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Rosiglitazone Usage And Synthesis
Description Rosiglitazone is a type of thiazolidinedione antidiabetics. Thiazolidinedione are agonists for peroxisome-proliferator–activated receptor γ (PPAR-γ). PPAR-γ receptors are ligand-activated nuclear transcription factors that modulate gene expression, lowering blood glucose primarily by increasing insulin sensitivity in peripheral tissues.
Rosiglitazone is widely used to lower blood glucose levels in patients with type 2 diabetes mellitus. Rosiglitazone functionalizes by makes
the cells of the body more sensitive to the naturally produced insulin in body. It shouldn’t be used if the patient is injecting or inhaling insulin. Using rosiglitazone with insulin could increase the risk of heart failure.
Patients having heart failure with symptoms or moderate to severe heart failure should not use Rosiglitazone.
Rosiglitazone Medical uses
Rosiglitazone was approved by the US FDA in 1999 and by the EMEA in 2000; the EMEA however required two postmarketing studies on longterm adverse effects, one for chronic heart failure and the other for cardiovascular effects. The drug was approved for glycemic control in people with type 2 diabetes, as measured by glycosylated haemoglobin A1c (HbA1c) as a surrogate endpoint, similar to that of other oral antidiabetic drugs. The controversy over adverse effects has dramatically reduced the use of rosiglitazone.
Rosiglitazone Side effects:
There was no difference in all cause and vascular death in a meta-analysis of 4 trials against controls. Two meta-analyses of cohort studies found excess deaths against pioglitazone.
An retrospective observational study performed using Medicare data found that patients treated with rosiglitazone had a 27% higher risk of stroke compared to those treated with pioglitazone.
GlaxoSmithKline reported a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. The information was based on data from the ADOPT trial The same increase has been found with pioglitazone (Actos), another thiazolidinedione.
The risk of hypoglycaemia is reduced with thiazolidinediones when compared with sulfonylureas; the risk is similar to the risk with metformin (high strength of evidence).
Both thiazolidinediones cause a similar degree of weight gain to that caused by sulfonylureas (moderate strength of evidence).