설파피리딘

개요Sulfapyridine is a sulfonamide antibiotic with antibacterial and anti-inflammatory activities. It is also a metabolite of sulfasalazine formed through bacterial conversion in the colon. It is active against strains of Y. enterocolitica and Salmonella (MICs = 3.1-25 and 25-100 μg/ml, respectively), as well as S. aureus (MBC = 0.8 μM). It is an inhibitor of recombinant P. carinii dihydropteroate synthetase (DHPS; IC50 = 0.18 μM). Sulfapyridine scavenges peroxyl radicals in an oxygen radical absorbance capacity (ORAC) assay. It inhibits histamine release induced by compound 48/80 from isolated rat peritoneal mast cells in a dose-dependent manner. Sulfapyridine (1 μg/kg) also inhibits compound 48/80-induced systemic allergic reaction in rats. Formulations containing sulfapyridine have previously been used in the treatment of dermatological conditions and ulcerative colitis.

용도Used in treatment of dermatitis herpetiformis; antibacterial.

일반 설명Sulfapyridine’s plasma half-life is 9 hours.This compound is a white, crystalline, odorless, and tastelesssubstance. It is stable in air but slowly darkens on exposureto light. It is soluble in water (1:3,500), in alcohol(1:440), and in acetone (1:65) at 25°C. It is freely soluble indilute mineral acids and aqueous solutions of sodium andpotassium hydroxide. The pKa is 8.4. Its outstanding effectin curing pneumonia was first recognized by Whitby; however,because of its relatively high toxicity, it has been supplantedlargely by sulfadiazine and sulfamerazine. Severalcases of kidney damage have resulted from acetylsulfapyridinecrystals deposited in the kidneys. It also causes severenausea in most patients. Because of its toxicity, it is usedonly for dermatitis herpetiformis.Sulfapyridine was the first drug to have an outstandingcurative action on pneumonia. It gave impetus to the studyof the whole class of N1 heterocyclically substituted derivativesof sulfanilamide.