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Pharmacological properties

Flupentixol is a neuroleptic of the thioxanthene group.

The antipsychotic effect of antipsychotics is associated with blockade of dopamine receptors, as well as a possible blockade of 5-HT receptors. In vitro and in vivo flupentixol has a high degree of affinity for dopamine D1- and D2to receptors. The atypical antipsychotic (clozapine) has a flupentixol-like affinity for D1- and D2receptors in vitro and in vivo.

Flupentixol has a high degree of affinity for α1-adrenoreceptors and 5-HT2-receptors, but lower than chlorprotixene, high-dose phenothiazines and clozapine, and has no affinity for cholinergic muscarinic receptors. It has weak antihistaminergic properties and does not inhibit α2-adrenoreceptors.

Like most other antipsychotics, flupentixol increases plasma prolactin levels.

Fluanxol has a wide dose-dependent spectrum of activity. Flupentixol in a low dose (1-2 mg / day) has an antidepressant, anxiolytic and activating effect. At an average dose (3–25 mg / day), flupentixol is used to treat acute and chronic psychosis; in this dose range, the drug has practically no non-specific sedative effect and is not suitable for the treatment of patients with severe psychomotor agitation. In addition to significantly reducing or completely eliminating the nuclear symptoms of schizophrenia, such as hallucinations, delusions and impaired thinking, flupentixol also has a disinhibition (anti-autistic and activating) effect, improves mood, which makes fupentixol especially effective in treating apathetic, autistic, depressed patients with weak motivation.

Antipsychotic effect increases with increasing dose; in addition, slight sedation can be expected. Flupentixol in the entire dose range has an anxiolytic effect, and even when using the drug in a high dose, the effects of disinhibition and mood enhancement are preserved. The use of the drug in a high dose does not increase the incidence of extrapyramidal symptoms.

Fluanxol Depot is a prolonged injection form of the drug. Fluanxol Depot is effective in the treatment of chronic psychoses. The antipsychotic effect increases with increasing dose. At low and medium doses (up to 100 mg once every 2 weeks), flupentixol decanoate does not have a sedative effect, a slight non-specific sedative effect can be expected when using the drug in a high dose.

Flupentixol decanoate is especially effective in treating patients with apathy, autism, depression, lack of motivation.

Fluanxol Depot provides the possibility of continuous treatment, which is very important for patients who do not follow the doctors prescription. Thus, the use of Fluanxol Depot prevents the occurrence of frequent relapses, which are associated with interruption of patients taking oral medications.

Pharmacokinetics

Fluanxol tablets. The bioavailability of flupentixol after oral administration is approximately 40%, and the maximum plasma concentration is reached after 4–5 hours. Binding to plasma proteins is approximately 99%. Metabolites do not have antipsychotic activity. T½ is approximately 35 hours, systemic clearance is about 0.29 l / min. Excretion occurs mainly with feces and partially with urine. Flupentixol in small amounts passes into breast milk. The kinetics is linear, the equilibrium concentration in the blood plasma is reached after 7 days.

Fluanxol Depot. After the administration of flupentixol, the decanoate is enzymatically digested into the active component cis (Z) -flupentixol and decanoic acid. WITHmax plasma flupentixol is reached by the end of the 1st week after injection. T½ Fluanxole Depot after i / m injection is 3 weeks (release period from the depot), the equilibrium plasma concentration is reached after 3 months with repeated use. T½ cis (Z) -flupentixol is about 35 hours; systemic clearance is about 0.29 l / min. Binding to plasma proteins is about 99%.

Pharmacokinetically, the dose of Fluanxole Depot 40 mg once every 2 weeks is equivalent to 10 mg of Fluanxol Depot per day when taken orally. Studies of pharmacokinetics when using Fluanxol Depot in elderly patients have not been performed. However, for such a drug from the thioxanthene group - zuclopentixol - the pharmacokinetic parameters are mainly independent of the patients age.

A significant change in the concentration of the drug in blood plasma is not expected in case of impaired renal function.

There is no data on changes in the pharmacokinetic parameters of the drug in case of impaired liver function.

Indications

Fluanxol tablets: depression, accompanied by anxiety, asthenia and lack of initiative. chronic neurotic disorders accompanied by anxiety, depression and inactivity. psychosomatic disorders with asthenic reactions. schizophrenia and other psychoses, especially with symptoms such as hallucinations, delirium, and thinking disorders, complicated by apathy, anergy, depressed mood, and autism.

