Instructions for use of the drug Fluanxol and reviews about it

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.

Composition of the drug and its release form

What active substance does the medicine “Fluanxol” contain? The instructions for use of this medication state that the active ingredient in it is flupenthixol hydrochloride.

As for the release form, today this remedy can only be found in drops, tablets and an oil-based solution intended for intramuscular administration. The first medicine goes on sale in dark glass of 10 ml, the second - in cardboard packaging of 100 or 50 pieces, and the third - in ampoules of 10 pieces.

Pharmacodynamics and pharmacokinetics

A thioxanthene derivative , flupenthixol is an antipsychotic (psychotropic drug) with a pronounced activating, anxiolytic and antipsychotic effect.

The antipsychotic effects of the drug are associated with blocking dopamine receptors of 5-HT serotonin receptors is also suggested . Fluanxol has been proven to reduce the main symptoms of psychosis , including thinking disorders , paranoid delusions , and hallucinations .

The antipsychotic effectiveness of Fluanxol is observed when taking tablets orally at a daily dose of 3 mg. An increase in effect is observed with increasing both oral and intramuscular dosages of the drug.

Flupenthixol exhibits a disinhibitory (activating and anti-autistic) effect, and also reduces secondary signs of general mood disorder, which, in turn, helps stimulate patients with depressive symptoms, improves their communication skills and promotes rapid social adaptation .

In medium and small dosages (orally up to 25 mg per day and intramuscularly up to 100 mg once every 14 days), the drug does not have sedative effects . Nonspecific sedative effects may occur when high doses are used. When taken orally in small daily doses (up to 3 mg), antidepressant effectiveness of the drug is observed.

The intramuscular oil solution of flupenthixol is intended for depot injections and is a deposited form of the drug (Fluanxol Depot). The injection solution has a significantly longer duration of action compared to tablets, which is especially important when carrying out continuous antipsychotic treatment of patients who do not comply with all medical prescriptions.

The use of ampoule Fluanxol prevents frequent relapses observed when patients taking the drug orally interrupt therapy on their own. The intramuscular solution can be administered, depending on the pathology, at a frequency of once every 2-4 weeks.

Cmax in the blood is observed 3-6 hours after internal administration of the drug. Bioavailability at 40%.

The active ingredient of the ampoules is cis(Z)-flupenthixol decanoate , after intramuscular injection, amenable to enzymatic cleavage to release cis(Z)-flupenthixol and decanoic acid. In the blood, Cmax of cis(Z)-flupenthixol is observed approximately 7 days after administration.

The apparent Vd is 14.1 l/kg. The connection with plasma proteins is almost complete (99%). If the drug is used by intramuscular injection, Css is achieved after 3 months.

In small quantities, the active ingredient of the ampoules is present in mother's milk and also penetrates the placental barrier .

Metabolic products do not reveal neuroleptic activity.

When taken orally, T1/2 is approximately 35 hours. With intramuscular injections, the concentration of the drug decreases exponentially with T1/2 for about 3 weeks.

The drug is excreted to a greater extent in feces, and to a lesser extent in urine.

An IM dose of Fluanxol 40 mg, with a single administration every 14 days, is pharmacokinetically equivalent to a tableted daily dose of 10 mg, taken daily for 2 weeks.

Pathogenesis of complications development

Fluanxol, as a thioxanthene derivative, has a wide spectrum of action, directly affecting individual structures of the central nervous system. The complexity of using the drug leads to a specific form of addiction to it. The drug does not cause drug dependence, but during and after stopping its use, side effects and Fluanxol withdrawal syndrome may occur.

The mechanism of development of such reactions is determined by the peculiarities of the functioning of the central nervous system. The complications are based on changes in the sensitivity of the corresponding brain structures to the effects of chemical compounds. The absence of the usual inhibitory effect on synapses or an inadequate response of cells to the action of the drug leads to a deterioration in the patient’s well-being. This condition is accompanied by neurological, mental and other symptoms.

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 .

