Bisoprolol: Uses, Dosage & Side Effects

What Is Bisoprolol and What Is It Used For?

Bisoprolol belongs to a class of medications called beta-adrenergic blocking agents, commonly known as beta blockers. Specifically, bisoprolol is a highly selective beta-1 receptor blocker, which means it primarily affects the heart while having minimal impact on the beta-2 receptors found in the lungs and blood vessels. This selectivity makes it particularly suitable for patients who may have mild respiratory conditions, although caution is still necessary in asthma.

The medication works by blocking the action of certain natural chemicals in the body, such as adrenaline (epinephrine), on the heart. This results in a slower heart rate, reduced force of cardiac contractions, and lower cardiac output. In the context of heart failure, bisoprolol counteracts the harmful chronic activation of the sympathetic nervous system, which over time leads to improved heart function and reduced mortality.

Primary Indications

Bisoprolol is approved for the treatment of stable chronic heart failure with reduced systolic function, used in combination with standard heart failure therapy including ACE inhibitors (or angiotensin receptor blockers), diuretics, and optionally cardiac glycosides such as digoxin. The landmark CIBIS-II (Cardiac Insufficiency Bisoprolol Study II) trial, published in The Lancet, demonstrated that bisoprolol reduced all-cause mortality by 34% and sudden death by 44% in patients with moderate to severe heart failure.

In many countries, bisoprolol is also widely prescribed for hypertension (high blood pressure) and angina pectoris (chest pain caused by insufficient blood flow to the heart muscle). For hypertension, the European Society of Cardiology (ESC) and European Society of Hypertension (ESH) guidelines recommend beta blockers when other compelling indications exist, such as heart failure, previous myocardial infarction, or tachyarrhythmias.

It is important to note that bisoprolol may also be prescribed for conditions not explicitly listed in all product labels, such as rate control in atrial fibrillation or prevention of migraine. Your prescribing physician will determine whether bisoprolol is appropriate for your specific condition. Always follow your doctor's instructions and never adjust or discontinue your dose without medical supervision.

How Bisoprolol Works in the Body

After oral administration, bisoprolol is almost completely absorbed from the gastrointestinal tract with a bioavailability of approximately 90%. It reaches peak plasma concentrations within 2–3 hours and has a plasma elimination half-life of 10–12 hours, allowing for once-daily dosing. Approximately 50% of the drug is metabolized by the liver and 50% is excreted unchanged by the kidneys, providing a balanced pharmacokinetic profile that generally does not require dose adjustment in mild to moderate hepatic or renal impairment.

What Should You Know Before Taking Bisoprolol?

Contraindications

Bisoprolol should not be taken if you have any of the following conditions:

• Allergy to bisoprolol fumarate or any of the inactive ingredients in the formulation
• Acute or decompensated heart failure requiring intravenous inotropic therapy
• Cardiogenic shock – a life-threatening condition where the heart cannot pump enough blood
• Severe bradycardia (very slow heart rate, typically below 50 beats per minute before treatment)
• Second- or third-degree atrioventricular (AV) block without a pacemaker
• Sick sinus syndrome without a pacemaker
• Severe bronchial asthma or severe chronic obstructive pulmonary disease (COPD)
• Severe peripheral arterial circulatory disorders (e.g., advanced Raynaud’s syndrome causing tingling, pallor, or blueness in fingers and toes)
• Untreated pheochromocytoma – a rare tumor of the adrenal gland
• Metabolic acidosis – a condition where the blood becomes too acidic
• Severe hypotension (very low blood pressure)

Warnings and Precautions

Before starting bisoprolol, inform your doctor if you have any of the following conditions, as special monitoring or dose adjustments may be required:

• Diabetes mellitus – bisoprolol may mask symptoms of hypoglycemia (low blood sugar), especially rapid heartbeat
• Strict fasting – increased risk of hypoglycemic episodes
• Prinzmetal’s angina (variant angina) – chest pain at rest caused by coronary artery spasm
• First-degree AV block or other conduction disorders
• Mild to moderate asthma or COPD – a bronchodilator should be co-prescribed; contact your doctor immediately if you develop new breathing difficulties, cough, or wheezing
• Peripheral vascular disease (less severe) – symptoms such as intermittent claudication may initially worsen
• Kidney or liver problems – dose adjustments may be necessary in severe impairment
• Psoriasis or history of psoriasis – beta blockers may trigger or worsen psoriatic skin lesions
• Thyroid disorders (particularly hyperthyroidism) – bisoprolol may mask the signs of thyrotoxicosis
• Pheochromocytoma (treated) – an alpha blocker must be established before bisoprolol can be used

Use in Children and Adolescents

Bisoprolol is not recommended for use in children and adolescents under 18 years of age, as there is insufficient data on safety and efficacy in this population. Pediatric heart failure and hypertension should be managed by a pediatric cardiologist using medications with established safety profiles in younger patients.

