Levomepromazine (Levomepromazinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation
  • Tizerzin®
    solution w / m d / infusion 
    EGIS ZAO Pharmaceutical Plant     Hungary
  • Tizerzin®
    pills inwards 
    EGIS ZAO Pharmaceutical Plant     Hungary
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.05.A.A   The phenothiazine derivatives with an aliphatic structure

    N.05.A.A.02   Levomepromazine

    Pharmacodynamics:

    Has antipsychotic effect due to blockade of dopamine D2receptors of the mesocortical and mesolimbic system.

    Acts as a sedative by blockade of adrenoreceptors of the reticular formation of the brain stem.

    Has antiemetic effect, blocking dopamine D2receptors of the trigger zone of the vomiting center.

    It causes hyperthermia due to blockade of hypothalamus dopamine receptors.

    It has moderate antihistaminic and M-cholinoblocking action. Reduces blood pressure. Increases the pain threshold.

    Pharmacokinetics:

    After oral administration, the maximum concentration in the blood plasma is reached after 1-3 hours. After intramuscular injection - after 30-90 minutes. It binds to plasma proteins by 90%. Metabolised in the liver by demethylation with the formation of inactive metabolites.

    The half-life is 15-78 hours.

    Elimination by the kidneys and with feces.
    Indications:

    It is used for the treatment of endogenous psychoses, with alcoholic psychosis, reactive psychiatric disorders. Used to enhance the effect of antihistamines and analgesics.

    ICD-10

    V.F20-F29.F20   Schizophrenia

    VI.G50-G59.G50.0   Neuralgia of the trigeminal nerve

    XVIII.R50-R69.R52.2   Another constant pain

    V.F10-F19.F10.4   Mental and behavioral disorders caused by alcohol use - abstinent state with delirium

    Contraindications:

    Closed-angle glaucoma, urinary retention, multiple sclerosis, Parkinson's disease, myasthenia gravis, chronic heart failure, severe hepatic and renal insufficiency, arterial hypotension, porphyria.

    Individual intolerance.

    Carefully:

    Children with diseases of the respiratory system.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. During pregnancy and lactation, the use of the drug is contraindicated. If it is not possible to cancel the intake of levomepromazine during pregnancy, minimal maintenance doses are applied, with a temporary cancellation for the period of labor to prevent atropine-like effects in newborns.

    Dosing and Administration:

    Children

    1-12 years: 0.35-3 μg / kg after 24 hours. The maximum daily dose for children under 12 years is 40 mg.

    Adults

    At the expressed excitation parenteral introduction of a preparation on 25-75 mg, with increase to 75-100 mg at intravenous introduction and 200-250 mg at intramuscular introduction is appointed or nominated. After cupping the acute phase, the drug is taken internally at 50-100 mg, if necessary, the dose rises to 400 mg per day.

    The highest daily dose: 400 mg.

    The highest single dose: 250 mg.

    Side effects:

    Central and peripheral nervous system: blurred vision, akathisia, rarely - parkinsonian syndrome, dystonic extrapyramidal reactions, thermoregulatory disorders, tardive dyskinesia, in a few cases a convulsive syndrome develops.

    The cardiovascular system: tachycardia, arterial hypotension.

    The system of hematopoiesis: agranulocytosis, and leukopenia.

    Digestive system: dyspeptic disorders, rarely - cholestatic jaundice.

    Endocrine system: disorders of the menstrual cycle, gynecomastia.

    Urinary system: retention of urination.

    Dermatological reactions: photosensitivity, skin pigmentation.

    Allergic reactions.

    Overdose:

    Symptoms: arterial hypotension, tachycardia, atrioventricular blockade, oppression of consciousness, extrapyramidal symptoms, epileptic seizures.

    Treatment: symptomatic.

    Interaction:

    When used simultaneously with drugs that depress the central nervous system (hypnotics, benzodiazepines, non-opioid and opioid analgesics, tricyclic antidepressants, anesthetics), the antihypertensive effect and inhibition of the central nervous system increase.

    MAO inhibitors contribute to the development of extrapyramidal disorders, due to a slowing of the metabolism of levomepromazine in the liver.

    Reduces the absorption of the drug with the simultaneous use of antacid agents, so you should maintain the interval between doses of 4 hours.

    Levomepromazine reduces the effects of levodopa when used simultaneously.

    Special instructions:

    With long-term use - monitoring the blood formula, electrocardiogram indicators, liver function, blood pressure.

    Excluded is the use of alcohol during treatment with levomeprozamine and within 5 days after discontinuation of the drug.

    When hyperthermia appears, it is recommended that the drug be withdrawn.

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