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Disulfiram (also known as Antabuse) is one of the oldest, proven drugs that have not lost their relevance for the treatment of alcohol addiction.

Indications

  • Alcohol addiction.
  • Certain forms of cancer.
  • Nickel poisoning.

Form and chemical properties

Crystalline powder, white with a weak yellowish-greenish tinge. It is difficult to dissolve in alcohol, practically insoluble in water, acids and alkalis. Molecular weight 296.54.

Pharmachologic

Inhibits acetaldehyde dehydrogenase and delays the enzymatic biotransformation of alcohol at the stage of acetaldehyde. The accumulation of the latter in the body causes intoxication, which (since consciousness is preserved) is accompanied by severe sensations.

A remedy for the treatment of alcohol addiction. Has an inhibitory effect on the enzyme aldehyde dehydrogenase, which is involved in the metabolism of ethanol. This leads to an increase in the concentration of the etatol metabolite – acetaldehyde, which causes flushing, nausea, vomiting, general malaise, tachycardia, and a decrease in blood pressure, which make alcohol consumption extremely unpleasant after taking disulfiram.

After oral administration, it is rapidly and completely (by 70–90%) absorbed in the gastrointestinal tract. It is extensively metabolized, recovering to diethyldithiocarbonate, excreted by the kidneys in the form of glucuronide, or decomposes to form diethylamine and carbon disulfide, part of which (4–53%) is excreted through the lungs.

Precautions for Disulfiram

Patients should be warned about the danger of manifestations of the reaction of 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.

It should be used with caution in patients with renal failure or hypothyroidism, especially at the risk of a possible combination with alcohol.

Dosage

By mouth. The dose is 125-500 mg/day, the scheme and duration of treatment are determined individually.

Overdose

Symptoms: coma, collapse, various neurological phenomena.

Treatment: symptomatic.

Where to buy online

You can purchase disulfiram 250 or 500 mg at many pharmacies. Before buying disulfiram (generic Antabuse), you should consult with your doctor. You must have a valid prescription. Disulfiram can be purchased over the counter from the UK. Delivery to your door. Confidential.

Disulfiram and Covid-19

Modeling has shown high efficiency of preparations containing sulfur. Disulfiram showed the most stable interaction with the coronavirus protein.

Disulfiram counteracts SARS-CoV-2 in two main ways. First, as it was previously also shown in laboratory experiments with SARS and MERS coronaviruses, it is a covalent inhibitor. In addition, it fights against such a symptom of COVID-19 as a significant reduction in the body’s reduced forms of glutathione, an important antioxidant. Its deficiency can lead to a severe course of the disease.
https://clinicaltrials.ucsf.edu/trial/NCT04485130
https://mypsych.nhsggc.org.uk/media/1343/adrs-covid-19-disulfiram-guidelines.pdf

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Contraindications

  • Individual intolerance. Allergy to disulfiram.
  • Cardiovascular insufficiency. Aortic aneurysm.
  • Hypertonic disease.
  • Bronchial asthma.
  • Malignant tumors.
  • Increased thyroid activity.
  • Epilepsy.
  • Pregnancy and breastfeeding.
  • Psychoses. Dementia
  • Erosions and ulcers, bleeding of the gastrointestinal tract.
  • Tuberculosis.
  • Severe diseases of the organs of hearing and vision.
  • Unconsciousness.

Indications and contraindications for taking disulfiram are determined by the doctor after examining the patient and assessing his condition.

Side effects

Due to the properties of disulfiram: a metallic taste in the mouth, an unpleasant odor in patients with colostomy (associated with carbon sulfide), rare cases of hepatitis (similar to those sometimes observed in patients with nickel eczema who do not suffer from alcoholism), polyneuritis of the lower extremities, optic neuritis, memory loss, confusion, asthenia, headache, skin allergic manifestations.

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

When alcohol is taken in an amount exceeding 50–80 ml of vodka, while taking disulfiram, severe disorders of the cardiovascular and respiratory systems, edema, convulsions can develop (detoxification therapy, the introduction of analeptics, symptomatic therapy are necessary).

Complications with prolonged use: rarely – psychosis, 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 extremities and the face area, the drug should be discontinued immediately; exacerbation of polyneuritis.

Interaction with other active ingredients

When taking disulfiram and tricyclic antidepressants, it is possible to increase the reaction of alcohol intolerance (reaction disulfiram – ethyl alcohol).

Disulfiram can enhance the sedative effect of benzodiazepines by inhibiting their microsomal oxidation and increasing their plasma concentration. Combined use requires caution. Benzodiazepine dosage should be adjusted according to clinical presentation.

Disulfiram increases the effectiveness of oral anticoagulants (reducing their metabolism in the liver) and the risk of bleeding. Combined use requires caution. It is recommended to monitor INR more often and adjust the dose of anticoagulant during administration of disulfiram and within 8 days after its cancellation.

When disulfiram is used together with nitroimidazole derivatives, delirious disorders, confusion are possible; Disulfiram is contraindicated in patients who are receiving or have recently received nitroimidazole derivatives.

Disulfiram can increase the concentration in the blood of some drugs that undergo microsomal oxidation in the liver with the participation of the isoenzyme CYP2E1.

The combined use of disulfiram and hepatotoxic drugs should be avoided due to possible liver damage.

The effect of disulfiram on the metabolism of barbiturates in the liver may lead to an increase in their concentration in the blood and toxicity.