Actions and Spectrum: 

Actions of bisoprolol include: 

• Lowering blood pressure: it works by blocking the effects of the hormone adrenaline on the blood vessels, which causes them to relax and widens, leading to a decrease in blood pressure. 
• Decreasing heart rate: it also blocks the effects of adrenaline on the heart, which slows down the heart rate and reduces the workload on the heart. 
• Improving heart function: By reducing the workload on the heart and lowering blood pressure, bisoprolol can help improve heart function in patients with heart failure. 
• Relieving angina symptoms: it can help to relieve symptoms of angina by decreasing the workload on the heart and reducing the need for oxygen in the heart muscle. 

The spectrum of bisoprolol includes: 

• High blood pressure: it is commonly used to treat high blood pressure, also known as hypertension. 
• Heart failure: it can be used to treat heart failure, a condition in which the heart is unable to pump enough blood to meet the body’s needs. 
• Angina: it can be used to treat angina, a type of chest pain caused by reduced blood flow to the heart. 
• Arrhythmias: it may also be used to treat certain types of arrhythmias or abnormal heart rhythms. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency Defined  

1-10%  

Insomnia (8%-10%)  

Dizziness (10%)  

Upper respiratory infection (5%)  

Rhinitis (4%)  

Arthralgia (3%)  

Diarrhea (4%)  

Cough (3%)  

Nausea (2%)  

Dyspnea (2%)  

Pharyngitis (2%)  

Vomiting (2%)  

Sinusitis (2%)  

<1%  

Hypotension  

Cold extremities  

Depression 

Bronchospasm   

Dyspepsia  

Frequency Not Defined  

Decrease HDL  

Aggravate CHF  

Hypertriglyceridemia  

Decreased exercise tolerance  

Mask symptoms of hypoglycemia

 

Black Box Warning 

bisoprolol carries a Black Box Warning for its potential to cause serious and potentially life-threatening heart failure in patients with existing heart disease. 

 

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity to bisoprolol or any component of the formulation 
• Cardiogenic shock 
• Second- or third-degree atrioventricular block (unless a pacemaker is in place) 
• Sick sinus syndrome (unless a pacemaker is in place) 
• Severe bradycardia (heart rate less than 50 beats per minute) 
• Uncontrolled heart failure 
• Metabolic acidosis 
• Severe peripheral arterial circulatory disorders 

Cautions: 

• Renal impairment 
• Hepatic impairment 
• Bronchospastic disease (asthma or chronic obstructive pulmonary disease (COPD)) 
• Thyrotoxicosis 
• Diabetes mellitus 
• Pheochromocytoma (bisoprolol should be used with caution in patients with pheochromocytoma as it may provoke an acute hypertensive crisis) 
• Pregnancy and breastfeeding (bisoprolol should be used with caution in pregnant and breastfeeding women as its safety has not been established) 
• Bisoprolol may mask symptoms of hypoglycemia in diabetic patients. 
• Bisoprolol may cause exacerbation of asthma or COPD. 
• Bisoprolol may cause bradycardia and may exacerbate symptoms of heart failure. 
• Bisoprolol may increase the risk of stroke in patients with hypertension. 
• Bisoprolol may cause sleep disturbances and depression. 

Pregnancy warnings:     

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk is unknown.  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

 

Pharmacology:  

bisoprolol is a beta-blocker medication that works by blocking the action of certain hormones, such as adrenaline, on the heart and blood vessels. This results in a decrease in heart rate and blood pressure.  

Pharmacodynamics:  

bisoprolol works by binding to beta-1 receptors in the heart and blood vessels, which results in a decrease in heart rate and blood pressure. It also reduces the workload on the heart and improves blood flow to the heart.  

Pharmacokinetics:  

Absorption  

It is rapidly and well absorbed after oral administration. The maximum concentration of the drug in the blood (Cmax) is reached within 1-2 hours. Food does not affect the absorption of bisoprolol.  

Distribution  

bisoprolol is highly bound to plasma proteins (about 98%) and has a large volume of distribution (about 12L/kg). It also crosses the blood-brain barrier and the placenta.  

Metabolism  

It is metabolized in the liver by the cytochrome P450 3A4 enzyme. The main metabolite is the inactive 4′-hydroxybisoprolol.  

Elimination and excretion  

bisoprolol is excreted mainly in the urine, with about 70% of the dose excreted within 24 hours. The elimination half-life of bisoprolol is about 9-12 hours.  

 

Administration:  

Oral administration: 

Bisoprolol is typically administered as a tablet or extended-release capsule, taken orally once or twice daily. The dosage and frequency of administration will depend on the condition being treated and the patient’s response to the medication. 

It is important to take bisoprolol exactly as prescribed by a healthcare provider, and not to change the dosage or frequency without consulting a healthcare professional. Bisoprolol should be taken with food and should be taken at the same time each day to maintain a consistent level of the drug in the bloodstream. 

Patients should be advised to swallow the tablet whole, and not to crush or chew it. If a dose is missed, it should be taken as soon as possible, unless it is close to the time for the next dose. In this case, the missed dose should be skipped, and the patient should continue with their regular dosing schedule. 

Patients should also be advised to avoid drinking alcohol while taking bisoprolol, as it may increase the risk of side effects such as dizziness or drowsiness. Bisoprolol should also be used with caution in elderly patients, as they may be more sensitive to the drug’s effects. 

  

 

Patient information leaflet 

Generic Name: bisoprolol 

Why do we use bisoprolol? 

bisoprolol is a beta-blocker medication that is used for several medical conditions, including: 

• Hypertension (high blood pressure): bisoprolol is used to lower blood pressure by blocking the effects of certain hormones, such as adrenaline, on the heart and blood vessels. 
• Angina (chest pain): bisoprolol is used to reduce the frequency and severity of angina attacks by slowing the heart rate and decreasing the workload on the heart. 
• Heart failure: it can improve symptoms and survival rates in patients with heart failure by reducing the workload on the heart and improving the heart’s pumping ability. 
• Post-myocardial infarction (heart attack): it may be used after a heart attack to reduce the risk of another heart attack and improve the heart’s pumping ability. 
• Atrial fibrillation: it may be used to slow down the heart rate and reduce symptoms in patients with atrial fibrillation.