Drug intelligence / Profile preview

halothane

Development stage
Unknown
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Inhalation
01

Overview

Halothane is a nonflammable, halogenated hydrocarbon general inhalation anesthetic used for the induction and maintenance of general anesthesia. It provides relatively rapid induction and recovery with little or no excitement. Halothane acts primarily by depressing nerve conduction, breathing, and cardiac contractility through its effects on multiple ion channels in the central nervous system. Its immobilizing effects are attributed to binding to potassium channels in cholinergic neurons as well as NMDA receptors and calcium channels, leading to neuronal hyperpolarization and overall inhibition of neural activity. About 15–20% of halothane is metabolized hepatically (mainly via CYP2E1), which can rarely result in immune-mediated hepatitis. Halothane was discovered in 1951 and approved for medical use in the United States in 1958; it has largely been replaced by newer agents such as sevoflurane but remains on the World Health Organization's List of Essential Medicines[1][2][6].

Brand names
Fluothane
Other names
2-bromo-2-chloro-1,1,1-trifluoroethane
02

Targets

NaV (Voltage-gated sodium channels)HTR3A (5-hydroxytryptamine receptor 3A)GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)CHRNA7 (α7 nicotinic receptor)KCNK2 (Potassium channel subfamily K member 2)

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