Haloperidol
Haloperidol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Haloperidol
ATX code: N05AD01
Active ingredient: haloperidol (haloperidol)
Manufacturer: Gedeon Richter (Hungary), Moskhimpharmpreparaty them. N. A. Semashko (Russia)
Description and photo update: 2019-16-08
Prices in pharmacies: from 19 rubles.
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Haloperidol is an antiemetic, neuroleptic and antipsychotic drug.
Release form and composition
Dosage forms of Haloperidol:
- Solution for intravenous and intramuscular administration of 5 mg / ml (in 1 ml ampoules, in contour plastic packaging (pallets) of 5 pcs., 1, 2 pallets in a cardboard box; in 1 ml ampoules, in blisters of 10 pcs.., 1 package in a cardboard box);
- Solution for intramuscular injection of 5 mg / ml (in 1 ml ampoules with an ampoule knife, 10 pcs. In a cardboard box; in 1 ml and 2 ml ampoules, in blisters 5 pcs., 1, 2 packs in cardboard box; in 2 ml ampoules, in contour plastic packages (pallets), 5 pcs., 1, 2 pallets in a cardboard box);
- Tablets: 1 mg (in vials of 40 pcs., 1 bottle in a cardboard box; in blisters of 10 pcs., 3 blisters in a cardboard box; 20 pcs. In blisters, 2 packages in a cardboard box); 1.5 mg (10 pcs. In blisters, 1, 2, 3, 4, 5, 6, 10 packs in a cardboard box; 20 or 30 pcs. In blisters, 1, 2, 3 packages in a cardboard box; 25 pcs. in blister packs, 2 packages in a cardboard box; 50 pcs. in blister packs, 2, 3, 4, 5, 6, 8, 10 packs in a cardboard box; in jars (jars) of 50, 100, 500, 600, 1000, 1200 pcs., 1 can each in wrapping paper; in bottles (bottles) of 100, 500, 1000 pcs., 1 bottle in a cardboard box; in a polymer container 10, 20, 30, 40, 50, 100 pcs., 1 container in a cardboard box);2 mg (in cans (jars) of 25 pcs., 1 can in a cardboard box); 5 mg (in blisters of 10 pcs., 3 or 5 blisters in a cardboard box; 10 pcs. In blisters, 1, 2, 3, 4, 5, 6, 8, 10 packs in a cardboard box; each 15 pcs. In blister packs, 2 packs in a cardboard box; 20 or 30 pcs. In blister packs, 1, 2, 3 packs in a cardboard box; 50 pcs. In blister packs, 1, 2 each, 3, 4, 5, 6, 8, 10 packages in a cardboard box; in bottles (vials) of 30, 100, 500, 1000 pcs., 1 bottle in a cardboard box; in cans of 50, 100, 500, 600, 1000, 1200 pcs., 1 can each in wrapping paper; in a polymer container, 10, 20, 30, 40, 50 and 100 pcs., 1 container in a cardboard box); 10 mg (10 pcs. In blisters, 2 packages in a cardboard box; in vials of 20 pcs., 1 bottle in a cardboard box).
1 tablet contains:
- Active substance: haloperidol - 1; 1.5; 2; 5 or 10 mg;
- Auxiliary components: potato starch, lactose monohydrate (milk sugar), medical gelatin, talc, magnesium stearate.
The composition of 1 ml solution for injection includes:
- Active ingredient: haloperidol - 5 mg;
- Auxiliary components: lactic acid; water for injections.
Pharmacological properties
Pharmacodynamics
Haloperidol, a butyrophenone derivative, is an antipsychotic (neuroleptic). Has pronounced antipsychotic, sedative and antiemetic effects, in small doses provides an activating effect. Causes extrapyramidal disorders. Virtually no anticholinergic action. The sedative effect of the drug is provided due to the mechanism of blockade of α-adrenergic receptors of the reticular formation of the brain stem, the antiemetic effect due to the blockade of dopamine D 2 receptors of the chemoreceptor trigger zone. With blockade of dopamine receptors of the hypothalamus, the hypothermic effect and galactorrhea are manifested.
