Alfaxalone

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Alfaxalone
Alphaxolone.svg
Clinical data
AHFS/Drugs.com International Drug Names
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability The alfaxalone molecule is solubilised using SBECD. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.164.405
Chemical and physical data
Formula C21H32O3
Molar mass 332.477 g/mol
3D model (Jmol)
 NYesY (what is this?)  (verify)

Alfaxalone (INN, JAN), also known as alphaxalone or alphaxolone (BAN), is a neuroactive steroid and general anaesthetic.[1] It is used in veterinary practice under the trade name Alfaxan,[2] and is licensed for use in both dogs and cats.[citation needed] Along with alfadolone, it is also one of the constituents of anesthetic drug mixture althesin.

Unlike some of its predecessors alfaxalone is not associated with histamine release and anaphylaxis.[citation needed]

A study 1987 found the primary mechanism for the anaesthetic action of alfaxalone to be modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to GABAA cell surface receptors.[3]

A 1994 study found that alfaxalone binds to a different region of this receptor than the benzodiazepines.[4] These benzodiazepine-insensitive GABAA receptors are located extrasynaptically and are responsible for tonic inhibition. The occurrence of tonic GABAA inhibition coincides with the expression of relatively rare receptor subunits, particularly the α4, α6, and δ subunits, and as a rule of thumb, δ subunit-containing receptors are extrasynaptic.[5]

Alfaxalone is metabolised rapidly in the liver. It has a very short plasma elimination half-life in dogs and cats.[citation needed]

See also[edit]

References[edit]

  1. ^ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1094–. ISBN 978-0-412-46630-4. 
  2. ^ "Alfaxalone". Drugs.com. 
  3. ^ Harrison, N. L.; Vicini, S.; Barker, J. L. (1987). "A steroid anesthetic prolongs inhibitory postsynaptic currents in cultured rat hippocampal neurons" (pdf). Journal of Neuroscience. 7 (2): 604–609. PMID 3819824. 
  4. ^ Mihic, S. J.; Whiting, P. J.; Klein, R. L.; Wafford, K. A.; Harris, R. A. (1994). "A single amino acid of the human gamma-aminobutyric acid type A receptor gamma 2 subunit determines benzodiazepine efficacy" (pdf). The Journal of Biological Chemistry. 269 (52): 32768–32773. PMID 7806498. 
  5. ^ Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research 86 (2-3): 113–23. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226.