Галоперидол-Ферейн®

General characteristics. Structure:

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

Excipients: lactic acid, water for injections.

Pharmacological properties:

Pharmacodynamics. Галоперидол-Ферейн® (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 and - adre-nergicheskikh receptors in mesocortical and limbic structures of a brain. Blockade of D2 receptors of a hypothalamus leads to decrease in body temperature, a galactorrhoea, owing to the increased 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 leads to extrapyramidal disturbances. The expressed antipsychotic activity is combined with moderate sedation (in small doses has the activating effect).

Exponentiates effect of the hypnotic drugs, drugs, analgetics and other means oppressing the TsNS function.

Pharmacokinetics. The maximum concentration in blood after intramuscular introduction are reached in 20 minutes. 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. The haloperidol is allocated with kidneys (40%) and with a stake (60%). Plasma elimination half-life after intramuscular introduction - 21 hour (17-25 h), after intravenous - 14 hours (10-19 h).

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 of Galoperidol-Fereyn® in the first days appoint intramusculary 2-5 mg 2-3 times a day, or intravenously in the same dosage (the ampoule should be parted in 10-15 ml of water for injections), 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,Z ml of solution), the maximum daily dose – 5 mg (1 ml of solution).

For children the dose is more senior 3kh than 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 Galoperidol-Fereyn® has to be carried out under careful control of the doctor, especially upozhily patients and children, at achievement of therapeutic effect it is necessary to pass to administration of drug inside.

Side effects:

TsNS: paroxysmal and acute extrapyramidal frustration of different degree of manifestation. At most of patients the passing akineto-rigid syndrome, okulogirny crises, an akathisia, the dystonic phenomena are noted. For stopping of these phenomena appoint antiparkinsonichesky means (Cyclodolum, etc.), symptomatic therapy.

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.

Development of the antipsychotic malignant syndrome (AMS) is possible. 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, a headache undergoing later appointments of proofreaders can be observed.

Cardiovascular system: tachycardia, arterial hypotension, sometimes hypertensia, changes from an ECG.

Blood: tranzitorny leukopenia or leukocytosis, anemia, лимфомоноцитоз, seldom agranulocytosis.

Liver: dysfunctions, jaundice are possible.

Skin: toksikodermiya, xeroderma, photosensitization, hyperfunction of sebaceous glands.

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

Endocrine system: amenorrhea, frigidity, gynecomastia, galactorrhoea, impotence.

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

Interaction with other medicines:

The haloperidol exponentiates effects of hypotensive drugs of the central action, opioid analgetics, hypnagogues, antidepressants, anesthetics, alcohol.

At simultaneous use with antiparkinsonichesky drugs (a levodopa, etc.) therapeutic action of these means because of antagonistic influence on dofaminergichesky structures can decrease. The haloperidol can reduce intensity of effect of adrenaline and other sympathomimetics and cause a paradoxical lowering of arterial pressure at their use.

At the combined reception with antiepileptic means, doses of the last should be raised since. The haloperidol reduces a threshold of convulsive activity.

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 owing to what their level in plasma increases and toxicity increases. At a concomitant use of a haloperidol with fluoxetine and lithium the risk of side effect on TsNS, especially extrapyramidal reactions increases. At co-administration with antihistamines strengthening of anticholinergic effects is possible.

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

Contraindications:

• 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.

It is necessary to be careful at cardiovascular diseases, with the decompensation phenomena, disturbance of conductivity of a cardiac muscle; at a serious illness of kidneys, a liver and lungs.

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.

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:

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

Issue conditions:

According to the recipe

Packaging:

On 1 ml in ampoules of neutral glass; on 5 ampoules in a blister strip packaging; on 1-2 blister strip packagings in a pack with the application instruction.