Pharmacokinetics and Pharmacodynamics of Ketamine - UTU Research Portal

A3 Refereed book chapter or chapter in a compilation book

Pharmacokinetics and Pharmacodynamics of Ketamine

Authors: Saari, Teijo I.; Himmelseher, Sabine; Peltoniemi, Marko; Brinck, Elina C.

Editors: Himmelseher, Sabine

Edition: 1

Publisher: Humana Press Inc.

Publication year: 2025

Book title : Ketamine: From Neurobiology to Emergency and Anesthesia Care, Volume I

Series title: Neuromethods

Number in series: 224

Volume: 224

First page : 359

Last page: 373

ISBN: 978-1-0716-4602-1

eISBN: 978-1-0716-4603-8

ISSN: 0893-2336

eISSN: 1940-6045

DOI: https://doi.org/10.1007/978-1-0716-4603-8_17

Publication's open availability at the time of reporting: No Open Access

Publication channel's open availability : No Open Access publication channel

Web address : https://doi.org/10.1007/978-1-0716-4603-8_17

Abstract

The non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist ketamine offers a complex pharmacological profile which has led to its established role in anesthesia, analgesia, and psychiatry. Pharmacokinetic (PK) and pharmacodynamic (PD) models have characterized ketamine’s unique pharmacokinetics which are affected by many factors, such as route of administration, bioavailability, and patient characteristics. Ketamine’s rapid onset and offset of effects can be described with two- or three-compartment models without taking metabolites into account. Ketamine racemate is an equimolar mixture of dextrorotatory S(+)- and levorotatory R(−)-ketamine. PK/PD models have helped to explain the differences between the racemate and its stereoisomers, confirming the approximately two times greater clinical potency of esketamine versus racemate in analgesic and anesthetic, and likely antidepressant action. Recent PK/PD data highlight new insights for patient management, including better-informed approaches to opioid-related respiratory depression and chronic pain. PK/PD models can feature the complex relationships between ketamine administration, clinical response, and safety issues, improving ketamine use schedules while reducing unwanted effects.