Lercanidipine

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Lercanidipine on Prescriptsy

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Lercanidipine is a prescription-only medicine used to treat high blood pressure (hypertension).

It belongs to the dihydropyridine class of calcium channel blockers (CCBs) and is sometimes described as a third-generation CCB because of its distinct pharmacological properties.

Lercanidipine is available as 10 mg and 20 mg film-coated tablets and is taken once daily.

It is widely used in UK general practice, particularly for patients who have experienced peripheral oedema (ankle swelling) with other calcium channel blockers such as amlodipine, as lercanidipine produces significantly less of this troublesome side effect.

Hypertension is one of the most important modifiable risk factors for cardiovascular disease.

According to the British Heart Foundation, approximately one in three adults in the United Kingdom has high blood pressure, though many are unaware because the condition rarely causes symptoms until organ damage has occurred.

Untreated hypertension increases the risk of stroke, myocardial infarction, heart failure, chronic kidney disease, peripheral arterial disease, and vascular dementia.

Effective treatment with antihypertensive medicines, combined with lifestyle modifications, substantially reduces these risks.

This page provides a thorough clinical overview of lercanidipine, including how it works, how it compares with other blood pressure treatments, dosage guidance, side effects, important warnings, and how to obtain it in the UK.

Important safety information about lercanidipine

Before reading further, note these essential safety points about lercanidipine.

• Lercanidipine is a prescription-only medicine and must be used under medical supervision.
• Take lercanidipine at least 15 minutes before food. Food significantly increases absorption and can cause excessive blood pressure lowering.
• Do not eat grapefruit or drink grapefruit juice during treatment, as this increases drug levels in the blood.
• Do not take lercanidipine with other calcium channel blockers or strong CYP3A4 inhibitors.
• Report persistent dizziness, severe ankle swelling, chest pain, or palpitations to your prescriber.

Understanding hypertension

Blood pressure is the force exerted by circulating blood on the walls of the arteries.

It is measured in millimetres of mercury (mmHg) and recorded as two values: systolic (when the heart contracts) over diastolic (when the heart relaxes between beats).

NICE guideline NG136 defines hypertension as a clinic reading of 140/90 mmHg or above, confirmed by ambulatory or home monitoring showing an average of 135/85 mmHg or above.

Hypertension is classified into stages: Stage 1 (140/90 to 159/99 mmHg), Stage 2 (160/100 to 179/119 mmHg), and Stage 3 or severe hypertension (180/120 mmHg or above, requiring urgent assessment).

Most cases are primary (essential) hypertension with no single identifiable cause.

Secondary hypertension, caused by conditions such as renal artery stenosis, primary aldosteronism, or phaeochromocytoma, accounts for a smaller proportion and is typically investigated when hypertension is resistant to treatment or presents in younger patients.

NICE recommends a stepped approach to antihypertensive treatment.

Step 1 for patients aged 55 and over, or patients of Black African or African-Caribbean descent at any age, is a calcium channel blocker or a thiazide-like diuretic.

For patients under 55 (not of Black African or African-Caribbean descent), an ACE inhibitor or ARB is first-line.

Lercanidipine is an appropriate calcium channel blocker option at any step where a CCB is indicated.

How lercanidipine works: mechanism of action

Lercanidipine selectively blocks L-type voltage-gated calcium channels in vascular smooth muscle cells.

Calcium influx through these channels is essential for smooth muscle contraction and the maintenance of vascular tone.

By inhibiting calcium entry, lercanidipine causes relaxation of arterial smooth muscle, arteriolar dilatation, and a reduction in total peripheral vascular resistance.

This lowers blood pressure without significantly affecting cardiac conduction, contractility, or venous tone at therapeutic doses.

The defining pharmacological characteristic of lercanidipine is its extreme lipophilicity.

The drug dissolves readily into the lipid bilayer of cell membranes, forming a membrane depot from which it is released slowly to interact with calcium channels over an extended period.

This accounts for its gradual onset of action (peak effect at 2 to 3 hours but sustained over 24 hours) and its smooth, prolonged blood pressure-lowering profile.

By contrast, first-generation dihydropyridines such as nifedipine immediate-release produced a rapid and pronounced blood pressure drop that triggered reflex sympathetic activation, causing tachycardia and flushing.

Lercanidipine avoids this because its slow receptor association and dissociation kinetics prevent abrupt haemodynamic changes.

The vascular selectivity of lercanidipine is approximately 100 times greater than its cardiac selectivity, meaning it dilates blood vessels without significantly reducing cardiac contractility or slowing heart rate.

This is an advantage in patients who need blood pressure lowering without negative inotropic effects, particularly those with mildly impaired left ventricular function (though it is contraindicated in untreated heart failure).

Why lercanidipine causes less ankle oedema than amlodipine

Peripheral oedema is the most common reason patients discontinue dihydropyridine CCBs.

It occurs because arteriolar dilatation increases pre-capillary hydrostatic pressure while venular tone remains unchanged, driving fluid from the intravascular space into the interstitium.

With amlodipine (a second-generation CCB), ankle oedema has been reported in up to 10 to 15% of patients at the 10 mg dose.

Clinical trials have consistently demonstrated that lercanidipine produces significantly less peripheral oedema.

A randomised, double-blind, crossover study published in the Journal of Hypertension comparing lercanidipine 10 to 20 mg with amlodipine 5 to 10 mg found that ankle oedema occurred 2 to 3 times less frequently with lercanidipine at equivalent blood pressure-lowering doses.

This is thought to be because the gradual onset of vasodilatation with lercanidipine allows compensatory venular adjustments, reducing the capillary pressure imbalance.

