Alfaxalone
Systematic (IUPAC) name | |
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3-hydroxypregnane-11,20-dione | |
Clinical data | |
AHFS/Drugs.com | International Drug Names |
Pregnancy cat. | ? |
Legal status | ? |
Pharmacokinetic data | |
Bioavailability | The alfaxalone molecule is solubilised in the Alfaxan formulation using 2α- hydroxypropyl β 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 |
PubChem | CID 104845 |
ChemSpider | 94637 |
UNII | BD07M97B2A |
KEGG | D07282 |
ChEMBL | CHEMBL190279 |
Chemical data | |
Formula | C21H32O3 |
Mol. mass | 332.477 g/mol |
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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. [1]
It is licensed for use in both dogs and cats.[citation needed]
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. [2]
A 1994 study found that alfaxalone binds to a different region of this receptor than the benzodiazepines. [3]
Alfaxalone is metabolised rapidly in the liver. Alfaxalone has a very short plasma elimination half-life in dogs and cats.[citation needed]
See also [edit]
References [edit]
- ^ "Alfaxalone". Drugs.com.
- ^ Harrison, N. L.; Vicini, S.; Barker, J. L. (1987). "A steroid anesthetic prolongs inhibitory postsynaptic currents in cultured rat hippocampal neurons" (pdf). The Journal of neuroscience 7 (2): 604–609. PMID 3819824.
- ^ 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.
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