Fluanxol ampoules (for injection) 20mg 1 ml №10

Trade name
FLYUANKSOL DEPOT

International name
flyupentiksol decanoate

Latin name
FLUANXOL DEPOT

General Characteristics
colorless glass vials, which contain the cis (Z) - flyupentiksol decanoate as a solution in a light oil. Composition: 1 ml solution for injection contains 20 or 100 mg of cis (Z)-flyupentiksola decanoate; Excipients: liquid oil.

Form release
Injection in oil

Farmgruppa
Neuroleptic without sedative effects for long-term therapy.

Pharmacological properties
Flyuanksol Depot - thioxanthenes derivative with pronounced antipsychotic activating and anxiolytic activity. Antipsychotic effect of neuroleptics is usually associated with the blockade of dopamine receptors, which can cause a chain reaction that involve other neurotransmitter systems. Flyuanksol Depot is especially suitable for the treatment of patients with chronic psychoses. It weakens the main symptoms of psychosis such as hallucinations, paranoid delusions and thought disorders. Antipsychotic effect increases with increasing dosage. At doses ranging from small to moderate Flyuanksol Depot does not have a sedative effect. At higher doses can be expected uncharacteristically sedation. Flyuanksol Depot has the inhibitor and increases the mood of the action that makes the apathetic, depressed patients with low motivation for more active and those who are better and interact more actively looking for social contacts. Therapeutic effect Flyuanksola Depot is much more prolonged compared with Flyuanksolom. Flyuanksol Depot allows continuous antipsychotic medication, particularly those who have been unfairly take their prescribed medicines. Thus, Flyuanksol Depot warns frequent relapses are caused by not taking oral medicines.

Pharmacokinetics
Clinical trials Flyuanksola Depot showed that the injection can be conducted at intervals of 2 to 4 weeks. Cis (Z)-flyupentiksol decanoate in the body is subjected to enzymatic cleavage in the active component of the cis (Z)-flyupentiksol and decanoic acid. The maximum concentration in serum is achieved by the end of the first week after injection. He is in small quantities penetrate the placental barrier and small amounts excreted in breast milk. Metabolites have no pharmacological activity and are derived primarily from feces and partially - in the urine. The curve of serum concentration decreases exponentially with a half-life of about 3 weeks, which reflects the rate of release from custody. Pharmacokinetic dose Flyuanksola Depot 40 mg (2 weeks) is equivalent to a daily oral dose of 10 mg Flyuanksola.

Indications for Use
Schizophrenia and other psihotichnye disorders, especially with symptoms such as hallucinations, paranoid delusions and thought disorder, which are accompanied by apathy, anergy, and autism.

Dosing and Administration
Dose and the interval between injections is determined individually, respectively, a therapeutic response. Flyuanksol Depot is administered as an intramuscular injection. Local tolerance is good. Flyuanksol Depot 20 mg / ml: For maintenance treatment of the dosing range is typically 20 - 40 mg (1 - 2 ml) every 2-4 weeks. Some patients may need higher doses or shorter intervals between injections. If the required volume of solution (20 mg / ml) than 2-3 ml, then it is advisable to use a more concentrated solution (Flyuanksol Depot 100 mg / ml). Flyuanksol Depot 100 mg / ml: 50 - 200 mg (0.5 -1.5 ml) every 2 - 4 weeks. During an acute exacerbation or recurrence of the disease, you may need every 2 weeks or even a week at least one injection of 400 mg. Upon reaching effect was the gradual reduction to the corresponding dose (20-200 mg) every 2-4 weeks. In the transition from oral therapy to maintenance treatment Flyuanksolom Flyuanksolom Depot should be guided by the following scheme: an oral daily dose Flyuanksola (mg) x 4 = Flyuanksol Depot (mg) intramuscularly every 2 weeks. Patients should continue taking oral Flyuanksol during the first week after the first injection, but at a reduced dose. The following dose intervals between injections should be used appropriately the patient's response.

Side Effects
The nervous system: possible development of extrapyramidal symptoms, especially at the initial stage of treatment. In most cases, they are adjusted dose reduction and / or antiparkinsonian medication. Routine prophylactic use of antiparkinsonian medication is not recommended. Occasionally, long-term therapy, patients may develop tardive dyskinesia. Antiparkinsonian medications do not relieve these symptoms. Recommended dose reduction or, if possible, discontinuation of therapy. On the part of mental activity: transient insomnia, especially when the patient was transferred to the sedative neuroleptics. In high doses, some patients may experience sedation. From the autonomic nervous system and cardiovascular system: disturbances are very rare in the range of therapeutic doses. Part of the liver: there may be minor transient changes in liver samples.

Contraindications
Acute poisoning by alcohol, barbiturates and opiates; coma. Not recommended for patients who are agitated or over-active, because its activating effect may lead to an increase of these features. Flyuanksol Depot is not recommended during pregnancy and lactation.

Interaction with other drugs
Flyuanksol Depot may enhance response to alcohol and effect of barbiturates and other inhibitors of central nervous system. Flyuanksol Depot should not be administered together with guanetidinom and similar operating funds, since neuroleptics may block their hypotensive effect. Flyuanksol Depot may decrease the effectiveness of levodopa and other adrenergic funds, and joint reception with metoclopramide and piperazine increases the risk of extrapyramidal disorders.

Overdose
Symptoms: drowsiness, hypo-or hyperthermia, coma, extrapyramidal symptoms, seizures, hypotension, shock. Treatment: symptomatic and supportive. Measures should be taken with respect to support respiratory and cardiovascular systems. Do not use epinephrine, because it may lead to a consequent reduction in blood pressure. Cramps can be treated with diazepam and extrapyramidal symptoms biperidenom.

Features of
Flyuanksol Depot with caution to patients with convulsive syndrome, which was launched hepatitis and cardiovascular disease. If previously the patient was treated tranquilizers, which have sedative effects, should stop taking them gradually. Need to monitor closely and periodic assessment of patients with long-term therapy, especially in large doses to make the decision to reduce the maintenance dose. Neuroleptic malignant syndrome (NMS) is a rare but possible complication with a fatal outcome in the application of neuroleptics. The main characteristics of the CSN is hyperthermia, muscle rigidity, and impaired consciousness, combined with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, excessive sweating). In addition to immediate discontinuation of neuroleptics, it is important to use common support measures and symptomatic treatment. Despite the fact that Flyuanksol Depot does not cause sedation, is its possible impact on the ability to drive a car or machinery. Therefore, at the initial stage should be identified and careful until you set a reaction face for treatment.

Conditions and terms of
Store at or above the 25 ° C in a dark place. Shelf life of 4 years.

Conditions of supply
Prescription.

Packing
Oily solution for injection, 1 ml (20 mg / ml, 100 mg / ml) in ampoules № 10, 2 ml (20 mg / ml) in ampoules № 10

Manufacturer's name and address
H. Lundbeck A / S Address: Ottiliavej 9, DK - 2500 Copenhagen - Valby, Denmark