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Alfaxalone (INN, also known as alphaxalone or alphaxolone) is a neurosteroid general anaesthetic. It is one of the constituents of althesin. It is used in veterinary practice under the tradename Alfaxan. It is licensed for use in both dogs and cats. Unlike some of its predecessors Alfaxalone is not associated with histamine release and anaphylaxis. The primary mechanism for the anaesthetic action of alfaxalone is modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to GABAA cell surface receptors. It has also been shown that Alfaxalone binds to a different region of this receptor than the benzodiazipines (1). Alfaxalone is metabolised rapidly in the liver. Alfaxalone has a very short plasma elimination half-life in dogs and cats
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- Mihic SJ, Whiting PJ, Klein RL, et al. A single amino acid of the human gamma-aminobutyric acid type A receptor gamma 2 subunit determines benzodiazepine efficacy. J Biol Chem 1994;269:32768-32773.