Pregnancy and Breastfeeding

Bisoprolol should generally be avoided during pregnancy unless the potential benefit to the mother outweighs the risk to the fetus. Beta blockers as a class can reduce placental perfusion (blood flow), which may lead to intrauterine growth restriction, premature delivery, or fetal death. In the newborn, they may cause hypoglycemia (low blood sugar), bradycardia (slow heart rate), and hypotension (low blood pressure) in the first 48–72 hours of life.

If you are pregnant, planning to become pregnant, or discover that you are pregnant while taking bisoprolol, contact your doctor immediately. Alternative antihypertensive agents with better established safety profiles in pregnancy, such as methyldopa or labetalol, may be considered.

It is not known whether bisoprolol passes into breast milk. Therefore, breastfeeding is not recommended during treatment with bisoprolol. If breastfeeding is strongly desired, discuss the risks and benefits with your doctor.

Driving and Operating Machinery

Bisoprolol may cause dizziness, fatigue, or lightheadedness, particularly at the start of treatment, during dose adjustments, or when combined with alcohol. These effects may impair your ability to drive vehicles or operate heavy machinery. Assess how you respond to the medication before engaging in activities that require alertness. If you experience symptoms that affect your concentration or reaction time, avoid driving until the effects resolve.

How Does Bisoprolol Interact with Other Drugs?

Drug interactions with bisoprolol can be clinically significant and, in some cases, dangerous. Bisoprolol affects the heart rate, cardiac conduction, and blood pressure, meaning that combining it with other medications that have similar effects can lead to additive or synergistic reactions including severe bradycardia, hypotension, or heart block. The following sections outline the most important drug interactions based on international guidelines and the European Medicines Agency (EMA) Summary of Product Characteristics (SmPC).

Major Interactions – Avoid Combination Without Specialist Advice

Moderate Interactions – Use with Caution and Medical Monitoring

What Is the Correct Dosage of Bisoprolol?

Bisoprolol dosing varies depending on the indication and individual patient response. The hallmark of bisoprolol therapy in heart failure is the gradual up-titration protocol, where the dose is increased slowly to allow the heart to adapt. This approach is based on evidence from large clinical trials (CIBIS-II, CIBIS-III) and is endorsed by the ESC Heart Failure Guidelines. Patients must be clinically stable before each dose increase.

Heart Failure Titration Schedule (Adults)

The maximum recommended daily dose is 10 mg. Depending on how well you tolerate the medication, your doctor may extend the interval between dose increases. If your condition worsens or you experience intolerable side effects, the dose may need to be reduced. For some patients, a lower maintenance dose than 10 mg may be sufficient and appropriate.

Hypertension and Angina Dosage (Adults)

When bisoprolol is used for hypertension or angina pectoris (note: this indication may vary by country and specific product license), the typical starting dose is 5 mg once daily. The dose may be increased to 10 mg once daily if needed. In some cases, up to 20 mg daily may be used, though this is uncommon. Your doctor will determine the optimal dose based on your blood pressure response and heart rate.

Elderly Patients

No dose adjustment is generally required for elderly patients. However, as elderly patients may be more sensitive to the effects of beta blockers and may have age-related reductions in kidney function, treatment should be initiated with caution. Careful monitoring of heart rate, blood pressure, and symptoms is recommended, particularly during the titration phase.

Patients with Kidney or Liver Impairment

For patients with mild to moderate hepatic or renal impairment, no dose adjustment is usually necessary due to bisoprolol’s balanced elimination (50% hepatic, 50% renal). In patients with severe renal impairment (creatinine clearance <20 mL/min) or severe hepatic impairment, the maximum daily dose should not exceed 10 mg, and close monitoring is advised. Limited data exist for these populations in the context of heart failure.

