Fluanxol pills 1 mg №50

Mechanism of action

Antipsychotic agent (neuroleptic), a derivative of thioxanthene with a pronounced antipsychotic, activating, anxiolytic, as well as antidepressant effects.
The antipsychotic effect of Fluanxol begins to appear when using the drug in a dose of 3 mg / day, and the intensity of the action increases with increasing dose.
In doses up to 25 mg / day, the drug does not have a sedative effect, however, in high doses it can cause a nonspecific sedative effect.
In the entire range of recommended doses, the drug has a pronounced anxiolytic effect.
When used at a dose of up to 3 mg / day, the drug may have an antidepressant effect.
Fluanxol eliminates the main symptoms of psychosis, incl. hallucinations, paranoid delusions and thinking disorders. It has disinhibiting (anti-anthracistic and activating) properties, and also weakens secondary mood disorders, which contributes to the revitalization of patients with depressive symptoms, fenced off, lack of initiative, increases sociability and facilitates social adaptation.
When using the solution for injection depot in small and medium doses (up to 100 mg 1 time in 2 weeks), the nonspecific sedative effect of the drug does not manifest itself, but can develop with high doses.
Fluanxol in the form of a depot injection solution has a significantly longer duration of action than Fluanxol in the form of tablets. The use of a depot injection solution helps prevent frequent relapses associated with the voluntary interruption of treatment by patients.

Suction
After ingestion C_max flupentixol in plasma is reached after 3-6 hours. Bioavailability is about 40%.
Distribution
Flupentiksol and cis- (Z) -flupentixol decanoate slightly penetrate the placental barrier, in small quantities excreted in breast milk. Metabolites do not possess neuroleptic activity.
Metabolism
After i / m administration of flupentixol, decanoate is subjected to enzymatic cleavage into the active component of cis- (Z) -flupentixol and decanoic acid. C_max Serum cis- (Z) -fupentixol is reached by the end of the first week after injection.
Removal
When ingested biological T_1/2 is approximately 35 h.
When using a depot injection solution, the serum concentration curve decreases exponentially with T_1/2equal to about 3 weeks, which reflects the rate of release of flupentixol from the depot.
Flupentiksol is excreted in the form of metabolites, mainly through the intestines and partially by the kidneys.

Indications and usage

For use of the drug in doses up to 3 mg / day
- mild to moderate depression with anxiety, asthenia and lack of initiative;
- chronic neurotic disorders with anxiety, depression and apathy;
- psychosomatic disorders with asthenic reactions;
- acute and situationally conditioned anxiety, stressful conditions in which a sedative / hypnotic effect is not required (especially if you suspect that the patient is prone to abuse of tranquilizers);
To use the drug in doses of 3-40 mg / day
- psychotic states with a predominance of hallucinations, paranoid delusions and thinking disorders, also accompanied by apathy, anergy and autism;
To use the drug in doses of 40-150 mg / day
- acute and chronic psychosis (including schizophrenia) resistant to therapy;
- alcohol withdrawal syndrome.

For therapy depressive and anxiety disorders The initial dose of the drug for oral administration is 1 mg 1 time / day in the morning or 500 mcg 2 times / day. In the absence of a satisfactory therapeutic effect after 1 week, the dose may be increased to 2 mg / day. The daily dose, comprising from 2 mg to 3 mg, should be divided into several doses. If there is no therapeutic effect when using Fluanxol at a maximum dose of 3 mg / day for 1 week, the drug should be withdrawn.
During therapy psychotic states the dose is set individually, depending on the condition of the patient. The initial daily dose is 3-15 mg in 2-3 doses. If necessary, the dose is usually increased to 40 mg / day.
During therapy acute and chronic psychosis Perhaps the appointment of the drug in high doses - 40-150 mg / day. The daily dose depends on the severity of the disease, the degree of its resistance to therapy, the age and body weight of the patient. The frequency of use of the drug is highest at the beginning of therapy, usually 4 times / day, then it usually decreases to 1-3 times. For maintenance therapy, the drug is used in a dose of 5-20 mg 1 time per day in the morning.
Solution for injection depot injected into / m in the upper outer quadrant of the buttocks.The dose and the interval between injections set individually, depending on the therapeutic effect.
Depot injection solution (20 mg / ml) is usually administered in a dose of 20-40 mg (1-2 ml) every 2-4 weeks.
Depot injection solution (100 mg / ml) is administered in a dose of 50-200 mg (0.5-2 ml) every 2-4 weeks. With exacerbation or acute recurrence of the disease, it may be necessary to administer the drug in a dose of up to 400 mg at one time at intervals of 2 or even 1 week. After relief of acute symptoms, a gradual reduction of the dose to maintenance is carried out - usually 20-200 mg every 2-4 weeks.
When switching from treatment with oral forms of the drug to maintenance treatment with a depot injection solution, you should follow the following scheme: daily dose (mg) of the oral preparation x 4 = single dose (mg) of the solution for injectable v / m every 2 weeks At the same time within 1 week after the introduction of the solution should continue taking the drug inside, but in a reduced dose. Subsequent doses and intervals between injections are set in accordance with the clinical effect.

