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

Excipients: potato starch - 40,0 / 99,4 mg, lactose monohydrate (milk sugar) - 75,6 / 188,4 mg, gelatin medical - 0,5 / 1,2 mg, talc - 1,2 / 3,0 mg , magnesium stearate - 1,2 / 3,0 mg.

Description:

Tablets from white to white with a slightly yellowish hue of color.

For dosages of 1.5 mg - flat-cylindrical shape, with a facet;

for dosages of 5 mg - flat-cylindrical shape, with a risk and chamfer.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.D.01 Haloperidol

Pharmacodynamics:

Haloperidol is a neuroleptic belonging to butyrofenone derivatives. Has a pronounced antipsychotic and antiemetic effect. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect).

The antipsychotic effect 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). Interaction with dopaminergic structures of the extrapyramidal system can lead to extrapyramidal disorders.The inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect.

Haloperidol enhances the effect of hypnotics, narcotic analgesics, agents for general anesthesia, analgesics and other drugs that depress the central nervous system (CNS).

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 90% bound to plasma proteins. 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;

- dlingering and resistant to hiccup therapy and vomiting, including those associated with antitumor therapy;

- 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.

Due to the presence of lactose (milk sugar) in the formulation, its administration is contraindicated in cases of congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

With decompensated cardiovascular diseases (including angina pectoris, intracardiac conduction disorders, lengthening of the interval Q-T or a predisposition to this - hypokalemia, simultaneous use of others.drugs (LS), which can cause lengthening of the interval Q-T); 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:

Assign inside, half an hour before meals (you can with milk to reduce the irritating effect on the mucous membrane of the stomach).

The initial daily dose is 0.5 to 5 mg, divided into 2-3 doses. Then the dose is gradually increased by 0.5-2 mg (in resistant cases by 2-4 mg), until the necessary therapeutic effect is achieved.

The maximum daily dose is 100 mg.

On average, the therapeutic dose is 10-15 mg / day, with chronic forms of schizophrenia 20-40 mg / day, in resistant cases to 50-60 mg / day.

The duration of treatment, on average, 2-3 months.

Supporting doses (outside the exacerbation) from 0.5 to 5 mg / day (the dose is reduced gradually).

Children 3-12 years (with a body weight of 15-40 kg) - 0.025-0.05 mg per kilogram of body weight per day 2-3 times a day, increasing the dose no more often than every 5-7 days, to a daily dose of 0 , 15 mg / kg.Older patients and weakened patients are prescribed 1 / 3-1 / 2 of the usual dose for adults, with its increase not more often than every 2-3 days.

As an antiemetic, appoint 1.5 mg.

For more accurate dosing, another dosage form of the drug, for example, drops for oral administration, may be required.

Side effects:

From the nervous system: extrapyramidal disorders of varying severity, parkinsonism, transient akineto-rigid syndrome, oculogic crises, headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, anxiety, psychomotor agitation, fear, akathisia, euphoria, depression, epileptic seizures, in rare cases, exacerbation of psychosis, incl. hallucinations; extrapyramidal disorders; long-term dyskinesia (lip smearing and puckering, cheeks inflating, rapid and wormlike movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the hands and feet), late dystonia (rapid blinking or spasms of the eyelids, unusual facial expression or body position,uncontrolled curving movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle rigidity, shortness of breath, tachycardia, arrhythmia, increased or decreased blood pressure, increased sweating, urinary incontinence, convulsive disorders, ).

From the cardiovascular system: when used in high doses - reduced blood pressure, orthostatic hypotension, arrhythmias, tachycardia, changes in the electrocardiogram (ECG) (lengthening interval Q-T, signs of flutter and fibrillation of the ventricles).

From the digestive system: when used in high doses - decreased appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, impaired liver function, until the development of jaundice.

On the part of the organs of hematopoiesis: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

From the genitourinary system: retention of urine (with hyperplasia of the prostate gland), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinaemia, violation of the menstrual cycle, decreased potency, increased libido, priapism.

From the sense organs: cataract, retinopathy, blurred vision.

Allergic reactions: maculopapular and acne-like skin changes, photosensitization, rarely - bronchospasm, laryngospasm.

From the skin: hyperfunction of the sebaceous glands.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia, increased activity of "hepatic" transaminases.

Other: alopecia, weight gain.

Overdose:

Symptoms: when 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.

Treatment: gastric lavage, Activated carbon. With respiratory depression - artificial ventilation. To improve blood circulation in / in, inject plasma or albumin solution, norepinephrine. Epinephrine in these cases, use is strictly prohibited! Reduction of extrapyramidal symptoms - central holinoblokatory and antiparkinsonian drugs. Dialysis is ineffective.

Interaction:

Haloperidol increases the severity of oppressive effects on the CNS of opioid analgesics, hypnotics, tricyclic antidepressants, agents 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 to its displacement from the α-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.

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 psychostimulant effect of amphetamines are reduced, due to the blockade of α-adrenergic receptors by haloperidol.

Haloperidol can reduce the effect of bromocriptine.

Anticholinergic, antihistamine (1st generation) and antiparkinsonian drugs can enhance the m-cholinoblock effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).

The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.

Special instructions:

During therapy, patients should regularly monitor the ECG, the blood formula, and "liver" tests.

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

With the development of tardive dyskinesia, it is recommended that the dose be gradually reduced (until the drug is completely discontinued).

Care must be taken when performing heavy physical work, taking a hot bath (it is possible to develop a heat stroke due to the suppression of central and peripheral thermoregulation in the hypothalamus).

During treatment, it is not necessary to take "anti-cold" OTC medicines (possibly intensifying anticholinergic effects and the risk of heat stroke).

Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.

Treatment is stopped gradually to avoid the occurrence of the "withdrawal" syndrome.

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

It was noted that doses for children 6 mg / day cause additional improvement in behavioral disorders and tics.

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

During the reception of haloperidol it is prohibited to drive vehicles, service mechanisms and other types of work requiring increased concentration of attention, as well as alcohol intake.

Form release / dosage:

Tablets, 1.5 mg and 5 mg.

Packaging:

10 tablets per contour cell pack.

By 1, 2, 3, 4, 5 contour mesh packages together with instructions for use in a pack of cardboard.

100 tablets per can of polymer.

For 500, 600, 1000, 1200 tablets in a can of polymer (for hospitals).

Each jar along with instructions for use in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003760 / 01

Date of registration:05.11.2009

Expiration Date:Unlimited

The owner of the registration certificate:ALSI Pharma, ZAO ALSI Pharma, ZAO Russia

Manufacturer: & nbsp

ALSI Pharma, ZAO Russia

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Haloperidol (Haloperidol)