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]
Insulin glulisine is indicated for the treatment of diabetes mellitus.[3][2]
Mechanism behind the rapid bioavailabilityedit
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]
Referencesedit
^ ab"Insulin glulisine Use During Pregnancy". Drugs.com. 6 April 2020. Retrieved 21 September 2020.
^ abc"Apidra- insulin glulisine injection, solution Apidra SoloStar- insulin glulisine injection, solution". DailyMed. 6 December 2019. Retrieved 21 September 2020.
^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.
insulin, glulisine, rapid, acting, modified, form, medical, insulin, that, differs, from, human, insulin, that, amino, acid, asparagine, position, replaced, lysine, lysine, position, replaced, glutamic, acid, developed, sanofi, aventis, approved, marketing, 20. 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 Insulin glulisinePDB 6gv0 Clinical dataTrade namesApidra Apidra SoloStarAHFS Drugs comMonographMedlinePlusa607033License dataEU EMA by INN US DailyMed Insulin glulisinePregnancycategoryAU B3 1 Routes ofadministrationSubcutaneous intravenousATC codeA10AB06 WHO Legal statusLegal statusAU S4 Prescription only UK POM Prescription only US only 2 EU Rx only 3 IdentifiersCAS Number207748 29 6 NDrugBankDB01309 YChemSpidernoneUNII7XIY785AZDKEGGD04540 YChemical and physical dataFormulaC 258H 384N 64O 78S 6Molar mass5822 64 g mol 1 N Y what is this verify The most common side effects include hypoglycaemia low blood glucose levels 3 Contents 1 Medical uses 2 Mechanism behind the rapid bioavailability 3 References 4 External linksMedical uses editInsulin glulisine is indicated for the treatment of diabetes mellitus 3 2 Mechanism behind the rapid bioavailability editThe 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 edit a b Insulin glulisine Use During Pregnancy Drugs com 6 April 2020 Retrieved 21 September 2020 a b c Apidra insulin glulisine injection solution Apidra SoloStar insulin glulisine injection solution DailyMed 6 December 2019 Retrieved 21 September 2020 a b c Apidra EPAR European Medicines Agency EMA Retrieved 7 October 2020 Apidra insulin glulisine injection solution DailyMed Apidra FDA Approval History Drugs com Retrieved 25 August 2022 Apidra ema europa eu Retrieved 3 December 2023 Jasek W ed 2007 Austria Codex in German 2007 2008 ed Vienna Osterreichischer Apothekerverlag ISBN 978 3 85200 181 4 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 Insulin Glulisine Drugs com 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 External links edit Insulin glulisine Drug Information Portal U S National Library of Medicine Portal nbsp Medicine nbsp This drug article relating to the gastrointestinal system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Insulin glulisine amp oldid 1193535523, wikipedia, wiki, book, books, library,
