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

The action of haloperidol is associated with blockade of central dopamine (D₂) and α-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 inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect. 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 analgetics, means for general anesthesia, analgesics and other means of suppressing the function of the central nervous system.

Pharmacokinetics:

Haloperidol is absorbed, mainly in the small intestine, by passive diffusion. Bioavailability of 60-70%. When administered orally, the maximum concentration in the blood is reached after 3-6 hours.

Haloperidol binds to plasma proteins by 90%. The ratio of concentration in erythrocytes to plasma concentration is 1:12. The concentration of haloperidol in the tissues is higher than in the blood.

Haloperidol is metabolized in the liver, the metabolite is not pharmacologically active.

Haloperidol is excreted by the kidneys (40%) and with feces (60%), it penetrates into breast milk. The half-life from plasma after oral administration is an average of 24 hours (12-37 hours).

Indications:

The drug is used strictly according to the doctor's prescription.

- Acute and chronic psychoses accompanied by excitement, hallucinatory and delusional disorders, manic conditions, psychosomatic disorders;

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

- tGottington's chorea;

- dresistant to hiccough therapy and vomiting, including those associated with antitumor therapy4

- premedication before surgery.

Contraindications:

- Severe toxic oppression of the CNS function caused by xenobiotics, coma of various genesis;

- zCNS abnormalities, accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease, etc.);

- Pan increased sensitivity to butyrophenone derivatives;

- bVariability, the period of breastfeeding;

- dUp to 3 years old.

Carefully:Care should be taken with uncompensated cardiovascular diseases (including angina pectoris), impaired conduction of the heart muscle; with severe diseases of the kidneys, liver, pulmonary heart disease (including bronchial asthma and acute infections), epilepsy, zakratougolnoy glaucoma, hyperthyroidism (thyrotoxicosis), prostatic hyperplasia (urinary retention), active alcoholism.

Dosing and Administration:

For relief of psychomotor agitation HALOPERIDOL in the early days, intramuscularly prescribed 2-5 mg 2-3 times a day, or intravenously in the same dosage (the ampoule should be diluted in 10-15 ml of water for injection), the maximum daily dose of 60 mg.After achieving a stable sedative effect, they switch to taking the drug inside.

For elderly patients 0.5-1.5 mg (0.1-0.3 ml of solution), the maximum daily dose is 5 mg (1 ml of solution).

For children older than 3 years, the dose is 0.025-0.05 mg per day, divided by 2 doses. The maximum daily dose is 0.15 mg / kg.

The parenteral route of administration of HALOPERIDOL should be performed under the close supervision of the physician, especially in elderly patients and children, when the therapeutic effect is achieved, the preparation should be taken orally.

Side effects:

CNS: extrapyramidal disorders of varying severity, parkinsonism. Most patients have transient akineto-rigid syndrome, oculogic crises, akathisia, dystonic phenomena.

Perhaps the development of neuroleptic malignant syndrome (NZS), one of the first signs of which is an increase in body temperature, drowsiness.

With long-term administration of haloperidol, it is possible to develop late dyskinesias, especially in elderly patients and patients with organic deficiency of the central nervous system, so doses for this category of patients should be reduced.

At the beginning of therapy, there may be lethargy, drowsiness or insomnia, headaches that occur after the appointment of correctors.

The cardiovascular system: arrhythmias, tachycardia, orthostatic hypotension, lability of arterial pressure, changes in the ECG.

Blood: transient leukopenia or leukocytosis, erythropenia, lymphomonocytosis. rarely - agranulocytosis.

Liver: increased activity of "liver" transaminases. jaundice.

Leather: allergic reactions, rash, toxicodermia, dry skin, photosensitivity, hyperfunction of the sebaceous glands.

GIT: anorexia, dyspepsia, dry mouth, sometimes hypersalivation, nausea, vomiting, constipation, diarrhea.

Endocrine system: dysmenorrhea, frigidity, gynecomastia, galactorrhea, impotence, priapism, weight gain.

Other: urine retention, blurred vision, increased fatigue, decreased thirst, heat stroke, alopecia, hyponatremia, hyper- or hypoglycemia.

