Description

Simple

A medication used to control blood sugar in diabetes.

Clinical

A short-acting form of insulin used for glycemic control in type 1 and type 2 diabetes mellitus.

Overview

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 improve... Read more

Pharmacology

Indication

Insulin glulisine is indicated to improve glycemic control in adults and pediatric patients with diabetes mellitus.

Pharmacodynamic

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Postprandial insulin spikes are responsible for the metabolic changes that occur as the body transitions from a postabsorpti... Read more

Mechanism of action

Insulin glulisine binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The... Read more

Absorption

In a study in patients with type 1 diabetes (n=20) after subcutaneous administration of 0.15 units/kg, the median time to maximum concentration (Tmax) was 60 minutes (range 40 to 120 minutes) and the peak concentration (Cmax) was 83 microunits/mL (range 40 to 131 microunits/mL) for insulin glulisine... Read more

Protein binding

Information currently not available.

Volume of distribution

13 L

Clearance

Information currently not available.

Half life

Elimination half life= 42 minutes (following subcutaneous injection)

Route of elimination

Information currently not available.

Toxicity

Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Ne... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Infusion-site reaction US
  • Kind: experimental
    • Percent: 10.3
  • Kind: comparator
    • Percent: 13.3
  • Clinical Trial
    Nasopharyngitis US
    • adult
  • Kind: experimental
    • Percent: 10.6
  • Kind: comparator
    • Percent: 12.9
  • Clinical Trial
    Headache US
    • pediatric
  • Kind: experimental
    • Percent: 6.9
  • Kind: comparator
    • Percent: 11.2
  • Clinical Trial
    Upper Respiratory Tract Infections US
    • pediatric
  • Kind: experimental
    • Percent: 8.3
  • Kind: comparator
    • Percent: 10.8
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 10.5
  • Kind: comparator
    • Percent: 7.7
  • Clinical Trial
    Nasopharyngitis US
    • pediatric
  • Kind: experimental
    • Percent: 9.0
  • Kind: comparator
    • Percent: 9.5
  • Clinical Trial
    Nasopharyngitis US
    • adult
  • Kind: experimental
    • Percent: 7.6
  • Kind: comparator
    • Percent: 8.2
  • Clinical Trial
    Peripheral Edema US
    • adult
  • Kind: experimental
    • Percent: 7.5
  • Kind: comparator
    • Percent: 7.8
  • Clinical Trial
    Severe Hypoglycemia US
    • adult
  • Kind: experimental
    • Percent: 6.8
  • Kind: comparator
    • Percent: 6.7
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 6.6
  • Kind: comparator
    • Percent: 5.6
  • Clinical Trial
    Arthralgia US
    • adult
  • Kind: experimental
    • Percent: 5.9
  • Kind: comparator
    • Percent: 6.3
  • Clinical Trial
    Influenza US
    • adult
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 4.2
  • Clinical Trial
    Seizure US
    • pediatric
  • Kind: experimental
    • Percent: 6.1
  • Kind: comparator
    • Percent: 4.7
  • Clinical Trial
    Hypertension(HTN) US
    • adult
  • Kind: experimental
    • Percent: 3.9
  • Kind: comparator
    • Percent: 5.3
  • Clinical Trial
    Influenza US
    • adult
  • Kind: experimental
    • Percent: 4.0
  • Kind: comparator
    • Percent: 5.0
  • Clinical Trial
    Weight Gain US
    Clinical Trial
    Peripheral Edema US
    Clinical Trial
    Lipodystrophy US
    Clinical Trial
    Acute painful peripheral neuropath US
    Clinical Trial
    Worsening of diabetic retinopathy US
    Clinical Trial
    Transitory, reversible ophthalmologic refraction disorder US
    Clinical Trial
    Injection site reaction US
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Hypoglycemic Episodes
        • Drugbank Id: DBCOND0079438

    Food Interactions

    Avoid alcohol. Alcohol may impair blood glucose control.