Calcineurin Inhibitors: Pharmacologic Mechanisms Impacting Both Insulin Resistance and Insulin Secretion Leading to Glucose Dysregulation and Diabetes Mellitus

Research output: Contribution to journalReview article

20 Citations (Scopus)

Abstract

Calcineurin inhibitors (CNIs), including tacrolimus and cyclosporine, are immune-modulating agents used in autoimmune disorders, glomerulonephritides, and after transplantation. CNIs are implicated as diabetogenic drugs but the mechanism is not clearly elucidated. Calcineurin is a cytosolic-phosphatase critical for T-lymphocyte activation. Calcineurin is widely distributed in different tissues responsible for glucose-regulation including pancreas, liver, skeletal muscle, adipocytes, brain, and gut. We describe the pharmacologic effects of CNIs in different tissues and impact on glucose regulation.

Original languageEnglish (US)
Pages (from-to)114-120
Number of pages7
JournalClinical Pharmacology and Therapeutics
Volume101
Issue number1
DOIs
StatePublished - Jan 1 2017

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Insulin Resistance
Diabetes Mellitus
Calcineurin
Insulin
Glucose
Tacrolimus
Lymphocyte Activation
Glomerulonephritis
Phosphoric Monoester Hydrolases
Adipocytes
Cyclosporine
Pancreas
Skeletal Muscle
Transplantation
T-Lymphocytes
Liver
Brain
Pharmaceutical Preparations
Calcineurin Inhibitors

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

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abstract = "Calcineurin inhibitors (CNIs), including tacrolimus and cyclosporine, are immune-modulating agents used in autoimmune disorders, glomerulonephritides, and after transplantation. CNIs are implicated as diabetogenic drugs but the mechanism is not clearly elucidated. Calcineurin is a cytosolic-phosphatase critical for T-lymphocyte activation. Calcineurin is widely distributed in different tissues responsible for glucose-regulation including pancreas, liver, skeletal muscle, adipocytes, brain, and gut. We describe the pharmacologic effects of CNIs in different tissues and impact on glucose regulation.",
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AB - Calcineurin inhibitors (CNIs), including tacrolimus and cyclosporine, are immune-modulating agents used in autoimmune disorders, glomerulonephritides, and after transplantation. CNIs are implicated as diabetogenic drugs but the mechanism is not clearly elucidated. Calcineurin is a cytosolic-phosphatase critical for T-lymphocyte activation. Calcineurin is widely distributed in different tissues responsible for glucose-regulation including pancreas, liver, skeletal muscle, adipocytes, brain, and gut. We describe the pharmacologic effects of CNIs in different tissues and impact on glucose regulation.

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