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

Pharmacodynamics:Antipsychotic agent (neuroleptic), a derivative of bougirofenone. Has a pronounced antipsychotic effect, blocks postsynaptic dopamine receptors in the mesolimbic and mesocortical structures of the brain. High antipsychotic activity is combined with a moderate sedative effect (in small doses has an activating effect) and pronounced antiemetic effect. Causes extrapyramidal disorders, virtually no cholinoblocking effect.

Sedative action is due to blockade of alpha-adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action and galactorrhea - blockade of dopamine receptors of the hypothalamus.Prolonged reception is accompanied by a change in the endocrine status, in the anterior pituitary gland prolactin production increases and decreases - gonadotropic hormones.

Pharmacokinetics:The maximum concentration in the blood after intramuscular injection is reached after 20 minutes. Haloperidol 90% bound to plasma proteins, 10% is a free fraction. The ratio of concentration in erythrocytes to plasma concentration is 1:12. The concentration of haloperidol in tissues is higher than in blood, the drug tends to accumulate in tissues. Haloperidol metabolized in the liver, the metabolite is not active. Also haloperidol is subjected to oxidative N-dealkylation and glucuronation. The half-life from the plasma after intramuscular injection is 21 hours (17-25 h). Haloperidol It is excreted in the form of metabolites with caloric masses - 60% (including bile 15%) and urine 40%, (including 1% - unchanged). Easily penetrates through gistogematicheskie barriers: in t.ch. through placental and blood-brain, penetrates into breast milk.

Indications:Coping and treatment of psychotic disorders of different etiologies.Premedication before surgery.

Contraindications:Hypersensitivity, severe toxic oppression of the central nervous system and coma of any etiology; CNS diseases, accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease, etc.); hypersensitivity to butyrophenone derivatives; pregnancy, the period of breastfeeding; children up to 3 years.

Carefully:Decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disorders, prolongation of QT interval or predisposition to it - hypokaemia, simultaneous use of other drugs that can cause prolongation of the QT interval, epilepsy, angle-closure glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis), pulmonary-cardiac and respiratory failure (including COPD and acute infectious diseases), hyperplasia is present th gland with urinary retention, alcoholism.

Pregnancy and lactation:The drug is contraindicated.

Dosing and Administration:For relief of psychomotor agitation haloperidol in the early days, intramuscularly administered 2.5-5 mg 2-3 times a day, 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 solution), the maximum daily dose is 5 mg (1 ml solution).

For children older than 3 years, the dose is 0.025-0.05 mg per day, divided into 2 divided 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 a physician, especially in elderly patients and children; when the therapeutic effect is achieved, it is necessary to switch to taking the drug inside.

Side effects:From the nervous system: headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, akathisia, euphoria, depression, convulsive disorders, extrapyramidal disorders; with long-term treatment - tardive dyskinesia (smacking lips and lips, inflating cheeks, fast 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, uncontrollable bending movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle stiffness, shortness of breath, tachycardia, arrhythmia, increased or decreased blood pressure, increased sweating, incontinence urine, convulsive disorder, depression of consciousness).

From the cardiovascular system: when used in high doses - decreased blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (prolongation of the QT interval, 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.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

Other: alopecia, weight gain.

Overdose:In case of an overdose of the drug, the appearance of acute neuroleptic reactions, listed above, is possible.

Symptoms: rigidity of muscles, tremor, drowsiness, decrease, sometimes increase in blood pressure, in severe cases - coma, respiratory depression, shock, QT interval prolongation, arrhythmia. 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: In case of respiratory depression, artificial ventilation of the lungs may be required. With hypotension and collapse intravenously, to maintain blood circulation, plasma or concentrated albumin is injected, dopamine, or norepinephrine. Epinephrine in these cases it is strictly forbidden to apply, as it can provoke a pronounced hypotension! For relief of extrapyramidal symptoms, central holinoblokatory and antiparkinsonian drugs. Intravenously injected diazepam, glucose solution, nootropics, B and C vitamins. Dialysis is ineffective. There is no specific antidote.

Interaction:Increases the severity of the inhibitory effect on the CNS of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotic drugs, funds for general anesthesia.

Strengthens the action of peripheral m-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due to its displacement from alpha-adrenergic neurons and suppression of its capture by these neurons).

It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, while their (mutually) sedative effect and toxicity increase.

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

Reduces the effect of anticonvulsants (reducing the convulsive threshold with haloperidol).

Weaken the vasoconstrictive effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of alpha-adrenoreceptors by haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure).

Reduces the effect of antiparkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system). Changes (may increase or decrease) the effect of anticoagulants.

Reduces the effect of bromocriptine (dose adjustment may be required).

When used with methyldopa increases the risk of developing mental disorders (including disorientation in space, slowing and hindering thinking processes).

Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psycho-stimulating effect (haloperidol blockade of alpha-adrenergic receptors).

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).

Long-term administration of carbamazepine, barbiturates, etc.inducers of microsomal oxidation reduces the concentration of haloperidol in plasma.

In combination with lithium preparations (especially in high doses), the development of encephalopathy (can cause irreversible neurointoxication) and an increase in extrapyramidal symptoms.

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

With simultaneous use with drugs that cause extrapyramidal reactions, increases the frequency and severity of estropyramide disorders.

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

Special instructions:Parenteral administration should be carried out under the strict supervision of a physician, especially in the case of elderly and children. When the therapeutic effect is achieved, the oral form of treatment should be switched.

Because the haloperidol may cause prolongation of the QT interval, caution should be exercised if there is a risk of prolongation of QT (QT syndrome, hypokalemia, drugs causing prolongation of the QT interval), especially with parenteral administration.

In connection with the metabolism of haloperidol in the liver, it is important to exercise caution when prescribing it to patients with impaired hepatic function. During treatment, patients should regularly monitor ECG, blood formulas, "hepatic" samples.

There are cases of development of seizures caused by haloperidol. Patients with epilepsy and patients, in conditions predisposing to the development of convulsive syndrome (alcoholism, a history of brain trauma), the drug should be used with extreme caution.

For relief of extrapyramidal disorders, antiparkinsin agents (cyclodol, etc.), nootropics, vitamins are prescribed; their use continues after haloperidol withdrawal, if they are excreted from the body more quickly than haloperidol to avoid extrapyramidal symptoms.

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.

During reception of haloperidol it is forbidden to drink alcohol:

Effect on the ability to drive transp. cf. and fur:During the reception of haloperidol it is prohibited to drive vehicles, service mechanisms and perform other types of work requiring increased concentration of attention.

Form release / dosage:Solution for intramuscular injection 5 mg / ml.

Packaging:1 ml or 2 ml in ampoules. 5 ampoules per contour cell packaging made of polyvinylchloride film and aluminum foil or without foil. For 1 or 2 contour packs with a scarifier ampoule ceramic or knife for opening ampoules and instructions for use in a pack of cardboard.When using ampoules with a fracture ring or break point, the knife or scarifier is not inserted.

Storage conditions:Store at a temperature of 15 to 25 ° C in a dark place. Keep out of the reach of children.

Shelf life:2 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005199/09

Date of registration:29.06.2009 / 22.04.2015

Expiration Date:Unlimited

The owner of the registration certificate:BINNOFARM, CJSC BINNOFARM, CJSC Russia

Manufacturer: & nbsp

BINNOFARM, CJSC Russia

STATE FACTORY OF MEDICAL PREPARATIONS, FSUE Russia

Representation: & nbspBINNOFARM CJSC BINNOFARM CJSC Russia

Information update date: & nbsp14.03.2017

Illustrated instructions

Instructions

Haloperidol (Haloperidol)