Additionally, some data suggest that lercanidipine may have a more balanced effect on arteriolar and venular tone than amlodipine.

For patients who have discontinued or are reluctant to take amlodipine because of ankle swelling, lercanidipine represents a clinically valuable alternative that offers equivalent blood pressure reduction with substantially improved tolerability in this regard.

Clinical evidence and UK prescribing guidance

Lercanidipine has been evaluated in numerous clinical trials involving over 20,000 patients. These studies confirm its efficacy as an antihypertensive agent with a favourable tolerability profile.

A large observational study (the ELYPSE study) of over 9,000 patients treated with lercanidipine in routine clinical practice demonstrated significant reductions in both systolic and diastolic blood pressure, with a discontinuation rate due to adverse events of less than 1%.

NICE NG136 recommends calcium channel blockers as first-line therapy for certain patient groups and as add-on therapy in others.

Although the guideline does not specify individual CCBs by name, the BNF lists lercanidipine as an option alongside amlodipine, felodipine, lacidipine, and nifedipine modified-release.

In practice, lercanidipine is frequently chosen when amlodipine has been poorly tolerated due to ankle oedema, or when a CCB with a lower oedema profile is preferred from the outset.

Dosage and administration

The starting dose is 10 mg once daily, taken at least 15 minutes before food in the morning.

If blood pressure is not controlled after 2 to 4 weeks, the dose may be increased to 20 mg daily. The maximum dose is 20 mg.

Taking the tablet before food is important because fatty food significantly increases absorption and can cause an unpredictable blood pressure drop. Swallow the tablet whole with water.

Elderly patients should start at 10 mg daily, with cautious dose adjustment.

Mild to moderate renal impairment does not require dose reduction, but lercanidipine should be avoided in severe renal impairment.

In mild to moderate hepatic impairment, monitor blood pressure closely; the drug is contraindicated in severe liver disease.

Side effects of lercanidipine

Common side effects

Headache, flushing, dizziness, and palpitations are the most frequently reported effects. These are typically mild, transient, and related to the vasodilatory mechanism.

They are most likely at the start of treatment or following a dose increase and usually resolve within a few days to weeks.

Peripheral oedema

As discussed above, ankle swelling is possible but occurs significantly less often than with amlodipine. If oedema does develop, it is not dangerous but can be uncomfortable.

Your prescriber may reduce the dose, add an ACE inhibitor or ARB (which can help counteract CCB-related oedema by dilating venules as well as arterioles), or consider switching to a different antihypertensive class.

Uncommon and rare side effects

Gastrointestinal symptoms (nausea, dyspepsia), fatigue, muscle pain, skin rash, and increased urination occur uncommittedly. Gingival hyperplasia is very rare with lercanidipine.

Hypotension, angina, and allergic reactions (including angioedema) are rare. Lercanidipine does not adversely affect blood sugar, lipids, or uric acid.

When to seek urgent medical advice

Contact your GP or call NHS 111 if you experience persistent dizziness, significant ankle swelling, or palpitations.

Call 999 or attend A&E if you develop chest pain, swelling of the face or throat, difficulty breathing, or signs of a stroke (facial drooping, arm weakness, speech difficulty).

Report any suspected adverse reactions to the MHRA at yellowcard.mhra.gov.uk .

Warnings and precautions

Contraindications

Lercanidipine must not be used in untreated heart failure, unstable angina, within one month of a myocardial infarction, severe aortic stenosis, severe hepatic or renal impairment, or in patients taking strong CYP3A4 inhibitors or ciclosporin.

It must not be combined with other calcium channel blockers.

Drug interactions

CYP3A4 inhibitors increase lercanidipine levels. Avoid ketoconazole, itraconazole, ritonavir, and erythromycin. Grapefruit juice must be avoided. CYP3A4 inducers (rifampicin, carbamazepine, phenytoin) may reduce efficacy.

Beta-blockers can be combined but with blood pressure and heart rate monitoring. Digoxin levels should be monitored.

Cimetidine (but not ranitidine) may increase lercanidipine levels at doses above 800 mg daily.

Pregnancy and breastfeeding

Lercanidipine is not recommended in pregnancy. Women of childbearing potential should use effective contraception. Breastfeeding is not recommended during treatment. Alternative CCBs with more safety data in pregnancy (such as nifedipine modified-release) are available.

How to get lercanidipine in the UK

Lercanidipine is a prescription-only medicine available through the NHS.

Your GP or an authorised online prescriber registered with the General Pharmaceutical Council (GPhC) can prescribe it after an appropriate clinical assessment including blood pressure measurement.

The standard NHS prescription charge in England is currently 9.90 pounds per item; prescriptions are free in Scotland, Wales, and Northern Ireland. Generic lercanidipine is widely available.

Lifestyle advice for blood pressure management

Medication is most effective when combined with lifestyle changes. Reduce your salt intake to less than 6 g per day.

Eat a balanced diet rich in fruit, vegetables, wholegrains, and lean protein. Maintain a healthy weight.

Exercise regularly, aiming for at least 150 minutes of moderate-intensity activity per week. Limit alcohol to no more than 14 units per week. Stop smoking.

Manage stress through relaxation techniques, adequate sleep, and social support. Home blood pressure monitoring is encouraged by NICE and helps track the effectiveness of your treatment.

Sources

• Lercanidipine 10 mg Tablets, Summary of Product Characteristics (EMC)
• Lercanidipine hydrochloride, British National Formulary (BNF)
• NICE NG136: Hypertension in adults, diagnosis and management
• High blood pressure (hypertension), NHS
• MHRA Yellow Card Scheme