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Fluanxol is an antipsychotic of the group of thioxanthenes.
The antipsychotic action of neuroleptics is associated with the blockade of dopamine receptors, but, possibly, with the blockade of 5 HT (5-hydroxytryptamine) receptors.
The antipsychotic effect of Fluanxol begins to appear as soon as the daily dose of 3 mg is prescribed and its severity increases with increasing dose. Fluanxol has a pronounced anxiolytic effect. The drug has disinhibitory (anti-anthracistic and activating) properties, helps revitalize patients, increases their interpersonal skills and facilitates social adaptation.
In small and medium doses (up to 25 mg per day) Fluanxol does not have a sedative effect, however, when prescribing the drug in a dose of more than 25 mg / day. may develop sedation.
When taking small doses (up to 3 mg / day.) Fluanxol has an antidepressant effect.
After ingestion Cmax Flupentixol in plasma is reached in 3-6 hours. Bioavailability is about 40%.
After intramuscular injection of cis (Z) -flupentixol, decanoate is subjected to enzymatic cleavage into the active component of cis (Z) -flupentixol and decanoic acid. Cmax Serum cis (Z) -flupentixol is reached by the end of the first week after injection.
Seeming vd is about 14.1 l / kg. Plasma protein binding is about 99%. With intramuscular injection of solution for injection Css is achieved after 3 months of use of the drug.
Flupentixol and cis (Z) -flupentixol slightly penetrate the placental barrier, in small quantities are excreted in breast milk.
Metabolites do not possess neuroleptic activity.
With intramuscular injection of the solution for injection, the serum concentration curve decreases exponentially with T1/2equal to about 3 weeks, which reflects the rate of release of flupentixol from the depot.
Metabolites Flupentixola not possess antipsychotic activity. Excreted mainly in the feces and, in part, with the urine. T1/2 is approximately 35 hours.
A pharmacokinetic dose of Fluanxol 40 mg when administered intramuscularly 1 time in 2 weeks is equivalent to a dose of Fluanxol 10 mg / day when taken orally for 2 weeks.
Schizophrenia and other psychotic states occurring with hallucinations, delusions and thinking disorders, accompanied by apathy, anergy, decreased mood and autism.
1 ml solution for intramuscular injection contains:
active substance: cis (Z) -flupentixol decanoate 20 mg,
Excipients: triglycerides with medium chains.
Flupentixol is marketed under different brands and generic names, and comes in different dosage forms:
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Dosage and 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. With exacerbation or acute relapse of the disease It may be necessary to administer the drug in a dose of up to 400 mg simultaneously with 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 the solution for intramuscular administration every 2 weeks.
At the same time, during the 1st week after the 1st injection, the drug should be continued to be taken orally, but in a reduced dose.
Subsequent doses and intervals between injections are set in accordance with the clinical effect. The maximum dose of Fluanxol with intramuscular injection is 400 mg simultaneously with the interval between injections in 1 week.
Patients who are transferred from therapy with depo-forms of other drugs should receive Fluanxol taking into account the following ratios: 40 mg of flupentixol decanoate is equivalent to 25 mg of fluphenazine decanoate, 200 mg of suklopentyxol decanoate or 50 mg of haloperidol decanoate.
The frequency of occurrence of side effects and their severity are most pronounced at the beginning of treatment, decrease as therapy continues.
From the nervous system: drowsiness, dizziness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia; infrequently - attention disorders, extrapyramidal disorders (mainly muscular rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, late dystonia.
From the side of mental activity: insomnia, nervousness, agitation; infrequently - decreased libido, depression, confusion.
Since the cardiovascular system: infrequently - palpitations, orthostatic hypotension.
From the side of blood-forming organs: rarely - granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia.
From the organs of vision: accommodation disturbance, corneal and / or lens opacity with possible visual impairment; infrequently - oculogy crisis.
From the digestive system: dry mouth, indigestion 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 - loss of appetite, increased appetite.
On the part of the respiratory system: infrequently - shortness of breath.
On the part of the endocrine system: dysmenorrhea, gynecomastia, diabetes mellitus, reduced potency, changes in carbohydrate metabolism, hot flashes.
From the urinary system: infrequently - urinary retention, painful urination.
