Antabuse Disulfiram: Effective Way to Overcome Alcohol Dependence - Baltimore Post-ExaminerBaltimore Post-Examiner

Antabuse Disulfiram: Effective Way to Overcome Alcohol Dependence

Antabuse contains an active substance called Disulfiram. It is used in patients with alcohol dependence and for the prevention of alcohol dependence relapse.

The mechanism of action is based on the inhibition of acetaldehyde dehydrogenase, the enzyme responsible for the decomposition and thus the elimination of acetaldehyde from the body. Inhibition of this enzyme leads to the accumulation of acetaldehyde in the body leading to the appearance of unpleasant symptoms, such as nausea, vomiting, facial redness, low blood pressure, and rapid heart rate.

Pharmacokinetics

After oral administration, Antabuse is quickly and incompletely resorbed (70-90% of the drug is resorbed), and is rapidly metabolized to diet hylthiocarbamate. The major part is eliminated in the form of glucuronide, while the smaller portion is converted to diethylamine and carbon disulfide (which is eliminated through the lungs). Glucoronides are eliminated through the stool, while other metabolites are eliminated through the urine.

Contraindications

Antabuse is contraindicated in patients with severe hepatic impairment, as there have been reported cases of Disulfiram-induced hepatotoxicity, which can often lead to fatal outcome. It is very important to evaluate liver function before starting the treatment because it is well known that alcohol causes liver damage. If you notice the symptoms of liver damage (yellow skin, yellow eyes, and pain in the upper right stomach), you should immediately contact your doctor.

Patients who have severe respiratory insufficiency should not use Disulfiram, as the use of this medicine may lead to the exacerbation of symptoms and difficulty breathing.

In addition, Antabuse Disulfiram is also contraindicated in the following conditions:

  • In patients with type I or type II diabetes.
  • In patients with cardiovascular disease (heart failure, angina pectoris).
  • In patients with neuropsychiatric disorders (schizophrenia, manic disorders, panic disorders, depression, and agarophobia).
  • In patients with impaired renal function.
  • In patients who consumed alcoholic beverages or alcohol-containing drugs in the previous 24 hours.

Precautions

In clinical studies, rare cases (in less than 0.1% of patients) of fulminant hepatitis (inflammation of the liver) were reported. If you notice symptoms, such as chronic exhaustion, nausea, anorexia, vomiting, jaundice, or pain in the upper right abdomen, contact your doctor immediately. In such cases, it is necessary to immediately perform functional tests of the liver.

Before starting therapy, it is necessary to inform the patient of the possible occurrence of Disulfiram reactions. This reaction occurs in patients who consume alcohol (even in very small amounts) while the Antabuse therapy. Concomitant use with alcohol leads to the appearance of very unpleasant and uncomfortable symptoms, such as low blood pressure accompanied by fainting, severe nausea and vomiting, fatigue, and rapid heart rate. These unpleasant symptoms occur 10 minutes after alcohol intake and last for several hours. Severe symptoms of Disulfiram reaction have also been reported, including arrhythmias, angina pectoris attacks, myocardial infarction, sudden death, cardiovascular collapse, confusion, and seizures. Therefore, the simultaneous use of alcohol is strictly contraindicated. Reactions to alcohol can also occur two weeks after discontinuation of Antabuse. Patients have to avoid the use of alcohol-containing medicines (usually oral suspensions or solutions).

Antabuse Disulfiram reaction may occur if the medicine is administered concurrently with the following drugs:

  • Metronidazole and Tinidazole – antibiotics used to treat many infections.
  • Phenytoin – a drug used to treat epilepsy.
  • Isoniazid – a drug used to treat tuberculosis.

Antabuse should not be used during pregnancy, as it may cause damage to the fetus. Use appropriate contraceptives while using this drug. The use of Antabuse during breastfeeding is not recommended because it is not known whether it is excreted in breast milk.

If the Antabuse reaction occurs, the use of an oxygen mixture (95% oxygen and 5% carbon dioxide) is recommended. High doses of vitamin C administered intravenously (1000mg) can be useful in treating the Disulfiram reaction. The use of ephedrine is also recommended in order to stabilize blood pressure and heart function.

Since Antabuse can cause sedation, caution is recommended when driving vehicles and operating machines.

Dosage

Antabuse contains 250mg of Disulfiram. The recommended starting dosage when looking to Meds4sure Pharmacy: Antabuse Generic Disulfiram 500 mg Dosage Pills is 50 mg once daily for 1-2 weeks. It is recommended to take the tablet in the morning, just before or after breakfast. The drug may cause sedation as an adverse effect. In those cases, Antabuse can be used before bedtime.

The recommended maintenance dose ranges from 125 to 500mg per day. The maximum daily dosage is 500mg.

The duration of the therapy is usually long-lasting and in some patients, it must last for years until a complete recovery is achieved and the patient does not become capable of self-controlling.

Drug Interaction

The following drugs used in the HIV therapy contain alcohol and should not be administered concurrently with Antabuse:

  • Ritonavir (brand names Norvir and Kaletra)
  • Amprenavir oral solution
  • Tipranavir capsules

Disulfiram should not be used at the same time with any of the following medicines:

  • Leflunomide and Teriflunomide – drugs used to treat multiple sclerosis relapse. The simultaneous administration of these medicines increases the risk of liver damage.
  • Benznidazole – an antiprotozoal agent used to treat American trypanosomiasis (Changas disease). The simultaneous administration of this medicine can lead to hallucinations, delusions, and other psychic reactions.
  • Lomitapide – a drug used to treat familial hypercholesterolemia. The simultaneous administration with this medicine increases the risk of liver damage.
  • Paraldehyde – a drug used to treat epileptic seizures. The concomitant administration with this medicament increases the risk of the Disulfiram reaction.
  • Sertraline oral solution – a drug used in the treatment of anxiety and depression. The oral solution of sertraline may contain alcohol, and the concomitant administration is not recommended.

Side Effects

Antabuse may cause the following side effects:

  • Eye pain
  • Mood changes
  • Dark-colored urine
  • Gray-colored stool
  • Severe abdominal pain
  • Nausea
  • Vomiting
  • Hepatitis
  • Drowsiness and sedation
  • Fatigue
  • Decreased libido
  • Headache
  • Metallic taste in the mouth
  • Peripheral neuritis
  • Psychotic reactions
  • Depression
  • Paranoia
  • Schizophrenia
  • Confusion
  • Memory impairment

Tell your doctor if you notice any above-mentioned adverse effects.

Important Note

In many cases, patients suffering from alcohol dependence do not want to be treated, and sometimes the family on its own initiative try to add Antabuse in patient’s meals/drinks without letting him/her know. Keep in mind that Disulfiram should never be given to patients without their knowledge, because there is a high chance that the patient will take alcohol while under the influence of this drug, and this may lead to adverse reactions (including death!).

Final Thoughts

Antabuse Disulfiram is probably the most effective treatment for alcohol dependence. However, its concomitant use with alcohol may lead to severe side effects, and patients using this drug must be aware of these adverse effects and take precautions accordingly.


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