Scroll

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

Stem definition	Drug id	CAS RN
	1109	33125-97-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: etomidate (+)-Etomidate amidate D-Etomidate hypnomidate	Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic. Molecular weight: 244.29 Formula: C14H16N2O2 CLOGP: 2.42 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 44.12 ALOGS: -2.71 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

etomidate
(+)-Etomidate
amidate
D-Etomidate
hypnomidate

Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.

Molecular weight: 244.29
Formula: C14H16N2O2
CLOGP: 2.42
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 44.12
ALOGS: -2.71
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.05 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.46 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	2.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	13 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.23 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 7, 1982	FDA	HOSPIRA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac arrest	94.89	42.49	48	1536	83603	50519937
Anaphylactic shock	86.76	42.49	30	1554	20125	50583415
Fear	75.78	42.49	25	1559	14524	50589016
Renal injury	75.27	42.49	22	1562	8589	50594951
Bradycardia	73.06	42.49	37	1547	64389	50539151
Hypotension	61.61	42.49	54	1530	235415	50368125
Emotional distress	55.94	42.49	24	1560	28639	50574901
Renal failure	55.71	42.49	37	1547	106596	50496944
Anhedonia	52.13	42.49	17	1567	9507	50594033
Multiple organ dysfunction syndrome	45.86	42.49	25	1559	50312	50553228
Injury	43.74	42.49	24	1560	48901	50554639

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Fear	121.42	38.61	39	1998	9465	29563025
Injury	108.80	38.61	43	1994	19003	29553487
Renal injury	106.72	38.61	36	2001	10166	29562324
Multiple organ dysfunction syndrome	105.27	38.61	61	1976	63055	29509435
Emotional distress	99.51	38.61	37	2000	13858	29558632
Anhedonia	93.79	38.61	30	2007	7170	29565320
Anaphylactic shock	79.23	38.61	31	2006	13305	29559185
Unevaluable event	78.16	38.61	39	1998	29812	29542678
Serotonin syndrome	67.82	38.61	30	2007	17482	29555008
Renal failure	66.47	38.61	59	1978	118540	29453950
Stress	58.95	38.61	29	2008	21461	29551029
Thyrotoxic crisis	50.07	38.61	10	2027	349	29572141
Anxiety	48.78	38.61	43	1994	85322	29487168
Hyperthermia malignant	47.76	38.61	13	2024	1771	29570719
Methaemoglobinaemia	46.88	38.61	14	2023	2657	29569833
Pseudomonal sepsis	45.55	38.61	14	2023	2928	29569562
Burkholderia test positive	39.88	38.61	10	2027	989	29571501

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Fear	175.72	36.88	59	3569	20112	64474992
Renal injury	174.47	36.88	55	3573	15374	64479730
Anaphylactic shock	155.79	36.88	60	3568	30268	64464836
Multiple organ dysfunction syndrome	145.78	36.88	83	3545	101330	64393774
Anhedonia	139.05	36.88	45	3583	13661	64481443
Emotional distress	135.62	36.88	57	3571	35981	64459123
Injury	129.39	36.88	63	3565	55929	64439175
Unevaluable event	114.20	36.88	56	3572	50433	64444671
Renal failure	112.53	36.88	88	3540	181600	64313504
Cardiac arrest	81.24	36.88	68	3560	153996	64341108
Stress	69.67	36.88	43	3585	60491	64434613
Renal impairment	67.86	36.88	58	3570	134959	64360145
Hypotension	67.15	36.88	94	3534	380880	64114224
Anxiety	59.96	36.88	65	3563	202584	64292520
Hyperthermia malignant	55.46	36.88	15	3613	2444	64492660
Serotonin syndrome	50.57	36.88	30	3598	39252	64455852
Shock	46.10	36.88	28	3600	38212	64456892
Methaemoglobinaemia	42.93	36.88	14	3614	4334	64490770
Bradycardia	42.23	36.88	42	3586	118177	64376927
Thyrotoxic crisis	40.78	36.88	10	3618	1106	64493998