Allergic reactions: infrequently - itching, dermatitis, skin rash, photosensitivity, increased sweating.
Violations of the musculoskeletal system and connective tissue: infrequently - arthralgia.
From the reproductive system: infrequently - erectile dysfunction, galactorrhea.
On the part of the body as a whole: weakness, asthenia; infrequently - weight gain.
There is evidence of the development of neuroleptic malignant syndrome (SNS). The main symptoms of ZNS 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 the immediate cessation of neuroleptic intake, the use of general supportive measures and symptomatic treatment is essential.
Patients undergoing long-term treatment may develop tardive dyskinesia. Antiparkinsonic drugs do not eliminate its symptoms and may aggravate them. A dose reduction or, if possible, discontinuation of treatment is recommended.
Benzodiazepines or propranolol may be useful in persistent akathisia.
There are isolated reports on the development of minor transient changes in the performance of functional liver function tests.
When taking flupentixol, the following side effects have also been reported when taking other neuroleptics: in rare cases, prolongation of the QT interval, ventricular (ventricular) arrhythmia - ventricular fibrillation, ventricular tachycardia, sudden death, and development of ventricular tachycardia paroxysms (Torsade de Poistes)
Patients in a state of excitement or hyperactivity should not be prescribed in high enough doses (up to 3 mg).
Fluanxol can enhance the sedative effect of alcohol, the effect of barbiturates and other CNS depressants.
Fluanxol should not be prescribed together with guanethidine or similarly acting drugs because of the possible weakening of the hypotensive effect of these agents.
The simultaneous use of neuroleptics and lithium increases the risk of neurotoxicity.
Tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism.
Fluanxol can reduce the effect of levodopa and the action of adrenergic drugs, and the combination with metoclopramide and piperazine increases the risk of extrapyramidal disorders.
An increase in the QT interval, characteristic of antipsychotic therapy, can be enhanced while taking drugs that prolong the QT interval: anti-arrhythmic drugs Class I and III (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, increased vayuschih QT interval. It is necessary to avoid simultaneous administration of Fluanxol and the above mentioned drugs.
Fluanxol should be prescribed with caution simultaneously with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics), and drugs that can increase the concentration of flupentixol in the blood plasma, because of the possible increase in the risk of prolonged QT interval and the occurrence of life-threatening arrhythmias.
Fluanxol in the form of a solution for intramuscular injections should not be mixed with deposited forms based on sesame oil, because this may have a significant effect on the pharmacokinetics of the drugs administered.
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 outweighs 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, excessive irritability. In addition, these newborns have a low Apgar score.
Breast-feeding is allowed during treatment with Fluanxol, if it is considered clinically necessary. In such cases, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.
With the concomitant treatment of diabetes mellitus, the prescription of Fluanxole may require correction of the insulin dose.
If the patient was previously treated with neuroleptics or tranquilizers with a sedative effect, then their reception should be stopped gradually.
With long-term therapy, especially with the use of large doses of Fluanxol, it is necessary to conduct careful monitoring and periodic assessment of the patients.
During pregnancy, Fluanxol should be used only if the intended benefit to the mother outweighs the potential risk to the fetus.
Newborns whose mothers took antipsychotic drugs in the last 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.
During treatment with Fluanxol, breastfeeding is allowed, if it is considered 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 practicing potentially hazardous activities that require increased concentration and psychomotor speed.
Symptoms Drowsiness, coma, extrapyramidal symptoms, convulsions, shock, hyperthermia / hypothermia.
When taken simultaneously with drugs that affect cardiac activity, ECG changes, prolonged QT interval, development of paroxysmal ventricular tachycardia (Torsade de Pointes), cardiac arrest, ventricular arrhythmia were recorded.
Treatment. Symptomatic and supportive. Gastric lavage should be performed as soon as possible, the use of activated carbon is recommended. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use epinephrine (adrenaline), because this can lead to a subsequent lowering of blood pressure. Convulsions can be stopped by diazepam, and extrapyramidal symptoms biperidenom.
- Brand name: Fluanxol®
- Active ingredient: Flupentixol
- Dosage form: The solution for intramuscular oil
- Manufacturer: Lundbeck AS
- Country of Origin: Denmark
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