Bisoprolol

Bisoprolol Fumarate (中文：比索洛爾)

Common Strengths of Bisoprolol

Bisoprolol is available in the following strengths:

• 2.5 mg
• 5 mg

Drug Trade Name of Bisoprolol

The brand names for metoprolol is Concor.

Mechanism of Action

Beta-blockers prevent adrenaline and noradrenaline from reaching the beta receptors in the heart, blood vessels, liver, pancreas, and bronchi.

Bisoprolol is a cardioselective beta blocker, which is β1blockade, and mainly affects the heart, reducing heart rate, myocardial contractility, and rate of conduction of impulses through the conducting system. As a result, it can decrease the heart conduction and output and lead to reduce the blood pressure effectively. It also leads to suppression of adrenergic-induced renin release and lipolysis. Moreover, it have lower affinity for bronchial and vascular β2 receptors. In the generally, it only have little influence on the bronchial and vascular β2 receptor.

Route of Administration

Bisoprolol tablet should be taken in morning and can be taken with food. They should be swallowed in liquid and should not be chewed.

Dosages

• Therapeutic indications
  • Treatment of hypertension
  • Treatment of stable chronic angina
  • Treatment of stable heart failure with reduced systolic left ventricular function in addition to ACE inhibitors, and diuretics

• In Hypertension or Angina Pectoris
  • By mouth
  • Adult: The usual dose is 5 to 10 mg as a single daily dose; The maximum recommended dose is 20 mg daily
• In Heart failure
  • The initial oral dose of bisoprolol fumarate is 1.25 mg once daily. If tolerated, the dose should be doubled after 1 week, and then increased gradually at 1 to 4 week intervals to the maximum dose tolerated; This should not exceed 10 mg once daily.
• Administration in Hepatic or Renal Impairment
  • The initial dose for hypertension should be 2.5 mg once daily, the dose should be increased cautiously in patients with severe hepatic impairment and renal impairment (creatinine clearance less than 40ml/min); A maximum dose of 10 mg daily for both angina pectoris and hypertension.
  • Bisoprolol is not dialysable.

• Discontinuation of treatment
  • The treatment should not be stopped suddenly. The dose should be diminished slowly by weekly halving of the dose.
  • Abrupt stopping may precipitate angina and other unwanted heart effects including myocardial infarction.

Side Effects

Frequency	Adverse reactions
Very common (≥1/10)	Bradycardia (In patients with chronic heart failure)
Common (≥1/100 to <1/10)	Dizziness
	Headache
	Worsening of pre-existing heart failure (In patients with chronic heart failure)
	Feeling of coldness or numbness in the extremities
	Hypotension especially in patient with heart failure
	Gastrointestinal complaints such as nausea, vomiting, diarrhoea, constipation
Uncommon (≥1/1,000 to <1/100)	Bronchospasm in patients with asthma or COPD
Rare (≥1/10,000 to <1/1,000)	Reduced tear flow (To be considered if the patient uses lenses)