Alfaxolone/alfadolone (brand names Althesin (human), Saffan (veterinary)) is a short acting intravenous anesthetic agent. It was withdrawn from the market due to severe drug reactions. It is composed of a 3:1 mixture of alfaxalone and alfadolone, two neurosteroids.
Alfaxolone/alfadolone is short-duration, intravenous anesthetic made from a combination of two steroidal compounds, alfaxalone and alfadolone, of which the former is the primary anesthetic agent. Alfadolone acts to increase the solubility of the mixture in which it is dissolved, a polyethylated castor oiladjuvant.[1] Anesthetic efficacy is achieved by allosteric potentiation of the GABAA chloride channel to produce 'fast' synaptic inhibition.[2]
Clinical useedit
Alfaxolone/alfadolone is short-acting, rapid onset anesthetic which has been used for out-patient surgery. It does not have significant analgesic properties and anesthesia has often been maintained with inhalational anesthetics such as halothane. These have also been accompanied by neuromuscular blockers. Procedures carried out under this drug are greatly varied and have included orthopedic, gynecological, dental and urological surgery. Notable effects include a drop in arterial and venous pressure in a quarter of patients; this is accompanied by a compensatory mild tachycardia in around 35% of those observed in a population skewed towards geriatrics.[1]
Cremophor EL (aka. Polyoxyl 35 Castor Oil, a surfactant and derivative of castor oil) was the solubilizing agent (excipient / additive) of Althesin. [3]
A study 2001 found that Cremophor EL, when previously used as a solubilizing agent in lipid emulsions, was responsible for severe anaphylactoid reactions. Drugs using it were reformulated to use other emulsifiers. [4] Alfaxolone/alfadolone has been re-branded as "Saffan" and is available for use in veterinary anaesthesia. [5][6]
Referencesedit
^ abDechêne JP (March 1976). "Alphathesin, a new steroid anaesthetic agent". Canadian Anaesthetists' Society Journal. 23 (2): 163–9. doi:10.1007/BF03005687. PMID 943212.
^Clarke RS, Dundee JW, Carson IW (October 1973). "Proceedings: A new steroid anaesthetic-althesin". Proceedings of the Royal Society of Medicine. 66 (10): 1027–30. doi:10.1177/003591577306601023. PMC1645602. PMID 4148526.
^MacPherson RD (October 2001). "Pharmaceutics for the anaesthetist". Anaesthesia. 56 (10): 965–79. doi:10.1111/j.1365-2044.2001.02216.x. PMID 11576099. S2CID 10768907.
^Dyson DH, Allen DG, Ingwersen W, Pascoe PJ, O'Grady M (April 1987). "Effects of saffan on cardiopulmonary function in healthy cats". Canadian Journal of Veterinary Research. 51 (2): 236–9. PMC1255310. PMID 3111675.
^Nadeson R, Goodchild CS (May 2001). "Antinociceptive properties of neurosteroids III: experiments with alphadolone given intravenously, intraperitoneally, and intragastrically". British Journal of Anaesthesia. 86 (5): 704–8. doi:10.1093/bja/86.5.704. PMID 11575348.
January 01, 1970
alfaxolone, alfadolone, brand, names, althesin, human, saffan, veterinary, short, acting, intravenous, anesthetic, agent, withdrawn, from, market, severe, drug, reactions, composed, mixture, alfaxalone, alfadolone, neurosteroids, combination, ofalfaxalonegener. Alfaxolone alfadolone brand names Althesin human Saffan veterinary is a short acting intravenous anesthetic agent It was withdrawn from the market due to severe drug reactions It is composed of a 3 1 mixture of alfaxalone and alfadolone two neurosteroids Alfaxolone alfadoloneCombination ofAlfaxaloneGeneral anaestheticAlfadoloneHypnoticClinical dataTrade namesAlthesin SaffanOther namesCT 1341 Alphadione Alphathesin Aurantex AlfatesineRoutes ofadministrationIntravenousIdentifiersCAS Number23930 19 0 Y14107 37 0PubChem CID24732UNIIBD07M97B2AOE1C96974E YCompTox Dashboard EPA DTXSID001001405 N Y what is this verify Mechanism editAlfaxolone alfadolone is short duration intravenous anesthetic made from a combination of two steroidal compounds alfaxalone and alfadolone of which the former is the primary anesthetic agent Alfadolone acts to increase the solubility of the mixture in which it is dissolved a polyethylated castor oil adjuvant 1 Anesthetic efficacy is achieved by allosteric potentiation of the GABAA chloride channel to produce fast synaptic inhibition 2 Clinical use editAlfaxolone alfadolone is short acting rapid onset anesthetic which has been used for out patient surgery It does not have significant analgesic properties and anesthesia has often been maintained with inhalational anesthetics such as halothane These have also been accompanied by neuromuscular blockers Procedures carried out under this drug are greatly varied and have included orthopedic gynecological dental and urological surgery Notable effects include a drop in arterial and venous pressure in a quarter of patients this is accompanied by a compensatory mild tachycardia in around 35 of those observed in a population skewed towards geriatrics 1 Cremophor EL aka Polyoxyl 35 Castor Oil a surfactant and derivative of castor oil was the solubilizing agent excipient additive of Althesin 3 A study 2001 found that Cremophor EL when previously used as a solubilizing agent in lipid emulsions was responsible for severe anaphylactoid reactions Drugs using it were reformulated to use other emulsifiers 4 Alfaxolone alfadolone has been re branded as Saffan and is available for use in veterinary anaesthesia 5 6 References edit a b Dechene JP March 1976 Alphathesin a new steroid anaesthetic agent Canadian Anaesthetists Society Journal 23 2 163 9 doi 10 1007 BF03005687 PMID 943212 Belelli D Lambert JJ July 2005 Neurosteroids endogenous regulators of the GABA A receptor Nature Reviews Neuroscience 6 7 565 75 doi 10 1038 nrn1703 PMID 15959466 S2CID 12596378 Clarke RS Dundee JW Carson IW October 1973 Proceedings A new steroid anaesthetic althesin Proceedings of the Royal Society of Medicine 66 10 1027 30 doi 10 1177 003591577306601023 PMC 1645602 PMID 4148526 MacPherson RD October 2001 Pharmaceutics for the anaesthetist Anaesthesia 56 10 965 79 doi 10 1111 j 1365 2044 2001 02216 x PMID 11576099 S2CID 10768907 Dyson DH Allen DG Ingwersen W Pascoe PJ O Grady M April 1987 Effects of saffan on cardiopulmonary function in healthy cats Canadian Journal of Veterinary Research 51 2 236 9 PMC 1255310 PMID 3111675 Nadeson R Goodchild CS May 2001 Antinociceptive properties of neurosteroids III experiments with alphadolone given intravenously intraperitoneally and intragastrically British Journal of Anaesthesia 86 5 704 8 doi 10 1093 bja 86 5 704 PMID 11575348 Retrieved from https en wikipedia org w index php title Alfaxolone alfadolone amp oldid 1184337828, wikipedia, wiki, book, books, library,
