A Pharmacokinetic-Pharmacodynamic Model of Morphine Exposure and Subsequent Morphine Consumption in Postoperative Pain

Pharm Res. 2016 May;33(5):1093-103. doi: 10.1007/s11095-015-1853-5. Epub 2016 Jan 11.

Abstract

Purpose: To characterize the pharmacokinetic-pharmacodynamic (PK-PD) relationship between exposure of morphine and subsequent morphine consumption and to develop simulation tools for model validation.

Methods: Dose, formulation and time of morphine administration was available from a published study in 63 patients receiving intravenous, oral immediate release or oral controlled release morphine on request after hip surgery. The PK-PD relationship between predicted exposure of morphine and morphine consumption was modeled using repeated time to event (RTTE) modeling in NONMEM. To validate the RTTE model, a visual predictive check method was developed with simulated morphine consumption given the exposure of preceding morphine administration.

Results: The probability of requesting morphine was found to be significantly related to the exposure of morphine as well as night/day. Oral controlled release morphine was more effective than intravenous and oral immediate release formulations at equivalent average concentrations. Maximum effect was obtained for 8 h by oral controlled release doses ≥ 15 mg, where probability of requesting a new dose was reduced to 20% for a typical patient.

Conclusion: This study demonstrates the first quantitative link between exposure of morphine and subsequent morphine consumption and introduces an efficient visual predictive check approach with simulation of adaptive dosing.

Keywords: non-linear mixed effects modeling; opioid consumption; pharmacokinetics-pharmacodynamics; postoperative pain; repeated time to event.

MeSH terms

  • Administration, Intravenous
  • Administration, Oral
  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / pharmacokinetics*
  • Analgesics, Opioid / pharmacology
  • Analgesics, Opioid / therapeutic use*
  • Computer Simulation
  • Humans
  • Models, Biological
  • Morphine / administration & dosage
  • Morphine / pharmacokinetics*
  • Morphine / pharmacology
  • Morphine / therapeutic use*
  • Pain, Postoperative / drug therapy*

Substances

  • Analgesics, Opioid
  • Morphine