Haloperidol

General characteristics. Structure:

Active ingredient: 1,5 mg or 5 mg of a haloperidol.

Excipients: potato starch, lactoses monohydrate (sugar milk), gelatin medical, talc, magnesium stearate.

Neuroleptic, effective and powerful drug for stopping of conditions of excitement, correction of disorders of behavior. It is capable to reduce pain, body temperature, to remove spasms. Has antihistaminic effect. In moderate degree is the sedative (calming) means. Eliminates hallucinations, nonsense. Drug has also rather strong antiemetic action. It is applied also at treatment of stutter.

In comparison with other psychotropic drugs the haloperidol favourably differs in what does not cause in preferential number of patients apathy, block, but at first can result in drowsiness. At the same time, it is capable to strengthen effect of somnolent drugs, as well as analgetics.

Meanwhile, it is important to understand: the haloperidol is not soothing or antidepressive drug, this much more powerful tool for successful treatment first of all of any heavy mental disorders. Drug has to be appointed by the doctor, taking into account a full clinical picture of a disease. It is necessary to consider what else drugs are accepted by the patient (including vitamin complexes) as the haloperidol can clash with them.

Pharmacological properties:

Pharmacodynamics. A haloperidol – the neuroleptic belonging to phenyl propyl ketone derivatives. Renders the expressed antipsychotic and antiemetic effect. The expressed antipsychotic activity is combined with moderate sedation (in small doses has the activating effect).

Antipsychotic action of a haloperidol is connected with blockade of central dopamine (D2) and - adrenergic receptors in mesocortical and limbic structures of a brain. Blockade of D2 receptors of a hypothalamus leads to decrease in body temperature, a galactorrhoea (increase in production of prolactin). Interaction with dofaminergichesky structures of extrapyramidal system can lead to extrapyramidal disturbances. Oppression of dopamine receptors in a trigger zone of the emetic center is the cornerstone of antiemetic action.

The haloperidol strengthens action of somnolent, narcotic analgetics, means for the general anesthesia, analgetics and other means oppressing function of the central nervous system (CNS).

Pharmacokinetics. The haloperidol is soaked up, generally in a small intestine by passive diffusion. Bioavailability of 60-70%. At oral administration, the maximum concentration in blood are reached in 3 - 6 hours. The haloperidol for 90% contacts proteins of plasma. The concentration relation in erythrocytes to concentration in plasma 1:12.

Concentration of a haloperidol in fabrics is higher, than in blood.

The haloperidol is metabolized in a liver, the metabolite is pharmacological not active.

The haloperidol is allocated with kidneys (40%) and with a stake (60%), gets into breast milk. Plasma elimination half-life after oral administration averages 24 hours (12-37 hours).

Indications to use:

Drug is used strictly on doctor's orders.

1. The acute and chronic psychoses which are followed by excitement, hallucinatory and crazy frustration, maniacal states, psychosomatic frustration.

2. Disorders of behavior, change of the personality (paranoid, schizoid, and others), Gilles de la Turett's syndrome, both at children's age, and at adults.

3. Tics, chorea of Gettington.

4. It is long the hiccups and vomiting, remaining and steady against therapy, including connected with antineoplastic therapy.

5. Premedication before an operative measure.

Route of administration and doses:

Appoint inside, for half an hour to food (it is possible with milk for reduction of irritant action by a mucous membrane of a stomach).

The initial daily dose makes 0,5 – 5 mg, divided into 2-3 receptions. Then the dose is gradually increased by 0,5-2 mg (in resistant cases on 2-4 mg), before achievement of necessary therapeutic effect. The maximum daily dose – 100 mg. The therapeutic dose averages 10-15 mg/days, at chronic forms of schizophrenia of 20-40 mg/days, in resistant cases to 50-60 mg/days. Duration of a course of treatment, on average, 2-3 months. Maintenance doses (out of an aggravation) from 0,5 to 5 mg/days (the dose is reduced gradually).

Children are 3-12 years old (with the body weight of 15-40 kg) – 0,025-0,05 mg on kilogram of body weight a day 2-3 times a day, raising a dose than time in 5-7 days, to a daily dose of 0,15 mg/kg is not more often.

