Fluanxol tablets 0.5 mg №100

Description Fluanxol tablets 0.5 mg №100

Trade name: FLYUANKSOL

International Nonproprietary Name: flupentiksol

Chemical name: 2 - [4 - [3 - [(EZ) -2 - (trifluoromethyl)-9H-thioxanthenes-9-ylidene] propyl] piperazin-1-yl] ethanol dihydrochloride.

Dosage form: tablets, coated tablets.

Composition: active ingredient - flupentiksola dihydrochloride (tablets 0.5 mg - 0.584 mg tablets)

Description:
0.5 mg and 1 mg - round, biconvex brownish-yellow tablets, covered with sugar shell;
5 mg - oval, biconvex brownish-yellow tablets, covered with sugar shell.

Pharmacotherapeutic group: antipsychotic (neuroleptic).

ATC code: N05AF01.

Pharmacological properties
Flyuanksol is a group of antipsychotic drugs tioksantenov.

Pharmacodynamics
Antipsychotic action of neuroleptics is associated with blockade of dopamine receptors, but possible, and blockade of 5 HT (5-gidroksitriptaminovyh) receptors.
Antipsychotic action Flyuanksola begins to emerge already in the appointment of a daily dose of 3 mg and its severity increases with dose. Flyuanksol has a pronounced anxiolytic action. The drug has a disinhibiting (antiautisticheskim and activating) properties, helps to activate patients, improves their communication skills and facilitating social adaptation.
In small and medium doses (25 mg / day) Flyuanksol has no sedative effect, however, the appointment of the drug in doses exceeding 25 mg / day. may develop sedation.
At lower doses (3 mg / day). Flyuanksol has antidepressant effects.

Pharmacokinetics
Flupentiksola bioavailability after oral administration is about 40%. The maximum concentration in serum is reached after 4-5 hours. The apparent volume of distribution (Vd) β is about 14.1 L / kg. Binding to plasma proteins around 99%. Flupentiksol slightly crosses the placental barrier and small amounts excreted in breast milk. Metabolites have no neuroleptic activity, distinguished mainly in feces, and partly in the urine. The half-life of approximately 35 hours.

Indications for Use

At a dose of 3 mg / day.
Depression, mild to moderate severity, coupled with anxiety, asthenia and lack of initiative.
Chronic neurotic disorders with anxiety, depression and apathy.
Psychosomatic disorders with asthenic manifestations.

At a dose of 3 mg / day. and more.
Schizophrenia and schizophrenia-like psychosis, with a predominance of hallucinatory symptoms, delusions and thought disorder, are also accompanied by apathy, anergy, depressed mood and autism.

Contraindications
Hypersensitivity to flupentiksolu or any of the excipients (including known hypersensitivity to phenothiazines), a hereditary galactose intolerance and / or fructose, lactose deficiency Lapa, the lack of sucrose and izomaltazy, impaired absorption of glucose and galactose.
Vascular collapse, depression of consciousness of any origin (including those caused by alcohol, barbiturates or opiates), coma.
Children's age (18 years).

Precautions: organic brain disease, seizure disorders, severe hepatic insufficiency, hypokalemia, hypomagnesemia, cardiovascular disease history (risk of transient reduction in blood pressure), including QT interval prolongation, bradycardia <50 beats per minute, recently transferred acute myocardial infarction, Non-compensable heart failure, arrhythmia, presence of risk factors for stroke, glaucoma (or predisposition to it), gastric ulcer and duodenal ulcer, alcoholism (may increase CNS depression), pheochromocytoma, leukopenia, respiratory failure associated with acute infectious diseases , asthma or emphysema, Parkinson's disease (enhancement of extrapyramidal effects), urinary retention, prostatic hyperplasia with clinical manifestations (the risk of urinary retention), Reye's syndrome (increased risk of hepatotoxicity), pregnancy, breast-feeding.
Not recommended for patients in a state of psychomotor agitation dose of 25 mg / day. Because activating effect Flyuanksola may lead to an exacerbation of this symptom.

Dosing and Administration
Tablets taken orally with water.

