Description

Simple

A medication used to control blood sugar in diabetes.

Clinical

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

Overview

Insulin detemir is a 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 detemir, 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... Read more

Pharmacology

Indication

Insulin detemir 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, 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

Maximum serum concentrations are reached 6 to 8 hours following subcutaneous injection. The duration of action of insulin detemir is mediated by slowed systemic absorption of insulin detemir molecules from the injection site due to self-association of the drug molecule. When single dose of 0.5 units... Read more

Protein binding

More than 98% of insulin detemir in the bloodstream is bound to albumin. The results of in vitro and in vivo protein binding studies demonstrate that there is no clinically relevant interaction between insulin detemir and fatty acids or other protein-bound drugs.

Volume of distribution

Insulin detemir has an apparent volume of distribution of approximately 0.1 L/kg.

Clearance

Apparent clearance (CL/F), type 1 diabetes adult patients = 3.41 ± 1.00 L/min·kg

Half life

After subcutaneous administration in patients with type 1 diabetes, insulin detemir has a terminal half-life of 5 to 7 hours depending on dose.

Route of elimination

Information currently not available.

Toxicity

Hypoglycemia may occur with inappropriately high doses. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, c... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Upper Respiratory Tract Infection US
Peripheral Edema US
Weight Gain US
Lipodystrophy US
Severe Hypoglycemia US
Vomiting US
Rhinitis US
Nausea US
Infection Viral US
Cough US
Pyrexia US
Bronchitis US
Gastroenteritis US
Back Pain US
Hypoglycemia US
Abdominal Pain US
Influenza-like Illness US
Pharyngitis US
Headache US

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Hypoglycemia
      • Drugbank Id: DBCOND0020360

Food Interactions

Take with food. Once daily administration should be given with the evening meal or prior to bedtime.