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Insulin glulisine

Rapid-acting insulin analogue

Summary

Rapid-acting insulin analogue

Field	Value
Verifiedfields	changed
Watchedfields	changed
verifiedrevid	458271650
image	Insulin glulisine 6GV0 cartoon.png
caption
tradename	Apidra, Apidra Solostar
Drugs.com
MedlinePlus	a607033
DailyMedID	Insulin glulisine
pregnancy_AU	B3
pregnancy_AU_comment
routes_of_administration	Subcutaneous, intravenous
ATC_prefix	A10
ATC_suffix	AB06
legal_AU	S4
legal_BR
legal_CA
legal_DE
legal_NZ
legal_UK	POM
legal_US	Rx-only
legal_US_comment
legal_EU	Rx-only
legal_EU_comment
legal_UN
legal_status
CAS_number_Ref
CAS_number	207748-29-6
DrugBank_Ref
DrugBank	DB01309
ChemSpiderID_Ref
ChemSpiderID	none
UNII_Ref
UNII	7XIY785AZD
KEGG_Ref
KEGG	D04540
PDB_ligand	6gv0
C	258	H=384	N=64	O=78	S=6

| Drugs.com =

| elimination_half-life =

Insulin glulisine, sold under the brand name Apidra among others, is a rapid-acting modified form of medical insulin used for the treatment of diabetes. It differs from human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine in position B29 is replaced by glutamic acid. When injected subcutaneously, it appears in the blood earlier than regular human insulin (RHI). Intravenous injections may be used for extreme hyperglycemia. It was developed by Sanofi-Aventis.

The most common side effects include hypoglycaemia (low blood glucose levels).

Insulin glulisine was approved for medical use in the United States and in the European Union in 2004.

Medical uses

Insulin glulisine is indicated for the treatment of diabetes.

Mechanism behind the rapid bioavailability

The monomer-monomer interactions are weaker in insulin glulisin compared to unmodified human insulin, and therefore, it does not as readily form dimers and hexamers, which are dominant in unmodified insulin. Due to their large size, insulin hexamers need to break up into dimers or monomers before they are able to enter the blood and become biologically active. Specifically, the B3 mutation causes electrostatic repulsion in the hexamer to arginine-22 in the B chain of other insulin molecules in the same hexamer, while the B29 mutation causes fewer hydrogen bonds to stabilize the dimer. Furthermore, the isoelectric point of insulin glulisine insulin, which is shifted from 5.5 (of unmodified human insulin) to 5.1, increases the solubility at physiological pH levels.

References

(6 April 2020). "Insulin glulisine Use During Pregnancy".
(May 2009). "Insulin glulisine: a review of its use in the management of diabetes mellitus". Drugs.
(25 July 2023). "Apidra- insulin glulisine injection, solution; Apidra Solostar- insulin glulisine injection, solution".
"Drug Approval Package: Apidra (Insulin Glulisine [rDNA Origin]) NDA #021629".
(27 July 2009). "Apidra EPAR".
(January 2021). "Analysis of Insulin Glulisine at the Molecular Level by X-Ray Crystallography and Biophysical Techniques". Scientific Reports.

Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

insulin-analogues sanofi

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