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Antabuse

Antabuse
Antabuse is a drug used in the treatment of alcoholism. The action of the drug is based on the blockade of acetaldehyde dehydrogenase, which is involved in the metabolism of ethyl alcohol.

Brand: Disulfiram

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Antabuse 500 mg
360 pills - 500 mg
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270 pills - 500 mg
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120 pills - 500 mg
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60 pills - 500 mg $61.99 $1.03 $21.91 Add to cart
30 pills - 500 mg $41.95 $1.40 No Add to cart
Antabuse 250 mg
360 pills - 250 mg
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$171.95 $0.48 $187.45 Add to cart
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Product description

Pharmacodynamics of Antabuse

Buy Antabuse tablets in Canada

The action of the drug 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 ethyl alcohol metabolite - acetaldehyde, which causes negative sensations (flushing, nausea, vomiting, tachycardia, lowering blood pressure, etc.), which make alcohol consumption extremely unpleasant after taking Antabus. This leads to a conditioned reflex aversion to the taste and smell of alcoholic beverages.

Pharmacokinetics

After oral administration, the absorption of disulfiram from the gastrointestinal tract ranges from 70 to 90%; it is rapidly metabolized, being reduced to diethyldithiocarbamate, which itself is excreted in the form of a glucurone conjugate or converted into diethylamine and carbon sulfide, part of which (4–53%) is excreted through the lungs.

Contraindications

Packaging of tablets Antabuse

Absolute:

  • severe diseases of the cardiovascular system, hearing organs (auditory nerve neuritis) and eyes (glaucoma, optic neuritis);
  • bronchial asthma, pulmonary emphysema;
  • pulmonary tuberculosis;
  • severe liver failure;
  • diseases of the hematopoietic organs;
  • diabetes;
  • thyrotoxicosis;
  • epilepsy and convulsive syndrome of any genesis;
  • mental illness;
  • exacerbation of peptic ulcer;
  • kidney disease;
  • malignant tumors;
  • polyneuritis of any etiology;
  • pregnancy;
  • period of breastfeeding;
  • increased individual sensitivity to the drug.

Relative:

  • cardiovascular diseases in the stage of compensation;
  • advanced age (over 60);
  • peptic ulcer of the stomach and duodenum in remission;
  • residual effects after cerebrovascular accident;
  • previously transferred disulfiramic (antabuse) psychoses.

 

Dosing and Administration of Antabuse

Antabuse tablet

Inside. The effervescent tablet is dissolved in water in an amount sufficient to completely dissolve the drug (half a glass). Treatment is prescribed after a thorough examination of the patient and warning of the consequences and complications. Take 200-500 mg 1-2 times a day according to an individual scheme. After 7–10 days, a disulfiram-alcohol test is performed (20–30 ml of vodka after taking 500 mg of the drug); in case of a weak reaction, the dose of alcohol is increased by 10–20 ml (the maximum dose of vodka is 100–120 ml). The test is repeated after 1–2 days in a hospital and after 3–5 days on an outpatient basis with the correction of alcohol and / or drug doses as needed. In the future, you can use a maintenance dose of 150-200 mg / day for 1-3 years.

 


Interaction

Reaction to ethanol is reduced by ascorbic acid.

Contraindicated combinations

Alcohol. Intolerance reaction (flushing, erythema, vomiting, tachycardia). You should avoid taking alcoholic beverages and drugs containing alcohol.


Undesirable combinations of isoniazid.

Behavior and coordination disorders.


Nitro-5-imidazoles (metronidazole, ordinazole, secnidazole, tinidazole). Delirious disorders, confusion.


Phenytoin. A significant and rapid rise in the level of phenytoin in plasma with toxic symptoms (suppression of its metabolism).


If the combination cannot be avoided, clinical observation and monitoring of plasma concentrations of the drug during and after treatment with disulfiram should be carried out.

Combinations requiring caution

Warfarin (and other oral anticoagulants). Increased effect of oral anticoagulants and the risk of bleeding (reduced breakdown of warfarin in the liver). It is recommended that more frequent monitoring of the concentration of warfarin and adjustment of the dose of anticoagulants within 8 days after discontinuation of Antabus are recommended.


Theophylline. Disulfiram inhibits theophylline metabolism. As a result, the dose of theophylline should be adjusted (reduced dosage) depending on the clinical symptoms and the plasma concentration of the drug.


Benzodiazepines. Disulfiram can potentiate the sedative effect of benzodiazepines by inhibiting their oxidative metabolism (especially chlordiazepoxide and diazepam). The benzodiazepine dosage should be adjusted according to clinical presentation.


Tricyclic antidepressants. An increase in the reaction of alcohol intolerance is possible if patients take alcoholic beverages while taking disulfiram.

Special instructions

Patients should be warned of the dangers of a reaction intolerance to alcoholic beverages. In the case of simultaneous administration with oral anticoagulants, it is necessary to carry out more frequent monitoring of the prothrombin content and adjust the doses of anticoagulants, which is associated with an increased risk of bleeding.


Antabuse should be taken with caution in patients with renal insufficiency or hypothyroidism, especially at the risk of a possible combination with alcohol.


Side effects

Due to the properties of disulfiram:

- metallic taste in the mouth;

- an unpleasant smell in patients with colostomy (associated with carbon sulfide);

- rare cases of hepatitis (similar to those sometimes found in patients with nickel eczema who do not suffer from alcoholism);

- polyneuritis of the lower extremities, optic neuritis;

- memory loss, confusion, asthenia;

- headaches;

- skin allergic manifestations.

Associated with the combination of disulfiram-ethyl alcohol: cases of respiratory failure, cardiovascular collapse, cardiac arrhythmias are described; angina pectoris, sometimes myocardial infarction, as well as neurological disorders; swelling of the brain.

Complications with long-term use: rarely - psychoses, reminiscent of alcohol; hepatitis, gastritis; in persons suffering from cardiovascular diseases, thrombosis of the cerebral vessels is possible, therefore, in case of complaints of paresthesia in the limbs and face, the drug should be discontinued immediately; exacerbation of polyneuritis.

When taking alcohol doses over 50–80 ml of vodka while taking disulfiram, severe disorders of the cardiovascular and respiratory systems, edema, and convulsions can develop. In this case, detoxification therapy is urgently carried out, analeptics are administered, symptomatic treatment is carried out.

The combination of disulfiram-ethanol can cause depression of consciousness, up to coma, cardiovascular collapse, neurological complications.