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Loperamide-induced Cardiac Depression Is Enhanced by Hyperglycemia: Evidence Relevant to Loperamide Abuse

Shih-Hsiang Lo1, Ho-Shan Niu2, Yung-Ze Cheng3

  • 1Department of Internal Medicine, Division of Cardiology, Zhongxing Branch of Taipei City Hospital, Taipei City, Taiwan; Department of Nursing, Tzu Chi University of Science and Technology, Hualien City, Taiwan.

Archives of Medical Research
|June 5, 2017
PubMed
Abstract

Insights

Loperamide abuse is particularly dangerous for individuals with hyperglycemia, as high blood sugar increases cardiac μ-opioid receptor (MOR) expression via STAT3, enhancing loperamide

Area of Science:

  • Cardiology
  • Pharmacology
  • Endocrinology

Background:

  • Loperamide abuse can lead to cardiac dysrhythmias and death.
  • The mechanism of cardiac depression from loperamide is unclear.
  • Loperamide acts as a μ-opioid receptor (MOR) agonist.

Purpose of the Study:

  • Investigate the impact of hyperglycemia on cardiac MOR expression.
  • Determine the role of STAT3 in hyperglycemia-induced changes in cardiac MOR.
  • Assess the effect of hyperglycemia on loperamide's cardiac effects.

Main Methods:

  • Used streptozotocin-induced diabetic rats (STZ rats) to model hyperglycemia.
  • Measured cardiac performance and MOR levels in STZ rats treated with loperamide.
  • Investigated STAT3 and MOR expression in cultured cardiomyocytes under high glucose conditions.

Main Results:

  • Loperamide reduced cardiac performance more significantly in STZ rats.
  • Increased cardiac MOR in STZ rats was linked to hyperglycemia and reversed by glucose reduction.
  • High glucose increased MOR and STAT3 in cardiomyocytes; STAT3 inhibition reversed this.

Conclusions:

  • Hyperglycemia enhances loperamide-induced cardiac depression by increasing cardiac MOR expression.
  • Increased cardiac MOR expression is associated with elevated STAT3 levels in the heart.
  • Loperamide abuse poses a heightened risk to individuals with hyperglycemia.
Keywords:
Cardiac performanceSTAT3StatticsiRNAμ-opioid receptor

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