Drug intelligence / Profile preview

methoxyflurane

Development stage
Phase 4
Lead developer
Medical Developments International
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation
01

Overview

Methoxyflurane is a fluorinated isopropyl ether and volatile inhalation anesthetic, primarily used today as an inhaled analgesic for the short-term relief of moderate to severe pain, especially following trauma or during brief medical procedures. Originally introduced in the 1960s as a general anesthetic, its use for anesthesia has been largely discontinued due to concerns about nephrotoxicity at higher doses. At lower analgesic doses (typically up to 6 mL per day), it provides rapid-onset pain relief with minimal risk of kidney toxicity in most patients. Methoxyflurane acts by potentiating gamma-aminobutyric acid (GABA) receptor and glycine receptor activity in the central nervous system, reducing neuronal excitability and altering gap junction-mediated cell-cell coupling. It also interacts with other targets such as ATP synthase and NADH dehydrogenase. The drug is self-administered via a portable hand-held inhaler device under supervision, offering a non-opioid alternative to morphine or nitrous oxide for acute pain management[1][2][3][4][6][8].

Brand names
Penthrox
Other names
2,2-dichloro-1,1-difluoroethyl methyl ether
02

Targets

Gap junction alpha-8 proteinGlycine receptorGABRR (GABA-A receptor subunit rho)

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