Trifluoperazin

Unlike chlorpromazine, trifluoperazin has a weak adrenolytic effect, almost does not give a hypotensive effect. Potentiates the effect of sleeping pills less; does not have antihistamine, antispasmodic and anticonvulsant activity. It has a strong cataleptogenic effect.

They are used in psychiatric practice to treat various forms of schizophrenia, especially paranoid , and other mental disorders that occur with delusional symptoms and hallucinations, and are also used for alcoholic psychoses ^[3] , involutional psychoses, anxiety disorders, and other diseases of the central nervous system . A randomized, placebo-controlled study showed the efficacy of trifluoperazin in generalized anxiety disorder , but the benefit / risk ratio is unclear due to side effects ^{[5] [6]} .

Trifluoperazin has a more pronounced effect on productive psychotic symptoms (hallucinations, delirium) than chlorpromazine. A distinctive feature of trifluoperazin is the lack of stiffness, general weakness, and stupor in its use; on the contrary, patients often become more lively, begin to show interest in the environment, are more easily involved in labor processes. In the early days of treatment, drowsiness may occur.

The drug is able to stop hallucinatory and delusional excitement, however, anxious, catatonic , manic excitement not only does not relieve, but can also enhance ^[7] .

Trifluoperazin is prescribed orally (after eating) and intramuscularly. A single dose when taken orally at the beginning of treatment is usually 0.005 g (5 mg). In the future, the dose is gradually increased by 0.005 g per dose to a total daily dose of 0.03-0.08 g (in some cases, up to 0.1-0.12 g per day); the daily dose is divided into 2–4 doses. Upon reaching the therapeutic effect, the optimal doses are maintained for 1-3 months, then they are reduced to 0.02-0.005 g per day. These doses are subsequently prescribed as supportive.

Trifluoperazin is administered intramuscularly in cases requiring a quick effect. Initial doses are 0.001-0.002 g (1-2 mg). Injections are repeated after 4-6 hours. The daily dose is usually up to 0.006 g (6 mg), in rare cases, up to 0.01 g (10 mg).

In patients with alcoholism, trifluoperazin is used to treat acute and chronic hallucinatory and delusional psychoses, and to stop psychomotor agitation. In acute psychotic conditions, treatment begins with intramuscular injections, moving on to ingestion after the removal of the acute phenomena of psychosis. Trifluoperazin is also prescribed for the treatment of neurosis and psychopathic disorders in patients with alcoholism, in the event of apato-abulic conditions .

Treatment with trifluoperazin can be combined with the appointment of other antipsychotics, tranquilizers, antidepressants.

As an antiemetic, trifluoperazin is used for vomiting of various etiologies at 0.001-0.004 g (1-4 mg) per day.

During treatment with trifluoperazin, extrapyramidal disorders are often observed (in 60–78% of patients ^[8] ): parkinsonism , dyskinesias , akathisia , tremor . Dyskinesias are especially common ^[8] : torticollis, grimacing, trismus , loss of tongue and involuntary eye movements (including oculomotor crises ) ^[9] ; dyskinesias are often accompanied by the affect of anxiety, fear, depression ^[10] . Antiparkinsonian drugs are prescribed as correctors for extrapyramidal disorders: cyclodol , tropacin, and others. Dyskinesias are stopped with caffeine-benzoate sodium (2 ml of a 20% solution under the skin) or chlorpromazine (1-2 ml of a 2.5% solution intramuscularly ).

With prolonged use, the development of tardive dyskinesia is possible (which develops more often with trifluoperazin than with most other antipsychotics) ^[10] , a malignant antipsychotic syndrome .

Other side effects of the central nervous system : feeling tired, drowsiness, dizziness, passing anxiety, insomnia, muscle weakness, anorexia , decreased ability to concentrate ^[9] , vegetovascular disorders ^[11] , depression ^[12] , antipsychotic deficiency syndrome ^[10] .

From the gastrointestinal system: dry mouth, anorexia ^[11] ; toxic effects on the liver , up to the development of cholestatic jaundice , sometimes chronic liver damage ^[13] .

