Bisoprolol

beta-Adrenergic Blocker — CARDIOVASCULAR SYSTEM

Key facts

Bisoprolol is an ofp drug in the beta-Adrenergic Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1992. Its mechanism of action is classified as Adrenergic beta-Antagonists. DrugCentral lists 4 molecular targets, including Adrb1, ADRB1 and ADRB2. Recorded indications include Atrial fibrillation and Hypertensive disorder.

• Approval status: ofp (first approved 1992 by the FDA).
• Drug class: beta-Adrenergic Blocker.
• Mechanism of action: Adrenergic beta-Antagonists.
• Molecular targets: Adrb1, ADRB1, ADRB2 and ADRB3 (4 listed in DrugCentral).
• Indications: Atrial fibrillation and Hypertensive disorder.
• ATC code: C07AB07 (Beta blocking agents, selective).
• Molecular formula: C18H31NO4; molecular weight 325.45 g/mol.

Indications & contraindications

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

Indications (2)

• Atrial fibrillation
• Hypertensive disorder

Off-label uses (4)

• Angina pectoris
• Chronic heart failure
• Diastolic heart failure
• Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation

Contraindications (41)

• Acute exacerbation of asthma
• Acute pancreatitis
• Anaphylaxis
• Anuria
• Asthma
• Azotemia
• Cardiogenic shock
• Complete atrioventricular block
• Decompensated cardiac failure
• Dehydration
• Depressive disorder
• Diabetes mellitus
• Disease of liver
• Gout
• Hepatic coma
• Hypercalcemia
• Hypercholesterolemia
• Hyperparathyroidism
• Hyperuricemia
• Hypochloremic alkalosis
• Hypokalemia
• Hypomagnesemia
• Hyponatremia
• Hypovolemia
• Kidney disease
• Myasthenia gravis
• Neonatal hyperbilirubinemia
• Partial atrioventricular block
• Peripheral arterial occlusive disease
• Peripheral vascular disease
• + 11 more

Mechanism & targets

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

Molecular targets (4)

Target	Gene	Action	Activity
Beta-1 adrenergic receptor	Adrb1	unknown	Ki 8.28
Beta-1 adrenergic receptor	ADRB1	antagonist	Ki 7.65
Beta-2 adrenergic receptor	ADRB2	unknown	Ki 5.94
Beta-3 adrenergic receptor	ADRB3	unknown	Ki 5.04

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2013-06-28	PMDA	—	TOA EIYO LTD.
1992-07-31	FDA	—	TEVA WOMENS

ATC classification

ATC code	Therapeutic hierarchy
C07AB07	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS › Beta blocking agents, selective
C07BB07	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS AND THIAZIDES › Beta blocking agents, selective, and thiazides
C07FB07	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS, OTHER COMBINATIONS › Beta blocking agents and calcium channel blockers
C07FX04	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS, OTHER COMBINATIONS › Beta blocking agents, other combinations
C09BX02	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ACE INHIBITORS, COMBINATIONS › ACE inhibitors, other combinations
C09BX04	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ACE INHIBITORS, COMBINATIONS › ACE inhibitors, other combinations
C09BX05	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ACE INHIBITORS, COMBINATIONS › ACE inhibitors, other combinations
C09BX06	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ACE INHIBITORS, COMBINATIONS › ACE inhibitors, other combinations

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
Acute kidney injury	4257.3
Bradycardia	3017.8
Cardiac failure	2342.0
Drug interaction	2101.0
Hyperkalaemia	1879.2
Atrial fibrillation	1568.5
Hypotension	1424.5
Drug ineffective	1263.6
Syncope	1126.1
Glossodynia	1069.1
Pemphigus	1059.2
Hand deformity	1058.3

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Bisoprolol is on its molecule page.

• Molecular formula: C₁₈H₃₁NO₄
• Molecular weight: 325.45 g/mol
• CAS number: 66722-44-9
• InChIKey: VHYCDWMUTMEGQY-UHFFFAOYSA-N
• PubChem CID: 2405

CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1

Frequently asked questions

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

What is Bisoprolol used for?

DrugCentral lists the following indications for Bisoprolol: Atrial fibrillation and Hypertensive disorder.

How does Bisoprolol work?

Bisoprolol is classified as Adrenergic beta-Antagonists; its molecular targets in DrugCentral include Adrb1, ADRB1 (antagonist), ADRB2 and ADRB3.

When was Bisoprolol first approved?

Bisoprolol was first approved by the FDA in 1992.

What drug class does Bisoprolol belong to?

Bisoprolol is in the beta-Adrenergic Blocker class.

What is the chemical formula of Bisoprolol?

Bisoprolol has the molecular formula C18H31NO4 and a molecular weight of 325.45 g/mol.

Sources

• DrugCentral drug card 380 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1472989 — compound record and bioactivity
• PubChem CID 2405 — chemical identifiers
• DrugBank DB00612 — drug record
• FDA UNII Y41JS2NL6U — substance identity
• DailyMed: FDA labels for Bisoprolol — current prescribing information (label search)
• UniProt P08588 (ADRB1) — target protein
• UniProt P07550 (ADRB2) — target protein
• UniProt P13945 (ADRB3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.