Haloperidol - instructions for use, analogs, reviews and release forms (injections in injectable ampoules, decanoat forte oil solution or prolong tablets) for the treatment of schizophrenia, autism in adults, children and pregnancy

In this article, you can read the instructions for using the drug Haloperidol. Presented are reviews of visitors to the site - consumers of this medication, as well as the opinions of physicians specialists on the use of Haloperidol in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of haloperidol in the presence of existing structural analogues.Use for the treatment of schizophrenia, autism and other psychoses in adults, children, as well as in pregnancy and lactation. Interaction of the drug with alcohol.

Haloperidol - neuroleptic, belonging to the derivatives of butyrofenone. Has a pronounced antipsychotic and antiemetic effect.

The effect of haloperidol is associated with blockade of central dopamine (D2) and alpha-adrenergic receptors in mesocortical and limbic structures of the brain. Blockade of D2-receptors of the hypothalamus leads to a decrease in body temperature, galactorrhea (increased production of prolactin). The inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect. Interaction with dopaminergic structures of the extrapyramidal system can lead to extrapyramidal disorders. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect).

Strengthens the action of hypnotics, narcotic analgesics, means for general anesthesia, analgesics and other means of suppressing the function of the central nervous system.

Pharmacokinetics

Absorbed by passive diffusion, in a non-ionized form, mainly from the small intestine. Bioavailability is 60-70%. Haloperidol is metabolized in the liver, the metabolite is pharmacologically inactive. Haloperidol is also subjected to oxidative N-dealkylation and glucuronation. It is excreted in the form of metabolites through the intestine - 60% (including bile 15%), kidneys - 40%, (including 1% - unchanged). Easily penetrates through gistogematicheskie barriers, incl. through placental and blood-brain, penetrates into breast milk.

Indications

• acute and chronic psychoses accompanied by excitement, hallucinatory and delusional disorders, (schizophrenia, affective disorders, psychosomatic disorders);
• behavior disorders, personality changes (paranoid, schizoid, and others), incl. and in childhood, autism, Gilles de la Tourette syndrome;
• tics, Huntington's chorea;
• long-lasting and unyielding hiccups;
• vomiting that is not amenable to treatment with classical antiemetics, including those associated with antitumor therapy;
• premedication before surgery.

Forms of release

Solution for intravenous and intramuscular injection (injections in ampoules for injection).

Solution for intramuscular administration (oily) Haloperidol Decanoate (forte or prolong formula).

Tablets 1 mg, 1.5 mg, 2 mg, 5 mg and 10 mg.

There are no other forms, be it drops or capsules.

Instructions for use and dosage

Dosage depends on the clinical response of the patient. Most often, this means a gradual increase in the dose in the acute phase of the disease, in the case of maintenance doses, a gradual dose reduction in order to ensure the lowest effective dose. High doses are used only in cases of ineffectiveness of smaller doses. The following are the average doses.

Solution for intravenous and intramuscular injection

To stop psychomotor agitation in the early days, haloperidol is administered intramuscularly 2.5-5 mg 2-3 times a day, or intravenously in the same dosage (the ampoule should be diluted in 10-15 ml of water for injection), the maximum daily dose - 60 mg. After achieving a stable sedative effect, they switch to taking the drug inside.

For elderly patients: 0.5-1.5 mg (0.1-0.3 ml of solution), the maximum daily dose is 5 mg (1 ml of solution).

For children older than 3 years, the dose is 0.025-0.05 mg per day, divided into 2 injections. The maximum daily dose is 0.15 mg / kg.

The parenteral route of administration of haloperidol should be carried out under close medical supervision, especially in elderly patients and children. After achieving a therapeutic effect, you should switch to taking the drug inside.

Pills

Assign inside, 30 minutes before a meal (you can with milk to reduce the irritant effect on the gastric mucosa).

The initial daily dose is 1.5-5 mg, divided into 2-3 doses. Then the dose is gradually increased by 1.5-3 mg (in resistant cases to 5 mg), until the necessary therapeutic effect is achieved. The maximum daily dose is 100 mg. On average, the therapeutic dose is 10-15 mg per day, with chronic forms of schizophrenia - 20-40 mg per day, if necessary, the dose can be increased to 50-60 mg per day. On average, the duration of treatment is 2-3 months. Supporting doses (outside the exacerbation) range from 0.5-0.75 mg to 5 mg per day (dose is reduced gradually).

Children aged 3-12 years (with a body weight of 15-40 kg): 0.025-0.05 mg / kg of body weight per day 2-3 times a day, increasing the dose no more than once in 5-7 days, to a daily dose 0.15 mg / kg.

In case of behavioral disorders, Tourette's syndrome: 0.05 mg / kg per day, dividing by 2-3 doses and increasing the dose no more often than 1 time in 5-7 days to 3 mg per day. At an autism - 0.025-0.05 mg / kg per day.