Contraindications to the use of antipsychotic drugs

In what cases is it not recommended to use the drug "Fluanxol"? Instructions for use include the following list of contraindications:

• children's age (up to 18 years);
• CNS depression;
• lactation period;
• pregnancy period;
• intoxication (acute) with barbiturates;
• collapse;
• acute intoxication with opioid analgesics;
• pheochromocytoma;
• acute alcohol poisoning;
• comatose states;
• bone marrow suppression;
• pathological blood changes;
• hypersensitivity to antipsychotics with a thioxanthene structure.

It should also be noted that in a state of hyperactivity or agitation, it is not recommended to prescribe the drug in small dosages (up to 3 mg).

Contraindications

• any conditions accompanied by suppression of consciousness , including due to the use of alcohol , opioid analgesics or barbiturates ;
• congenital intolerance to fructose and/or galactose;
• deficiency of isomaltase, lactase, sucrase;
• impaired absorption of galactose and glucose (for tablets);
• vascular collapse;
• coma;
• age under 18 years;
• hypersensitivity to the ingredients of the drug or phenothiazines .

Carefully:

• organic pathologies of the brain;
• convulsive conditions, epilepsy (possible increase in the frequency of seizures as a result of a decrease in convulsive readiness);
• increased risk of stroke ;
• liver failure ;
• hypomagnesemia , hypokalemia ;
• history of cardiovascular diseases (increased risk of low blood pressure ), including bradycardia (less than 50 beats/min), prolongation of the QT interval , recent myocardial infarction , arrhythmia , heart failure (uncompensated);
• glaucoma or risk factors for its development;
• gastrointestinal ulcer;
• alcoholism (possibly increased CNS depression);
• leukopenia;
• pheochromocytoma;
• breathing disorders that are associated with acute infections, emphysema , bronchial asthma ;
• Parkinson's disease (exacerbation of extrapyramidal effects);
• Reye's syndrome (possible increase in hepatotoxicity);
• urinary retention and prostate adenoma with clinical manifestations;
• periods of breastfeeding and pregnancy .

Patients with psychomotor agitation are not recommended to use Fluanxol in a daily dose of up to 25 mg, due to the activating effect of small doses of the drug (up to 3 mg per day for oral administration and 10-20 mg once every 14 days for intramuscular injections), which may cause exacerbation of existing symptoms.

Drug analogues

Due to its complex targeted action, the drug does not have many analogues. The ones closest in action are called:

1. Fluanxol Depot. Oil injection. The disadvantages, compared to the original, include a higher price. The advantages are a faster and stronger effect.
2. Clopixol. The price is close to the original. Available in tablets of 2, 10 and 25 mg of zuclopenthixol. It has fewer contraindications than Fluanxol. The readings are close to the original. Strictly prohibited for use by pregnant women and children under 18 years of age. The disadvantages of the drug include a ban on driving a vehicle and high-precision equipment. The price is approximately the same as the original.
3. Truxal . Available in film-coated tablets of 25 and 50 mg of chlorprothixene. The main advantage of the drug is its use in children from three years of age. Has similar contraindications. Also not recommended for pregnant and nursing mothers. The price is slightly higher than the original.

Side effects

Nervous system (NS):

• headache;
• drowsiness;
• tremor;
• parkinsonism;
• akathisia;
• hypokinesia;
• speech disorders;
• dystonia;
• depression;
• nervousness;
• insomnia;
• agitation;
• dizziness;
• extrapyramidal disorders (hyperkinesis, muscle rigidity);
• attention disorders;
• dyskinesia;
• seizure disorders;
• amnesia;
• aggression;
• confusion;
• decreased libido;
• tardive dystonia.

It must be remembered that when taking antipsychotics , the group of which includes flupentixol , the development of NMS ( neuroleptic malignant syndrome ) was sometimes observed.

The main symptoms of NMS are manifested by hyperthermia , impaired consciousness and muscle rigidity with parallel dysfunction of the autonomic nervous system ( tachycardia , labile blood pressure , increased sweating ). If these symptoms occur, the antipsychotic and symptomatic and supportive treatment should be prescribed.

