A double-blind, randomized, dose-response study investigating the pharmacodynamic and pharmacokinetic properties of the long-acting insulin analog detemir

Diabetes Care. 2005 May;28(5):1107-12. doi: 10.2337/diacare.28.5.1107.

Abstract

Objective: To investigate the pharmacodynamic profile and duration of action for five subcutaneous doses of insulin detemir (0.1, 0.2, 0.4, 0.8, and 1.6 units/kg; 1 unit = 24 nmol) and one subcutaneous dose of NPH insulin (0.3 IU/kg; 1 IU = 6 nmol).

Research design and methods: This single-center, randomized, double-blind, six-period, crossover study was carried out as a 24-h isoglycemic clamp (7.2 mmol/l) in 12 type 1 diabetic patients.

Results: Duration of action for insulin detemir was dose dependent and varied from 5.7, to 12.1, to 19.9, to 22.7, to 23.2 h for 0.1, 0.2, 0.4, 0.8, and 1.6 units/kg, respectively. Interpolation of the dose-response relationships for AUC(GIR) (area under the glucose infusion rate curve) revealed that a detemir dose of 0.29 units/kg would provide the same effect as 0.3 IU/kg NPH but has a longer duration of action (16.9 vs. 12.7 h, respectively). Lower between-subject variability was observed for insulin detemir on duration of action (0.4 units/kg insulin detemir vs. 0.3 IU/kg NPH, P < 0.05) and GIR(max) (maximal glucose infusion rate) (0.2 and 0.4 units/kg insulin detemir vs. 0.3 IU/kg NPH, both P < 0.05). Assessment of endogenous glucose production (EGP) and peripheral glucose uptake (PGU) resulted in an AOC(EGP) (area over the EGP curve) of 636 mg/kg (95% CI 279-879) vs. 584 (323-846) and an AUC(PGU) (area under the PGU curve) of 173 (47-316) vs. 328 (39-617) for 0.29 units/kg detemir vs. 0.3 IU/kg NPH, respectively.

Conclusions: This study shows that insulin detemir provides a flat and protracted pharmacodynamic profile.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Cross-Over Studies
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Double-Blind Method
  • Fatty Acids, Nonesterified / blood
  • Female
  • Glucose / pharmacokinetics
  • Glucose Clamp Technique
  • Humans
  • Hypoglycemic Agents / administration & dosage*
  • Hypoglycemic Agents / pharmacokinetics*
  • Injections, Subcutaneous
  • Insulin / administration & dosage*
  • Insulin / analogs & derivatives*
  • Insulin / pharmacokinetics*
  • Insulin Detemir
  • Insulin, Isophane / administration & dosage
  • Insulin, Isophane / pharmacokinetics
  • Insulin, Long-Acting
  • Male

Substances

  • Blood Glucose
  • Fatty Acids, Nonesterified
  • Hypoglycemic Agents
  • Insulin
  • Insulin, Long-Acting
  • Insulin Detemir
  • Insulin, Isophane
  • Glucose