Insulin glulisine

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Insulin glulisine
Insulin glulisine 6GV0 cartoon.png
PDB: 6gv0 ​
Clinical data
Trade names Apidra, Apidra SoloStar
AHFS/Drugs.com Monograph
MedlinePlus a607033
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
Formula C258H384N64O78S6
Molar mass 5822.64 g·mol−1
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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]

Contents

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]

Related Research Articles

<span class="mw-page-title-main">Insulin</span> Peptide hormone

Insulin is a peptide hormone produced by beta cells of the pancreatic islets encoded in humans by the insulin (INS) gene. It is the main anabolic hormone of the body. It regulates the metabolism of carbohydrates, fats, and protein by promoting the absorption of glucose from the blood into cells of the liver, fat, and skeletal muscles. In these tissues the absorbed glucose is converted into either glycogen, via glycogenesis, or fats (triglycerides), via lipogenesis; in the liver, glucose is converted into both. Glucose production and secretion by the liver are strongly inhibited by high concentrations of insulin in the blood. Circulating insulin also affects the synthesis of proteins in a wide variety of tissues. It is thus an anabolic hormone, promoting the conversion of small molecules in the blood into large molecules in the cells. Low insulin in the blood has the opposite effect, promoting widespread catabolism, especially of reserve body fat.

Drugs used in diabetes treat diabetes mellitus by decreasing glucose levels in the blood. With the exception of insulin, most GLP-1 receptor agonists, and pramlintide, all diabetes medications are administered orally and are thus called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of hypoglycemic drugs, and selection of the appropriate agent depends on the nature of diabetes, age, and situation of the person, as well as other patient factors.

<span class="mw-page-title-main">Insulin glargine</span> Long-acting insulin

Insulin glargine sold under the brand name Lantus among others is a long-acting modified form of medical insulin, used in the management of type I and type II diabetes. It is injected just under the skin. Effects generally begin an hour after use.

<span class="mw-page-title-main">Pramlintide</span> Diabetes medication

Pramlintide is an injectable amylin analogue drug for diabetes, developed by Amylin Pharmaceuticals. Pramlintide is sold as an acetate salt.

An insulin analog is any of several types of medical insulin that are altered forms of the hormone insulin, different from any occurring in nature, but still available to the human body for performing the same action as human insulin in terms of controlling blood glucose levels in diabetes. Through genetic engineering of the underlying DNA, the amino acid sequence of insulin can be changed to alter its ADME characteristics. Officially, the U.S. Food and Drug Administration (FDA) refers to these agents as insulin receptor ligands, although they are usually just referred to as insulin analogs or even just insulin.

<span class="mw-page-title-main">Exenatide</span> Medication

Exenatide, sold under the brand name Byetta among others, is a medication used to treat type 2 diabetes. It is used together with diet, exercise, and potentially other antidiabetic medication. It is a treatment option after metformin and sulfonylureas. It is given by injection under the skin.

Insulin detemir, sold under the brand name Levemir among others, is a long-acting modified form of medical insulin used to treat both type 1 and type 2 diabetes. It is used by injection under the skin. It is effective for up to 24 hours.

<span class="mw-page-title-main">Insulin aspart</span> Rapid-acting man-made insulin

Insulin aspart, sold under the brand name NovoLog, among others, is a modified type of medical insulin used to treat type 1 and type 2 diabetes. It is generally used by injection under the skin but may also be used by injection into a vein. Maximum effect occurs after about 1–3 hours and lasts for 3–5 hours. Generally a longer-acting insulin like insulin NPH is also needed.

<span class="mw-page-title-main">Insulin lispro</span> Rapid-acting insuline analog

Insulin lispro, sold under the brand name Humalog among others, is a modified type of medical insulin used to treat type 1 and type 2 diabetes. It is delivered subcutaneously either by injection or from an insulin pump. Onset of effects typically occurs within 30 minutes and lasts about 5 hours. Often a longer-acting insulin like insulin NPH is also needed.

<span class="mw-page-title-main">Liraglutide</span> Anti-diabetic medication

Liraglutide, sold under the brand names Victoza and Saxenda among others, is an anti-diabetic medication used to treat type 2 diabetes, and chronic obesity. It is a second-line therapy for diabetes following first-line therapy with metformin. Its effects on long-term health outcomes like heart disease and life expectancy are unclear. It is given by injection under the skin.

<span class="mw-page-title-main">Insulin (medication)</span> Use of insulin protein and analogs as medical treatment

As a medication, insulin is any pharmaceutical preparation of the protein hormone insulin that is used to treat high blood glucose. Such conditions include type 1 diabetes, type 2 diabetes, gestational diabetes, and complications of diabetes such as diabetic ketoacidosis and hyperosmolar hyperglycemic states. Insulin is also used along with glucose to treat hyperkalemia. Typically it is given by injection under the skin, but some forms may also be used by injection into a vein or muscle. There are various types of insulin, suitable for various time spans. The types are often all called insulin in the broad sense, although in a more precise sense, insulin is identical to the naturally occurring molecule whereas insulin analogues have slightly different molecules that allow for modified time of action. It is on the World Health Organization's List of Essential Medicines. In 2021, it was the 179th most commonly prescribed medication in the United States, with more than 2 million prescriptions.

<span class="mw-page-title-main">Canagliflozin</span> Chemical compound

Canagliflozin, sold under the brand name Invokana among others, is a medication used to treat type 2 diabetes. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth.

Lixisenatide is a once-daily injectable GLP-1 receptor agonist for the treatment of type 2 diabetes.

<span class="mw-page-title-main">Insulin degludec</span> Ultralong-acting basal insulin analogue

Insulin degludec (INN/USAN) is an ultralong-acting basal insulin analogue that was developed by Novo Nordisk under the brand name Tresiba. It is administered via subcutaneous injection to help control the blood sugar level of those with diabetes. It has a duration of action that lasts up to 42 hours, making it a once-daily basal insulin, that is one that provides a base insulin level, as opposed to the fast- and short-acting bolus insulins.

<span class="mw-page-title-main">Empagliflozin/linagliptin</span> Pharmaceutical drug

Empagliflozin/linagliptin, sold under the brand name Glyxambi, is a fixed-dose combination anti-diabetic medication used to treat type 2 diabetes. It is a combination of empagliflozin and linagliptin. It is taken by mouth.

Insulin degludec/liraglutide, sold under the brand name Xultophy, is a fixed-dose combination medication for the treatment of adults with type 2 diabetes to improve glycemic control in combination with diet and exercise. It contains insulin degludec and liraglutide. It is administered by subcutaneous injection.

Insulin glargine/lixisenatide, sold under the brand name Soliqua among others, is a fixed-dose combination medication that combines insulin glargine and lixisenatide and is used to treat diabetes.

Empagliflozin/metformin, sold under the brand name Synjardy among others, is a fixed-dose combination anti-diabetic medication used to treat type 2 diabetes. It contains empagliflozin and metformin hydrochloride. It is taken by mouth.

Insulin degludec/insulin aspart, sold under the brand name Ryzodeg, is a fixed-dose combination medication for the treatment of diabetes mellitus. It contains insulin degludec and insulin aspart. It is given as an injection under the skin in the abdominal wall, upper arm or thigh.

<span class="mw-page-title-main">Tirzepatide</span> Anti-diabetic medication

Tirzepatide, sold under the brand names Mounjaro and Zepbound, is an antidiabetic medication used for the treatment of type 2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections.

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.
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