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Active ingredient: Dapsone - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Leprostatic Agents
  • Antimalarials
  • Anti-inflammatory Agents
  • Anti-Infectives
  • Antimycobacterials

Dosage Forms

  • Tablet

Brands / Synonyms

Acedapsone; Araldite Ht; Avlosulfon; Avlosulfone; Avlosulphone; Croysulfone; Croysulphone; DADPS; Dapson; Dapsone; Dapsonum; DDS; Dds, Diaphenylsulfone; Dds, Pharmaceutical; Diaminodifenilsulfona; Diaminodiphenyl Sulfone; Diaphenylsulfon; Diaphenylsulfone; Diaphenylsulphon; Diaphenylsulphone; Dimitone; Diphenasone; Diphone; Disulone; DSS; Dubronax; Dumitone; Eporal; ICI; Maloprim; Metabolite C; N, N'-Diphenyl Sulfondiamide; Normet; Novophone; P, P'-Sulfonyldianiline; P,P'-Diaminodiphenyl Sulfone; P,P-Diaminodiphenyl Sulphone; P,P-Sulfonylbisbenzamine; P,P-Sulfonylbisbenzenamine; P,P-Sulphonylbisbenzamine; P,P-Sulphonylbisbenzenamine; P,P-Sulphonyldianiline; P-Aminophenyl Sulfone; Recolip; Sulfadione; Sulfanona-Mae; Sulfon-Mere; Sulfona; Sulfona-Mae; Sulfone Ucb; Sulfonyldianiline; Sulphadione; Sulphon-Mere; Sulphonyldianiline; Sumicure S; Tarimyl; Udolac

Indications

For the treatment and management of leprosy and dermatitis herpetiformis

Pharmacology

Dapsone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Dapsone 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. Dapsone is absorbed rapidly and nearly completely from the gastrointestinal tract. Dapsone 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.

Mechanism of Action

Dapsone 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.

Absorption

Not Available

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

ACZONEÔ Gel, 5%, is contraindicated in persons with a hypersensitivity to dapsone or any other component of the formulation.

Drug Interactions

A drug-drug interaction study evaluated the effect of the use of ACZONE Gel, 5%, in combination with double strength (160 mg/800 mg) trimethoprim/sulfamethoxazole (TMP/SMX). During co-administration, systemic levels of TMP and SMX were essentially unchanged. However, levels of dapsone and its metabolites increased in the presence of TMP/SMX. Systemic exposure (AUC0-12) of dapsone and N-acetyl-dapsone (NAD) were increased by about 40% and 20% respectively in presence of TMP/SMX. Notably, systemic exposure (AUC0-12) of dapsone hydroxylamine (DHA) was more than doubled in the presence of TMP/SMX. Exposure from the proposed topical dose is about 1% of that from the 100 mg oral dose, even when co-administered with TMP/SMX.

Certain concomitant medications (such as rifampin, anticonvulsants, St. Johnís wort) may increase the formation of dapsone hydroxylamine, a metabolite of dapsone associated with hemolysis. With oral dapsone treatment, folic acid antagonists such as pyrimethamine have been noted to possibly increase the likelihood of hematologic reactions.

 

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