Flyuanksol of depot

General characteristics. Structure:

Solution for injections: 1 ml contains 20 mg or 100 mg цис (Z) - a flyupentiksola of a dekanoat in vegetable oil (Viscoleo®).

Pharmacological properties:

Pharmacodynamics. Flyuanksol of depot is derivative thioxanthene with the expressed antipsychotic, activating and anxiolytic action.

Antipsychotic action of neuroleptics is usually connected with blockade of dopamine receptors that, apparently, causes chain reaction in which also other mediator systems are involved.

FLYUANKSOL is especially shown to DEPOT for treatment of patients with chronic psychoses. It reduces the main symptoms of psychosis such as hallucinations, paranoid nonsense and disturbances of thinking. Antipsychotic action amplifies with increase in a dose. In small and medium doses (to 100 mg of 1 times in 2 weeks) FLYUANKSOL of DEPOT does not show nonspecific sedative action which, however, can develop when using drug in high doses. FLYUANKSOL renders to DEPOT rastormazhivayushchy (anti-autistic and activating) action, and also weakens secondary frustration of mood that promotes activation of patients with depressive symptomatology, an otgorozhennost, lack of initiative, increases skill to communicate and facilitates social adaptation. FLYUANKSOL of DEPOT has considerably the big duration of action, than FLYuANKSOL. It allows to carry out continuous antipsychotic therapy FLYUANKSOLY DEPOT that is especially important for treatment of the patients who are not carrying out medical appointments. Thus, FLYUANKSOL of DEPOT prevents the frequent recurrence connected with any interruption by patients of reception of peroral medicines.

Pharmacokinetics. Clinical tests FLYUANKSOL DEPOTS showed that its injections can be made bucketed in 2-4 weeks. After an injection цис (Z) - флюпентиксол деканоат is exposed to zymolysis on active component цис (Z) - флюпентиксол and decanoic acid. Tsis (Z) - флюпентиксол slightly gets through a placental barrier and in small amounts is allocated with breast milk. Metabolites have no antipsychotic activity and are allocated, generally with a stake and, partially, with urine. The maximum concentration цис (Z) - a flyupentiksola in serum is reached by the end of the first week after an injection.

The concentration curve in serum decreases exponential with the elimination half-life equal to about 3 weeks that reflects the speed of release of drug from depot.
Pharmacokinetically the dose FLYUANKSOL to DEPOT of 40 mg of 1 times in 2 weeks is equivalent to daily reception of FLYuANKSOLA orally in a dose of 10 mg within 2 weeks.

Indications to use:

The psychotic states with dominance of gallyutsinatsinatorny symptomatology, paranoid nonsense and disturbances of thinking which are followed also by apathy, an anergy and autism.

Route of administration and doses:

Adults: FLYUANKSOL of DEPOT is appointed in the form of an intramuscular injection in an upper outside quadrant of a rump. Good local tolerance. The dosage and an interval between injections are defined individually according to therapeutic effect.

FLYUANKSOL of DEPOT of 20 mg/ml: At the supporting treatment the range of dosages usually makes 20-40 mg (1-2 ml) each 2-4 weeks. Higher doses or shorter intervals between injections can be necessary for some patients.

If the necessary volume of FLYUANKSOLA solution of DEPOT, 20 mg/ml exceeds 2-3 ml for 1 injection, then transition to solution with bigger concentration is recommended (FLYUANKSOL of DEPOT of 100 mg/ml).

FLYUANKSOL of DEPOT of 100 mg/ml: 50-200 mg (0,5-2 ml) each 2-4 weeks. At an aggravation or an acute recurrence of a disease administration of drug in a dose up to 400 in one step bucketed mg in 2 can be required or even 1 week. After stopping of acute symptomatology gradual decrease to a maintenance dose is made - usually to 20-200 mg there are each 2-4 weeks.

