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Meglitinide

From Wikipedia, the free encyclopedia
Chemical substance
Meglitinide
Drug class
Meglitinide, the prototype of this drug class
Class identifiers
UseType 2 diabetes
ATC codeA10BX
Mode of actioninsulin secretagogue (release stimulator)
Mechanism of actionclosepotassium channels ofbeta cells
Clinical data
Drugs.comDrug Classes
Legal status
In Wikidata

Meglitinides orglinides are a class of drugs used to treattype 2 diabetes.[1]

Drugs

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Repaglinide (trade name Prandin)[2] gained USFood and Drug Administration approval in 1997.

Other drugs in this class includenateglinide (Starlix)[3] andmitiglinide (Glufast).

Side effects

[edit]

Side effects include weight gain andhypoglycemia. While the potential for hypoglycemia is less than for those onsulfonylureas,[citation needed] it is still a serious potential side effect that can be life-threatening. Patients on this medication should know the signs and symptoms of hypoglycemia and appropriate management.

Repaglinide caused an increased incidence in male rats of benign adenomas (tumors) of the thyroid and liver.[2] No such effect was seen with another drug of this class, nateglinide.[3]

A 2020 Cochrane systematic review did not find enough evidence of reduction of all-cause mortality, serious adverse events, cardiovascular mortality, non-fatalmyocardial infarction, non-fatalstroke orend-stage renal disease when comparingmetformin monotherapy to meglitinide for the treatment of type 2 diabetes.[4]

Mechanism of action

[edit]

They bind to anATP-dependentK+ (KATP) channel on the cell membrane of pancreaticbeta cells in a similar manner tosulfonylureas but have a weaker binding affinity and faster dissociation from the SUR1 binding site. This increases the concentration of intracellular potassium, which causes the electric potential toward the intracellular side of the membrane to become more positive. Thisdepolarization opens voltage-gatedCa2+ channels. The rise in intracellular calcium leads to increased fusion ofinsulin granula in the cell membrane, and therefore increased secretion of (pro) insulin.

References

[edit]
  1. ^Blicklé JF (April 2006). "Meglitinide analogues: a review of clinical data focused on recent trials".Diabetes & Metabolism.32 (2):113–120.doi:10.1016/S1262-3636(07)70257-4.PMID 16735959.
  2. ^abPrandin (repaglinide) prescribing information, fda.gov
  3. ^abStarlix (nateglinide) prescribing information, fda.gov
  4. ^Gnesin F, Thuesen AC, Kähler LK, Madsbad S, Hemmingsen B (June 2020). Cochrane Metabolic and Endocrine Disorders Group (ed.)."Metformin monotherapy for adults with type 2 diabetes mellitus".The Cochrane Database of Systematic Reviews.2020 (6): CD012906.doi:10.1002/14651858.CD012906.pub2.PMC 7386876.PMID 32501595.
Oraldiabetes medication,insulins andinsulin analogues, and other drugs used in diabetes (A10)
fast-acting
short-acting
long-acting
ultra-long-acting
inhalable
  • Exubera
  • Afrezza
Oral
Non-insulins
Insulin sensitizers
Biguanides
TZDs/"glitazones" (PPAR)
Dual PPAR agonists
Amylin analogues andDACRAs
Secretagogues
K+ATP
Sulfonylureas
Meglitinides/"glinides"
GLP-1 receptor agonists
GLP1 poly-agonist peptides
DPP-4 inhibitors/"gliptins"
Other
Aldose reductase inhibitors
Alpha-glucosidase inhibitors
SGLT2 inhibitors/"gliflozins"
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Combinations
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