alfaxalone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	133	23930-19-0

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alfaxolone
alfaxalone
alfadione
alphaxalone

Molecular weight: 332.48
Formula: C21H32O3
CLOGP: 3.18
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 54.37
ALOGS: -4.14
ROTB: 1

Drug dosage:

None

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1972	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N01AX05	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Other general anesthetics
MeSH PA	D000777	Anesthetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D000081227	Neurosteroids
MeSH PA	D018377	Neurotransmitter Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

None

🐶 Veterinary Drug Use

Species	Use	Relation
Cats	Induction and maintenance of general anesthesia	Indication
Cats	Anesthesia followed by maintenance with an inhalant anesthetic	Indication
Dogs	Induction and maintenance of general anesthesia	Indication
Dogs	Anesthesia followed by maintenance with an inhalant anesthetic	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Alfaxan Multidose	Jurox Pty. Ltd.	1

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sodium- and chloride-dependent GABA transporter 1	Transporter	P30531	SC6A1_HUMAN					WOMBAT-PK
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN		EC50	5.70		WOMBAT-PK
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel	P18507 P47869 P47870	GBRG2_HUMAN GBRA2_HUMAN GBRB2_HUMAN		EC50	5.70		CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	6.52		CHEMBL

External reference:

ID	Source
D07282	KEGG_DRUG
1544577	RXNORM
C0051482	UMLSCUI
CHEBI:34531	CHEBI
EY4	PDB_CHEM_ID
CHEMBL190279	ChEMBL_ID
DB11371	DRUGBANK_ID
C006477	MESH_SUPPLEMENTAL_RECORD_UI
5461	IUPHAR_LIGAND_ID
3218	INN_ID
BD07M97B2A	UNII
104845	PUBCHEM_CID
116553001	SNOMEDCT_US
387037009	SNOMEDCT_US

Pharmaceutical products:

None