Long-term therapy with Fluanxol can lead to the development of tardive dyskinesia . The use of antiparkinsonian drugs does not eliminate symptoms, but, on the contrary, can intensify them.

In this case, a dose reduction is indicated until treatment is discontinued.

In case of persistent akathisia , effective drugs are: Propranolol or benzodiazepines .

Feelings of anxiety or transient insomnia may occur especially when previously taking antipsychotics that have a sedative effect .

motility disorders may occur .

These disorders are leveled out by lowering doses and/or prescribing antiparkinsonian drugs, the constant use of which, in order to prevent side effects, is not recommended.

The cardiovascular system:

• tachycardia;
• orthostatic hypotension ;
• ventricular arrhythmia (ventricular tachycardia , ventricular fibrillation , tachycardia of the “pirouette” type, sudden death );
• prolongation of the QT interval.

Hematopoietic system:

• hemolytic anemia ;
• agranulocytosis (most often during the period between 4 and 10 weeks of therapy);
• granulocytopenia;
• leukopenia.

Organ of vision:

• clouding of the lens and/or cornea, with the possibility of visual impairment;
• disturbance of accommodation;
• accommodation paresis;
• oculogyric crisis.

Gastrointestinal system:

• digestive disorders ( diarrhea , nausea , dyspepsia , constipation );
• dry mouth;
• increased salivation ;
• vomit;
• dysphagia;
• cholestatic jaundice (most often during the period between 4 and 10 weeks of therapy);
• decreased appetite;
• transient minor changes in liver enzymes.

Endocrine system:

• gynecomastia;
• galactorrhea;
• dysmenorrhea;
• decreased libido;
• weight gain;
• impotence;
• increased appetite;
• carbohydrate metabolism disorders;
• tides.

Reproductive system:

• erectile disfunction.

Urinary system:

• painful urination;
• urinary retention.

Musculoskeletal system:

• arthralgia.

Allergic manifestations:

• increased sweating;
• dermatitis;
• skin rash and itching ;
• photosensitivity.

Local complications:

• swelling;
• erythema;
• abscess;
• inflammation.

Other:

• asthenia;
• weakness.

Instructions:

Clinical and pharmacological group

02.001 (Antipsychotic drug (neuroleptic))

Release form, composition and packaging

Tablets, coated with a brownish-yellow sugar coating; round, biconvex.

Excipients: lactose monohydrate, potato starch, gelatin, talc, magnesium stearate.

Sugar shell composition: gelatin, sucrose, sucrose powder, yellow iron oxide (E172).

50 pcs. — plastic containers, 100 pcs. - plastic containers.

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

Excipients: lactose monohydrate, potato starch, gelatin, talc, magnesium stearate.

Sugar shell composition: gelatin, sucrose, sucrose powder, yellow iron oxide (E172).

50 pcs. — plastic containers, 100 pcs. - plastic containers.

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

Excipients: lactose monohydrate, potato starch, gelatin, talc, magnesium stearate.

Sugar shell composition: gelatin, sucrose, sucrose powder, yellow iron oxide (E172).

100 pieces. - plastic containers.

The solution for intramuscular administration is oily, transparent, colorless to slightly yellowish, practically free of particles.

Excipients: triglycerides with medium chains.

1 ml - colorless glass ampoules (10) - cardboard packs.

pharmachologic effect

Antipsychotic drug (neuroleptic), a thioxanthene derivative with pronounced antipsychotic, activating and anxiolytic effects. The antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, but possibly also with blockade of serotonin 5-HT receptors.

Fluanxol reduces the main symptoms of psychosis, incl. hallucinations, paranoid delusions and thinking disorders.

The antipsychotic effect of Fluanxol begins to appear when the drug is administered orally at a dose of 3 mg/day; the intensity of action increases with increasing dose both when taken orally and when administered intramuscularly.

Fluanxol has disinhibiting (anti-autistic and activating) properties, and also weakens secondary mood disorders, which promotes the activation of patients with depressive symptoms, increases their sociability and facilitates social adaptation.

