Triftazin-Darnitsa

General characteristics. Structure:

Active ingredient: trifluoperazine;

1 ml of solution contains a trifluoperazin of a hydrochloride in terms of 100% dry matter – 2 mg;

excipients: sodium citrate, water for injections.

Pharmacological properties:

Pharmacodynamics. Triftazin-Darnitsa – antipsychotic means (neuroleptic), piperazinovy derivative a fenotiazina. Possesses the antipsychotic, sedative, antiemetic, cataleptic, hypotensive, hypothermal and weak holinoblokiruyushchy action which is also directed against a hiccups.

Antipsychotic action is connected with blockade of D2 - dopamine receptors of mesolimbic and mesocortical systems, blockade of α-adrenoceptors in the central nervous system, increase in release of hormones of a hypothalamus and a hypophysis.

Sedative action develops owing to blockade of adrenoceptors of a reticular formation of a trunk of a brain.

Antiemetic action is connected with blockade of peripheral and central D2 - dopamine receptors, blockade of the terminations of a vagus nerve in digestive tract.

Hypothermal action develops due to blockade of dopamine receptors of a hypothalamus.

Sedative action and influence on the autonomic nervous system is expressed more weakly, than at other derivatives of a fenotiazin, extrapyramidal and antiemetic action – is stronger.

Pharmacokinetics. After intramuscular introduction has effect of "primary passing" through a liver. Strongly contacts proteins of a blood plasma, the level of communication makes 95%. Time of achievement of the maximum concentration (Tmax) in blood – 1-2 hours. Gets through a blood-brain barrier, into breast milk. It is intensively metabolized in a liver, metabolism products pharmacological are inactive. The elimination half-life (T1/2) makes 15-30 hours. Metabolites are brought out of an organism by bile and kidneys. It is poorly dialyzed in connection with high linkng with proteins of plasma.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless or slightly yellowish liquid.

Incompatibility.

Solutions of a trifluoperazin and other drugs of a fenotiazinovy row are incompatible with solutions of barbiturates, carbonates, Ringer's solution (formation of a deposit).

It is not necessary to enter in one syringe with other medicines.

Indications to use:

Psychotic frustration, including schizophrenia.

Route of administration and doses:

Apply intramusculary. The initial dose for adults makes 1-2 mg. Repeated introduction is made in 4-6 hours; at more frequent injections the cumulation phenomena are possible. The daily dose is, as a rule, equal to 6 mg, in exceptional cases – 10 mg.

At depressive and hallucinatory and depressive and crazy states Triftazin-Darnitsa apply together with antidepressants.

Treatment of Triftazinom-Darnitsa has to be strictly individualized depending on the course of a disease. The term of treatment should not exceed 12 weeks.

Features of use:

Use during pregnancy or feeding by a breast.

Drug is contraindicated during pregnancy. In need of drug use feeding by a breast should be stopped. 

Children.

It is not recommended to use drug for treatment of children in view of limited clinical experience.

At treatment by drug it is necessary to avoid influence of high temperature (possibly thermal control disturbance).

Use of fenotiazinovy drugs for elderly patients with dementia increases risk of a lethal outcome.

Use of drug has to continue not longer, than 12 weeks as it can lead to development of constant late dyskinesia which can be irreversible.

With care appoint drug to patients with glaucoma (it is contraindicated at a closed-angle form of glaucoma), cardiovascular diseases.

At emergence of symptoms of late dyskinesia or a malignant antipsychotic syndrome administration of drug should be stopped.

To patients with a syndrome to Reja, an ischuria, chronic diseases of a respiratory organs, vomiting drug is appointed only after comparison of risk and advantage of treatment.

At treatment of not psychotic alarm трифлуоперазин most of patients should appoint after use of alternative drugs (for example, benzodiazepines) which have no side reactions inherent in a trifluoperazin.

Patients of advanced age are more inclined to development of arterial hypotension and neuromuscular reaction; for such patients during treatment careful observation is necessary. The drug dosage in the lower range is sufficient for most of elderly patients. The dosage has to be adapted for the level of individual reaction and is appropriately corrected. Increase in a dose to such patients has to happen more slowly and gradually. Use of drug can cause display of irreversible dyskinesia in elderly patients.

It is not recommended by drug to take alcohol during treatment.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

During treatment by drug it is necessary to abstain from control of motor transport and from occupations potentially dangerous types of activity demanding the high speed of psychomotor reactions.

Side effects:

From the central and peripheral nervous system: headache, drowsiness, dizziness, sleeplessness, akathisia, dystonic extrapyramidal reactions, pseudoparkinsonism, late disamneziya, malignant antipsychotic syndrome, phenomena of mental indifference, overdue reaction to external irritants, akinetiko-rigid phenomena, hyperkinesias, tremor, vegetative disturbances, late dyskinesia of facial muscles, dystonia, thermal control disturbance, fatigue, consciousness disturbance, muscle tension, spasms.

From sense bodys: accommodation paresis, retinopathy, phacoscotasmus and corneas, disturbances of visual perception, conjunctivitis.

From digestive tract: dryness in a mouth, anorexia, bulimia, nausea, vomiting, diarrhea, a lock, a gastralgia, intestines paresis, a lockjaw, a language protrusion.

From a liver and biliary tract: cholestatic jaundice, hepatotoxic, hepatitis.

