Clofazimine: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Erythema nodosum leprosum (Type 2)

Adult: In combination with baseline antileprosy treatment and corticosteroids (as clinically indicated): 100-200 mg daily for up to 3 months. Gradually taper the dose to 100 mg daily as soon as possible after the reactive episode is controlled.

Oral
Multibacillary leprosy

Adult: Recommended regimen by World Health Organisation (WHO): As a 3-drug regimen: 300 mg clofazimine and 600 mg rifampicin, both given once a month with daily doses of 50 mg clofazimine and 100 mg dapsone. Treatment is given for 12 months. Refer to local treatment guidelines for other dosage regimen recommendations.
Child: 10-14 years Recommended regimen by WHO: As a 3-drug regimen: 150 mg clofazimine with 450 mg rifampicin and 50 mg dapsone once a month, taken with 50 mg dapsone daily and 50 mg clofazimine on alternate days. Treatment is given for 12 months. Refer to local treatment guidelines for other dosage regimen recommendations.

Oral
Dapsone-resistant leprosy

Adult: 100 mg daily in combination with 1 or more other antileprosy agents for 3 years, then continue as a monotherapy at 100 mg daily.

Administration

Should be taken with food.

Special Precautions

Patient with gastrointestinal disorders, including diarrhoea and abdominal pain; risk factors for QT prolongation; history of depression. Hepatic and severe renal impairment. Pregnancy and lactation.

Adverse Reactions

Significant: Torsades de pointes with QT prolongation; accumulation of crystals in organs, including intestinal mucosa, spleen, and liver; discolouration of the skin, conjunctivae, and body fluids (e.g. sweat, tears, breast milk, sputum, urine, faeces); depression (due to skin discolouration); photosensitivity. Rarely, suicidal ideation.
Eye disorders: Burning sensation, dryness, pruritus, and irritation of eyes.
Gastrointestinal disorders: Abdominal or epigastric pain, nausea, vomiting, diarrhoea.
General disorders and administration site conditions: Fatigue.
Investigations: Increased blood glucose and erythrocyte sedimentation rate (ESR).
Nervous system disorders: Headache, dizziness, drowsiness.
Skin and subcutaneous tissue disorders: Ichthyosis, dry skin, pruritus, rash.
Potentially Fatal: Splenic infarction, gastrointestinal bleeding.

Patient Counseling Information

Avoid prolonged exposure to sunlight. Contact lenses may be stained; remove contact lenses during treatment.

Monitoring Parameters

Perform pregnancy test before initiation of treatment. Monitor LFTs and serum creatinine periodically; ECG. Assess for gastrointestinal symptoms, skin discolouration, and depression or suicidal ideation.

Drug Interactions

Increased risk of additive torsades de pointes and QT prolongation with other agents known to prolong QT interval (e.g. bedaquiline). May increase the serum concentrations of CYP3A4/5 substrates.

Food Interaction

Absorption may be increased with food.

Action

Description:
Mechanism of Action: Clofazimine, an antimycobacterial agent with anti-inflammatory and immunosuppressive effects. Its exact mechanism is not yet known; however, it appears to inhibit mycobacterial replication and growth by binding into the DNA of Mycobacterium leprae.
Pharmacokinetics:
Absorption: Variably and incompletely (45-70%) absorbed from the gastrointestinal tract. Increased absorption with food.
Distribution: Primarily deposited into fatty tissues and reticuloendothelial cells, including macrophages. Distributed to most tissues and organs (except the brain and CSF). Crosses the placenta and enters breast milk.
Excretion: Mainly via faeces (as unchanged drug); urine (approx 1% as unchanged drug and metabolites); sebaceous or sweat glands and sputum (small amounts). Elimination half-life: Approx 25 (range: 6.5-160) days.

Chemical Structure

Storage

Store at 25°C. Protect from moisture.

MIMS Class

Antileprotics / Anti-TB Agents

ATC Classification

J04BA01 - clofazimine ; Belongs to the class of drugs used in the systemic treatment of lepra.

References

Anon. Clofazimine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/08/2020.

Anon. Clofazimine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/08/2020.

Buckingham R (ed). Clofazimine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/08/2020.

Clofazimine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 04/08/2020.

Joint Formulary Committee. Clofazimine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/08/2020.

Lamprene Capsules (Novartis Pharmaceuticals Corporation). U.S. FDA. https://www.fda.gov/. Accessed 04/08/2020.

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