Older patients and weakened patients are prescribed 1 / 3-1 / 2 of the usual dose for adults, the dose is increased no more often than every 2-3 days.

As an antiemetic, appoint inwards for 1.5-2.5 mg.

Oily solution (Decanoate)

The drug is intended exclusively for adults, exclusively for the / m introduction!

Do not administer intravenously!

Injections are recommended to enter the gluteal region. Doses exceeding 3 ml should be avoided, in order to avoid an unpleasant feeling of bursting at the injection site.

Adults: patients who are on long-term treatment with oral antipsychotics (mainly haloperidol), we can recommend a switch to depot injections.

The dose should be selected on an individual basis in view of significant individual differences in the responses to treatment. Selection of the dose should be carried out with strict medical supervision of the patient. The choice of the initial dose is made taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during the previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times higher than oral haloperidol, which usually corresponds to 25-75 mg of the drug Haloperidol Decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.

Depending on the effect, the dose can be stepped up, 50 mg, until the optimal effect is obtained. Usually, the maintenance dose corresponds to a 20-fold daily dose of oral haloperidol. When the symptoms of the underlying disease recur in the period of dose selection, treatment with the drug Haloperidol Decanoate can be supplemented with oral haloperidol.

Usually injections are administered every 4 weeks, however, in view of the large individual differences in efficacy, a more frequent use of the drug may be required.

Older patients and patients with oligophrenia: a lower initial dose is recommended, for example 12.5-25 mg every 4 weeks. Further, depending on the effect, the dose can be increased.

Side effect

• headache;
• insomnia or drowsiness (especially at the beginning of treatment);
• anxiety;
• anxiety;
• excitation;
• fears;
• euphoria or depression;
• lethargy;
• seizures of epilepsy;
• development of a paradoxical reaction - exacerbation of psychosis and hallucinations;
• tardive dyskinesia (smacking lips, puffing cheeks, quick 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, uncontrollable bending movements of the neck, trunk, arms and legs);
• malignant neuroleptic syndrome (shortness or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness);
• a decrease in blood pressure;
• orthostatic hypotension;
• arrhythmias;
• tachycardia;
• changes on the ECG (prolongation of the QT interval, signs of flutter and fibrillation of the ventricles);
• decreased appetite;
• dry mouth;
• hyposalivation;
• nausea, vomiting;
• diarrhea or constipation;
• transient leukopenia or leukocytosis, agranulocytosis, erythropenia;
• retention of urine (with prostatic hyperplasia);
• peripheral edema;
• pain in the mammary glands;
• gynecomastia;
• hyperprolactinemia;
• violation of the menstrual cycle;
• decreased potency;
• increased libido;
• priapism;
• cataract;
• retinopathy;
• blurred vision;
• photosensitization;
• bronchospasm;
• laryngospasm;
• development of local reactions associated with injection;
• alopecia;
• increase in body weight.

Contraindications

• oppression of the central nervous system, incl. and severe toxic oppression of the central nervous system caused by xenobiotics, coma of various origins;
• CNS diseases, accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease);
• lesions of the basal ganglia;
• children up to 3 years;
• depression;
• hypersensitivity to butyrophenone derivatives;
• hypersensitivity to the ingredients of the drug.

Application in pregnancy and lactation

Haloperidol does not cause a significant increase in the number of cases of congenital malformations. Individual cases of congenital defects are known when taking haloperidol concomitantly with other medications during pregnancy. The intake of haloperidol during pregnancy is only permissible in cases where the intended benefit to the mother exceeds the risk to the fetus. Haloperidol excreted in breast milk.In cases where haloperidol is unavoidable, the benefits of breastfeeding in relation to a potential hazard should be justified. In some cases, estradiramidal symptoms were observed in newborns whose mothers took haloperidol during lactation.

Use in children

Contraindicated in children under 3 years.

Solution for intravenous and intramuscular injection

For children older than 3 years, the dose is 0.025-0.05 mg per day, divided into 2 injections. The maximum daily dose is 0.15 mg / kg.

The parenteral route of administration of haloperidol should be performed under the close supervision of the physician, especially in children. After achieving a therapeutic effect, you should switch to taking the drug inside.

Pills

Children aged 3-12 years (with a body weight of 15-40 kg): 0.025-0.05 mg / kg of body weight per day 2-3 times a day, increasing the dose no more than once in 5-7 days, to a daily dose 0.15 mg / kg.

In case of behavioral disorders, Tourette's syndrome: 0.05 mg / kg per day, dividing by 2-3 doses and increasing the dose no more often than 1 time in 5-7 days to 3 mg per day. At an autism - 0.025-0.05 mg / kg per day.

special instructions

Parenteral administration should be carried out under the strict supervision of a physician, especially in the case of elderly and children.When the therapeutic effect is achieved, the oral form of treatment should be switched.

