-brain barrier) and are found in the cerebrospinal fluid. At the same time, the ratio of the content of metabolites in the cerebrospinal fluid to their content in blood plasma is higher than the same ratio for unchanged thioridazine, which is evidence of the significant role of metabolites in the mechanism of antipsychotic action of Thiodazine;
- Excretion: T 1/2 (half-life) is approximately 10 hours. Excretion is carried out mainly through the intestines (50%), as well as through the kidneys (in the form of metabolites - approximately 30% of the dose, unchanged - less than 4%).
Indications for use
Schizophrenia and other mental disorders:
- exacerbation of schizophrenia;
- chronic course of schizophrenia (therapy, including long-term treatment of inpatients, and long-term maintenance therapy of outpatients with schizophrenia).
Depression and anxiety syndromes:
- psychiatric practice: agitated depression - in the form of monotherapy and as part of combination therapy;
- general medical practice: treatment of a variety of syndromes manifested in anxiety, a combination of anxiety and depression, agitation and tension, emotional disorders and psychosomatic disorders;
- psychotic depression or mixed anxiety-depressive states - for long-term treatment.
Application in geriatric practice:
- severe cognitive and behavioral disorders in elderly patients with organic brain lesions of any severity - as an antipsychotic and neuroleptic agent;
- anxiety states, mixed anxiety-depressive states, senile agitation, insomnia - as an anxiolytic or sedative.
Application in pediatric practice:
- childhood schizophrenia, severe behavioral disturbances against the background of organic brain damage or mental retardation;
- states of anxiety, agitation, tension, concentration disorders in children with severe behavioral disturbances, cases of hyperactivity resistant to stimulants, sleep disorders - as a sedative or anxiolytic agent.
Other disorders of various origins:
- severe behavioral disturbances in mentally retarded adults and patients with symptoms of deficiency syndrome;
- alcohol withdrawal syndrome - to reduce the severity of agitation, anxiety, hostility, hallucinations and other mental manifestations;
- vomiting of central genesis.
Contraindications
Absolute:
- coma or severe depression of the central nervous system (CNS);
- a history of serious hematological diseases, including inhibition of bone marrow hematopoiesis;
- severe heart disease, especially clinically significant arrhythmias (including ventricular tachycardia);
- arrhythmias of the heart (including a history), congenital long QT syndrome;
- combined use with drugs that lengthen the QT interval;
- depression of consciousness of a severe degree (including coma) of any etiology (as a result of the use of drugs, including);
- simultaneous use of substrates or inhibitors of the isoenzyme CYP2D6;
- severe form of arterial hypertension or arterial hypotension;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- pregnancy, lactation period;
- children under 3 years old;
- anamnestic information about reactions of severe photosensitization or individual hypersensitivity to other phenothiazine derivatives;
- individual hypersensitivity to thioridazine hydrochloride or any auxiliary component of the drug.
According to the instructions, Thiodazine should be prescribed with caution for: alcoholism (due to a predisposition to hepatotoxic reactions), pathological changes in the blood (due to the risk of hematopoiesis disorders), angle-closure glaucoma, breast cancer (due to an increase in the potential risk of disease progression and resistance to cytostatic and endocrine drugs as a result of the secretion of prolactin caused by thioridazine), renal and / or hepatic failure, hyperplasia of the prostate gland with clinical manifestations, gastric and duodenal ulcers (in the acute stage), diseases with a high risk of thromboembolic complications, epilepsy, disease - for enhancing extrapyramidal effects), myxedema,Reye's syndrome (due to an increased likelihood of developing hepatotoxicity in children and adolescents), chronic diseases with respiratory failure (especially in children), cachexia, vomiting (since vomiting associated with an overdose of other drugs can be masked by the antiemetic effect of thioridazine) and in the elderly age.
Instructions for the use of Thiodazine: method and dosage
Thiodazin tablets are taken orally.
The doctor selects the dose and time of taking the drug individually, taking into account the disease and the severity of symptoms. It is recommended to start treatment with the minimum doses in the specified interval. Then, in the course of therapy, the dose is gradually increased to the maximum effective. Upon reaching the maximum therapeutic effect, the dose of Thiodazine is gradually reduced to a maintenance one. As a rule, the daily dose is divided into 2-4 doses.
Schizophrenia and other mental disorders:
- exacerbation of schizophrenia in adult hospitalized patients: 100–600 mg per day, maximum daily dose of 800 mg;
- chronic course of schizophrenia: in inpatients - 100–600 mg per day, in outpatients - 50–300 mg per day.
