Disulfiram

Registered South African indications:

• Alcoholism

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to other thiuram compounds
• Porphyria
• Cardiac failure
• Coronary artery disease
• History of cerebrovascular accident
• Hypertension
• Severe personality disorder
• Suicidal risk or psychosis
• Consumption of alcohol
• Drug addiction
• Coadministration with chlorpromazine

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Respiratory disease
• Diabetes mellitus
• Hypothyroidism
• Epilepsy
• Cerebral damage
• Alcohol intake during treatment and within 14 days of disulfiram use
• Intake and use of alcohol containing products such as food, medicines and toiletries
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab

Adjunct in the treatment of chronic alcoholism

• Oral (tab): 200-400mg, dly (see additional prescriber points)

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Dissolve the whole or part of dispergette into a quarter glass of water or liquid

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Suspension should be drunk before it has had time to settle

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Dispergettes may be swallowed whole without chewing

Not established for use in children

Pregnancy

• Caution
• The use of disulfiram in the first trimester of pregnancy is not advised. The risk/benefit ratio in assessing adverse effects of alcoholism in pregnancy should be taken into account when considering the use of disulfiram in pregnant patients. There have been rare reports of congenital abnormalities in infants whose mothers have received disulfiram in conjunction with other medicines

Breastfeeding

• Caution; not recommended
• Should not be used. No information is available on whether disulfiram is excreted in breast milk. Its use during breastfeeding is not advised especially where there is a possibility of interaction with medicines that the baby may be taking

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended
  Start at lower end of dose range

Porphyria Information

• Probably porphyrinogenic (PRP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Psychotic reactions
• Depression
• Paranoia
• Schizophrenia
• Mania
• Reduction in libido
• Drowsiness (during initial treatment)
• Peripheral neuritis
• Optic neuritis
• Encephalopathy
• Fatigue (during initial treatment)
• Headache
• Restlessness
• Coma (DAR)
• Convulsions (DAR)
• Anxiety (DAR)
• Dizziness (DAR)

Cardiovascular Disorders

• Flushing (DAR)
• Palpitations (DAR)
• Hypotension (DAR)
• Hypertension (DAR)
• Chest pain (DAR)
• QT prolongation (DAR)
• ST depression (DAR)
• Arrhythmias (DAR)

Respiratory Disorders

• Hyperventilation (DAR)
• Respiratory depression (DAR)
• Dyspnoea
• Bronchospasm (DAR)

Gastrointestinal Disorders

• Nausea and vomiting
• Halitosis

Hepatobiliary Disorders

• Hepatic cell damage

Genitourinary Disorders

• Impotence

Endocrine and Metabolic Disorders

• Increased body temperature(DAR)
• Sweating (DAR)

Skin and Subcutaneous Tissue Disorders

• Prurititis (DAR)
• Urticaria (DAR)

Immune, Blood and Lymphatic System Disorders

• Blood dyscrasias
• Allergic dermatitis
• Methaemoglobinaemia
• Acetoanaemia

Sensory Disorders

• Taste disorders
• Blurred vision (DAR)

Others

• Body odour

*DAR : Adverse effects attributable to the Disulfiram- alcohol reaction

• Alcohol
• Alcohol containing products
• Monoamine oxidase inhibitors
• Barbiturates
• Alfentanil
• Rifampicin
• Centrally active agents
• Pimozide
• Anticonvulsants
• Chlorpromazine
• Amitriptyline
• Benzodiazipines
• Agents metabolised in the liver
• Phenytoin
• Theophylline
• Warfarin
• Pethidine
• Morphine
• Amphetamines
• Metronidazole
• Isoniazid
• Paraldehyde

• Liver function tests
• Full blood count
• Kidney function
• Blood glucose
• Blood lipid profile
• Blood protein
• Electrolytes

None routine. Specific cases may require

• Cardiac function

Dose can be given at longer intervals if desired, i.e; 400mg, 48hrly instead of 200mg, 24hrly.

Disulfiram is a thiuram derivative which blocks the oxidation of alcohol at the acetaldehyde stage, by irreversible inactivation of liver aldehyde dehydrogenase. The metabolism of alcohol is blocked, and intracellular acetaldehyde levels increase. High acetaldehyde cause uncomfortable symptoms collectively termed as the Disulfiram-alcohol reaction (DAR)  which include; flushing, throbbing in head and neck, nausea, vomiting, diaphoresis, thirst, palpitations, chest pain, dyspnea, hyperventilation, tachycardia, syncope, weakness, blurred vision, confusion, vertigo, and hypotension.

Tablet 400mg

• Antabuse (Teva Pharmaceuticals) originator