Abstract
Gliflozins are a new pharmacological class of drug approved to treating patients with type 2 diabetes and act by inhibiting the sodium-glucose co-transporter 2 (SGLT2) on the epithelial cells of the proximal convoluted tubule of the kidneys. Cardiovascular diseases (CVDs) are a major challenge in the management of type 2 diabetes mellitus, and Gliflozins have shown to improve cardiovascular and renal outcomes in subjects with type 2 diabetes presenting cardiovascular diseases. The mechanism by which cardiovascular protection is attributed to gliflozins remains unknown, although there is some research about a hypothetical effect in the myocardial cells. Although platelets are essential for human homeostasis the cells fragments are involved in the pathophysiology of cardiovascular-related diseases. Therefore, the aim of this study is to carry out a pharmacological characterization of the gliflozins (empagliflozin, canagliflozin and dapagliflozin) available on the market in isolated platelets from helathy volunteers. All the experimental protocols were approved by the Ethic Committee from UNICAMP (Number 2.412.312). Our preliminary results showed that markedly inhibited platelet aggregation-challenged by collagen and ADP, although to a lesser extent, also reduced platelet aggregation challenged by U-46619 and thrombin. Moreover, the addition of low concentrations of endothelial mediators potentiated the effects of gliflozins on platelet inhibition.
Highlights
Gliflozins are a new pharmacological class approved to treating patients with type 2 diabetes and act by inhibiting the transporter named sodium-glucose co-transporter 2 (SGLT2) expressed on the proximal convoluted tubule (1)
Because platelets are involved on thrombus formation and EMPA reduced the risk of combined endpoint of hospitalization for heart failure or cardiovascular death our hypothesis is that gliflozins will reduce platelet reactivity
Platelet aggregation was performed with an optical aggregometer at 37 °C with 200 μL of washed platelets placed in glass cuvettes containing a disposable stir bar for constant stirring
Summary
Gliflozins are a new pharmacological class approved to treating patients with type 2 diabetes and act by inhibiting the transporter named sodium-glucose co-transporter 2 (SGLT2) expressed on the proximal convoluted tubule (1). To date three gliflozins named empagliflozin, dapagliflozin and Canagliflozin were approved by the Brazilian regulatory agency to be used in association with metformin for the treatment of diabetes type 2.
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