Flyuanksol

General characteristics. Structure:

Active ingredient: 0,584 mg, 1,168 mg or 5,84 mg of a flupentiksol of dihydrochloride that corresponds to 0,5 mg, 1 mg, 5 mg of a flupentiksol.

Excipients - lactoses monohydrate, potato starch, gelatin, talc, magnesium stearate.

Cover - gelatin, sucrose, sucrose powder, ferrous oxide yellow (E172).

Pharmacological properties:

Pharmacodynamics. Flyuanksol is antipsychotic means of group of thioxanthenes. Antipsychotic action of neuroleptics is connected with blockade of dopamine receptors, but, perhaps, and blockade of 5 HT (5-gidroksitriptaminovy) receptors.

Antipsychotic action of Flyuanksol begins to be shown already at purpose of a daily dose of 3 mg and its expressiveness increases with increase in a dose. Flyuanksol has the expressed anxiolytic effect. Drug possesses rastormazhivayushchy (anti-autistic and activating) properties, promotes activation of patients, increases their skill to communicate and facilitates social adaptation.

In small and medium doses (to 25 mg a day) Flyuanksol has no sedative effect, however, at purpose of drug in a dose over 25 mg/days can develop sedation.

At reception of small doses (to 3 mg/days) Flyuanksol has antidepressive effect.

Pharmacokinetics. Bioavailability of a flupentiksol at oral administration makes about 40%. The maximum concentration in blood serum is reached in 4-5 hours. The seeming volume of distribution (Vd) β makes about 14,1 l/kg. Linkng with proteins of a blood plasma about 99%. Flupentiksol slightly gets through a placental barrier and in small amounts is allocated with breast milk. Metabolites have no antipsychotic activity; are allocated, generally with a stake and, partially, with urine. The elimination half-life makes about 35 hours.

Indications to use:

In a dose to 3 mg/days. Depressions easy and moderate severity, combined with alarm, an adynamy and lack of an initiative. Chronic neurotic frustration with alarm, a depression and apathy. Psychosomatic disturbances with asthenic manifestations.

In a dose of 3 mg/days and more. The schizophrenia and shizofrenopodobny psychoses with dominance of hallucinatory symptomatology, nonsense and disturbances of thinking which are followed also by apathy, an anergy, decrease in mood and autism.

Route of administration and doses:

Pill is taken inside, washing down with water. In a dose to 3 mg/days (in boundary psychiatry). Initially 1 mg daily as single morning dose or 0,5 mg twice a day. In a week at insufficient therapeutic effect the dose can be increased to 2 mg a day. The daily dose more than 2 mg and to 3 mg should be divided into several receptions.

Elderly patients: the recommended daily dose makes 0,5-1,5 mg.

Reaction of patients on Flyuanksol usually comes within 2-3 days. If the effect of the maximum dose (3 mg a day) is not observed within a week, then drug should be cancelled.

In a dose of 3 mg/days and more (at treatment of psychoses). Doses of drug have to be selected individually depending on a condition of the patient. As a rule, originally it is necessary to use small doses which then are quickly increased to optimum effective level depending on clinical effect.

The initial daily dose - 3-15 mg - is divided into 2-3 receptions. If necessary it is possible to increase a dose to 20-30 mg a day. The maximum daily dose makes 40 mg. A usual maintenance therapy - 5-20 mg a day. Elderly patients: lower doses are recommended.

Features of use:

At the accompanying treatment of a diabetes mellitus Flyuanksol's appointment can demand insulin dose adjustment.

If earlier the patient was treated by neuroleptics or tranquilizers with sedative action, then their reception should be stopped gradually.

At long therapy, especially with use of high doses of Flyuanksol, it is necessary to carry out careful control and periodic assessment of a condition of patients.

During pregnancy Flyuanksol it is necessary to apply, only if the estimated advantage for mother exceeds potential risk for a fruit.

At newborns whose mothers accepted neuroleptics in the last trimester of pregnancy or at the time of delivery, symptoms of intoxication, such as lethargy, tremor and hyperexcitability can be observed. Besides, at such newborns the low point on a scale Apgar is noted.

During treatment by Flyuanksol feeding is allowed by a breast if it is recognized as clinically necessary. Nevertheless, it is recommended to watch a condition of the newborn, especially in the first 4 weeks after the birth.

During treatment it is necessary to refrain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of emergence of side effects and their weight are most expressed in an initiation of treatment, decrease in process of therapy continuation.

From a nervous system: drowsiness, dizziness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia; infrequently - disturbances of attention, extrapyramidal frustration (generally muscular rigidity and a hyperkinesia), dyskinesia, amnesia, convulsive frustration, late dystonia.

From mental activity: sleeplessness, nervousness, agitation; infrequently - decrease a libido, a depression, confusion of consciousness.

From cardiovascular system: infrequently - heartbeat, orthostatic hypotension.

From bodies of a hemopoiesis: seldom - a granulocytopenia, an agranulocytosis (is more probable between 4 and 10 weeks of treatment), a leukopenia, hemolitic anemia.

From organs of sight: accommodation disturbance, opacification of a cornea and/or crystalline lens with a possible vision disorder; infrequently - okulogirny crisis.

From the alimentary system: dryness in a mouth, digestive disturbances (including a lock, diarrhea, dyspepsia, nausea), the increased salivation, vomiting, cholestatic jaundice (is more probable between 2 and 4 weeks of treatment).

Disturbances of metabolism and frustration of food: infrequently - a loss of appetite, increase in appetite.

From respiratory system: infrequently - an asthma.

From endocrine system: dysmenorrhea, gynecomastia, diabetes mellitus, decrease in a potentiality, change of carbohydrate metabolism, inflows.

From an urinary system: infrequently - an ischuria, an urodynia.