Fluanxol Depot: A supportive treatment for schizophrenia and other psychoses, especially those with symptoms of hallucinations, delusions and impaired thinking, complicated by apathy, anergy, depression, and autism.

Application

Fluanxol tablets

Depression Chronic neurotic and psychosomatic disorders

The initial dose is 1 mg 1 time per day in the morning or 0.5 mg 2 times a day. After 1 week with insufficient clinical effect, the dose can be increased to 2 mg / day. If the daily dose exceeds 2 mg, then the drug is taken in several doses, up to a maximum of 3 mg per reception.

Elderly patients should be taken 1/2 the recommended dose is 0.5-1.5 mg / day.

The clinical effect when using Fluanxol usually occurs within 2-3 days. If the effect is not achieved when applying the maximum dose for 1 week, the drug should be discontinued.

Schizophrenia and other psychoses

The dose of the drug is determined individually, taking into account the condition of the patient. Initially, the drug should be used in a low dose and as soon as possible increase it to an optimally effective level, according to the therapeutic effect. The initial dose is 3-15 mg / day in 2-3 doses, which is increased if necessary to 40 mg / day. The maintenance dose is usually 5–20 mg / day, which can be taken once in the morning.

Elderly patients should be prescribed the drug in low doses.

In case of impaired renal function, flupentixol is prescribed in the usual dose.

In case of impaired liver function, careful selection of a therapeutic dose is recommended and, if possible, determination of the level of the drug in blood plasma.

The tablets are swallowed with water.

Fluanxol Depot

The dose of the drug and the interval between injections are determined individually, based on the achievement of maximum inhibition of psychotic symptoms with minimal side effects.

With maintenance treatment, the dose range is usually 20–40 mg (1–2 ml) every 2–4 weeks. Some patients are shown the use of the drug in a higher dose or less short intervals between injections.

Flupentixol decanoate is not suitable for the treatment of patients in need of sedation.

When switching from oral therapy with Fluanxol to maintenance treatment with Fluanxol Depot, the following scheme should be followed:

Oral daily dose of Fluanxol (mg) x 4 = Fluanxol Depot (mg) IM every 2 weeks.

Oral daily dose of Fluanxol (mg) x 8 = Fluanxol Depot (mg) IM every 4 weeks.

Patients should continue to take oral fluanxol during the 1st week after the 1st injection, but in a reduced dose.

When switching to the treatment of flupentixol decanoate with other deposited drugs, the following ratio should be observed: 40 mg of flupentixol decanoate corresponds to 25 mg of flufenazine decanoate, 200 mg of zuclopentixol decanoate or 50 mg of haloperidol decanoate.

Subsequent doses and intervals between injections are set according to the patients clinical response to therapy.

Elderly patients should be given the minimum therapeutic dose.

In case of impaired renal function, flupentixol is prescribed in usual doses.

In case of impaired liver function, it is necessary to titrate the therapeutic dose with caution, and also, if possible, determine the level of the drug in the blood plasma.

Route of administration. Fluanxol Depot is used as an intramuscular injection into the upper quadrant of the buttock. A 2 ml preparation should be divided between two injection sites. Local tolerance is satisfactory.

Contraindications

Hypersensitivity to the components of the drug, vascular collapse, inhibition of central nervous system function of various origins (e.g. alcohol, barbiturate or opioid intoxication), coma.

Side effects

In most cases, dose-dependent. their frequency and severity are more pronounced at the beginning of therapy and decrease with further treatment.

Extrapyramidal symptoms may develop, especially at the beginning of therapy. In most cases, they are adjusted by dose reduction and / or the use of anti-Parkinsonian drugs. Regular prophylactic use of the latter is not recommended. Antiparkinsonian drugs do not stop tardive dyskinesia and can exacerbate it. It is recommended to reduce the dose or, if possible, stop treatment with flupentixol. In cases of persistent akathisia, benzodiazepine or propranolol is recommended.

The frequency of adverse reactions in the following table is defined as: very often (≥1 / 10); often (≥1 / 100, but 1/10); infrequently (≥1 / 1000, but 1/100); rarely (≥1 / 10,000, but 1/1000) or very rarely (1/10 000).

