Fluanxol, 5 mg 100 pcs

Fluenxol is an antipsychotic of the thioxanthene group.

Pharmacodynamics

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

The antipsychotic effects of Fluanxol begin to appear at a daily dose of 3 mg and become more pronounced with increasing dose. Fluanksol has a pronounced anxiolytic effect. The drug has disinhibiting (anti-anxiety and activating) properties, promotes activation of patients, increases their sociability and facilitates their social adaptation.
In small and medium doses (up to 25 mg per day) Fluanxol has no sedative effect, but when prescribing the drug in doses over 25 mg/day a sedative effect can develop.

In low doses (up to 3 mg/day), Fluanxol has an antidepressant effect.

Pharmacokinetics

Intake

After oral administration, C_max flupentixol in plasma is reached after 3-6 hours. Bioavailability is about 40%.

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

Distribution

The apparent V_d is about 14.1 L/kg. Binding to plasma proteins is about 99%. C_ss is achieved after 3 months of drug administration when administered intramuscularly in a solution for injection.

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

Metabolism

The metabolites have no neuroleptic activity.

The serum concentration curve decreases exponentially with a T_1/2 of approximately 3 weeks upon intramuscular administration of the solution for injection, reflecting the rate of release of flupentixol from the depot.

Flupentixol metabolites have no neuroleptic activity. They are excreted mainly in the feces and partially in the urine. T_1/2 is approximately 35 hours.

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

Indications

Anxiety, Depression, Moodiness, Mental Disorders, Schizophrenia

For oral 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.

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

Schizophrenia and schizophrenic-like psychoses with predominant hallucinatory symptoms, delirium, thought disorders, accompanied also by apathy, anergy, lowered mood and autism.

For intramuscular administration

Schizophrenia and other psychotic conditions occurring with hallucinations, delirium and thought disorders, accompanied by apathy, anergy, decreased mood and autism.

Active ingredient

Flupentixol

Composition

Active ingredient:

flupentixol dihydrochloride, which corresponds to 5 mg of flupentixol;

Ancillary substances:

Lactose monohydrate,

potato starch,

gelatin,

talc,

magnesium stearate;

Shell:

gelatin,

sucrose,

sucrose powder,

iron oxide yellow (E172).

How to take, the dosage

For therapy of depressive and anxiety disorders, the initial oral dose is 1 mg once daily in the morning or 500 mcg twice daily.

In case of absence of satisfactory therapeutic effect after 1 week the dose can be increased to 2 mg/day. The daily dose of 2 mg to 3 mg should be divided into several doses. In case of no therapeutic effect when using Fluanksol in a maximum dose of 3 mg/day for 1 week, the drug should be discontinued.

In therapy 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 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 once a day in the morning.

Interaction

When used concomitantly, Fluanxol may increase the sedative effect of ethanol, barbiturates and other CNS depressant drugs.

Fluanksol should not be used with guanethidine and agents with similar effects because neuroleptics may decrease their hypotensive effect.

Concomitant use of Fluanxol may decrease the effectiveness of levodopa and other adrenergic agents.

Concomitant use of Fluanksol with metoclopramide and piperazine increases the risk of extrapyramidal disorders.
Fluanksol should not be mixed with other fluids for injection.

Special Instructions

In concomitant treatment of diabetes mellitus, administration of Fluanksol may require adjustment of the insulin dose.

If the patient has previously been treated with neuroleptics or tranquilizers with a sedative effect, their administration should be stopped gradually.
In long-term therapy, especially with high doses of Fluanksol, careful monitoring and periodic evaluation of patients is necessary.

During pregnancy, Fluanksol should be used only if the anticipated benefit to the mother exceeds the potential risk to the fetus.
Newborns whose mothers have taken neuroleptic drugs in the last trimester of pregnancy or during delivery may show signs of intoxication, such as lethargy, tremors, and excessive excitability. In addition, such newborns have a low Apgar score.

Breastfeeding is allowed during treatment with Fluanxol if clinically necessary. However, it is recommended that the condition of the newborn be monitored, especially during the first 4 weeks after birth.

During treatment, it is necessary to refrain from driving and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

• high sensitivity to the ingredients of Fluanxol;
• vascular collapse;
• consciousness depression of any origin (including that caused by taking alcohol or barbiturates or opioid analgesics;
• coma;

children and adolescents before 18 years of age.

