Usage
Lercanidipine is prescribed for the treatment of mild to moderate essential hypertension (high blood pressure). It belongs to the pharmacological class of calcium channel blockers, specifically dihydropyridines. Lercanidipine works by blocking the influx of calcium ions into vascular smooth muscle cells, leading to vasodilation (widening of blood vessels) and a reduction in peripheral vascular resistance, thus lowering blood pressure.
Alternate Names
Lercanidipine hydrochloride is the chemical name. Brand names include Zanidip, Lercadip, and Lecalpin. It may also be available in combination tablets with other antihypertensive medications.
How It Works
Pharmacodynamics: Lercanidipine primarily affects the cardiovascular system by causing vasodilation, reducing peripheral vascular resistance, and lowering blood pressure. It has high vascular selectivity, meaning it preferentially acts on vascular smooth muscle with minimal effect on cardiac contractility or conduction.
Pharmacokinetics:
- Absorption: Lercanidipine is well-absorbed orally, but its absorption is significantly increased by high-fat meals. Therefore, it’s advised to take it at least 15 minutes before breakfast or on an empty stomach.
- Metabolism: Extensively metabolized in the liver, primarily by CYP3A4 enzymes. This is a crucial consideration for drug interactions.
- Elimination: Primarily eliminated through hepatic metabolism and biliary excretion; less than 1% is excreted unchanged in the urine.
Mode of Action: Lercanidipine blocks L-type calcium channels in vascular smooth muscle cells. This inhibits calcium influx, preventing muscle contraction and leading to vasodilation.
Receptor Binding/Enzyme Inhibition: Binds to L-type calcium channels, inhibiting their function. Metabolized by CYP3A4 enzymes.
Elimination Pathways: Primarily hepatic metabolism and biliary excretion.
Dosage
Standard Dosage
Adults:
The initial dose is 10 mg once daily, taken orally at least 15 minutes before breakfast. The dose may be increased to 20 mg once daily if needed, based on blood pressure response. The maximum recommended dose is 20 mg per day.
Children:
Lercanidipine is not recommended for use in children under 18 years of age as safety and efficacy have not been established.
Special Cases:
- Elderly Patients: No initial dose adjustment is typically required, but special care should be taken when initiating treatment.
- Patients with Renal Impairment: Caution is needed in patients with mild to moderate renal impairment. Dosage increase to 20 mg should be approached cautiously. Contraindicated in severe renal impairment (GFR < 30 mL/min).
- Patients with Hepatic Dysfunction: Caution is needed in patients with mild to moderate hepatic impairment. Dosage increase to 20 mg should be considered cautiously. Contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Dosage adjustments may be needed for patients with certain comorbid conditions (e.g., heart failure). Consult specialized resources for specific recommendations.
Clinical Use Cases
Lercanidipine’s primary clinical use is for chronic hypertension management. It is not typically used in acute settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like cardiac arrest. Other medications are more suitable for rapid blood pressure control in these scenarios.
Dosage Adjustments
Dosage adjustments are based on patient response to therapy and may be needed for patients with renal or hepatic impairment. Close monitoring of blood pressure and potential side effects is essential. Genetic polymorphisms affecting CYP3A4 activity may influence drug metabolism and require individualised dosing.
Side Effects
Common Side Effects:
- Headache
- Dizziness
- Flushing
- Peripheral edema (swelling of ankles and feet)
- Palpitations
- Fatigue
Rare but Serious Side Effects:
- Hypotension
- Angina
- Myocardial infarction
- Allergic reactions (rash, itching, angioedema)
Long-Term Effects:
Long-term use can potentially exacerbate pre-existing cardiovascular conditions if not adequately monitored.
Adverse Drug Reactions (ADR):
Clinically significant ADRs requiring immediate attention are rare but include severe hypotension, allergic reactions, and signs of myocardial ischemia.
Contraindications
- Hypersensitivity to lercanidipine or other dihydropyridines.
- Severe hepatic impairment.
- Severe renal impairment (GFR < 30 mL/min).
- Left ventricular outflow obstruction.
- Untreated congestive heart failure.
- Unstable angina.
