Alfaxalone
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
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. 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.
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 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.
References
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)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand - ↑ PMID 7806498 (PMID 7806498)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand - ↑ 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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