Generic
Bisoprolol Fumarate
2 brands available in the market
At a glance
Bisoprolol Fumarate is a cardioselective beta-blocker used in the treatment of hypertension, angina pectoris, and moderate to severe heart failure. It slows heart rate and reduces cardiac workload.
Description
Bisoprolol Fumarate is a highly cardioselective β1-adrenoceptor blocking agent. It selectively blocks β1-adrenergic receptors in the heart and vascular smooth muscle, reducing heart rate and cardiac output, thereby lowering blood pressure. It exhibits the highest level of affinity for the β1 receptor among currently available beta-blockers.
At therapeutic doses, it has no effect on β2-adrenoceptors, resulting in minimal bronchial effects in patients with asthma or COPD. It does not adversely affect lipid metabolism.
The drug is almost completely (>90%) absorbed from the gastrointestinal tract with 88% bioavailability. It has a half-life of 10-12 hours.
Indications
- Hypertension
- Angina pectoris
- Stable chronic heart failure (in addition to ACE inhibitors, diuretics, and cardiac glycosides)
Therapeutic class
Beta-adrenoceptor blocking drugs
Pharmacological class
Cardioselective Beta-blocker
Pharmacology
Bisoprolol Fumarate is a highly cardioselective β1-adrenoceptor blocker that reduces heart rate and cardiac output. At therapeutic doses, it has no effect on β2-receptors. It is almost completely absorbed (88% bioavailability), has a half-life of 10-12 hours, and is metabolized by CYP3A4 (≈95%) and CYP2D6 in the liver.
Mechanism of action
Bisoprolol selectively blocks β1-adrenergic receptors, reducing heart rate and myocardial contractility, thereby lowering blood pressure and decreasing myocardial oxygen demand. Its antihypertensive effect also involves decreased cardiac output, inhibition of renin release, and reduction of central sympathetic outflow.
Dosage
Hypertension and Angina: Initial dose: 5 mg once daily. May be increased to 10 mg and up to 20 mg once daily (2-week interval for titration).
Stable Chronic Heart Failure: Titrate according to the following scheme:
Week 1: 1.25 mg once daily
Week 2: 2.5 mg once daily
Week 3: 3.75 mg once daily
Weeks 4-7: 5 mg once daily
Weeks 8-11: 7.5 mg once daily
Thereafter: 10 mg once daily (maximum)
Renal/Hepatic Impairment: No dose adjustment for mild-moderate impairment. In severe impairment (CrCl <20 mL/min or severe hepatic disease), daily dose should not exceed 10 mg.
Administration
Take in the morning with or without food. Swallow whole; do not chew or crush. Long-term therapy as advised by your doctor.
Missed dose
If you miss a dose, take it as soon as you remember. Skip if it is almost time for your next dose. Do not double the dose.
Side effects
Common (>1%): Fatigue (8.2%), headache (10.9%), dizziness (3.5%), nausea (2.2%), diarrhea (3.5%), dyspnea (1.5%), bradycardia, cold extremities, muscle weakness/cramps.
Uncommon: Insomnia, depression, vivid dreams, paresthesia, dry mouth, bronchospasm (in asthma/COPD patients).
Precautions & warnings
- Do not stop abruptly (may worsen condition, especially in ischemic heart disease). Withdraw gradually if necessary.
- Diabetic patients should monitor blood glucose regularly (may mask hypoglycemia symptoms).
- Caution in patients with history of severe anaphylactic reactions (usual epinephrine doses may be ineffective).
- Know your response to the medicine before driving or operating machinery.
- Caution in asthma/COPD patients (keep bronchodilator available).
- May mask symptoms of thyrotoxicosis.
Contraindications
- Cardiogenic shock
- Overt heart failure
- Second or third degree AV block
- Right ventricular failure secondary to pulmonary hypertension
- Marked sinus bradycardia
Drug interactions
- Other beta-blockers: Should not be combined.
- Catecholamine-depleting drugs (reserpine, guanethidine): May produce excessive sympathetic reduction; monitor closely.
- Clonidine: Discontinue bisoprolol several days before clonidine withdrawal (avoid rebound hypertension).
- Calcium channel blockers (verapamil, diltiazem): Prolongation of SA and AV conduction.
- Class I antiarrhythmics (disopyramide, quinidine): Increased negative inotropic effect and AV conduction time.
- Digitalis glycosides: Increased risk of bradycardia.
- NSAIDs: Reduced antihypertensive effect.
- Sulfonylureas: Risk of severe hypoglycemia.
Food interactions
Avoid alcohol consumption (may cause excessive drowsiness and hypotension).
Use in pregnancy
There are no adequate and well-controlled studies in pregnant women. Animal studies showed no teratogenic effects but fetotoxicity (increased resorptions). Use only if potential benefit justifies risk to the fetus.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Bisoprolol is excreted in rat milk (<2% of dose). Not known if excreted in human milk. If use is essential, discontinue nursing.
Pediatric use
Safety and effectiveness in pediatric patients have not been established.
Geriatric use
No dose adjustment required for elderly patients.
Renal / hepatic impairment
Hepatic impairment: In severe hepatic disease, daily dose should not exceed 10 mg.
Overdose effects
Common signs of overdose: bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia. Maximum reported overdose: 2000 mg. Treatment: supportive and symptomatic. May require atropine IV, isoproterenol, vasopressors, glucagon, bronchodilators.
Storage conditions
Store in a dry place below 30°C, away from light and heat. Keep out of reach of children.
Chemical structure
Molecular Formula: C₁₈H₃₁NO₄