The use of fluanxol in narcology and side effects

Content:

1. Area and methods of application
2. Fluanxol: side effects
3. Manifestations of withdrawal syndrome
4. Contraindications for antipsychotic treatment

The effectiveness of treatment with psychotropic drugs depends on the correct choice of pharmacological agent, taking into account the history of the disease and the patient’s well-being.
In narcology, as in any other field of medicine, when planning drug therapy, it is important to take into account the entire range of medications used. Since their interaction may change the expected result or cause accompanying reactions. The drug fluanxol, which belongs to the group of antipsychotics, is widely used in the treatment of alcohol dependence. Thanks to its antipsychotic and antidepressant effect, it helps patients overcome difficult periods of struggle with addiction.

Fluanxol 1 mg 50 pcs. film-coated tablets

pharmachologic effect

Antipsychotic drug (neuroleptic), thioxanthene derivative.
It has a pronounced antipsychotic effect, as well as activating, antidepressant and anxiolytic effects. The manifestation of the effects of flupenthixol depends on its dose. It is believed that the antipsychotic effect of neuroleptics is due to the blockade of dopamine receptors in the central nervous system. Thioxanthene derivatives have a high affinity for dopamine D1 and D2 receptors.

Unlike flupenthixol hydrochloride, flupenthixol decanoate is a depot form, its effect lasts for 2-4 weeks.

Composition and release form Fluanxol 1 mg 50 pcs. film-coated tablets

Tablets - 1 tablet:

• Active substance: flupenthixol dihydrochloride 1.168 mg, which corresponds to the content of flupenthixol 1 mg.
• Excipients: lactose monohydrate - 37 mg, potato starch - 73.5 mg, gelatin - 2.76 mg, talc - 8.4 mg, magnesium stearate - 0.6 mg.
• Shell composition: gelatin - 0.558 mg, sucrose - 50 mg, sucrose powder - 16.2 mg, iron oxide yellow (E172) - 0.25 mg, polishing wax Capol 1295® (a mixture of white beeswax and carnauba wax) - qs

50 pcs. - plastic containers (1) - cardboard packs.

Description of the dosage form

Tablets, coated (sugar), brownish-yellow, round, biconvex.

Directions for use and doses

The dose, frequency and duration of use are set individually depending on the indications, the dosage form used and the treatment regimen.

When taken orally, the daily dose varies from 1 mg to 40 mg in 1-3 doses.

With intramuscular administration, a single dose varies from 20 mg to 200 mg with an interval of 2-4 weeks.

Pharmacokinetics

After oral administration, Cmax of flupenthixol in plasma is achieved within 3-6 hours. Bioavailability is about 40%.

Flupenthixol and cis-(Z)-flupenthixol decanoate slightly penetrate the placental barrier and are excreted in small quantities in breast milk. Metabolites do not have neuroleptic activity.

After intramuscular administration of flupenthixol, decanoate undergoes enzymatic cleavage into the active component cis-(Z)-flupenthixol and decanoic acid. Cmax of cis-(Z)-flupenthixol in serum is achieved by the end of the first week after injection.

When taken orally, the biological T1/2 is approximately 35 hours.

Flupentixol is excreted in the form of metabolites, mainly through the intestines and partly by the kidneys.

Indications for use Fluanxol 1 mg 50 pcs. film-coated tablets

For use 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 determined anxiety, stressful conditions in which sedative/hypnotic effects are not required (especially if there is a suspicion that the patient is predisposed to abuse tranquilizers).

For use 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.

For use in doses of 40-150 mg/day: acute and chronic psychoses (including schizophrenia), resistant to therapy; alcohol withdrawal syndrome.

Contraindications

Acute alcohol intoxication, acute intoxication with barbiturates, opioid analgesics, coma, NMS, history of central hyperthermia, impaired liver function, impaired renal function, history of toxic agranulocytosis, parkinsonism, acute febrile states, hypersensitivity to antipsychotics of the thioxanthene structure.

Application of Fluanxol 1 mg 50 pcs. film-coated tablets during pregnancy and breastfeeding

Flupentixol and its active metabolite penetrate the placental barrier in small quantities and are excreted in breast milk in small concentrations. Use during pregnancy and lactation (breastfeeding) is not recommended.

special instructions

Flupenthixol should not be used in insufficiently high doses in patients in a state of agitation or hyperactivity.

Use with caution in patients with convulsive syndrome, chronic hepatitis, and cardiovascular diseases.

If NMS develops, you should immediately stop using flupenthixol and begin emergency symptomatic therapy.

In case of previous therapy with antipsychotics with sedative effects, their use should be discontinued gradually.

With long-term use of flupenthixol in high doses, it is necessary to regularly examine the patient's condition in order to switch to treatment using lower doses.

During treatment with flupenthixol, antiparkinsonian drugs should be prescribed only if there are appropriate indications and should not be used prophylactically.

Flupenthixol should not be used simultaneously with guanethidine and other drugs with a similar mechanism of action.

Impact on the ability to drive vehicles and operate machinery

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 flupenthixol (especially at the beginning of treatment), potentially hazardous activities should be avoided until the individual response is determined.