From the endocrine system : hyperprolactinemia ^[4] . An increase in prolactin caused by the use of antipsychotics can lead to a decrease in sexual desire and sexual dysfunction, amenorrhea , galactorrhea ^[14] , gynecomastia , a decrease or lack of potency ^[15] , infertility ^{[15] [16]} , the development of osteoporosis , and the occurrence of cardiovascular disorders ^[15] , weight gain, autoimmune disorders , water and electrolyte imbalance ^[17] , the risk of developing breast cancer ^[14] , type II diabetes mellitus ^[18] , and the pituitary tumor ^[19] . Mental manifestations of prolonged hyperprolactinemia can include depression, anxiety, irritability, sleep disturbances, as well as increased fatigue, weakness, and memory loss ^[15] .

From the hemopoietic system: thrombocytopenia , anemia , agranulocytosis , rarely - pancytopenia ^[9] .

From the cardiovascular system: tachycardia , moderate hypotension with a change in body position, cardiac arrhythmias, ECG changes ^[9] .

Allergic reactions: skin rash, urticaria , angioedema ^[9] .

Other: dry mouth, blurred vision, constipation, urinary retention, hyperthermia , weight gain, edema ^[9] , with prolonged use - pigmentation of the conjunctiva and cornea ^[10] .

Trifluoperazin is less likely to cause impaired liver function and agranulocytosis than chlorpromazine; allergic skin reactions are rarely observed.

The drug is contraindicated in coma ^[9] , acute inflammatory liver diseases, heart diseases with impaired conduction and decompensation, in acute blood diseases, severe liver and kidney diseases, pregnancy ^[9] , breastfeeding ^[9] , and increased sensitivity to the drug ^[9] .

With caution, the drug is prescribed for patients suffering from glaucoma , cardiovascular diseases, epilepsy , prostatic hypertrophy ^[9] .

Patients engaged in potentially hazardous activities requiring increased concentration of attention, as well as rapid mental and motor reactions, should be warned about the possibility of reducing the speed of response and reducing concentration ^[9] .

Trifluoperazin should not be prescribed for mental illness with depressive symptoms ^[9] .

If the patient has had hypersensitivity reactions during previous treatment with phenothiazine antipsychotics (for example, blood dysrasia , jaundice ), phenothiazine antipsychotics, in particular trifluoperazin, should not be prescribed to the patient, unless the doctor considers that the potential benefits of taking the drug may outweigh the potential risk ^[11] .

With prolonged use of trifluoperazin in high doses, it is necessary to take into account the possibility of cumulative effects with the sudden onset of severe symptoms from the central nervous system and vasomotor disorders ^[11] .

In the treatment of trifluoperazin, alcohol should not be consumed ^[20] .

Trifluoperazin potentiates the effect on the central nervous system of strong analgesics , sleeping pills, and alcohol ^[9] . Enhances the effects of anxiolytics . The combination of trifluoperazin with paroxetine enhances the effect of both drugs ^[21] . With simultaneous administration with levodopa (in patients with Parkinson's disease ), it can cause a deterioration in the course of Parkinson's disease. The drug reduces the hypotensive effect of guanethidine . With simultaneous use with related prochlorperazines , a prolonged unconscious state may occur ^[9] . When combined with sedatives or with procarbazine , the sedation is enhanced ^[21] .

In the USSR, the industrial production of triftazine was first mastered at the Kirov-Chepetsk Chemical Plant in April 1966 on the basis of technology developed by the Institute of Pharmacology and Chemotherapy of the USSR Academy of Medical Sciences . The need for an effective psychotropic drug was due to the appearance of tens of thousands of patients in need after a catastrophic Tashkent earthquake ^[22] .

• Mashkovsky M. D. Medicines. - 15th ed. - M .: New Wave, 2005 .-- S. 57. - 1200 p. - ISBN 5-7864-0203-7 .
• Mashkovsky M. D. Medicines. - 16th ed. - M .: “The New Wave”, 2012. - S. 59. - 1216 p. - ISBN 978-5-7864-0218-7 .

• Trifluoperazin // Medicines / M.D. Mashkovsky . - Reference Mashkovsky on-line .