Esperal® (Esperal®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceDisulfiramDisulfiram
Similar drugsTo uncover
  • Antabus®
    pills inwards 
    Actavis PTS ehf Group     Iceland
  • Teturam
    pills inwards 
    AVVA RUS, OJSC     Russia
  • Teturam
    pills inwards 
    TATHIMFARMPREPARATY, JSC     Russia
  • Teturam
    pills inwards 
    PHARMSTANDART-FORESTRY, OJSC     Russia
  • Esperal®
    pills inwards 
    Sanofi-Aventis France     France
    • Dosage form: & nbspPills.
    Composition:
    One tablet contains:
    active substance: disulfiram - 500 mg;
    Excipients: magnesium stearate - 0.7 mg, povidone - K30 - 15 mg, carmellose sodium - 16.25 mg, cellulose microcrystalline -158.05 mg.
    Description:
    Round tablets of white with a cream shade of color with engraving "ESPERAL" on one side and crosswise risk on another.
    Pharmacotherapeutic group:Treatment for alcoholism.
    ATX: & nbsp

    N.07.B.01.01   Disulfiram

    Pharmacodynamics:
    The action of disulfiram is based on the blockade of acetaldehyde dehydrogenase, which is involved in the metabolism of ethyl alcohol. This leads to an increase in the concentration of the metabolite of ethyl alcohol - acetaldehyde, which causes a number of unpleasant sensations ("hot flashes" of the face skin, nausea, vomiting, tachycardia, lowering blood pressure, etc.). As a result, a conditioned reflex reaction to the taste and smell of ethanol takes place.
    The maximum therapeutic effect is achieved 12 hours after ingestion and can last for 10-14 days after discontinuation of treatment.
    Pharmacokinetics:After oral administration disulfiram quickly and almost completely absorbed (70-90%). It is rapidly metabolized in the liver, recovering to diethyldithiocarbamate, which is excreted as glucuronide by the kidneys or transformed into diethylamine and carbon disulfide, the proportion of which varies from 4% to 53%. The latter is secreted through the lungs. The remaining metabolites are excreted in the urine. It is an inhibitor of CYP2E1.
    Indications:Treatment and prevention of recurrences of chronic alcoholism.
    Contraindications:
    - Hypersensitivity to disulfiram or any of the components of the drug.

    - Severe hepatic insufficiency.

    - Severe respiratory failure.

    - Diabetes.

    - Neuropsychiatric disorders.

    - Epilepsy and convulsive syndrome of any genesis.

    - Diseases of the cardiovascular system, including ischemic heart disease.

    - Reception of alcoholic beverages or medications containing ethanol, during the preceding 24 hours.

    - Pregnancy and childbearing age (in case of not using contraception).

    - Lactation period.

    - Simultaneous reception of isoniazid, metronidazole, ornidazole, secnidazole, tinidazole, phenytoin (see "Interaction with other drugs").
    Carefully:
    - Renal insufficiency (danger of more severe disulfiram-ethanol reaction).
    - Hypothyroidism (danger of heavier disulfiram-ethanol reaction).
    - Nickel dermatitis (increased risk of developing hepatitis).
    - Peptic ulcer of stomach and duodenum, (see "Side effect").
    - Optic neuritis (see "Side effect").
    Pregnancy and lactation:
    Pregnancy
    The drug Esperal® is contraindicated for use in pregnant women (due to the lack of clinical data).
    Breastfeeding period
    The safety of the use of Esperal® during breastfeeding has not been established.
    Therefore, the drug is contraindicated in women breastfeeding.

