Klopiksol of depot

General characteristics. Structure:

Active agent: 200 mg or 500 mg of a zuklopentiksol деканоат.

Excipients: triglycerides.

Pharmacological properties:

Pharmacodynamics. Klopiksol of depot is antipsychotic means (neuroleptic) derivative of thioxanthene. Klopiksol depot possesses the expressed antipsychotic and specific braking action. Nonspecific sedation weakens after several weeks of treatment.

Antipsychotic action of neuroleptics is usually connected with blockade of dopamine receptors that, apparently, causes chain reaction in which also other mediator systems are involved.

The specific braking action Klopiksol of depot is especially favorable at treatment of psychotic patients with agitation, concern, hostility or aggression.

Therapeutic action Klopiksol by depot is considerably more prolonged in comparison with Klopiksol. It allows to carry out surely continuous antipsychotic treatment Klopiksoly depot that is especially important for the patients who are not carrying out medical appointments. Klopiksol of depot prevents development of the frequent recurrence connected with any interruption by patients of reception of peroral medicines.

Pharmacokinetics. Pharmacokinetic and clinical tests of KLOPIKSOL of DEPOT showed that injections Klopiksol the depot is the most reasonable to spend bucketed 2-4 weeks. After introduction of a zuklopentiksol деканоат is exposed to zymolysis on active component зуклопентиксол and decanoic acid. The maximum concentration of a zuklopentiksol in blood serum is reached by the end of the first week after an injection. The concentration curve exponential decreases with the elimination half-life equal to 19 days that reflects release speed from depot. Zuklopentiksol slightly gets through a placental barrier and in small amounts is allocated with breast milk. Metabolites have no antipsychotic activity and are allocated, generally with a stake and, partially, with urine.

Pharmacokinetically Klopiksol's dose of depot of 200 mg of 1 times and 2 weeks is equivalent to a day peroral dose of 25 mg of Klopiksol within 2 weeks.

Indications to use:

Acute and chronic schizophrenia and other psychotic frustration, especially with hallucinations, paranoid nonsense and disturbances of thinking, and also a condition of agitation, the increased concern, hostility or aggression.

Route of administration and doses:

Klopiksol is deeply entered by depot intramusculary into an upper outside quadrant of a rump (good local tolerance). The dosage and an interval between injections are defined individually according to a condition of the patient.

Klopiksol of depot of 200 mg/ml: At the supporting treatment the range of dosages usually makes 200-400 mg (1-2 ml) each 2-4 weeks. Higher doses or shorter intervals between injections can be necessary for some patients. If the volume of the solution (200 mg/ml) entered intramusculary exceeds 2-3 ml, then it is more preferable to use solution of bigger concentration (Klopiksol of depot of 500 mg/ml).

Klopiksol of depot of 500 mg/ml: usually each 1-4 weeks enter 250-750 mg (0,5-1,5 ml). Upon transition from treatment by peroral Klopiksol or Klopiksolom-Akufaz on the supporting treatment KLOPIKSOLY DEPOT it is necessary to be guided by the following scheme:

Transition from peroral Klopiksol on Klopiksol depot intramusculary: a peroral daily dose of Klopiksol (mg) x 8 = Klopiksy depot (mg) intramusculary in 2 weeks.

Patients should continue to accept Klopiksol orally during the first week after the first injection, but in the reduced dose.

Transition from Klopiksola-Akufaz intramusculary on Klopiksol depot intramusculary: along with the last injection Klopiksola-Akufaz it is necessary to appoint intramusculary 200-400 mg (1-2 ml) of Klopiksl of depot. Repeated injections of Klopiksol of depot carry out 1 time in 2 weeks. If necessary higher doses or shorter intervals between injections can be used.

Features of use:

The Malignant Antipsychotic Syndrome (MAS) is a rare, but possible complication with a lethal outcome when using neuroleptics. 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 long therapy, especially in high doses, it is necessary to carry out careful control, periodically estimating a condition of patients to make the decision on reduction of the supporting dosage.

Klopikol's influence by depot on ability of driving and other mechanisms is possible. Therefore at the beginning of therapy it is necessary to show care until reaction of the patient to treatment is defined.

Side effects:

- from a nervous system. At the initial stage of treatment development of extrapyramidal symptoms is possible. In most cases they korrigirutsya by decrease in dosages and/or purpose of antiparkinsonichesky drugs. However regular preventive use of the last is not recommended. At long therapy some patients very seldom can have a late dyskinesia. Antiparkinsonichesky medicines do not eliminate its symptoms. Reduction of a dosage or if it is possible, the therapy termination is recommended.

- from mental activity. Drowsiness at an initial stage.

- from the autonomic nervous system and cardiovascular system. Dryness in a mouth, accommodation disturbance, an ischuria, a lock, tachycardia, orthostatic hypotension and dizziness.

- from a liver. Minor passing changes of level of "hepatic" transaminases and an alkaline phosphatase are seldom noted.

Interaction with other medicines:

Klopiksol of depot can strengthen sedative effect of alcohol, barbiturates and other inhibitors of the central nervous system.

Klopiksol the depot should not appoint together with guanetidiny and similarly operating means since neuroleptics can block their hypotensive action.

Klopiksol of depot can reduce efficiency of a levodopa and other adrenergic means, and the combination with Metoclopramidum and piperazin increases risk of development of extrapyramidal symptoms.

Klopiksol of depot can mix up with Klopiksolom-Akufaz, containing the same Viscoleo® oil.

Contraindications:

Acute alcoholic poisoning, barbiturates and opiates; comas. Klopiksol is not recommended to appoint depot during pregnancy and feeding a breast.

Klopiksol of depot has to be appointed with care to patients with a convulsive syndrome, chronic hepatitis and cardiovascular diseases.

Overdose:

Symptoms: Drowsiness, hypo - or a hyperthermia, hypotension, extrapyramidal symptoms, spasms, shock, a coma.

Treatment: Symptomatic and supporting. 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:

To store at a temperature not above 25 °C in the place protected from light. To store in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction (oil), 200 mg/ml, 500 mg/ml (ampoule) of 1 ml. Klopiksol of depot of 200 mg/ml: on 1 ml in an ampoule from colourless glass of type 1 (Evr. Pharm.). 1 or 10 ampoules with the application instruction in a cardboard pack with perforated control of the first opening (a uvula for opening) on the substrate from a cardboard pasted to a pack bottom. The red point specifying the place of a break is applied on an ampoule.

Klopiksol of depot of 500 mg/ml: on 1 ml in an ampoule from colourless glass of type 1 (Evr. Pharm.). 5 ampoules with the application instruction in a cardboard pack with perforated control of the first opening (a uvula for opening) on the substrate from a cardboard pasted to a pack bottom. The red point specifying the place of a break is applied on an ampoule.