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etomidate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1109 | 33125-97-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.
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 |
| BA (Bioavailability) | 0 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.841 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.334 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 77.804 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 62.087 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 17.410 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 28.100 | % | High | 1 |
| herg | hERG pIC50 | 4.458 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 178.238 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 233.346 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 19.750 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAP3K7,MAPK7,MAPK9,MARK4,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 33 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.290 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 358.922 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 17.650 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.420 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 29.040 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 260.615 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.470 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 16.470 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 277.332 | uM | High | 1 |
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 | 133.26 | 45.05 | 59 | 2008 | 104876 | 90521504 |
| Anaphylactic shock | 129.85 | 45.05 | 42 | 2025 | 31575 | 90594805 |
| Bradycardia | 86.96 | 45.05 | 41 | 2026 | 83806 | 90542574 |
| Hypotension | 84.29 | 45.05 | 65 | 2002 | 325332 | 90301048 |
| Fear | 76.07 | 45.05 | 24 | 2043 | 16598 | 90609782 |
| Renal injury | 73.81 | 45.05 | 21 | 2046 | 10222 | 90616158 |
| Ventricular fibrillation | 71.48 | 45.05 | 22 | 2045 | 14022 | 90612358 |
| Anaesthetic complication neurological | 66.84 | 45.05 | 12 | 2055 | 729 | 90625651 |
| Renal failure | 61.92 | 45.05 | 38 | 2029 | 130969 | 90495411 |
| Phaeochromocytoma crisis | 60.73 | 45.05 | 10 | 2057 | 363 | 90626017 |
| Multiple organ dysfunction syndrome | 54.61 | 45.05 | 28 | 2039 | 68308 | 90558072 |
| Emotional distress | 54.19 | 45.05 | 23 | 2044 | 36639 | 90589741 |
| Anhedonia | 50.19 | 45.05 | 16 | 2051 | 11415 | 90614965 |
| Drug abuse | 49.70 | 45.05 | 28 | 2039 | 82319 | 90544061 |
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 | 118.72 | 35.63 | 39 | 2685 | 10926 | 42607685 |
| Anaphylactic shock | 109.82 | 35.63 | 45 | 2679 | 23472 | 42595139 |
| Injury | 108.64 | 35.63 | 44 | 2680 | 22272 | 42596339 |
| Anaesthetic complication neurological | 107.26 | 35.63 | 21 | 2703 | 715 | 42617896 |
| Renal injury | 102.74 | 35.63 | 36 | 2688 | 12244 | 42606367 |
| Multiple organ dysfunction syndrome | 101.75 | 35.63 | 68 | 2656 | 96967 | 42521644 |
| Emotional distress | 100.44 | 35.63 | 38 | 2686 | 16055 | 42602556 |
| Anhedonia | 94.19 | 35.63 | 30 | 2694 | 7610 | 42611001 |
| Hyperthermia malignant | 80.41 | 35.63 | 21 | 2703 | 2637 | 42615974 |
| Unevaluable event | 75.72 | 35.63 | 39 | 2685 | 34249 | 42584362 |
| Serotonin syndrome | 64.67 | 35.63 | 32 | 2692 | 25813 | 42592798 |
| Renal failure | 64.17 | 35.63 | 61 | 2663 | 143665 | 42474946 |
| Thyrotoxic crisis | 64.08 | 35.63 | 14 | 2710 | 820 | 42617791 |
| Rhabdomyolysis | 59.28 | 35.63 | 45 | 2679 | 77974 | 42540637 |
| Diabetes insipidus | 55.91 | 35.63 | 17 | 2707 | 3696 | 42614915 |
| Cardiac arrest | 55.73 | 35.63 | 50 | 2674 | 109270 | 42509341 |
| Stress | 46.23 | 35.63 | 31 | 2693 | 44181 | 42574430 |
| Anxiety | 44.81 | 35.63 | 46 | 2678 | 118514 | 42500097 |
| Coma | 43.10 | 35.63 | 32 | 2692 | 53522 | 42565089 |
| Pseudomonal sepsis | 41.50 | 35.63 | 14 | 2710 | 4235 | 42614376 |
| Hypotension | 41.16 | 35.63 | 65 | 2659 | 257566 | 42361045 |
| Methaemoglobinaemia | 40.98 | 35.63 | 15 | 2709 | 5759 | 42612852 |
| Burkholderia test positive | 40.13 | 35.63 | 10 | 2714 | 1040 | 42617571 |
| Shock | 39.32 | 35.63 | 24 | 2700 | 29097 | 42589514 |
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 |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 238.30 | 34.65 | 88 | 4704 | 51458 | 110533049 |
| Fear | 178.56 | 34.65 | 58 | 4734 | 23135 | 110561372 |
