Phthalylsulfathiazole Explained

Phthalylsulfathiazole (also known as sulfathalidine)[1] is a sulfonamide broad-spectrum antimicrobial used primarily for treating gastrointestinal infections.[2] [3]

Medical uses

Phthalylsulfathiazole is indicated for treating various intestinal conditions, including dysentery, colitis, gastroenteritis, and for preoperative preparation in intestinal surgery.[4] It may be administered in combination with other antimicrobials such as metronidazole, furazolidone, or neomycin for enhanced efficacy.

Like all antibiotics, phthalylsulfathiazole should be carefully monitored to avoid promoting bacterial resistance.

Available forms

Phthalylsulfathiazole is typically given orally in tablet form to target intestinal infections directly. Due to the phthalic acid substitution on the aniline nitrogen, it remains unabsorbed in the bloodstream, focusing its action within the gut.[5]

Adverse Effects

Common side effects include nausea, stomach upset, and skin rash.[6] Rare but serious adverse effects may involve vitamin B deficiency, agranulocytosis, or aplastic anemia.[7]

Mechanism of action

Phthalylsulfathiazole acts by competitive antagonism with para-aminobenzoic acid, inhibiting the dihydropteroate synthetase enzyme crucial for dihydrofolic acid synthesis. This inhibition disrupts purine and pyrimidine synthesis, impairing bacterial growth and reproduction.[8] Once in the large intestine, phthalylsulfathiazole hydrolyzes to release sulfathiazole, the active antimicrobial component.[9]

Notes and References

  1. Askue WE, Tufts E . Phthalylsulfathiazole (sulfathalidine) in the treatment of enterobiasis (pinworm infection) . The Journal of Pediatrics . 44 . 4 . 380–385 . April 1954 . 13152646 . 10.1016/s0022-3476(54)80210-1 .
  2. Web site: Phthalylsulfathiazole . 1 November 2024 . . National Center for Biotechnology Information (NCBI), U.S. National Library of Medicine .
  3. Web site: Phthalylsulfathiazole . live . https://web.archive.org/web/20240623000716/https://go.drugbank.com/drugs/DB13248 . 23 June 2024 . 1 November 2024 . . University of Alberta.
  4. Deng Z, Li X, Shi Y, Lu Y, Yao W, Wang J . A Novel Autophagy-Related IncRNAs Signature for Prognostic Prediction and Clinical Value in Patients With Pancreatic Cancer . Frontiers in Cell and Developmental Biology . 8 . 606817 . 14 December 2020 . 33384999 . 7769875 . 10.3389/fcell.2020.606817 . free .
  5. Book: Prescott JF . Sulfonamides, Diaminopyrimidines, and Their Combinations . 2013-09-20 . Giguère S, Prescott JF, Dowling PM . Antimicrobial Therapy in Veterinary Medicine . 279–294 . 1st . Wiley . en . 10.1002/9781118675014.ch17 . 978-0-470-96302-9 .
  6. Web site: Singh P . Preetha SM . Side effect(s) of Phthalylsulfathiazole . Medindia .
  7. Turell R, Vallecillo LA, Paradny R, Danza AL . Preoperative preparation of the colon with sulfonamides or antibiotics . The Surgical Clinics of North America . 35 . Nationwide No . 1211–1220 . October 1955 . 13267698 . 10.1016/s0039-6109(16)34682-5 .
  8. Varenina I, Bilandžić N, Kolanović BS, Božić Đ, Sedak M, Đokić M, Varga I . 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 . 2 March 2016 . 26933907 . 10.1080/19440049.2016.1152569 .
  9. Book: Rohilla S, Sharma D . Sulfonamides, quinolones, antiseptics, and disinfectants. . Medicinal Chemistry of Chemotherapeutic Agents . January 2023 . 21-63 . Academic Press . 10.1016/B978-0-323-90575-6.00015-6 .

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