Dapsone: Targeted Antimicrobial and Anti-Inflammatory Therapy

Dapsone

Dapsone

Dapsone is used to treat leprosy (Hansen’s disease) and to help control a skin problem called dermatitis herpetiformis, and a fungal disease called Actinomycotic mycetoma.
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Dapsone is a synthetic sulfone antimicrobial agent with a well-established history in dermatology and infectious disease. Its primary mechanisms of action include bacterial folate synthesis inhibition and potent anti-inflammatory effects via neutrophil suppression. This dual functionality makes it a cornerstone therapy for specific dermatoses and certain infections, particularly those caused by Mycobacterium leprae. Its efficacy is backed by decades of clinical use and a robust understanding of its pharmacokinetic profile.

Features

  • Synthetic sulfone antimicrobial (diaminodiphenyl sulfone).
  • Available in oral tablet formulations (25 mg and 100 mg).
  • Demonstrated bactericidal and bacteriostatic activity.
  • Potent anti-inflammatory properties, specifically inhibiting neutrophil myeloperoxidase and chemotaxis.
  • High tissue penetration, particularly effective in the skin and nerves.

Benefits

  • Provides effective first-line treatment for all forms of leprosy (Hansen’s disease), halting disease progression and preventing disability.
  • Induces and maintains remission in dermatitis herpetiformis, offering significant relief from intense pruritus and blistering.
  • Serves as a effective steroid-sparing agent for various neutrophilic dermatoses, reducing long-term corticosteroid exposure.
  • Offers a proven therapeutic option for Pneumocystis jirovecii pneumonia (PJP) prophylaxis in immunocompromised patients, particularly those with sulfa allergies.
  • Manages acne vulgaris, especially inflammatory and cystic forms, when conventional therapies have failed.

Common use

Dapsone is indicated for the treatment of leprosy, always as part of a multi-drug therapy (MDT) regimen to prevent resistance. It is a first-line therapy for dermatitis herpetiformis, a cutaneous manifestation of celiac disease. It is also used off-label for a spectrum of inflammatory dermatoses, including linear IgA disease, subcorneal pustular dermatosis, and other neutrophil-mediated conditions. Its role in PJP prophylaxis is well-documented in HIV-positive patients and other immunocompromised states.

Dosage and direction

Dosage is highly indication-specific and must be individualized under strict medical supervision.

  • Leprosy (Multibacillary): 100 mg daily, unsupervised, plus other agents as per WHO MDT guidelines. Treatment duration is 12 months.
  • Leprosy (Paucibacillary): 100 mg daily, unsupervised, plus other agents. Treatment duration is 6 months.
  • Dermatitis Herpetiformis: Initial adult dose is typically 50 mg daily, titrated upward to a maintenance dose of 25-300 mg daily based on clinical response. The goal is the lowest effective dose.
  • PJP Prophylaxis: 100 mg daily or 50 mg twice daily. Tablets should be swallowed whole with a full glass of water. Administration with food may mitigate gastrointestinal upset.

Precautions

  • G6PD Deficiency Screening is Mandatory: Prior to initiation, all patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency due to the high risk of dose-related hemolysis and methemoglobinemia.
  • Complete Blood Count (CBC) Monitoring: Regular monitoring of CBC, including hemoglobin, is required, especially during the initial phase of therapy, to detect hemolytic anemia or agranulocytosis.
  • Peripheral Neuropathy: Cases of motor and sensory peripheral neuropathy have been reported; neurological assessments are advised during prolonged therapy.
  • Hepatic and Renal Function: Use with caution in patients with significant hepatic or renal impairment; dosage adjustment may be necessary.
  • Hypersensitivity Reactions: Monitor for signs of the “dapsone hypersensitivity syndrome” (fever, rash, lymphadenopathy, hepatitis), which requires immediate drug discontinuation.

Contraindications

  • Known hypersensitivity to dapsone or any component of the formulation.
  • Documented severe G6PD deficiency (absolute contraindication due to risk of severe hemolysis).
  • History of dapsone-induced agranulocytosis or aplastic anemia.

Possible side effect

Common and less severe side effects include:

  • Hemolytic anemia (dose-related, common in individuals with even partial G6PD deficiency).
  • Methemoglobinemia (can cause cyanosis, shortness of breath, fatigue).
  • Headache, nausea, vomiting, and dizziness.
  • Mild skin eruptions.

Serious adverse effects requiring immediate medical attention include:

  • Agranulocytosis and aplastic anemia.
  • Peripheral neuropathy.
  • Dapsone Hypersensitivity Syndrome (DHS): a severe, multi-system reaction featuring fever, rash, hepatitis, and eosinophilia.
  • Cholestatic jaundice and hepatitis.
  • Exfoliative dermatitis and toxic epidermal necrolysis.

Drug interaction

Dapsone has significant pharmacokinetic and pharmacodynamic interactions:

  • Probenecid: May increase dapsone levels by reducing renal excretion.
  • Rifampin: Significantly decreases plasma levels of dapsone by inducing its metabolism.
  • Trimethoprim: May increase levels of both drugs, potentiating the risk of adverse effects, particularly hematologic toxicity.
  • Didanosine: Concomitant use may reduce the absorption of dapsone.
  • Other Hemolytic Drugs: Concurrent use with other agents known to cause hemolysis or methemoglobinemia (e.g., nitrofurantoin, primaquine) increases toxic risk.

Missed dose

If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The patient should not double the dose to make up for the missed one. Maintaining a consistent dosing schedule is important for efficacy.

Overdose

Overdose exacerbates the drug’s primary toxicities. Symptoms include severe nausea, vomiting, hyperexcitability, cyanosis (from methemoglobinemia), and profound hemolytic anemia. Treatment is supportive and symptomatic. Gastric lavage or activated charcoal may be considered if ingestion was recent. Methylene blue is the specific antidote for methemoglobinemia. Management of severe hemolysis may require transfusion support.

Storage

Store dapsone tablets at controlled room temperature (20°C to 25°C or 68°F to 77°F). Keep the container tightly closed and protect from light and moisture. Keep all medications out of the reach of children and pets. Do not flush medications down the toilet or pour them into a drain unless instructed to do so.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“Dapsone has been a life-changing medication for my dermatitis herpetiformis. After years of suffering, it provided relief within weeks. The mandatory blood monitoring is a necessary inconvenience for the benefit it provides.” - Patient, 42

“As an infectious disease specialist, dapsone remains an invaluable component of our multidrug therapy for leprosy. Its efficacy is proven, and its safety profile is manageable with vigilant monitoring.” - Dr. A. Sharma, MD

“While effective for my patient’s neutrophilic dermatosis, we encountered a mild drop in hemoglobin that stabilized. It underscores the critical need for baseline G6PD testing and ongoing hematologic surveillance.” - Dermatologist, Clinical Practice