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Morbid Obesity Alters Both Pharmacokinetics and Pharmacodynamics of Propofol: Dosing Recommendation for Anesthesia Induction

Dong Dong, Xuemei Peng, Jie Liu, Hao Qian, Jiayang Li and Baojian Wu
Drug Metabolism and Disposition October 2016, 44 (10) 1579-1583; DOI: https://doi.org/10.1124/dmd.116.071605
Dong Dong
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Xuemei Peng
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Jie Liu
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Hao Qian
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Jiayang Li
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Baojian Wu
Ocular Surface Research Center and Institute of Ophthalmology, School of Medicine, Jinan University, Guangzhou, China (D.D.) Department of Anesthesiology, First Affiliated Hospital of Jinan University, Guangzhou, China (X.P., J.Li) Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, China (H.Q., B.W.); and Department of Pharmacy, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China (J.Liu)
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Abstract

The prevalence of obesity has markedly increased worldwide. Obese patients pose significant challenges to anesthesiologists with regard to accurate dosing of anesthetics due to potentially altered pharmacokinetics (PK). Here we determined the PK and pharmacodynamics (PD) of propofol for anesthesia induction in morbidly obese (MO) subjects (body mass index >35 kg/m2) at two dosing regimens: dosing based on total body weight and lean body weight (LBW), respectively. The propofol pharmacokinetic profile was well fitted with a two-compartment model. Both elimination clearance (223%–243% of controls, who had a body mass index <25 kg/m2; P < 0.01) and peripheral compartment volume (156%–180% of controls; P < 0.01) were significantly increased in MO subjects, resulting in an equal or decreased propofol level in plasma (total body weight–based dosing). Furthermore, propofol PD (measured by the bispectral index) was adequately described by a PK/PD model that linked an effect compartment to the two-compartment PK model through a sigmoidal Emax model. All PD parameters except EC50 values (the half maximal effect concentration) were similar (P > 0.05) between MO subjects and controls. Morbid obesity led to a significant decrease (37.9%–38.6%; P < 0.01) in EC50 values, which suggests increased brain sensitivity to propofol in the MO population. Moreover, dose reduction (i.e., dosing based on LBW) generated identical anesthetic effects in MO subjects compared with controls. In conclusion, morbid obesity significantly altered both PK and PD of propofol. LBW was a better weight-based dosing scalar for anesthesia induction with propofol in MO subjects.

Footnotes

    • Received May 16, 2016.
    • Accepted July 29, 2016.
  • D.D. and X.P. contributed equally to this work

  • This research was supported by the Fundamental Research Funds for the Central Universities [Grant 21615463] and the Natural Science Foundation of Guangdong Province PhD Start-Up Fund [Grant 2015A030310339].

  • dx.doi.org/10.1124/dmd.116.071605.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 44 (10)
Drug Metabolism and Disposition
Vol. 44, Issue 10
1 Oct 2016
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Rapid CommunicationShort Communication

Effects of Morbid Obesity on Propofol Pharmacokinetics/Pharmacodynamics

Dong Dong, Xuemei Peng, Jie Liu, Hao Qian, Jiayang Li and Baojian Wu
Drug Metabolism and Disposition October 1, 2016, 44 (10) 1579-1583; DOI: https://doi.org/10.1124/dmd.116.071605

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Rapid CommunicationShort Communication

Effects of Morbid Obesity on Propofol Pharmacokinetics/Pharmacodynamics

Dong Dong, Xuemei Peng, Jie Liu, Hao Qian, Jiayang Li and Baojian Wu
Drug Metabolism and Disposition October 1, 2016, 44 (10) 1579-1583; DOI: https://doi.org/10.1124/dmd.116.071605
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