General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics

The introduction of general anesthetics in the mid-19th century is considered one of the greatest contributions to medical practice. It was the first time that complicated surgical interventions became feasible, without putting an excessive strain on the patient. The first general anesthetics—diethy...

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Main Authors: Ružena Čižmáriková, Ladislav Habala, Jindra Valentová
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Pharmaceuticals
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Online Access:https://www.mdpi.com/1424-8247/18/2/250
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author Ružena Čižmáriková
Ladislav Habala
Jindra Valentová
author_facet Ružena Čižmáriková
Ladislav Habala
Jindra Valentová
author_sort Ružena Čižmáriková
collection DOAJ
description The introduction of general anesthetics in the mid-19th century is considered one of the greatest contributions to medical practice. It was the first time that complicated surgical interventions became feasible, without putting an excessive strain on the patient. The first general anesthetics—diethyl ether, chloroform, and nitrous oxide—were limited by often severe adverse reactions and a narrow therapeutic window. They were later succeeded by modern anesthetics, with high anesthetic effect along with diminished toxicity. As with other medical drugs, many anesthetic compounds contain chiral centers in their molecules. Although currently used as racemates, the pharmacological activity of the respective enantiomerically pure antipodes can vary considerably, as can their adverse effects. Herein, we report on the available studies into the differences in bioactivity and toxicity between the enantiomers of chiral anesthetic agents. Both inhalational and intravenous anesthetics are discussed. Aspects of pharmacodynamics and pharmacokinetics are surveyed as well. The results could stimulate further research into the potential application of single-enantiomer anesthetics in clinical practice.
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spelling doaj-art-2cb4c5fa82d34725923c1fdb2cfcd7892025-08-20T02:03:27ZengMDPI AGPharmaceuticals1424-82472025-02-0118225010.3390/ph18020250General Anesthetics: Aspects of Chirality, Pharmacodynamics, and PharmacokineticsRužena Čižmáriková0Ladislav Habala1Jindra Valentová2Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Odbojárov 10, SK-833232 Bratislava, SlovakiaDepartment of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Odbojárov 10, SK-833232 Bratislava, SlovakiaDepartment of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Odbojárov 10, SK-833232 Bratislava, SlovakiaThe introduction of general anesthetics in the mid-19th century is considered one of the greatest contributions to medical practice. It was the first time that complicated surgical interventions became feasible, without putting an excessive strain on the patient. The first general anesthetics—diethyl ether, chloroform, and nitrous oxide—were limited by often severe adverse reactions and a narrow therapeutic window. They were later succeeded by modern anesthetics, with high anesthetic effect along with diminished toxicity. As with other medical drugs, many anesthetic compounds contain chiral centers in their molecules. Although currently used as racemates, the pharmacological activity of the respective enantiomerically pure antipodes can vary considerably, as can their adverse effects. Herein, we report on the available studies into the differences in bioactivity and toxicity between the enantiomers of chiral anesthetic agents. Both inhalational and intravenous anesthetics are discussed. Aspects of pharmacodynamics and pharmacokinetics are surveyed as well. The results could stimulate further research into the potential application of single-enantiomer anesthetics in clinical practice.https://www.mdpi.com/1424-8247/18/2/250general anestheticsinhalational anestheticsintravenous anestheticsenantiomersstereochemistrychirality
spellingShingle Ružena Čižmáriková
Ladislav Habala
Jindra Valentová
General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
Pharmaceuticals
general anesthetics
inhalational anesthetics
intravenous anesthetics
enantiomers
stereochemistry
chirality
title General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
title_full General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
title_fullStr General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
title_full_unstemmed General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
title_short General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
title_sort general anesthetics aspects of chirality pharmacodynamics and pharmacokinetics
topic general anesthetics
inhalational anesthetics
intravenous anesthetics
enantiomers
stereochemistry
chirality
url https://www.mdpi.com/1424-8247/18/2/250
work_keys_str_mv AT ruzenacizmarikova generalanestheticsaspectsofchiralitypharmacodynamicsandpharmacokinetics
AT ladislavhabala generalanestheticsaspectsofchiralitypharmacodynamicsandpharmacokinetics
AT jindravalentova generalanestheticsaspectsofchiralitypharmacodynamicsandpharmacokinetics