Active substanceHaloperidolHaloperidol
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  • Dosage form: & nbspRAsterol for intramuscular injection
    Composition:

    1 ml of the solution contains:

    Active substance: haloperidol - 5 mg;

    Auxiliary substances: dairy acids in terms of 100% substance - 5 mg, water for injection - up to 1 ml.

    Description:Popaque or slightly opalescent, colorless or slightly colored liquid.
    Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.D.01   Haloperidol

    Pharmacodynamics:

    Haloperidol is a neuroleptic, belonging to butyrofenone derivatives. Has a pronounced antipsychotic and antiemetic effect.

    The action of haloperidol is associated with blockade of central dopamine (D2) and α-adrenergic receptors in the mesocarcical and limbic structures of the brain. Blockade D2- receptors of the hypothalamus leads to a decrease in body temperature, galactorrhea, due to increased production of prolactin. The inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect. Interaction with the dopaminergic structures of the extrapyramidal system leads to extrapyramidal disorders. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect).Potentsiruet action of hypnotics, drugs, analgesics and other means of suppressing the function of the central nervous system (CNS).

    Pharmacokinetics:

    The maximum concentration in the blood after intramuscular injection is reached after 20 minutes. Haloperidol 90% bound to plasma proteins, 10% is a free fraction. The ratio of concentration in erythrocytes - to the concentration in the plasma is 1:12.

    The concentration of haloperidol in tissues is higher than in blood, the drug tends to accumulate in tissues.

    Haloperidol is metabolized in the liver, the metabolite is not active.

    Haloperidol is excreted by the kidneys (40%) and with feces (60%). The half-life from the plasma after intramuscular injection is 21 hours (17-25 h).

    Indications:

    Coping and treatment of psychotic disorders of different etiologies.

    Contraindications:

    - Severe toxic oppression of the central nervous system and coma of any etiology;

    - zCNS abnormalities, accompanied by pyramidal and extrapyramidal disorders (including Parkinson's disease);

    - Pan increased sensitivity to butyrophenone derivatives;

    - bVariability, the period of breastfeeding;

    - dup to 3 years.

    Carefully:

    Decompensated diseases of the cardiovascular system (CVS) (including angina pectoris, intracardiac conduction disorders, lengthening of the interval Q-T or a predisposition to this - hypokalemia, the simultaneous use of other drugs (LS), which can cause lengthening of the interval Q-T), epilepsy, zakratougolnaya glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis), pulmonary-cardiac and respiratory failure (including chronic obstructive pulmonary disease and acute infectious diseases), prostatic hyperplasia with a delay in urine , alcoholism.

    Dosing and Administration:

    For relief of psychomotor agitation haloperidol in the early days, intramuscularly administered 2-5 mg 2-3 times a day, the maximum daily dose of 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 by 2 doses. The maximum daily dose is 0.15 mg / kg.

    The parenteral route of administration of haloperidol should be carried out under the close supervision of the physician, especially in elderly patients and children, when the therapeutic effect is achieved, the preparation should be taken orally.

    Side effects:

    From the nervous system: headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, anxiety, psychomotor agitation, fear, akathisia, euphoria, depression, epileptic seizures, in rare cases, exacerbation of psychosis, including hallucinations; extrapyramidal disorders; long-term dyskinesia (smacking lips and lips, inflating cheeks, quick and wormlike movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the hands and feet), late dystonia (rapid blinking or spasms of the eyelids, unusual facial expression or body position, uncontrollable curved movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle rigidity, difficulty or rapid breathing, tachycardia, arrhythmia, increased or decreased arterial tension (blood pressure),increased sweating, urinary incontinence, convulsive disorders, depression of consciousness).

    From the cardiovascular system: when used in high doses - reduced blood pressure, orthostatic hypotension, arrhythmias, tachycardia, changes in ECG (lengthening interval Q-T, signs of flutter and fibrillation of the ventricles).

    From the digestive system: when used in high doses - decreased appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, impaired liver function, until the development of jaundice.

    On the part of the organs of hematopoiesis: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

    From the genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinaemia, menstrual cycle disorders, decreased potency, increased libido, apopism.

    From the sense organs: cataract, retinopathy, blurred vision.

    Allergic reactions: maculopapular and acne-like skin changes, photosensitivity; rarely - bronchospasm, laryngospasm.

    Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

    Other: alopecia, weight gain.

    Overdose:

    Symptoms: muscle rigidity, tremor, drowsiness, lowering blood pressure, sometimes - raising blood pressure. In severe cases - coma, respiratory depression, shock.

    Treatment: discontinuation of the drug. With respiratory depression - artificial ventilation. To improve blood circulation, intravenously injected plasma or albumin solution, norepinephrine. Epinephrine in these cases, use is strictly prohibited! Reduction of extrapyramidal symptoms - central holinoblokatory and antiparkinsonian drugs. Dialysis is ineffective.

    Interaction:

    Haloperidol increases the severity of the CNS CNS depression, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotic drugs, and means for general anesthesia.

    Strengthens the action of peripheral m-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due to its displacement from alpha-adrenergic neurons and suppression of its capture by these neurons).

    It inhibits the metabolism of tricyclic antidepressants and monoamine oxidase inhibitors, thus increasing (mutually) their sedative effect and toxicity.

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

    Reduces the effect of anticonvulsants (reducing the convulsive threshold with haloperidol).

    Weakens vasoconstrictive action of dopamine, phenylephrine, norepinephrine, epinephrine and ephedrine (alpha adrenoceptor blockade haloperidol, which can lead to distortion of the action of epinephrine and a paradoxical decrease in blood pressure).

    Reduces the effect of antiparkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system).

    Changes (may increase or decrease) the effect of anticoagulants.

    Reduces the effect of bromocriptine (dose adjustment may be required).

    In the application with methyldopa increases the risk of developing mental disorders (including disorientation in space, slowing and difficulty thinking processes).

    Amphetamines reduce antipsychotic effect of haloperidol, which, in turn, reduces their inducing effect (haloperidol blockade of alpha-adrenoceptors).

    Anticholinergic,antihistamines (I generations) and antiparkinsonian drugs can enhance the m-cholinoblock effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).

    Long-term administration of carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in plasma.

    In combination with lithium preparations (especially in high doses), the development of encephalopathy (can cause irreversible neurointoxication) and an increase in extrapyramidal symptoms.

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

    With simultaneous use with drugs that cause extrapyramidal reactions, increases the frequency and severity of estropyramide disorders.

    The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.

    Special instructions:

    During therapy, patients should regularly monitor the ECG, the blood formula, and "liver" tests.

    Care must be taken when performing heavy physical work,taking a hot bath (it is possible to develop a heat stroke due to the suppression of central and peripheral thermoregulation in the hypothalamus).

    During treatment, it is not necessary to take "anti-cold" OTC medicines (possibly intensifying anticholinergic effects and the risk of heat stroke). Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.

    Treatment is stopped gradually to avoid the occurrence of the "withdrawal" syndrome.

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

    Effect on the ability to drive transp. cf. and fur:

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

    Form release / dosage:

    Solution for intramuscular injection, 5 mg / ml.

    Packaging:

    1 ml per ampoule of neutral glass.

    By 5-ampoules are placed in a contour mesh package made of a polyvinyl chloride film.2 contour mesh packages together with the instruction for use and the ampoule disk ceramic ceramic scriber are put in a pack of cardboard.

    At packing of ampoules with notches the scarifier is not put.

    Storage conditions:

    Store in a dark place at a temperature of no higher than 25 ° C.

    Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N001029 / 01
    Date of registration:05.06.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.03.2017
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