Lepsone
Lepsone Uses, Dosage, Side Effects, Food Interaction and all others data.
Lepsone inhibits folic acid synthesis by preventing normal bacterial utilization of PABA (Para-aminobenzoic acid).
Lepsone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Lepsone is the principal drug in a multidrug regimen recommended by the World Health Organization for the treatment of leprosy. As an anti-infective agent, it is also used for treating malaria and, recently, for Pneumocystic carinii pneumonia in AIDS patients. Lepsone is absorbed rapidly and nearly completely from the gastrointestinal tract. Lepsone is distributed throughout total body water and is present in all tissues. However, it tends to be retained in skin and muscle and especially in the liver and kidney: traces of the drug are present in these organs up to 3 weeks after therapy cessation.
| Trade Name | Lepsone |
| Availability | Prescription only |
| Generic | Dapsone |
| Dapsone Other Names | DADPS, Dapsona, Dapsone, Dapsonum, Diaphenylsulfone |
| Related Drugs | prednisone, clindamycin, dexamethasone, sulfamethoxazole / trimethoprim, Bactrim, Decadron, rifampin, Bactrim DS, Deltasone, Cleocin |
| Weight | 100mg |
| Type | Tablet |
| Formula | C12H12N2O2S |
| Weight | Average: 248.301 Monoisotopic: 248.061948328 |
| Protein binding | 70 to 90% |
| Groups | Approved, Investigational |
| Therapeutic Class | Anti-Leprotic drugs |
| Manufacturer | Gaco Pharmaceuticals Ltd |
| Available Country | Bangladesh |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lepsone is used for Primary and secondary prophylaxis of Pneumocystis (carinii) jirovecii pneumonia, Multibacillary leprosy, Paucibacillary leprosy, Dermatitis herpetiformis, Acne
Lepsone is also used to associated treatment for these conditions: Acne Vulgaris, Bullous Systemic Lupus Erythematosus, Bullous dermatitis herpetiformis, Hansen's Disease, Pemphigus Vulgaris (PV), Relapsing Polychondritis, Mild Pneumocystis pneumonia, Mild Toxoplasma gondii encephalitis, Moderate Pneumocystis pneumonia, Moderate Toxoplasma gondii encephalitis, Refractory Idiopathic thrombocytopenic purpura
How Lepsone works
Lepsone acts against bacteria and protozoa in the same way as sulphonamides, that is by inhibiting the synthesis of dihydrofolic acid through competition with para-amino-benzoate for the active site of dihydropteroate synthetase. The anti-inflammatory action of the drug is unrelated to its antibacterial action and is still not fully understood.
Dosage
Lepsone dosage
Primary and secondary prophylaxis of Pneumocystis (carinii) jirovecii pneumonia:
- Adult: 50 mg daily, with pyrimethamine 50 mg once wkly. Alternatively, 100 mg with pyrimethamine 50 mg twice wkly.
- Child: 1 mth-18 yr: 2 mg/kg daily (max: 100 mg daily) or 4 mg/kg wkly (max: 200 mg wkly).
Multibacillary leprosy:
- Adult: 100 mg daily with clofazimine 50 mg daily, together with rifampicin 600 mg and clofazimine 300 mg once a mth for 12 mth.
- Child: and child 10-14 yr old: daily doses of dapsone 50 mg, or 1 to 2 mg/kg if their body-weight is low
Paucibacillary leprosy:
- Adult: 100 mg daily with 600 mg rifampicin once a mth, both given for 6 mth.
- Child: Reduce dose as for multibacillary leprosy.
Dermatitis herpetiformis:
- Adult: Initially, 50 mg daily increased gradually to 300 mg daily if required.
Side Effects
Anaemia, peripheral neuropathy, haemolysis and methaemoglobinaemia (dose-related), nephrotic syndrome, psychological changes, hepatitis. Others: Nausea, vomiting, anorexia, headache, maculopapular rash, toxic epidermal necrolysis, Stevens-Johnson syndrome. Topical: Dryness, redness, oiliness and peeling at application site.
Toxicity
Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.
Precaution
G6PD deficiency, methaemoglobin or Hb M. Perform regular blood counts and monitor liver function regularly. Pregnancy and lactation.
Interaction
Decreased serum conc of dapsone when used with rifampicin. Increased plasma conc with probenecid, trimethoprim. Antagonize clofazimine.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Lepsone Drug Interaction
Moderate: hydroxychloroquine, hydroxychloroquineUnknown: mycophenolate mofetil, mycophenolate mofetil, duloxetine, duloxetine, furosemide, furosemide, pregabalin, pregabalin, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, ondansetron, ondansetron, cetirizine, cetirizine
Lepsone Disease Interaction
Elimination Route
Bioavailability is 70 to 80% following oral administration.
Half Life
28 hours (range 10-50 hours)
Elimination Route
Renal
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Hypersensitivity. Severe anaemia, porphyria.
Acute Overdose
Symptoms: nausea, vomiting, hyperexcitability (within a few min to up to 24 hr later), methemoglobin-induced depression, haemolysis (7-14 days after ingestion), seizures and severe cyanosis.
Treatment: activated charcoal (20g four times daily) and haemolysis may enhance elimination of dapsone and its monoacetyl derivative. For patients without G6PD deficiency, methemoglobinemia may be treated with methylene blue 1-2 mg/kg given by slow IV injection (repeated if methemoglobin reaccumulates) or in less severe cases, 3-5 mg/kg every 4-6 hr orally.
Storage Condition
Tablet: Store between 15-30°C. Protect from light. Topical Gel: Store between 20-25°C. Do not freeze.
Innovators Monograph
You find simplified version here Lepsone
Lepsone contains Dapsone see full prescribing information from innovator Lepsone Monograph, Lepsone MSDS, Lepsone FDA label
