IngentaConnect A century of the synthesis of dapsone: its anti-infective capacit...

Abstract:

Background

Although dapsone was first synthesized in 1908, a quarter of a century was to pass before it was used in the treatment of bacterial infections. Dapsone was, however, too toxic for humans (because of the excess dosage which was administered at that time) and was thus considered to be of no value in the treatment of common bacterial infections. Since the early 1950s, dapsone has been recognized as being uniquely effective against a number of noninfectious, inflammatory diseases and, today, this is its main indication. Thus, the reason why dapsone was first introduced into medicine, namely the treatment of bacterial infections, has been set aside and its main current applications are the treatment of noninfectious, inflammatory, autoimmune, and bullous diseases. Objective

To study the anti-infective capacity of dapsone against common bacterial infections. As many patients who receive dapsone for the treatment of noninfectious, inflammatory diseases have a concomitant bacterial infection or a superinfection of their skin disease, we thought that, if dapsone proved to be effective against common bacterial infections, it may obviate the need for an additional antimicrobial drug in these patients. Methods

Three bacterial ATCC> strains (Streptococcus pyogenes, Staphylococcus aureus, and Escherichia coli) were tested by a macrodilution minimal inhibitory concentration (MIC) test for dapsone. Dapsone concentrations were between 0.06 and 1125 μg/mL. Results

Even the highest concentration of dapsone of 1125 μg/mL did not inhibit bacterial growth. Conclusions

Our results indicate that dapsone has no antibacterial effects whatsoever. Even at very high concentrations, it does not suppress the growth of most susceptible strains of bacteria. The story of dapsone (i.e. the long time that elapsed between its synthesis to its use for the chemotherapy of infectious diseases) will not repeat itself this time.

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A century of the synthesis of dapsone: its anti-infective capacity now and then