Phthalylsulfathiazole (also known assulfathalidine)[1] is a sulfonamidebroad-spectrum antimicrobial used primarily for treating gastrointestinal infections.[2][3]
Phthalylsulfathiazole is indicated for treating various intestinal conditions, includingdysentery,colitis,gastroenteritis, and for preoperative preparation in intestinal surgery.[2][4] It may be administered in combination with other antimicrobials such asmetronidazole,furazolidone, orneomycin for enhanced efficacy.[3]
Like all antibiotics, phthalylsulfathiazole should be carefully monitored to avoid promotingbacterial resistance.[3]
Phthalylsulfathiazole is typically given orally in tablet form to target intestinal infections directly.[2] Due to thephthalic acid substitution on the aniline nitrogen, it remains unabsorbed in the bloodstream, focusing its action within the gut.[5]
Phthalylsulfathiazole acts by competitive antagonism withpara-aminobenzoic acid, inhibiting thedihydropteroate synthetase enzyme crucial fordihydrofolic acid synthesis. This inhibition disruptspurine andpyrimidine synthesis, impairing bacterial growth and reproduction.[8] Once in the large intestine, phthalylsulfathiazole hydrolyzes to release sulfathiazole, the active antimicrobial component.[9]
^Askue WE, Tufts E (April 1954). "Phthalylsulfathiazole (sulfathalidine) in the treatment of enterobiasis (pinworm infection)".The Journal of Pediatrics.44 (4):380–385.doi:10.1016/s0022-3476(54)80210-1.PMID13152646.
^abc"Phthalylsulfathiazole".PubChem. National Center for Biotechnology Information (NCBI), U.S. National Library of Medicine. Retrieved1 November 2024.
^Prescott JF (2013-09-20). "Sulfonamides, Diaminopyrimidines, and Their Combinations". In Giguère S, Prescott JF, Dowling PM (eds.).Antimicrobial Therapy in Veterinary Medicine (1st ed.). Wiley. pp. 279–294.doi:10.1002/9781118675014.ch17.ISBN978-0-470-96302-9.
^Turell R, Vallecillo LA, Paradny R, Danza AL (October 1955). "Preoperative preparation of the colon with sulfonamides or antibiotics".The Surgical Clinics of North America.35 (Nationwide No):1211–1220.doi:10.1016/s0039-6109(16)34682-5.PMID13267698.
^Varenina I, Bilandžić N, Kolanović BS, Božić Đ, Sedak M, Đokić M, et al. (2 March 2016). "Validation of a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of sulfonamides, trimethoprim and dapsone in muscle, egg, milk and honey".Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment.33 (4):656–667.doi:10.1080/19440049.2016.1152569.PMID26933907.
^Rohilla S, Sharma D (January 2023). "Sulfonamides, quinolones, antiseptics, and disinfectants.".Medicinal Chemistry of Chemotherapeutic Agents. Academic Press. pp. 21–63.doi:10.1016/B978-0-323-90575-6.00015-6.