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QuickView for Bisoprolol (compound)


PubChem
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...
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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...
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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:
TolazamideThe beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
IbuprofenRisk of inhibition of renal prostaglandins
ErgonovineIschemia with risk of gangrene
ErgotamineIschemia with risk of gangrene
ProcaterolAntagonism
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Targets


Enzymes