Truxal

General characteristics. Structure:

Active ingredient: 5 mg, 15 mg, 25 mg or 50 mg of chlorprothixene of a hydrochloride.

Excipients: starch corn, lactoses monohydrate, коповидон, glycerin of 85%, cellulose microcrystallic, sodium of a kroskarmelloz, talc, magnesium stearate.

Cover: опадрай OY-S-9478 brown (Е 172; Е 171) RM 1030.

Truxal is the neuroleptic derivative of thioxanthene. Renders the antipsychotic, expressed sedative and moderate antidepressive action.

Pharmacological properties:

Pharmacodynamics. Antipsychotic effect of Truxal is connected with its blocking impact on dopamine receptors. Also antiemetichesky and analgesic properties of drug are connected with blockade of these receptors. Truxal is capable to block 5-HT2 - receptors, α1 - adrenoceptors, and also H1 - histamine receptors, than also antihistaminic properties are defined its adrenoceptor blocking, hypotensive.

Pharmacokinetics. Bioavailability of chlorprothixene at oral administration makes about 12%. Chlorprothixene is quickly absorbed from intestines, the maximum concentration in blood serum is reached in 2 hours. Time of semi-removal makes about 16 hours. Chlorprothixene gets through a placental barrier and in small amounts is emitted with breast milk. Metabolites have no antipsychotic activity, are allocated with a stake and urine.

Indications to use:

Truxal is a sedative neuroleptic with a wide range of indications which enter:

- psychoses, including the schizophrenia and maniacal states proceeding with psychomotor excitement, agitation and alarm
- a hungover abstinence syndrome at alcoholism and drug addiction,
- a hyperactivity, irritability, excitement, confusion of consciousness at elderly patients,
- behavior disorders at children,
- depressions, neurosises, psychosomatic frustration,
- sleeplessness,
- pains (in a combination with analgetics).

Route of administration and doses:

Psychoses, including schizophrenia and maniacal states. Treatment is begun with 50 - 100 mg/days, gradually increasing a dose before achievement of optimum effect, usually to 300 mg/days. In some cases the dose can be increased to 1200 mg/days. The maintenance dose usually makes 100 - 200 mg/days.

The daily dose of Truxal is usually divided into 2 - 3 receptions, considering the expressed sedative effect of Truxal, it is recommended to appoint a smaller part of a daily dose in the afternoon, and the most part - in the evening.

Hungover abstinence syndrome at alcoholism and drug addiction. The daily dose divided into 2 - 3 receptions makes 500 mg. The course of treatment usually lasts 7 days. After disappearance of manifestations of abstinence the dose gradually decreases. The maintenance dose of 15 - 45 mg/days allows to stabilize a state, reduces risk of development of the next hard drinking.

At elderly patients in the presence of a hyperactivity, irritability, excitement, confusion of consciousness 15 - 90 mg/days are appointed. The daily dose, as a rule, is divided into 3 receptions.

At children for correction of behavior disorders Truxal is appointed at the rate of 0,5 - 2 mg to 1 kg of weight.

Depressions, neurosises, psychosomatic frustration. Truxal can be applied at the depressions which are especially combined with alarm, tension as addition to therapy with antidepressants or independently. Truxal can be appointed at the neurosises and psychosomatic disturbances which are followed by alarm and depressive frustration to 90 mg/days. The daily dose, as a rule, is divided into 2-3 receptions. As reception of Truxal does not cause development of accustoming or medicinal dependence, it can be applied is long.

Sleeplessness. On 15 - 30 mg in the evening in 1 hour prior to a dream.

Pains. Ability of Truxal exponentiate action of analgetics can be used at treatment of patients with pains. In these cases Truxal appoint together with analgetics in doses from 15 to 300 mg.

Features of use:

Truxal has to be appointed with care to the patients having epilepsy, parkinsonism at the expressed atherosclerosis of vessels of a brain, at tendency to collapses, at the expressed cardiovascular and respiratory insufficiency, at the expressed abnormal liver functions and kidneys, a diabetes mellitus, a prostatauxe.

Use of Truxal can lead to a false positive take when carrying out the immunobiological test of urine for pregnancy, to false increase in level of bilirubin in blood, to change of an interval of QT on the electrocardiogram.

During treatment Truxal recommends to refrain from the use of alcoholic drinks, to avoid the increased insolation.

Reception of Truxal exerts negative impact on the activity demanding the high speed of mental and physical reactions (for example, control of vehicles, service of cars, work at height, etc.).

Side effects:

Drowsiness, tachycardia, dryness in a mouth, the increased perspiration or difficulties of accommodation. These side effects which are usually arising at the beginning of therapy often disappear in process of its continuation.

Orthostatic hypotension can be observed, especially at use of Truxal in high dosages. Dizziness, a dysmenorrhea, skin rashes, locks meet seldom.

Extrapyramidal symptoms are especially rare. Isolated cases of decrease in a convulsive threshold, emergence of a tranzitorny high-quality leukopenia and hemolitic anemia are described.

At prolonged use, especially in high doses, can be observed: cholestatic jaundice, galactorrhoea, gynecomastia, weakening of a potentiality and libido, increase in appetite, increase in body weight.

Interaction with other medicines:

The oppressing effect of chlorprothixene on TsNS can amplify at a concomitant use with ethanol and etanolsoderzhashchy drugs, anesthetics, opioid analgetics, sedative, somnolent, neuroleptics.

Anticholinergic effect of chlorprothixene amplifies at simultaneous use of anticholinergic, antihistaminic and protivoparkinsonichesky means.

Drug strengthens action of antihypertensives.

Simultaneous use of chlorprothixene and adrenaline can lead to arterial hypotension and tachycardia.

Use of chlorprothixene leads to reduction of the threshold of convulsive activity that demands additional dose adjustment of antiepileptic means from patients with epilepsy.

Ability of chlorprothixene to block dopamine receptors reduces efficiency of action of a levodopa.

Emergence of extrapyramidal frustration at simultaneous use of fenotiazin, Metoclopramidum, haloperidol, Reserpinum is possible.

Contraindications:

Oppression of TsNS of any origin (including caused by alcohol intake, barbiturates or opiates), comas, a vascular collapse, diseases of bodies of a hemopoiesis, a pheochromocytoma.

Hypersensitivity to drug components.

Truxal should not be appointed, whenever possible, to pregnant women and during breastfeeding.

Overdose:

Symptoms. Drowsiness, hypo - or a hyperthermia, extrapyramidal symptoms, spasms, shock, a coma.

Treatment. Symptomatic and supporting. The gastric lavage has to be as soon as possible made, use of a sorbent is recommended. The measures directed to maintenance of activity of respiratory and cardiovascular systems have to be taken. It is not necessary to use adrenaline since it can lead to the subsequent lowering of arterial pressure. Spasms can be stopped diazepam, and extrapyramidal symptoms Biperidinum.

Storage conditions:

List B. At a temperature not above 25 °C. To store in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated 5, 15, 25 and 50 mg. Packaging: on 50 or 100 tablets in the plastic container with a transparent bottom and control of the first opening corked by the plastic cover having a cavity in which the application instruction invests.