Alfaxalone

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Alfaxalone
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	N01AX05 (WHO) ;
Legal status
Legal status	US: Schedule IV ;
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
	IUPAC name 3α-hydroxy-5α-pregnane-11,20-dione;
CAS Number	23930-19-0 ;
PubChem CID	104845;
ChemSpider	94637 ;
UNII	BD07M97B2A;
KEGG	D07282 ;
ChEMBL	ChEMBL190279 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C21H32O3
Molar mass	332.477 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C2[C@H]3[C@H]([C@@H]1CC[C@H](C(=O)C)[C@@]1(C)C2)CC[C@H]4C[C@H](O)CC[C@]34C;
	InChI InChI=1S/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/m0/s1 ; Key:DUHUCHOQIDJXAT-OLVMNOGESA-N ;
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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 GABA_A 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 GABA_A receptors are located extrasynaptically and are responsible for tonic inhibition. The occurrence of tonic GABA_A inhibition coincides with the expression of relatively rare receptor subunits, particularly the α4, α6, and δ subunits, and as a general 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]}

References

↑ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1094–. ISBN 978-0-412-46630-4.
↑ "Alfaxalone". Drugs.com.
↑ PMID 3819824 (PMID 3819824)
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↑ PMID 7806498 (PMID 7806498)
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↑ 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.

Template:General anesthetics Template:GABAAR PAMs

Template:Nervous-system-drug-stub

[GanellinTriggle1996-1] 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] PMID 3819824 (PMID 3819824)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand

[4] PMID 7806498 (PMID 7806498)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand

[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.

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Alfaxalone

Overview

See also

References

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