In small and medium doses (up to 25 mg/day when taken orally and up to 100 mg intramuscularly once every 2 weeks), the drug does not have a sedative effect, but in high doses it can cause a nonspecific sedative effect.

When taken orally in small doses (up to 3 mg/day), the drug has an antidepressant effect.

Fluanxol oil solution for intramuscular administration is intended for depot injection, being a deposited form of flupenthixol. In this dosage form, the drug has a significantly longer duration of action than Fluanxol in tablet form, and allows for continuous antipsychotic therapy, which is especially important for the treatment of patients who do not comply with medical prescriptions. The use of Fluanxol in the form of a solution for intramuscular administration prevents frequent relapses associated with arbitrary interruption of treatment by patients when taking the drug orally. Fluanxol injections can be carried out at intervals of 2-4 weeks.

Pharmacokinetics

Suction

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

After intramuscular administration of cis(Z)-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.

Distribution

The apparent Vd is about 14.1 l/kg. Plasma protein binding is about 99%. With the intramuscular injection of the solution for injection, Css is achieved after 3 months of using the drug.

Flupentixol and cis(Z)-flupenthixol slightly penetrate the placental barrier and are excreted in small quantities in breast milk.

Metabolism

Metabolites do not have neuroleptic activity.

Removal

With intramuscular administration of the solution for injection, the serum concentration curve decreases exponentially with a T1/2 of approximately 3 weeks, which reflects the rate of release of flupenthixol from the depot.

Metabolites of flupenthixol do not have neuroleptic activity. They are excreted mainly in feces and partly in urine. T1/2 is approximately 35 hours.

Pharmacokinetically, a dose of Fluanxol 40 mg when administered intramuscularly once every 2 weeks is equivalent to a dose of Fluanxol 10 mg/day when taken orally for 2 weeks.

Dosage

For oral administration at a dose of up to 3 mg/day

For mild to moderate depression with anxiety, asthenia and lack of initiative; chronic neurotic disorders with anxiety, depression and apathy; psychosomatic disorders with asthenic reactions, the initial dose of the drug is 1 mg 1 time / day in the morning or 500 mcg 2 times / day. If there is no satisfactory therapeutic effect after 1 week, the dose can be increased to 2 mg/day. The daily dose, ranging from 2 mg to 3 mg, should be divided into several doses. For elderly patients, the recommended daily dose is 0.5-1.5 mg.

The therapeutic effect usually appears within 2-3 days. If, when taking a maximum dose of 3 mg/day, the effect is not observed within a week, then the drug should be discontinued.

For oral administration at a dose of 3 mg/day or more

When treating psychotic conditions, the dose is set individually, depending on the patient’s condition. At the beginning of treatment, it is recommended to use the drug in low doses, which are then, depending on the patient’s response to treatment, quickly increased until the optimal clinical effect is achieved.

The initial daily dose is 3-15 mg in 2-3 doses. If necessary, the dose can be increased to 20-30 mg/day. The maximum daily dose is 40 mg. For maintenance therapy, the drug is used at a dose of 5-20 mg/day.

For intramuscular administration

The solution for intramuscular injection is injected deep intramuscularly into the upper outer quadrant of the buttock. It is not recommended to inject into other muscles. If the required volume of solution exceeds 2 ml, it is recommended to divide it into 2 parts and make 2 injections.

The drug in the form of a solution for intramuscular administration of 20 mg/ml is usually administered in a dose of 20-40 mg (1-2 ml) every 2-4 weeks. Some patients may need higher doses or shorter intervals between injections. In case of exacerbation or acute relapse of the disease, it may be necessary to administer the drug in a dose of up to 400 mg at a time at intervals of 2 or even 1 week.

Transition from Fluanxol for oral administration to intramuscular administration

Daily dose (mg) of the drug for oral administration x 4 = single dose (mg) of solution for intramuscular administration every 2 weeks.

In this case, during the 1st week after the 1st injection, you should continue to take the drug orally, but in a reduced dose.

