Haloperidol - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Haloperidol neuroleptic, butyrophenone derivative. Has antiemetic and pronounced antipsychotic effect. The effect of the drug is associated with blockade of central dopamine (D₂) and a-adrenergic receptors in the mesocortical and limbic structures of the brain. Blockade D₂- receptors of the hypothalamus leads to a decrease in body temperature, galactorrhea (increased production of prolactin). The antiemetic effect is based on oppression of dopamine receptors in the trigger zone of the vomiting center. Interaction with dopaminergic structures of the extrapyramidal system can lead to extrapyramidal disorders. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect). Strengthens the effect of hypnotics, narcotic analgesics, means for general anesthesia, analgesics and other drugs that depress the function of the central nervous system.

Pharmacokinetics:Bioavailability is 70%. V_d - 18 l / kg. The connection with plasma proteins is 92%. Biotransformation in the liver. Half-life with oral administration - 24 hours (12-37 hours), intramuscular injection - 21 hours (17-25 hours), intravenous administration - 14 hours (10-19 hours), haloperidol decanoate - 3 weeks. Clearance - 12 ml / min.Elimination by the kidneys (40%, 1% unchanged) and faeces (15%). The effect of presystemic elimination is characteristic.

Indications:- acute and chronic psychoses accompanied by excitement, hallucinatory and delusional disorders, manic conditions, psychosomatic disorders;

- behavioral disorders, personality changes (paranoid, schizoid, and others), Gilles de la Tourette's syndrome, both in childhood and adults;

- ticks, Huntington's chorea;

- long-lasting and resistant to therapy hiccups and vomiting, including those associated with antitumor therapy;

- Premedication before surgery.

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F22.0 Delusional Disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F30-F39.F30 Manic episode

V.F40-F48.F45 Somatoform disorders

V.F60-F69.F60.2 Dissocial personality disorder

V.F70-F79.F79 Mental retardation, unspecified

V.F90-F98.F91 Behavioral disorders

V.F90-F98.F95.2 Combining vocalisms and multiple motor tics [de la Tourette's syndrome]

V.F90-F98.F98.5 Stuttering [stammering]

VI.G10-G13.G10 Huntington's disease

XVIII.R10-R19.R11 Nausea and vomiting

XVIII.R40-R46.R44.3 Other hallucinations

Contraindications:Hypersensitivity, CNS diseases, accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease), depression, hysteria, coma of various etiologies, pregnancy, breast-feeding, age of up to 3 years (for parenteral use).

Carefully:Diseases of the cardiovascular system (in the stage of decompensation), impaired conduction of the heart muscle, epilepsy, zakratougolnaya glaucoma, hepatic and / or renal failure, hyperthyroidism, thyrotoxicosis, pulmonary heart disease, prostate hyperplasia, alcoholism.

Pregnancy and lactation:Recommendations FDA category C. When used during pregnancy - developmental disorders of limbs, teratogenic effects. When administered to animals at doses 2-20 times higher than the maximum daily doses for a person, a decrease in fertility is established. When administered to mice at doses 15 times higher than the maximum daily doses for humans, it is possible to develop cleft palate (wolf mouth). Do not apply!

Lactation. Do not apply. Drowsiness, extrapyramidal disorders in newborns was recorded.

Dosing and Administration:Inside (30 minutes after eating) for 0.5-5 mg 2-3 times a day with a gradual increase to 10-15 mg; with chronic forms of schizophrenia - up to 20-60 mg. Duration of treatment - 2-3 months.

Reduce the dose slowly, maintenance doses - 5-10 mg per day. The average single dose for intramuscular injection is 2-5 mg, the interval between administrations is 4-8 hours. The maximum dose is 100 mg per day. The maximum daily intake for adults is 30-40 mg (orally). Elderly or weakened patients - 0.5-1.5 mg per day. In chronic forms of schizophrenia - up to 20-60 mg.

With indomitable vomiting - 2 mg 2 times a day. If there is no clinical effect within 1 month, treatment should not be continued. In acute conditions and in cases when ingestion is impossible - intravenously or intramuscularly. With acute alcoholic psychosis - intravenously in a dose of 5-10 mg, with inefficiency - an additional infusion in a dose of 10-20 mg with a speed of not more than 10 mg / min.

Solution for injection containing haloperidol decanoate - strictly intramuscular by 25 mg every 15-30 days; if necessary, increase the dose to 100-150 mg.

Use in children

Psychoses: 3-12 years - 12,5-25 mkg / kg 2 times a day; the maximum daily dose is 10 mg.12-18 years - 0.5-3 mg 3 times a day. With resistant schizophrenia - 30 mg per day, maintenance therapy - 5-10 mg per day.

Psychomotor agitation of different etiology: 3-12 years - 12,5-25 mkg / kg 2 times a day; the maximum daily dose is 10 mg. 12-18 years - 0.5-3 mg 3 times a day.

Gilles de La Tourette syndrome: 3-12 years - 12.5-25 mcg / kg twice a day; the maximum daily dose is 10 mg. 12-18 years - 0.5-3 mg 3 times a day.

Violation of behavior in children's age (including hyperreactivity, autism): 3-12 years - 12.5-25 μg / kg 2 times a day; the maximum daily dose is 10 mg. 12-18 years - 0.5-3 mg 3 times a day.

Side effects:

Movement disorders: akathisia (6 hours after taking the drug), dystonic extrapyramidal effects (most often in young people, at the beginning of treatment), parkinsonian extrapyramidal effects (more often in the elderly, both with long-term, and with a single application), persistent late dyskinesia.

Orthostatic hypotension.

Hallucinations.

Neuroleptic malignant syndrome (there is no proven connection between fatal cases with the use of haloperidol).

Heat stroke, obstructive jaundice, anticholinergic effect, thirst, unusual fatigue, allergic reactions.

Agranulocytosis.

Overdose:

Symptoms: difficulty breathing, trembling, muscle twitching, muscle stiffness or uncontrolled movements, coma.

Treatment symptomatic. With respiratory depression - artificial ventilation. To maintain blood pressure - intravenous injection of plasma (albumin solution), norepinephrine. Epinephrine in these cases, use is strictly prohibited!

Interaction:

Alcohol and other drugs that cause CNS depression - increased oppression of the central nervous system, respiration and hypotensive effect.

Means that cause extrapyramidal reactions (metoclopramide) - increased severity and frequency of extrapyramidal effects.

Epinephrine - blocking α-adrenoreceptors and lowering blood pressure.

Special instructions:In severe violations of kidney function, the dose of the drug should be reduced.

At the time of taking the drug, it is prohibited to drive vehicles, service mechanisms and perform other types of work that require a high concentration of attention, as well as alcohol intake.

Instructions

Haloperidol (Haloperidolum)