Allergic reactions: infrequently - an itch, dermatitis, skin rash, a photosensitization, the increased sweating.

Disturbances of a musculoskeletal system and connecting fabric: infrequently - an arthralgia.

From reproductive system: infrequently - erectile dysfunction, a galactorrhoea.

From an organism in general: weakness, adynamy; infrequently - increase in weight.

There are data on development of the malignant antipsychotic syndrome (MAS). The main symptoms of ZNS are the hyperthermia, muscular rigidity and disturbance of consciousness in combination with dysfunction of the autonomic nervous system (labile arterial pressure, tachycardia, the increased sweating). Except the immediate termination of reception of neuroleptics use of the general supporting measures and a symptomatic treatment is extremely necessary.

At the patients who are on prolonged treatment late dyskinesia can develop. Antiparkinsonichesky drugs do not eliminate its symptoms and can aggravate them. The dose decline or if it is possible, the treatment termination is recommended.

At a persistent akathisia there can be useful benzodiazepines or propranolol.

There are single messages on development of minor passing changes of indicators of functional hepatic trials.

At reception of a flupentiksol the following side effects arising at reception and other neuroleptics were also registered: in rare instances lengthening of an interval of QT, ventrikulyarny (ventricular) arrhythmia - fibrillation of ventricles, ventricular tachycardia, sudden death and development of paroxysms of ventricular tachycardia (Torsade de Pointes).

Interaction with other medicines:

Flyuanksol can strengthen sedative effect of alcohol, action of barbiturates and other oppressing TsNS of substances.

Flyuanksol it is not necessary to appoint together with guanetidiny or similarly operating drugs because of possible weakening of hypotensive action of these means.

Simultaneous use of neuroleptics and lithium increases risk of a neurotoxicity.

Tricyclic antidepressants and neuroleptics mutually inhibit metabolism of each other.

Flyuanksol can reduce effect of a levodopa and effect of adrenergic drugs, and the combination with Metoclopramidum and piperazin increases risk of development of extrapyramidal disturbances.

The increase in QT of an interval characteristic of therapy by antipsychotic means, can be strengthened at a concomitant use of the drugs extending QT an interval: antiarrhytmic IA and III medicines of classes (quinidine, Amiodaronum, соталол, дофетилид), some antipsychotic means (thioridazine), some antibiotics macroleads (erythromycin) and antibiotics of a hinolonovy row (гатифлоксацин, moxifloxacin), some antihistamines (терфенадин, астемизол), and also a tsizaprida, lithium and other medicines increasing QT an interval. It is necessary to avoid a concomitant use of Flyuanksol and the drugs stated above.

Flyuanksol it is necessary to appoint with care along with the drugs causing electrolytic disturbances (thiazide and tiazidopodobny diuretics) and the drugs capable to increase concentration of a flupentiksol in a blood plasma, because of possible increase in risk of lengthening of QT of an interval and developing of life-threatening arrhythmias.

Contraindications:

Hypersensitivity to a flupentiksol or any of excipients (including the known hypersensitivity to fenotiazina), hereditary intolerance of a galactose and/or fructose, insufficiency of lactase the Paw, insufficiency of invertase and isomaltase, disturbance of absorption of glucose and a galactose.

Vascular collapse, oppression of consciousness of any origin (including caused by alcohol intake, barbiturates or opiates), a coma. Children's age (up to 18 years).

With care: organic diseases of a brain, convulsive frustration, a heavy liver failure, a hypopotassemia, a hypomagnesiemia, cardiovascular diseases in the anamnesis (risk of a tranzitorny lowering of arterial pressure), including lengthening of QT of an interval, bradycardia <50 beats per minute, recently postponed acute myocardial infarction, unindemnifiable heart failure, arrhythmia; existence of risk factors of development of a stroke, glaucoma (and predisposition to it), a peptic ulcer of a stomach and duodenum, alcoholism (oppression of TsNS can amplify); pheochromocytoma, leukopenia; the breath disturbance connected with acute infectious diseases, bronchial asthma or emphysema of lungs; Parkinson's disease (strengthening of extrapyramidal effects), an ischuria, a prostate hyperplasia with clinical manifestations (risk of an ischuria), a syndrome to Reja (increase in risk of development of a hepatotoxic action); pregnancy, breastfeeding period.
It is not recommended to appoint to patients in a condition of psychomotor excitement of a dose of drug to 25 mg/days since the activating Flyuanksol's action can lead to an aggravation of this symptomatology.

Overdose:

Symptoms. Drowsiness, coma, extrapyramidal symptoms, spasms, shock, hyperthermia/hypothermia. At a concomitant use with the drugs exerting impact on cordial activity changes on an ECG, lengthening of an interval of QT, development of paroxysms of ventricular tachycardia (Torsade de Pointes), a cardiac standstill, ventrikulyarny arrhythmia were registered.

Treatment. Symptomatic and supporting. The gastric lavage has to be as soon as possible made, use of absorbent carbon is recommended. The measures directed to maintenance of activity of respiratory and cardiovascular systems have to be taken. It is not necessary to use Epinephrinum (adrenaline) since it can lead to the subsequent lowering of arterial pressure. Spasms can be stopped diazepam, and extrapyramidal symptoms Biperidinum.

Storage conditions:

List B. At a temperature not above 30 °C. To store in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

0,5 mg and 1 mg: On 50 or 100 tablets in the plastic container with a transparent bottom and control of the first opening corked by the plastic cover having a cavity in which the application instruction invests. On a cover the method of a stamping applied the scheme of opening of a container. 5 mg: On 100 tablets in the plastic container with a transparent bottom and control of the first opening corked by the plastic cover having a cavity in which the application instruction invests. On a cover the method of a stamping applied the scheme of opening of a container.