Indications Bisopro, a highly selective β 1 blocker, is indicated for the treatment of:
- Hypertension (High blood pressure)
- Angina (Chest pain)
- Moderate to severe heart failure
- Note: It is not recommended for the emergency treatment of hypertensive crises.
Pharmacology Bisoprolol Fumarate is the most selective β 1 blocker, primarily targeting β 1 adrenergic receptors in the heart and vascular smooth muscle. This action reduces heart rate and cardiac output, leading to a decrease in arterial hypertension. Unlike non-selective β -blockers, Bisoprolol does not adversely affect the cholesterol fraction, including HDL -cholesterol, in long-term therapy. Its elimination half-life is 10 − 12 hours, supporting once-daily dosing.
Dosage & Administration (Adults) The dose must be individualized.
- Starting Dose: 5 mg once daily (alone or added to a diuretic).
- Dose Titration: If the response is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily. Doses are increased at 2 -week intervals.
- Maximum Dose: Increasing the dose beyond 20 mg once daily provides minimal additional benefit.
Special Populations:
- Renal or Hepatic Impairment: Initial daily dose should be 5 mg . Titration must be used with caution due to the possibility of drug accumulation.
- Geriatrics: Dose adjustment is usually unnecessary, unless significant renal or hepatic dysfunction is present.
- Children: Safety and effectiveness have not been established.
Contraindications Do not use Bisopro in patients with:
- Cardiogenic shock
- Overt heart failure
- Second or third-degree A-V block
- Right ventricular failure secondary to pulmonary hypertension
- Sinus bradycardia
Side Effects Side effects are primarily related to CNS depression and may include:
- Fatigue, dizziness, headache
- Disturbances of the gut (nausea, vomiting, diarrhea, constipation, or abdominal pain)
- Cold or numb extremities
- Muscle weakness or cramps
- Slower than normal heart rate ( bradycardia )
- Breathing difficulties ( bronchospasm ) in people with asthma or COPD .
Interactions
- Other β -blockers: Should not be combined.
- Calcium Channel Blockers (e.g., Verapamil, Diltiazem) and Antiarrhythmic Agents (e.g., Disopyramide): Concurrent use may lead to severe hypotension, bradycardia, and cardiac failure.
- Clonidine: The β -blocker should be withdrawn several days before discontinuing clonidine to avoid rebound hypertension.
Therapeutic Class: Anti adrenergic agent ( Beta blockers ), Beta-adrenoceptor blocking drugs .
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