Overdose:

In case of an overdose of the drug, the appearance of acute neuroleptic reactions, listed above, is possible. Particularly should alarm the increase in body temperature, which may be one of the symptoms of malignant neuroleptic syndrome.In severe cases of overdose, various forms of impaired consciousness can be observed, including coma, convulsive reactions.

Measures of assistance: cessation of therapy with neuroleptics, appointment of correctors. intravenous diazepam, glucose solution, nootropics, B and C vitamins, symptomatic therapy.

Interaction:

Haloperidol increases the severity of oppressive effects on the central nervous system, opioid analgesics, hypnotics, tricyclic antidepressants, funds for general anesthesia, alcohol.

With simultaneous use with antiparkinsonian drugs (levodopa and others), the therapeutic effect of these agents may decrease because of the antagonistic effect on the dopaminergic structures.

When used with methyldopa, development of disorientation, difficulty and slowing down of thinking processes is possible.

Haloperidol can reduce the intensity of action of epinephrine (epinephrine) and other sympathomimetics, cause a "paradoxical" reduction in arterial pressure and tachycardia when combined.

Strengthens the action of peripheral M-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due todisplacement of it from a-adrenergic neurons and suppression of its capture by these neurons).

When combined with anticonvulsants (including barbiturates and other inducers of microsomal oxidation), the doses of the latter should be increased, haloperidol reduces the threshold of convulsive activity; serum concentrations of haloperidol may also decrease. In particular, with the simultaneous use of tea or coffee, the effect of haloperidol may decrease.

Haloperidol can reduce the effect of indirect anticoagulants, so when combined, the dose of the latter should be adjusted.

Haloperidol slows the metabolism of tricyclic antidepressants and MAO inhibitors, which increases their plasma levels and increases toxicity.

With simultaneous use with bupropion reduces the epileptic threshold and increases the risk of epileptic seizures.

With the simultaneous administration of haloperidol with fluoxetine, the risk of side effects on the central nervous system increases, especially extrapyramidal reactions.

With the simultaneous administration of haloperidol with lithium, especially in high doses, it can cause irreversible neurointoxication, as well as intensify extrapyramidal symptoms.

With simultaneous reception with amphetamines, the antipsychotic effect of haloperidol and the psychostimulatory effect of amphetamines are reduced, owing to the blockade of haloperidol α-adrenergic receptors.

Haloperidol can reduce the action of bromocriptine.

Anticholinergic, antihistamine (1 generation), antidiskinetic drugs can enhance anticholinergic side effects and reduce the antipsychotic effect of haloperidol.

Special instructions:

During treatment, patients should regularly monitor ECG, blood formulas, hepatic samples.

For relief of extrapyramidal disorders, antiparkinsonian agents (cyclodol, etc.), nootropics, vitamins are prescribed.

The severity of extrapyramidal disorders is associated with a dose, often with a decrease in dose they may decrease or disappear.

In a number of cases, signs of neurological disorders are observed when the drug is withdrawn after a long course of treatment, therefore, it should be canceled haloperidol gradually reducing the dose.

With the development of tardive dyskinesia should not abruptly cancel the drug; a gradual dose reduction is recommended.

It is necessary to protect the exposed areas of the skin from excessive sunlight due to the increased risk of photosensitization.

The antiemetic effect of haloperidol can mask the signs of drug toxicity and make it difficult to diagnose conditions, the first symptom of which is nausea.

Effect on the ability to drive transp. cf. and fur:

During the reception, haloperidol prohibited from driving vehicles, machinery maintenance and other work requiring high concentration, as well as reception of alcohol.

Form release / dosage:RAsterol for intravenous and intramuscular administration, 5 mg / ml.

Packaging:

To 1 ml ampoules made of amber glass (glass type I, European Pharmacopoeia) with two rings and a refractive coding point.

10 ampoules in a contour squamous package.

2 contour squares in a cardboard box with instructions for use.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Shelf life:

5 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014639 / 01

Date of registration:13.08.2010

Expiration Date:Unlimited

The owner of the registration certificate:Biocanol Farma GmbHBiocanol Farma GmbH Germany

Manufacturer: & nbsp

WEIMER PHARMA, GmbH Germany

Representation: & nbspSVYCH LLC SVYCH LLC Russia

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Haloperidol (Haloperidol)