Adverse reactions

From the side of the central nervous system: possibly transient insomnia, especially after previous treatment with neuroleptics with a sedative effect; when used in high doses in some cases, a sedative effect is observed; mainly at the beginning of treatment may develop extrapyramidal disorders. Rarely, with prolonged therapy - tardive dyskinesia.
Gastrointestinal: possibly transient changes in laboratory functional hepatic tests.
It is believed that with the use of the drug in the recommended therapeutic doses, the development of side effects from the cardiovascular system and the autonomic nervous system is unlikely.

Contraindications

- CNS depression;
- acute alcohol intoxication;
- acute intoxication with barbiturates;
- acute intoxication with opioid analgesics;
- coma;
- Malignant neuroleptic syndrome (MNS);
- Central hyperthermia in history;
- abnormal liver function;
- renal dysfunction;
- pathological changes in the blood;
- bone marrow depression;
- Toxic agranulocytosis in history;
- parkinsonism;
- Acute febrile states;
- collapse;
- pregnancy;
- lactation;
- childhood;
- Hypersensitivity to neuroleptics thioksantenovoy structure.
Patients in a state of excitement or hyperactivity should not be given an insufficiently high dose of Fluanxol.

Pregnancy and breastfeeding

Flyuksol not recommended for use during pregnancy and lactation (breastfeeding).

With caution, the drug is prescribed to patients with convulsive syndrome, chronic hepatitis, cardiovascular diseases.
In the case of prior treatment with neuroleptics or tranquilizers with a sedative effect, their intake should be stopped gradually.
The use of a depot injection solution allows continuous antipsychotic therapy, which is especially important for the treatment of patients who do not fulfill medical prescriptions.
With long-term therapy, especially with the use of the drug in high doses, it is necessary to carefully monitor and periodically assess the condition of patients in order to timely adjust the maintenance dose.
In most cases, extrapyramidal disorders that occur at the beginning of treatment are adjusted by lowering the dose and / or prescribing anti-parkinsonian drugs. However, their use for prevention is not recommended.
Anti-Parkinsonian drugs do not eliminate tardive dyskinesia, which can develop during the use of Fluanxol. In such cases, it is recommended to reduce the dose of the drug or, if possible, discontinue therapy.
It should be borne in mind that when using neuroleptics, including flupentiksol, in rare cases, the development of a fatal nervous system. The main characteristics of the NMS are: hyperthermia, muscle rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, increased sweating). When these symptoms appear, an urgent withdrawal of the neuroleptic and the appointment of symptomatic and supportive therapy is necessary.
Influence on ability to drive motor transport and control mechanisms
Although in most cases the drug does not cause a sedative effect, it is necessary to take into account the possibility of its influence on the ability to drive a car and other mechanisms.
When using the drug (especially at the beginning of treatment), you should avoid practicing potentially hazardous activities until you determine the individual response to Fluanxol.

Symptoms: drowsiness, hyper- or hypothermia, extrapyramidal disorders, convulsions, hypotension, shock, coma are possible.
Treatment: conduct symptomatic and supportive therapy. In the case of taking the drug inside it is necessary to wash the stomach as soon as possible, it is recommended to take a sorbent. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use adrenaline, because this can lead to a subsequent decrease in blood pressure. Spasms can be stopped by diazepam, and extrapyramidal symptoms - biperidenom.

With simultaneous use Fluanxol may enhance the sedative effect of ethanol, barbiturates and other means that have a inhibitory effect on the central nervous system.
Fluanxol should not be used in conjunction with guanethidine and agents with a similar effect, because antipsychotics can block their hypotensive action.
With simultaneous use Fluanxol can reduce the effectiveness of levodopa and other adrenergic agents.
With simultaneous use of Fluanxol with Metoclopramide and piperazine increases the risk of extrapyramidal disorders.
Solution for injection depot can not be mixed with other solutions for injection (except klopiksola-Akufaz - in the form of co-injection).

List B. Tablets should be stored at a temperature not exceeding 30 ° C.