Drug intelligence / Profile preview

bisoprolol

Development stage
Approved
Lead developer
Merck KGaA
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Bisoprolol is a highly selective β1-adrenergic receptor blocker (beta-blocker) used primarily for the treatment of hypertension, angina pectoris (coronary heart disease/angina), certain arrhythmias (such as rapid supraventricular arrhythmias and ventricular premature beats), and chronic stable heart failure with reduced ejection fraction. It has no intrinsic sympathomimetic activity or membrane-stabilizing effect. Bisoprolol exhibits a high affinity for β1 receptors—11 to 34 times greater than for β2 receptors—and its selectivity is about four times that of atenolol. The drug has a long duration of action (>24 hours), minimal respiratory side effects at therapeutic doses, and does not significantly affect lipid metabolism. It is well absorbed orally with high bioavailability (~90%), low first-pass effect (<10%), peak plasma concentration in 1.7–3 hours, and an elimination half-life of about 10 hours[2][5][6].

Brand names
博苏山益新
Other names
富马酸比索洛尔bisoprolol fumarate
02

Targets

ADRB1 (β1)

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