Myocor tablet is indicated in-
Myocor is not recommended for the emergency treatment of hypertensive crises.
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Bisoprolol Fumarate is a highly selective β₁-adrenergic receptor blocker, demonstrating the greatest affinity for cardiac β₁ receptors compared to other available beta-blockers. By selectively inhibiting β₁-receptors in the heart and vascular smooth muscle, it lowers heart rate and cardiac output, resulting in reduced arterial blood pressure. Unlike non-selective beta-blockers, Bisoprolol does not negatively affect lipid metabolism and has no adverse impact on cholesterol fractions, including HDL, during long-term therapy.
Pharmacokinetics:
Absorption & Bioavailability: Bisoprolol is almost completely absorbed (>90%) from the gastrointestinal tract with a minimal first-pass effect (<10%), leading to an absolute bioavailability of approximately 88%. Food does not influence its absorption.
Distribution: The drug exhibits extensive distribution with an average distribution volume of 3.5 L/kg.
Metabolism: It undergoes oxidative metabolism primarily via the CYP3A4 enzyme (≈95%), with CYP2D6 playing a minor role. Its metabolites are pharmacologically inactive and are excreted through the kidneys.
Elimination: Approximately half of the drug is excreted unchanged via the kidneys, while the remainder is metabolized hepatically and then eliminated renally. The total clearance is about 15 L/h, and the elimination half-life is between 10–12 hours, allowing for once-daily dosing.
Adults: For mild to moderate hypertension, the recommended starting dose is 5 mg once daily, either alone or with a diuretic. If the response is inadequate, the dose may be gradually increased to 10 mg or up to 20 mg once daily at 2-week intervals. Doses above 20 mg offer limited additional benefit.
Children: Safety and efficacy in children have not been established.
Renal or Hepatic Impairment: Patients with renal (creatinine clearance <40 mL/min) or hepatic dysfunction should start with 5 mg daily. Dose adjustments should be made cautiously due to potential accumulation. Bisoprolol is not dialyzable, so replacement after dialysis is unnecessary.
Elderly: Dose adjustments are generally unnecessary unless significant hepatic or renal impairment is present.
Myocor should not be used in patients with cardiogenic shock, overt heart failure, second or third-degree AV block, sinus bradycardia, or right ventricular failure secondary to pulmonary hypertension.
Pregnancy: Animal studies indicate no teratogenicity but show fetotoxicity at high doses. Use only if potential benefits outweigh the potential risks.
Lactation: Trace amounts have been detected in animal milk; human excretion is unknown. Discontinue breastfeeding if treatment is necessary.
Use cautiously in patients with impaired hepatic or renal function.
Beta-blockers may mask hypoglycemia symptoms in diabetic patients.
Patients with a history of severe anaphylaxis may be less responsive to epinephrine while on Bisoprolol.
Keep in original packaging in a cool, dry place, away from children and pets.
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