Haloperidol decanoate ampoules 50mg 1ml №5

Solution for i / m injection (oil) transparent, yellow or greenish yellow.

Excipients:benzyl alcohol, sesame oil.

1 ml - ampoules of dark glass (5) - plastic planimetric packagings (1) - packs cardboard.

Antipsychotic drug (neuroleptic)

• rr d / in / m introduction (oil) 50 mg / 1 ml: amp. 5 - P N015065 / 01, May 13, 2009. Validity reg. beats. is not limited.VED. DLO.

• Mechanism of action

  Haloperidol decanoate is an ester of haloperidol and decanoic acid. When i / m administration during slow hydrolysis, haloperidol is released, which then enters the systemic circulation.Haloperidol decanoate refers to the neuroleptic-derived butyrophenone. Haloperidol is a pronounced antagonist of central dopamine receptors and is considered a strong neuroleptic.

  Haloperidol is highly effective in treating hallucinations and delusions, due to the direct blockade of central dopamine receptors (probably acting on mesocortical and limbic structures), affects the basal ganglions (nigrostrium). It has a pronounced sedative effect in case of psychomotor agitation, is effective in mania and other agitations.

  The limbic activity of the drug is manifested in a sedative effect, effective as an additional remedy for chronic pain.

  Impact on the basal ganglions causes extrapyramidal reactions (dystonia, akathisia, parkinsonism).

  In socially isolated patients, social behavior is normalized.

  Severe peripheral anti-dopamine activity is accompanied by the development of nausea and vomiting (irritation of chemoreceptors), relaxation of the gastroduodenal sphincter and increased release of prolactin (blocks prolactin inhibitory factor in the adenohypophysis).

  Pharmacokinetics

  C_maxhaloperidol, released from the depot of haloperidol after the / m injection, is achieved in 3-9 days. T_1/2 about 3 weeks With regular monthly administration, the plasma saturation stage is reached in 2-4 months. Pharmacokinetics with a / in the introduction of a dose-dependent nature. At doses below 450 mg, there is a direct relationship between the dose and the plasma concentration of haloperidol. To achieve a therapeutic effect, a plasma concentration of haloperidol of 20–25 mcg / L is necessary. Haloperidol easily penetrates the blood-brain barrier. Communication with plasma proteins - 92%. Excreted through the intestines (60%) and the kidneys (40%, including 1% unchanged).

  Indications for use of the drug GALOPERIDOL DECANOAT

  - chronic schizophrenia and other psychosis, especially when treatment with quick-acting haloperidol was effective and requires an effective neuroleptic of moderately sedative action;

  - other disorders of mental activity and behavior, proceeding with psychomotor agitation and requiring long-term treatment.