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Cutaneous Adverse Events Caused by Sulfonamide-Containing Drugs: Reality or Perception?
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-02-24 , DOI: 10.1021/acs.jmedchem.9b01932
Falgun Shah 1 , Ian M Bell 2
Affiliation  

The term “sulfa allergy”, originally coined for the sulfonamide antibiotics, has become associated with any drugs that contain a sulfonamide moiety. This raises a question: should medicinal chemists avoid making sulfonamide-containing compounds in drug discovery programs? The negative perception of sulfonamides is not supported by any systematic study or data analysis. To address this gap, an analysis of postmarketing reports of cutaneous AEs for drugs with and without a sulfonamide group was conducted. The analysis revealed no evidence of association between the presence of a sulfonamide moiety and a high reporting rate of cutaneous AEs and indicated that the risk of such AEs was associated with the presence of certain structural alerts and higher daily doses. These results strongly suggest that sulfonamide-containing compounds are not at a higher risk of presenting with a cutaneous adverse drug reaction compared with non-sulfonamides and that medicinal chemists should not avoid use of the sulfonamide group.

中文翻译:

含磺胺类药物引起的皮肤不良事件:现实还是知觉?

最初为磺胺类抗生素所创造的“磺胺类过敏”一词已与包含磺酰胺部分的任何药物联系在一起。这就提出了一个问题:药物化学家应避免在药物开发计划中制造含磺酰胺的化合物吗?任何系统的研究或数据分析均不支持对磺胺类药物的否定看法。为了弥补这一差距,对具有或不具有磺酰胺基团的药物的皮肤AE上市后报告进行了分析。分析显示,没有证据表明存在磺酰胺部分与皮肤AE的报告率高相关,并表明此类AE的风险与某些结构警报和更高的每日剂量有关。
更新日期:2020-02-24
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