Fluanxol, (oil) 20 mg/ml 1 ml 10 pcs

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

The antipsychotic effects of Fluanxol begin to appear as early as at a daily dose of 3 mg and their intensity increases 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

For oral doses up to 3 mg/day

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

Composition

1 ml of solution for intramuscular administration contains:

the active ingredient:

cis(Z)-flupentixol decanoate 20 mg,

excipients:

Medium chain triglycerides.

.

How to take, the dosage

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

The drug in the form of an intramuscular solution of 20 mg/ml is usually given in a dose of 20-40 mg (1-2 ml) every 2-4 weeks. Some patients may require higher doses or shorter intervals between injections. An acute exacerbation or acute relapse may require injections of up to 400 mg at a single dose at 2 or even 1 week intervals.

Transition from oral Fluanksol to intramuscular administration

The daily dose (mg) of oral medication x 4 = a single dose (mg) of intramuscular solution every 2 weeks.

In this case, for the 1st week after the 1st injection, the oral dose should continue, but at a reduced dose.

The subsequent doses and intervals between injections are set according to clinical effect. The maximum dose of Fluxol when administered intramuscularly is 400 mg at a time with an injection interval of 1 week.

Patients who are being transferred from depot form therapy of other drugs should receive Fluanxol in the following ratios: 40 mg of flupentixol decanoate is equivalent to 25 mg of fluphenazine decanoate, 200 mg of zuclopentixol decanoate, or 50 mg of haloperidol decanoate.

Interaction

Fluanxol may increase the sedative effect of alcohol, the effect of barbiturates and other CNS depressants.
Fluanxol should not be administered together with guanethidine or similarly acting drugs because of possible weakening of hypotensive effect of these drugs.

The concomitant use of neuroleptics and lithium increases the risk of neurotoxicity.

Tricyclic antidepressants and neuroleptics mutually inhibit each other’s metabolism.

Fluenxol may decrease the effects of levodopa and the effects of adrenergic drugs, and combination with metoclopramide and piperazine increases the risk of extrapyramidal disorders.

The QT interval prolongation characteristic of antipsychotic therapy may be enhanced by concomitant administration of QT interval prolonging drugs: Class IA and III antiarrhythmic drugs (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs that increase QT interval. You should avoid concomitant administration of Fluanksol and the above mentioned drugs.
Fluanksol should be used with caution concomitantly with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and with drugs that can increase the plasma concentration of flupentixol because of the possible increased risk of prolonged QT interval and life-threatening arrhythmias.

Pharmaceutical Interactions

Fluenxol in the form of intramuscular injection solution should not be mixed with deposited sesame oil-based forms, as this may have a significant effect on the pharmacokinetics of the injected drugs.

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

Side effects

The frequency of side effects and their severity are most pronounced at the beginning of treatment and 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, seizure 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 likely between 4 and 10 weeks 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 2 and 4 weeks 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: prolongation of the QT interval, ventricular arrhythmias – ventricular fibrillation, ventricular tachycardia, sudden death and development of paroxysms of ventricular tachycardia (Torsade de Pointes) in rare cases.

Overdose

Symptoms. Drowsiness, coma, extrapyramidal symptoms, seizures, shock, hyperthermia/hypothermia.

In concomitant use with drugs that affect cardiac activity, changes in ECG, prolongation of the QT interval, development of paroxysms of ventricular tachycardia (Torsade de Pointes), cardiac arrest, ventricular arrhythmia have been reported.

Treatment. Symptomatic and supportive. Gastric lavage should be performed as soon as possible, the use of activated charcoal is recommended. Measures aimed at maintaining respiratory and cardiovascular system activity should be taken. Epinephrine (adrenaline) should not be used as it may lead to a subsequent drop in blood pressure. Seizures can be controlled with diazepam and extrapyramidal symptoms 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.