Drug intelligence / Profile preview

alfaxalone

Development stage
Unknown
Lead developer
Jurox
Modality
Small Molecules, Peptides
Administration
Intravenous, Intramuscular
01

Overview

Alfaxalone is a synthetic neuroactive steroid and general anesthetic primarily used in veterinary medicine for the induction and maintenance of anesthesia in dogs and cats. It acts as a central nervous system depressant by modulating gamma aminobutyric acid type A (GABAA) receptors in the brain. At low concentrations it positively modulates chloride current through these receptors; at higher concentrations it acts as a GABA agonist similar to barbiturates. This results in hyperpolarization of neuronal membranes and profound sedation or anesthesia depending on dose. Alfaxalone is structurally related to allopregnanolone but lacks progestogenic or endocrine hormonal activity. It has a high therapeutic index and is considered fast acting with minimal cardiorespiratory effects when used appropriately[1][3][4][5][6].

Brand names
AlfaxanAlfaxan Multidose
Other names
3α-hydroxy-5α-pregnane-11,20-dione11-oxo-3α,5α-tetrahydroprogesterone5α-pregnan-3α-ol-11,20-dione
02

Targets

GABRR (GABA-A receptor subunit rho)PXR (Pregnane X receptor)

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