Azaleptol таб. 0.025, 0.1 g No. 50

General characteristics. Structure:

Active ingredient: Clozapine

Pharmacological properties:

Has the expressed antipsychotic and sedative effect. Practically does not cause extrapyramidal disturbances; in this regard clozapine is carried to group of "atypical" neuroleptics. The mechanism of antipsychotic effect of clozapine is not finalized. The greatest activity is noted concerning dopamine receptors of limbic area of a brain where clozapine interferes with linkng of dopamine with D1-and D2 - dopamine receptors. This effect is less expressed, than at "typical" neuroleptics. Clozapine contacts preferential in nedofaminergichesky sites (alpha adrenoceptors, serotoninovy, histamine and holinoretseptor). Clozapine poorly influences or does not influence concentration of prolactin at all in a blood plasma as does not communicate dopamine receptors in a tuberoinfundibulyarny path. Characteristic pharmacological features of an azaleptol are the oppression of reaction of activation registered on the electroencephalogram at electric irritation of a reticular formation average of a brain, the expressed central and peripheral anticholinergic action, peripheral adrenolytic action: drug has no kataleptogenny effect: according to the available data, slows down dopamine release by presynaptic nerve terminations.
Clinically differs in strong antipsychotic action in combination with a sedative component in the absence of extrapyramidal by-effects inherent to other neuroleptics (that, perhaps, is connected with the central cholinolytic effect of drug). Does not cause strong general oppression as aminazine and other aliphatic fenotiazina.

Pharmacokinetics. At intake it is soaked up quickly and almost completely. The maximum concentration in plasma is reached on average during 2,5 h. Equilibrium concentration are reached in 8-10 days of reception. Is exposed to intensive metabolism at "the first passing" through a liver with formation of metabolites of low activity or inactive. Distribution intensive and bystry, passes through a blood-brain barrier. Linkng with proteins – 95%.
The elimination half-life makes 8 h. It is removed by kidneys – 50% and through intestines - 30%.

Indications to use:

Apply at hallucinatory-dilision. katatono-gebefrenny katatonogallyutsinatorny conditions and conditions of psychomotor excitement at schizophrenia, at a maniacal syndrome within maniac-depressive psychosis, at affective tension and frustration of mood, at psychopathies at the excited patients. In certain cases drug is effective at resistance to treatment by other neuroleptics.

Route of administration and doses:

Individually. Appoint inside (after food) 2-3 times a day. A single dose for adult 50 - 200 mg: daily dose of 200-400 mg. Treatment usually begin 25 - 50 mg with a dose, then gradually increase by 25 - 50 mg a day up to 200 - 300 mg a day within 7-14 days. For a maintenance therapy and an ambulatory appoint 25-200 mg a day (it is possible in the form of the single dose accepted in the evening). In small doses (25-50mg) drug can be used at frustration of a dream of various genesis. At cancellation of treatment it is necessary to reduce gradually a dose within 1 - 2 weeks. The maximum daily dose of 600 mg (0,6 g) in days.

Features of use:

As well as other neuroleptics, it is not necessary to appoint drug an ambulatory in case of performance of the work demanding bystry mental and physical reaction by them (drivers of transport, etc.).
With extra care apply at suspicion of closed-angle glaucoma, at a prostatauxe, epilepsy (including in the anamnesis), and also at patients with diseases of cardiovascular system, digestive tract, at a renal failure.
During treatment systematic control of a picture of peripheral blood is necessary. At use of clozapine it is necessary to exclude alcohol intake.

Side effects:

Azaleptol is usually well had: in connection with the expressed central cholinolytic action and moderate influence on dopamine receptors does not cause extrapyramidal disturbances. Nevertheless, at treatment azaleptoly muscular weakness, drowsiness, confusion of consciousness, dryness in a mouth, orthostatic hypotension, tachycardia can be observed. The most serious complication - a granulocytopenia (up to an agranulocytosis). Therefore it is necessary to watch carefully a blood picture Blood tests carry out to the first 18 weeks of treatment every week, then through more long periods. Exercise control also of a condition of cardiovascular system.

Interaction with other medicines:

At simultaneous use of clozapine with the etanolsoderzhashchy drugs, ethanol and other means having the oppressing effect on TsNS. increase of weight and frequency of manifestation of depressive action on TsNS is possible; with the drugs causing a miyelodepressiya - strengthening of the oppressing action on marrow is possible; with lithium drugs - increase in risk of epileptic seizures, confusion of consciousness, NZS and diskineziya is possible; with anticholinergics - strengthening of their effects is possible; with digoxin or with the drugs which are characterized by high linkng with proteins (including heparin, warfarin, Phenytoinum) - increase in their concentration in a blood plasma, is possible also replacement of clozapine with these drugs from sites of its linkng with proteins; with the drugs causing arterial hypotension - the perhaps additive hypotensive action.

Contraindications:

Drug is contraindicated to patients with changes of a picture of blood, at alcoholic and other toxic psychoses, a spasmophilia, epilepsy, a serious illness of a liver, kidneys, cardiovascular system, diseases of the hemopoietic system, closed-angle glaucoma, a prostatauxe, an intestines atony, at pregnancy, comas.

Overdose:

About cases of overdose of drug it was not reported.

Storage conditions:

To store in the dry, protected from light place. To store in the place, unavailable to children.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 50 tablets in jars polymeric.