Insulin detemir
- CAS Number: 169148-63-4
Insulin detemir (trade name LEVEMIR ®, manufactured by Novo Nordisk) is a long-acting insulin analogue for the treatment of diabetes mellitus. It was approved in June 2004 by the European Commission. The effect lasts depending on the dose of up to 24 hours. It can be used in combination with anti-diabetic medicines ( oral hypoglycemic agents ) or mahlzeitenbezogenem short or rapid acting insulin.
- 2.1 Mechanism of action ( pharmacodynamics )
- 2.2 Absorption and distribution in the body ( pharmacokinetics )
- 3.1 Chemical and pharmaceutical information
- 3.2 studies
Clinical information
Areas of application (indications )
Insulin detemir is used in the treatment of diabetes mellitus in adults, adolescents and children aged 6-17 years.
Type and duration of application
Insulin detemir is a long-acting insulin analog that is used as a basal insulin. It is injected, depending on the regimen once or twice daily subcutaneously (under the skin). The dosage should be adjusted individually.
Contraindications ( contraindications)
In case of hypersensitivity or allergy to insulin detemir the drug should not be used.
Use during pregnancy and lactation
There are so far no clinical experience with use in pregnancy or lactation.
Pharmacological properties
Mechanism of action ( pharmacodynamics )
Insulin detemir is a soluble, long-acting insulin analogue with a prolonged duration of action, which is applied as a basal insulin. The blood glucose lowering effect is based on the ability of the molecule to promote binding of insulin to receptors on muscle and fat cells, the uptake of glucose. Simultaneously, the release of glucose from the liver is inhibited.
Uptake and distribution in the body ( pharmacokinetics )
The maximum serum concentration is reached within 6-8 hours after administration. The intra-individual variability in absorption is lower with insulin detemir than with other basal insulin.
Other Information
Chemical and pharmaceutical information
The C-terminal threonine (B30 ) has been removed and condensed at the ε -amino function of the lysine B29 of a myristic acid molecule. The pH of the preparation is 7.4. The prolonged action of insulin detemir is detemir molecules at the injection site and albumin binding mediated by the strong self-association of insulin via the fatty acid side chain.
Detemir ┌ ─ ─ ─ ─ ─ ─ ─ ─ ─ ┐ G-I - V -E -Q- C- C-T - S-I -S -C -L- Y -Q -L- E -N- Y -C -N │ ┌ ─ ┘ FVNQHLCGSHLVEALYLVCGE - RGFFYTPK │ HN -CO- C13H27 The preparation is carried genetically recombinant DNA in Saccharomyces cerevisiae. Additives are mannitol, phenol, m- cresol, zinc acetate, disodium hydrogen phosphate, sodium chloride, hydrochloric acid 2N ( pH adjustment ), sodium hydroxide 2N ( pH adjustment ), water for injections.
With regard to the IGF -1 receptor affinity to insulin analogues differ, sometimes significantly. Insulin detemir has similar favorable properties such as human insulin. Binding to the IGF -1 receptor is comparable to that of human insulin, or even lower.
Studies
Studies have shown that patients with type 2 diabetes, insulin detemir compared with NPH insulin achieve comparable HbA1c values, but with a significantly lower risk of hypoglycaemia. Similar results are available for type 1 diabetics.