Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H32O3 |
Molecular Weight | 332.477 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@H](C(C)=O)[C@@]1(C)CC(=O)[C@@]3([H])[C@@]2([H])CC[C@@]4([H])C[C@H](O)CC[C@]34C
InChI
InChIKey=DUHUCHOQIDJXAT-OLVMNOGESA-N
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
DescriptionSources: http://www.alfaxan.co.uk/what-is-alfaxanCurator's Comment: description was created based on several sources, including:
http://www.vasg.org/pdfs/alfaxalone_vasg_05_11.pdf | https://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/UCM326904.pdf
Sources: http://www.alfaxan.co.uk/what-is-alfaxan
Curator's Comment: description was created based on several sources, including:
http://www.vasg.org/pdfs/alfaxalone_vasg_05_11.pdf | https://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/UCM326904.pdf
Alfaxalone is a rapidly acting hydrophobic synthetic neurosteroid. It is indicated for the induction and maintenance of anesthesia and for induction of anesthesia followed by maintenance with an inhalant anesthetic, in cats and dogs. Alfaxalone induces anaesthesia through activity at the gamma amino butyric acid sub-type A receptor (GABAA) present on cells in the Central Nervous System (CNS). Alfaxalone enhances the effects of GABA at the GABAA receptors resulting in opening of channels into the cells and an influx of chloride ions. This causes hyperpolarisation of the cells and inhibition of neural impulse transmission. Alfaxalone can be safely combined with premedicants (xylazine, (dex)medetomidine, acepromazine, midazolam), opioids (morphine, methadone, hydromorphone, butorphanol, nalbuphine, buprenorphine, fentanyl), and NSAIDs. Alfaxalone’s adverse reactions are: hypotension, tachycardia, apnea, hypertension, bradypnea and others.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL4187 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22538831 |
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Target ID: CHEMBL2072 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22538831 |
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Target ID: GABAA receptor (Bovine) Sources: https://www.ncbi.nlm.nih.gov/pubmed/3032320 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Alfaxan Approved UseALFAXAN is indicated for the induction and maintenance of anesthesia and for induction of anesthesia followed by maintenance with an inhalant anesthetic, in cats and dogs. Launch Date1.3468032E12 |
PubMed
Title | Date | PubMed |
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Selective cyclodextrin inhibition of alfaxolone-induced ataxia. | 1996 May |
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Plasma pharmacokinetics of alfaxalone in dogs after an intravenous bolus of Alfaxan-CD RTU. | 2006 Jul |
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In silico prediction of pregnane X receptor activators by machine learning approaches. | 2007 Jan |
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Changes in relative potency among positive GABA(A) receptor modulators upon discontinuation of chronic benzodiazepine treatment in rhesus monkeys. | 2007 May |
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A comparison of microbial growth in alfaxalone, propofol and thiopental. | 2008 Apr |
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Cardiorespiratory and anesthetic effects of clinical and supraclinical doses of alfaxalone in dogs. | 2008 Nov |
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Effect of propofol and alfaxalone on pain after ovariohysterectomy in cats. | 2010 Mar 13 |
Patents
Sample Use Guides
Induction of general anesthesia in cats: range 2.2 - 9.7 mg/kg for cats that did not receive a preanesthetic and 1.0 - 10.8 mg/kg for cats that received a preanesthetic.
Induction of general anesthesia in dogs: range 1.5 - 4.5 mg/kg for dogs that did not receive a preanesthetic and between 0.2 - 3.5 mg/kg for dogs that received a preanesthetic.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19535226
Alfaxalone at a concentration of 50 uM reversibly blocked ongoing Seizure like events (SLEs) in organotypic hippocampal slice cultures. At a concentration of 20 uM it did not block ongoing SLEs but significantly reduced strength and duration of SLEs.
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NCI_THESAURUS |
C245
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WHO-VATC |
QN01AX05
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WHO-ATC |
N01AX05
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CFR |
21 CFR 522.52
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DEA NO. |
2731
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SUB05316MIG
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m1498
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3218
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1544577
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BD07M97B2A
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C72161
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CHEMBL190279
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C006477
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ALFAXALONE
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133
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23930-19-0
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104845
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ACTIVE MOIETY