| The pharmacologic basis for clinical differences among GLP-1 receptor agonists and DPP-4 inhibitors. | |
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MedLine Citation:
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PMID: 22104467 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The incretin system plays an important role in glucose homeostasis, largely through the actions of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1). Unlike GIP, the actions of GLP-1 are preserved in patients with type 2 diabetes mellitus, which has led to the development of injectable GLP-1 receptor (GLP-1R) agonists and oral dipeptidyl peptidase-4 (DPP-4) inhibitors. GLP-1R agonists-which can be dosed to pharmacologic levels-act directly upon the GLP-1R. In contrast, DPP-4 inhibitors work indirectly by inhibiting the enzymatic inactivation of native GLP-1, resulting in a modest increase in endogenous GLP-1 levels. GLP-1R agonists generally lower the fasting and postprandial glucose levels more than DPP-4 inhibitors, resulting in a greater mean reduction in glycated hemoglobin level with GLP-1R agonists (0.4%-1.7%) compared with DPP-4 inhibitors (0.4%-1.0%). GLP-1R agonists also promote satiety and reduce total caloric intake, generally resulting in a mean weight loss of 1 to 4 kg over several months in most patients, whereas DPP-4 inhbitors are weight-neutral overall. GLP-1R agonists and DPP-4 inhibitors are generally safe and well tolerated. The glucose-dependent manner of stimulation of insulin release and inhibition of glucagon secretion by both GLP-1R agonists and DPP-4 inhibitors contribute to the low incidence of hypoglycemia. Although transient nausea occurs in 26% to 28% of patients treated with GLP-1R agonists but not DPP-4 inhibitors, this can be reduced by using a dose-escalation strategy. Other adverse events (AEs) associated with GLP-1R agonists include diarrhea, headache, and dizziness. The main AEs associated with DPP-4 inhibitors include upper respiratory tract infection, nasopharyngitis, and headache. Overall, compared with other therapies for type 2 diabetes mellitus with similar efficacy, incretin-based agents have low risk of hypoglycemia and weight gain. However, GLP-1R agonists demonstrate greater comparative efficacy and weight benefit than DPP-4 inhibitors. |
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Authors:
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Javier Morales |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Postgraduate medicine Volume: 123 ISSN: 1941-9260 ISO Abbreviation: Postgrad Med Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-11-22 Completed Date: 2012-01-23 Revised Date: 2012-03-15 |
Medline Journal Info:
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Nlm Unique ID: 0401147 Medline TA: Postgrad Med Country: United States |
Other Details:
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Languages: eng Pagination: 189-201 Citation Subset: AIM; IM |
Affiliation:
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Advanced Internal Medicine Group, PC, New Hyde Park, NY, USA. saxodoc@optonline.net |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Blood Glucose
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drug effects*,
metabolism Body Weight / drug effects Diabetes Mellitus, Type 2 / drug therapy* Dipeptidyl-Peptidase IV Inhibitors / adverse effects, pharmacology*, therapeutic use Drug Hypersensitivity Glucagon-Like Peptide 1 / adverse effects, analogs & derivatives, pharmacology, therapeutic use Homeostasis / drug effects Humans Hypoglycemic Agents / adverse effects, pharmacology*, therapeutic use Incretins / metabolism Pancreatitis / chemically induced Peptides / adverse effects, pharmacology, therapeutic use Receptors, Glucagon / agonists* Venoms / adverse effects, pharmacology, therapeutic use |
| Chemical | |
Reg. No./Substance:
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0/Blood Glucose; 0/Dipeptidyl-Peptidase IV Inhibitors; 0/Hypoglycemic Agents; 0/Incretins; 0/Peptides; 0/Receptors, Glucagon; 0/Venoms; 0/glucagon-like peptide receptor; 0/liraglutide; 141732-76-5/exenatide; 89750-14-1/Glucagon-Like Peptide 1 |
| Comments/Corrections | |
Erratum In:
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Postgrad Med. 2012 Jan;124(1):177-8 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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