Thiodasin - instructions for use, dose, side effects, contraindications

Composition:in 1 tablet coated with a film coating contains: active substances: Thioridazine hydrochloride 10, 25, 50 or 100 mg of inactive substances: lactose, starch, microcrystalline cellulose, magnesium stearate, colloidal silica, talc, E-100, sodium lauryl sulfate, polyethylene glycol . Dyes: sunset yellow, indigo carmine, titanium dioxide.

Description:

Tablets 10 mg: Round, film-coated tablets from light orange to light orange color with a pink tinge, with a dividing risk on one side.

Tablets 25 mg: Round, film-coated tablets of blue color, with a dividing risk on one side.

Tablets 50 mg: Round, film-coated tablets of yellow color, with a dividing risk on one side.

Tablets of 100 mg: Round, film-coated tablets of blue color, without dividing risks.

Pharmacotherapeutic group:antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.C.02 Thioridazine

Pharmacodynamics:

The basic pharmacological properties of thioridazine are similar to those of other phenothiazines, however its clinical spectrum differs significantly from the spectrum of other drugs of this class. Distinctive features of Tiodazine are a low ability to cause extrapyramidal disorders, its quite pronounced sedative and anxiolytic activity. Has moderate alpha-adrenoblocking and M-cholinoblocking action. It causes hypotensive and antiemetic effects. When used in low doses, thiodazine has an anxiolytic effect. Relieves feelings of tension and anxiety; It is also effective for mild depressive disorders. With the use of Thiodazine, there is an improvement in the patient's adaptation to the surrounding reality.

When used in high doses, thiodazine has an antipsychotic effect. Thiodasin has a wide therapeutic range. When used in the recommended dose range, the drug is well tolerated.

Pharmacokinetics:

Suction. Thiodasin is rapidly absorbed from the gastrointestinal tract.Maximum plasma concentrations are achieved 2-4 hours after admission. Bioavailability averages about 60%. Significant interindividual variability of this indicator was noted. Binding to proteins is high (more than 95%).

Thiodazine penetrates the placenta and is excreted into breast milk. Thiodasin and its major metabolites (sulfonidazine and mesoridazine) penetrate across

the blood-brain barrier and are found in the cerebrospinal fluid. The ratio of the concentration of metabolites in the cerebrospinal fluid to their plasma concentration is higher than the same ratio for the unchanged drug, which indicates the essential role of metabolites in the implementation of the antipsychotic action of the drug. Excretion. Excretion is carried out mainly with feces (50%), as well as through the kidneys (less than 4% in the form of an unchanged drug, about 30% - in the form of metabolites). The plasma half-life is approximately 10 hours.

Indications:

A) Schizophrenia and other psychosis

B) Treatment of exacerbations of schizophrenia.

C) Treatment of schizophrenia of chronic course. Thiodasin is also indicated for long-term treatment of patients undergoing inpatient treatment and long-term maintenance treatment of outpatients with schizophrenia.

B) Syndromes of anxiety and depression

- In psychiatric practice - as a monotherapy or as part of a combination therapy of patients with agitated depression.

- In general medical practice - as a sedative and anxiolytics - treatment of various syndromes characterized by anxiety, a combination of anxiety and depression, tension and agitation, psychosomatic disorders and emotional disorders.

- Long-term treatment of mixed anxiety-depressive conditions or psychotic depression.

B) Indications in geriatric practice

- As a neuroleptic and antipsychotic agent - treatment of severe cognitive disorders and behavioral disorders in geriatric patients with organic brain damage of varying severity.

- As an anxiolytic or sedative - treatment of anxiety states, mixed anxiety-depressive states, senile agitation and insomnia.

D) Indications in pediatric practice

- As a neuroleptic - treatment of childhood schizophrenia, as well as severe behavioral disorders against the backdrop of mental retardation and organic brain damage.

- As an anxiolytic or sedative - treatment of anxiety, tension, agitation; treatment of violations of concentration in children with pronounced behavioral disorders; treatment of cases of hyperactivity resistant to stimulants; treatment of sleep disorders.

E) Other indications

- Treatment of severe behavioral disorders in mentally retarded adult patients and patients with deficiency symptoms.

- To reduce the severity of such mental manifestations as anxiety, agitation, hostility and hallucinations in the syndrome of alcoholic abscess.

- Vomiting of the central genesis.

Contraindications:

Increased individual sensitivity to thioridazine hydrochloride, thioridazine base or any other component of the drug. Comatose conditions or conditions of severe central nervous system depression, anamnestic data on serious hematological diseases, in particular, oppression of bone marrow hematopoiesis.

Anamnestic information on reactions of increased individual sensitivity, such as severe photosensitivity or increased individual sensitivity to other phenothiazines.

Severe heart disease, especially clinically significant arrhythmias (in particular, ventricular tachycardia).

Pregnancy and lactation:

Pregnancy, the period of breastfeeding.

TIODAZIN should not be administered to children under 2 years of age.

