Haloperidol

General characteristics. Structure:

Active ingredient: 5 mg of a haloperidol in 1 ml of solution.

Excipients: lactic acid, water for injections.

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic) derivative of a bugirofenon. Possesses the expressed antipsychotic action, blocks postsynaptic dopamine receptors in mesolimbic and mesocortical structures of a brain. High antipsychotic activity is combined with moderate sedation (in small doses has the activating effect) and the expressed antiemetic action. Causes extrapyramidal frustration, has practically no holinoblokiruyushchy effect.

Sedative action is caused by blockade of alpha adrenoceptors of a reticular formation of a trunk of a brain; antiemetic action - blockade dopamine D2 receptors of a trigger zone of the emetic center; hypothermal action and a galactorrhoea - blockade of dopamine receptors of a hypothalamus. Long reception is followed by change of the endocrine status, in a front share of a hypophysis products of prolactin increase and decrease - gonadotropic hormones.

Pharmacokinetics. The maximum concentration in blood after intramuscular introduction are reached in 20 min. The haloperidol for 90% contacts proteins of plasma, 10% represent free fraction. The concentration relation in erythrocytes to concentration in plasma 1:12. Concentration of a haloperidol in fabrics is higher, than in blood, drug tends to cumulation in fabrics. The haloperidol is metabolized in a liver, the metabolite is not active. Also the haloperidol is exposed to oxidizing N-dealkylation and a glyukuronirovaniye. Plasma elimination half-life after intramuscular introduction - 21 hour (17-25 h). The haloperidol is removed in the form of metabolites with a fecal masses - 60% (including with bile - 15%) and with urine of 40%, (in т.ч 1% - in is not changed - number)))). Easily gets through gistogematichesky barriers: including through placental and hematoencephalic, gets into breast milk.

Indications to use:

Stopping and treatment of psychotic frustration of various etiology. Premedication before an operative measure.

Route of administration and doses:

For stopping of psychomotor excitement the haloperidol in the first days is appointed intramusculary on 2,5-5 mg by 2-3 times a day, the maximum daily dose of 60 mg. On reaching steady sedation pass to administration of drug inside.

For patients of advanced age of 0,5-1,5 mg (0,1-0,3 ml of solution), the maximum daily dose - 5 mg (1 ml of solution).

For children the dose is more senior than 3 years makes 0,025-0,05 mg a day, divided into 2 receptions. The maximum daily dose - 0,15 mg/kg.

The parenteral way of introduction of a haloperidol has to be carried out under careful control of the doctor, especially at elderly patients and children; at achievement of therapeutic effect it is necessary to pass to administration of drug inside.

Features of use:

Pregnancy and lactation: administration of drug is contraindicated.

Parenteral administration has to be carried out under strict control of the doctor, especially, in case of patients of advanced and children's age. On reaching therapeutic effect it is necessary to pass to a peroral form of treatment.

As the haloperidol can cause lengthening of an interval of QT, it is necessary to be careful with risk of prolongation of QT (QT syndrome, a hypopotassemia, drugs causing lengthening of an interval of QT), especially at parenteral administration.

Due to the metabolism of a haloperidol in a liver, it is important to show care at appointment as his patient with disturbance of hepatic function. During treatment by the patient it is regularly necessary to carry out monitoring of an ECG, blood count, "hepatic" tests.

Cases of development of the spasms caused by a haloperidol are known. The patient with epilepsy and the patient, in states; contributing to development of a convulsive syndrome (alcoholism, a brain injury in the anamnesis), drug should be used with extra care.

For stopping of extrapyramidal frustration appoint protivoparkinsoinchesky means (Cyclodolum, etc.), nootropa, vitamins; their use is continued also after cancellation of a haloperidol if they are brought from an organism quicker, than a haloperidol in order to avoid strengthening of extrapyramidal symptoms.

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 фотосенсибилизацин.

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.

During reception of a haloperidol alcohol intake is forbidden.

Influence on ability to manage vehicles and mechanisms. During reception of a haloperidol driving of vehicles, service of mechanisms and performance of other types of the works demanding the increased concentration of attention is forbidden.

