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	109.48	46.25	52	1648	92493	63394829
Anaphylactic shock	86.65	46.25	30	1670	23603	63463719
Bradycardia	79.99	46.25	39	1661	73188	63414134
Fear	77.63	46.25	25	1675	15741	63471581
Renal injury	76.65	46.25	22	1678	9417	63477905
Hypotension	72.39	46.25	59	1641	272545	63214777
Renal failure	60.13	46.25	38	1662	117614	63369708
Emotional distress	56.60	46.25	24	1676	32525	63454797
Anhedonia	52.36	46.25	17	1683	10957	63476365
Multiple organ dysfunction syndrome	49.53	46.25	26	1674	56726	63430596

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	121.28	38.42	39	2152	10437	34944303
Multiple organ dysfunction syndrome	110.03	38.42	65	2126	76501	34878239
Injury	109.26	38.42	43	2148	20644	34934096
Renal injury	106.75	38.42	36	2155	11159	34943581
Emotional distress	100.06	38.42	37	2154	14989	34939751
Anhedonia	95.02	38.42	30	2161	7555	34947185
Anaphylactic shock	90.73	38.42	35	2156	15906	34938834
Unevaluable event	78.38	38.42	39	2152	32551	34922189
Serotonin syndrome	66.80	38.42	30	2161	19903	34934837
Renal failure	66.33	38.42	59	2132	130498	34824242
Hyperthermia malignant	65.23	38.42	17	2174	2160	34952580
Stress	52.08	38.42	29	2162	30318	34924422
Thyrotoxic crisis	49.57	38.42	10	2181	405	34954335
Anxiety	46.60	38.42	43	2148	99385	34855355
Pseudomonal sepsis	44.26	38.42	14	2177	3533	34951207
Methaemoglobinaemia	44.13	38.42	14	2177	3567	34951173
Burkholderia test positive	40.58	38.42	10	2181	1013	34953727

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	179.09	38.10	59	3822	21927	79718580
Renal injury	177.27	38.10	55	3826	16872	79723635
Anaphylactic shock	168.54	38.10	64	3817	35932	79704575
Multiple organ dysfunction syndrome	157.26	38.10	88	3793	120158	79620349
Anhedonia	141.75	38.10	45	3836	14853	79725654
Emotional distress	137.87	38.10	57	3824	39912	79700595
Injury	118.61	38.10	63	3818	77433	79663074
Renal failure	118.13	38.10	89	3792	200879	79539628
Unevaluable event	116.76	38.10	56	3825	55529	79684978
Cardiac arrest	98.37	38.10	75	3806	172021	79568486
Hypotension	81.00	38.10	103	3778	440214	79300293
Hyperthermia malignant	74.22	38.10	19	3862	2898	79737609
Renal impairment	67.28	38.10	58	3823	157725	79582782
Stress	64.56	38.10	43	3838	79569	79660938
Shock	57.10	38.10	32	3849	43516	79696991
Anxiety	56.76	38.10	65	3816	248447	79492060
Serotonin syndrome	50.79	38.10	30	3851	44997	79695510
Bradycardia	46.27	38.10	44	3837	135513	79604994
Methaemoglobinaemia	41.55	38.10	14	3867	5543	79734964
Thyrotoxic crisis	40.83	38.10	10	3871	1274	79739233

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
667484	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	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	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
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	55150-221	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	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	65219-445	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	20 sections