Gliflumide, a new oral antidiabetic of high potency and efficacy.
Gliflumide is an optically active sulfonylaminopyrimidine. In rats, the drug exhibited a long-lasting hypoglycemic effect following oral as well as intravenous administration. This effect resembled the action of glibenclamide, but was brought about by doses 5-10 times lower. In healthy volunteers, oral administration (0.0125 mg/kg) or intravenous injection (0.01mg/kg) of gliflumide resulted in a 30-40 per cent decrease of blood glucose characterized by slow onset and long duration. The stimulation of insulin secretion was studied after intravenous injection of gliflumide (0.01 mg/kg) and compared to the action of glibenclamide (0.01 mg/kg) and tolbutamide (10 mg/kg). Although the effect of these doses, measured by the area above the initial level, was similar, a different time course of action was found. Gliflumide and glibenclamide, compared with tolbutamide, produced a delayed and prolonged response. These characteristics were more pronounced with gliflumide. Maximal serum insulin levels were found after 3, 23, and 90 minutes for tolbutamide, glibenclamide, and gliflumide, respectively. In maturity-onset diabetics requiring glibenclamide or glibenclamide + biguanide, gliflumide was shown to have about the same efficacy as glibenclamide, the corresponding doses being 1.5-5 (generally 3) times lower.
D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D006224:Cricetinae; D004285:Dogs; D005230:Fatty Acids, Nonesterified / Q000097:blood; D005947:Glucose / Q000494:pharmacology; D005905:Glyburide / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000378:metabolism / Q000494:pharmacology*; D007275:Injections, Intravenous; D007328:Insulin / Q000097:blood / Q000378:metabolism; D000078790:Insulin Secretion; D007700:Kinetics; D011743:Pyrimidines / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013449:Sulfonamides / Q000378:metabolism / Q000494:pharmacology; D013806:Theophylline / Q000494:pharmacology; D014044:Tolbutamide / Q000494:pharmacology
D001786:Blood Glucose; D005230:Fatty Acids, Nonesterified; D007004:Hypoglycemic Agents; D007328:Insulin; D011743:Pyrimidines; D013449:Sulfonamides; D014044:Tolbutamide; D013806:Theophylline; D005947:Glucose; D005905:Glyburide