Rosiglitazone maleate

Asia Bio-Pharmaceutical Research Institute

Rosiglitazone maleate

Product name:Rosiglitazone maleate
Molecular Formula:C22H23N3O7S
Formula Weight:473.5
 Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
Some reports have found that rosiglitazone is associated with a increased risk of heart attacks, but other reports have not found a statistically significant increase. Concern about adverse effects has reduced the use of rosiglitazone despite its sustained effects on glycemic control. The drug is currently the subject of many lawsuits against GSK. Over 13,000 have been brought against the company due to the drug.
Rosiglitazone maleate is a thiazolidinedione insulin synergist. It can increase the sensitivity of liver, fat, muscle and other tissues to insulin, affect the activity of insulin receptor kinase, phosphorylation of insulin receptor, liver glucose metabolism and reduce the metabolism of systemic and local adipose tissue. Rosiglitazone can reduce blood sugar and triacylglycerol at the same time, but also can reduce or prevent diabetic nephropathy and islet cell degeneration.
The absorption of Rosiglitazone maleate by oral administration was good, and the absorption was not affected by food. The peak time of plasma drug concentration was 1h, and the plasma half-life was 3-4h. In liver metabolism, metabolites are excreted in combination, 60% in urine and 33% in faeces. Plasma drug concentration can be increased several times in patients with liver dysfunction.


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