In patients with hypertension and other diseases treated with thiazide derivatives for hypotensive and diuretic purposes, we observed decreased glucose tolerances in comparison with those before treatment. When thiazide diuretics were withdrawn, glucose tolerances were found to recover rapidly to normal. Oral tolbutamide test in these cases showed the blood sugar response curves between those i...

Correct orientation of the amino and carboxyl groups and of the bicyclic ring of the compound 2-aminonorbornane-2-carboxylic acid is essential for its induction of a tolbutamide-potentiated hypoglycemia in the rat, an effect which we have already shownto arise from stimulation of insulin release. Only that isomer with its carboxyl group ~xo and the absolute configuration 12, 2S, 4S has this act...

A clinical case of hypoglycemia was reported. Hypoglycemia in this case was characterized by delayed recovery and low stationary values of blood sugar in insulin and tolbutamide tests. Since the results of glucose tolerance test in this case met precisely the diagnostic criteria of early diabetes described by Seltzer et al., a possible relation between hypoglycemia and early diabetes was discus...

Abnormality in glucose tolerance appears to correlate with arteriosclerotic disease, even when the abnormality is quite mild. Though there is no evidence for prevention of these vascular problems by correction of the carbohydrate abnormality, it seems reasonable to attempt such a correction in an investigational setting. We have used sulfonylurea (tolbutamide, chlorpropamide) in children and yo...

We have conducted short-term and prolonged studies in normal men and in diabetic subjects to compare the physiological properties of chlorpropamide and tolbutamide. The primary objectives of the investigation were: first, to correlate the hypoglycemic effect with the serum sulfonylurea level for each compound; and, second, to compare the rates of disappearance of the two drugs from the blood. I...

We describe a new class of NO-donor hypoglycemic products obtained by joining tolbutamide, a typical hypoglycemic sulfonylurea, with a NO-donor moiety through a hard link. As NO-donors we chose either furoxan (1,2,5-oxadiazole 2-oxide) derivatives or the classical nitrooxy function. A preliminary biological characterization of these compounds, including stimulation of insulin release from cultu...

The purpose of the present study was to evaluate the enhancement of tolbutamide (TBM) oral bioavailability and hypoglycaemic activity through complexation with beta-cyclodextrin (beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD). TBM and its freeze-dried inclusion complexes were administered to rabbits (New zealand breed; n=6), in a dose of 20 mg/kg. TMB plasma levels were measured by H...