Subsequent doses and intervals between injections are adjusted according to the clinical effect. The maximum dose of Fluanxol for intramuscular administration is 400 mg at a time with an interval between injections of 1 week.

Patients who are transferred from therapy with depot forms of other drugs should receive Fluanxol taking into account the following ratios: 40 mg of flupenthixol decanoate is equivalent to 25 mg of fluphenazine decanoate, 200 mg of zuclopenthixol decanoate or 50 mg of haloperidol decanoate.

Overdose

Symptoms: possible drowsiness, hyper- or hypothermia, extrapyramidal disorders, convulsions, shock, coma.

When taken simultaneously with drugs that affect cardiac activity, changes in the ECG, prolongation of the QT interval, ventricular arrhythmias, incl. ari, cardiac arrest.

Treatment: provide symptomatic and supportive therapy. If the drug is taken orally, it is necessary to rinse the stomach as quickly as possible; it is recommended to take a sorbent. Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Epinephrine (adrenaline) should not be used because this may lead to a subsequent decrease in blood pressure. Seizures can be treated with diazepam, and extrapyramidal symptoms with biperiden.

Drug interactions

With simultaneous use, Fluanxol can enhance the sedative effect of ethanol, barbiturates and other drugs that have a depressant effect on the central nervous system.

Fluanxol should not be used together with guanethidine and drugs with similar effects, because antipsychotics may weaken their hypotensive effect.

Tricyclic antidepressants and antipsychotics (including Fluanxol) mutually inhibit metabolism.

Concomitant use of antipsychotics and lithium increases the risk of neurotoxicity.

With simultaneous use, Fluanxol may reduce the effectiveness of levodopa and the effect of adrenergic drugs.

When Fluanxol is used simultaneously with metoclopramide and piperazine, the risk of developing extrapyramidal disorders increases.

Prolongation of the QT interval, characteristic of therapy with antipsychotic drugs, may increase with simultaneous use of drugs that have the same effect, incl. antiarrhythmics of classes IA and III (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), cisapride, lithium preparations. The simultaneous use of Fluanxol and the listed drugs should be avoided.

When used simultaneously with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of flupenthixol or flupenthixol decanoate in the blood plasma, the risk of QT prolongation and life-threatening arrhythmias may increase.

Pharmaceutical interactions

Fluanxol in the form of a solution for intramuscular injection should not be mixed with deposited forms based on sesame oil, because this may have a significant impact on the pharmacokinetics of administered drugs.

Use during pregnancy and lactation

The use of Fluanxol during pregnancy and lactation (breastfeeding) is possible only in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Newborns whose mothers took antipsychotics in the third trimester of pregnancy or during childbirth may experience signs of intoxication, such as lethargy, tremor, and excessive excitability. In addition, these newborns have a low Apgar score.

During treatment with Fluanxol, breastfeeding is allowed if deemed clinically necessary. In such cases, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

Side effects

From the nervous system: drowsiness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia, speech disorders, depression, insomnia, nervousness, agitation; sometimes - dizziness, attention problems, extrapyramidal disorders (mainly muscle rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, aggression, decreased libido, confusion; rarely - tardive dystonia.

It should be borne in mind that when using antipsychotics, incl. flupenthixol, in rare cases, the development of NMS is possible. The main symptoms of NMS are: hyperthermia, muscle rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, increased sweating). If these symptoms appear, immediate discontinuation of the antipsychotic and administration of symptomatic and supportive therapy is necessary.

With long-term treatment with the drug, tardive dyskinesia may develop. Antiparkinsonian drugs do not relieve symptoms and may make them worse. It is recommended to reduce the dose or, if possible, discontinue treatment.

For persistent actatisia, benzodiazepines or propranolol may be effective.

In the first few days after the injection and in the early stages of treatment, motor problems may occur. In most cases, such effects are controlled by dose reduction and/or antiparkinsonian drugs. However, routine use of antiparkinsonian drugs to prevent side effects is not recommended.

Transient insomnia or anxiety may occur especially if patients have previously taken antipsychotics that have a sedative effect.

