Dosing & Uses
Dosage Forms & Strengths
capsule
- 50mg
Leprosy
Indicated for treatment of lepromatous leprosy, including dapsone-resistant leprosy complicated by erythema nodosum leprosum
No longer commercially available in the United States; only available by obtaining an investigational new drug (IND), see Dosing Considerations
Preferably used in combination with 1 or more other antileprosy agents to prevent the emergence of drug resistance
Most patients today are treated with dapsone and rifampin, and, in multibacillary cases, clofazimine
Dapsone-sensitive multibacillary leprosy
- 50 mg PO qDay in combination with dapsone 100 mg/day and rifampicin 600 mg/day
- Administer for at least 2 years and continued, if possible, until negative skin smears are obtained
- At this time, monotherapy with an appropriate antileprosy drug can be instituted
- Well tolerated when dose does not exceed 100 mg/day
Dapsone-resistant leprosy
- 100 mg PO qDay in combination with 1 or more other antileprosy drugs for 3 years, followed by monotherapy with 100 mg of clofazimine daily
- Clinical improvement usually can be detected within 1-3 months of treatment and is usually clearly evident by the 6 months
Dosage Modifications
Erythema nodosum leprosum reactions
- Treatment depends on the severity of symptoms
- Basic antileprosy treatment should be continued, and if nerve injury or skin ulceration is threatened, corticosteroids should be given
- Where prolonged corticosteroid therapy becomes necessary, clofazimine administered at dosages of 100 to 200 mg daily for up to 3 months may be useful in eliminating or reducing corticosteroid requirements
- Dosages >200 mg/day are not recommended
- Taper dose to 100 mg/day as quickly as possible after the reactive episode is controlled
Hepatic impairment
- Child-Pugh Class A, B, and C: Avoid therapy unless benefit outweighs risk
Renal impairment
- Mild to moderate: Dose adjustment not necessary
- Severe: Use caution
Dosing Considerations
No longer commercially available in the United States
Clofazimine can be obtained by submitting an IND through the National Hansen’s Disease (Leprosy) Program (NHDP)
The prescriber is considered to be an investigator and must submit an FDA form 1572 and curriculum vitae to the National Hansen’s Disease Program from the U.S. Department of Health and Human Services
The institutional review board is provided by the Centers for Disease Control and Prevention Consent forms and other documents will be provided to the prescriber upon request
For more information, visit www.hrsa.gov/hansensdisease/ or call 1-800-642-2477
Tuberculosis (Orphan)
Orphan designation for treatment of active tuberculosis
Orphan sponsor
- Novartis Pharmaceuticals Corp; One Health Plaza, Bldg 135/409; East Hanover, NJ 07936-1080
Mycobacterial Infections (Orphan)
Orphan designation for treatment of pulmonary nontuberculous mycobacterial infections
Orphan sponsor
- Qrumpharma, Inc; 215 Decatur St; Doylestown, Pennsylvania 18901
Safety and efficacy not established; limit data are available from the National Hansen’s Disease (Leprosy) Program (NHDP)
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- ceritinib
ceritinib and clofazimine both increase QTc interval. Contraindicated.
- clarithromycin
clarithromycin and clofazimine both increase QTc interval. Contraindicated.
Serious - Use Alternative (11)
- adagrasib
adagrasib, clofazimine. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- entrectinib
clofazimine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole and clofazimine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.
- glasdegib
clofazimine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
- ivosidenib
ivosidenib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.
- lefamulin
lefamulin and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
- macimorelin
macimorelin and clofazimine both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.
- mobocertinib
mobocertinib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pitolisant
clofazimine and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- ribociclib
ribociclib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (25)
- amisulpride
amisulpride and clofazimine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended if coadministered.
- azithromycin
azithromycin increases toxicity of clofazimine by QTc interval. Modify Therapy/Monitor Closely.
- chloroquine
chloroquine increases toxicity of clofazimine by QTc interval. Modify Therapy/Monitor Closely.
- citalopram
citalopram and clofazimine both increase QTc interval. Use Caution/Monitor.
- crizotinib
crizotinib and clofazimine both increase QTc interval. Use Caution/Monitor.
- dofetilide
dofetilide increases toxicity of clofazimine by QTc interval. Modify Therapy/Monitor Closely.
- doxepin
doxepin and clofazimine both increase QTc interval. Use Caution/Monitor.
- escitalopram
escitalopram increases toxicity of clofazimine by QTc interval. Modify Therapy/Monitor Closely.
- fostemsavir
clofazimine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gadobenate
gadobenate and clofazimine both increase QTc interval. Use Caution/Monitor.
- gemifloxacin
gemifloxacin and clofazimine both increase QTc interval. Use Caution/Monitor.
- gemtuzumab
clofazimine and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- gilteritinib
gilteritinib and clofazimine both increase QTc interval. Use Caution/Monitor.
- lofexidine
clofazimine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.
- mirtazapine
mirtazapine and clofazimine both increase QTc interval. Use Caution/Monitor.
- osilodrostat
osilodrostat and clofazimine both increase QTc interval. Use Caution/Monitor.
- oxaliplatin
oxaliplatin will increase the level or effect of clofazimine by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.
- ozanimod
ozanimod and clofazimine both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- quizartinib
quizartinib, clofazimine. Either increases effects of the other by QTc interval. Modify Therapy/Monitor Closely. Monitor patients more frequently with ECG if coadministered with QT prolonging drugs.
