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

Neuroleptic, a phenothiazine derivative. Competitive blockade of postsynaptic dopamine D₂receptors in the mesolimbic structures of the brain. Has a pronounced antiemetic, extrapyramidal effect.

Pharmacokinetics:

High binding to plasma proteins. Excretion through the kidneys, a minor part - with bile.

Indications:

Psychotic disorders, including schizophrenia. Psychomotor agitation. Neuroses with a predominance of anxiety and fear. Symptomatic treatment of nausea and vomiting.

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F21 Chrysotile disorder

V.F20-F29.F22 Chronic delusional disorders

V Mental and behavioral disorders

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F40-F48.F40 Phobic anxiety disorders

V.F40-F48.F41.2 Mixed anxiety and depressive disorder

XVIII.R10-R19.R11 Nausea and vomiting

Contraindications:

Hypersensitivity (including to other phenothiazines), severe cardiovascular diseases (decompensated chronic heart failure, arterial hypotension), severe CNS depression (including on the background of taking medications) and coma of any etiology, head trauma, progressive headache and spinal cord, oppression of bone marrow hematopoiesis, severe hepatic insufficiency, children under three years of age, pregnancy, breast-feeding.

Carefully:

Alcoholism, stenocardia, heart valve damages, limiting the amount of minute blood volume (possibly the development of severe arterial hypotension), pathological changes in the blood, breast cancer, zakratougolnaya glaucoma, prostate hyperplasia, hepatic and / or renal failure, peptic ulcer of the stomach and duodenum exacerbations), diseases accompanied by an increased risk of thromboembolic complications, Parkinson's disease,epilepsy, myxedema, chronic diseases accompanied by respiratory failure (especially in children), Reye's syndrome (increased risk of hepatotoxicity in children and adolescents), cachexia, vomiting, advanced age, patients exposed to high temperatures.

Pregnancy and lactation:

Trifluoperazine is contraindicated for use in pregnancy and lactation.

Recommendations for FDA - Category C.

Dosing and Administration:

Inside adults - 1-5 mg 2 times a day; if necessary, within 2-3 weeks, the dose is increased to 15-20 mg per day, the frequency of application is 3 times a day. Children 6 years and older - 1 mg 2-3 times a day, if necessary, the dose can be increased to 5-6 mg per day.

Intramuscularly, adults - 1-2 mg every 4-6 hours. Children - 1 mg 1-2 times a day.

Maximum doses: adults with oral administration - 40 mg per day, intramuscularly - 10 mg per day.

Side effects:

From the side CNS: drowsiness, dizziness, dry mouth, sleep disorders, fatigue, visual impairment; extrapyramidal disorders, tardive dyskinesia.

From the side digestive system: anorexia, cholestatic jaundice.

From the side hematopoiesis system: thrombocytopenia, anemia, agranulocytopenia, pancytopenia.

From the side of cardio-vascular system: tachycardia, mild orthostatic hypotension, heart rhythm disturbances, ECG changes (prolongation of the QT interval, smoothing of the T wave).

Allergic reactions: skin rash, hives, angioedema.

From the side endocrine system: galactorrhea, amenorrhea.

Overdose:

Not described.

Treatment is symptomatic.

Interaction:

With the simultaneous use of drugs that exert a depressing effect on the central nervous system, ethanol, ethanol-containing drugs, it is possible to increase the inhibitory effect on the central nervous system and respiratory function.

With simultaneous use with anticonvulsants, the threshold of convulsive readiness may be reduced; with agents that cause extrapyramidal reactions, it is possible to increase the incidence and severity of extrapyramidal disorders.

When used simultaneously with tricyclic antidepressants, maprotiline, MAO inhibitors, the risk of developing malignant neuroleptic syndrome.

With simultaneous application with fluoxetine, extrapyramidal symptoms and dystonia may develop.

At simultaneous application with the preparations causing an arterial hypotension, the expressed orthostatic hypotension is possible.

With simultaneous use with methyldopa, a case of paradoxical arterial hypertension is described.

With simultaneous use with drugs for the treatment of hyperthyroidism, the risk of developing agranulocytosis increases.

With simultaneous use with anticholinergic drugs, their anticholinergic effects are enhanced, while the antipsychotic effect of the antipsychotic may decrease.

With the simultaneous use of antacids, antiparkinsonian drugs, absorption of phenothiazines is impaired.

With simultaneous application, the effect of oral anticoagulants is weakened, it is possible to reduce the effectiveness of amphetamines, levodopa, clonidine, guanethidine, epinephrine, and ephedrine.

With simultaneous use with lithium salts neurotoxic effects are possible, the development of extrapyramidal symptoms.

Special instructions:

In the treatment of schizophrenia trifluoperazine in small doses is equal in effectiveness to other neuroleptics, but long-term studies of good quality are required. The frequency of side effects caused is comparable with other antipsychotics.

When appointing elderly patients with mood disorders and senile psychoses is safe and equal in effectiveness to haloperidol (when taking trifluoperazine 1 mg per day for 1.5 months extrapyramidal reactions are not noted).

In the treatment of psychosis demonstrates the effectiveness in smaller doses (10 mg per day) than chlorpromazine.

The optimal minimum dose for the treatment of acute schizophrenia is 5 mg per day.

Instructions

Trifluoperazine (Trifluoperazinum)