The patient of advanced age and the weakened patient appoint 1/3-1/2 usual doses for adults, with its increase not more often than each 2-3 days.

As an antiemetic appoint 1,5 mg.

For more exact dosing other dosage form of drug, for example, of a drop for intake can be required.

Features of use:

During therapy by the patient it is regularly necessary to exercise control of an ECG, a blood count, "hepatic" tests.

Expressiveness of extrapyramidal frustration is connected with a dose, often at a dose decline they can decrease or disappear.

At development of late dyskinesia the gradual dose decline (is recommended up to full drug withdrawal).

It is necessary to be careful during the performing of hard physical activity, acceptance of a hot bathtub (development of heatstroke owing to suppression of the central and peripheral thermal control in a hypothalamus is possible).

During treatment it is not necessary to accept "anti-cold" nonprescription HP (possibly strengthening of anticholinergic effects and risk of emergence of heatstroke).

It is necessary to protect open sites of skin from excess sunlight owing to the increased risk of a photosensitization.

Treatment is stopped gradually in order to avoid emergence of a syndrome of "cancellation".

Antiemetic action can mask signs of medicinal toxicity and complicate diagnosis of states which first symptom is nausea.

It is noted that doses for children of 6 mg/days cause additional improvement at behavior disorders and tics.

During reception of the Haloperidol driving of vehicles, service of mechanisms and other types of the works demanding the increased concentration of attention, and also alcohol intake is forbidden.

Side effects:

From a nervous system: extrapyramidal frustration of different degree of manifestation, parkinsonism, passing akineto-rigid syndrome, okulogirny crises, headache, dizziness, sleeplessness or drowsiness (various degree of manifestation), condition of concern, uneasiness, psychomotor excitement, fear, akathisia, euphoria, depression, epileptic seizures, in rare instances exacerbation of psychosis, including hallucination; extrapyramidal frustration; at prolonged treatment - late dyskinesia (smacking and wrinkling of lips, inflation of cheeks, the bystry and worm-shaped movements of language, the uncontrollable chewing movements, the uncontrollable movements of hands and legs), late dystonia (the speeded-up blinking or spasms a century, an unusual look or position of a body, the uncontrollable bent movements of a neck, a trunk, hands and legs) and a malignant antipsychotic syndrome (a hyperthermia, muscular rigidity, the complicated or hurried breathing, tachycardia, arrhythmia, increase or a lowering of arterial pressure (ABP), the increased sweating, an urine incontience, convulsive frustration, consciousness oppression).

From cardiovascular system: when using in high doses - decrease in the ABP, orthostatic hypotension, arrhythmias, tachycardia, changes on the electrocardiogram (ECG) (lengthening of an interval of Q-T, signs of trembling and ventricular fibrillation).

From the alimentary system: at use in high doses - a loss of appetite, dryness in a mouth, a hypoptyalism, nausea, vomiting, diarrhea or locks, an abnormal liver function, up to development of jaundice.

From bodies of a hemopoiesis: seldom - a temporary leukopenia or a leukocytosis, an agranulocytosis, an erythropenia and a tendency to a monocytosis.

From urinogenital system: an ischuria (at a prostate hyperplasia), peripheral hypostases, pains in chest glands, a gynecomastia, a giperprolaktinemiya, disturbance of a menstrual cycle, decrease in a potentiality, increase in a libido, a priapism.

From sense bodys: cataract, retinopathy, sight illegibility.

Allergic reactions: makulopapulezny and akneobrazny changes of skin, a photosensitization, it is rare - a bronchospasm, a laryngospasm.

From skin: hyperfunction of sebaceous glands.

Laboratory indicators: a hyponatremia, hyper - or a hypoglycemia, increase in activity of "hepatic" transaminases.

Others: alopecia, increase in body weight.

Interaction with other medicines:

The haloperidol increases expressiveness of the oppressing influence on TsNS of opioid analgetics, hypnagogues, tricyclic antidepressants, means for the general anesthesia, alcohol.

At simultaneous use with protivoparkinsonichesky drugs (a levodopa, etc.) therapeutic action of these means because of antagonistic influence on dofaminergichesky structures can decrease.

