Галоперидол-Акри®

General characteristics. Structure:

Active ingredient: 0,0015 g or 0,005 g (1,5 mg or 5 mg) of a haloperidol in 1 tablet.

Excipients: lactose, potato starch, silicon dioxide colloid (aerosil), talc, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. A haloperidol — the neuroleptic belonging to phenyl propyl ketone derivatives. Renders the expressed antipsychotic and antiemetic effect. Action of a haloperidol is connected with blockade of central dopamine (D2) and α-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). Oppression of dopamine receptors in a trigger zone of the emetic center is the cornerstone of antiemetic action.

Interaction with dofaminergichesky structures of extrapyramidal system can lead to extrapyramidal disturbances. The expressed antipsychotic activity is combined with moderate sedation (in small doses has the activating effect). Strengthens action of somnolent, narcotic analgetics, means for the general anesthesia, analgetics and other means oppressing the TsNS function.

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.
• The acute and chronic psychoses which are followed by excitement, hallucinatory and crazy frustration, maniacal states, psychosomatic frustration.
• 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.
• Tics, chorea of Gettington.
• It is long the hiccups and vomiting, remaining and steady against therapy, including connected with antineoplastic therapy.
• 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 on mucous 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 inside 1,5-2 mg.

Features of use:

During treatment by the patient it is regularly necessary to carry out monitoring of an ECG, blood count, hepatic tests. For stopping of extrapyramidal frustration appoint antiparkinsonichesky means (Cyclodolum, etc.), nootropa, vitamins.

Expressiveness of extrapyramidal frustration is connected with a dose, often at a dose decline they can decrease or disappear. In some cases signs of neurologic frustration are observed at drug withdrawal, after a long course of treatment therefore it is necessary to cancel a haloperidol, gradually reducing doses.

At development of late dyskinesia it is not necessary to cancel drug sharply; the gradual dose decline is recommended. It is necessary to protect open sites of skin from excess sunlight owing to the increased risk of a photosensitization.

Antiemetic action of a haloperidol can mask signs of medicinal toxicity and complicate diagnosis of states which first symptom is nausea. During reception ^{ГАЛОПЕРИДОЛа-АКРИ®} 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:

TsNS: extrapyramidal frustration of different degree of manifestation, parkinsonism. At most of patients the passing akineto-rigid syndrome, okulogirny crises, an akathisia, the dystonic phenomena are noted. Development of the antipsychotic malignant syndrome (AMS) is possible, one of the first signs of which is fervescence, drowsiness.

At long reception of a haloperidol development of late diskineziya, especially at elderly patients and patients with organic insufficiency of TsNS therefore drug doses for this category of patients have to be lowered is possible. At the beginning of therapy the slackness, drowsiness or sleeplessness, a headache undergoing later appointments of proofreaders can be observed.

Cardiovascular system: arrhythmias, tachycardia, orthostatic hypotension, lability of arterial pressure, change from an ECG.

Blood: a tranzitorny leukopenia or a leukocytosis, an erythropenia, лимфомоноцитоз, it is rare — an agranulocytosis.

Liver: increase in activity of "hepatic" transaminases, jaundice.

Skin: allergic reactions, rash, toksikodermiya, xeroderma, photosensitization, hyperfunction of sebaceous glands.

GIT: anorexia, dyspepsia, dryness in a mouth, sometimes hypersalivation, nausea, vomiting, a lock, diarrhea.

Endocrine system: dysmenorrhea, frigidity, gynecomastia, galactorrhoea, impotence, priapism, increase in body weight.

Others: an ischuria, a sight illegibility, increased fatigue, the lowered feeling of thirst, heatstroke, an alopecia, a hyponatremia, hyper - or a hypoglycemia.

Interaction with other medicines:

The haloperidol increases expressiveness of the oppressing influence on TsNS, 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), doses of the last should be raised 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.

At the simultaneous use of tea or coffee action of a haloperidol can decrease.

The haloperidol interferes with suppression by insulin release diazoxide; can reduce action of a bromkriptin.

Anticholinergic, antihistaminic (1 generations), antidiskinetichesky means can strengthen anticholinergic side effects and reduce antipsychotic effect of a haloperidol.

Contraindications:

• The heavy toxic oppression of the TsNS function caused by xenobiotics, a coma of various genesis.
• TsNS diseases which are followed by pyramidal and extrapyramidal frustration (a disease of Par-kinsona, etc.).
• Hypersensitivity to phenyl propyl ketone derivatives.
• Pregnancy, breastfeeding period.
• Children's age up to 3 years.

It is necessary to be careful at dekompensirovanny cardiovascular diseases (including stenocardias), disturbance of conductivity of a cardiac muscle; 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:

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.

Help measures: therapy termination by neuroleptics, appointment of proofreaders, intravenous administration of diazepam, solution of glucose, nootrop, vitamins of group B and C, symptomatic therapy.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use drug after the period of validity specified on packaging. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,0015 g or on 0,005 g. On 10 tablets in a blister strip packaging and on 2, 3, 5 or 10 blister strip packagings in a cardboard pack together with the application instruction.