Depression and anxiety syndromes:
- psychiatric practice for agitated depression: 25-200 mg per day;
- general medical practice as anxiolytic and / or sedative: 10–75 mg per day.
For the treatment of diseases of old age, Thiodazin is used as:
- antipsychotic and / or neuroleptic agent: 25-200 mg per day;
- sedative and / or anxiolytic agent: 10–75 mg per day.
In pediatric practice, Thiodazine is used as:
- antipsychotic agent for severe emotional and mental disorders in children over 3 years of age: 1-4 mg / kg of body weight per day;
- anxiolytic and / or sedative in children from 3 years of age: 0.5–2 mg / kg of body weight per day.
Treatment of other disorders of various origins:
- severe behavioral disturbances in mentally retarded adults and patients with symptoms of deficiency syndrome: 100–600 mg per day, maximum daily dose - 800 mg;
- alcohol withdrawal syndrome (to reduce the severity of mental disorders): 100-200 mg per day.
In hospitalized patients with schizophrenia, a marked improvement in the condition is observed, as a rule, after 2-3 weeks or more from the start of therapy. In patients with chronic mental disorders, it may take from 6 weeks to six months to achieve maximum clinical effect. And in acute psychoses, a positive effect can be observed within 24–48 hours.
Treatment of patients with impaired renal / liver function, underweight, as well as children and the elderly requires careful medical supervision. It is recommended to start therapy in such patients with especially low doses and increase them very slowly.
Since the sudden withdrawal of Thiodazine in patients who received it for a long time or in high doses can cause nausea, vomiting, dizziness, tremors, anxiety, insomnia, agitation, transient dyskinesias, when long-term treatment is canceled, the dose of the drug should be reduced gradually, over several weeks.
Side effects
Side effects of Thiodazine are dose-dependent. When using the drug in doses corresponding to the recommended interval, negative reactions in most cases are weak and go away on their own. When using high doses of thioridazine, severe side effects are observed.
The incidence of side effects from systems and organs on a special scale (very often - more than 1/10; often - 1 / 100-1 / 10; infrequently - 1 / 1000-1 / 100; rarely - 1 / 10000-1 / 1000; extremely rare - less than 1/10000):
- CNS: often - sedation, dizziness, drowsiness; infrequently - increased irritability, psychomotor agitation, headache, impaired consciousness, hallucinations; rarely - extrapyramidal symptoms (akathisia, muscle rigidity, tremor, dystonia, dyskinesia), seizures, tardive dyskinesia; extremely rare - insomnia, depression, NNS (neuroleptic malignant syndrome);
- cardiovascular system: often - orthostatic hypotension; infrequently - tachycardia, prolongation of the QT interval; rarely - arrhythmias; extremely rare - flutter-fibrillation of the ventricles, sudden death;
- autonomic nervous system / m-anticholinergic effects: often - blurred vision, dry mouth, nasal congestion, paresis of accommodation; infrequently - nausea, vomiting, constipation, diarrhea, loss of appetite, incontinence or urinary retention; rarely - tremor, pallor; extremely rare - paralytic intestinal obstruction;
- endocrine system: often (with prolonged use) - galactorrhea, hyperprolactinemia; infrequently - changes in body weight, amenorrhea, menstrual irregularities, erection and ejaculation disorders; rarely priapism; extremely rare - peripheral edema, gynecomastia, engorgement of the mammary glands;
- peripheral blood: rarely - thrombocytopenia, agranulocytosis, leukopenia; extremely rare - anemia, leukocytosis;
- liver: infrequently - changes in the activity of hepatic transaminases; rarely - hepatitis;
- skin: rarely - skin rash (including allergic), dermatitis, urticaria, photosensitivity reactions, angioedema;
- others: rarely - hyperthermia, edema in the parotid gland, breathing disorders.
Overdose
In cases of an overdose of Thiodazine, an increase in adverse reactions, the development of acute neuroleptic complications are possible. You should especially pay attention to the increase in body temperature, which is one of the symptoms of NNS. In severe overdose, impaired consciousness can occur in various forms, up to a coma.
With prolonged therapy with the drug, rare cases of retinopathy pigmentosa have been recorded that occurred in patients who took thioridazine in doses exceeding the recommended maximum daily dose of 800 mg.
In case of an overdose, you must stop taking Thiodazine, like any other antipsychotic drugs. It is recommended to use central anticholinergics, activated carbon in high doses, gastric lavage, in the presence of seizures, intravenous diazepam, neurometabolic stimulants, glucose solution, vitamins B and C, careful monitoring of the functioning of the respiratory, cardiovascular and central nervous system, symptomatic treatment.
