Fluanxol pills 5mg, 100pcs

Composition

Active ingredient:

flupentixol dihydrochloride, which corresponds to 5 mg of flupentixol;

Auxiliary substances:

lactose monohydrate,

potato starch,

gelatin,

talc,

magnesium stearate;

Shell:

gelatin,

sucrose,

sucrose powder,

iron oxide yellow (E 172).

Pharmacological action

Fluanxol is an antipsychotic agent of the thioxanthene group.

Pharmacodynamics

The antipsychotic effect of neuroleptics is associated with the blockade of dopamine receptors, but possibly also with the blockade of 5 HT (5-hydroxytryptamine) receptors.

The antipsychotic effect of Fluanxol begins to manifest itself already with the appointment of a daily dose of 3 mg and its severity increases with increasing dose. Fluanxol has a pronounced anxiolytic effect. The drug has disinhibiting (anti-autistic and activating) properties, promotes activation of patients, increases their sociability and facilitates social adaptation. In small and medium doses (up to 25 mg per day), Fluanxol does not have a sedative effect, however, when the drug is prescribed at a dose of more than 25 mg/ day. sedation may occur.

When taking small doses (up to 3 mg/day), Fluanxol has an antidepressant effect.

Pharmacokinetics

Suction

After oral use, the plasma cmax of flupentixol is reached in 3-6 hours. Bioavailability is about 40%.

After intramuscular use of cis(Z)-flupentixol, decanoate undergoes enzymatic cleavage into the active component of cis(Z) – flupentixol and decanoic acid. Serum cis(Z)-flupentixol cmax is reached by the end of the first week after injection.

Distribution

The apparent Vd is about 14.1 l / kg. Binding to plasma proteins is about 99%. With intramuscular injection of a solution for injection, C_ss is achieved after 3 months of using the drug.

Flupentixol and cis (Z) – flupentixol slightly penetrate the placental barrier, and are excreted in small amounts in breast milk.

Metabolism

The metabolites do not have neuroleptic activity.

Deduction

With intramuscular injection of the solution, the serum concentration curve decreases exponentially with T_1/2equal to approximately 3 weeks, which reflects the rate of release of flupentixol from the depot.

Flupentixol metabolites do not have neuroleptic activity. They are mainly excreted in the faeces and, in part, in the urine. T_1/2 is approximately 35 hours.

Pharmacokinetically, the dose of Fluanxol 40 mg when administered intramuscularly 1 time in 2 weeks is equivalent to the dose of Fluanxol 10 mg / day when taken orally for 2 weeks.

Indications

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

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

For intramuscular use

, Schizophrenia and other psychotic states that occur with hallucinations, delusions and thinking disorders, accompanied by apathy, anergy, mood decline and autism.

Use during pregnancy and lactation

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

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

Breast-feeding is permitted during treatment with Fluanxol if it is clinically necessary. In such cases, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

Contraindications

• hypersensitivity to the components of the drug Fluanxol;
• vascular collapse;
• depression of consciousness of any origin (including caused by alcohol, barbiturates, or opioid analgesics);
• coma;
• childhood and adolescence to 18 years;
• hypersensitivity to fenotiazinas;
• hereditary intolerance to galactose and/or fructose; the lapp lactase deficiency; deficiency of sucrase and isomaltase; impaired absorption of glucose and galactose (when the pill).

Use with caution in patients with organic brain diseases, convulsive disorders, including epilepsy (as a result of a decrease in the threshold of convulsive readiness, seizures may become more frequent); with severe liver failure; with hypokalemia, hypomagnesemia; with a history of cardiovascular diseases (risk of a transient decrease in blood pressure), including with QT interval prolongation, bradycardia less than 50 beats/min, with a recent acute myocardial infarction, with non-compensable heart failure, arrhythmia; with risk factors for stroke; with glaucoma (and predisposition to it); with peptic ulcer of the stomach and duodenum; with alcoholism (possibly increased depressive effect on the central nervous system); with pheochromocytoma; with leukopenia; respiratory disorders associated with acute infectious diseases, bronchial asthma or emphysema of the lungs; 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 hepatotoxic effects); during pregnancy, 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, since the activating effect of Fluanxol in small doses (when taken orally up to 3 mg/day or with an intravenous use of 10-20 mg 1 time in 2 weeks) can lead to an exacerbation of these symptoms.

Side effects

The frequency of side effects and their severity are most pronounced at the beginning of treatment, and decrease with the continuation of therapy.

