Bisoprolol

Cardiovascular Drug

Drug class: Beta blockers

Bisoprolol Fumarate (CONCOR) (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)

Pharmacokinetics

• Bisoprolol is almost completely absorbed from the GI tract and undergoes only minimal first-pass metabolism resulting in an oral bioavailability of about 90%
• After an oral dose, peak plasma concentrations occur 2 to 4 hours.
• Bisoprolol is about 30% bound to plasma proteins.
• It has a plasma elimination half-life of 10 to 12 hours and gives a 24-hour effect after dosing once daily.
• The half-life of bisoprolol is increased three-fold in people with kidney disease and a creatinine clearance of less than 40 mL/min.
• It is metabolized in the liver and excreted in urine, about 50% as unchanged drug and 50% as metabolites.

Drug Management

Drug Interaction

Combinations not recommended

• Applies only to chronic heart failure
  • Antiarrhythmic drugs (e.g. quinidine, disopyramide, flecanide)
    • Effect on atrio-ventricular conduction time may be potentiated and negative inotropic effect increased
• Applies to all indications
  • Calcium channel blocker of the non-dihydropyridine type such as verapamil type
    • Negative influence on contractility and atrio-ventricular conduction
  • Centrally-acting antihypertensive drugs such as methyldopa
    • Concomitant use of centrally acting antihypertensive drugs may worsen heart failure by a decrease in the central sympathetic tonus (Reduction of heart rate and cardiac output, vasodilation)

This list is not all-inclusive and includes only common medications that may interact with bisoprolol.

Caution

• Bronchospasm (bronchial asthma, obstructive airways diseases)
• Diabetes mellitus with large fluctuations in blood glucose values; symptoms of hypoglycaemia (e.g. tachycardia, palpitations or sweating) can be masked.
• Patients with psoriasis or with a history of psoriasis should only be given beta-blockers (e.g. bisoprolol) after carefully balancing the benefits against the risks.

Contraindication

• Acute heart failure or during episodes of heart failure decompensation requiring i.v. inotropic therapy
• Cardiogenic shock
• Second or third degree AV block (without a pacemaker)
• Sick sinus syndrome
• Sinoatrial block
• Symptomatic bradycardia
• Symptomatic hypotension
• Severe bronchial asthma or severe chronic obstructive pulmonary disease
• Metabolic acidosis
• Untreated phaeochromocytoma

FAQs

How should I take the tablet?

• Bisoprolol tablet should be taken in morning and can be taken with food. They should be swallowed in liquid and should not be chewed.
• Do not skip doses or stop taking bisoprolol without first talking to your doctor. Stopping suddenly may make your condition worse or cause other serious heart problems.
• If you need surgery, tell the surgeon ahead of time that you are using bisoprolol.

What should I avoid while taking?

• This medicine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
• Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.
• Minimize drinking alcohol. It can increase some of the side effects of bisoprolol.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Slip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.