Fluanxol (Flupenthixol) - instructions: indications, contraindications, side effects

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.

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.

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.

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 solution in / m oil.
20 mg/ml 1 ml 10 pcs. Lundbeck 1010 rub. order
Fluanxol tab. p/o captivity. 1mg №50H.Lundbeck A/S
409 rub. order

Pharmacy Dialogue

Fluanxol (tablet p/o 1 mg No. 50) Lundbeck
RUB 388 order
Fluanxol (tablet p/o 5 mg No. 100) Lundbeck
RUB 1,043 order

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

Indications

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

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 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.

Fluanxol 1 mg 50 pcs. film-coated tablets

pharmachologic effect

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.

When taken orally, 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 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: transient insomnia is possible (especially after previous treatment with antipsychotics with a sedative effect), sedation (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.

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

The main spectrum of side effects associated with Fluanxol therapy is neuroleptic syndrome. Its main symptoms are extrapyramidal disorders, characterized by hyper- or hypokinetic disorders.

Hypokinetic side effects are represented by drug-induced parkinsonism, which manifests itself in the form of muscle rigidity and stiffness, slowness of speech and speed of reactions, and drowsiness. Hyperkinetic disorders include tremor, increased excitability, hyperthermia, and sweating.

In combination with extrapyramidal disorders, symptoms of akathisia may be observed - lack of perseverance, “restless legs syndrome”, sleep disorders, increased anxiety. Disturbances in the functioning of the autonomic nervous system cause the development of orthostatic hypotension, weight gain, pathological changes in appetite, problems with stool, and increased sweating.

Anticholinergic side effects such as visual disturbances and dysuria are sometimes observed. Possible disturbances in the functioning of the heart and blood vessels with characteristic changes on the ECG in the form of brady- or tachycardia, an increase in the Q-T interval. Some patients while taking Fluanxol develop skin reactions - pathological pigmentation, dermatoses, allergic reactions such as urticaria.