From the cardiovascular system: sometimes - orthostatic hypotension, tachycardia; in rare cases (as when taking other antipsychotics) - prolongation of the QT interval, ventricular arrhythmia (ventricular fibrillation, ventricular tachycardia, development of paroxysms of ventricular tachycardia of the “pirouette” type, sudden death).

From the hematopoietic system: rarely - granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia.

From the organ of vision: disturbance of accommodation, clouding of the cornea and/or lens with possible visual impairment; sometimes - oculogyric crisis, accommodation paresis.

From the digestive system: dry mouth, digestive disorders (including constipation, diarrhea, dyspepsia, nausea), increased salivation, dysphagia, vomiting, cholestatic jaundice (more likely between 2 and 4 weeks of treatment), decreased appetite; in isolated cases - minor transient changes in liver function test parameters.

From the endocrine system: galactorrhea, gynecomastia, dysmenorrhea, impotence, decreased libido, increased appetite, weight gain, hot flashes, changes in carbohydrate metabolism.

From the urinary system: sometimes - urinary retention, painful urination.

From the musculoskeletal system: sometimes - arthralgia.

From the reproductive system: sometimes - erectile dysfunction.

Allergic reactions: sometimes - itching, skin rash, dermatitis, photosensitivity, increased sweating.

Local reactions: rarely - erythema, swelling, inflammation or abscess.

Other: weakness, asthenia.

Storage conditions and periods

List B. Tablets should be stored at a temperature not exceeding 30°C. Shelf life: 3 years.

The oil solution for intramuscular administration should be stored in a place protected from light at a temperature not exceeding 25°C. Shelf life: 4 years.

The drug should be stored out of the reach of children.

Indications

For oral administration at a dose of 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.

For oral administration at a dose of 3 mg/day or more

- schizophrenia and schizophrenia-like psychoses with a predominance of hallucinatory symptoms, delusions, thinking disorders, also accompanied by apathy, anergy, decreased mood and autism.

For intramuscular administration

- schizophrenia and other psychotic conditions, occurring with hallucinations, delusions and thinking disorders, accompanied by apathy, anergy, decreased mood and autism.

Contraindications

- vascular collapse;

- depression of consciousness of any origin (including those caused by the intake of alcohol, barbiturates or opioid analgesics);

- coma;

- children and adolescents up to 18 years of age;

- hypersensitivity to the components of the drug;

- hypersensitivity to phenothiazines;

— hereditary intolerance to galactose and/or fructose; lapp lactase deficiency; sucrase and isomaltase deficiency; impaired absorption of glucose and galactose (when taking tablets).

Use with caution in patients with organic brain diseases, seizure disorders, incl. with epilepsy (as a result of a decrease in the threshold of convulsive readiness, an increase in seizures is possible); with severe liver failure; with hypokalemia, hypomagnesemia; history of cardiovascular diseases (risk of transient decrease in blood pressure), incl. with prolongation of the QT interval, bradycardia less than 50 beats/min, with recent acute myocardial infarction, with uncompensated heart failure, with arrhythmia; with risk factors for stroke; with glaucoma (and predisposition to it); with peptic ulcer of the stomach and duodenum; with alcoholism (possible increased inhibitory effect on the central nervous system); with pheochromocytoma; with leukopenia; breathing problems associated with acute infectious diseases, bronchial asthma or emphysema; with Parkinson's disease (increased extrapyramidal effects); with urinary retention, prostatic hyperplasia with clinical manifestations (risk of urinary retention); with Reye's syndrome (increased risk of hepatotoxicity); during pregnancy, during lactation (breastfeeding).

It is not recommended to prescribe Fluanxol at a dose of up to 25 mg/day to patients in a state of psychomotor agitation, because the activating effect of Fluanxol in small doses (when taken orally up to 3 mg/day or when administered intramuscularly 10-20 mg once every 2 weeks) can lead to an exacerbation of these symptoms.

special instructions

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

During long-term therapy, especially with the use of Fluanxol in high doses, it is necessary to carefully monitor and periodically assess the patient's condition in order to timely adjust the maintenance dose.