In the case of prolonged use, the endocrine status changes, the production of prolactin increases, the production of gonadotropic hormones in the anterior pituitary gland decreases.
Pharmacokinetics
When taken orally, 60% of haloperidol is absorbed, the maximum plasma concentration is reached after 3 hours. The volume of distribution is 18 l / kg. 92% binds to plasma proteins. Easily penetrates the blood-brain barriers, including the blood-brain barrier.
Metabolized in the liver with a first-pass effect. Isoenzymes CYP3A3, CYP2D6, CYP3A7, CYP3A5 are involved in the metabolism of the drug. It is a CYP2D6 inhibitor. No active metabolites were found. When taken orally, the elimination half-life is 24 hours (12 to 37 hours).
It is excreted in the bile (15%) and urine (40%, with 1% unchanged). It is excreted into breast milk.
Indications for use
Indications for Haloperidol:
- Chronic and acute psychotic disorders, including schizophrenia, epileptic, manic-depressive and alcoholic psychoses;
- Psychomotor agitation, hallucinations and delusions of various origins;
- Chorea of Huntington;
- Agitated depression;
- Oligophrenia;
- Stuttering;
- Behavioral disorders in childhood and old age (including childhood autism and hyperreactivity in children);
- Tourette's disease;
- Hiccups and vomiting (persistent and resistant to therapy);
- Psychosomatic disorders;
- Nausea and vomiting during chemotherapy (treatment and prevention).
Contraindications
- Severe toxic depression of the central nervous system caused by drugs;
- Diseases of the central nervous system, accompanied by symptoms of extrapyramidal disorders, hysteria, depression, coma of various etiologies;
- Pregnancy and lactation;
- Children under 3 years old;
- Hypersensitivity to drug components and other butyrophenone derivatives.
According to the instructions, Haloperidol should be used with caution in the following diseases / conditions:
- Closed-angle glaucoma;
- Epilepsy;
- Cardiovascular diseases with symptoms of decompensation, myocardial conduction disturbances, an increase in the QT interval or the risk of an increase in the QT interval (including hypokalemia and concomitant use with drugs that can increase the QT interval);
- Renal and / or hepatic impairment;
- Respiratory and pulmonary heart failure, including chronic obstructive pulmonary disease (COPD) and acute infectious diseases;
- Thyrotoxicosis;
- Chronic alcoholism;
- Hyperplasia of the prostate with urinary retention;
- Simultaneous use with anticoagulants.
Instructions for the use of Haloperidol: method and dosage
Haloperidol tablets are taken orally, 30 minutes before meals. An adult single initial dose is 0.5-5 mg, the frequency of administration is 2-3 times a day. For elderly patients, a single dose should not exceed 2 mg.
Depending on the response of patients to the therapy, the dose is gradually increased, usually up to 5-10 mg per day. Higher doses (more than 40 mg per day) are used in some cases in the absence of concomitant diseases and for a short time.
For children, the dose is usually calculated on the basis of body weight - 0.025-0.075 mg / kg per day in 2-3 doses.
With intramuscular administration of Haloperidol, an adult initial single dose varies from 1 to 10 mg, the interval between repeated injections can be 1-8 hours.
For intravenous administration, Haloperidol is prescribed in a single dose of 0.5-50 mg, the dose with repeated administration and the frequency of use are determined by the indications and the clinical situation.
The maximum daily dose for adults for oral and intramuscular administration is 100 mg per day.
