Haloperidol, tablets 1.5 mg 50 pcs

Haloperidol

Indications

Acute and chronic psychotic disorders (including schizophrenia, manic-depressive, epileptic, alcoholic psychoses), psychomotor agitation of various origins, delusions and hallucinations of various origins, Huntington’s chorea, mental retardation, agitated depression, behavioral disorders in old age and childhood (including hyperactivity in children and childhood autism), psychosomatic disorders, illness Tourette’s, stuttering, long-term and treatment-resistant vomiting and hiccups, prevention and treatment of nausea and vomiting during chemotherapy.

Pharmacological effect

Pharmacotherapeutic group: Psycholeptics, antipsychotics, butyrophenone derivatives

Pharmacological action

Antipsychotic drug (neuroleptic), butyrophenone derivative. It has a pronounced antipsychotic effect due to the blockade of depolarization or a decrease in the degree of excitation of dopamine neurons (reduced release) and blockade of postsynaptic dopamine D2 receptors in the mesolimbic and mesocortical structures of the brain.

It has a moderate sedative effect due to the blockade of α-adrenergic receptors of the reticular formation of the brain stem; pronounced antiemetic effect due to blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect and galactorrhea caused by blockade of dopamine receptors of the hypothalamus.

Long-term use is accompanied by changes in endocrine status; in the anterior lobe of the pituitary gland, the production of prolactin increases and the production of gonadotropic hormones decreases.

Blockade of dopamine receptors in the dopamine pathways of the substantia nigra striata promotes the development of extrapyramidal motor reactions; blockade of dopamine receptors in the tuberoinfundibular system causes a decrease in the release of GH.

It has virtually no anticholinergic effect.

Eliminates persistent personality changes, delusions, hallucinations, mania, and increases interest in the environment. Effective in patients resistant to other antipsychotics. Has some activating effect. In hyperactive children, it eliminates excessive motor activity and behavioral disorders (impulsivity, difficulty concentrating, aggressiveness).

Unlike haloperidol, haloperidol decanoate is characterized by a prolonged action.

Pharmacokinetics

When taken orally, it is absorbed from the gastrointestinal tract by 60%. Cmax in plasma when taken orally is achieved after 3-6 hours, with intramuscular administration – after 10-20 minutes, with intramuscular administration of haloperidol decanoate – 3-9 days. Subject to first pass effect through the liver.

Protein binding is 92%. Vd at equilibrium concentration is 18 l/kg. Actively metabolized in the liver with the participation of isoenzymes CYP2D6, CYP3A3, CYP3A5, CYP3A7. It is an inhibitor of the CYP2D6 isoenzyme. There are no active metabolites.

Easily penetrates histohematic barriers, including the BBB. Excreted in breast milk.

T1/2 when administered orally – 24 hours, with intramuscular administration – 21 hours, with intravenous administration – 14 hours. Haloperidol decanoate is excreted within 3 weeks.

Excreted by the kidneys – 40% and with bile through the intestines – 15%.

Special instructions

Parenteral use in children is not recommended.

Use with caution in cardiovascular diseases with symptoms of decompensation, myocardial conduction disorders, an increase in the QT interval or the risk of an increase in the QT interval (including hypokalemia, simultaneous use with drugs that can increase the QT interval); for epilepsy; angle-closure glaucoma; liver and/or kidney failure; with thyrotoxicosis; pulmonary-cardiac and respiratory failure (including with COPD and acute infectious diseases); with prostatic hyperplasia with urinary retention; for chronic alcoholism; simultaneously with anticoagulants.

If tardive dyskinesia develops, it is necessary to gradually reduce the dose of haloperidol and prescribe another drug.

There are reports of the possibility of symptoms of diabetes insipidus, exacerbation of glaucoma, and a tendency (with long-term treatment) to the development of lymphomonocytosis during haloperidol therapy.

Elderly patients usually require a lower initial dose and a more gradual dose titration. This group of patients is characterized by a high probability of developing extrapyramidal disorders. Close monitoring of the patient is recommended to detect early signs of tardive dyskinesia.

During treatment with antipsychotics, the development of NMS is possible at any time, but most often it occurs soon after the start of therapy or after transferring a patient from one antipsychotic drug to another, during combination treatment with another psychotropic drug, or after increasing the dose.

Avoid drinking alcohol during treatment.

Impact on the ability to drive vehicles and machinery

During the period of use of haloperidol, you should refrain from engaging in potentially hazardous activities that require increased attention and high speed of psychomotor reactions.

Active ingredient

Haloperidol

Composition

Active substance: haloperidol

Excipients: lactose monohydrate (milk sugar) – 76.5 mg, corn starch – 6 mg, povidone K17 – 3.3 mg, microcrystalline cellulose – 10 mg, magnesium stearate – 0.7 mg, pregelatinized starch – 2 mg.

Pregnancy

Haloperidol is contraindicated during pregnancy and lactation.

