Description

Simple

A medication used to control blood sugar in diabetes.

Clinical

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

Overview

Insulin aspart is a rapid-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 aspart, 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 i... Read more

Pharmacology

Indication

Insulin aspart is indicated to improve glycemic control in adults and children 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 aspart 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 bou... Read more

Absorption

In studies of healthy volunteers and patients with type 1 diabetes, the median time to maximum concentration of insulin aspart in these trials was 40 to 50 minutes versus 80 to 120 minutes, for regular human insulin respectively. Compared to human insulin, insulin aspart has a faster absorption, a f... Read more

Protein binding

Insulin aspart has a low binding affinity to plasma proteins (

Volume of distribution

Information currently not available.

Clearance

1.2 L/h/kg

Half life

Elimination half-life was found to be 81 minutes (following subcutaneous administration in healthy subjects).

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
Severe Hypoglycemia US
  • adult
  • Kind: experimental
    • Percent: 17%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 12
  • Kind: comparator
    • Percent: 10
  • Clinical Trial
    Hyporeflexia US
    • adult
  • Kind: experimental
    • Percent: 11
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Accidental injury US
    • adult
  • Kind: experimental
    • Percent: 11
  • Kind: comparator
    • Percent: 10
  • Clinical Trial
    Onychomycosis US
    • adult
  • Kind: experimental
    • Percent: 10
  • Kind: comparator
    • Percent: 5
  • Clinical Trial
    Severe Hypoglycemia US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Sensory disturbance US
    • adult
  • Kind: experimental
    • Percent: 9
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Urinary Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 8
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 7
  • Kind: comparator
    • Percent: 5
  • Clinical Trial
    Severe Hypoglycemia US
    • pediatric
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Sinusitis US
    • adult
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Skin disorder US
    • adult
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Chest Pain US
    • adult
  • Kind: experimental
    • Percent: 5
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Acute painful peripheral neuropath US
    Clinical Trial
    Worsening of diabetic retinopathy US
    Clinical Trial
    Transitory, reversible ophthalmologic refraction disorder US
    Clinical Trial
    Weight Gain US
    Clinical Trial
    Peripheral Edema US
    Clinical Trial
    Lipodystrophy US
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Hypoglycemica
        • Drugbank Id: DBCOND0101703

    Food Interactions

    Information currently not available.