clofazimine (Rx)

Brand and Other Names:Lamprene
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Dosing & Uses

AdultPediatric

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)

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Interactions

Interaction Checker

and clofazimine

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (2)

            • ceritinib

              ceritinib and clofazimine both increase QTc interval. Contraindicated.

            • clarithromycin

              clarithromycin and clofazimine both increase QTc interval. Contraindicated.

            Serious - Use Alternative (10)

            • 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 (19)

            • 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.

            • deutetrabenazine

              clofazimine and deutetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely. For patients requiring deutetrabenazine doses >24 mg/day and are taking other drugs known to prolong QTc, assess the QTc interval before and after increasing the dose of deutetrabenazine or other medications known to prolong QTc.

            • dofetilide

              dofetilide increases toxicity of clofazimine by QTc interval. Modify Therapy/Monitor Closely.

            • 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.

            • gemtuzumab

              clofazimine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

            • lofexidine

              clofazimine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

            • 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.

            • 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.

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            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

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            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
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            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.

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            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

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            Administration

            Oral Administration

            Take with meals

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            A Patient Handout is not currently available for this monograph.
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            Formulary

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.