Description

Simple

A medication used to control blood sugar in type 1 or 2 diabetes.

Clinical

A long acting insulin used to treat hyperglycemia caused by type 1 and 2 diabetes mellitus.

Overview

Insulin degludec is an ultra-long-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 degludec, 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 imp... Read more

Pharmacology

Indication

Insulin degludec is indicated to improve glycemic control in patients 1 year of age and older with diabetes mellitus.

Pharmacodynamic

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, the pancreas produces a continuous supply of low levels of basal insulin along with spikes of insulin following meals. Increased insulin secretion following meals is responsible for the metabolic change... Read more

Mechanism of action

Insulin detemir 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 bo... Read more

Absorption

In patients with type 1 diabetes, after 8 days of once daily subcutaneous dosing with 0.4 U/kg, maximum degludec concentrations of 4472 pmol/L were attained at a median of 9 hours (tmax). After the first dose of, median onset of appearance was around one hour. The glucose lowering effect lasted at l... Read more

Protein binding

The affinity of insulin degludec to serum albumin corresponds to a plasma protein binding of >99% in human plasma. The results of the in vitro protein binding studies demonstrate that there is no clinically relevant interaction between insulin degludec and other protein bound drugs.

Volume of distribution

Information currently not available.

Clearance

The mean apparent clearance of insulin degludec is 0.03 L/kg (2.1 L/h in 70 kg individual) after single subcutaneous dose of 0.4 units/kg.

Half life

The half-life after subcutaneous administration is determined primarily by the rate of absorption from the subcutaneous tissue. On average, the half-life at steady state is approximately 25 hours independent of dose.

Route of elimination

Information currently not available.

Toxicity

Observe for signs and symptoms of hypoglycemia, hypokalemia, and fluid retention and heart failure with concomitant use of Thiazolidinediones.
Pregnancy Category C

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nasopharyngitis US
  • adult
  • Kind: experimental
    • Percent: 23.9
  • Clinical Trial
    Severe Hypoglycemia US
    • pediatric
  • Kind: experimental
    • Percent: 17.8
  • Clinical Trial
    Nasopharyngitis US
    • adult
  • Kind: experimental
    • Percent: 12.9
  • Clinical Trial
    Formation of antibodies US
  • Kind: experimental
    • Percent: 12.3
  • Clinical Trial
    Severe Hypoglycemia US
    • adult
  • Kind: experimental
    • Percent: 12.3
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 11.9
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 11.8
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 8.8
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 8.4
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 6.3
  • Clinical Trial
    Gastroenteritis US
    • adult
  • Kind: experimental
    • Percent: 5.1
  • Clinical Trial
    Sinusitis US
    • adult
  • Kind: experimental
    • Percent: 5.1
  • Clinical Trial
    Injection Site Reactions US
  • Kind: experimental
    • Percent: 3.8
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 3.0
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 0.9
  • Clinical Trial
    Lipodystrophy US
  • Kind: experimental
    • Percent: 0.3
  • Clinical Trial
    Weight Gain US
    Clinical Trial
    Weight Gain US
    Clinical Trial
    Hypokalemia Canada
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Hypoglycemic Episode
        • Drugbank Id: DBCOND0106966

    Food Interactions

    Avoid alcohol. Alcohol may impair blood glucose control.