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The Pharmacology of Intravenous Opioids

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Geriatric Anesthesiology

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Abstract

This chapter reviews the pharmacology of the intravenously administered opioids in the practice of geriatric anesthesiology. These drugs include morphine, meperidine, hydromorphone, fentanyl, sufentanil, and methadone. It is important that anesthesiologists understand the differences in pharmacology of opioids in elderly patients, in order to choose the appropriate drug and titrate precisely to achieve the desired analgesic effects while minimizing the risks of opioid toxicity. The key points for this chapter are as follows: (1) Elderly patients need about half the dose as younger patients, (2) The primary reason is pharmacodynamics (the elderly brain is more sensitive to opioids), (3) The pharmacokinetic changes with age are modest, (4) Studies in elderly animals show reduced numbers of μ receptors with increased age. That does not explain the reduction in dose, as decreased receptor density should decrease sensitivity to opioids. The enhancement in drug effect seen in the clinic is more likely attributable to changes in cyclonucleotide coupling and other downstream changes that occur in aging, and (5) Mepiridine should be used with caution in elderly patients due to its effects on myocardium, pharmacokinetics related to its metabolites, and its delirogenic properties.

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Notes

  1. 1.

    Data extensively reanalyzed to obtain volume and clearance estimates.

  2. 2.

    Original data provided by S. Bjorkman and fit using population model to create estimates in Table 18.1.

  3. 3.

    Based on a time to peak of 8.5 min in goats ()! It is not great, but it is the best onset data available.

  4. 4.

    Based on a time to peak effect of 15–20 min.

  5. 5.

    Scaled to fentanyl based on relative electroencephalogram (EEG) potency of fentanyl [63] and sufentanil [79].

  6. 6.

    Scaled to fentanyl based on the relative EEG potency of fentanyl and remifentanil [65].

  7. 7.

    he MEC range given by Dahlstrom was 6–31 ng/mL, with a mean of 16 ng/mL. We chose 8 ng/mL, at the lower end of the reported range, because the average value of 16 ng/mL predicted equianalgesic morphine that seemed excessive.

  8. 8.

    This was the most difficult potency to determine from the literature. Hill and Zacny documented a tenfold bolus dose potency difference versus morphine, which was the final basis for calculating this number and is similar to the value suggested by the Coda paper.

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Authors and Affiliations

  1. Department of Anesthesiology, Medical University of South Carolina, Charleston, SC, USA

    Stephanie Whitener

  2. Department of Anesthesiology, Vanderbilt University Medical Center, Nashville, TN, USA

    Matthew D. McEvoy

  3. Department of Anesthesiology, Perioperative and Pain Medicine, Stanford University, Palo Alto, CA, USA

    Steven L. Shafer & Pamela Flood

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  1. Stephanie Whitener
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  2. Matthew D. McEvoy
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  3. Steven L. Shafer
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  4. Pamela Flood
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Correspondence to Stephanie Whitener .

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Editors and Affiliations

  1. Department of Anesthesia and Perioperative Medicine, Medical University of South Carolina, Charleston, South Carolina, USA

    J. G. Reves

  2. Department of Anesthesia, Critical Care and Pain Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts, USA

    Sheila Ryan Barnett

  3. Department of Anesthesia and Perioperative Medicine, Department of Anesthesiology, Medical University of South Carolina, Charleston, South Carolina, USA

    Julie R. McSwain

  4. Department of Anesthesiology and Pain Medicine, University of Washington, Seattle, Washington, USA

    G. Alec Rooke

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Whitener, S., McEvoy, M.D., Shafer, S.L., Flood, P. (2018). The Pharmacology of Intravenous Opioids. In: Reves, J., Barnett, S., McSwain, J., Rooke, G. (eds) Geriatric Anesthesiology. Springer, Cham. https://doi.org/10.1007/978-3-319-66878-9_18

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