Dosing and Administration:

The dose and time of taking the drug should be selected individually depending on the disease and the severity of the symptoms. It is recommended to start treatment with doses at the lower limit of the specified range. Then, during the treatment, the dose is gradually increased to achieve the maximum effective dose. When the maximum therapeutic effect is achieved, the dose is gradually reduced to a supporting dose. The daily dose is usually divided into 2-4 admission.

Schizophrenia and other psychosis

Exacerbations of schizophrenia in adults hospitalized patients: 100-600 mg / day - up to a maximum dose of 800 mg / day.

Schizophrenia of chronic course: 100-600 mg / day. in hospitalized patients; 50-300 mg / day - for outpatients.

Syndromes of anxiety and depression

In psychiatric practice, patients with agitated depression: 25-200 mg / day.

In general medical practice, as a sedative and anxiolytic: 10-75 mg / day.

In geriatric practice

As a neuroleptic / antipsychotic agent: 25-200 mg / day.

As an anxiolytic / sedative: 10-75 mg / day.

In pediatric practice

As a neuroleptic for the treatment of severe mental and emotional disorders in children older than 2 years: 1-3 mg / kg / day.

As an anxiolytic / sedative in children over 2 years of age: 0.5-2 mg / kg / day.

Other indications

Treatment of severe behavioral disorders in mentally retarded adult patients and patients with deficiency symptoms: 100-600 mg / day; the maximum dose is 800 mg / day. To reduce the severity of mental disorders in alcohol withdrawal syndrome: 100-200 mg / day.

Treatment of patients with a deficiency of body weight, impaired renal and / or liver function, as well as patients of the elderly and children is recommended to be carefully controlled and started with especially small doses and to increase them very slowly.

In patients with schizophrenia who are on inpatient treatment, a clear positive effect is usually achieved in 2-3 weeks or more from the start of treatment. In patients with chronic psychoses, it may take from 6 weeks to 6 months to achieve the most pronounced effect.On the contrary, in patients with acute psychosis, improvement of the condition can be noted after 24-48 hours.

In case of cancellation of long-term therapy with Thiodazine, its dose is recommended to be reduced gradually, within a few weeks, since sudden withdrawal in patients receiving the drug for a long time or at high doses can in some cases lead to such phenomena as nausea, vomiting, tremor, dizziness, excitation, insomnia, transient dyskinesia. These phenomena can create an erroneous impression of the patient's depressive or psychotic state.

Side effects:

Side effects of Thiodazine, like other phenothiazines, depend on the dose and, as a rule, are due to the pronounced pharmacological effects of the drug. When applying the drug in the recommended dose range, adverse events are mostly mild and transient in nature. Severe events are noted when high doses of thiodazine are used.

From the side of the central nervous system: sedative effect, drowsiness; dizziness; sometimes - a violation of consciousness, psychomotor agitation, hallucinations, increased irritability,headache; rarely - convulsions, extrapyramidal symptoms (tremor, muscle rigidity, akathisia, dyskinesia, dystonia), tardive dyskinesia; very rarely - depression, insomnia, malignant neuroleptic syndrome.

On the part of the autonomic nervous system / anticholinergic effects: often - dry mouth, blurred vision, paresis of accommodation, nasal congestion; sometimes - nausea, vomiting, diarrhea, constipation, loss of appetite, delay or incontinence; rarely pallor, tremor; very rarely - paralytic intestinal obstruction.

From the cardiovascular system: often - orthostatic hypotension; sometimes, ECG changes (prolongation of the QT interval), tachycardia; rarely - arrhythmia; very rarely - fluttering-fibrillation of the ventricles, sudden death.

On the part of the endocrine system: often, with prolonged admission - hyperprolactinaemia, galactorrhea; sometimes - amenorrhea, menstrual irregularities, changes in body weight, erectile dysfunction and ejaculation; rarely - priapism; very rarely - engorgement of the mammary glands, gynecomastia, peripheral edema.

From the peripheral blood: rarely - leukopenia, agranulocytosis,

thrombocytopenia; very rarely - anemia, leukocytosis.

From the side, sometimes deviations from the norm of hepatic enzyme activity; rarely hepatitis.

From the skin: rarely - dermatitis, skin rash (including allergic), urticaria, increased photosensitivity, angioedema.

Other: rarely - swelling in the parotid gland, hyperthermia, respiratory depression. With prolonged therapy with Chiodazine, there are reports of rare cases of pigment retinopathy, developed in patients who received the drug at a dose exceeding the recommended maximum dose of 800 mg per day.

Overdose:

Increased side effects, the emergence of acute neuroleptic reactions. Particularly should alarm the increase in body temperature, which may be one of the symptoms of malignant neuroleptic syndrome. In severe cases of overdose, various forms of impairment of consciousness, up to coma, can occur.

