Overview
| Generic Names: | Bisoprolol Fumarate; Bisoprolol Hemifumarate; Bisoprolol fumerate |
|---|---|
| Trade Names: | Cardicor; Concor; Condyline; Condylox; Detensiel; Emconcor; Emcor; Euradal; Isoten; Monocor; Soloc; Soprol; Zebeta |
| Brand Mixtures: | Ziac (bisoprolol + hydrochlorothiazide) |
| PharmGKB Accession Id: | PA448641 |
Description
A cardioselective beta-1-adrenergic blocker. It is effective in the management of hypertension and angina pectoris. PubChem (source: Drug Bank)
Indication
For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure. (source: Drug Bank)
ATC Therapeutic Category
- C07AB:Beta blocking agents, selective
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Bisoprolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm. (source: Drug Bank)
Pharmacology
Bisoprolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Bisoprolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as Bisoprolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity. (source: Drug Bank)
Food Interactions
Take without regard to meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
Binding to serum proteins is approximately 30% (source: Drug Bank)
Absorption
80% (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub> = 100 mg/kg; Skin, rabbit: LD<sub>50</sub> = 200 mg/kg; Skin, rat: LD<sub>50</sub> = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat. (source: Drug Bank)
Isomeric SMILES Code:
CC(C)NCC(COc1ccc(cc1)COCCOC(C)C)O (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ADRB1 |
|
(source: Drug Bank) |
| ADRB2 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| chlorpropamide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| clonidine |
|
Increased hypertension when clonidine stopped (source: Drug Bank) |
| disopyramide |
|
The beta-blocker increases toxicity of disopyramide (source: Drug Bank) |
| epinephrine |
|
Hypertension, then bradycardia (source: Drug Bank) |
| ergonovine |
|
Ischemia with risk of gangrene (source: Drug Bank) |
| fenoterol |
|
Antagonism (source: Drug Bank) |
| formoterol |
|
Antagonism (source: Drug Bank) |
| glibenclamide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| gliclazide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| glipizide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| ibuprofen |
|
Risk of inhibition of renal prostaglandins (source: Drug Bank) |
| indomethacin |
|
Risk of inhibition of renal prostaglandins (source: Drug Bank) |
| insulin-glargine |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| isoproterenol |
|
Antagonism (source: Drug Bank) |
| lidocaine |
|
The beta-blocker increases the effect and toxicity of lidocaine (source: Drug Bank) |
| orciprenaline |
|
Antagonism (source: Drug Bank) |
| pirbuterol |
|
Antagonism (source: Drug Bank) |
| piroxicam |
|
Risk of inhibition of renal prostaglandins (source: Drug Bank) |
| prazosin |
|
Risk of hypotension at the beginning of therapy (source: Drug Bank) |
| repaglinide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| rifampin |
|
Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank) |
| salbutamol |
|
Antagonism (source: Drug Bank) |
| salmeterol |
|
Antagonism (source: Drug Bank) |
| terbutaline |
|
Antagonism (source: Drug Bank) |
| tolbutamide |
|
The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank) |
| verapamil |
|
Increased effect of both drugs (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.