Abstract

The first sulfonamide therapy was discovered by Domagk, who, in 1932, discovered that an orange-red sulfonamide dye named prontosil rubrum was safe and effective in curing streptococcal infections in mice. He confirmed the effectiveness of the dye through various experiments The discovery of the sulfonamides represented the first real breakthrough in selective antimicrobial therapy. The sulfonamides (Fig 1) are synthetic bacteriostatic antimicrobials with a wide spectrum against most Gram-positive and many Gram-negative organisms. The widespread use of sulfonamides as a result of their low cost has resulted in the development of many sulfonamide-resistant strains of bacteria. In general, the sulfonamides exert only a bacteristatic effect, and cellular and humoral defense mechanisms of the host are essential for the final eradication of the infection. The earliest report on the use of sulfapyridine in a noninfectious dermatologic disease was in 1939, when it was used to treat a patient with acrodermatitis of Hallopeau. 1 The age of antibacterial chemotherapy started in 1935 when Gerhard Domagk published his successful application of “Prontosil rubrum” in animals and humans to fight streptococcal infections. The chemical agent was the azo dye sulfachrysoidine. Shortly thereafter, it was shown by another European group that this dye is metabolized to the therapeutically active, colorless sulfanilamide. 2 Various chemical modifications of this parent sulfonamide compound yielded a great number of sulfonamides with a relatively constant antibacterial spectrum yet with a widely varying number of pharmacokinetic and toxicological properties. In the beginning, sulfonamides were grouped according to their half-time of elimination. Today, we distinguish middle- and long-acting and poorly absorbed sulfonamides. Typical middle-acting sulfonamides are sulfadiazine and sulfamethoxazole, and long-acting ones are sulfalene and sulfadoxine.

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