Esmolol

beta-Adrenergic Blocker — CARDIOVASCULAR SYSTEM

Key facts

Esmolol is an ofp drug in the beta-Adrenergic Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1986. Its mechanism of action is classified as Adrenergic beta-Antagonists. DrugCentral lists 3 molecular targets, including ADRB1, ADRB1 and Adrb2. Recorded indications include Atrial fibrillation, Perioperative hypertension, Perioperative Tachycardia and Supraventricular tachycardia.

• Approval status: ofp (first approved 1986 by the FDA).
• Drug class: beta-Adrenergic Blocker.
• Mechanism of action: Adrenergic beta-Antagonists.
• Molecular targets: ADRB1, ADRB1 and Adrb2 (3 listed in DrugCentral).
• Indications: Atrial fibrillation, Perioperative hypertension, Perioperative Tachycardia and Supraventricular tachycardia.
• ATC code: C07AB09 (Beta blocking agents, selective).
• Molecular formula: C16H25NO4; molecular weight 295.38 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (4)

• Atrial fibrillation
• Perioperative hypertension
• Perioperative Tachycardia
• Supraventricular tachycardia

Off-label uses (5)

• Acute coronary syndrome
• Dissection of aorta
• Hypertensive urgency
• Malignant essential hypertension
• Prevention of Hypertension in Pheochromocytoma

Contraindications (10)

• Acute exacerbation of asthma
• Anaphylaxis
• Bronchospasm
• Cardiogenic shock
• Decompensated cardiac failure
• Diabetes mellitus
• Heart block
• Kidney disease
• Pulmonary emphysema
• Sinus bradycardia

Mechanism & targets

• Mechanism of action (MoA): Adrenergic beta-Antagonists
• Established pharmacologic class: beta-Adrenergic Blocker

Molecular targets (3)

Target	Gene	Action	Activity
Beta-1 adrenergic receptor	ADRB1	unknown	Kd 7.00
Beta-1 adrenergic receptor	ADRB1	antagonist	Ki 6.90
Beta-2 adrenergic receptor	Adrb2	unknown	Kd 5.20

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1986-12-31	FDA	—	BAXTER HLTHCARE

ATC classification

ATC code	Therapeutic hierarchy
C07AB09	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS › Beta blocking agents, selective

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug ineffective	332.4
Cardiac arrest	127.2
Bradycardia	117.3
Hypotension	91.8
Pulseless electrical activity	62.0
Drug ineffective for unapproved indication	57.5
Anaesthetic complication neurological	55.6
Haemodynamic instability	51.4
Neuromuscular block prolonged	49.7
Apallic syndrome	49.5
Circulatory collapse	45.2
Ventricular fibrillation	43.6

Chemical structure

• Molecular formula: C₁₆H₂₅NO₄
• Molecular weight: 295.38 g/mol
• CAS number: 81147-92-4
• InChIKey: AQNDDEOPVVGCPG-UHFFFAOYSA-N
• PubChem CID: 59768

COC(=O)CCC1=CC=C(OCC(O)CNC(C)C)C=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Esmolol used for?

DrugCentral lists the following indications for Esmolol: Atrial fibrillation, Perioperative hypertension, Perioperative Tachycardia and Supraventricular tachycardia.

How does Esmolol work?

Esmolol is classified as Adrenergic beta-Antagonists; its molecular targets in DrugCentral include ADRB1, ADRB1 (antagonist) and Adrb2.

When was Esmolol first approved?

Esmolol was first approved by the FDA in 1986.

What drug class does Esmolol belong to?

Esmolol is in the beta-Adrenergic Blocker class.

What is the chemical formula of Esmolol?

Esmolol has the molecular formula C16H25NO4 and a molecular weight of 295.38 g/mol.

Sources

• DrugCentral drug card 1054 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201115 — compound record and bioactivity
• PubChem CID 59768 — chemical identifiers
• DrugBank DB00187 — drug record
• FDA UNII MDY902UXSR — substance identity
• DailyMed: FDA labels for Esmolol — current prescribing information (label search)
• UniProt P08588 (ADRB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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