Haloperidol, 5 mg/ml 1 ml 10 pcs

Pharmacotherapeutic group

Antipsychotic drug (neuroleptic)

ATX code: N05AD01

Pharmacodynamics:

Haloperidol is an antipsychotic (neuroleptic) butyrophenone derivative. It has a pronounced antipsychotic effect blocks postsynaptic dopamine receptors in mesolimbic and mesocortical structures of the brain. High antipsychotic activity is combined with a moderate sedative effect (in small doses it has an activating effect) and a pronounced antiemetic effect. It causes extrapyramidal disorders practically does not have m-cholinoblocking action.

Sedative action is caused by blockade of alpha-adrenoreceptors of reticular formation in brain stem; antiemetic action – by blockade of dopamine D2-receptors of trigger zone of vomiting center; hypothermic action and galactorrhea – by blockade of dopamine receptors of hypothalamus. Prolonged use is accompanied by changes in endocrine status in the anterior pituitary gland lobe; prolactin production increases and gonadotropic hormones production decreases.

Pharmacokinetics:

When administered intravenously the bioavailability is 100%. With intramuscular injection maximum concentration (Cmax) is reached in 20 minutes. Ratio
of concentration in erythrocytes to plasma concentration 1:12. Protein binding is approximately 92%. The concentration of haloperidol in tissues is higher than in blood The drug tends to cumulate in tissues. Easily penetrates through histohematic barriers including placental and blood-brain barriers and penetrates into breast milk.

Hapoperidol is metabolized in liver metabolite is not active. The CYPZase and/or CYP2D6 isoenzyme has been found to be involved in the metabolism of haloperidol. Haloperidol also undergoes oxidative N-dealkylation and glucuronidation. The plasma elimination half-life after intramuscular administration is 21 hours (17-25 hours). Haloperidol is excreted as metabolites in the feces – 60% (including 15% in the bile) and in the urine – 40% (including 1% unchanged).

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

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Side effects

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Pregnancy use

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