| Renal injury | 173.83 | 34.65 | 54 | 4738 | 18659 | 110565848 |
| Cardiac arrest | 165.62 | 34.65 | 104 | 4688 | 196649 | 110387858 |
| Multiple organ dysfunction syndrome | 160.76 | 34.65 | 93 | 4699 | 151617 | 110432890 |
| Anhedonia | 141.09 | 34.65 | 44 | 4748 | 15384 | 110569123 |
| Emotional distress | 137.85 | 34.65 | 57 | 4735 | 44790 | 110539717 |
| Renal failure | 122.14 | 34.65 | 91 | 4701 | 226483 | 110358024 |
| Unevaluable event | 116.42 | 34.65 | 55 | 4737 | 59172 | 110525335 |
| Hypotension | 112.05 | 34.65 | 125 | 4667 | 523724 | 110060783 |
| Hyperthermia malignant | 110.24 | 34.65 | 27 | 4765 | 3873 | 110580634 |
| Phaeochromocytoma crisis | 82.73 | 34.65 | 15 | 4777 | 499 | 110584008 |
| Injury | 77.58 | 34.65 | 63 | 4729 | 177202 | 110407305 |
| Shock | 76.33 | 34.65 | 40 | 4752 | 53548 | 110530959 |
| Diabetes insipidus | 69.65 | 34.65 | 21 | 4771 | 6549 | 110577958 |
| Renal impairment | 66.12 | 34.65 | 59 | 4733 | 188386 | 110396121 |
| Rhabdomyolysis | 61.72 | 34.65 | 47 | 4745 | 120354 | 110464153 |
| Stress | 60.42 | 34.65 | 44 | 4748 | 105304 | 110479203 |
| Ventricular fibrillation | 59.28 | 34.65 | 31 | 4761 | 41282 | 110543225 |
| Thyrotoxic crisis | 57.02 | 34.65 | 14 | 4778 | 2026 | 110582481 |
| Bradycardia | 53.16 | 34.65 | 48 | 4744 | 155469 | 110429038 |
| Anxiety | 51.78 | 34.65 | 69 | 4723 | 345009 | 110239498 |
| Serotonin syndrome | 51.44 | 34.65 | 32 | 4760 | 59121 | 110525386 |
| Coma | 43.48 | 34.65 | 38 | 4754 | 117831 | 110466676 |
| Pulseless electrical activity | 40.55 | 34.65 | 18 | 4774 | 16739 | 110567768 |
| Respiratory failure | 40.11 | 34.65 | 48 | 4744 | 215284 | 110369223 |
| Methaemoglobinaemia | 39.89 | 34.65 | 15 | 4777 | 9153 | 110575354 |
| Generalised tonic-clonic seizure | 38.71 | 34.65 | 26 | 4766 | 54654 | 110529853 |
| Fibrinolysis increased | 35.96 | 34.65 | 5 | 4787 | 27 | 110584480 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01AX07 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Other general anesthetics |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D006993 | Hypnotics and Sedatives |
| MeSH PA | D018686 | Anesthetics, Intravenous |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:35717 | sedative |
| CHEBI has role | CHEBI:38877 | intravenous anaesthetic |
| FDA EPC | N0000175681 | General Anesthetic |
| FDA PE | N0000175975 | General Anesthesia |
Related Drugs by ATC class:
N01AX Other general anesthetics 8 drugs
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]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE MODULATOR | EC50 | 5.46 | WOMBAT-PK | CHEMBL | |||
| Gamma-aminobutyric acid receptor subunit alpha-1 | Ion channel | EC50 | 4.96 | CHEMBL | |||||
| Cytochrome P450 11B1, mitochondrial | Enzyme | IC50 | 9.30 | CHEMBL | |||||
| Cytochrome P450 11B2, mitochondrial | Enzyme | IC50 | 10 | CHEMBL | |||||
| GABA A receptor alpha-2/beta-2/gamma-2 | Ion channel | EC50 | 5.46 | CHEMBL | |||||
| Acetylcholine receptor subunit delta | Ion channel | 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 | 0143-9311 | 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 | 0143-9507 | 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(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 |
| ETOMIDATE injection, solution | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1634 | 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 | 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 |
| Etomidate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65219-447 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 20 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 |
| Etomidate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72266-146 | SOLUTION | 2 mg | INTRAVENOUS | ANDA | 12 sections |
| Etomidate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72266-147 | SOLUTION | 2 mg | INTRAVENOUS | ANDA | 12 sections |
| Etomidate | Human Prescription Drug Label | 1 | 72485-508 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 19 sections |
| Etomidate | Human Prescription Drug Label | 1 | 72485-509 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 19 sections |
| Etomidate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72572-160 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 17 sections |
| Etomidate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72572-161 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 17 sections |