Key result
Sitagliptin inhibited platelet aggregation in patients with type-2 diabetes by 30 ± 5% at 3 months and showed concentration-dependent anti-platelet activity in vitro.
Why the study?
Does sitagliptin reduce platelet aggregation in patients with type-2 diabetes and in vitro healthy human platelets?
Observational (n=60)
Does sitagliptin reduce platelet aggregation in patients with type-2 diabetes and in vitro healthy human platelets?
Sitagliptin demonstrates concentration-dependent anti-platelet activity by inhibiting intracellular free calcium and tyrosine phosphorylation.
Sitagliptin-associated platelet inhibition in T2D should not change practice; leaves open clinical relevance pending randomized outcome trials.
Sitagliptin, a selective dipeptidyl peptidase-4 inhibitor drug is used to treat type-2 diabetes (T2DM). We investigated the anti-platelet activity of sitagliptin in patients with T2DM and in in vitro samples obtained from healthy humans. Patients with T2DM (27 male + 23 female) were selected and followed up before (control) and after treatment with sitagliptin for up to 3 months. Platelets were isolated from the blood of sitagliptin treated patients and controls. Patients with T2DM treated with sitagliptin for 1and 3 months, showed 10 ± 2% and 30 ± 5% inhibition of platelet aggregation, respectively. For the in vitro study, platelets from 10 normal humans (n = 10) were isolated. Platelet aggregation, intracellular free calcium and tyrosine phosphorylation of multiple proteins were measured by aggregometer, spectrofluorometer and western blotting, respectively. Platelets pre-treated with 5 and 10 µg/ml of sitagliptin, showed 25 ± 4% and 40 ± 6% inhibition of thrombin-induced platelet aggregation, respectively. Sitagliptin decreased intracellular free calcium (2.5-fold) and tyrosine phosphorylation of multiple proteins in thrombin-induced platelet activation. Sitagliptin inhibited platelet aggregation in T2DM as well as in healthy humans. Sitagliptin has significant concentration-dependent anti-platelet activity. This activity was due to its inhibitory effect on intracellular free calcium and tyrosine phosphorylation.
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Gupta et al. (2012) conducted an observational in Type-2 diabetes (n=60). Sitagliptin vs. Before treatment (baseline) and untreated in vitro samples was evaluated on Inhibition of platelet aggregation. Sitagliptin inhibited platelet aggregation in patients with type-2 diabetes by 30 ± 5% at 3 months and showed concentration-dependent anti-platelet activity in vitro.
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