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Bisoprolol – Effect, Application & Risks

Bisoprolol

Bisoprolol is a drug and is used to treat tachycardia , angina pectoris , high blood pressure and coronary artery disease (CHD). Bisoprolol has an antagonistic effect on ß-adrenoreceptors (beta-adrenoreceptors) and belongs to the group of beta- blockers . Side effects such as fatigue , dizziness , and headaches may occur as a result of taking the drug .

What is bisoprolol?

Bisoprolol belongs to the group of selective ß-adrenoceptor blockers and has an antagonistic effect on ß1-adrenoreceptors. As a selective beta-blocker, bisoprolol acts specifically on the heart and has no effect on other organs .

Medically, bisoprolol is referred to as a cardioselective drug. Chemically, bisoprolol is a phenol ether that exists as a racemic mixture. Bisoprolol is a chiral compound and the drug is used in a 1:1 mixture of the (R) and (S) stereoisomers. The (S) form of the drug is the active stereoisomer and has high binding affinity to ß1-adrenoreceptors. (S)-bisoprolol displaces adrenaline from the binding site of the ß1-adrenoreceptor and acts as an antagonist.

The drug is used to treat angina pectoris, tachycardia, chronic heart failure and high blood pressure. The drug requires regular intake. Sudden cessation of therapy leads to withdrawal symptoms and serious side effects .

Pharmacological effect on body & organs

The beta-blocker bisoprolol occupies ß1-adrenoreceptors and prevents adrenaline and noradrenaline from binding to the receptors . Noradrenaline is a neurotransmitter that is produced in the human brain and in the adrenal cortex . Adrenaline is a hormone produced in the human adrenal cortex . Adrenaline and noradrenaline differ in chemical structure by a methyl group. Adrenaline has a methyl group substituted on the amino group. Norepinephrine and adrenaline bind to ß1-adrenoceptors in the heart and lead to an increased activity of the heart muscle . theHeart rate increases by lowering the pacing threshold in the heart. The pumping power of the heart increases and blood pressure rises. 

Bisoprolol displaces adrenaline and noradrenaline from the ß1-adrenoceptors and occupies the binding sites. As an antagonist, the drug weakens the effects of adrenaline and noradrenaline. As a result of the receptor binding and the reduced effect of adrenaline and noradrenaline, the blood pressure is lowered and the stimulus threshold is increased. The heart requires less energy and oxygen consumption is reduced. Overall, the heart muscle is relieved by bisoprolol. Medicine speaks of a negative inotropic effect that all beta blockers have.

Binding and effects of bisoprolol are long-lasting. The half-life in the blood is 10 to 11 hours. Bisoprolol is administered orally and about 90% is absorbed. The bioavailability is excellent at 90% and the maximum plasma concentration is reached about 3 hours after ingestion. The beta-blocker is excreted renally and metabolised in the liver . The ratio between renal excretion and liver elimination is 50:50.

Due to the targeted effect of bisoprolol on the ß1-adrenoreceptor, the drug has a cardio-specific effect. Nevertheless, a central nervous effect can occur. Effects and side effects of bisoprolol on the central nervous system ( CNS ) are due to the lipophilic properties of the drug. Intrinsic sympathomimetic activity (ISA) has not been demonstrated.

Medicinal Application & Use for Treatment & Prevention

The beta-blocker bisoprolol is used to treat arterial hypertension (high blood pressure), chronic heart failure, angina pectoris and tachycardia. Coronary heart disease (CHD) can trigger angina pectoris. The beta blocker is often used for high blood pressure and is therefore used to prevent serious heart disease.

The treatment of arterial hypertension and angina pectoris is usually started with a dose of 5 mg bisoprolol per day. The dose depends on the severity of the findings. A daily dose of 2.5 mg is recommended for mild high blood pressure. If a dose of 5 mg bisoprolol is not sufficient, an increase to 10 mg bisoprolol per day is recommended. Only in exceptional cases should the daily dose be above 10 mg. The dosage should be gradually increased or slowly decreased as needed. If the drug is suddenly discontinued, withdrawal symptoms and serious side effects are the result. Discontinuation of bisoprolol is only possible by tapering off and must be accompanied by a doctor.

Bisoprolol should not be used in patients with bronchial asthma , bradycardia , diabetes mellitus and severe heart failure. Patients who apply MAO inhibitors should also refrain from taking the drug.

Risks & side effects

Taking bisoprolol can cause side effects. Common complaints are tiredness, exhaustion , sensory disturbances , dizziness and headaches. Uncommon side effects of the drug include depression , trouble sleeping , mood swings and confusion .Furthermore, taking the drug can lead to circulatory disorders , muscle weakness , skin rashes , joint diseases and skin itching . Disturbed heart function and a slow heartbeat are also part of the symptoms. A drop in blood pressure caused by getting up quickly from a sitting or lying position is also an uncommon side effect.

Vomiting , constipation , diarrhea , abdominal pain and nausea are also occasionally occurring side effects in the gastrointestinal area. Rarely do reactions such as increased blood fat levels , increased sweating , reduced tear flow , weight gain and sexual listlessness occur.

 

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.