Alfaxolone
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| Clinical data | |
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| Trade names | Alfaxan |
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| Pharmacokinetic data | |
| Protein binding | 30–50% |
| Metabolism | Hepatic |
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| Excretion | Mostly renal |
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| Synonyms | Alphaxalone; Alphaxolone; Alfaxolone; 3α-Hydroxy-5α-pregnane-11,20-dione; PHAX-001; Phaxan |
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| ECHA InfoCard | 100.164.405 |
| Chemical and physical data | |
| Formula | C21H32O3 |
| Molar mass | 332.477 g/mol |
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Alfaxalone, also known as alphaxalone or alphaxolone, is a neuroactive steroid and general anesthetic. It is used in veterinary practice under the trade name Alfaxan as an induction agent for anesthesia and as an injectable anesthetic. Though it is more expensive than other induction agents, it often preferred due to the lack of depressive effects on the cardiovascular system. The most common side effect is respiratory depression; when premedications aren't given, patients also become agitated and hypersensitive when waking up.
Alfaxalone works as a positive allosteric modulator on GABAA receptors and, at high concentrations, as a direct agonist of the GABAA receptor. It is cleared quickly by the liver, giving it a relatively short terminal half-life and preventing it from accumulating in the body, lowering the chance of overdose.
Alfaxalone is used as an induction agent, an injectable anesthetic, and as a sedative in animals. While its commonly used in cats and dogs, it has also been successfully used in rabbits,horses, sheep, pigs, and exotics such as red-eared turtles, axolotl, green iguanas, marmosets, and koi fish. As an induction agent, alfaxalone causes the animal to relax enough to be intubated, allowing inhalational anesthesia to be administered. Premedication (administering sedative drugs prior this event) increases the potency of alfaxalone as an induction agent. It can be used instead of gas anesthetics in surgeries that are under 30 minutes, where it is being given at a constant rate via IV (constant rate infusion); this is especially useful in procedures such as bronchoscopies or repairing tracheal tears, as there is no endotracheal tube in the way. Once the administration of alfaxalone stops, the animal quickly recovers from anesthesia.
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