[Rosiglitazone(BRL-49653)].
Rosiglitazone(RSG) is an oral antidiabetic agent of the thiazolidinedion(TDZ) class that exerts its antihyperglycemic effect by reducing insulin resistance. Actions of TDZs is thought to be mediated primarily through activating the nuclear receptor peroxisome proliferator activated receptor-gamma (PPAR-gamma). RSG has a higher affinity for PPAR-gamma than troglitazone or pioglitazone and the in vivo antidiabetic potency of RSG is correlated with its high biding affinity. In animal models of insulin resistance, RSG decreased plasma glucose, triglyceride and insulin levels and also prevented diabetic nephropathy and pancreatic islet cell degeneration. In clinical study, RSG, alone or in combination with other diabetic agents(metformin or sulphonylurea), produces significant improvements in HbA1c levels with type 2 diabetes mellitus. Attention should be paid on liver function in patients taking RSG.
Yonezawa
N
N
Third Department of Internal Medicine, Yamaguchi University School of Medicine.
Oka
Y
Y
D000818:Animals; D018849:Controlled Clinical Trials as Topic; D003920:Diabetes Mellitus / Q000188:drug therapy / Q000503:physiopathology; D004359:Drug Therapy, Combination; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology / Q000627:therapeutic use; D050356:Lipid Metabolism; D011972:Receptor, Insulin; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000378:metabolism; D000077154:Rosiglitazone; D013844:Thiazoles / Q000494:pharmacology / Q000627:therapeutic use; D045162:Thiazolidinediones; D014157:Transcription Factors / Q000819:agonists / Q000378:metabolism
D007004:Hypoglycemic Agents; D018160:Receptors, Cytoplasmic and Nuclear; D013844:Thiazoles; D045162:Thiazolidinediones; D014157:Transcription Factors; D000077154:Rosiglitazone; D011972:Receptor, Insulin