Insulin resistance
and endothelial dysfunction are frequently comorbid
states. Insulin resistance is characterized by the
diminished ability of insulin to initiate
intracellular signaling. Endothelial cells are a
very active substrate, secreting mediators essential
in modulating vascular tone, inflammation,
haemostasis, cell proliferation and oxidative
stress. Endothelial dysfunction is defined as
inadequate endothelial-mediated vasodilatation. The
2007 European Society of Cardiology (ESC) and
European Association for the Study of Diabetes (EASD)
guide on pre-diabetes and cardiovascular disease
recommended following drugs for the insulin
resistance therapy: biguanides, thiazolidinediones
and alpha-glucosidase inhibitors. This article
discusses the choice of specific antihyperglycemic
agents targeting insulin resistance, not only for
their effectiveness in lowering glucose, but also
for their extraglycemic effects, especially on
endothelial dysfunction in order to reduce
cardiovascular complications. The choise of the
insulin sensitizing agent with the best
cardioprotective profile depends on duration and
complications of disease, safety profiles,
tolerability, ease of use and expense.
Key words: insulin resistance, insulin sensitizers,
endothelial dysfunction, cardiovascular disease.