Initial phase II clinical studies on midaglizole (DG-5128). A new hypoglycemic agent.

Abstract

Midaglizole (DG-5128), 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine dihydrochloride sesquihydrate, is a new type of oral antidiabetic agent that has an alpha 2-adrenoceptor-antagonizing effect. As previously reported, midaglizole reduces plasma glucose, mainly by stimulation of insulin secretion, and inhibits epinephrine-induced platelet aggregation in normal human subjects. In this study, the clinical safety and efficacy of short-term administration of midaglizole were evaluated in 47 patients with non-insulin-dependent diabetes mellitus (NIDDM). After an observation period on diet or sulfonylurea treatment (1 patient was on insulin), patients received 150-250 mg 3 times a day of midaglizole for 2-4 wk, (some patients continued treatment for greater than 4 wk). In 20 of the patients first treated with diet and then switched to midaglizole treatment, fasting plasma glucose (FPG) decreased significantly from 187 +/- 10 mg/dl (mean +/- SE) to 147 +/- 13 mg/dl (P less than .05) and 120 +/- 6 mg/dl (P less than .01) 2 and 4 wk, respectively, after administration of midaglizole. Glycosylated hemoglobin (HbA1) also decreased from 12.0 +/- 0.7 to 11.3 +/- 1.1 and 10.7 +/- 0.6% after 2 and 4 wk, respectively. In 23 of the patients whose treatment was changed from sulfonylureas to midaglizole, FPG, and HbA1 levels were maintained at the same values obtained before administration of midaglizole. In patients treated with midaglizole for greater than 12 wk, FPG and HbA1 were kept at the lowered levels.(ABSTRACT TRUNCATED AT 250 WORDS)

• Authors: S Kawazu, M Suzuki, K Negishi, J Ishii, H Sando, H Katagiri, Y Kanazawa, S Yamanouchi, Y Akanuma, H Kajinuma
• Journal: Diabetes (Diabetes) Vol. 36 Issue 2 Pg. 221-6 (Feb 1987) ISSN: 0012-1797 [Print] United States
• PMID: 3803733 (Publication Type: Journal Article)

Chemical References

• Blood Glucose
• Glycated Hemoglobin A
• Hypoglycemic Agents
• Imidazoles
• midaglizole

Topics

• Administration, Oral
• Blood Glucose (metabolism)
• Diabetes Mellitus, Type 2 (drug therapy)
• Drug Evaluation
• Female
• Glucose Tolerance Test
• Glycated Hemoglobin (metabolism)
• Humans
• Hypoglycemic Agents (administration & dosage, therapeutic use)
• Imidazoles (administration & dosage, therapeutic use)
• Male
• Middle Aged
• Time Factors