Measures of assistance: End of therapy with Thiodazin and any other

antipsychotic drugs (neuroleptics), the appointment of correctors (central holinoblokatorov), the appointment of high doses of activated carbon, gastric lavage,with convulsions, intravenous diazepam, glucose solution, nootropic drugs, B and C vitamins, careful monitoring of the functions of the cardiovascular, respiratory and central nervous system, symptomatic therapy.

In cramps, the use of barbiturates should be avoided, as they can enhance respiratory depression caused by the phenothiazine derivative.

Interaction:

Metabolism mediated by cytochrome P450 2D6. TIODAZINE is metabolized by the enzyme cytochrome P450 2D6, and, in addition, itself is an inhibitor of this pathway of metabolism. In this regard, drugs that inhibit this isoenzyme (for example, cimetidine, fluoxetine, paroxetine, moclobemide), can enhance and prolong the effects of thiodazine.

Tricyclic antidepressants. The simultaneous use of tricyclic antidepressants and phenothiazine derivatives can lead to an increase in plasma concentrations of these drugs and / or a phenothiazine derivative, which can lead to cardiac arrhythmias.

Anticonvulsants. Thiodazine, like other phenothiazines, can reduce the threshold of convulsive readiness.With simultaneous use with Thiodasin, an increase or decrease in the concentration in the serum of phenytoin is possible, which may require correction of its dose. With the combined use of thiodazine and carbamazepine, the concentrations of these drugs in the serum do not change. Antihypertensive agents and beta-blockers. Due to the inhibition of metabolism, the combined use of these agents by Thiodasin can lead to an increase in the plasma concentrations of each drug, which can probably lead to severe hypotension, cardiac rhythm disturbances, or side effects from the CNS.

Indirect anticoagulants. Co-administration with Tiodazine may cause an increase in hypoprothrombinemic action, which is mainly due to competitive interaction at the enzyme level. In this case, a careful monitoring of the prothrombin concentration in the plasma is necessary.

Means with inhibitory effect on the central nervous system. Thiodasin can enhance the effects of alcohol and other drugs that have a depressing effect on the central nervous system, benzodiazepines, narcotic analgesics, barbiturates, antidepressants and anesthesia.

MAO inhibitors.Simultaneous use of MAO inhibitor and Thiodazine may prolong and intensify the sedative and antimuscarinic action of each of the drugs. Lithium preparations. Possible occurrence of severe neurotoxic complications, extrapyramidal disorders and somnambulism in patients receiving both a lithium preparation and a phenothiazine derivative, including Thiodazine.

Means with anticholinergic action. With simultaneous application with Thiodazine, the anticholinergic effects of M-cholinoblockers (atropine-like drugs), antihistamines and tricyclic antidepressants, up to such manifestations as "atropine psychosis", severe constipation, paralytic intestinal obstruction, hyperpyrexia with possible thermal shock are possible. In these cases, careful monitoring of the patient and correction of the doses of the drugs are shown.

Antiparkinsonian means. With the simultaneous use of thiodazine and levodopa, the effects of each drug may be weakened.

Vasoconstrictors. Due to its a-adrenoblocking properties, thiodazine can weaken the pressor effect of vasoconstrictors (epinephrine, dopamine, ephedrine, phenylephrine).

Heaney din. With the simultaneous use of quinidine and thiodazine, the inhibitory effect of quinidine on the myocardium can be increased.

Antiarrhythmic agents / QT interval prolongation. Given that phenothiazines, including Thiodasin, can cause such changes in the ECG as an extension of the QT interval, caution should be exercised when they are used simultaneously with drugs with a similar property.

Thiazide diuretics .. Simultaneous use of thiodazine and thiazide diuretic can lead to severe arterial hypotension. In addition, diuretic-induced hypokalemia may enhance the cardiotoxic effects of thiodazine. Antidiabetic drugs. Thiodasin affects the carbohydrate metabolism, and as a result, when it is used, the stable state of the patient, achieved against the background of treatment with antidiabetic agents, can be violated.

Antacids and protivogodirayanye funds can reduce absorption from the gastrointestinal tract of Chiodazine.

Special instructions:

With extreme caution apply in patients with glaucoma (especially the closed-angle form), with cardiovascular diseases, severe respiratory diseases, kidney failure, Parkinson's disease,epilepsy, prostatic hypertrophy, myasthenia gravis, pheochromocytoma.

During the period of treatment with Chiodazine, alcohol intake is prohibited, as well as driving vehicles, working with mechanisms and other activities requiring quick reaction.

Form release / dosage:

covered with a film coating of 10 mg, 100 mg, 25 mg, 50 mg.

Packaging:

10 tablets in aluminum strips, 10 strips in a cardboard box.

Storage conditions:

: List B. Released by prescription.

At a temperature not higher than + 25 ° C, in a dry place, protected from light, out of reach of children.

Shelf life:4 years. Do not use after expiration date

Terms of leave from pharmacies:On prescription

Registration number:П N014622 / 01-2002

Date of registration:23.03.2009

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Information update date: & nbsp10.09.2015

Illustrated instructions

Instructions

Thiodasin (Thiodazine)