At use with metildopy development of a disorientation, difficulty and delay of processes of thinking is possible.

The haloperidol can reduce intensity of effect of adrenaline (Epinephrinum) and other sympathomimetics, cause a "paradoxical" lowering of arterial pressure and tachycardia at their combined use.

Strengthens action peripheral M-holinoblokatorov and the majority of antihypertensives (reduces action of a guanetidin owing to replacement it from α-adrenergic neurons and suppression of its capture by these neurons).

At the combined reception with anticonvulsants (including barbiturates, etc. inductors of a microsomal oxidation), it is necessary to raise doses of the last since the haloperidol reduces a threshold of convulsive activity; also serumal concentration of a haloperidol can decrease.

The haloperidol can reduce effect of indirect anticoagulants therefore at joint reception the dose of the last should be adjusted.

The haloperidol slows down metabolism of tricyclic antidepressants and MAO inhibitors owing to what their level in plasma increases and toxicity increases.

At simultaneous use with bupropiony reduces an epileptic threshold and increases risk of developing of epileptic seizures.

At a concomitant use of a haloperidol with fluoxetine the risk of side effect on TsNS, especially extrapyramidal reactions increases.

At co-administration of a haloperidol with lithium, especially in high doses, can cause irreversible neurointoxication, and also strengthen extrapyramidal symptomatology.

At a concomitant use with amphetamines the antipsychotic effect of a haloperidol and psychogogic effect of amphetamines, owing to blockade by a haloperidol of α-adrenergic receptors decreases.

The haloperidol can reduce action of Bromocriptinum.

Anticholinergic, antihistaminic (the I generations) and protivoparkinsonichesky HP can strengthen m-holinoblokiruyushchee influence of a haloperidol and reduce its antipsychotic action (dose adjustment can be required).

The use of strong tea or coffee (especially in large numbers) reduces action of a haloperidol.

Contraindications:

1. The heavy toxic oppression of the TsNS function caused by xenobiotics, a coma of various genesis.

2. TsNS diseases which are followed by pyramidal and extrapyramidal frustration (Parkinson's disease, etc.).

3. Hypersensitivity to phenyl propyl ketone derivatives.

4. Pregnancy, breastfeeding period.

5. Children's age up to 3 years.

Due to the existence in composition of drug of lactose (milk sugar), its reception is contraindicated at an inborn lactose intolerance, a lactose intolerance, glucosic галактозной to malabsorption.

With caution it is necessary to take a haloperidol at dekompensirovanny cardiovascular diseases (including stenocardia, disturbances of endocardiac conductivity, lengthening of an interval of Q-T or predisposition to it is a hypopotassemia, simultaneous use of other medicines (M) which can cause lengthening of an interval of Q-T); at a serious illness of kidneys, a liver, a pulmonary heart (including at bronchial asthma and acute infections), epilepsy, closed-angle glaucoma, a hyperthyroidism (thyrotoxicosis), a prostate hyperplasia (ischuria), active alcoholism.

Overdose:

Symptoms: at overdose of drug emergence of the acute antipsychotic reactions which are listed above is possible. Especially fervescence which can be one of symptoms of a malignant antipsychotic syndrome has to guard. In hard cases of overdose various forms of disturbance of consciousness can be observed, up to a coma, convulsive reactions.

Treatment: gastric lavage, absorbent carbon. At respiratory depression – artificial ventilation of the lungs. For improvement of blood circulation in/in enter plasma or solution of albumine, Norepinephrinum. Epinephrinum in these cases is strictly forbidden to be applied! Reduction of extrapyramidal symptoms – the central holinoblokator and protivoparkinsonichesky HP. Dialysis is inefficient.

Storage conditions:

In the dry, protected from light place at a temperature not over 25 ˚С. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets on 1,5 mg or 5 mg. On 10 tablets in a blister strip packaging. On 1, 2, 3, 4, 5 blister strip packagings together with the application instruction in a pack from a cardboard. On 100 tablets in bank polymeric. On 500, 600, 1000, 1200 tablets in bank polymeric (for hospitals). Each can together with the application instruction in a pack from a cardboard.