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

Antipsychotic agent (neuroleptic), a derivative of butyrophenone. It 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 brain stem; antiemetic effect - blockade of dopamine D₂receptors of 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 if taken orally - 60%.The time to reach the maximum concentration (T_Сmах) for oral administration - 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 (BBB).

Metabolized in the liver, has the effect of "first pass" through the liver. In the metabolism of the drug, isozymes participate CYP2D6, CYP3A3, CYP3A5, CYP3A7. It is an inhibitor of CYP2D6. There are no active metabolites. The half-life (T_1/2) for oral administration - 24 h (12-37 h).

It is excreted with bile and urine: after ingestion with bile 15% are excreted, with 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;

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

- TGottington's chorea;

- Dvomiting, resistant to therapy, including those associated with antitumor therapy, and hiccups.

Contraindications:

- Hypersensitivity;

- severe oppression of central nervous system (CNS) function against xenobiotic intoxication, coma of various genesis;

- CNS diseases, accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease);

- pregnancy, lactation period;

- childhood (up to 12 years).

Carefully:

Decompensated diseases of the cardiovascular system (CVS) (including angina pectoris, intracardiac conduction disorders, lengthening of the interval Q-T or a predisposition to this - hypokalemia, the simultaneous use of other drugs (LS), which can cause lengthening of the interval Q-T), epilepsy and convulsive conditions in anamnesis, closed-angle glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis), pulmonary-cardiac and respiratory failure (including COPD and acute infectious diseases), prostatic hyperplasia with a delay in urine , alcoholism.

Pregnancy and lactation:

Contraindicated.

Dosing and Administration:

Inside, during or after a meal, with a full (240 ml) glass of water or milk, the initial dose for adults is 0.5-5 mg 2-3 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). The maximum dose is 100 mg / day.

The duration of treatment is 2 to 3 months.

Reduce the dose slowly, maintenance doses - 5-10 mg / day.

Elderly or weakened patients at the beginning of treatment appoint inwards for 0.5-2 mg 2-3 times a day.

If there is no effect within 1 month, treatment should not be continued.

Side effects:

From the nervous system: headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, anxiety, psychomotorarousal, 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, ).

On the part of the CAS: when used in high doses - reduced blood pressure, orthostatic hypotension, arrhythmias, tachycardia, changes in 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.

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, 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, photosensitivity; rarely - bronchospasm, laryngospasm.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

Other: alopecia, weight gain.

Overdose:

Symptoms: oppression of consciousness, rigidity of muscles, tremor, drowsiness, lowering blood pressure, sometimes - raising blood pressure. In severe cases - coma, respiratory depression, shock.

Treatment: when ingested - gastric lavage, Activated carbon.

With respiratory depression - IVL. 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:

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 antihypertensive drugs(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-adrenoreceptors).

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 oxidation reduces the concentration of haloperidol in plasma.

In combination with drugs Li+ (especially in high doses), the development of encephalopathy (may cause irreversible neurointoxication) and increased 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:

During therapy, patients should regularly monitor the ECG, 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, 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 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, 1.5 mg and 5.0 mg.

Packaging:

10 tablets per contour cell pack.

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

For hospitals. For 100, 500 and 1000 tablets in a polymer bottle with a screw cap, equipped with the protection of the first dissection in the form of a ring.

1 bottle 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:LSR-010213/08

Date of registration:15.12.2008

Expiration Date:Unlimited

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

Manufacturer: & nbsp

BIOKOM, CJSC Russia

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Haloperidol (Haloperidol)