esmolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 1054 | 81147-92-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 20 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.68 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 1.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 290 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.59 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.15 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 31, 1986 | FDA | BAXTER HLTHCARE |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Drug ineffective | 54.01 | 41.41 | 55 | 694 | 363115 | 29210663 |
| Bradycardia | 50.37 | 41.41 | 27 | 722 | 65602 | 29508176 |
| Cardiac arrest | 48.87 | 41.41 | 29 | 720 | 85562 | 29488216 |
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 |
|---|---|---|---|---|---|---|
| Drug ineffective | 88.47 | 41.95 | 93 | 1146 | 840154 | 63657339 |
| Cardiac arrest | 75.69 | 41.95 | 43 | 1196 | 154021 | 64343472 |
| Neuromuscular block prolonged | 52.84 | 41.95 | 10 | 1229 | 967 | 64496526 |
| Bradycardia | 52.64 | 41.95 | 31 | 1208 | 118188 | 64379305 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AB09 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| CHEBI has role | CHEBI:35530 | beta-adrenergic blockers |
| CHEBI has role | CHEBI:38070 | antiarrhythmic agent |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D058671 | Adrenergic beta-1 Receptor Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Supraventricular tachycardia | indication | 6456007 | |
| Atrial fibrillation | indication | 49436004 | DOID:0060224 |
| Perioperative hypertension | indication | 434711000124103 | |
| Perioperative Tachycardia | indication | ||
| Malignant essential hypertension | off-label use | 78975002 | DOID:10823 |
| Dissection of aorta | off-label use | 308546005 | |
| Acute coronary syndrome | off-label use | 394659003 | |
| Hypertensive urgency | off-label use | 443482000 | |
| Prevention of Hypertension in Pheochromocytoma | off-label use | ||
| Bronchospasm | contraindication | 4386001 | |
| Anaphylaxis | contraindication | 39579001 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Cardiogenic shock | contraindication | 89138009 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Heart block | contraindication | 233916004 | |
| Acute exacerbation of asthma | contraindication | 708038006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.19 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Ki | 6.90 | IUPHAR | IUPHAR | |||
| Beta-2 adrenergic receptor | GPCR | Kd | 5.20 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | Kd | 7 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019746 | VUID |
| N0000147837 | NUI |
| D00644 | KEGG_DRUG |
| 81161-17-3 | SECONDARY_CAS_RN |
| 4019349 | VANDF |
| 4019746 | VANDF |
| C0116569 | UMLSCUI |
| CHEBI:4856 | CHEBI |
| CHEMBL768 | ChEMBL_ID |
| CHEMBL1201115 | ChEMBL_ID |
| DB00187 | DRUGBANK_ID |
| C036604 | MESH_SUPPLEMENTAL_RECORD_UI |
| 59768 | PUBCHEM_CID |
| 7178 | IUPHAR_LIGAND_ID |
| 5365 | INN_ID |
| MDY902UXSR | UNII |
| 151448 | RXNORM |
| 3762 | MMSL |
| 4681 | MMSL |
| 47065 | MMSL |
| d00224 | MMSL |
| 001861 | NDDF |
| 004745 | NDDF |
| 35318005 | SNOMEDCT_US |
| 372847006 | SNOMEDCT_US |
| 77856005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9825 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9825 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9858 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 17 sections |
| Esmolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-2965 | INJECTION | 10 mg | INTRAVENOUS | NDA | 17 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-055 | INJECTION | 10 mg | INTRAVENOUS | NDA | 24 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-055 | INJECTION | 10 mg | INTRAVENOUS | NDA | 24 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-075 | INJECTION | 20 mg | INTRAVENOUS | NDA | 24 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-075 | INJECTION | 20 mg | INTRAVENOUS | NDA | 24 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-115 | INJECTION | 10 mg | INTRAVENOUS | NDA | 24 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-115 | INJECTION | 10 mg | INTRAVENOUS | NDA | 24 sections |
| Esmolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-120 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| BREVIBLOC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-666 | INJECTION | 20 mg | INTRAVENOUS | NDA | 25 sections |
| BREVIBLOC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-668 | INJECTION | 20 mg | INTRAVENOUS | NDA | 25 sections |
| BREVIBLOC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-670 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| BREVIBLOC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10019-672 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| esmolol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-308 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 26 sections |
| esmolol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-309 | INJECTION, SOLUTION | 20 mg | INTRAVENOUS | ANDA | 26 sections |
| esmolol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-314 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 26 sections |
| Esmolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44567-811 | INJECTION | 10 mg | INTRAVENOUS | NDA | 22 sections |
| Esmolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44567-812 | INJECTION | 20 mg | INTRAVENOUS | NDA | 22 sections |
| Esmolol Hydrochloride | Human Prescription Drug Label | 1 | 50090-4512 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 25 sections |
| Esmolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4699 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 25 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1322 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 18 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1371 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 18 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1427 | INJECTION | 10 mg | INTRAVENOUS | NDA | 18 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1444 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 18 sections |
| Esmolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-017 | INJECTION | 10 mg | INTRAVENOUS | NDA | 11 sections |
| Brevibloc | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-115 | INJECTION | 10 mg | INTRAVENOUS | NDA | 25 sections |
| ESMOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-194 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 17 sections |
| Esmolol Hydrochloride | Human Prescription Drug Label | 1 | 55150-194 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 25 sections |