Cardicor 2.5 mg

Description

Indications

Cardicor Tablet is prescribed for the treatment of:

• Hypertension (high blood pressure)
• Angina (chest pain)
• Moderate to severe heart failure

Cardicor is not suitable for the emergency treatment of hypertensive crises.

Always take the medicine as advised by a registered healthcare provider.

Pharmacology

Bisoprolol Fumarate is a highly selective β1 receptor blocker, offering the greatest affinity for the β1 receptor compared to other beta-blockers. It specifically targets the β1 adrenergic receptors found in the heart and blood vessels, leading to a reduction in heart rate and cardiac output, thereby lowering blood pressure.

Unlike non-selective beta-blockers, Bisoprolol does not negatively affect lipid metabolism or reduce the levels of cardioprotective HDL cholesterol during long-term use.

Absorption and Bioavailability: Bisoprolol is almost fully absorbed (>90%) from the gastrointestinal tract. The absorption rate is high, and the first-pass effect is minimal (<10%), resulting in an absolute bioavailability of approximately 88%. Food intake does not influence its absorption.

Distribution: The drug is widely distributed in the body, with a medium volume of distribution of 3.51 L/kg.

Metabolism: Bisoprolol undergoes metabolism via oxidative pathways without conjugation. Its metabolites are highly polar and are excreted in the urine. Studies indicate that Bisoprolol is primarily metabolized by CYP3A4 (95%) with minimal involvement of CYP2D6.

Elimination: The drug’s clearance is equally distributed between renal elimination (about 50%) and hepatic metabolism (about 50%). The total clearance rate is approximately 15 L/h, and its half-life ranges from 10 to 12 hours, allowing for once-daily dosing.

Dosage & Administration

• Adults: For mild to moderate hypertension, the initial dose of Bisoprolol fumarate is 5 mg once daily, either alone or with a diuretic. If the response is inadequate, the dosage may be increased to 10 mg and, if necessary, to 20 mg daily. Dosage adjustments should occur at 2-week intervals, and increasing the dose beyond 20 mg provides limited additional benefits.
• Children: Safety and efficacy in children have not been established.
• Patients with Renal or Hepatic Impairment: In individuals with liver disease (such as cirrhosis or hepatitis) or kidney dysfunction (creatinine clearance <40 mL/min), the starting dose should be 5 mg. Dose adjustments should be made cautiously, with a focus on avoiding accumulation. Bisoprolol is not dialyzable, so no dose adjustment is required for dialysis patients.
• Geriatric Patients: Elderly patients generally do not require dose adjustments unless there is significant renal or hepatic dysfunction.

Always follow the advice of your healthcare provider when using this medication.

Interaction

• Other β-blocking Agents: Cardicor should not be used alongside other β-blockers due to the risk of additive effects.
• Catecholamine-Depleting Drugs: Medications such as reserpine or guanethidine should be used cautiously with Cardicor, as it may lead to excessive reduction in sympathetic activity.
• Centrally Active Antihypertensive Drugs: Cardicor may enhance rebound hypertension after clonidine withdrawal. If both drugs are prescribed, Cardicor should be discontinued several days before stopping clonidine. When replacing clonidine with a β-blocker, delay the initiation of the β-blocker until several days after stopping clonidine.
• Antiarrhythmic Drugs and Calcium Channel Blockers: Care should be taken when combining Cardicor with myocardial depressants or calcium channel blockers (especially verapamil or diltiazem), as they may prolong A-V conduction and cause severe hypotension, bradycardia, or cardiac failure.

Contraindications

Cardicor is contraindicated in patients with:

• Cardiogenic shock
• Overt heart failure
• Second or third-degree A-V block
• Right ventricular failure due to pulmonary hypertension
• Sinus bradycardia

Side Effects

Side effects associated with Cardicor may vary from person to person. Some common side effects include:

• Fatigue
• Dizziness
• Headaches
• Gastrointestinal issues such as nausea, vomiting, diarrhea, constipation, or abdominal discomfort
• Cold or numb extremities (hands and feet)
• Muscle weakness or cramps
• Bradycardia (slower-than-normal heart rate)
• Breathing difficulties due to bronchospasm, especially in individuals with asthma or chronic obstructive pulmonary disease (COPD)

Pregnancy & Lactation

• Pregnancy: Bisoprolol fumarate has shown no teratogenic effects in rats at doses up to 375 times the recommended human daily dose. However, it caused fetal toxicity and maternal toxicity at higher doses. The drug has not been studied in pregnant women, so it should be used only when the potential benefits outweigh the risks to the fetus.
• Lactation: Bisoprolol fumarate has been detected in small amounts in the milk of lactating rats (<2% of the dose). It is unclear whether it passes into human breast milk. If it is necessary to use Cardicor, breastfeeding should be discontinued.

Precautions & Warnings

• Renal and Hepatic Impairment: Care should be taken when adjusting the dosage in patients with impaired renal or hepatic function.
• Anaphylaxis: Patients with a history of severe anaphylactic reactions to allergens may have an exaggerated response to repeated exposures while taking beta-blockers, and may be less responsive to typical doses of epinephrine.

Therapeutic Class

Cardicor is classified as an anti-adrenergic agent and a beta-blocker.

Storage Conditions

Store Cardicor in a dry place, away from light and heat. Keep out of reach of children.

Chemical Structure

• Molecular Formula: C18H31NO4

Common Questions about Cardicor 2.5 mg Tablet

• What is Cardicor 2.5 mg Tablet?
  Cardicor 2.5 mg Tablet is a beta-blocker that helps reduce heart rate, blood pressure, and the workload on the heart.

• What is Cardicor used for?
  Cardicor 2.5 mg Tablet is prescribed to manage high blood pressure, chest pain (angina), and heart failure.

• How should I take Cardicor 2.5 mg Tablet?
  Take the tablet by mouth, once daily, with or without food. For best results, take it at the same time each day.

• What are the side effects of Cardicor?
  Common side effects may include dizziness, fatigue, headache, slow heart rate, difficulty breathing, and cold extremities.

• Is it safe to take Cardicor 2.5 mg Tablet?
  Cardicor is generally safe when prescribed by a healthcare professional. Consult your doctor before taking it if you have pre-existing health conditions like asthma, diabetes, heart issues, or kidney/liver problems.

• Should I take Cardicor 2.5 mg Tablet before or after food?
  It is recommended to take Cardicor 2.5 mg Tablet after food, as per the prescribed dosage.

• How should I store Cardicor 2.5 mg Tablet?
  Store it in a cool, dry place, in its original packaging, and keep it out of reach of children and pets.

Quick Tips

• Be cautious when standing up quickly, as Cardicor may cause dizziness.
• If you’re diabetic, monitor your blood sugar levels closely, as Cardicor may mask symptoms of low blood sugar.
• Do not stop taking Cardicor suddenly, as it could cause a sudden increase in blood pressure, raising the risk of heart attack or stroke.