Empagliflozin: A sodium–glucose cotransporter 2 inhibitor for treatment of type 2 diabetes

• Published in: American journal of health-system pharmacy Vol. 72; no. 22; pp. 1943 - 1954
• Main Authors: DIXIT, DIVISHA, YOON, YOUNGMIN, VOLINO, LUCIO R, MANSUKHANI, RUPAL PATEL
• Format: Journal Article
• Language: English
• Published: England Copyright American Society of Health-System Pharmacists, Inc. All rights reserved 15.11.2015; Oxford University Press
• Subjects: Benzhydryl Compounds - adverse effects; Benzhydryl Compounds - pharmacology; Benzhydryl Compounds - therapeutic use; Blood Glucose - drug effects; Diabetes Mellitus, Type 2 - drug therapy; Dosage and administration; Drug Interactions; Drug therapy; Empagliflozin; Glucosides - adverse effects; Glucosides - pharmacology; Glucosides - therapeutic use; Humans; Hypoglycemic Agents - adverse effects; Hypoglycemic Agents - pharmacology; Hypoglycemic Agents - therapeutic use; Sodium-Glucose Transporter 2 Inhibitors; Type 2 diabetes; United States
• ISSN: 1079-2082; 1535-2900
• DOI: 10.2146/ajhp150071

PURPOSEThe pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, adverse effects, dosage and administration, and drug–drug interactions of empagliflozin are reviewed. SUMMARYEmpagliflozin is a direct inhibitor of sodium–glucose cotransporter 2 (SGLT2), which acts to lower the renal threshold and increase urinary glucose excretion. SGLT2 is found in the proximal tubules of the kidneys and reabsorbs about 90% of the filtered glucose. Because the mechanism of action of empagliflozin is not insulin dependent or insulin sensitive, it may be used in patients at different stages of diabetes with nonfunctional or impaired pancreatic β cells. Furthermore, empagliflozin can be used with other antidiabetic drugs due to its lack of any additive hypoglycemic effects. Long-term efficacy studies revealed significant reductions with empagliflozin in glycosylated hemoglobin (HbA1c) values at week 78 compared with placebo. Secondary endpoints in clinical trials showed improvements in lowering blood pressure and reductions in body weight. The risk:benefit ratio must be assessed for empagliflozin as the safety profile includes an increase in urinary and genital infections. CONCLUSIONEmpagliflozin has shown efficacy in lowering HbA1c and blood glucose levels both as monotherapy and as an add-on to existing therapy. Despite the drugʼs promising outlook, empagliflozin also leads to common but serious adverse events not seen with other classes of antihyperglycemic agents. Considering the current data on its efficacy and its safety profile, empagliflozin can be used as a second- or third-line agent in treating diabetes.