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Sulfonamides Revisited, With an Emphasis on Dapsone

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The sulfonamide moiety is a remarkable structure giving rise to diverse drugs in arious therapeutic areas such as antibiotics, antidiabetics, diuretics and anti-inflammatory agents. In regards to antibiotics, sulfonamides are in common use as antifungals (P. jiroveci), antiparasitics (toxoplasmosis, cyclospora, isospora, malaria) antibacterials (including against nocardia and certain ones causing STDs) Continue reading Sulfonamides Revisited, With an Emphasis on Dapsone→

A Patch? YES – A Fix? NO: This Emperor Has No Clothes

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The NIH Department of HHS released its Final Rule on “Clinical Trials Registration and Results Information Submission” [1]. This Rule is meant to address frustrating maintenance and compliance issues in the ClinicalTrials.gov database, especially the results reporting section which has been neglected or totally ignored, (we commented on this in Continue reading A Patch? YES – A Fix? NO: This Emperor Has No Clothes→

Timely New Information on Next-Generation Tetracyclines – Part 2: Eravacycline and Protein Binding

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A recent paper by Thabit describes a curious finding [1]. The authors measured total and free (i.e., nonprotein-bound) eravacycline levels at ascending doses in a mouse model. They found strikingly small increases in free drug levels when titrating up total doses. The effect was rather dramatic: an increase in protein binding from 12% Continue reading Timely New Information on Next-Generation Tetracyclines – Part 2: Eravacycline and Protein Binding→