Because barbiturates can increase the respiratory depression caused by phenothiazines, their use should be avoided in the event of seizures.
special instructions
Thiodazine should be used with extreme caution in patients with cardiovascular diseases, glaucoma (especially with closed-angle form), renal failure, severe respiratory diseases, epilepsy, Parkinson's disease, myasthenia gravis, prostatic hypertrophy, pheochromocytoma.
It is contraindicated to take alcoholic beverages during thioridazine therapy.
Influence on the ability to drive vehicles and complex mechanisms
It is prohibited to drive vehicles, perform any work associated with an increased risk of accidents, requiring a high concentration of attention, a quick mental and physical reaction, during the period of treatment with Thiodazine.
Application during pregnancy and lactation
Thiodazine is contraindicated for use in pregnant and breastfeeding women.
Pediatric use
It is prohibited to prescribe Thiodazine to children under 3 years of age.
With impaired renal function
In case of renal failure, Thiodazine should be used with extreme caution.
For violations of liver function
Liver dysfunctions are a relative contraindication to the use of Thiodazine.
Use in the elderly
The appointment of Thiodazine to elderly patients requires caution.
Drug interactions
The use of thioridazine concurrently with certain drugs can lead to the development of the following effects:
- drugs that inhibit the CYP2D6 isoenzyme (for example, fluoxetine, cimetidine, moclobemide, paroxetine): strengthening and prolonging the action of thioridazine due to the fact that it itself causes suppression of this isoenzyme;
- tricyclic antidepressants (TCA): an increase in plasma concentration of TCA and / or thioridazine, which can lead to the development of arrhythmias;
- antihypertensive drugs and beta-blockers: an increase in plasma concentrations of each drug due to the suppression of metabolism, which can lead to a significant decrease in blood pressure, heart rhythm disorders or negative reactions from the central nervous system;
- thiazide diuretics: increased risk of severe arterial hypotension, increased cardiotoxic effects of thioridazine (due to diuretic-induced hypokalemia);
- anticonvulsants: a decrease in the seizure threshold, a change in the concentration of phenytoin in the blood serum, which may require a dose adjustment. With the simultaneous use of carbamazepine with thioridazine, the serum concentrations of these drugs do not change;
- indirect anticoagulants: increased hypoprothrombinemic effect due to competitive interaction at the level of cytochrome P450 isoenzymes. In this case, it is necessary to carefully monitor the concentration of prothrombin in the blood plasma;
- drugs with a depressing effect on the central nervous system (including alcohol, narcotic analgesics, benzodiazepines, barbiturates, antidepressants, anesthetics): increasing their effect;
- MAO (monoamine oxidase) inhibitors: prolongation and enhancement of the sedative and m-anticholinergic action of each of the drugs;
- hypoglycemic agents: an increase in the risk of violation of the patient's glucose tolerance achieved as a result of their use due to the effect of thioridazine on carbohydrate metabolism;
- lithium preparations: increased risk of extrapyramidal disorders, severe neurotoxic complications and somnambulism;
- m-anticholinergics (atropine-like drugs), antihistamines and TCAs: enhancement of their m-anticholinergic effects up to the onset of atropine psychosis, severe constipation, paralytic intestinal obstruction, hyperpyrexia with possible heat stroke. Dose adjustment of medications and careful observation of the patient is required;
- antiparkinsonian drugs: weakening the action of each of the drugs;
- dopamine, epinephrine, phenylephrine, ephedrine and other vasoconstrictors: weakening of their pressor effect due to the α-adrenergic blocking properties of thioridazine;
- quinidine: enhancement of its inhibitory effect on the myocardium;
- antiarrhythmic drugs: when used simultaneously with thioridazine, caution must be exercised because of the possible excessive prolongation of the QT interval;
- antidiarrheal and antacid agents: reducing the absorption of thioridazine in the gastrointestinal tract.
Analogs
Analogs of Thiodazin are: Sonapax, Thioril, Tison and others.
Terms and conditions of storage
Store in a dark, dry place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Thiodazin
Reviews about Thiodazine are varied, since the drug acts on each patient individually. It can improve sleep, relieve anxiety, fear, emotional disorders. But there are complaints about the lack of any positive effect even with prolonged use of pills, as well as side negative effects such as lowering blood pressure, the development of tachycardia and arrhythmias.
Price for Thiodazine in pharmacies
There is no information on the price of Thiodazine, as the drug is currently not available for sale.
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!
