Mechanism-based pharmacodynamic model for propofol haemodynamic effects in healthy volunteers☆. 2022

Hong Su, and Douglas J Eleveld, and Michel M R F Struys, and Pieter J Colin
Department of Anesthesiology, University Medical Center Groningen, University of Groningen, Groningen, the Netherlands.

The adverse haemodynamic effects of the intravenous anaesthetic propofol are well known, yet few empirical models have explored the dose-response relationship. Evidence suggests that hypotension during general anaesthesia is associated with postoperative mortality. We developed a mechanism-based model that quantitatively characterises the magnitude of propofol-induced haemodynamic effects during general anaesthesia. Mean arterial pressure (MAP), heart rate (HR) and pulse pressure (PP) measurements were available from 36 healthy volunteers who received propofol in a step-up and step-down fashion by target-controlled infusion using the Schnider pharmacokinetic model. A mechanistic pharmacodynamic model was explored based on the Snelder model. To benchmark the performance of this model, we developed empirical models for MAP, HR, and PP. The mechanistic model consisted of three turnover equations representing total peripheral resistance (TPR), stroke volume (SV), and HR. Propofol-induced changes were implemented by Emax models on the zero-order production rates of the turnover equations for TPR and SV. The estimated 50% effective concentrations for propofol-induced changes in TPR and SV were 2.96 and 0.34 μg ml-1, respectively. The goodness-of-fit for the mechanism-based model was indistinguishable from the empirical models. Simulations showed that predictions from the mechanism-based model were similar to previously published MAP and HR observations. We developed a mechanism-based pharmacodynamic model for propofol-induced changes in MAP, TPR, SV, and HR as a potential approach for predicting haemodynamic alterations. NCT02043938.

UI MeSH Term Description Entries
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000768 Anesthesia, General Procedure in which patients are induced into an unconscious state through use of various medications so that they do not feel pain during surgery. Anesthesias, General,General Anesthesia,General Anesthesias
D015742 Propofol An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS. Disoprofol,2,6-Bis(1-methylethyl)phenol,2,6-Diisopropylphenol,Aquafol,Diprivan,Disoprivan,Fresofol,ICI-35,868,ICI-35868,Ivofol,Propofol Abbott,Propofol Fresenius,Propofol MCT,Propofol Rovi,Propofol-Lipuro,Recofol,2,6 Diisopropylphenol,ICI 35,868,ICI 35868,ICI35,868,ICI35868
D018686 Anesthetics, Intravenous Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174) Intravenous Anesthetic,Intravenous Anesthetics,Anesthetic, Intravenous
D064368 Healthy Volunteers Persons with no known significant health problems who are recruited to participate in research to test a new drug, device, or intervention as controls for a patient group. (from http://clinicalcenter.nih.gov/recruit/volunteers.html, accessed 2/14/2013) Healthy Participants,Healthy Subjects,Human Volunteers,Normal Volunteers,Healthy Participant,Healthy Subject,Healthy Volunteer,Human Volunteer,Normal Volunteer,Participant, Healthy,Participants, Healthy,Subject, Healthy,Subjects, Healthy,Volunteer, Healthy,Volunteer, Human,Volunteer, Normal,Volunteers, Human,Volunteers, Normal

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