QuickView for Bisoprolol (compound)

Summary
General Info

PubChem

PubChem Compound 10892731

Name:	Bisoprolol
PubChem Compound ID:	10892731
Description:	A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.
Molecular formula:	C₁₈H₃₁NO₄
Molecular weight:	325.443 g/mol

DrugBank

Identification

Name:	Bisoprolol
Name (isomeric):	DB00612
Drug Type:	small molecule
Description:	A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.
Synonyms:	Bisoprolol fumerate; Bisoprolol Fumarate; Bisoprolol Hemifumarate
Brand:	Isoten, Condyline, Euradal, Concor, Emcor, Detensiel, Emconcor, Cardicor, Soloc, Condylox, Soprol, Monocor, Zebeta
Brand name mixture:	Ziac(bisoprolol + hydrochlorothiazide)
Category:	Sympatholytics, Adrenergic Agents, Adrenergic beta-Antagonists, Antihypertensive Agents
CAS number:	66722-44-9

Pharmacology

Indication:	For management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI).
Pharmacology:	Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to... show more » Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. They are routinely prescribed in patients with ischemic heart disease. In addition, β1-selective blockers prevent the release of renin, a hormone produced by the kidneys causes constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane-stabilizing activity. show less «
Mechanism of Action:	Bisoprolol selectively blocks catecholamine stimulation of β1-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. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block &b... show more » Bisoprolol selectively blocks catecholamine stimulation of β1-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. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block β2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation. show less «
Absorption:	Well absorbed. Bioavailability > 80%. Absorption is not affected by food. Peak plasma concentrations occur within 2-4 hours.
Protein binding:	Binding to serum proteins is approximately 30%
Biotransformation:	Approximately 50% of the dose is metabolized primarily metabolized by CYP3A4 to inactive metabolites. In vitro studies have shown that bisoprolol is also metabolized by CYP2D6 though this does not appear to be clinically significant. Approximately half the administered dose is excreted in unchanged in urine.
Route of elimination:	Eliminated equally by renal and non-renal pathways. Approximately 50% of the total orally administered dose is excreted unchanged in urine with the remainder appearing as inactive metabolites. Less than 2% of the dose is excreted in the feces.
Half Life:	9-12 hours; prolonged in the elderly and those with decreased renal function
Toxicity:	Oral, mouse: LD₅₀ = 100 mg/kg; Skin, rabbit: LD₅₀ = 200 mg/kg; Skin, rat: LD₅₀ = 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.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take without regard to meals.

Drug interaction:

Tolazamide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Procaterol	Antagonism

Tolazamide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Procaterol	Antagonism
Epinephrine	Hypertension, then bradycardia
Glyburide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Clonidine	Increased hypertension when clonidine stopped
Insulin Aspart	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Insulin Glulisine	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Glycodiazine	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Insulin Lispro	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Insulin Glargine	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Salmeterol	Antagonism
Repaglinide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Glisoxepide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Terbutaline	Antagonism
Disopyramide	The beta-blocker, bisoprolol, may increase the toxicity of disopyramide.
Methysergide	Ischemia with risk of gangrene
Lidocaine	The beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tolbutamide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Salbutamol	Antagonism
Fenoterol	Antagonism
Pipobroman	Antagonism
Voriconazole	Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of bisoprolol by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bisoprolol if voriconazole is initiated, discontinued or dose changed.
Orciprenaline	Antagonism
Formoterol	Antagonism
Dihydroergotamine	Ischemia with risk of gangrene
Dihydroergotoxine	Ischemia with risk of gangrene
Insulin Detemir	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Isoproterenol	Antagonism
Glipizide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Verapamil	Increased effect of both drugs
Pirbuterol	Antagonism
Telithromycin	Telithromycin may reduce clearance of Bisoprolol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bisoprolol if Telithromycin is initiated, discontinued or dose changed.
Gliclazide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Prazosin	Risk of hypotension at the beginning of therapy
Chlorpropamide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Rifampin	Rifampin may decrease the serum concentration of bisprolol by increasing its metabolism.
Acetohexamide	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Piroxicam	Risk of inhibition of renal prostaglandins
Indomethacin	Risk of inhibition of renal prostaglandins
Insulin	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.

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Targets

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

Enzymes

Cytochrome P450 3A4

Cytochrome P450 2D6