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N01AX07	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Other general anesthetics
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:38877	intravenous anesthetics
MeSH PA	D000777	Anesthetics
MeSH PA	D018686	Anesthetics, Intravenous
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D006993	Hypnotics and Sedatives
FDA EPC	N0000175681	General Anesthetic
FDA PE	N0000175975	General Anesthesia

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

Disease	Relation	SNOMED_ID	DOID
General anesthesia	indication	50697003
Low blood pressure	contraindication	45007003
Adrenal cortical hypofunction	contraindication	386584007	DOID:10493

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.22	Basic

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])	Bioact source	MoA source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE MODULATOR	EC50	5.46	WOMBAT-PK	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1	Ion channel	P14867	GBRA1_HUMAN		EC50	4.96	CHEMBL
Cytochrome P450 11B1, mitochondrial	Enzyme	P15538	C11B1_HUMAN		IC50	9.30	CHEMBL
Cytochrome P450 11B2, mitochondrial	Enzyme	P19099	C11B2_HUMAN		IC50	10	CHEMBL
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel	P18507 P47869 P47870	GBRG2_HUMAN GBRA2_HUMAN GBRB2_HUMAN		EC50	5.46	CHEMBL
Acetylcholine receptor subunit delta	Ion channel		ACHD_TORCA		IC50	4.30	CHEMBL

External reference:

ID	Source
4018743	VUID
N0000147047	NUI
D00548	KEGG_DRUG
4018743	VANDF
C0015131	UMLSCUI
CHEBI:4910	CHEBI
V8D	PDB_CHEM_ID
CHEMBL681	ChEMBL_ID
DB00292	DRUGBANK_ID
CHEMBL23731	ChEMBL_ID
D005045	MESH_DESCRIPTOR_UI
36339	PUBCHEM_CID
5463	IUPHAR_LIGAND_ID
1926	INN_ID
Z22628B598	UNII
215216	RXNORM
10178	MMSL
374	MMSL
4708	MMSL
d00931	MMSL
001402	NDDF
387218008	SNOMEDCT_US
40429005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9310	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9310	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9311	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9311	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9506	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9506	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9507	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9507	INJECTION	2 mg	INTRAVENOUS	ANDA	17 sections
Amidate	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9811	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	12 sections
Amidate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-6695	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	21 sections
Amidate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-6695	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	21 sections
Amidate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-8060	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	21 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-160	INJECTION	2 mg	INTRAVENOUS	ANDA	18 sections
etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	25021-674	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	21 sections
AMIDATE(TM) ETOMIDATE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1455	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	13 sections
AMIDATE(TM) ETOMIDATE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1459	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	13 sections
ETOMIDATE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1485	INJECTION	2 mg	INTRAVENOUS	ANDA	13 sections
ETOMIDATE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1542	INJECTION, SOLUTION	40 mg	INTRAVENOUS	ANDA	12 sections
Amidate	HUMAN PRESCRIPTION DRUG LABEL	1	52584-695	INJECTION, SOLUTION	2 mg	INTRAVENOUS	NDA	12 sections
ETOMIDATE	Human Prescription Drug Label	1	55150-221	INJECTION, SOLUTION	20 mg	INTRAVENOUS	ANDA	12 sections
ETOMIDATE	Human Prescription Drug Label	1	55150-222	INJECTION, SOLUTION	40 mg	INTRAVENOUS	ANDA	12 sections
Etomidate	Human Prescription Drug Label	1	65145-127	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	19 sections
Etomidate	Human Prescription Drug Label	1	65145-128	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	19 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	65219-445	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	20 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	65219-447	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	20 sections
etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	65841-818	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	1 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	67457-902	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	18 sections
Etomidate	HUMAN PRESCRIPTION DRUG LABEL	1	67457-903	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	18 sections
Etomidate	Human Prescription Drug Label	1	68083-234	SOLUTION	2 mg	INTRAVENOUS	ANDA	12 sections
Etomidate	Human Prescription Drug Label	1	68083-235	SOLUTION	2 mg	INTRAVENOUS	ANDA	12 sections