Insulin glulisine
PDB: 6gv0​
Clinical data
Trade namesApidra, Apidra SoloStar
AHFS/Drugs.comMonograph
MedlinePlusa607033
License data
Pregnancy
category
Routes of
administration		Subcutaneous, intravenous
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC258H384N64O78S6
Molar mass5822.64 g·mol−1
 ☒NcheckY (what is this?)  (verify)

Insulin glulisine is a rapid-acting modified form of medical insulin that 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.[4] It was developed by Sanofi-Aventis and approved for marketing by the FDA[5] and the EMA[6] in 2004; it is sold under the trade name Apidra.[7] When injected subcutaneously, it appears in the blood earlier than regular human insulin (RHI).[8] When used as a meal time insulin, the dose is to be administered within 15 minutes before or 20 minutes after starting a meal.[9] Intravenous injections may also be used for extreme hyperglycemia, but must be performed under the supervision of a medical professional.[2]

The most common side effects include hypoglycaemia (low blood glucose levels).[3]

Medical uses

Insulin glulisine is indicated for the treatment of diabetes mellitus.[3][2]

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.[10]

References

  1. ↑ "Insulin glulisine Use During Pregnancy". Drugs.com. 6 April 2020. Retrieved 21 September 2020.
  2. 1 2 3 "Apidra- insulin glulisine injection, solution Apidra SoloStar- insulin glulisine injection, solution". DailyMed. 6 December 2019. Retrieved 21 September 2020.
  3. 1 2 3 "Apidra EPAR". European Medicines Agency (EMA). Retrieved 7 October 2020.
  4. ↑ "Apidra (insulin glulisine) injection, solution". DailyMed.
  5. ↑ "Apidra FDA Approval History". Drugs.com. Retrieved 25 August 2022.
  6. ↑ "Apidra". ema.europa.eu. Retrieved 3 December 2023.
  7. ↑ Jasek W, ed. (2007). Austria-Codex (in German) (2007/2008 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 978-3-85200-181-4.
  8. ↑ Garnock-Jones KP, Plosker GL (May 2009). "Insulin glulisine: a review of its use in the management of diabetes mellitus". Drugs. 69 (8): 1035–57. doi:10.2165/00003495-200969080-00006. PMID 19496630. S2CID 41839395.
  9. ↑ "Insulin Glulisine". Drugs.com.
  10. ↑ Gillis RB, Solomon HV, Govada L, Oldham NJ, Dinu V, Jiwani SI, Gyasi-Antwi P, Coffey F, Meal A, Morgan PS, Harding SE, Helliwell JR, Chayen NE, Adams GG (January 2021). "Analysis of Insulin Glulisine at the Molecular Level by X-Ray Crystallography and Biophysical Techniques". Scientific Reports. 11: 1737. doi:10.1038/s41598-021-81251-2. PMC 7814034. PMID 33462295.


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.