Alfaxalone

Alfaxalone

File:Alphaxolone-2D-skeletal.png
Systematic (IUPAC) name
3-hydroxypregnane-11,20-dione
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.
Identifiers
CAS Number	23930-19-0
ATC code	N01AX05 (WHO)
PubChem	CID 104845
ChemSpider	94637
Chemical data
Formula	C21H32O3
Molar mass	332.477 g/mol[[]]

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

• Ganaxolone
• Minaxolone

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.

pt:Alfaxalona