- Recent myocardial infarction (within 1 month).
- Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir) or cyclosporine.
- Pregnancy and breastfeeding (unless benefits outweigh risks).
Drug Interactions
- CYP3A4 Inhibitors: Increase lercanidipine levels and risk of side effects.
- CYP3A4 Inducers: Decrease lercanidipine levels and efficacy.
- Cyclosporine: Increases levels of both drugs.
- Grapefruit Juice: Increases lercanidipine levels and hypotensive effect.
- Alcohol: Can potentiate the hypotensive effect.
- Other antihypertensive medications: Additive hypotensive effects.
- Digoxin, simvastatin, beta-blockers: Monitor for potential interactions.
Pregnancy and Breastfeeding
Lercanidipine should be avoided during pregnancy and breastfeeding unless the potential benefits outweigh the risks. It is unknown if lercanidipine is excreted in breast milk. If use is necessary, discuss alternative medications with the patient.
Drug Profile Summary
- Mechanism of Action: Calcium channel blocker (dihydropyridine), causes vasodilation.
- Side Effects: Headache, dizziness, flushing, peripheral edema, palpitations.
- Contraindications: Hypersensitivity, severe hepatic/renal impairment, certain cardiovascular conditions, CYP3A4 inhibitor/cyclosporin use.
- Drug Interactions: CYP3A4 inhibitors/inducers, cyclosporine, grapefruit juice, alcohol.
- Pregnancy & Breastfeeding: Avoid unless benefits outweigh risks.
- Dosage: 10-20 mg once daily.
- Monitoring Parameters: Blood pressure, heart rate, signs of peripheral edema, liver/kidney function tests if indicated.
Popular Combinations
Lercanidipine can be combined with other antihypertensive agents like beta-blockers (e.g., atenolol), diuretics (e.g., hydrochlorothiazide), or ACE inhibitors (e.g., enalapril, captopril) for enhanced blood pressure control when monotherapy is insufficient.
Precautions
- Assess renal and hepatic function before and during treatment, especially in elderly patients.
- Monitor blood pressure regularly.
- Caution patients about potential for dizziness and orthostatic hypotension.
- Advise patients to avoid grapefruit juice and alcohol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Lercanidipine?
A: The initial dose is 10 mg once daily, taken orally at least 15 minutes before a meal. This can be increased to 20mg if blood pressure is not adequately controlled.
Q2: How does Lercanidipine differ from other calcium channel blockers?
A: Lercanidipine has high vascular selectivity, leading to fewer cardiac side effects compared to some other calcium channel blockers. It also has a longer half-life, allowing for once-daily dosing.
Q3: Can Lercanidipine be used in patients with diabetes?
A: Yes, lercanidipine can be used cautiously in patients with diabetes. It has shown renal protective effects in some studies. Blood glucose levels should be monitored.
Q4: What are the most important drug interactions to consider?
A: Strong CYP3A4 inhibitors (like ketoconazole, itraconazole, ritonavir), cyclosporine, and grapefruit juice can significantly increase lercanidipine levels. CYP3A4 inducers (like rifampicin, phenytoin) can reduce its effectiveness.
Q5: Can Lercanidipine be used in pregnant or breastfeeding women?
A: Lercanidipine should generally be avoided during pregnancy and breastfeeding unless the potential benefits clearly outweigh the risks. Consult specialist resources and discuss alternatives with the patient.
Q6: What should be done if a patient misses a dose?
A: The patient should take the missed dose as soon as they remember, unless it’s close to the time of the next dose. They should not double the dose.
Q7: How should Lercanidipine be administered?
A: Lercanidipine is administered orally, typically once a day, at least 15 minutes before a meal. Tablets should be swallowed whole with water.
Q8: What are the signs of Lercanidipine overdose?
A: Overdose can cause severe hypotension, reflex tachycardia, and potentially other cardiovascular complications. Supportive care and symptomatic treatment are indicated.
Q9: What are the monitoring parameters for patients on Lercanidipine?
A: Regularly monitor blood pressure, heart rate, and look for signs of peripheral edema. Monitor renal and hepatic function, especially in patients with pre-existing impairment.
