The antidiabetic effect and pharmacokinetic properties of glipizide. Comparison of a single dose with divided dose regime.
In 13 patients with maturity-onset diabetes mellitus which did not respond to diet therapy alone, serum concentration of glipizide, blood glucose (B-G) concentration, serum immunoreactive insulin (S-IRI) and plasma glycerol (P-G) were monitored hourly over 12 hours after placebo, an initial dose of glipizide (5 mg p.o.) and long-term treatment with glipizide (range 7.5--20 mg, mean 10.4), which produced fasting B-G of less than 8 mmol/l. During the long-term treatment, glipizide was given in a random, cross-over pattern, either as a single dose in the morning or as a three-part divided dose regime, in the same total daily amount. The duration of the immediate effects of glipizide on B-G, S-IRI and S-IRI/B-G was 9, 4.5 and 6.5 hours, respectively. The mean apparent half-life of glipizide was 4.1 hours, the mean distribution volume 0.13 l/kg and the mean plasma clearance 0.023 l/kg x h. The area under the concentration curve from 7.30 a.m. to 7.30 p.m. was 15% higher after the single dose regime. The serum levels of glipizide at 10 hours were only 30% lower than after the three-part divided dose regime. There were no significant differences between the single and divided dose regimes as regards B-G, S-IRI and S-IRI/B-G, although the mean B-G for the 12-hour period was somewhat lower after the former than after the latter (7.0 against 8.7 mmol/l).
D000368:Aged; D001786:Blood Glucose / Q000032:analysis; D002986:Clinical Trials as Topic; D003920:Diabetes Mellitus / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005913:Glipizide / Q000008:administration & dosage* / Q000097:blood; D005990:Glycerol / Q000097:blood; D006801:Humans; D007328:Insulin / Q000097:blood; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011897:Random Allocation; D013453:Sulfonylurea Compounds / Q000008:administration & dosage*
D001786:Blood Glucose; D007328:Insulin; D013453:Sulfonylurea Compounds; D005990:Glycerol; D005913:Glipizide