Side effects
During therapy, the development of disorders from some body systems is possible:
- Cardiovascular system: when using high doses of haloperidol - tachycardia, arterial hypotension, arrhythmia, changes in the electrocardiogram (ECG), including signs of flutter, ventricular fibrillation and an increase in the QT interval;
- Central nervous system: insomnia, headache, anxiety, anxiety and fear, agitation, drowsiness (especially at the beginning of therapy), akathisia, euphoria or depression, an epileptic seizure, lethargy, the development of a paradoxical reaction (hallucinations, exacerbation of psychosis); with long-term treatment - extrapyramidal disorders, including tardive dyskinesia, tardive dystonia and neuroleptic malignant syndrome;
- Digestive system: when using the drug in high doses - diarrhea or constipation, dry mouth, decreased appetite, hyposalivation, vomiting, nausea, liver functional disorders up to the development of jaundice;
- Endocrine system: menstrual irregularities, pain in the mammary glands, gynecomastia, hyperprolactinemia, increased libido, decreased potency, priapism;
- Hematopoietic system: rarely - agranulocytosis, leukocytosis, temporary and mild leukopenia, a tendency to monocytosis and slight erythropenia;
- Organ of vision: retinopathy, cataract, visual acuity and accommodation disorders;
- Metabolism: peripheral edema, hyper- and hypoglycemia, increased sweating, hyponatremia, weight gain;
- Dermatological reactions: acne-like and maculopapular skin changes; rarely - alopecia, photosensitivity;
- Allergic reactions: rarely - skin rash, laryngospasm, bronchospasm, hyperpyrexia;
- Effects due to cholinergic action: hyposalivation, dry mouth, constipation, urinary retention.
Overdose
Symptoms: muscle stiffness, tremors, depression of consciousness, drowsiness, lowering (in some cases, increasing) blood pressure. In severe cases, a coma, shock, respiratory depression occurs.
Treatment of an overdose with oral administration: gastric lavage is indicated, activated charcoal is prescribed. In case of respiratory depression, artificial lung ventilation is performed. In order to improve blood circulation, intravenous administration of a solution of albumin or plasma, norepinephrine is indicated. Epinephrine is strictly prohibited to use. To reduce extrapyramidal symptoms, antiparkinsonian drugs and central anticholinergic drugs are used. Dialysis is ineffective.
Treatment of overdose with intravenous or intramuscular administration: cessation of therapy with neuroleptics, use of correctors, intravenous administration of glucose solution, diazepam, B vitamins, vitamin C, nootropics, symptomatic therapy.
special instructions
Parenteral use of the drug in children is not recommended.
Elderly patients usually require a lower initial dose and a slower dose adjustment. These patients are characterized by an increased likelihood of developing extrapyramidal disorders. In order to detect early signs of tardive dyskinesia in time, careful monitoring of the patient's condition is recommended.
If tardive dyskinesia develops, the dose of Haloperidol should be gradually reduced and another drug prescribed.
There is evidence of the possibility of symptoms of diabetes insipidus, exacerbation of glaucoma during therapy, and a tendency to the development of lymphomonocytosis with prolonged treatment.
When treating with antipsychotics, the development of a malignant neuroleptic syndrome is possible at any time, but most often it occurs soon after the start of using the drug or after transferring the patient from one neuroleptic drug to another, after increasing the dose or during combination therapy with another psychotropic drug.
During the use of Haloperidol, alcohol should be avoided.
During the period of therapy, one should not engage in potentially hazardous activities that require a high speed of psychomotor reactions and increased attention.
Application during pregnancy and lactation
It is forbidden to use Haloperidol according to indications during pregnancy and lactation.
Pediatric use
It is forbidden to use Haloperidol for the treatment of patients under the age of 3 years. In children over the specified age, parenteral administration of the drug should be carried out under the special supervision of a physician. After reaching the therapeutic effect, it is recommended to switch to Haloperidol tablets.
With impaired renal function
In severe kidney disease, the drug should be used with caution.
For violations of liver function
In severe liver disease, the drug should be used with caution.
Use in the elderly
When treating elderly patients, parenteral administration of haloperidol should be carried out under the special supervision of a physician. After achieving a therapeutic effect, it is recommended to switch to oral administration of the drug.
