Bisoprolol blocks the action of the sympathetic nervous system on the heart by blocking the heart's beta-1 adrenergic receptors. Bisoprolol reduces the heart rate and force of contraction, thus lowering blood pressure.
Absorption: Rapid and almost complete.
Distribution: Widely distributed, with the highest concentrations in the heart, liver, lungs, and saliva.
Metabolism: Extensively hepatic, with a significant first-pass effect (~20%).
Excretion: Primarily through urine (50% as unchanged drug, remainder as inactive metabolites); feces (<2%).
Betafix® (Bisoprolol) is indicated for the management of hypertension and the treatment of angina and heart failure. It may be used alone or in combination with other antihypertensive agents.
The dose of Betafix® must be individualized according to the patient's needs. The usual starting dose is Betafix® 5 mg once daily. In some patients, Betafix® 2.5 mg may be an appropriate starting dose. If the antihypertensive effect of Betafix® 5 mg is inadequate, the dose may be increased to Betafix® 10 mg and then, if necessary, to 20 mg once daily.
Patients with Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance <40 ml/min), the initial daily dose should be 2.5 mg, and caution should be exercised during dose titration. Since limited data suggest that Bisoprolol fumarate is not dialyzable, drug replacement is not necessary for patients undergoing dialysis.
Geriatric Patients: No dose adjustment is necessary in the elderly unless there is significant renal or hepatic dysfunction.
Pediatric Patients: There is no pediatric experience with Bisoprolol.
Bisoprolol is contraindicated in patients with cardiogenic shock, overt cardiac failure, second- or third-degree AV block, and marked sinus bradycardia.
Pregnancy: Bisoprolol should not be used during pregnancy unless clearly necessary. If treatment is considered essential, uteroplacental blood flow and fetal growth should be monitored. If any harmful effects on the pregnancy or fetus occur, alternative treatment should be considered. The newborn must be closely monitored, as symptoms of hypoglycemia and bradycardia are generally expected within the first three days after birth.
Lactation: It is unknown whether this drug is excreted in human milk. Therefore, breastfeeding is not recommended during Bisoprolol administration.
Common side effects include fatigue, dizziness, headache, nausea, vomiting, diarrhea, constipation, abdominal pain, cold or numb extremities (hands and feet), muscle weakness or cramps, bradycardia (slower than normal heart rate), worsening of heart failure, sleep disturbances, depression, and breathing difficulties due to bronchospasm, especially in patients with asthma or COPD.
Impaired Renal or Hepatic Function: Caution is advised when adjusting the dose in patients with renal or hepatic impairment.
Risk of Anaphylactic Reactions: Patients with a history of severe anaphylactic reactions may have an increased risk when exposed to allergens while taking beta-blockers. Such patients may be unresponsive to standard doses of epinephrine used to treat allergic reactions.
The most common signs of Bisoprolol overdose include bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia. Few cases of Bisoprolol overdose have been reported, with symptoms mainly involving bradycardia and hypotension. Some patients required sympathomimetic agents for recovery. If overdose occurs, Bisoprolol therapy should be discontinued, and supportive and symptomatic treatment should be provided.
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Medicine: Keep out of reach of children.
