Rapidly absorbed from the gastrointestinal tract. Maximum plasma concentration is achieved 2-4 hours after administration. Bioavailability is an average of about 60%. There was a considerable interindividual variability of this parameter. Protein binding is high (over 95%). Crosses the placenta and is excreted into breast milk. Tiodazin and its main metabolites (sulforidazin and clomiphene citrate mesoridazine) cross the blood-brain barrier and are found in the cerebrospinal fluid. The ratio of the concentration of metabolites in the cerebrospinal fluid in their plasma concentrations higher than the same ratio for the unchanged drug, indicating the important role of metabolites in the implementation of the antipsychotic drug action. Withdrawal. Withdrawal is carried out mainly in the feces (50%), via the kidneys as well as (at least 4% of unchanged drug in the form of about 30% – as metabolites). Plasma half-life is approximately 10 hours.
Indications for use:
A) schizophrenia and other psychoses
- Treatment of exacerbations of schizophrenia.
- Treatment of chronic schizophrenia. Clomiphene citrate also indicated for long-term treatment of patients who are hospitalized, and long-term maintenance treatment of outpatients with schizophrenia.
B) anxiety and depression syndromes
- In psychiatric practice – as monotherapy or as part of combination therapy in patients with agitated depression.
- In general medical practice – as a sedative and anxiolytic – treatment of a variety of syndromes characterized by anxiety, a combination of anxiety and depression, tension and agitation, psychosomatic disorders and emotional disorders.
- Long-term treatment of mixed anxiety and depression or psychotic depression.
Bed and) indications in geriatric practice
- As a neuroleptic and antipsychotic – treatment of severe cognitive disorders and behavioral disorders in geriatric patients with organic brain damage of varying severity.
- As anxiolytics or sedative – treatment of anxiety, mixed anxiety-depressive states, senile agitation and insomnia.
D) Indications in pediatric practice
- As an antipsychotic – treatment of childhood schizophrenia, and severe behavioral disorders on the background of mental retardation and organic brain damage.
- As anxiolytics or sedative – treatment of anxiety, tension and agitation; treatment of disorders of concentration in children with severe behavioral problems; hyperactivity treatment of cases that are resistant to stimulants; treatment of sleep disorders.
D) Other readings
- Treatment pronounced behavioral disorders in mentally retarded adults and in patients with deficiency of symptoms.
- To reduce the severity of clomiphene citrate psychotic episodes as anxiety, agitation, hostility, hallucinations, and the syndrome of alcoholic absistentsii.
- Vomiting of central origin.
Increased individual sensitivity to thioridazine hydrochloride, thioridazine base, or any other component of the formulation. Comatose states or state of severe depression of the central nervous system, history of severe hematological diseases, in particular depression medullary hematopoiesis.
A history information of individual hypersensitivity reactions, such as severe photosensitivity or increased individual sensitivity to other phenothiazines.
Severe heart disease, especially clinically significant arrhythmias (such as ventricular tachycardia).
Dosage and administration:
The dose and timing of the doses should be individualized depending on the severity of the disease and symptoms. Initiate therapy with the recommended dose, are at the lower boundary of the range. Then, in the course of treatment the dose is gradually increased to achieve maximum efficiency. When you achieve the maximum therapeutic effect gradually reduce the dose to maintenance. The daily dose is usually divided into 2-4 reception. Schizophrenia and other psychoses Exacerbation of schizophrenia in adult hospitalized patients: 100-600 mg / day – up to a maximum dose of 800 mg / day.Schizophrenia is a chronic flow: 100-600 mg / day. in hospitalized patients; 50-300 mg / day – in outpatients. Anxiety and depression syndromes in psychiatric practice with agitated depression patients: 25-200 mg / day. In general practice as a sedative and anxiolytic: 10-75 mg / day. In geriatric practice as neuroleptic / antipsychotic: 25-200 mg / day. As anxiolytics / sedatives: 10-75 mg / day. In the pediatric practice as an antipsychotic for the treatment of serious mental and emotional disorders in children older than 2 years: 1-3 mg / kg / day.
- As an anxiolytic / sedative in children older than 2 years: 0.5-2 mg / kg / day. Other indications Treatment pronounced behavioral disorders in mentally retarded adults and in patients with deficiency of symptoms: 100-600 mg / day; the maximum dose – 800 mg / day. To reduce the severity of mental disorders with alcohol withdrawal syndrome:. 100-200 mg / day treatment of patients with low body weight, impaired renal function and / or liver, clomiphene citrate as well as elderly patients and children recommended under close supervision and to start with especially low doses and increase them slowly. patients with schizophrenia who are hospitalized, a clear positive effect is usually achieved within 2-3 weeks or more from the start of treatment. In patients with chronic psychosis in order to achieve the most pronounced effect it may take 6 weeks to 6 months. In contrast, in patients with acute psychotic condition improvement can be observed after 24-48 hours. In case of cancellation of long-term therapy Tiodazinom the dose recommended to be reduced gradually, over several weeks, as the sudden cancellation of the patients receiving the drug for a long time or in high doses, can lead in some cases to such phenomena as nausea, vomiting, tremor, dizziness, anxiety, agitation, insomnia, transient dyskinesia. These phenomena can create a false impression of occurrence in a patient of a depressive or psychotic state.