Osmotic diuresis with SGLT2 inhibition: analysis of events related to volume reduction in dapagliflozin clinical trials

Postgrad Med. 2016 May;128(4):346-55. doi: 10.1080/00325481.2016.1153941. Epub 2016 Mar 2.

Abstract

Objective: Dapagliflozin reduces hyperglycemia in type 2 diabetes mellitus (T2DM) and lowers blood pressure, at least in part, secondary to mild diuresis consequent to dapagliflozin-induced glucosuria. While blood-pressure lowering may contribute to cardiovascular risk reduction, dapagliflozin-induced diuresis may potentially contribute to adverse events (AEs) of volume reduction. The present analysis compared the frequency of AEs of volume reduction between dapagliflozin and placebo.

Methods: Pooled data were assessed from 13 placebo-controlled dapagliflozin clinical trials ≤24 weeks in patients with T2DM, overall, and in those at risk (aged ≥65y, estimated glomerular filtration rate [eGFR] <60 mL/min/1.73 m(2), or on antihypertensive therapy). Longer-term (≤104 weeks) data were available for 9 of these trials.

Results: The frequency of patients experiencing ≥1 AE of volume reduction over 24 weeks was low overall; 27/2360 (1.1%) with dapagliflozin 10 mg and 17/2295 (0.7%) with placebo; and slightly more frequent in patients ≥65 years (11/665 [1.7%] and 6/711 [0.8%], respectively) and in patients receiving loop diuretics (6/236 [2.5%] and 4/267 [1.5%], respectively). Over 104 weeks, AEs of volume reduction occurred in 38/2026 (1.9%) with dapagliflozin 10 mg and in 27/1956 (1.4%) with placebo; serious AEs of volume reduction in 4/2026 (0.2%) and 6/1956 (0.3%), respectively; and 2 patients in each group discontinued therapy due to these AEs. Dapagliflozin versus placebo incidence rate ratios did not suggest any meaningful increase in frequency of these AEs with dapagliflozin 10 mg, either overall or in those at risk. Although mean eGFR declined by 4.2 ml/min/1.73 m(2) within the first week of dapagliflozin therapy, thereafter eGFR gradually recovered to baseline levels by 104 weeks (mean change from baseline +0.02 mL/min/1.73 m(2); 95%CI: -0.9, 1.0).

Conclusion: No meaningful increase in frequency of AEs of volume reduction occurred with dapagliflozin 10 mg in patients with T2DM, either overall, or in those at increased risk of these events. However, caution should nevertheless be exercised when prescribing dapagliflozin to elderly patients, those with reduced eGFR, and those receiving antihypertensive medication.

Keywords: SGLT2; dapagliflozin; dehydration; eGFR; hypotension; syncope.

MeSH terms

  • Age Factors
  • Aged
  • Benzhydryl Compounds / adverse effects*
  • Benzhydryl Compounds / pharmacology
  • Blood Pressure / drug effects
  • Blood Urea Nitrogen
  • Diuresis / drug effects
  • Female
  • Fractures, Bone / chemically induced
  • Fractures, Bone / epidemiology
  • Glomerular Filtration Rate / drug effects
  • Glucosides / adverse effects*
  • Glucosides / pharmacology
  • Humans
  • Hypoglycemic Agents / adverse effects*
  • Hypoglycemic Agents / pharmacology
  • Hypotension, Orthostatic / epidemiology
  • Hypovolemia / chemically induced
  • Hypovolemia / epidemiology*
  • Incidence
  • Male
  • Middle Aged
  • Osmosis / drug effects
  • Placebos / adverse effects
  • Polyuria / chemically induced
  • Polyuria / epidemiology
  • Randomized Controlled Trials as Topic
  • Risk Factors
  • Sodium Potassium Chloride Symporter Inhibitors / adverse effects
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors*

Substances

  • Benzhydryl Compounds
  • Glucosides
  • Hypoglycemic Agents
  • Placebos
  • SLC5A2 protein, human
  • Sodium Potassium Chloride Symporter Inhibitors
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors
  • dapagliflozin