Side effects Fluanxol 1 mg 50 pcs. film-coated tablets

From the side of the central nervous system: possible transient insomnia (especially after previous treatment with antipsychotics with sedative effects), sedative effects (when used in high doses), extrapyramidal disorders (mainly at the beginning of treatment); rarely, with long-term therapy - tardive dyskinesia.

From the digestive system: transient changes in liver function tests are possible.

Drug interactions

With simultaneous use, flupenthixol enhances the effects of drugs that have a depressant effect on the central nervous system, as well as ethanol; may potentiate the effect of anesthetics.

With simultaneous use, it is possible to reduce and completely suppress the hypotensive effect of guanethidine and drugs with a similar mechanism of action.

With simultaneous use, it is possible to reduce the effects of levodopa and adrenergic drugs.

When used simultaneously with lithium carbonate, the development of extrapyramidal disorders is possible; with metoclopramide, piperazine - the risk of developing extrapyramidal disorders increases.

Area and methods of application

Features of the chemical structure of a pharmacological agent directly affect its clinical properties. Substances of this class are used in the treatment of psychotic conditions that occur in patients of drug treatment clinics. These include mental disorders, paranoid manifestations, various psychoses, anxieties and phobias.

The effect of fluanxol on the human body is not limited to this list. In certain doses and in combination with other psychotropic medications, it is used to overcome obsessive-compulsive and personality disorders. This remedy has a sedative and neurotropic property, reduces psychomotor activity, and even has an antiemetic effect.

Tablet forms are taken in strict accordance with the doctor's prescription. If the substance is administered through intramuscular injections into the soft tissue of the buttock, then at certain doses the entire volume is divided into two injections and administered to different places.

Fluanxol is widely used in many areas of medicine, but most often in psychiatry and narcology. When prescribing this drug, the narcologist takes into account the physical and mental state of the patient to calculate the optimal dose. In addition, medical monitoring of the client’s well-being will be required in order to respond in a timely manner to negative manifestations from the antipsychotic.

Compound

flupenthixol as an active ingredient .
Auxiliary ingredients: lactose monohydrate, potato starch, gelatin, magnesium stearate, talc.

Shell: sucrose, gelatin, E172.

One milliliter of injection solution contains 20 mg or 100 mg of cis(Z)-flupenthixol decanoate , the active substance.

Additional components: medium chain triglycerides.

Fluanxol: side effects

All pharmacological drugs of the psychotropic group cause certain unpleasant sensations and changes in human behavior, which are mostly dose-dependent. The intensity and severity of their manifestations depend on the dosage and duration of treatment.

One of the main negative effects from treatment with fluanxol is considered to be neuroleptic syndrome. It is accompanied by:

• the appearance of drowsiness;
• decreased reactions;
• slow speech;
• increased body temperature;
• possible muscle spasms;
• increased sweating.

Some patients develop aggressiveness, anxiety, irritation, and lack of perseverance. There are frequent cases of malfunction of the gastrointestinal tract, increased appetite, and, consequently, a significant increase in body weight.

The use of fluanxol can cause allergies and skin diseases: dermatitis, rash, itching, irritation. Vision problems, cardiovascular disorders, depression and epileptic seizures may occur.

Most often, the intensity of side effects is controlled by adjusting the dose and appropriate drug treatment.

Indications for use

When taken orally at a daily dose of up to 3 mg:

• depressive states of moderate and mild severity, accompanied by anxiety , lack of initiative and asthenia ;
• neurotic disorders of a chronic nature, with apathy , depression and anxiety ;
• psychosomatic disorders with asthenic conditions.

When taken orally, a daily dose of 3 mg or more:

• schizophrenia-like psychoses and schizophrenia with a dominance of hallucinatory symptoms, thinking disorders , delusions , which are accompanied by autism , anergy , apathy and low mood.

When used as an intramuscular injection:

• schizophrenia and other psychotic disorders with autism , anergy , apathy and low mood, accompanied by hallucinations , thinking disorders, delusions .

Manifestations of withdrawal syndrome

Stopping taking the antipsychotic fluanxol may trigger a withdrawal reaction. This condition is in some ways similar to withdrawal syndrome, but is not so severe and can be treated with medication.

It appears a few days after stopping treatment, and the duration is directly related to the previous course of use of the drug: the longer a person took the medicine, the longer the adaptation phase. Typically this period lasts from seven days to a month.

At this time, the body gets used to living without antipsychotics and experiences stress, during which the following side effects of fluanxol withdrawal are possible:

• nausea, vomiting, diarrhea and other digestive tract disorders;
• sleep disturbance, anxiety and nervousness;
• increased sweating;
• hand tremors, muscle spasms;
• headaches and sudden changes in blood pressure;
• heart failure;
• disorders of consciousness.

Throughout the entire period until the patient’s state of health stabilizes, the patient needs the help of a specialist who can, if necessary, prescribe a course of maintenance drug therapy.

Interaction

When using Fluanxol, it is possible to enhance the sedative effects of barbiturates , ethanol and other drugs that have a depressant effect on the central nervous system.

