Insulin glulisine
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| Clinical data | |
|---|---|
| Trade names | Apidra, Apidra SoloStar |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607033 |
| License data |
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| Pregnancy category |
|
intravenous | |
| ATC code | |
| Legal status | |
| Legal status | |
| Identifiers | |
| CAS Number | |
| DrugBank | |
| ChemSpider |
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| UNII | |
| KEGG | |
| Chemical and physical data | |
| Formula | C258H384N64O78S6 |
| Molar mass | 5822.64 g·mol−1 |
  (what is this?) (verify) | |
Insulin glulisine is a rapid-acting
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
- ^ 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.
- ISBN 978-3-85200-181-4.
- S2CID 41839395.
- ^ "Insulin Glulisine". Drugs.com.
- PMID 33462295.
External links
- "Insulin glulisine". Drug Information Portal. U.S. National Library of Medicine.
