Alfaxolone

Alfaxolone (also known as Alphaxalone) is a neuroactive steroid and general anesthetic. It is used in veterinary medicine, particularly for the induction of anesthesia in animals. Alfaxolone acts on the GABA receptor, enhancing its effects and leading to a state of general anesthesia.

History

Alfaxolone was first synthesized in the 1970s by Organon International, a pharmaceutical company. It was initially marketed under the brand name Althesin for use in human anesthesia, but was withdrawn from the market due to concerns about its safety profile.

Pharmacology

Alfaxolone is a potent positive allosteric modulator of the GABA receptor, the main inhibitory receptor in the brain. By enhancing the effects of GABA, alfaxolone induces a state of general anesthesia. It is also a potent anxiolytic, anticonvulsant, and muscle relaxant.

Clinical use

In veterinary medicine, alfaxolone is used for the induction and maintenance of anesthesia in a variety of animals, including dogs, cats, and horses. It is also used in laboratory research to study the effects of neuroactive steroids on the brain and behavior.

Side effects

The most common side effects of alfaxolone include respiratory depression, hypotension, and bradycardia. Rare but serious side effects include allergic reactions and anaphylaxis.

See also

• Neuroactive steroid
• General anesthetic
• GABA receptor