Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Smart Pharmaceuticals (Pty) Ltd, 247 Voortrekker Road, Kraaifontein, Cape Town, 7570
Pharmacological classification: A 5.2 Adrenolytics (sympathicolytics)
Pharmacotherapeutic group: Beta blocking medicines, selective
ATC Code: C07AB07
Bisoprolol is a highly β1-selective beta-adrenoceptor antagonist, with low β2-receptor affinity.
It has neither intrinsic sympathomimetic activity nor membrane-stabilising properties.
It reduces blood pressure, and by blockade of the cardiac β1-receptors, it reduces cardiac action, and hence myocardial oxygen demand.
The mechanism of action of β1-adrenergic blocking medicines in hypertension is not clear, but it is known that bisoprolol reduces the heart rate and depresses plasma renin levels.
Bisoprolol is rapidly absorbed after oral administration in man and displays a high bioavailability of 90% after an oral dose.
The distribution volume is 3,5 L/kg. The plasma protein binding of bisoprolol is about 30%.
In man 50% of a dose is metabolised in the liver while the other 50% is eliminated unchanged via the kidneys. None of the metabolites found in man has ß1-receptor blocking action.
In man, the plasma elimination half-life is 10-12 hours resulting in duration of action of 24 hours. Because of its moderate hepatic metabolism, it is subject only to a very small hepatic first pass metabolism.
Not applicable.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.