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

Excipients: lactose monohydrate (sugar milk) - 93.9 mg, potato starch - 21.0 mg, silicon dioxide colloidal brand A-300 or A-380 - 1.2 mg, talc - 1.2 mg, magnesium stearate - 1.2 mg .

Description:Tablets are white or white with a slightly yellowish hue of a flat-cylindrical shape.

Pharmacotherapeutic group:Antipsychotic (antipsychotic) remedy

ATX: & nbsp

N.05.A.D.01 Haloperidol

Pharmacodynamics:Antipsychotic agent (neuroleptic), a derivative of butyrophenone. Has a pronounced antipsychotic effect, a sedative effect, (in small doses has an activating effect) and a 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 brainstem, 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:Absorption of 60%. The time of maximum concentration with oral intake is 3 hours. The volume of distribution is -18 l / kg, the connection with plasma proteins is 92%. Easily passes through the histohematological barriers, including the blood-brain barrier.

Metabolized in the liver, has the effect of "first pass" through the liver. In the metabolism of the drug, isoenzymes CYP2D6, CYRZAZ, CYPZA5, CYPZA7 are involved. It is an inhibitor of CYP2D6. There are no active metabolites. The half-life is 24 hours (12-37 hours). It is excreted with bile - 15% and urine - 40% (including 1% - unchanged). Penetrates into breast milk.

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 Tourette's syndrome, both in childhood and adults.

- Tiki, Gentingon's chorea.

- Long-lasting and resistant to therapy vomiting, including associated with antitumor therapy, and hiccups.

Contraindications:Hypersensitivity, severe inhibition of central nervous system function against xenobiotic intoxication, coma of various genesis, central nervous system diseases, accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease), lactase deficiency, lactose intolerance, glucosogalactose malabsorption, pregnancy, lactation , children's age (up to 3 years).

Carefully:Decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disturbances, prolongation of the QT interval or a predisposition to this hypokalemia, concomitant use of other drugs that can induce prolongation of the QT interval), epilepsy and convulsions in the anamnesis, closed-angle glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis phenomena), pulmonary-cardiac and respiratory failure (including chronic obstructive th lung disease and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Pregnancy and lactation:Contraindicated in lactation.

Dosing and Administration:

Dosing and Administration Inside, 30 minutes after meals, the initial dose for adults 0.5-5 mg 2-Z times a day. If necessary, the dose is gradually increased to achieve the desired therapeutic effect (on average - up 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 of 5-10 mg / day.

Elderly or weakened patients at the beginning of treatment appoint 0.5-1.5 mg / day.

Children under 5 years of age - 0.5-1 mg / day, 6-15 years - 1-2 mg / day.

In the absence of clinical effect for 1 month. treatment is not recommended.

To achieve optimal doses, it is advisable to use other dosage forms.

Side effects:From the nervous system: 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; 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 hands and feet),late dystonia (rapid blinking or spasms of the eyelids, unusual facial expression or position of the body, uncontrolled curving movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle stiffness, difficulty or rapid breathing, tachycardia, arrhythmia, pressure, increased sweating, urinary incontinence, convulsive disorders, depression of consciousness).

From the cardiovascular system: when used in high doses - lowering blood pressure, orthostatic hypotension, arrhythmia, tachycardia, changes in the electrocardiogram (prolongation of the Q-T 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.

From the 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, hyperprolakinemia, 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:Symptoms: oppression of consciousness, rigidity of muscles, tremor, drowsiness, lowering of arterial pressure, sometimes increase - of arterial pressure. In severe cases, coma, respiratory depression, shock. Treatment: gastric lavage, Activated carbon. With respiratory depression - artificial ventilation. To improve blood circulation, intravenously injected plasma or albumin solution, norepinephrine. EPinephrine in these cases is strictly prohibited! Reduction of extrapyramidal symptoms - central holinoblokatory and antiparkinsonian drugs. Dialysis is ineffective.

Interaction:Increases the severity of the inhibitory effect on the central nervous system of ethanol, three cyclic antidepressants, opioid analgesics, barbiturates and hypnotics, 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 monoamine oxidase inhibitors, thus increasing (mutually) their sedative effect and toxicity.

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 agents (antagonistic effect on the dopaminergic structure 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, and other inducers of microsomal oxidase enzymes 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 ectrapiramid reactions, increases the incidence and severity of extrapyramidal disorders.

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 electrocardiogram, the blood formula, and "liver" tests.

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, do not take "cold" non-prescription drugs (possibly increasing the anticholinergic effects and the risk of heat stroke).

Protect exposed skin from excessive sunlight due to increased riskphotosensitization.

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.

When mixing a concentrated solution of haloperidol for ingestion with coffee, tea is free haloperidol may precipitate.

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 treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 1.5 mg.

Packaging:

10 tablets per cell loop packaging made of polyvinylchloride film and aluminum foil printed lacquered; 50 tablets in a jar of lightproof glass.

5 contour packs or a bank together with instructions for medical use in a pack of cardboard box.

Storage conditions:Store in a dark place at a temperature of no more than 30 ° C.

Keep out of the reach of children.

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:LS-000645

Date of registration:24.08.2010 / 18.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp14.03.2017

Illustrated instructions

Instructions

Haloperidol (Haloperidol)