Drug intelligence / Profile preview

isoflurane

Development stage
Approved
Lead developer
Baxter Healthcare Corporation
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation
01

Overview

Isoflurane (Chinese name: 异氟醚 or 异氟烷) is a volatile halogenated ether used as an inhalational general anesthetic for both induction and maintenance of anesthesia in humans and animals. It is a structural isomer of enflurane with similar pharmacological properties but greater chemical stability. Isoflurane acts primarily by enhancing the activity of gamma-aminobutyric acid type A (GABA-A) receptors in the central nervous system and also modulates other ion channels such as glycine receptors and certain potassium channels. Its effects include deep suppression of respiratory and cardiovascular systems proportional to dose; it provides good muscle relaxation but can irritate airways causing cough or breath-holding during induction. Isoflurane has minimal hepatic metabolism (<0.17%), resulting in low hepatotoxicity risk compared to older agents like halothane; however, rare cases of severe liver injury have been reported. It may trigger malignant hyperthermia in susceptible individuals due to its action on skeletal muscle calcium regulation[1][4][6]. Isoflurane was first approved for clinical use in the United States in 1979 and remains on the World Health Organization's List of Essential Medicines[1][5].

Brand names
Forane
Other names
异氟醚异氟烷1-氯-1-(二氟甲氧基)-2,2,2-三氟乙烷1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
02

Targets

GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)Nicotinic Acetylcholine ReceptorGLRA1 (Glycine receptor subunit Alpha-1)KCNK2 (Potassium channel subfamily K member 2)

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