Sulphamethazine

Tetrahydrobiopterin Biosynthesis as an Off-Target of Sulfa Drugs

“…Furthermore, sulfa drugs not inhibiting SPR also show diminished CNSrelated side effects. In early studies on the efficacy of sulfamethazine in treatment of labor pneumonia (73 patients), it was noted that "The striking difference, however, was that the patients never complained of the severe mental and physical depression which often accompanies sulfapyridine treatment" (25). CNS-related side effects have not been published for first-generation sulfonylureas tolbutamide and chlorpropamide and second-generation sulfonylurea glibenclamide.…”

Prognosis and treatment of pneumonia in children

“…Satisfactory results of treatment with sulphamezathine have recently been reported in the literature by Macartney et al (1942) and Morgan and Wylie-Smith (1943), also by Peters and Easby (1943), who reported one case of suppression of urine lasting one day in a child of two years, one case of transient haematuria and two cases of brawny oedema of the limbs; and by Jennings and Patterson (1942), who noted three children who developed rashes.…”

Pharmacology of Sulphonamides: Recent Work

“…Similarly as regards the penetration into the cerebrospinal fluid, if the concentration in the plasma is 1.0, that in the cerebrospinal fluid (when equilibrium is reached) is: r (Marshall and Litchfield, 1939; Sulphanladmide .. 0.7 1.0 Sadusk, Blake, and Seymour Sulphapyridinle .0.750. 1940;Banks, 1941;Long, 1941;Sulphathiazole .. 0.15-0.4 Reinhold, Flippin, Schwartz, Sulpadizine .. .5-08 J and Domm, 1941) Sulphadimethyl- (Macartney,Smith,Luxton, Ramsay, and Goldman, 1942) Sulphamerazine.. 0.3-0.7 (Murphy, Clark, and Flippin, 1943) (Probably the differences between the various compounds are due to the differing amounts " bound " to the plasma proteins; see below.) Actually the ratio (concentration in C.S.F./concentration in plasma) is lower than these figures during the earlier part of treatment, when the blood concentration is rising, and higher when administration of the drug is stopped and the blood concentration falls.…”

“…It is considered that these effects are probably due to lack of substances, such as folic acid, which are synthesized by the bacteria of the large bowel (Ashburn, Daft, Endicott, and Sebrell, 1942;Black, Overman, Elvehjem, and Link, 1942;Mackenzie, Mackenzie, and McCollum, 1941 Sprague, Kissinger, and Lincoln (1941), and by others, and introduced (as sulphamethazine) for clinical use by Macartney et al (1942). More soluble than sulphadiazine or sulphamerazine.…”