Organ systems Frequency Manifestations
Disorders of the cardiovascular system Often Tachycardia, palpitations
Infrequently Arterial hypotension, blush
Rarely ECG Q-T interval extension
Disorders from the hematopoietic and lymphatic system Rarely Thrombocytopenia, neutropenia, leukopenia, agranulocytosis
Disorders of the nervous system Often Drowsiness, akathisia, hyperkinesia, hypokinesia
Often Tremor, dystonia, dizziness, headache
Infrequently or rarely Tardive dyskinesia, parkinsonism, speech impairment, convulsions
Rarely Malignant antipsychotic syndrome
Violations of the organ of vision Often Violation of accommodation, vision
Infrequently Eye movements
Respiratory system disorders Often Dyspnea
Gastrointestinal Disorders Often Dry mouth
Often Hypersalivation, constipation, vomiting, dyspepsia, diarrhea
Infrequently Abdominal pain, nausea, flatulence
Urinary system disorders Often Impaired urination, urinary retention
Disorders of the skin and subcutaneous tissue Often Hyperhidrosis, itching
Infrequently Rash, photosensitivity reactions, dermatitis
Musculoskeletal disorders Often Myalgia
Infrequently Muscle stiffness
Disorders from the endocrine system Rarely Hyperprolactinemia
Metabolic disorders Often Increased appetite, weight gain
Infrequently Decreased appetite
Rarely Hyperglycemia, impaired glucose tolerance
General disorders and local reactions Often Asthenia, fatigue
Infrequently Injection site reactions
Immune System Disorders Rarely Hypersensitivity, anaphylactic reaction
Disorders from the hepatobiliary system Infrequently Functional test failure
Rarely Jaundice
Disorders from the reproductive system and mammary glands Infrequently Lack of ejaculation, erectile dysfunction
Rarely Gynecomastia, galactorrhea, amenorrhea
Mental disorders Often Insomnia, depression, anxiety, nervousness, decreased libido
Infrequently Confusion

There are reports of rare cases of prolongation of the Q – T interval, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, torsade de pointes arrhythmias and sudden death when using drugs of the antipsychotic group, including flupentixol.

Abrupt cessation of therapy with flupentixol can cause withdrawal symptoms, the most common of which are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, anxiety, anxiety and agitation. Dizziness, variable sensations of heat or cold, and tremors may also occur. Withdrawal symptoms usually develop within 1–4 days after discontinuation of therapy and decrease over 7–14 days.

special instructions

The likelihood of developing a malignant antipsychotic syndrome (hyperthermia, muscle stiffness, impaired consciousness, autonomic nervous system dysfunction) exists with the use of any antipsychotic. the risk increases with the use of several drugs. among fatal cases, patients with organic syndrome, mental retardation, abuse of opiates and alcohol predominate.

Treatment: cessation of the use of antipsychotics, symptomatic therapy. Dantrolene and bromocriptine can be used.

Symptoms may persist for 1 week or more after discontinuation of oral forms and longer after taking deposited forms of drugs.

Like other antipsychotics, flupentixol is used with caution in the treatment of patients with organic brain syndrome, seizures, and progressive liver disease.

The use of flupentixol in a low dose is not recommended for the treatment of excitable, hyperactive patients, since the activating effect of the drug can enhance the severity of these manifestations. When switching to treatment with flupentixol, tranquilizers or sedative antipsychotics should be withdrawn gradually.

Like other antipsychotics, flupentixol can change the profiles of insulin and glucose in the body, therefore, correction of antidiabetic therapy in patients with diabetes is necessary.

During maintenance therapy, especially when using the drug in high doses, you should carefully monitor the patients condition and periodically evaluate the possibility of reducing the maintenance dose.

When using some atypical antipsychotics in randomized, placebo-controlled trials, a 3-fold increase in the risk of cerebrovascular side effects was observed among the patient population with dementia. The mechanism of this phenomenon is unknown. An increased risk cannot be excluded for other antipsychotics and patient populations. Flupentixol should be used with caution in patients with risk factors for stroke.

Just like other drugs of the antipsychotic group, flupentixol can lead to a prolongation of the Q – T interval. Existing Q-T prolongation may increase the risk of malignant arrhythmias. Therefore, flupentixol should be used with caution in patients with suspected hypokalemia, hypomagnesemia, or with a genetic tendency to these conditions, as well as in patients with a history of cardiovascular diseases, for example, an extended Q – T interval expressed by bradycardia (50 beats / min) recently undergoing myocardial infarction, uncompensated heart failure or cardiac arrhythmia. Concurrent use with other antipsychotics should be avoided.