The drug should not be prescribed in parallel with Guanethidine and drugs with similar effects, since Fluanxol may weaken their antihypertensive effectiveness.

Flupenthixol together with tricyclic antidepressants inhibit each other's metabolism.

Combined use with lithium preparations may increase neurotoxicity .

Fluanxol may reduce the effect of Levodopa and adrenergic drugs .

The risk of extrapyramidal disorders increases when Fluanxol is used together with Piperazine and Metoclopramide .

Due to a possible increase in the QT interval, it is not recommended to prescribe flupentixol simultaneously with drugs that have a similar effect.

Among these drugs are: antiarrhythmic drugs of classes IA and III ( Dofetilide , Amiodarone , Quinidine , Sotalol ); antipsychotic drugs ( Thioridazine ); macrolides ( Erythromycin ); quinolones ( Moxifloxacin , Gatifloxacin ); antihistamines ( Astemizole , Terfenadine ); lithium preparations; cisapride .

When used in parallel with drugs that cause electrolyte imbalance ( thiazide-like and thiazide diuretics ), as well as drugs that increase the content of flupenthixol in the blood, an increase in the QT interval and the development of life-threatening arrhythmias

Fluanxol IM solution cannot be mixed with deposited forms based on sesame oil due to a significant effect on their joint pharmacokinetics.

Contraindications for antipsychotic treatment

The drug is prescribed with extreme caution to patients in an excited or hyperactive position, since taking it only aggravates its painful symptoms.

It is prohibited to take the drug for children under 18 years of age, people with individual intolerance to the components of the drug, as well as those in a state of coma or depressed consciousness of any nature (caused by the effects of alcohol, drugs, etc.)

To reduce the risk of side effects from Fluanxol, it is recommended to prescribe it with extreme caution:

• pregnant and breastfeeding women;
• mentally retarded patients;
• with severe intoxication of the body;
• in case of severe brain diseases;
• in the presence of convulsions and fainting;
• for some cardiovascular diseases;
• in acute liver failure.

When treating older people, it is possible to use this medicine with reduced doses. For poisoning of various natures, treatment with fluanxol is possible after detoxification.

For pregnant and nursing mothers, the drug is used only if the existing threats to the child are significantly less than treatment with the drug.

Important! When treated with fluanxol, it is not recommended to drive vehicles, operate machinery or perform work that requires concentration, clarity and speed of movements. Violation of these recommendations may result in traffic accidents, injuries and loss of health.

Overdose

In case of an overdose of Fluanxol, the following may occur: drowsiness , hypo- or hyperthermia, shock , convulsions , extrapyramidal disorders , coma .

When used in combination with drugs that affect cardiac activity, the following are possible: changes in the ECG , ventricular arrhythmias , prolongation of the QT interval, cardiac arrest .

Supportive and symptomatic treatment is recommended. In case of oral administration of high doses of the drug, the stomach is washed and sorbents .

Measures should also be taken to maintain breathing and cardiovascular activity. Taking epinephrine ( Adrenaline ) is not recommended, as it can cause a decrease in blood pressure .

Seizures are relieved with Diazepam , and Biperiden .

Literature:

1. A short reference book on psychopharmacology, pharmacotherapy and mental pathology / Kozlovsky, Vladimir Leonidovich. / St. Petersburg: SpetsLit, 2015.
2. Modern psychotropic drugs used in psychiatry: educational and methodological manual / [Olga Fedorovna Pankova, Artem Vyacheslavovich Alekseev, Alexander Viktorovich Abramov]; Ministry of Health of the Russian Federation, Federal State Autonomous Educational Institution of Higher Education "Russian National Research Medical University named after N. I. Pirogov" (FGAU HE RNRMU named after N. I. Pirogov of the Ministry of Health of Russia), Department of Psychiatry and Medical Psychology. — Moscow: Federal State Autonomous Educational Institution of Russian National Research Medical University named after. N.I. Pirogova Ministry of Health of Russia, 2021. - 135 p.
3. Features of pathological craving for alcohol in patients with excitable personality traits in premorbidity (clinic, therapy): dissertation ... candidate of medical sciences: 14.00.45 / Volkova Elena Valentinovna; [Place of protection: Federal State Institution "National Scientific Center for Narcology"]. - Moscow, 2008. - 164 p.

During pregnancy and lactation

The use of Fluanxol during pregnancy and breastfeeding is possible only in cases where the expected benefit of treatment for the mother far outweighs the possible risk to the fetus.

Cases have been described of the use of antipsychotics during childbirth or in the third trimester of pregnancy , which led to signs of intoxication ( tremor , lethargy , excessive excitability ) in the newborn. In addition, they had a low Apgar score.

If there is a clinical need for the use of Fluanxol during lactation , you should monitor the health of the newborn, especially in the first month after birth, or stop breastfeeding.

Fluanxol price, where to buy

In Russian pharmacies the average price of Fluanxol is:

• tablets 0.5 mg No. 50 – 330 rubles;
• tablets 1 mg No. 50 – 480 rubles;
• tablets 5 mg No. 100 – 1100 rubles;
• ampoules 20 mg/ml 1 ml No. 10 – 2000 rubles.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

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