Impact of rosiglitazone on beta-cell function, insulin resistance, and adiponectin concentrations: results from a double-blind oral combination study with glimepiride

Rosiglitazone and glimeperide: review of clinical results supporting a fixed dose combination

“…Next to the reported effects on glucose control, rosiglitazone provided an additional beneficial effect on insulin resistance and β-cell function leading to lower HOMA IR scores, lower values for insulin, and intact proinsulin, and a more pronounced increase in adiponectin values. These results supported the clinical rationale of combining rosiglitazone with sulfonylurea drugs in patients with type 2 diabetes (Pfützner et al 2006a). …”

“…TZDs activate the nuclear peroxisome proliferator-activated receptor (PPAR)γ, which is expressed predominately in adipose tissue and regulates the gene transcription involved in adipocyte differentiation and glucose and lipid metabolism (Kersten et al 2000; Schoonjans et al 2000; Debril et al 2001). The metabolic effects of PPARγ activation by rosiglitazone comprise an increase in peripheral insulin sensitivity in muscle, liver, and adipose tissue (Hallsten et al 2002; Wagstaff et al 2002), improvement of postprandial and fasting glucose concentrations as well as long-term glucose control, improvement of adipogenesis leading to an increase in HDL cholesterol (Wagstaff et al 2002), reduction of vascular inflammation (Natali et al 2004), improvement of arterial elasticity (Shargorodsky et al 2003), and a reduction of laboratory markers for cardiovascular risk (Haffner et al 2002; Marx et al 2003a, b; Mohanty et al 2004; Pfützner et al 2006a). …”

“…Rosiglitazone positively affects CV risk markers, reducing plasmatic concentration of C-reactive protein (PCR-), matrix metallo-proteinases (MMP-9), tumor necrosis factor-alpha (TNF-alpha), serum amyloid, and soluble CD40L in type 2 diabetic patients with and without coronary disease (Wellington 2005). These effects seem to be conserved when rosiglitazone is used in combination with glimepiride (Pfützner et al 2006a) and both drugs are, therefore, interesting candidates also for multiple component therapies, especially when a fixed-dose combination of rosiglitazone and glimepiride may help to reduce the number of daily tablets.…”

Association of high-sensitive C-reactive protein with advanced stage β-cell dysfunction and insulin resistance in patients with type 2 diabetes mellitus

“…However, prospective studies using the same diagnostic markers as used in our current analysis have provided evidence of a beneficial impact of other therapeutic interventions compared to sulfonylurea therapy. Treatment of insulin resistance, e.g., using PPARg agonists seems to be an effective measure for decreasing cardiovascular and metabolic risk (29)(30)(31)(32).…”

A new type of orally active anti-diabetic Zn(II)-dithiocarbamate complex

“…In order to identify anti-diabetic drugs, most researchers have investigated organic compounds (Holman et al, 1999;Lechleitner et al, 2005;Pfutzner et al, 2006). However, these compounds sometimes produce severe side effects such as hypoglycemia, bloating sensation, and hepatic toxicity (Tos et al, 2000;Isley, 2003).…”