At a dose of 3 mg / day. (On the border of Psychiatry).
Initially 1 mg daily as a single morning dose or 0.5 mg twice a day. After a week with little therapeutic effect of the dose may be increased to 2 mg per day. Daily dose of more than 2 mg and 3 mg should be divided into several stages.
Elderly patients: The recommended daily dose of 0,5-1,5 mg.

Patient's response to Flyuanksol usually occurs within 2-3 days. If the effect of the maximum dose (3 mg / day) is not observed during the week, the drug should be discontinued.

At a dose of 3 mg / day. and more (for the treatment of psychoses).
The dose should be selected individually depending on the patient's condition. As a rule, the original should be used in small doses, which are then rapidly increased to the optimal effective level, depending on the clinical effect.
The initial daily dose - 3-15 mg - is divided into 2-3 doses. If necessary, the dose may be increased to 20-30 mg per day. The maximum daily dose is 40 mg.
Normal maintenance therapy - 5-20 mg / day.
Elderly patients: Recommended for lower doses.

Side effect
The incidence of side effects and their severity are most pronounced at the beginning of treatment, decrease with continued therapy.
The nervous system: drowsiness, dizziness, headache, tremor, akathisia, parkinsonism, hypokinesia, asthenia; infrequently - violations of attention, extrapyramidal disorder (mainly muscle rigidity and hyperkinesia), dyskinesia, amnesia, convulsive disorders, tardive dystonia.
On the part of mental activity: insomnia, nervousness, agitation, infrequently - decreased libido, depression, confusion.
Cardio-vascular system: Infrequent - palpitation, orthostatic hypotension.
On the part of hematopoiesis: rarely - granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia.
For part of the vision: disturbance of accommodation, corneal opacity and / or lens with possible visual impairment, rarely - oculogyric crisis.
From the digestive system: dry mouth, digestive disorders (including constipation, diarrhea, dyspepsia, nausea), excessive salivation, vomiting, cholestatic jaundice (more likely between 2 and 4 weeks of treatment).
Metabolic disorders and nutritional: Infrequent - decreased appetite, increased appetite.
From the respiratory system: Infrequent - shortness of breath.
On the part of the endocrine system: dysmenorrhea, gynecomastia, diabetes, reduced potency, changes in carbohydrate metabolism and tidal waves.
With the urinary system: Infrequent - urinary retention, painful urination.
Allergic reactions: seldom - itching, dermatitis, skin rashes, photosensitivity, increased sweating.
Violations of the musculoskeletal system and connective tissue disorders: Infrequent - arthralgia.
From the reproductive system: Infrequent - erectile dysfunction, galactorrhea.
From the body as a whole: weakness, fatigue; infrequently - weight gain.

There is evidence of the development of neuroleptic malignant syndrome (NMS). The main symptoms of NMS are hyperthermia, muscle rigidity, and impaired consciousness, combined with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, sweating). In addition to immediate discontinuation of antipsychotic essential use of common supportive measures and symptomatic treatment.
Patients who are on long-term treatment may develop tardive dyskinesia. Antiparkinsonian drugs do not eliminate her symptoms and may exacerbate them. Recommended dose reduction or, if possible, discontinuation of treatment.
In persistent akathisia may be useful benzodiazepines or propranolol.
There are few reports on the development of minor transient changes in indicators of liver function tests.
When you receive flupentiksola also registered the following side effects that occur when taking other antipsychotics: in rare cases, lengthening the interval QT, ventricular (ventricular) arrhythmia - ventricular fibrillation, ventricular tachycardia, sudden death and the development of ventricular tachycardia (Torsade de Pointes).

Drug overdose

Symptoms. Drowsiness, coma, extrapyramidal symptoms, convulsions, shock, hyperthermia / hypothermia.
When concomitantly with drugs that affect the heart's activity were recorded ECG changes, prolongation QT, the development of ventricular tachycardia (Torsade de Pointes), cardiac arrest, ventricular fibrillation.

Treatment. Symptomatic and supportive. As soon as possible should be produced gastric lavage is recommended the use of activated carbon. Measur