In experimental studies, teratogenic and fetotoxic effects were found in a number of cases. Haloperidol is excreted in breast milk. Concentrations of haloperidol in breast milk have been shown to be sufficient to cause sedation and impaired motor function in the infant.

Contraindications

Diseases of the central nervous system, accompanied by symptoms of extrapyramidal disorders, depression, hysteria, coma of various etiologies; severe toxic depression of the central nervous system caused by drugs. Pregnancy, lactation. Children under 3 years of age. Hypersensitivity to haloperidol and other butyrophenone derivatives.

Side Effects

From the central nervous system: headache, insomnia, anxiety, feelings of anxiety and fear, euphoria, agitation, drowsiness (especially at the beginning of treatment), akathisia, depression or euphoria, lethargy, epileptic attack, development of a paradoxical reaction (exacerbation of psychosis, hallucinations); with long-term treatment – extrapyramidal disorders (including tardive dyskinesia, tardive dystonia and NMS).

From the cardiovascular system: when used in high doses – arterial hypotension, tachycardia, arrhythmia, ECG changes (increased QT interval, signs of flutter and ventricular fibrillation).

From the digestive system: when used in high doses – loss of appetite, dry mouth, hyposalivation, nausea, vomiting, constipation or diarrhea, liver dysfunction, including the development of jaundice.

From the hematopoietic system: rarely – mild and temporary leukopenia, leukocytosis, agranulocytosis, slight erythropenia and a tendency to monocytosis.

From the endocrine system: gynecomastia, pain in the mammary glands, hyperprolactinemia, menstrual irregularities, decreased potency, increased libido, priapism.

Metabolism: hyper- and hypoglycemia, hyponatremia; increased sweating, peripheral edema, weight gain.

From the organ of vision: impaired visual acuity, cataracts, retinopathy, accommodation disorders.

Allergic reactions: rarely – skin rash, bronchospasm, laryngospasm, hyperpyrexia.

Dermatological reactions: maculopapular and acne-like skin changes; rarely – photosensitivity, alopecia.

Effects due to cholinergic action: dry mouth, hyposalivation, urinary retention, constipation.

Interaction

When used simultaneously with drugs that have a depressant effect on the central nervous system, ethanol may increase central nervous system depression, respiratory depression and hypotensive effects.

With the simultaneous use of drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal effects is possible.

With the simultaneous use of drugs with anticholinergic activity, the anticholinergic effects may be enhanced.

When used simultaneously with anticonvulsants, it is possible to change the type and/or frequency of epileptiform seizures, as well as reduce the concentration of haloperidol in the blood plasma; with tricyclic antidepressants (including desipramine) – the metabolism of tricyclic antidepressants decreases, the risk of developing seizures increases.

When used simultaneously, haloperidol potentiates the effect of antihypertensive drugs.

When used simultaneously with beta-blockers (including propranolol), severe arterial hypotension is possible. With the simultaneous use of haloperidol and propranolol, a case of severe arterial hypotension and cardiac arrest has been described.

With simultaneous use, a decrease in the effect of indirect anticoagulants is observed.

When used simultaneously with lithium salts, the development of more pronounced extrapyramidal symptoms is possible due to increased blockade of dopamine receptors, and when used in high doses, irreversible intoxication and severe encephalopathy are possible.

When used simultaneously with venlafaxine, it is possible to increase the concentration of haloperidol in the blood plasma; with guanethidine – it is possible to reduce the hypotensive effect of guanethidine; with isoniazid – there are reports of increased concentrations of isoniazid in the blood plasma; with imipenem – there are reports of transient arterial hypertension.

When used simultaneously with indomethacin, drowsiness and confusion may occur.

When used simultaneously with carbamazepine, which is an inducer of microsomal liver enzymes, it is possible to increase the rate of metabolism of haloperidol. Haloperidol may increase plasma concentrations of carbamazepine. Symptoms of neurotoxicity may occur.

With simultaneous use, the therapeutic effect of levodopa and pergolide may be reduced due to blockade of dopamine receptors by haloperidol.

When used simultaneously with methyldopa, sedation, depression, dementia, confusion, and dizziness are possible; with morphine – myoclonus may develop; with rifampicin, phenytoin, phenobarbital – a decrease in the concentration of haloperidol in the blood plasma is possible.

When used concomitantly with fluvoxamine, there are limited reports of a possible increase in the concentration of haloperidol in the blood plasma, which is accompanied by toxic effects.

When used simultaneously with fluoxetine, the development of extrapyramidal symptoms and dystonia is possible; with quinidine – an increase in the concentration of haloperidol in the blood plasma; with cisapride – prolongation of the QT interval on the ECG.

When used simultaneously with epinephrine, it is possible to “pervert” the pressor effect of epinephrine, and as a result of this, the development of severe arterial hypotension and tachycardia.

Manufacturer

Ozon, Russia