Haloperidol
(HALOPERIDOL)

Trade name: haloperidol.

International name: Haloperidol.

Chemical management title: 4-4 – (4 chlorophenyl)-4-hydroxy-1-piperidine-1-(4-fluorophenyl)-1-butanone.

Dosage Form: tablets.

Ingredients: One tablet contains the active substance – haloperidol 1.5 mg or 5 mg Other ingredients: potato starch, lactose, gelatin medical, talc, magnesium stearate.

Description: Tablets from white to white to slightly yellowish tint of color. For dosage 1,5 mg – flat-beveled. For dosage of 5 mg – and scored with a flat-facet.

Pharmacotherapeutic group: Antipsychotic (neuroleptic) drug. ATC Code (N05AD01)

Pharmacological properties

Haloperidol neuroleptic belonging to the derivatives butirofenona. Has a pronounced antipsychotic and antiemetic effects.
Effects of haloperidol is associated with the blockade of central dopamine (D2) and ?-adrenergic receptors in Mesocortical and limbic brain structures. The blockade of D2-receptors of the hypothalamus leads to a decrease in body temperature, galaktoree (increase in output of prolactin). Inhibition of dopamine receptors in the emetic trigger zone center is the basis of antiemetic action. Interaction with dopaminergic structures of the extrapyramidal system may lead to extrapyramidal disorders. Marked antipsychotic activity combined with a mild sedative effect (in small doses, has an activating effect). Increases the effects of hypnotics, narcotic analgesics, funds for general anesthesia, analgesics and other means of oppressing the function of CNS.
Pharmacokinetics
Haloperidol is absorbed, mainly in small intestine by passive diffusion. Bioavailability of 60-70%. After oral application, the maximum blood concentrations achieved after 3 – 6 hours. Haloperidol at 90% bound to plasma proteins. The ratio of concentration in red blood cells to plasma concentration 1:12.
The concentration of haloperidol in the tissues than in blood.
Haloperidol is metabolized in the liver, the metabolite is pharmacologically inactive.
Haloperidol is allocated kidneys (40%) and feces (60%), passes into breast milk. The half-life of plasma after oral administration of an average of 24 hours (12-37 hours).

Indications for use

The drug is used strictly under doctor’s prescription.

* Severe and chronic psychosis, accompanied by excitation, hallucinatory and delusional disorder, manic state, psychosomatic disorders.
* Conduct disorders, personality changes (paranoid, schizoid, and others), the syndrome of Gilles de la Tourette, as in childhood, and adults.
* Tiki, chorea Gettingtona.
* Long-term persistent and resistant to therapy hiccups and vomiting, including those related to anticancer therapy.
* Premedication before operative intervention.

Contraindications

* Heavy toxic function of the central nervous system depression caused by xenobiotics, coma of various origins.
* Diseases of the CNS, accompanied by pyramidal and extrapyramidal disorders (Parkinson’s disease, etc.).
* Increased sensitivity to derivatives butirofenona.
* Pregnancy, the period of breastfeeding.
* Children under 3 years.

Caution must be exercised with decompensated cardiovascular disease (including angina), conduction of the heart muscle, with severe diseases of the kidneys, liver, cardiopulmonary diseases (including bronchial asthma and acute infections), epilepsy, angle-closure glaucoma, hyperthyroidism (thyrotoxicosis), prostatic hyperplasia (urinary retention), active alcoholism.

Dosing and Administration

Assign inside half an hour before a meal (you can of milk to reduce the irritants in the gastric mucosa).
Initial daily dose is 0,5 – 5 mg, divided into 2-3 doses. Then gradually increase the dose of 0.5-2 mg (in resistant cases by 2-4 mg) to achieve the desired therapeutic effect. The maximum daily dose – 100 mg. The average therapeutic dose is 10-15 mg / day, for chronic forms of schizophrenia 20-40 mg / day, in resistant cases, up to 50-60 mg / day. The duration of treatment, an average of 2-3 months. Maintenance dose (outside exacerbations) from 0,5 to 5 mg / day (dose is decreased gradually).
Children 3-12 years old (weighing 15-40 kg) 0,025-0,05 mg per kilogram of body weight per day 2-3 times a day, increasing the dose no more frequently than once every 5-7 days until a daily dose of 0, 15 mg / kg.
Patients elderly and debilitated patients designate 1/3-1/2 normal dose for adults, with its increased no more frequently than every 2-3 days.
As an antiemetic appointed interior of 1,5-2 mg.