Side effects:

From a nervous system: headache, dizziness, sleeplessness or drowsiness (various degree of manifestation), alarm, akathisia, euphoria, depression, convulsive frustration, 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 an ECG (lengthening of an interval of QT, 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, эритропеиня 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.

Laboratory indicators: a hyponatremia, hyper - or a hypoglycemia.

Others: alopecia, increase in body weight.

Interaction with other medicines:

Increases expressiveness of the oppressing influence on TsNS of ethanol, tricyclic antidepressants, opioid analgetics, barbiturates and HP hypnotic drugs, means for the general anesthesia.

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

Slows down metabolism of tricyclic antidepressants and MAO inhibitors, at the same time their sedation and toxicity increases (mutually).

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

Reduces effect of anticonvulsants (decrease in a convulsive threshold a haloperidol).

Weakens vasoconstrictive action of a dopamine, Phenylephrinum, Norepinephrinum, ephedrine and Epinephrinum (blockade of alpha adrenoceptors a haloperidol that can lead to a perversion of action of Epinephrinum and to paradoxical decrease in the ABP).

Reduces effect of protivoparkinsonichesky means (antagonistic influence on dofaminergichesky structures of TsNS). Changes (can raise or reduce) effect of anticoagulants.

Reduces action of Bromocriptinum (correction of a dose can be required).

At use from metildopy increases risk of development of mental disturbances (including a disorientation in space, delay and difficulty of processes of thinking).

Amphetamines reduce antipsychotic action of a haloperidol which in turn reduces their psychogogic effect (blockade by a haloperidol of alpha adrenoceptors).

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).

Long purpose of carbamazepine, barbiturates, etc. inductors of a microsomal oxidation reduces concentration of a haloperidol in plasma.

In combination with lithium drugs (especially in high doses) development of encephalopathy (can cause irreversible neurointoxication) and strengthening of extrapyramidal symptomatology is possible.

At a concomitant use with fluoxetine the risk of development of side effects from TsNS increases, especially extrapyramidal reactions.

At simultaneous use with the drugs causing extrapyramidal reactions increases the frequency and weight of estrapyramidal frustration.

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

Contraindications:

Hypersensitivity, heavy toxic oppression of the TsNS function and comas of any etiology; TsNS diseases which are followed by pyramidal and extrapyramidal frustration (Parkinson's disease, etc.); hypersensitivity to phenyl propyl ketone derivatives; pregnancy, breastfeeding period; children up to 3 years.

With care. Dekompensirovanny diseases of cardiovascular system (including stenocardia, disturbances of endocardiac conductivity; lengthening of an interval of QT or predisposition to it is a gipokayemiya, simultaneous use of other medicines (M) which can cause lengthening of an interval of QT, epilepsy, closed-angle glaucoma, a liver and/or renal failure, a hyperthyroidism (with the thyrotoxicosis phenomena), pulmonary and cordial and respiratory insufficiency (including at HOBL and acute infectious diseases), a prostate hyperplasia with an ischuria, alcoholism.

Overdose:

At overdose of drug emergence of the acute antipsychotic reactions which are listed above is possible. Symptoms: muscle tension, a tremor, drowsiness, decrease, sometimes increase in arterial pressure, in hard cases - coma, respiratory depression, shock, lengthening of an interval of QT, arrhythmia. 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: At respiratory depression artificial ventilation of the lungs can be required. At hypotonia and a collapse intravenously, for maintenance of blood circulation enter plasma or the concentrated albumine, a dopamine, or Norepinephrinum. Epinephrinum in these cases is strictly forbidden to be applied as can provoke the expressed hypotonia! For stopping of extrapyramidal symptoms the central holinoblokator and protivoparkinsonichesky medicines. Intravenously enter diazepam, solution of glucose, a nootropa, vitamins of group B and C. Dialysis is inefficient. There is no specific antidote.

Storage conditions:

List B. To store at a temperature of 15-25 °C in the place protected from light. To store in the place, unavailable to children. A period of validity - 2 years. Not to use drug after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction of 5 mg/ml on 2 ml in ampoules. 5 ampoules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or without foil. On 1 or 2 planimetric packagings with the scarificator ampoule ceramic or a knife for opening of ampoules and the application instruction in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break the knife or the scarificator do not put.