    Dosing and Administration:
    Treatment is appointed after careful examination of the patient and warning of the consequences and complications. The drug is taken orally 0.5 g once a day in the morning during meals on an individual basis: the dose gradually decreases to 1/2 or 1/4 tablets per day. The dose can be increased or decreased depending on the response of the patient. After 7-10 days, an alcohol sample (20-30 ml of 40% ethanol after taking 0.5 g of the drug) is carried out, with a weak reaction, the dose of ethanol is increased by 10-20 ml (the maximum dose of 120 ml in terms of 40% ethanol).The sample is repeated after 1-2 days in the hospital and 3-5 days after an outpatient treatment, with the correction of the doses of ethanol and / or the drug as necessary. In the future, you can use a maintenance dose of 0.125-0.25 g (1/2 or 1/4 tablets) per day for 1-3 years.
    It is not recommended to conduct a trial with ethanol in patients older than 50 years.
    Side effects:
    Undesirable reactions associated with disulfiram
    Disorders from the gastrointestinal tract
    - "Metallic" taste in the mouth, halitosis (bad breath), nausea, vomiting, pain in the mouth
    epigastric region, diarrhea.
    - Unpleasant odor in patients with colostomy (associated with the release of carbon disulfide).
    Disturbances from the liver and bile ducts
    - Increased activity of "liver" transaminases.
    - Hepatic insufficiency, hepatitis (mainly cytolytic).
    Fulminatic hepatitis.
    - Jaundice.
    Disturbances from the nervous system
    - Peripheral neuropathy, polyneuropathy, optic neuritis.
    - Convulsions.
    - Encephalopathy.
    - Headache.
    Disorders from the psyche
    - Decreased memory.
    Confusion.
    - Asthenia.
    - Disorientation in time and space.
    - Drowsiness.
    Disturbances from the skin and subcutaneous tissues
    - Skin allergic reactions, possibly due to cross-allergy to rubber vulcanizers.
    - Itching, rash.
    Undesirable reactions associated with the disulfiram-ethanol combination
    - "Tides" of blood to the skin of the face, hyperemia of the skin, nausea, vomiting, weakness, tachycardia, decrease blood pressure.
    - Cases of more severe reactions, including heart rhythm disturbances, angina attacks, cardiovascular collapse, myocardial infarction (sometimes with fatal outcome), respiratory depression and neurologic symptoms (confusion, encephalopathy, seizures, cerebral edema, cerebral hemorrhage ).

    When long-term administration of disulfiram
    - Psychoses that resemble alcoholic, hepatitis, gastritis.
    - In patients with cardiovascular diseases, thrombosis of cerebral vessels is possible, so if complaints are made about paresthesia in the limbs and face, immediately discontinue the drug.
    - Exacerbation of polyneuritis.
    - When taking doses of ethanol more than 50-80 ml (in terms of 40% ethanol) on the background of taking the drug, severe disorders of the function of the cardiovascular and respiratory systems develop, swelling, convulsions.In this case, urgently carry out detoxification therapy, conduct symptomatic treatment.
    Overdose:
    An overdose of disulfiram alone alone can trigger the development of disorders from the nervous system: a disturbance of consciousness (including confusion, encephalopathy),
    extrapyramidal symptoms, convulsions, collapse.
    Overdose when taking a combination of disulfiram-ethanol (mainly with suicidal attempts) causes depression of consciousness down to coma, cardiovascular collapse, neurological complications.
    Treatment is symptomatic, aimed at restoring and maintaining functional
    the state of the cardiovascular and respiratory systems.
    Interaction:
    Disulfiram can increase the concentration of certain drugs that undergo microsomal oxidation in the liver with the help of the CYP2E1 isoenzyme (see the section "Pharmacokinetics").
    Contraindicated combinations
    With ethanol
    Disulfiram-ethanol reactions: "tides" of blood to the skin of the face, redness of the skin, nausea, vomiting,
    lowering blood pressure, tachycardia, weakness, or more severe reactions (see section
    "Side effect").Avoid taking alcoholic beverages and ethanol-containing medicines.
    Diazepam can relax the disulfiram-ethanol reaction, and it is slightly weakened
    ascorbic acid and antihistamines.
    Unwanted combinations
    With isoniazid
    Disulfiram increases the risk of behavioral and coordination disorders.
    With derivatives of nitroimidazole (metronidazole, ornidazole, secnidazole, tinidazole)
    Acute delirium, confusion.
    With phenytoin
    A significant and rapid increase in plasma concentrations of phenytoin, leading to an increased risk of developing its toxic effects (since disulfiram inhibits the metabolism of phenytoin). If this combination can not be avoided, the patient's condition and the concentration of phenytoin in the blood plasma should be monitored during and after treatment with disulfiram.
    With hepatotoxic drugs
    It is necessary to avoid joint admission
    disulfiram and hepatotoxic
    medicines due to
    possible liver damage.
    Combinations that require
    caution
    With warfarin and other indirect anticoagulants
    Increased anticoagulant action and increased risk of bleeding (reduced metabolism of warfarin in the liver). It is recommended more frequent monitoring of the international normalized ratio (MHO) and correction of the dose of anticoagulants at the beginning of disulfiram reception and within 8 days after its withdrawal.
    With theophylline
    Disulfiram reduces the metabolism of theophylline. Therefore, the dose of theophylline should be adjusted (reduced doses) depending on the clinical symptoms and the concentration of theophylline in the plasma.
    With benzodiazepines

