Usage
- This fixed-dose combination medication is primarily used to treat mild to moderate essential hypertension (high blood pressure) in adults when monotherapy with either drug alone proves insufficient. It can also be prescribed for angina (heart-related chest pain) and to prevent heart attacks.
- Pharmacological Classification: Antihypertensive (a combination of a beta-blocker and a dihydropyridine calcium channel blocker).
- Mechanism of Action: Atenolol, a beta-blocker, works by blocking the effects of adrenaline on the heart, reducing heart rate and the force of contractions. Lercanidipine, a calcium channel blocker, prevents calcium from entering the cells of the heart and blood vessels, causing vasodilation (widening of blood vessels) and reducing peripheral vascular resistance. The combined effect leads to a synergistic decrease in blood pressure.
Alternate Names
- Lercadip (common alternate name).
- Brand names vary depending on the region/country.
How It Works
- Pharmacodynamics: Atenolol reduces heart rate, cardiac output, and myocardial contractility. Lercanidipine reduces peripheral vascular resistance through vasodilation. Both effects contribute to lowering blood pressure.
- Pharmacokinetics:
- Atenolol is well-absorbed orally but has low bioavailability (approximately 50%) due to first-pass metabolism in the liver. It is primarily excreted unchanged in the urine.
- Lercanidipine is almost completely absorbed after oral administration, with high bioavailability due to minimal first-pass metabolism. It is extensively metabolized in the liver, primarily by CYP3A4 enzymes, with metabolites excreted in urine and feces.
- Mode of Action: Atenolol competitively blocks beta-1 adrenergic receptors in the heart. Lercanidipine blocks L-type calcium channels in vascular smooth muscle and cardiac cells.
- Elimination Pathways: Atenolol is primarily eliminated via renal excretion. Lercanidipine is eliminated via hepatic metabolism (CYP3A4) and subsequent excretion of metabolites in urine and feces.
Dosage
Standard Dosage
Adults:
- Initial dose: Atenolol 50 mg + Lercanidipine 10 mg once daily.
- The lercanidipine component may be increased to 20 mg daily after at least two weeks, depending on the patient’s blood pressure response.
- Administer orally at least 15 minutes before meals, preferably in the morning.
Children:
- Not recommended for children under 18 years old as safety and efficacy have not been established.
Special Cases:
- Elderly Patients: Initiate therapy with caution and close monitoring. No initial dosage adjustment is required, but dose titration should be done gradually with close monitoring.
- Patients with Renal Impairment: Mild to moderate: Use with caution; lercanidipine dose may need to be reduced. Severe (GFR < 30 mL/min): Lercanidipine is contraindicated. Atenolol dose reduction may be needed.
- Patients with Hepatic Dysfunction: Mild: Use with caution and close monitoring. Moderate to severe: Lercanidipine is contraindicated. Atenolol dose adjustment might be necessary.
- Patients with Comorbid Conditions: Caution advised in patients with asthma, COPD, diabetes, and peripheral vascular disease. Dose adjustments and close monitoring may be needed.
Clinical Use Cases
This combination is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Other medications are preferred in these scenarios.
Dosage Adjustments
- Adjust dosage based on individual patient response, renal/hepatic function, and comorbid conditions.
- Monitor blood pressure and heart rate during dose titration.
Side Effects
Common Side Effects:
- Headache, dizziness, flushing, peripheral edema (ankle swelling), palpitations, fatigue.
Rare but Serious Side Effects:
- Angina pectoris, bradycardia, hypotension, allergic reactions, syncope (fainting).
Long-Term Effects:
- Potential for worsening of pre-existing heart conditions if not monitored properly.
Adverse Drug Reactions (ADR):
- Severe allergic reactions (angioedema, anaphylaxis), significant hypotension, bradycardia requiring intervention.
Contraindications
- Hypersensitivity to atenolol, lercanidipine, or other dihydropyridines.
- Severe hepatic or renal impairment.
- Second or third-degree heart block (without a pacemaker).
- Cardiogenic shock.
- Untreated heart failure.
- Unstable angina.
- Recent myocardial infarction (within one month).
- Pregnancy and breastfeeding (unless benefits outweigh risks).
- Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir) and cyclosporine.
Drug Interactions
- CYP3A4 Inhibitors: Increase lercanidipine levels, potentially causing hypotension. Avoid concomitant use.
- CYP3A4 Inducers: Decrease lercanidipine levels, potentially reducing its effectiveness. Monitor and adjust dosage accordingly.
- Beta-blockers: Additive bradycardia and hypotension.
- Calcium Channel Blockers: Additive effects on blood pressure.
- Digoxin: May increase digoxin levels.
- Diabetes Medications: May mask symptoms of hypoglycemia.
- Grapefruit Juice: Increases lercanidipine levels. Avoid concomitant consumption.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C (FDA). Lercanidipine is generally avoided during pregnancy due to potential fetal risks. If antihypertensive treatment is necessary, other agents are preferred.
- Breastfeeding: Lercanidipine is contraindicated during breastfeeding. It is unknown if atenolol is excreted in breast milk. Consider alternative safer options.
Drug Profile Summary
- Mechanism of Action: Atenolol blocks beta-1 receptors, reducing heart rate and contractility. Lercanidipine blocks calcium channels, causing vasodilation.
- Side Effects: Common: headache, dizziness, flushing, edema. Serious: angina, hypotension, allergic reactions.
- Contraindications: Severe liver/kidney disease, heart block, heart failure, unstable angina, pregnancy, breastfeeding.
- Drug Interactions: CYP3A4 inhibitors/inducers, other antihypertensives, digoxin, grapefruit juice.
- Pregnancy & Breastfeeding: Avoid if possible due to potential fetal and neonatal risks.
- Dosage: Adults: Atenolol 50 mg + Lercanidipine 10-20 mg once daily. Adjust based on patient response.
- Monitoring Parameters: Blood pressure, heart rate, renal and liver function.
Popular Combinations
While this is already a combination product, additional antihypertensives like thiazide diuretics (hydrochlorothiazide) or ACE inhibitors (captopril, enalapril) might be added if blood pressure control is not adequate. This should be done under close medical supervision.
Precautions
- General Precautions: Assess renal and hepatic function, monitor blood pressure and heart rate.
- Specific Populations: Refer to “Special Cases” under “Dosage.”
- Lifestyle Considerations: Encourage a healthy lifestyle, including a low-sodium diet, regular exercise, and smoking cessation. Alcohol consumption should be limited. Advise patients about potential dizziness and to avoid operating heavy machinery until tolerance is assessed.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Atenolol + Lercanidipine?
A: The initial dose is Atenolol 50 mg + Lercanidipine 10 mg once daily. The lercanidipine component may be increased to 20 mg daily after two weeks if needed.
Q2: Can this combination be used in patients with severe renal impairment?
A: No, lercanidipine is contraindicated in patients with severe renal impairment (GFR < 30 mL/min). Atenolol dosage may require adjustment.
Q3: What are the most common side effects?
A: Common side effects include headache, dizziness, flushing, peripheral edema, palpitations, and fatigue.
Q4: Are there any significant drug interactions?
A: Yes, clinically significant interactions can occur with CYP3A4 inhibitors and inducers, other antihypertensives, digoxin, and grapefruit juice.
Q5: Can this combination be used during pregnancy or breastfeeding?
A: No, lercanidipine is contraindicated in pregnancy and breastfeeding. Atenolol use requires careful risk-benefit assessment. Safer alternative agents are preferred if possible.
Q6: How long does it take to see the full effect of this medication?
A: The maximal antihypertensive effect may take up to two weeks to develop.
Q7: What should be monitored in patients taking this combination?
A: Blood pressure, heart rate, and renal and hepatic function should be monitored regularly.
Q8: What should patients do if they miss a dose?
A: If a dose is missed, take it as soon as remembered unless it is close to the time for the next dose. Do not double the dose.
Q9: Can this combination be used to treat hypertensive emergencies?
A: No, this medication is not suitable for managing hypertensive emergencies. Other more rapidly acting medications are preferred.
Q10: Can this combination be crushed or chewed?
A: No, the tablets should be swallowed whole with water. Some brands may be scored for easier swallowing, but confirm this with the specific product information.
