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Aldapsone

Aldapsone - General Information

Aldapsone is a water-soluble sulfone used as an antileprosy drug. It has been used with limited success in the treatment of dermatitis herpetiformis.

 

Pharmacology of Aldapsone

Aldapsone is a sulfonamide antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus.

 

Aldapsone for patients

Take the drug with a full glass of water on an empty stomach. Increase fluid intake to 2L/day. Store in a tight, light-sensitive container at room temperature. Avoid sunlight or use sunscreen to prevent burns (avoid sunscreens containing PABA), avoid over-the-counter medications unless directed by a physician. Notify your doctor of skin rash, sore throat, fever, mouth sores, unusual bruising, and bleeding.

 

Aldapsone Interactions

Sulfoxone may increase the effects of barbiturates, tolbutamide, and uricosurics. It may also interact with thiazides (increased thrombocytopenia), cyclosporine (increased nephrotoxicity), sulfonylurea agents (increased hypoglycemic response), warfarin (increased anticoagulant effect), methotrexate (decreased renal excretion of methotrexate), phenytoin (decreased hepatic clearance of phenytoin).

 

Aldapsone Contraindications

Treatment with sulfoxone is contraindicated in the following: hypersensitivity to sulfonamides and sulfonylureas, thiazide and loop diuretics, salicyclates, sunscreen with PABA, lactation, infants less than 2 months old, pregnancy at term, and porphyria.

 

Additional information about Aldapsone

Aldapsone Indication: For the treatment of leprosy and dermatitis herpetiformis
Mechanism Of Action: Aldapsone is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Sulfoxone
Synonyms: Sulfoxone Sodium; Sodium Sulfoxone; Sodium Aldesulphone; Aldesulfone Sodium; Adesulfone Sodium
Drug Category: Anti-Infectives; Anti-Bacterial Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Sulfoxone: Aldapsone; DDF; Diamidin; Diason; Diasone; Diasone Sodium; Diasone Sodium Enterab; Diazon; Novotrone;
Absorption: Rapidly absorbed.
Toxicity (Overdose): Oral, rat LD50: 7000 mg/kg
Protein Binding: 69%
Biotransformation: Hepatic.
Half Life: 3-8 hours
Dosage Forms of Aldapsone: Not Available
Chemical IUPAC Name: [[4-[4-(sulfinomethylamino)phenyl]sulfonylphenyl]amino]methanesulfinic acid
Chemical Formula: C14H16N2O6S3
Sulfoxone on Wikipedia: Not Available
Organisms Affected: Enteric bacteria and other eubacteria