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Priscilla J. Garcia

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date: 28 January 2022

Opioids bind to stereospecific opioid receptors both centrally in the central nervous system (CNS) and peripherally outside the CNS to produce analgesia as well as other side effects. The intersubject variability in response to opioids is due to pharmacokinetic and pharmacodynamic parameters. The speed of onset of opioid effect is influenced by both the lipid solubility and its protein binding. The main pharmacodynamic difference between the different opioids is the potency and rate of equilibration between plasma and the site of drug effect. With regard to neuraxial administration, lipid solubility is a primary determinant of how well a drug will penetrate the dura. The properties of various opioids including morphine, fentanyl, sufentanil, remifentanil, alfentanil, and meperidine as well as the antagonist naloxone are discussed.

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