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Alfaxalone
Systematic (IUPAC) name
3-hydroxypregnane-11,20-dione
Identifiers
CAS number 23930-19-0
ATC code N01AX05
PubChem 104845
ChemSpider 94637
Chemical data
Formula C21H32O3 
Mol. mass 332.477 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability The alfaxalone molecule is solubilised in the Alfaxan formulation using 2α- hydroxypropyl ß cyclodextrin. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
Therapeutic considerations
Pregnancy cat.  ?
Legal status

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 (1), 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 (2). Alfaxalone is metabolised rapidly in the liver. Alfaxalone has a very short plasma elimination half-life in dogs and cats

See also

References

(1) Harrison NL, Vicini S, Barker JL. A steroid anesthetic prolongs inhibitory postsynaptic currents in cultured rat hippocampal neurons. The Journal of Neuroscience 1987;7(2):604-609.

(2) 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.

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