Clozapine - instructions for use, doses, side effects, contraindications

In the central nervous system predominantly blocks dopamine D₄-receptors (in comparison with D₂receptors) and serotonin 5-HT₂A receptors, as well as M-cholinergic receptors and α₁-adrenoceptors of the brain, due to which eliminates negative symptoms in patients with schizophrenia (poverty of speech, introversion, flattening of emotions).

Has a pronounced sedative effect, rarely causes extrapyramidal disorders, does not cause retardation.

Does not cause prolactinemia, therefore does not lead to the development of galactorrhea, gynecomastia, impotence.

Pharmacokinetics:

After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 2.5 hours. The connection with plasma proteins is 95%. Penetrates through the blood-brain barrier.

Metabolism in the liver to inactive metabolites.

The half-life is 12 hours. Elimination by the kidneys.

Indications:

It is used to treat all forms of schizophrenia, the manic stage of manic-depressive psychosis.

ICD-10

V.F20-F29.F20.9 Schizophrenia, unspecified

V.F20-F29.F20.8 Another type of schizophrenia

V.F20-F29.F20 Schizophrenia

V.F20-F29 Schizophrenia, schizotypic and delusional disorders

V.F20-F29.F22 Chronic delusional disorders

V.F20-F29.F23.8 Other acute and transient psychotic disorders

V.F20-F29.F23 Acute and transient psychotic disorders

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F30-F39.F30 Manic episode

V.F30-F39.F31 Bipolar affective disorder

V.F50-F59.F51.2 Sleep and wakefulness disorder inorganic etiology

Contraindications:

Diseases of the hematopoietic system, intoxication and alcoholic psychoses, coma, myasthenia gravis, individual intolerance, children's age.

Carefully:

Severe renal and hepatic insufficiency, prostatic hyperplasia, increased propensity to convulsions, epilepsy, angle-closure glaucoma, decompensated diseases of the cardiovascular system, intercurrent diseases with febrile syndrome.

Pregnancy and lactation:Contraindicated in pregnancy. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Single dose for children:

6-8 years: 5-10 mg;

8-15 years: 10-20 mg;

The highest daily intake for children: 100 mg.

Adults

Inside 50-200 mg 2-3 times a day, the dose is selected individually.

The highest daily dose: 450 mg.

The highest single dose: 200 mg.

Side effects:

Central and peripheral nervous system: drowsiness, depression, tardive dyskinesia.

The system of hematopoiesis: granulocytopenia, agranulocytosis, thrombocytopenia.

The cardiovascular system: tachycardia, hypotension, including orthostatic.

Digestive system: hypersalivation, increased appetite and body weight.

Musculoskeletal system: muscle weakness.

Sense organs: violation of accommodation.

Allergic reactions.

Overdose:

Areflexia, drowsiness, coma, convulsions, mydriasis, tachycardia, collapse, respiratory depression.

Treatment is symptomatic.

Interaction:

Potentiates the effect of MAO inhibitors and agents that depress the central nervous system: antihistamines, narcotic analgesics, benzodiazepine derivatives, ethanol.

With simultaneous administration of clozapine and drugs that have a high degree of binding to blood plasma proteins (eg, warfarin), it is possible to increase the blood content of a free fraction of any of the active substances, which can lead to side effects.

Special instructions:

Control of the composition of peripheral blood (agranulocytosis).

Patients receiving clozapine, it is not recommended to drive a car and work with moving machinery.

Instructions

Clozapine (Clozapinum)