Chlorpromazine (Chlorpromazinum)

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

Neuroleptics

Included in the formulation
  • Aminazine®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Aminazine
    solution w / m in / in 
    VALENTA PHARM, PAO     Russia
  • Aminazine®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Chlorpromazine hydrochloride
    solution w / m in / in 
    Health to the people - Kharkov Pharmaceutical Enterprise, LLC     Ukraine
    • 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.01   Chlorpromazine

    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, an empty stomach is absorbed in the gastrointestinal tract up to 50%. The maximum concentration in the blood plasma is achieved 1-2 hours after intramuscular injection and 2-4 hours after ingestion. The connection with plasma proteins is 99%.

    Penetrates through the blood-brain and placental barrier, excreted in breast milk.Metabolism in the liver.

    The half-life is from 30 hours to 4 weeks. Elimination with feces and kidneys in the form of metabolites.

    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. It is used as an antiemetic for Meniere's disease, radiation and chemotherapy. Used in the composition of the lytic mixture for the purpose of artificial hypothermia, as well as in the complex treatment of itching dermatoses.

    ICD-10

    V.F00-F09.F04   Organic amnestic syndrome not caused by alcohol or other psychoactive substances

    V.F00-F09.F06.2   Organic delusional [schizophreniform-like] disorder

    V.F00-F09.F07.2   Postcontasia syndrome

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

    V.F20-F29.F29   Inorganic psychosis, unspecified

    V.F10-F19.F11.9   Mental and behavioral disorders caused by the use of opioids - mental disorder and behavioral disorder, unspecified

    V.F20-F29.F20   Schizophrenia

    V.F30-F39.F30   Manic episode

    V.F30-F39.F32   Depressive episode

    V.F40-F48.F44   Dissociative [conversion] disorders

    V.F60-F69.F63   Disorders of habits and drives

    VI.G40-G47.G41   Epileptic status

    VI.G40-G47.G47.0   Disturbances of falling asleep and maintaining sleep [insomnia]

    VIII.H80-H83.H81.0   Ménière's disease

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    XVIII.R40-R46.R45.6   Physical aggressiveness

    XXI.Z100.Z100 *   CLASS XXII Surgical Practice

    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, children under 3 years.

    Carefully:Rheumatism in the active phase, peptic ulcer of the stomach and duodenum, cholelithiasis and urolithiasis, acute pyelitis, hypersensitivity.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Use in children

    Inside, depending on age and body weight.

    3-5 years (body weight not more than 23 kg): 0.55 mg / kg every 6-8 hours, not more than 40 mg per day;

    5-12 years (body weight not more than 46 kg): 75 mg per day.

    Adults

    Inside, to 25-100 mg per day for 1-4 admission. If necessary, the dose is increased by 25-50 mg every 3 days to achieve a therapeutic effect, but should not exceed 1.5 g per day.

    The highest daily dose: 1.5 g for oral administration; 150 mg for intramuscular administration and 100 mg for intravenous administration.

    The highest single dose: 0.3 g for oral administration; 1 g for intramuscular administration and 250 mg for intravenous administration.

    Side effects:

    Central and peripheral nervous system: akathisia, rarely - parkinsonian syndrome, dystonic extrapyramidal reactions, thermoregulation disorders, tardive dyskinesia, in single cases convulsive syndrome develops.

    Hemopoietic system: agranulocytosis, leukopenia.

    The cardiovascular system: tachycardia, arterial hypotension.

    Digestive system: dyspeptic disorders, rarely - cholestatic jaundice.

    Dermatological reactions: photosensitization, skin pigmentation.

    Sense organs: opacity of the lens, blurred vision.

    Urinary system: delay urination.

    Reproductive system: violations of the menstrual cycle, gynecomastia.

    Local Reactions: Postinjection infiltrate, phlebitis.

    Allergic reactions.

    Overdose:

    Arterial hypotension, tachycardia, atrioventricular blockade, oppression of consciousness, extrapyramidal symptoms, coma. With prolonged use - toxic hepatitis.

    Treatment is 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 slowdown in the metabolism of chlorpromazine in the liver).

    Reduces the absorption of the drug with the simultaneous use of antacid agents (should be able to withstand the interval of 4 hours).

    Chlorpromazine reduces the effects of levodopa with simultaneous application.

    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 chlorpromazine and within 5 days after discontinuation of the drug.

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

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

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