Humulin®

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What are the pharmacokinetics and pharmacodynamics of Humulin® R U-500 (insulin human injection)?

The time action characteristics of Humulin R U-500 (insulin human injection) reflect both prandial and basal activity and are attributed to the high concentration.

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Detailed Information

Humulin® R U-500 (insulin human injection) 500 units/mL (U-500R) formulation is available

  • as a sterile, aqueous, and colorless solution
  • in a concentration of 500 units/mL, and
  • for subcutaneous injection only.1

The time action characteristics reflect both prandial and basal activity, consistent with clinical experience. This effect has been attributed to the high concentration of U-500R.1

The time course of action of U-500R, as with any insulin, may vary

  • in different individuals, or
  • at different times in the same individual.1

In a euglycemic clamp study of 24 healthy obese subjects with a body mass index of 30 to 39 kg/m2, single doses of subcutaneously administered U-500R at 50 units (0.4-0.6 unit/kg) and 100 units (0.8-1.3 unit/kg) resulted in a

  • mean time of onset of action <15 minutes at both doses
  • mean duration of action of 21 hours with a range of 13 to 24 hours, and
  • median peak insulin concentration occurring between 4 hours (50-unit dose) and 8 hours (100‑unit dose) with a range of 0.5 to 8 hours.1

After subcutaneous administration of single doses of 50 and 100 units of U-500R to healthy obese subjects (N≥21), the mean apparent half-life was approximately 4.5 hours with a range of 1.9 to 10 hours.1

Reference

1Humulin R U-500 [package insert]. Indianapolis, IN: Eli Lilly and Company; 2019.

Date of Last Review: October 22, 2021


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