Drug information of Disulfiram

Mechanism of effect

Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage. During alcohol metabolism following Disulfiram intake, the concentration of acetaldehyde occurring in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. Accumulation of acetaldehyde in the blood produces a complex of highly unpleasant symptoms referred to hereinafter as the Disulfiram-alcohol reaction. This reaction, which is proportional to the dosage of both Disulfiram and alcohol, will persist as long as alcohol is being metabolized. Disulfiram does not appear to influence the rate of alcohol elimination from the body.

Pharmacodynamic

Disulfiram produces a sensitivity to alcohol which results in a highly unpleasant reaction when the patient under treatment ingests even small amounts of alcohol.

Pharmacokinetics

Disulfiram is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose). and is eliminated slowly from the body. One (or even two) weeks after a patient has taken his last dose of Disulfiram, ingestion of alcohol may produce unpleasant symptoms.metabolism: Hepatic.

Drug indications

an aid in the treatment and management of chronic alcoholism

Dosage

Usual Adult Dose for Alcohol Dependence
-Initial dose: 500 mg orally once a day (this dose is generally continued for the first 1 to 2 weeks)
-Maintenance dose: 250 mg orally once a day (range: 125 mg to 500 mg once a day) Maximum dose: 500 mg once a day
-Duration of therapy: Depending on the individual, therapy may last months or even years

Drug contraindications

hypersensitivity to drug or its components. , heart failure , cerebrovascular defects , Hypertension , coronary insufficiency , recently received metronidazole, paraldehyde, , recently receivedalcohol, or alcohol-containing pr , psychoses

Side effects

Headache , Dermatit , fatigue , peripheral neuritis , neuropathy , impotence , somnolence , hepatitis , metallic taste in mouth , Psychotic reactions

Interactions

Metronidazole , Atomoxetine , Aripiprazole , Amitriptyline , Aminophiline , Amiodarone , Aprepitant , Clarithromycin , Enzalutamide , Quinidine , Etoposide , Warfarin , Verapamil , Venlafaxine , Voriconazole , Carvedilol , Ketoconazole , Phenytoin , Fingolimod , Lovastatin , Mexiletine , Mitoxantrone , Nilotinib , Citalopram , Sildenafil , Cyclosporine , Fluvoxamine , Fluconazole , Phenobarbital , Tinidazole , Doxycycline , Dihydroergotamine , Diazepam , Diltiazem , Sertraline , Imatinib , Bupropion , Bortezomib , Bosentan , Posaconazole , Thalidomide , Ethosuximide , Erythromycin , Acetaminophen , Oxaliplatin , Itraconazole , Isoniazid , Amobarbital , ritonavir , Phenindione , Tipranavir , Paraldehyde , Lopinavir and Ritonavir , Remdesivir , Chlormethiazole , Dronabinol

Alerts

1-Disulfiram should never be administered to a patient when he is in a state of alcohol intoxication, or without his full knowledge. The physician should instruct relatives accordingly.
2- Because of the possibility of an accidental Disulfiram-alcohol reaction, Disulfiram should be used with extreme caution in patients with any of the following conditions: diabetes mellitus, hypothyroidism, epilepsy, cerebral damage, chronic and acute nephritis, hepatic cirrhosis or insufficiency.

Points of recommendation

1-Baseline and follow-up liver function tests (10-14 days) are suggested to detect any hepatic dysfunction that may result with Disulfiram therapy. In addition, a complete blood count and serum chemistries, including liver function tests, should be monitored.
2- Avoid alcohol for up to 14 days after treatment has been stopped.
3- Take without regard to meals.

Pregnancy level

Consult a physician before using