MedPath

Insulin Glulisine

Generic Name
Insulin Glulisine
Brand Names
Apidra
Drug Type
Biotech
CAS Number
207748-29-6
Unique Ingredient Identifier
7XIY785AZD
Background

Insulin glulisine is a short-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis among many other functions.

Insulin is an important treatment in the management of Type 1 Diabetes (T1D) which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce or synthesize the insulin needed to manage circulating blood sugar levels. As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin glulisine, to lower glucose levels in the blood. Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels. Without treatment or improvement in non-pharmacological measures such as diet and exercise to lower blood glucose, high blood sugar eventually causes cellular resistance to endogenous insulin, and in the long term, damage to pancreatic islet cells. Insulin is typically prescribed later in the course of T2D, after trying several oral medications such as Metformin, Gliclazide, or Sitagliptin have been tried, when sufficient damage has been caused to pancreatic cells that the body is no longer able to produce insulin on its own.

Marketed as the brand name product Apidra, insulin glulisine begins to exert its effects within 15 minutes of subcutaneous administration, while peak levels occur 30 to 90 minutes after administration. Due to its duration of action of around 5 hours, Apidra is considered "bolus insulin" as it provides high levels of insulin in a short period of time to mimic the release of endogenous insulin from the pancreas after meals. Bolus insulin is often combined with once daily, long-acting "basal insulin" such as Insulin detemir, Insulin degludec, and Insulin glargine to provide low concentrations of background insulin that can keep blood sugar stable between meals or overnight. Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with a goal of avoiding any periods of hypoglycemia.

Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of Escherichia coli (K12). This recombinant hormone differs from native human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin.

Without an adequate supply of insulin to promote absorption of glucose from the bloodstream, blood sugar levels can climb to dangerously high levels and can result in symptoms such as fatigue, headache, blurred vision, and increased thirst. If left untreated, the body starts to break down fat, instead of glucose, for energy which results in a build-up of ketone acids in the blood and a syndrome called ketoacidosis, which is a life-threatening medical emergency. In the long term, elevated blood sugar levels increase the risk of heart attack, stroke, and diabetic neuropathy.

Indication

用于治疗成人糖尿病。

Associated Conditions
Diabetes Mellitus, Type 1 Diabetes Mellitus, Hyperglycemia during critical illness

The Impact of Two Different Insulin Dose Calculation on Postprandial Glycemia After Mixed Meal.

Phase 4
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2019-10-11
Last Posted Date
2019-10-11
Lead Sponsor
Medical University of Warsaw
Target Recruit Count
70
Registration Number
NCT04124302

Super-Bolus: Effects on Postprandial Glycemia After High Glycemic Index Meal

Phase 4
Completed
Conditions
Diabetes Mellitus, Type 1
Interventions
First Posted Date
2019-07-15
Last Posted Date
2023-11-30
Lead Sponsor
Medical University of Warsaw
Target Recruit Count
72
Registration Number
NCT04019821
Locations
🇵🇱

Department of Pediatric Diabetology and Pediatrics, Pediatric Teaching Clinical Hospital, Warsaw, Poland

Comparison of Two Treatment Regimens in Patients With Type 2 Diabetes After Short-term Intensive Insulin Therapy

Phase 4
Completed
Conditions
Type 2 Diabetes Mellitus
Interventions
First Posted Date
2017-12-02
Last Posted Date
2022-04-25
Lead Sponsor
Sanofi
Target Recruit Count
384
Registration Number
NCT03359837
Locations
🇨🇳

CHINA, China, China

Impact on the Oxidative Stress of the Different Analogues of Insulin in People With Type 1 Diabetes. (Ineox Study)

Phase 4
Completed
Conditions
Type 1 Diabetes Mellitus
Interventions
First Posted Date
2017-11-01
Last Posted Date
2021-12-06
Lead Sponsor
Fundación Pública Andaluza para la Investigación de Málaga en Biomedicina y Salud
Target Recruit Count
300
Registration Number
NCT03328845
Locations
🇪🇸

Regional University Hospital of Málaga, Málaga, Spain

Beneficial Effect of Insulin Glulisine by Lipoatrophy and Type 1 Diabetes (LAS)

Phase 4
Completed
Conditions
Lipoatrophy
Type 1 Diabetes
Interventions
Drug: current insulin
First Posted Date
2016-09-26
Last Posted Date
2024-10-11
Lead Sponsor
Kinderkrankenhaus auf der Bult
Target Recruit Count
14
Registration Number
NCT02914886

A Study to Demonstrate Bioequivalence Between Insulin Glulisine U300 and Insulin Glulisine U100 After a Single Subcutaneous Dose Using the Euglycemic Clamp Technique, in Patients With Type 1 Diabetes Mellitus

Phase 1
Completed
Conditions
Type1 Diabetes Mellitus
Interventions
First Posted Date
2016-09-22
Last Posted Date
2022-04-25
Lead Sponsor
Sanofi
Target Recruit Count
44
Registration Number
NCT02910518
Locations
🇩🇪

Investigational Site Number 276001, Neuss, Germany

Insulin Requirement for Pure-protein Meal in Children With Type 1 Diabetes on Insulin Pumps.

Phase 4
Conditions
Diabetes type1
Interventions
First Posted Date
2016-02-18
Last Posted Date
2016-07-29
Lead Sponsor
Medical University of Warsaw
Target Recruit Count
70
Registration Number
NCT02685449
Locations
🇵🇱

Medical University, Warsaw, Poland

Intranasal Glulisine in Amnestic Mild Cognitive Impairment and Probable Mild Alzheimer's Disease

Phase 2
Terminated
Conditions
Alzheimer's Disease (AD)
Mild Cognitive Impairment
Interventions
First Posted Date
2015-07-21
Last Posted Date
2020-04-09
Lead Sponsor
HealthPartners Institute
Target Recruit Count
49
Registration Number
NCT02503501
Locations
🇺🇸

HealthPartners Neuroscience Center, Saint Paul, Minnesota, United States

🇺🇸

HealthPartners Riverside, Minneapolis, Minnesota, United States

Investigation of the Safety of Intranasal Glulisine in Down Syndrome

Phase 1
Completed
Conditions
Down Syndrome
Interventions
First Posted Date
2015-05-04
Last Posted Date
2019-12-06
Lead Sponsor
HealthPartners Institute
Target Recruit Count
12
Registration Number
NCT02432716
Locations
🇺🇸

HealthPartners Neuroscience Center, Saint Paul, Minnesota, United States

Normal Versus Dual Wave Insulin Bolus for High-protein Food

Phase 4
Completed
Conditions
Type 1 Diabetes
Interventions
First Posted Date
2014-10-28
Last Posted Date
2018-01-31
Lead Sponsor
Medical University of Warsaw
Target Recruit Count
70
Registration Number
NCT02276859
Locations
🇵🇱

Department of Pediatrics, Medical University of Warsaw, Poland, Warsaw, Poland

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