Pharmacokinetic and toxicological considerations for the treatment of diabetes in patients with liver disease

Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):839-57. doi: 10.1517/17425255.2014.902444. Epub 2014 Mar 26.

Abstract

Introduction: Patients with type 2 diabetes have an increased risk of chronic liver disease (CLD) such as non-alcoholic fatty liver disease and steatohepatitis and about one-third of cirrhotic patients have diabetes. However, the use of several antidiabetic agents may be a cause for concern in the case of hepatic impairment (HI).

Areas covered: An extensive literature search was performed to analyze the influence of HI on the pharmacokinetics (PK) of glucose-lowering agents and the potential consequences for clinical practice as far as the efficacy/safety balance of their use in diabetic patients with CLD is concerned.

Expert opinion: Almost no PK studies have been published regarding metformin, sulfonylureas, thiazolidinediones and α-glucosidase inhibitors in patients with HI. Only mild changes in PK of glinides, dipeptidyl peptidase-4 inhibitors and sodium glucose cotransporters type 2 inhibitors were observed in dedicated PK studies in patients with various degrees of HI, presumably without major clinical relevance although large clinical experience is lacking. Glucagon-like peptide-1 receptor agonists have a renal excretion rather than liver metabolism. Rare anecdotal case reports of hepatotoxicity have been described with various glucose-lowering agents contrasting with numerous reassuring data. Nevertheless, caution should be recommended, especially in patients with advanced cirrhosis, including with the use of metformin.

Keywords: chronic liver disease; cirrhosis; glucose-lowering therapy; hepatic impairment; hepatotoxicity; oral antidiabetic agent; pharmacokinetics; type 2 diabetes mellitus.

Publication types

  • Review

MeSH terms

  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacokinetics
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use
  • Hepatic Insufficiency / complications
  • Hepatic Insufficiency / metabolism*
  • Humans
  • Hypoglycemic Agents / pharmacokinetics*
  • Hypoglycemic Agents / therapeutic use
  • Liver Diseases / complications
  • Liver Diseases / metabolism
  • Metformin / pharmacokinetics
  • Metformin / therapeutic use
  • Sodium-Glucose Transporter 2 Inhibitors
  • Sulfonylurea Compounds / pharmacokinetics
  • Sulfonylurea Compounds / therapeutic use
  • Thiazolidinediones / pharmacokinetics
  • Thiazolidinediones / therapeutic use

Substances

  • Dipeptidyl-Peptidase IV Inhibitors
  • Hypoglycemic Agents
  • Sodium-Glucose Transporter 2 Inhibitors
  • Sulfonylurea Compounds
  • Thiazolidinediones
  • Metformin