Since haloperidol can induce prolongation of the QT interval, caution should be exercised if there is a risk of prolongation of QT (QT syndrome, hypokalemia, drugs causing prolongation of the QT interval), especially with parenteral administration. In connection with the metabolism of haloperidol in the liver, it is important to exercise caution when assigning it to patients with a violation of liver function.

There are cases of development of seizures caused by haloperidol. Patients with epilepsy and patients, in conditions predisposing to the development of convulsive syndrome (alcoholism, brain trauma), the drug should be used with extreme caution.

With lactose intolerance, it should be borne in mind that a 1.5 mg tablet contains 157 mg of lactose, a 5 mg tablet of -153.5 mg.

With severe physical exertion, taking a hot bath, care must be taken because of the possible development of a heat stroke as a result of ineffective central and peripheral thermoregulation of the hypothalamus due to the administration of the drug.

You should warn the patient about the need to avoid taking medicines against colds that are acquired without a prescription, becauseit is possible to enhance the anticholinergic effects of haloperidol and the development of a heat stroke. During treatment, patients should regularly monitor ECG, blood formulas, hepatic samples.

For relief of extrapyramidal disorders, antiparkinsonian agents (cyclodol), nootropics, Vitamins are prescribed; their use continues after haloperidol withdrawal if they are excreted from the body more quickly than haloperidol in order to avoid the increase of extrapyramidal symptoms.

The severity of extrapyramidal disorders is associated with a dose, often, with a decrease in dose, they can decrease or disappear.

In some cases, signs of neurological disorders are observed when the drug is withdrawn after a long course of treatment, therefore haloperidol should be canceled, gradually reducing the dose.

With the development of tardive dyskinesia should not abruptly cancel the drug; a gradual dose reduction is recommended.

Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitization in such cases.

The antiemetic effect of haloperidol can mask the signs of drug toxicity and make it difficult to diagnose conditions, the first symptom of which is nausea.

Impact on the ability to drive vehicles and manage mechanisms

During the reception of haloperidol it is prohibited to drive vehicles, service mechanisms and perform other types of work that require increased concentration of attention, as well as alcohol intake.

Drug Interactions

Haloperidol enhances the oppressive effects of opioid analgesics, hypnotics, tricyclic antidepressants, agents for general anesthesia, alcohol on the central nervous system.

With the simultaneous use with antiparkinsonian drugs (levodopa and others), the therapeutic effect of these drugs may decrease because of the antagonistic effect on the dopaminergic structures.

When used with methyldopa, development of disorientation, difficulty and slowing down of thinking processes is possible.

Haloperidol can weaken the action of epinephrine (epinephrine) and other sympathomimetics, cause a "paradoxical" decrease in blood pressure and tachycardia when they are used together.

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).

When combined with anticonvulsants (including barbiturates and other inducers of microsomal oxidation), the doses of the latter should be increased, haloperidol reduces the threshold of convulsive activity; in addition, the serum concentrations of haloperidol may decrease. In particular, with the simultaneous use of tea or coffee, the action of haloperidol may weaken.

Haloperidol may reduce the effectiveness of indirect anticoagulants, so when combined, the dose of the latter should be adjusted.

Haloperidol slows the metabolism of tricyclic antidepressants and MAO inhibitors, which increases their plasma levels and increases toxicity.

With simultaneous use with bupropion reduces the epileptic threshold and increases the risk of epileptic seizures.

With the simultaneous administration of haloperidol with fluoxetine, the risk of side effects on the central nervous system increases, especially extrapyramidal reactions.

With concomitant administration with lithium, especially in high doses, can cause irreversible neurointoxication, as well as enhance extrapyramidal symptoms.

With simultaneous reception with amphetamines, the antipsychotic effect of haloperidol and the psychostimulant effect of amphetamines are reduced as a result of the blockade of alpha-adrenergic receptors by haloperidol.

Haloperidol can reduce the effect of bromocriptine.

Anticholinergic, antihistamines (1 generation), antiparkinsonian drugs can enhance anticholinergic side effects and reduce the antipsychotic effect of haloperidol.

Thyroxine may increase the toxicity of haloperidol. With hyperthyroidism, haloperidol can be prescribed only with the simultaneous carrying out of appropriate thyreostatic therapy.

With simultaneous use with anticholinergic drugs may increase intraocular pressure.

Analogues of the drug Haloperidol

Structural analogs for the active substance:

• Apo Haloperidol;
• Haloper;
• Haloperidol decanoate;
• Haloperidol Acry;
• Haloperidol ratopharm;
• Haloperidol Richter;
• Haloperidol Ferein;
• Senorm.

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