From endocrine system and metabolic disturbances: hypo - or a hyperglycemia, a glucosuria, disturbance of a menstrual cycle (a dysmenorrhea, an amenorrhea), a gynecomastia, increase in body weight, a galactorrhoea, a stethalgia, a lactation, disturbance of a libido, a giperprolaktinemiya.

From cardiovascular system: tachycardia, a lowering of arterial pressure (orthostatic hypotension), disturbances of a heart rhythm, change of an ECG (lengthening of an interval of QT, smoothing of a tooth of T), stenocardia attacks, ventricular arrhythmia as torsades de pointes, a cardiac standstill.

From system of blood and a hemopoiesis: thrombocytopenia, agranulocytosis, anemia (hemolitic, aplastic), pancytopenia, leukopenia, Werlhof's disease, eosinophilia.

From urinogenital system: decrease in a potentiality, disturbance of an ejaculation, priapism, ischuria, oliguria, disturbance of an urination.

From a musculoskeletal system: myasthenia.

Dermatological disturbances: fotodermiya, erubescence, skin depigmentation, exfoliative dermatitis.

Allergic reactions: skin rash, small tortoiseshell, Quincke's disease, acute anaphylaxis.

Pathological results of laboratory researches: false positive tests for pregnancy, fenilketonuriya.

Others: hypostases.

Interaction with other medicines:

Means, the oppressing functions of the central nervous system (anesthetic, opioid analgetik, barbiturates, anxiolytics, ethanol, etanolsoderzhashchy drugs) – the effect of drug amplifies, the depression of the central nervous system amplifies and breath is oppressed.

The inductors CYP1A2 (carbamazepine, phenobarbital, rifampicin, aminoglutethimide) – reduce concentration and Triftazin-Darnits's effect.

CYP1A2 inhibitors (Amiodaronum, ciprofloxacin, флувоксамин, кетоконазол, norfloxacin, ofloxacin, рофекоксиб) – increase concentration and Triftazin-Darnits's effect.

α-adrenoblockers - - - - - - - - - – increase hypotensive effects of drug.

The levodopa and Phenaminums – reduce effect of drug.

Antiepileptic means – at simultaneous use the effect of antiepileptic drugs decreases.

Anti-thyroid drugs – the risk of development of an agranulocytosis increases.

Astemizol, Disopyramidum, erythromycin, procaineamide – increases risk of development of tachycardia.

Tricyclic antidepressants, Maprotilinum, MAO inhibitors – are possible lengthening and strengthening of sedative and anticholinergic effects of Triftazin-Darnits.

Lithium drugs – strengthening of extrapyramidal disturbances, early approach of symptoms of intoxication lithium is possible.

Adrenomimetiki and sympathomimetics – simultaneous use can lead to a paradoxical lowering of arterial pressure.

Mutually effects at a concomitant use of ethanol amplify.

Anticonvulsant drugs – decrease in a convulsive threshold is possible.

The drugs causing extrapyramidal reactions (Metoclopramidum) – increase in frequency and weight of extrapyramidal disturbances is possible.

Anti-hypertensive drugs – development of orthostatic arterial hypotension is possible.

Prochlorperazine – the long loss of consciousness is possible.

Drug can weaken vasoconstrictive effect of ephedrine and Epinephrinum, to strengthen anticholinergic effects of other drugs, to oppress effect of amphetamines, levodopas, a clonidine, a guanetidin.

Bromocriptinum – fenotiazina oppress ability of Bromocriptinum to reduce concentration of prolactin in blood serum.

Propranolol, sulphadoxine – increase Triftazin-Darnits's concentration in a blood plasma.

Polypeptide antibiotics – simultaneous use can cause paralysis of respiratory muscles.

Trazodonum – is observed the additive hypotensive effect.

Valproinovy acid – at simultaneous use is observed increase in concentration of valproinovy acid in a blood plasma.

Contraindications:

Hypersensitivity to drug components, other drugs of a fenotiaziny row. Dekompensirovanny heart failure, the expressed arterial hypotension. Coma of any etiology. The progressing general diseases of a head and spinal cord. Stenocardia. Breast cancer. Closed-angle glaucoma. Functional renal and liver failure. A peptic ulcer of a stomach and duodenum in the period of an aggravation. Epilepsy, Parkinson's disease. Disturbance of the mechanism of the central regulation of breath (especially at children), a syndrome to Reja. Cachexia. Myxedema. Prostate hyperplasia. The pathological changes of blood connected with hemopoiesis disturbance. Pregnancy and period of feeding by a breast.

Overdose:

The overdose is shown by dyskinesia, a dysarthtia, drowsiness and a stupor, extrapyramidal disturbances, involuntary reductions of muscles, arterial hypotension or hypertensia, cardiac arrhythmias, spasms, changes on an ECG, fever, vegetative frustration, dryness in a mouth, intestinal impassability. In hard cases the coma is possible.

Treatment. Treatment is symptomatic and supporting. At respiratory depression carry out artificial ventilation of the lungs, oxygen therapy. Correction of acid-base equilibrium, water and electrolytic balance, artificial diuresis.

Storage conditions:

Period of validity. 4 years. To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule; on 10 ampoules in a box; on 5 ampoules in a blister strip packaging; on the 2nd blister strip packagings in a pack.