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

Brands, Medical Use, Clinical Data

Drug Category

• Anti-Infectives
• Anti-bacterial Agents

Dosage Forms

• Tablet

Brands / Synonyms

Adesulfone Sodium; Aldapsone; Aldesulfone Sodium; DDF; Diamidin; Diason; Diasone; Diasone Sodium; Diasone Sodium Enterab; Diazon; Novotrone; Sodium Aldesulphone; Sodium Sulfoxone; Sulfoxone Sodium

Indications

For the treatment of leprosy and dermatitis herpetiformis

Pharmacology

Sulfoxone 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.

Mechanism of Action

Sulfoxone 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.

Absorption

Rapidly absorbed.

Toxicity

Oral, rat LD₅₀: 7000 mg/kg

Biotrnasformation / Drug Metabolism

Hepatic.

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.

Drug 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).