    Disulfiram can enhance the sedative effect of benzodiazepines by inhibiting their microsomal oxidation (especially chlordiazepoxide and diazepam). The dosage of benzodiazepine should be adjusted in accordance with clinical manifestations. With tricyclic antidepressants (amitriptyline) Enhancement of disulfiram-ethanol reaction (ethanol intolerance reaction) in the case of ethanol administration against disulfiram while receiving tricyclic antidepressants. FROM rifampicin Disulfiram slows down the oxidation and excretion of rifampicin by the kidneys. FROM pimozide When used simultaneously with pimozide, in very rare cases, amplification may occur organic brain syndrome

    Special instructions:This drug should only be used under medical supervision. Heavy toxic liver lesions have been reported (including fulminant hepatitis and necrosis of the liver), which can lead to liver failure, hepatic coma and death, or require liver transplantation. Before the beginning treatment with disulfiram should conduct a study of liver function, including the determination of the activity of "liver" transaminases (see the section "Contraindications"). These studies should be repeated on a regular basis during the administration of disulfiram, especially in the first three months of treatment (monthly). Threefold excess of the upper limit of the activity norm of "liver" transaminases requires immediate termination of
    treatment for a long time. In this case, carefully monitor the patient prior to the normalization of functional "hepatic" samples.
    Patients must be instructed to immediately inform the attending physician of the appearance of symptoms such as asthenia,anorexia (lack of appetite), nausea, vomiting, epigastric pain, or jaundice (manifestations of which may be dyeing of the skin and mucous membranes (eg, oral cavity, sclera) in yellow, itching, darkening of the urine, discoloration of the stool). When they appear, the patient should be immediately examined, including clinical examination and laboratory examination (assessment of the functional state of the liver). Patients should be warned about the dangers of developing disulfiram-ethanol reactions. Disulfiram-etaiol reactions develop in patients receiving disulfiram, when taking alcoholic beverages, including in small quantities. Patients should be warned about the presence of ethanol in certain medicines (in particular, in oral solutions), in food, as well as in some toiletries, such as after shaving lotions and perfumes. Unpleasant symptoms ("hot flushes" of blood to the skin of the face, redness of the skin, nausea and vomiting, a feeling of malaise, tachycardia and lowering of blood pressure) develop 10 minutes after receiving the ethanol drink and last from 30 minutes to several hours.A lethal outcome is possible with simultaneous the use of disulfiram and ethanol (alcohol). Reactions to ethanol may occur within 2 weeks after discontinuation of disulfiram treatment.
    Effect on the ability to drive transp. cf. and fur:
    Special attention should be paid to the issue of the possibility of management transport
    means and work with mechanisms, because of the risk of development in some patients of drowsiness associated with the reception of disulfiram.
    Form release / dosage:
    Tablets 500 mg.


    Packaging:
    For 20 tablets in a polypropylene vial, capped with a stopper with desiccant and control of the first autopsy.

    1 bottle with instructions for use in a cardboard box.
    Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N016145 / 01
    Date of registration:30.11.2009
    The owner of the registration certificate:Sanofi-Aventis FranceSanofi-Aventis France France
    Manufacturer: & nbsp
    Representation: & nbspSanofi Aventis GroupSanofi Aventis Group
    Information update date: & nbsp25.04.2016
    Illustrated instructions
      Instructions
      Up