Bisoprolol fumarate: Indications, Mechanism of Action and Side Effects

What is Bisoprolol fumarate?

Bisoprolol fumarate is the active ingredient in the prescription drug Bisoprolol, which belongs to the class of drugs known as beta-blockers. There is no difference between Bisoprolol and Bisoprolol fumarate, and they usually indicate the same medication, which is used to treat high blood pressure and congestive heart failure. Bisoprolol fumarate is a white crystalline powder, soluble in water, methanol, ethanol and chloroform. It is usually taken together with other medications using to help prevent heart failure and high blood pressure.

Hydrochlorothiazide, bisoprolol fumarate, is a synthetic antihypertensive phenoxy-2-propanol derivative compounded with thiazides, diuretics used in the treatment of hypertension, and is a selective beta-1 (cardiac) adrenergic antagonist with no membrane-stabilising or intrinsic sympathomimetic activity. Hydrochlorothiazide affects renal tubular electrolyte reabsorption and increases sodium and chloride excretion.

Indications

Bisoprolol fumarate is indicated for the treatment of chronic heart failure (CHF), hypertension and its related complications, and heart disease due to impaired coronary artery perfusion (ischaemic heart disease, angina). Studies have shown that bisoprolol fumarate, when used in smaller doses, is as effective as carvedilol in treating Japanese patients with mild to moderate atrial fibrillation and is well tolerated. In addition, bisoprolol fumarate and hydrochlorothiazide are also approved for the treatment of hypertension.

Mechanism of Action

Bisoprolol fumarate is a β1-adrenergic antagonist. It reduces contractility and oxygen demand by competitively inhibiting β1-adrenergic receptors, thereby reducing cardiac load, resulting in reduced cardiac output and lower blood pressure and heart rate.

Side Effects

Common side effects of Bisoprolol fumarate include constipation, cold hands and feet, dizziness, weakness, headache, low blood pressure, feeling unwell (nausea or vomiting) and diarrhoea. Rarer side effects may occur: hearing problems, dry eyes, decreased sexual performance, changes in blood test results, fainting, runny nose, hair loss and psoriasis-like rash. Please use with caution if you are allergic to this medication.

References:

[1] Bisoprolol Fumarate/Hydrochlorothiazide[J]. Definitions, 2020. DOI:10.32388/7bxh5x.

[2] MASATSUGU HORI. Efficacy and safety of bisoprolol fumarate compared with carvedilol in Japanese patients with chronic heart failure: results of the randomized, controlled, double-blind, Multistep Administration of bisoprolol IN Chronic Heart Failure II (MAIN-CHF II) study.[J]. Heart and Vessels, 2014. DOI:10.1007/s00380-013-0340-3.

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