Leponexum

• Structure
• Release form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications to use
• Contraindications
• Side effects
• Leponexum, application instruction (Way and dosage)
• Overdose
• Interaction
• Terms of sale
• Storage conditions
• Period of validity
• Analogs
• Responses

Structure

Tablets: clozapine, magnesium stearate, silicon colloid anhydrous, stearic acid, corn starch, polyvinylpirrolidone, talc, lactose, the purified water.

Solution for injections: clozapine, lauric acid, butylated hydroxyanisole, oil neutral.

Release form

Tablets are flat, rounded shape, yellow color 25 or 100 of mg in the blister in cardboard packaging No. 50, 100.

Solution for injections in glass ampoules of 1 and 2 ml in cardboard packaging No. 50.

Pharmacological action

Antipsychotic, sedative, antihistaminic.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Leponexum does not cause a katalepsy and, in difference from other HP neuroleptics, does not suppress a stereotyped behavior. Has the blocking effect of various degree of manifestation concerning dopamine receptors (D1 — D5), renders the expressed anticholinergic, adrenolytic, antihistaminic and slight antiserotoninergichesky action. Drug causes strong and fast sedation, has antipsychotic effect.

At the same time, the antipsychotic effect appears also at those at patients with schizophrenia who are steady against treatment in other HP. That is, drug effective in the relation both loss symptoms at schizophrenia, and productive symptomatology of a disease. Practically does not cause clinically significant extrapyramidal reactions (acute dystonia), does not increase prolactin levels that provides lack of side effects (an amenorrhea, impotence, a gynecomastia, a galactorrhoea).

Very seldom also parksinsonopodobny reactions meet. However, in connection with existence potentially dangerous side reactions of drug (an agranulocytosis, a granulocytopenia) recommend to appoint it only the patient with existence of resistance to other HP and which have a possibility of carrying out periodic control of composition of peripheral blood.

Pharmacokinetics

Drug is almost completely soaked up by their gastrointestinal tract, at the same time, meal does not influence the speed and extent of absorption. Bioavailability of drug about 55%. Cmax in blood are reached in two hours. It Biotransformirutsya in a liver, and in two stages. T1/2 — 12 hours, removal occurs in two phases and is carried out through kidneys and intestines.

Indications to use

• Treatment of schizophrenia at the patients having resistance to other neuroleptics or in the absence of therapeutic effect;
• The prevention of recurrence of suicide attempts at patients with schizoid frustration or schizophrenia;
• Treatment of psychoses at Parkinson's illness.

Contraindications

High sensitivity to drug, disorders of function of marrow, existence in the anamnesis of a granulocytopenia (toxic, idiosyncratic), epilepsy, psychoses of various genesis (alcoholic, toxic, medicinal), oppression TsNS, a vascular collapse, myocarditis, diseases of kidneys, a liver.

Side effects

Agranulocytosis, granulocytopenia, drowsiness, fatigue, sedation, headaches, dizzinesses, concern, delirium and excitement, confusion of consciousness, muscular rigidity, tremor, dryness in a mouth, disturbances of visual acuity, thermal control, the increased sweating, tachycardia, hypotension, a vascular collapse, changes on an ECG, nausea, vomiting, an ischuria, hepatitis.

Leponexum, application instruction (Way and dosage)

Pill is taken inside by 2-3 times a day after meal. The single dose varies within 50-200 mg, an average daily dose — 200-400 mg, maximum — 600 mg. The dosage of drug is selected individually, begin treatment with small doses gradually raising on 25-50 mg a day to emergence of therapeutic effect.

It is necessary to consider time of manifestation of this or that therapeutic effect: fast development of sedative and somnolent action; suppression of psychomotor excitement, concern or aggression can be expected in 3-6 days; anti-psychopathic action comes in 7-14 days, stopping of symptoms of negativism — 25-40 days. Then the patient is transferred to the supporting course which duration makes not less than half a year. At a daily dosage no more than 200 mg, it is possible to pass to a single dose of drug, it is desirable in the evening.

Solution of Leponexum is entered only by in oil 12,5 mg (0,5 ml) of 1 - 2 time in a dosage a day. In several days in transition to administration of drug inside is recommended.

Overdose

Mortality at overdose of drug in a dosage of 2 000 mg and more makes about 12%. Reception of Leponexum in a dose leads about 400 mg to development of heavy comas. Symptoms of overdose are drowsiness, hallucinations, an areflexia, a lethargy, a delirium, spasms, confusion of consciousness, a lump, excitement, extrapyramidal symptoms, increase of reflexes, a sight illegibility, expansion of pupils, the increased salivation, hypotension, a collapse, tachycardia, fluctuations of body temperature, arrhythmia, an asthma, respiratory depression.

Interaction

It is impossible to accept together with HP Leponexum, oppressing function of marrow. Also we will not combine Leponexum and alcohol as drug strengthens the central effect of alcohol. To observe extra care at a concomitant use of drug with the psychotropic HP, benzodiazepines, drugs with hypotensive and anticholinergic effect oppressing breath.

Use of Leponexum along with Cimetidinum or erythromycin leads to increase in concentration of drug in blood and to development of by-effects. Leponexum, thanks to adrenolytic activity weakens hypertensive effect of noradrenaline, and also drugs with an alpha adrenostimuliruyushchim action.

Terms of sale

According to the recipe.

Storage conditions

At a temperature up to 25 °C.

Period of validity

60 months.

Analogs

Azaleptol, Azaleptinum, Gedonin, Zipreksa, Azapin, Zilaire, Clozapine, Ketilept, Parnasan, Serokvel, Skizoril and others.

About Leponexum

According to doctors atypical neuroleptics of the last generation including Leponexum at rather expressed action "tearing off" psychosis in much smaller degree possess side effects. Except standard influence of drugs neuroleptics they are effective in the presence at the patient of symptoms of a shortcoming (deficit) of mental functions — emotional flatness, illogicalness of thinking, decrease cogitative function, lack of will, apathy.