Side effects

CNS: extrapyramidal disorders of different severity, parkinsonism. In most patients the transient akineto-rigid syndrome, oculogyric crises, akathisia, dystonic phenomenon.
Perhaps the development neuroleptic malignant syndrome (NZS), one of the first signs of which is the increase in body temperature, drowsiness.
With chronic administration of haloperidol may develop tardive dyskinesia, especially in elderly patients and patients with organic central nervous system failure, so the dose for this category of patients should be reduced.
At the beginning of therapy may experience lethargy, drowsiness or insomnia, headache, going after the appointment of correctors.
Cardiovascular system: arrhythmia, tachycardia, orthostatic hypotension, lability of blood pressure, changes in the ECG.
Blood: transient leukopenia or leukocytosis, eritropeniya, limfomonotsitoz, rarely – agranulocytosis.
Liver: increased activity of “liver” of transaminases, jaundice.
Skin: allergic reactions, rash, toksikodermiya, dry skin, photosensitivity, hyperfunction of the sebaceous glands.
GI: anorexia, dyspepsia, dry mouth, hygrostomia sometimes, nausea, vomiting, constipation, diarrhea.
Endocrine System: dysmenorrhea, frigidity, gynecomastia, galactorrhea, impotence, priapism, increased body weight.
Other: urinary retention, blurred vision, increased fatigue, decreased sense of thirst, heat stroke, alopecia, hyponatremia, hyper-or hypoglycemia.

Overdose

If overdose may result in acute neuroleptic reactions listed above. Of particular cause for concern increased body temperature, which may be a symptom of neuroleptic malignant syndrome. In severe cases of overdose may experience various forms of disorders of consciousness, even coma, convulsive reaction.
Measures of assistance: termination of neuroleptic therapy, the appointment of correctors, intravenous diazepam, glucose solution, nootropics, vitamins B and C, symptomatic therapy.

Interaction with other drugs

Haloperidol increases the severity of depressant effect on the CNS, opioid analgesics, hypnotics, tricyclic antidepressants, funds for general anesthesia, and alcohol.
In an application with protivoparkinsonicheskimi drugs (levodopa, etc.) may diminish the therapeutic effect of these funds due to an antagonistic effect on dopaminergic structures.
When applying to methyldopa may develop disorientation, difficulty and slowing of thought processes.
Haloperidol may reduce the intensity of the action of adrenaline (epinephrine) and other sympathomimetics, cause “paradoxical” decrease in blood pressure and tachycardia in their joint application.
Enhances the effect of peripheral M-holinoblokatorov and the majority of hypotensive drugs (reduces effect guanetidina by ousting him from the ?-adrenergic neurons and the suppression of its capture by these neurons).
When combined with the admission of anticonvulsant drugs (including barbiturates and other inducers of microsomal oxidation), the last dose should be increased, because haloperidol lowers the threshold for seizure activity, may also decrease serum concentrations of haloperidol. In particular, while drinking tea or coffee may decrease the effect of haloperidol.
Haloperidol may reduce the effect of indirect anticoagulants, so by sharing a recent dose should be adjusted.
Haloperidol slows metabolism of tricyclic antidepressants and MAO inhibitors, thus increasing their level in plasma and increased toxicity.
In an application with bupropion reduces epileptic threshold and increases the risk of epileptic seizures.
At the same time receiving haloperidol with fluoxetine increases the risk of side effects on the CNS, especially extrapyramidal reactions.
When concomitant administration of haloperidol with lithium, especially in high doses, can cause irreversible neyrointoksikatsiyu, as well as increase extrapyramidal symptoms.
In simultaneous reception with amphetamine reduced the effect of antipsychotic haloperidol and psihostimuliruyuschy effect of amphetamines, because of the blockade haloperidol ?-adrenergic receptors.
Haloperidol may reduce the effect bromkriptina.
Anticholinergic, antihistamine (1 generation), antidiskineticheskie funds may increase anticholinergic side effects and reduce the antipsychotic effect of haloperidol.

Cautions

During treatment, patients should regularly monitor ECG, blood counts, liver samples.
For relief of extrapyramidal disorders prescribed antiparkinsonian agents (tsiklodol, etc.), nootropics, vitamins.
Severity of extrapyramidal disorders associated with the dose, often at lower doses, they may diminish or disappear.
In some cases, signs of neurological disorders are observed to remove the drug, after a long course of treatment, therefore, should be lifted gradually reducing the dose of haloperidol.
In the development of tardive dyskinesia not be abruptly cancel the drug is recommended a gradual reduction in dose.
Should protect exposed skin from excessive solar radiation due to increased risk of photosensitivity.
Antiemetic effect of haloperidol may mask signs of drug toxicity and complicate diagnosis of states, the first symptom of which is nausea.
During the reception of haloperidol prohibits driving a vehicle, servicing arrangements and other work requiring high concentration, as well as alcohol intake.

Product

10 tablets of 1.5 mg or 5 mg in blister packaging.
1, 2, 3, 4, 5 stripes packages or 100 tablets in a jar of polymer with the instructions on the application in a pile of cardboard.
For hospitals – 500, 600, 1000, 1200 tablets in a jar of polymer, with instructions for use in a packet of cardboard.

Storage

List B. In dry, dark place at a temperature not exceeding 25 ° C.
Keep out of reach of children!

Shelf life: 3 years. Do not apply after the expiry date.

Conditions of supply of pharmacies: prescription.