Meglitinide | |
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Drug class | |
![]() Meglitinide, the prototype of this drug class | |
Class identifiers | |
Use | Type 2 diabetes |
ATC code | A10BX |
Mode of action | insulin secretagogue (release stimulator) |
Mechanism of action | closepotassium channels ofbeta cells |
Clinical data | |
Drugs.com | Drug Classes |
Legal status | |
In Wikidata |
Meglitinides orglinides are a class of drugs used to treattype 2 diabetes.[1]
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 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]
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.
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