- selpercatinib
selpercatinib increases toxicity of clofazimine by QTc interval. Use Caution/Monitor.
- sodium picosulfate/magnesium oxide/anhydrous citric acid
clofazimine decreases effects of sodium picosulfate/magnesium oxide/anhydrous citric acid by altering metabolism. Use Caution/Monitor. Coadministration with antibiotics decreases efficacy by altering colonic bacterial flora needed to convert sodium picosulfate to active drug.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of clofazimine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of clofazimine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- triclabendazole
triclabendazole and clofazimine both increase QTc interval. Use Caution/Monitor.
- voclosporin
voclosporin, clofazimine. Either increases effects of the other by QTc interval. Use Caution/Monitor.
Minor (1)
- rifampin
clofazimine decreases levels of rifampin by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
Adverse Effects
>10%
Skin discoloration (75-100%)
Gastrointestinal: Abdominal and epigastric pain, diarrhea, nausea, vomiting, GI intolerance (40%-50%)
Ichthyosis and dry skin (8-28%)
1-10%
Rash and pruritus (1-5%)
Ocular: Conjunctival and corneal pigmentation due to crystal deposits, dryness, burning, itching, irritation (>1%)
Discoloration of urine, feces, sputum, sweat (>1%)
Increased blood glucose (>1%) Increased ESR (>1%)
<1%
Skin: Phototoxicity, erythroderma, acneiform eruptions, monilial cheilosis
Body fluid discoloration and other skin reactions
Gastrointestinal: Bowel obstruction, GI bleeding, anorexia, constipation, weight loss, hepatitis, jaundice, eosinophilic enteritis, enlarged liver
Ocular: Diminished vision
Nervous: Dizziness, drowsiness, fatigue, headache, giddiness, neuralgia, taste disorder
Psychiatric: Depression secondary to skin discoloration
Laboratory: Elevated levels of albumin, serum bilirubin, and AST (SGOT), eosinophilia, hypokalemia
Ocular: Addition of maculopathy (bull’s eye retinopathy)
Other: Splenic infarction, thromboembolism, anemia, cystitis, bone pain, edema, fever, lymphadenopathy, vascular pain
Warnings
Contraindications
Contraindicated in patients with known hypersensitivity to clofazimine or any of the excipients of clofazimine
Cautions
Skin dryness and ichthyosis may occur; apply oil to skin may relieve this effect
Skin discoloration
- Causes orange-pink to brownish-black discoloration of skin, as well as discoloration of conjunctivae, tears, sweat, sputum, urine and feces in 75-100% of patients; advise patients that skin discoloration is likely to occur and may take several months or years to reverse after conclusion of therapy; other skin reactions associated with therapy include ichthyosis, dry skin and pruritus
- Advise patients regarding skin discoloration and monitor for depression or suicidal ideation during therapy (2 suicides reported)
Severe gastrointestinal symptoms
- Caution with GI problems (eg, abdominal pain and diarrhea)
- Dosages >100 mg daily should be given for as short a period as possible (<3 months) and only under close medical supervision
- Severe abdominal symptoms have necessitated exploratory laparotomies; rare reports have included splenic infarction, bowel obstruction, and GI bleeding; deaths reported with severe abdominal symptoms
- May accumulate in various organs as crystals, including mesenteric lymph nodes and histiocytes at lamina propria of intestinal mucosa, spleen and liver; deposition in intestinal mucosa may lead to intestinal obstruction that may necessitate exploratory laparotomy; splenic infarction, gastrointestinal bleeding, and death reported; ; doses > 100 mg daily should be given for as short period as possible < 3 months) and only under close medical supervision
- If patient complains of pain in abdomen, nausea, vomiting, or diarrhea, initiate appropriate medical assessment and reduce daily dose, increase dosing interval, or discontinue therapy
QT Prolongation
- Cases of Torsades de Pointes with QT prolongation reported in patients receiving dosage regimens containing > 100 mg daily or in combination with QT prolonging medications; for QT prolongation and Torsades de Pointes cases, patient must remain under medical surveillance; monitor electrocardiograms (ECGs) for QT prolongation and cardiac rhythm disturbances
- QT prolongation reported in patients receiving therapy in combination with bedaquiline at recommended dosage regimen for each drug; monitor ECGs if coadministered to patients receiving bedaquiline, and discontinue therapy if clinically significant ventricular arrhythmia noted or if QTcF interval is 500 ms or greater; if syncope occurs, obtain ECG to detect QT prolongation
Pregnancy & Lactation
Pregnancy Category: C
Crosses the human placenta; the skin of infants born to women who had received the drug during pregnancy was found to be deeply pigmented at birth
Lactation: Distributed in human breast milk; do not administer to breastfeeding women unless clearly indicated
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Exerts a slow bactericidal effect on Mycobacterium leprae (Hansen’s bacillus); inhibits mycobacterial growth and binds preferentially to mycobacterial DNA
Also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions; however, its precise mechanisms of action are unknown
Absorption
45-62% (PO): variable absorption rate in patients with leprosy
Serum concentration: 0.7-1 mcg/mL (100-300 mg/day)
Distribution
Highly lipophilic and tends to be deposited predominantly in fatty tissue and in cells of the reticuloendothelial system; taken up by macrophages throughout the body
Elimination
Half-life: 70 days (at steady state)
Excretion: Negligible in urine; small amount in feces and bile; small amount sputum, sebum, and sweat
Administration
Oral Administration
Take with meals
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