Upon transition from treatment by the FLYuANKSOLA peroral forms on the supporting treatment FLYUANKSOLY DEPOT it is necessary to be guided by the following scheme:

Peroral daily dose of FLYuANKSOLA (mg) x 4 = FLYUANKSOL of DEPOT (mg) intramusculary each 2 weeks.

At the same time within the first week it is necessary to continue oral administration of FLYuANKSOLA, but in the reduced dose. The subsequent doses and intervals between injections have to be established according to clinical effect.

Features of use:

The Malignant Antipsychotic Syndrome (MAS) is a rare, but possible complication with a lethal outcome when using neuroleptics. The main symptoms of ZNS are the hyperthermia, muscular rigidity and disturbance of consciousness in combination with dysfunction of the autonomic nervous system (labile arterial pressure, tachycardia, the increased sweating).

Except the immediate termination of reception of neuroleptics use of the general supporting measures and a symptomatic treatment is extremely necessary.

Side effects:

From a nervous system. There can be extrapyramidal symptoms, especially at the initial stage of treatment. In most cases these side effects korrigirutsya by decrease in dosages and/or purpose of antiparkinsonichesky drugs. However, regular preventive use of the last is not recommended. In rare instances at long therapy at patients late dyskinesia can develop. Antiparkinsonichesky drugs do not eliminate these symptoms. Reduction of a dosage or if it is possible, the therapy termination is recommended.

From mentality. Tranzitorny sleeplessness, especially when the patient is transferred from sedative neuroleptics. High doses of drug at some patients can lead to sedation.

From cardiovascular and vegetative nervous systems of disturbance are very rare in the range of therapeutic doses.

From a liver. Minor passing changes in hepatic tests can take place.

Interaction with other medicines:

FLYUANKSOL of DEPOT can strengthen effect of alcohol, barbiturates and other inhibitors of the central nervous system. FLYUANKSOL the DEPOT should not appoint together with guanetidiny or similarly operating drugs since neuroleptics can block hypotensive action of these means. FLYUANKSOL of DEPOT can reduce effect a levodopa and adrenergic medicines, and the combination with Metoclopramidum and piperazin increases risk of extrapyramidal symptoms.

FLYUANKSOL of DEPOT should not mix up with other liquids for injections.

Contraindications:

Acute alcoholic poisoning, barbiturates or opiates; comas. It is not recommended to appoint to patients with excitement or a hyperactivity since the activating action FLYUANKSOL can lead DEPOT to an aggravation of this symptomatology.

FLYUANKSOL is not recommended to appoint DEPOT during pregnancy and feeding a breast.

Precautionary measures. FLYUANKSOL of DEPOT has to be appointed with care to patients with a convulsive syndrome, chronic hepatitis and cardiovascular diseases. If earlier the patient was treated by neuroleptics with sedative action, then their reception should be stopped gradually. At long therapy, especially with use of high doses of FLYUANKSOL of DEPOT, it is necessary to carry out careful control and periodic assessment of a condition of patients to make the decision on reduction of the supporting dosage.

Though, in most cases, FLYUANKSOL of DEPOT does not cause sedation, nevertheless its influence on ability of driving and other mechanisms is possible. Therefore in an initiation of treatment it is necessary to show care until reaction of the patient to treatment is defined.

Overdose:

Symptoms: Drowsiness, coma, hypothermia or hyperthermia, hypotension, extrapyramidal symptoms, spasms, shock.

Treatment: Symptomatic and supporting. 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:

Flyuanksol has to be stored by depot at a temperature not above 25 °C in the place protected from light. On each packaging expiry date of the validity is specified. You store in places, inaccessible to children.

Issue conditions:

According to the recipe

Packaging:

Colourless glass ampoules in cardboard packaging and colourless bottles in cardboard packaging. Flyuanksol of depots 1 and 10 of ampoules on 1 ml (20 mg). 20 mg/ml: 1 and 10 ampoules on 2 ml (40 mg). Bottle of 10 ml (200 mg). Flyuanksol of depots 1 and 10 of ampoules on 1 ml (100 mg). 100 mg/ml: Bottle of 5 ml (500 mg).