Disulfiram (Disulfiramum)

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

Means for correcting disorders in alcoholism, toxic and drug addiction

Included in the formulation
  • Antabus®
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    Actavis PTS ehf Group     Iceland
  • Teturam
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    AVVA RUS, OJSC     Russia
  • Teturam
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    TATHIMFARMPREPARATY, JSC     Russia
  • Teturam
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    PHARMSTANDART-FORESTRY, OJSC     Russia
  • Esperal®
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    Sanofi-Aventis France     France
    • АТХ:

    N.07.B.01.01   Disulfiram

    Pharmacodynamics:
    Has anti-alcohol effect.
    Inhibits acetaldehyde dehydrogenase and delays enzymatic biotransformation of alcohol in the stage of acetic aldehyde. The accumulation of the latter in the body causes intoxication, which (as consciousness is preserved) is accompanied by severe sensations.
    Pharmacokinetics:After oral administration quickly and completely (by 70-90%) is absorbed in the digestive tract. It is sufficiently intensively metabolized, recovering to diethyldithiocarbamate excreted by the kidneys in the form of glucuronide, or decomposes with the formation of diethylamine and carbon disulphide, some of which (4-53%) is excreted through the lungs.
    Indications:Treatment and prevention of recurrences of chronic alcoholism; chronic nickel intoxication.
    ICD-10

    XXI.Z70-Z76.Z71.4   Counseling and monitoring about alcoholism

    XX.Y90-Y98.Y91.2   Severe alcohol intoxication

    XX.Y90-Y98.Y91.1   Alcohol Intoxication of the Middle Degree

    XX.Y90-Y98.Y91.0   Alcohol intoxication of mild degree

    Contraindications:Hypersensitivity, thyrotoxicosis, diseases of the cardiovascular system in the stage of decompensation (including severe cardiosclerosis, atherosclerosis of cerebral vessels, pre-and postinfarction states, aortic aneurysm, coronary insufficiency, arterial hypertension II-III degree, chronic heart failure), severe diseases organs of hearing (neuritis of the auditory nerve) and eyes (glaucoma, optic neuritis), diabetes mellitus, pulmonary tuberculosis with hemoptysis, bronchial asthma, severe emphysema, bostrenie ulcer disease, severe liver failure, kidney disease, malignant tumor of hematopoietic organ disease, mental illness, epilepsy and convulsions any genesis, polyneuritis, pregnancy, breast-feeding.
    Carefully:Cardiovascular diseases in the compensation stage, peptic ulcer of the stomach and duodenum (in remission), residual effects after cerebral circulation, endarteritis, previously suffered psychoses against disulfiram, age over 60 years.
    Pregnancy and lactation:Action category for fetus by FDA - C. Contraindications to use in pregnant and lactating children.
    Dosing and Administration:Inside, intramuscularly and subcutaneously. Inside the dose is selected individually and is, as a rule, 0.25-0.5 g per day; treatment begins after a thorough examination of the patient and a warning about the consequences and complications. Subcutaneously and intramuscularly, 8-10 tablets are implanted.
    Side effects:
    Due to the properties of disulfiram: metallic taste in the mouth, unpleasant odor in patients with colostoma (associated with carbon sulphide), rare cases of hepatitis (similar sometimes observed in patients with nickel eczema, not suffering from alcoholism), polyneuritis of the lower extremities, optic neuritis, memory loss, confusion, asthenia, headache, skin allergic manifestations.
    Associated with a combination of disulfiram-ethyl alcohol: cases of respiratory failure, cardiovascular collapse, heart rhythm disorders, angina pectoris, sometimes - myocardial infarction, as well as neurological disorders, cerebral edema, depression of consciousness, up to coma.
    When drinking alcohol in an amount exceeding 50-80 ml of vodka, severe disruption of the cardiovascular and respiratory systems, edema, convulsions (it is necessary to carry out detoxification therapy, the introduction of analeptics, the conduct of symptomatic therapy) can develop against disulfiram.
    Complications with long-term admission: rarely - psychoses resembling alcoholic; hepatitis, gastritis; in persons suffering from cardiovascular diseases, thrombosis of the cerebral vessels is possible, therefore, when complaints about paresthesia in the limbs and face area should immediately cancel the drug; aggravation of polyneuritis.
    Overdose:
    Symptoms: coma, collapse, various neurological phenomena.
    Treatment: symptomatic.
    Interaction:
    Reaction to ethanol reduces ascorbic acid.
    Contraindicated combinations
    Alcohol: reaction of intolerance (flushes of blood, erythema, vomiting, tachycardia). It is necessary to avoid simultaneous reception of alcoholic beverages and medicines containing alcohol.
    Unwanted combinations
    Isoniazid: impaired behavior and coordination.
    Nitro-5-imidazoles (metronidazole, ornidazole, secnidazole, tinidazole): delirious disorders, confusion.
    Phenytoin: a significant and rapid rise in the level of phenytoin in the plasma with toxic symptoms (suppression of its metabolism). If the combination can not be avoided, clinical monitoring and control of the drug concentration in the plasma should be performed during and after disulfiram treatment.
    Combinations that require caution
    Warfarin and other oral anticoagulants: increased effect of oral anticoagulants and the risk of bleeding (reduced metabolism of warfarin in the liver). It is recommended more frequent monitoring of the concentration of warfarin and correction of the dose of anticoagulants during the appointment of disulfiram and within 8 days after its withdrawal.
    Theophylline: disulfiram inhibits theophylline metabolism, so the dose of theophylline should be adjusted (reduced dosage) depending on the clinical symptoms and the concentration of the drug in the plasma.
    Benzodiazepines: disulfiram can potentiate the sedative effect of benzodiazepines by inhibiting their oxidative metabolism (especially chlordiazepoxide and diazepam).The dosage of benzodiazepine should be adjusted in accordance with clinical manifestations.
    Tricyclic antidepressants: it is possible to intensify the reaction of alcohol intolerance (disulfiram-ethyl alcohol reaction).
    Special instructions:
    Patients should be warned about the dangers of the reaction of alcohol intolerance. In the case of simultaneous administration with oral anticoagulants, more frequent monitoring of prothrombin content and correction of anticoagulant doses is necessary, which is associated with an increased risk of bleeding.
    It should be used with caution in patients with renal insufficiency or hypothyroidism, especially at the risk of a possible combination with alcohol.
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