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Pharmacokinetic and Toxicological Considerations of the SGLT2 Inhibitors

Are there differences between canagliflozin, dapagliflozin, and empagliflozin?… 

The study included healthy volunteers, patients with type 2 diabetes, and participants with mild to moderate renal or hepatic impairment. Researchers found that all three agents had a great oral bioavailability, a long half-life, did not accumulate to a great extent, did not have active metabolites, and drug-drug interactions were very rare.

In addition, patients with type 2 diabetes and those with mild to moderate renal or hepatic impairment were not found to have relevant changes in the pharmacokinetic parameters of these drugs as compared to healthy volunteers. All three SGLT2 inhibitors had the adverse effect of causing genitourinary infections, but the incidence was moderately rare.

The researchers concluded that when looking at the currently available information on these new medications there seems to be no discernible difference between the pharmacokinetics and side effects of the SGLT2 inhibitors.

Practice Pearls:
  • The three new SGLT2 inhibitors appear to have no clinically relevant pharmacokinetic differences.
  • The most common adverse effect for all three of the new SGLT2 inhibitors is the increased incidence of genitourinary infections.
  • The SGLT2 inhibitor pharmacokinetic parameters were not seen to be any different in patients with type 2 diabetes or mild to moderate renal or hepatic impairment as compared to the healthy volunteers.

Expert Opinion Drug Metabolism Toxicology, January 2014