SGLT-2 inhibitors: pharmacokinetics characteristics and effects on lipids. (2nd November 2018)

• Record Type: Journal Article
• Authors: Filippas-Ntekouan, Sempastian; Tsimihodimos, Vasilios; Filippatos, Theodosios; Dimitriou, Theodora; Elisaf, Moses
• Is Part Of: Expert opinion on drug metabolism and toxicology. Volume 14:Number 11(2018)
• Page Start: 1113
• Page End: 1121
• Publication Date: 2018-11-02
• Subjects: SGLT-2 -- pharmacokinetics -- bioavailability -- lipids -- cholesterol -- triglycerides -- cardiovascular; Drugs -- Toxicology -- Periodicals; Drugs -- Metabolism -- Periodicals; 615.7
• DOI: 10.1080/17425255.2018.1541348
• Languages: English
• ISSNs: 1742-5255

Abstract

ABSTRACT: Introduction : Type 2 diabetes mellitus is characterized by increased cardiovascular morbidity and mortality. Atherogenic dyslipidemia is common in this population, consisting of the triad of increased triglycerides, increased small dense low-density lipoprotein (LDL) particles and decreased high-density lipoprotein cholesterol (HDL-C) levels, leading to increased cardiovascular risk. Areas covered : Aim of the review is the presentation of pharmacokinetic characteristics of the currently available sodium-glucose cotransporters 2 (SGLT-2) inhibitors and the effects of these drugs on lipid metabolism. SGLT-2 inhibitors share a common favorable pharmacokinetic profile, are orally administered with long half-lives (allowing for a once daily dosing) and have been proven to be effective in reducing blood glucose levels. However, the SGLT-1 inhibitory capacity differs between these drugs, an effect that may affect their antidiabetic and cardiovascular effects. SGLT-2 inhibitors alter serum lipids modestly in a similar manner. Specifically, an increase of total cholesterol, LDL cholesterol, and HDL-C levels as well as a decrease of triglycerides concentration is observed. Additionally, the administration of these agents may reduce the atherogenic small dense LDL particle levels, an effect that could provide additional cardiovascular protection in the long term. Expert opinion : The effect of SGLT-2 inhibitors on diabetic dyslipidemia may be one of their cardioprotective mechanisms.