With concomitant treatment of diabetes, the administration of Fluanxol may require adjustment of the insulin dose.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, the patient should avoid engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Use for liver dysfunction

The drug is prescribed with caution to patients with liver failure.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Fluanxol tablets, instructions for use (Method and dosage)

Instructions for use of Fluanxol recommends taking it orally (orally) with water.

When taking tablets in a daily dose of up to 3 mg:

For the treatment of moderate and mild depressive states of anxiety , lack of initiative and asthenia ; chronic neurotic disorders apathy , depression and anxiety; For psychosomatic disorders with asthenia , Fluanxol is prescribed in an initial daily dose of 1 mg once in the morning, or in a half dose (500 mcg) twice a day.

In the absence of positive therapeutic dynamics over 7 days, you can increase the daily dose to 2 mg. The dosage of tablets is from 2 mg to 3 mg, must be taken in several doses. For elderly patients, a daily dose of 0.5 to 1.5 mg is recommended.

As a rule, the therapeutic effect of Fluanxol manifests itself within 2-3 days. If the maximum possible daily dosage of 3 mg tablets for a week is ineffective, therapy is discontinued.

When taking tablets in a daily dose of 3 mg or higher:

For the treatment of psychotic disorders, the dose of Fluanxol is selected individually, depending on the general condition of the patient.

At the beginning of therapy, it is recommended to take low doses of the drug, subsequently moving, depending on the individual response of the patient, to taking higher doses, until the optimal effective dosage is determined.

Therapy begins with a daily dose of 3 to 15 mg, depending on the severity of the condition. This dose must be divided into 2-3 doses. If necessary, this dosage can be increased to 20-30 mg.

The maximum permissible dose of tablets per day is 40 mg. Maintenance therapy is carried out in a daily dose of 5-20 mg.

When using IM injection solution:

The injection solution is indicated for intramuscular injection deep into the outer upper quadrant of one of the buttocks. Injecting the solution into other muscles is not advisable. If it is necessary to administer more than 2 ml of solution, it is recommended to make 2 injections.

The dosage of ampoules of 20 mg/ml is usually 1-2 ml (20-40 mg), administered once every 2-4 weeks. Some patients require higher doses of the drug or shorter intervals between doses.

In case of acute relapse or exacerbation of the disease, it may be necessary to administer high doses of the solution, up to 400 mg once, with a frequency of 14 or even 7 days.

When switching from the oral form of Fluanxol to intramuscular injection:

When switching from taking tablets to using intramuscular injections, it is necessary to calculate the daily dose of the solution.

To do this, the daily oral dose of tablets (mg) is multiplied by four, which will constitute a single dose of intramuscular solution (mg), administered once every 2 weeks.

In parallel, for 7 days after the 1st injection, it is necessary to continue taking the tablets, but in a smaller dose.

Subsequently, the dosage of injections and the intervals between them are established based on the individual clinical effect. The one-time maximum dose of the intramuscular solution is 400 mg with an interval of 7 days.

Patients switching to Fluanxol IM solution from other drugs in depot forms should use it in the following ratios: flupenthixol decanoate at a dose of 40 mg corresponds to 200 mg zuclopenthixol decanoate , 25 mg fluphenazine decanoate or 50 mg haloperidol decanoate .

Reviews about the use of Fluanxol

There are many reviews about Fluanxol from both psychiatrists and patients. They are all ambiguous.

Doctors

1. Victor Nechansky, doctor of the highest category: “I have been regularly prescribing this drug to my patients, including depressed patients, for the last 5 years. I see positive dynamics. It is distinguished by the rapid onset of desired effects. After the end of treatment, I never observed a re-exacerbation of the disease.”
2. Irina Cherkassova: “I prefer to prescribe this drug in combination with other antipsychotics, since it does not have the desired effect on its own. Yes, the symptoms of the acute disease subside. However, it does not go away completely. My colleagues like this medicine. I decided for myself that everything is purely individual.”