• consciousness depression of any origin (including alcohol, barbiturates, or opioid analgesics);
• coma;
• children and adolescents under 18 years of age;
• high sensitivity to phenothiazines;
• hereditary intolerance to galactose and/or fructose; lapp lactase deficiency; sucrose and isomaltase deficiency; glucose and galactose absorption disorders (when tablets are taken).

With caution, use in patients with organic brain disease, seizure disorders, including with epilepsy (as a result of decrease of seizure readiness threshold, increased frequency of seizures is possible); with severe hepatic insufficiency; with hypokalemia, hypomagnesemia; with cardiovascular diseases in anamnesis (risk of transient decrease of BP), includingwith prolongation of QT interval, bradycardia less than 50 bpm./min, with recent acute myocardial infarction, with uncompensated heart failure, with arrhythmia; with risk factors for stroke; with glaucoma (and predisposition to it); with gastric and duodenal ulcer disease; with alcoholism (possible increase of CNS suppressive effect); with pheochromocytoma; with leukopenia; respiratory disorders associated with acute infectious diseases, bronchial asthma or pulmonary emphysema; in Parkinson’s disease (increased extrapyramidal effects); with urinary retention, prostatic hyperplasia with clinical manifestations (risk of urinary retention); with Reye syndrome (increased risk of hepatotoxic effects); in pregnancy, during lactation (breastfeeding).

It is not recommended to prescribe Fluanksol at a dose of up to 25 mg/day to patients with psychomotor agitation, because the activating effect of Fluanksol in small doses (when taken orally up to 3 mg/day or when given by injection 10-20 mg once every 2 weeks) may lead to exacerbation of this symptomatology.

Side effects

The frequency of side effects and their severity are most pronounced at the beginning of treatment, they decrease as the therapy is continued.

Nervous system disorders: somnolence, dizziness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia; rarely – attention disorders, extrapyramidal disorders (mainly muscle rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, tardive dystonia.

Psychiatric disorders: insomnia, nervousness, agitation; infrequently – decreased libido, depression, confusion.

Cardiovascular system: infrequent – palpitations, orthostatic hypotension.

Hematopoietic system: rarely – granulocytopenia, agranulocytosis (more probable between weeks 4 and 10 of treatment), leukopenia, hemolytic anemia.

Visual organs: accommodation disorders, corneal and/or lens opacity with possible visual impairment; infrequent – oculogyric crisis.

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

Respiratory system disorders: infrequent – shortness of breath.

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

Urinary system disorders: infrequent urinary retention, painful urination.

Allergic reactions: infrequent itching, dermatitis, skin rash, photosensitization, increased sweating.

Muscular system and connective tissue disorders: infrequent – arthralgia.

Reproductive system disorders: infrequent – erectile dysfunction, galactorrhea.

As to the body in general: weakness, asthenia; infrequent – weight gain.

There are data about development of malignant neuroleptic syndrome (MNS). The main symptoms of MNS are hyperthermia, muscle rigidity and impaired consciousness combined with autonomic nervous system dysfunction (labile blood pressure, tachycardia, increased sweating). In addition to immediate discontinuation of neuroleptics, the use of general supportive measures and symptomatic treatment is essential.

Patients on long-term treatment may develop tardive dyskinesia. Antiparkinsonian medications do not eliminate its symptoms and may exacerbate them. Dose reduction or, if possible, discontinuation of treatment is recommended.

In persistent akathisia, benzodiazepines or propranololol may be helpful.

There have been isolated reports of minor transient changes in liver function tests.

The following side effects occurring with other neuroleptics have also been reported with flupentixol: 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).

Overdose

Symptoms: drowsiness, hyper- or hypothermia, extrapyramidal disorders, seizures, arterial hypotension, shock, coma are possible.
Treatment: symptomatic and supportive therapy is carried out.

In case of oral administration the stomach should be flushed as soon as possible, it is recommended to take a sorbent.

Measures should be taken to maintain respiratory and cardiovascular system activity. Adrenaline (epinephrine) should not be used as it may cause a subsequent decrease in BP.

Convulsions can be controlled with diazepam and extrapyramidal symptoms can be controlled with biperiden.

Pregnancy use

The use of Fluanksol in pregnancy and during lactation (breastfeeding) is possible only if the estimated benefit of therapy to the mother exceeds the potential risk to the fetus.

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

Breastfeeding is allowed during treatment with Fluanxol if it is clinically recognized as necessary. In such cases, it is recommended that the condition of the newborn be monitored, especially in the first 4 weeks after birth.