From the nervous system: drowsiness, dizziness, headache, tremor, akathisia, Parkinsonism, hypokinesia, dystonia; infrequently-attention disorders, extrapyramidal disorders (mainly muscle rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, late dystonia.

From the side of mental activity: insomnia, nervousness, agitation; infrequently-decreased libido, depression, confusion.

From the cardiovascular system: infrequently-palpitations, orthostatic hypotension.

Hematopoietic disorders: rarely-granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia.

From the side of the visual organs: impaired accommodation, opacity of the cornea and / or lens with possible visual impairment; infrequently-oculohiric crisis.

From the digestive system: dry mouth, digestive disorders (including constipation, diarrhea, dyspepsia, nausea), increased salivation, vomiting, cholestatic jaundice (more likely between 2 and 4 weeks of treatment). Metabolic disorders and eating disorders: infrequently-decreased appetite, increased appetite.

From the respiratory system: infrequently-shortness of breath.

From the endocrine system: dysmenorrhea, gynecomastia, diabetes mellitus, decreased potency, changes in carbohydrate metabolism, hot flashes.

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

Allergic reactions: infrequently-pruritus, dermatitis, skin rash, photosensitization, increased sweating.

Musculoskeletal and connective tissue disorders: infrequently-arthralgia.

From the reproductive system: infrequently-erectile dysfunction, galactorrhea.

From the body as a whole: weakness, asthenia; infrequently – weight gain.

There are data on the development of neuroleptic malignant syndrome (NMS). 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). In addition to immediate discontinuation of antipsychotic medications, general supportive measures and symptomatic treatment are essential.

Patients undergoing long-term treatment may develop tardive dyskinesia. Antiparkinsonian medications do not eliminate its symptoms and may worsen them. It is recommended to reduce the dose or, if possible, discontinue treatment.

For persistent akathisia, benzodiazepines or propranolol may be useful.

There are isolated reports of the development of minor transient changes in the indicators of functional liver tests.

When taking flupentixol, the following side effects that occur with other antipsychotics have also been reported: in rare cases, prolongation of the QT interval, ventricular (ventricular) arrhythmia – ventricular fibrillation, ventricular tachycardia, sudden death and the development of paroxysms of ventricular tachycardia (Torsade de Pointes).

Interaction

When used concomitantly, Fluanxol may enhance the sedative effect of ethanol, barbiturates and other drugs that have a depressing effect on the central nervous system.

Fluanxol should not be used in combination with guanethidine and drugs with a similar effect, since neuroleptics can weaken their hypotensive effect.

When used concomitantly, Fluanxol may reduce the effectiveness of levodopa and other adrenergic agents.

When Fluanxol is co-administered with metoclopramide and piperazine, the risk of extrapyramidal disorders increases. Fluanxol should not be mixed with other fluids for injection.

How to take, course of use and dosage

For the treatment of depressive and anxiety disorders, the initial dose of the drug for oral use is 1 mg 1 time / day in the morning or 500 mcg 2 times/day.

In the absence of a satisfactory therapeutic effect, the dose can be increased to 2 mg/day after 1 week. The daily dose, ranging 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 discontinued.

In the treatment of psychotic states, the dose is set individually, depending on the patient’s condition. The initial daily dose is 3-15 mg in 2-3 divided 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 in a dose of 5-20 mg 1 time/day in the morning.

Overdose

Symptoms: possible drowsiness, hyper-or hypothermia, extrapyramidal disorders, seizures, hypotension, shock, coma. Treatment: conduct symptomatic and supportive therapy.

If the drug is taken orally, it is necessary to flush the stomach as soon as possible, and it is recommended to take a sorbent.

Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Do not use epinephrine (epinephrine), as this may lead to a subsequent decrease in blood pressure.

Seizures can be treated with diazepam, and extrapyramidal symptoms can be treated with biperiden.

Special instructions

With concomitant treatment of diabetes mellitus, the appointment of Fluanxol may require an adjustment of the insulin dose.

If the patient has previously been treated with antipsychotics or sedative tranquilizers, they should be discontinued gradually. With long-term therapy, especially with the use of high doses of Fluanxol, it is necessary to carefully monitor and periodically assess the condition of patients.

During pregnancy, Fluanxol should only be used if the intended benefit to the mother outweighs the potential risk to the fetus. Newborns whose mothers took antipsychotic medications in the last trimester of pregnancy or during labor may experience signs of intoxication, such as lethargy, tremors, and excessive excitability. In addition, these newborns have a low Apgar score.

Breast-feeding is permitted during treatment with Fluanxol if it is clinically necessary. However, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Flupentixol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Mental Disorders, Schizophrenia, Depression