Depressed and other patients

1. Igor Evteenko: “I like this medicine in injection form. I had a worsening depression. With the injections, the symptoms regressed and no longer worsened. The injections are not painful, I did them myself at home. I recommend!".
2. Natalya Semenichko: “The price of medicine is high for me, given the fact that I have a disability due to a psychiatric illness. I prefer its cheaper domestic analogues. The efficiency is the same. I still don’t understand the difference, other than the high cost.”

The use of the highly effective new generation antipsychotic Fluanxol has improved the quality of life of patients with mental disorders and optimized therapeutic methods both at the active and maintenance (preventive) stages of treatment. The effectiveness of the drug has been proven by scientific research and daily clinical use.

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 .

Details about the injection form

The drug "Fluanxol Depot" is an oil solution intended for intramuscular depot injections. In other words, this medication is a deposited form of flupenthixol.

When using this solution in small and medium dosages (up to 100 mg once every 14 days), the patient does not have a nonspecific sedative effect. Although it still develops at high doses.

What do experts say about this form of the drug (“Fluanxol Depot”)? Reviews say that such a solution has a longer duration of effect on the patient than the medicine in tablets. Moreover, thanks to it, continuous antipsychotic treatment can be easily carried out, which is extremely important for patients who do not comply with medical prescriptions.

From all of the above, we can conclude that the drug “Fluanxol Depot” is able to prevent frequent relapses associated with spontaneous interruption of therapy. Intramuscular injections can be given at intervals of two or four weeks.

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.

Pharmacological properties of Fluanxol

Fluanxol is an antipsychotic that blocks dopamine receptors and adrenergic receptors in the brain. As a result of the action of flupenthixol, a sedative effect is achieved within 7 days of regular use of the drug.

Fluanxol has good reviews as a medicine that quickly eliminates symptoms of depression, psychosis and helps restore thinking. Patients with antisocial disorders gradually adapt to society and become sociable.

Fluanxol is rapidly absorbed and reaches maximum concentration within 4-7 hours. Bioavailability is 40-42%. The drug forms several inactive metabolites and is excreted from the body in feces and urine.

The drug enhances the effect of sedatives, ethanol and drugs that depress the nervous system. When taking Fluanxol and Guanethidine simultaneously, the therapeutic effect is reduced.

The interaction between Fluanxol and Piperazine increases the risk of adverse reactions and also contributes to the occurrence of extrapyramidal disorder.

special instructions

The use of Fluanxol in parallel treatment of diabetes mellitus may require adjustment of insulin .

With previous therapy with tranquilizers and antipsychotics with sedative effects, their use should be stopped gradually.

Long-term therapy with Fluanxol, especially in high doses, requires careful monitoring and assessment of the patient's condition for timely adjustment of maintenance doses.

You should refrain from driving vehicles, as well as precise and dangerous work.

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.

How does it work?

The action of Fluanxol is caused by blocking the activity of dopamine and serotonin receptors. The result of this process is a reduction in signs of brain malfunction. The bioavailability of internal administration of the drug is approximately 40%. It reaches its highest concentration in the blood after about 4-5 hours. It has a very high percentage of binding to blood proteins - almost 100%. Has the ability to penetrate the placenta in small quantities. It is excreted in feces and partially excreted in urine and breast milk. The half-life of the drug is about 35 hours.

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

ZdravCity

• Fluanxol tab.
  p/o captivity. 1 mg No. 50 NOT DEFINED 417 rub. order

Pharmacy Dialogue

• Fluanxol (tablet p/o 1 mg No. 50) Lundbeck

  RUR 442 order

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Pharmacy24

• Fluanxol 0.5 mg No. 100 tablets H. Lundbeck A/S, Denmark
  300 UAH. order
• Fluanxol depot 20 mg 1 ml No. 10 injection solution H. Lundbeck A/S, Denmark

  858 UAH order

• Fluanxol 1 mg No. 100 tablets H. Lundbeck A/S, Denmark

  261 UAH. order