How to Take Bisoprolol

Take the tablet once daily in the morning, with a small amount of water. It can be taken with or without food. Scored tablets can be split into two equal halves if needed. Do not crush or chew the tablet. Bisoprolol treatment is usually long-term and should not be discontinued without medical advice.

Missed Dose

If you forget to take a dose, do not take a double dose to compensate. Simply take your usual dose the next morning at the regular time. If you frequently forget doses, consider setting a daily alarm or using a pill organizer.

Overdose

Stopping Treatment

Never stop taking bisoprolol suddenly. Abrupt withdrawal of beta blockers can cause a dangerous rebound effect, including a rapid increase in heart rate, worsening of angina, and deterioration of heart failure – which may be life-threatening. Your doctor will instruct you to reduce the dose gradually, typically halving the dose every 1–2 weeks over a period of at least two weeks. This is especially critical in patients with ischemic heart disease.

What Are the Side Effects of Bisoprolol?

Like all medications, bisoprolol can cause side effects, although not everyone experiences them. The severity and frequency of side effects may vary between individuals and are often dose-related. Many side effects are mild and tend to improve as the body adjusts to the medication, particularly during the initial titration phase. However, some side effects affecting the heart can be serious and require prompt medical attention.

If you experience severe allergic reactions including swelling of the face, tongue, throat, or mouth, or have difficulty breathing, seek emergency medical help immediately. These symptoms may indicate anaphylaxis, a life-threatening allergic reaction.

This is not a complete list of all possible side effects. If you notice any symptoms that concern you while taking bisoprolol, consult your doctor, pharmacist, or nurse. You can also report side effects to your national pharmacovigilance authority (e.g., FDA MedWatch in the United States, Yellow Card Scheme in the United Kingdom, or EudraVigilance in the European Union).

How Should You Store Bisoprolol?

Proper storage of bisoprolol ensures that the medication remains safe and effective throughout its shelf life. Follow these storage guidelines:

• Temperature: Store at room temperature. This medication does not require any special temperature conditions.
• Light and moisture: Keep the tablets in their original blister packaging or container to protect them from light and moisture.
• Children: Store out of the sight and reach of children. Consider using a locked medicine cabinet.
• Expiry date: Do not use bisoprolol after the expiry date (EXP) stated on the blister pack and carton. The expiry date refers to the last day of that month.
• Disposal: Do not dispose of medications in household waste or via the sewage system. Return unused or expired medications to a pharmacy for safe disposal. This helps protect the environment.

If you notice any changes in the appearance of the tablets (discoloration, crumbling, unusual odor), do not take them and consult your pharmacist.

What Does Bisoprolol Contain?

Understanding the composition of your medication is important, particularly if you have known allergies to specific excipients (inactive ingredients). The formulation may vary slightly between manufacturers, but the active ingredient and core excipients are generally consistent across brands.

Active Ingredient

Each film-coated tablet contains bisoprolol fumarate as the active substance. The fumarate salt form ensures good absorption and stability. Available strengths include 1.25 mg, 2.5 mg, 3.75 mg, 5 mg, 7.5 mg, and 10 mg.

Inactive Ingredients (Excipients)

The following excipients are commonly found in bisoprolol film-coated tablets (specific composition may vary by manufacturer):

Tablet core:

• Microcrystalline cellulose (filler/binder)
• Anhydrous calcium hydrogen phosphate (filler)
• Pregelatinized starch (binder/disintegrant)
• Crospovidone (disintegrant)
• Colloidal anhydrous silicon dioxide (glidant)
• Magnesium stearate (lubricant)

Film coating:

• Hypromellose (film-forming agent)
• Titanium dioxide (opacifier/colorant)
• Macrogol/polyethylene glycol (plasticizer)
• Iron oxide yellow and/or red (colorant – in certain strengths only)

Bisoprolol tablets are available from multiple generic manufacturers as well as branded products. The tablets are typically round, biconvex, and film-coated. Color may vary by strength: lower strengths (1.25–2.5 mg) are usually white to off-white, while higher strengths may have a pale yellow or light pink hue depending on the manufacturer. Many tablets are scored to allow splitting for dose adjustment.