Alfaxalone
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Trade names | Alfaxan |
Other names | Alphaxalone; Alphaxolone; Alfaxolone; 3α-Hydroxy-5α-pregnane-11,20-dione; PHAX-001; Phaxan, Alphaxalone (BAN UK) |
AHFS/Drugs.com | International Drug Names |
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Pharmacokinetic data | |
Protein binding | 30–50% |
Metabolism | Hepatic |
Metabolites |
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Elimination half-life |
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renal | |
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Alfaxalone, also known as alphaxalone or alphaxolone and sold under the brand name Alfaxan, is a
Alfaxalone works as a
Veterinary use
Alfaxalone is used as an
Alfaxalone can be used as a sedative when given
Despite its use as an anesthetic, alfaxalone itself has no analgesic properties.[7]
Available forms
Though alfaxalone is not licensed for IM or
Alfaxalone is dissolved in 2-hydroxypropyl-β cyclodextrin.[14] The cyclodextrin is a large, starch-derived molecule with a hydrophobic core where alfaxalone stays, allowing the mixture to be dissolved in water and sold as an aqueous solution. They act as one unit, and only dissociate once in vivo.[11][15]
Specific populations
Alfaxalone has been used to perform
Alfaxalone has been noted to be a good anesthetic agent for dogs with
There seems to be marked difference in sex response: anaesthesia in the male rat requires about four times more than in the female.[19]
Side effects
Alfaxalone has relatively few side effects compared to other anesthetics; most notable is its lack of
Greyhounds, who are particularly susceptible to anesthetic side effects, can have decreased blood flow and oxygen supply to the liver.[17]
When no premedications are used, alfaxalone causes animals (especially cats) to be agitated when recovering.[4][13] Dogs and cats will paddle in the air, vocalize excessively, may remain rigid or twitch, and have exaggerated reactions to external stimuli such as light and noise. For this reason, it is recommended that animals recovering from anesthesia by alfaxalone stay in a quiet, dark area.[17]
Overdose
The quick metabolism and elimination of alfaxalone from the body decreases the chance of overdose.
Pharmacology
Pharmacodynamics
Alfaxalone is a
Pharmacokinetics
Alfaxalone is metabolized quickly and does not accumulate in the body; its use as an induction agent thus doesn't increase the time needed to recover from anesthesia.[4][10] If it administered more slowly by diluting it in sterile water, less actual alfaxalone is needed.[9] Alfaxalone binds to 30–50% of plasma proteins,[24] and has a terminal half-life of 25 minutes in dogs and 45 minutes in cats when given at clinical doses (2 mg/kg and 5 mg/kg respectively). The pharmacokinetics are nonlinear in cats and dogs.[14][25]
Most alfaxalone metabolism takes place in the liver, though some takes place in the
Alfaxalone is mostly excreted in the urine, though some is excreted in the bile as well.
Chemistry
Alfaxalone, also known as 11-oxo-3α,5α-tetrahydroprogesterone, 5α-pregnan-3α-ol-11,20-dione, or 3α-hydroxy-5α-pregnane-11,20-dione, is a
History
In 1941,
In 1971, a combination of alfaxalone and
Althesin was removed from the market in 1984 for causing
In 1999, a
Currently, a human form of alfaxalone is in development under the name "Phaxan": alfaxalone will be dissolved in 7-sulfo-butyl-ether-β-cyclodextrin, which, unlike the cyclodextrin used in Alfaxan, is not toxic to people.[14]
Society and culture
Generic names
Alfaxalone is the
Brand names
Alfaxalone was marketed in 1971 in combination with alfadolone acetate under the brand name Althesin for human use and Saffan for veterinary use.[17][29] Althesin was withdrawn from the market in 1984, whereas Saffan remained marketed.[30] A new formulation containing alfaxalone only was introduced for veterinary use in 1999 under the brand name Alfaxan.[17][29] Following the introduction of Alfaxan, Saffan was gradually discontinued and is now no longer marketed.[30][31] Another new formulation containing alfaxalone alone is currently under development for use in humans with the tentative brand name Phaxan.[14][32]
Availability
Alfaxalone is marketed for veterinary use under the brand name Alfaxan in a number of countries, including Australia, Belgium, Canada, France, Germany, Ireland, Japan, the Netherlands, New Zealand, South Africa, South Korea, Spain, Taiwan, the United Kingdom, and the United States.[3][33][34]
References
- ^ ISBN 978-1-4757-2085-3.
- ^ ISBN 978-94-011-4439-1.
- ^ a b c "Alfaxalone". Drugs.com.
- ^ a b c d e f Rezende M (June 2015). "Reintroduced Anesthetic Alfaxalone" (PDF). Clinician's Brief. Archived from the original (PDF) on July 23, 2015. Retrieved July 14, 2017.
- ^ a b "ALFAXAN- alfaxalone injection, solution". DailyMed. US National Library of Medicine. Retrieved July 15, 2017.
- ISBN 9780702049798.
- ^ ISBN 9780702027932.
- PMID 24754530.
- ^ ISBN 9780702027932.
- ^ PMID 16764587.
- ^ PMID 25582797.
- ^ a b Zeltzman P (November 17, 2014). "Why Administering Alfaxalone Requires A Bit of Education". Veterinary Practice News. Retrieved July 14, 2017.
- ^ a b c d e f g Nieuwendijk H (March 2011). "Alfaxalone". Veterinary Anesthesia & Analgesia Support Group. Retrieved July 14, 2017.
- ^ ISBN 9783319476094.
- PMID 21214708.
- PMID 20315061.
- ^ ISBN 9781118526200.
- ISBN 9780702027932.
- S2CID 4340317.
- PMID 3819824.
- PMID 12183676.
- ^ ISSN 0065-7743.
- PMID 7806498.
- ISBN 9780702028588.
- ^ PMID 22405473.
- ^ ISBN 9781118693148.
- ^ Liao PT (August 2016). Anesthetic and Cardio-pulmonary Effects of Propofol or Alfaxalone with or without Midazolam Co-Induction in Fentanyl Sedated Dogs (PDF) (DVM). Guelph, Ontario: University of Guelph.
- ^ "Substance Name: Alfaxalone [INN:BAN:DCF:JAN]". ChemIDplus. US National Library of Medicine.
- ^ ISBN 978-0-323-24485-5.
- ^ ISBN 978-0-7020-5423-5.
- ISBN 978-0-12-373898-1.
- ^ "Alfaxalone (PHAX-001; Phaxan)". AdisInsight. Retrieved 27 July 2017.
- ^ Official website of Alfaxan
- PMID 25428797.
[Alfaxalone] is approved in some countries (e.g., Australia, New Zealand, Europe, Korea, Japan, USA and Canada) as an IV anesthetic agent in dogs and cats.