Drug interactions
With the simultaneous use of Haloperidol with certain drugs, the possible consequences of such interaction should be taken into account:
- Drugs that have a depressing effect on the central nervous system (CNS), ethanol: respiratory depression and hypotensive action, increased CNS depression;
- Anticonvulsants: a change in the frequency and / or type of epileptiform seizures, as well as a decrease in the concentration of haloperidol in blood plasma;
- Drugs causing extrapyramidal reactions: increasing the severity and frequency of extrapyramidal effects;
- Tricyclic antidepressants (including desipramine): a decrease in their metabolism, an increased risk of seizures;
- Antihypertensive drugs: potentiation of the action of haloperidol;
- Medicines with anticholinergic activity: increased anticholinergic effects;
- Beta-blockers (including propranolol): development of severe arterial hypotension;
- Indirect anticoagulants: reducing their effect;
- Lithium salts: development of more pronounced extrapyramidal symptoms;
- Venlafaxine: increased plasma concentration of haloperidol;
- Imipenem: development of transient arterial hypertension;
- Guanethidine: a decrease in its hypotensive effect;
- Isoniazid: an increase in its concentration in blood plasma;
- Indomethacin: confusion, drowsiness;
- Rifampicin, phenytoin, phenobarbital: decrease in the concentration of haloperidol in blood plasma;
- Methyldopa: confusion, sedation, dementia, depression, dizziness;
- Carbamazepine: Increase the metabolic rate of haloperidol. Possible manifestation of symptoms of neurotoxicity;
- Levodopa, pergolide: decrease in their therapeutic effect;
- Quinidine: an increase in the concentration of haloperidol in blood plasma;
- Morphine: development of myoclonus;
- Cisapride: prolongation of the QT interval on the ECG;
- Fluoxetine: development of extrapyramidal symptoms and dystonia;
- Fluvoxamine: an increase in the concentration of haloperidol in blood plasma, accompanied by a toxic effect;
- Epinephrine: "perversion" of its pressor action, which leads to the development of tachycardia and severe arterial hypotension.
Analogs
Analogues of Haloperidol are: Haloperidol-Acri, Haloperidol-Richter, Haloperidol-Ferein, Apo-Haloperidol, Haloperidol decanoate, Galomond, Halopril, Senorm.
Terms and conditions of storage
Store in a dark, dry place out of reach of children.
Shelf life:
- Solution for injection - 5 years at a temperature of 15-30 ° C;
- Tablets - 3 years at temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Haloperidol
Reviews about Haloperidol are predominantly positive: the drug has a mild effect and is well suited for the treatment of hallucinatory disorders, psychosis.
At the same time, due to the large number of serious side effects (inhibition, drowsiness, extrapyramidal disorders), Haloperidol is considered an outdated drug.
Price for Haloperidol in pharmacies
The approximate price for Haloperidol is: 50 tablets 1.5 mg - 38-50 rubles, 10 ampoules 5 mg / ml - 65-75 rubles.
Haloperidol: prices in online pharmacies
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Drug name Price Pharmacy |
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Haloperidol 1.5 mg tablets 50 pcs. RUB 19 Buy |
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Haloperidol 5 mg tablets 50 pcs. 22 RUB Buy |
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Haloperidol 1.5 mg tablets 50 pcs. RUB 23 Buy |
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Haloperidol 5 mg tablets 50 pcs. RUB 24 Buy |
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Haloperidol 5 mg tablets 50 pcs. RUB 26 Buy |
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Haloperidol 5 mg / ml solution for intravenous and intramuscular administration 1 ml 5 pcs. RUB 61 Buy |
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Haloperidol 5 mg / ml solution for intravenous and intramuscular administration 1 ml 10 pcs. 82 RUB Buy |
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Haloperidol solution for intravenous and intramuscular injection. 5mg / ml 1ml 10 pcs. RUB 85 Buy |
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Haloperidol velpharm solution for intravenous and intramuscular injection. 5mg / ml amp. 1ml No. 10 202 RUB Buy |
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Haloperidol decanoate 50 mg / ml solution for intramuscular administration (oily) 1 ml 5 pcs. 295 RUB Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
