Source: Health Products Regulatory Authority (ZA) Revision Year: 2024 Publisher: Aurogen South Africa (Pty) Ltd, Woodhill Office Park, Building 1, First floor, 53 Phillip Engelbrecht Avenue, Meyersdal, Ext. 12, 1448, Johannesburg, South Africa
Pharmacological classification: A 5.2 Adrenolytics (sympathicolytics)
Pharmacotherapeutic group: Beta blocking agents, selective
ATC Code: C07AB07
Bisoprolol is a selective β1-adrenoceptor antagonist with low β2 receptor affinity. It is devoid of intrinsic sympathomimetic and membrane-stabilising activity.
It reduces blood pressure, and by blockade of the cardiac β1-receptors, it reduces cardiac action, and hence myocardial oxygen demand
Bisoprolol is well absorbed following oral administration with a resultant bioavailability of about 90%, Tmax is at 3 hours.
The plasma protein binding of bisoprolol is about 30%. The distribution volume is 3.5 l/kg. The total clearance is approximately 15 l/h. The kinetics of bisoprolol are linear.
The plasma elimination half-life is approximately 10 to 12 hours in healthy volunteers and the duration of action is about 24 hours.
About 50% of a dose is metabolised in the liver and the remainder is excreted unchanged via the kidneys. Since the elimination takes place in the kidneys and the liver to the same extent a dosage adjustment is not required for patients with impaired liver function or renal insufficiency
In patients with chronic heart failure, patients with renal impairment and in patients with liver cirrhosis, the plasma levels of bisoprolol are about one third higher and the half-life is prolonged. In the elderly with hypertension, the elimination is delayed, and plasma levels are higher.
Not applicable.
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