Bisoprolol Tablets

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Therapeutic Indication

Hypertension
Chronic stable angina
Chronic heart failure
Arrhythmias
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Bisoprolol

Tablet

This drug belongs to a class of drugs known as beta blockers. It works by blocking the action of certain natural chemicals in body such as epinephrine on the heart and blood vessels.We can use bisoprolol with or without other medications to treat high blood pressure also known as hypertension. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Bisoprolol is a cardioselective β1-adrenergic blocking agent.
This drug is considered as a potent drug with a long-half life that can be used once daily. Bisoprolol is generally well tolerated due to its β1-adrenergic receptor selectivity . It is a useful alternative to non-selective β-blocker drugs in the treatment of hypertension ( Carvedilol and Labetalol).
This drug can be used alone or in combination with other drugs to treat hypertension.Bisoprolol can be useful in patients with chronic obstructive pulmonary disease (COPD) due to its receptor selectivity.

Speciality Cardiology
Tags Beta Blocker | Antihypertensive | Cardiac Drug
Strength
  • 2.5 mg
  • 5 mg
Packing Size
  • 10 Tablets

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Mechanism

Bisoprolol is a potent highly beta1-selective-adrenoceptor blocking agent, lacking intrinsic sympathomimetic. It only shows low affinity to the beta2-receptor of the smooth muscles of bronchi and vessels as well as to the beta2-receptors which is concerned with metabolic regulation. Its beta1-selectivity extends beyond the therapeutic dose range.
Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension. Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, which leads to greater cardiovascular work, which increases the demand for oxygen. Bisoprolol reduce the output of renin in the kidneys, which normally increases blood pressure. some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate.

Pharmacokinetics

  • Absorption: Well absorbed orally with high bioavailability (~90%).
  • Distribution: Moderate protein binding (~30%).
  • Metabolism: Partially metabolized in liver.
  • Elimination: Excreted via kidney and liver; half-life ~10–12 hours.

Side Effects

  • Bradycardia
  • Dizziness
  • Fatigue
  • Hypotension
  • Cold extremities

Contraindication

  • Severe bradycardia
  • Cardiogenic shock
  • Second/third degree AV block
  • Uncontrolled heart failure
  • Hypersensitivity

Interaction

  • Calcium channel blockers (verapamil, diltiazem)
  • Other antihypertensives
  • Insulin (mask hypoglycemia)
  • NSAIDs (reduce effect)

Warning and Precautions

  • Do not stop abruptly
  • Use cautiously in asthma/COPD
  • Monitor heart rate and BP
  • Caution in diabetes patients