Schedule H

Oral

• Tablets: 10 mg, 20 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Essential Hypertension (Mild to Moderate)

Parameter Details

Starting dose 10 mg once daily, taken 15–30 minutes before a meal (preferably morning)

Titration May increase to 20 mg once daily after minimum 2 weeks if BP control inadequate

Usual maintenance dose 10–20 mg once daily

Maximum dose 20 mg once daily (higher doses do not improve efficacy but increase adverse effects)

Key clinical notes Must be taken on empty stomach — high-fat meals reduce bioavailability by approximately 70%. Third-generation DHP-CCB with high vascular selectivity and lipophilicity resulting in gradual onset and prolonged duration of action. Lower incidence of peripheral oedema compared to amlodipine.

Secondary Indications — Adults (Off-label)

Raynaud's Phenomenon (OFF-LABEL)

• Dose: 10–20 mg once daily

• Duration: Symptom-dependent; typically continued through cold months

• Specialist only: Rheumatology input recommended

• Evidence basis: Extrapolated from established efficacy of other dihydropyridine CCBs; limited direct evidence for lercanidipine specifically

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Not applicable — Lercanidipine is not approved for use in patients below 18 years. Safety and efficacy have not been established in the paediatric population.

Secondary Indications — Paediatrics (Off-label)

Not applicable — No paediatric dosing data available.

Age restriction statement: Not recommended below 18 years. Other antihypertensives with established paediatric safety profiles (e.g., amlodipine, enalapril) should be used in children requiring CCB therapy.

• Known hypersensitivity to lercanidipine or other dihydropyridine CCBs

• Severe hepatic impairment

• Untreated or uncontrolled heart failure

• Unstable angina pectoris

• Within 1 month of acute myocardial infarction

• Severe aortic stenosis

• Left ventricular outflow tract obstruction (including hypertrophic obstructive cardiomyopathy)

• Concurrent use with strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, nelfinavir)

• Concurrent use with ciclosporin

• Pregnancy and lactation

• Mild to moderate hepatic impairment — reduced clearance may increase drug levels

• Mild to moderate renal impairment — monitor closely

• Sick sinus syndrome (if pacemaker not in situ)

• Elderly patients — increased susceptibility to hypotension

• Patients with stable angina — may rarely precipitate or worsen angina, especially at initiation

• Concurrent use with moderate CYP3A4 inhibitors

• Avoid grapefruit juice consumption — significant CYP3A4 inhibition increases plasma levels

• Concomitant use with other antihypertensives — additive hypotensive effects

Parameter Details

Safety status Contraindicated — insufficient human data; animal studies show fetotoxicity

Risk Potential teratogenic and fetotoxic effects based on animal data

Preferred alternatives Labetalol, methyldopa, nifedipine (extended-release) — established safety in pregnancy

When may be used Not recommended at any stage of pregnancy

Monitoring If inadvertent exposure in early pregnancy: detailed fetal anomaly scan; specialist obstetric consultation

Parameter Details

Compatibility Contraindicated — excretion in human milk unknown; animal studies show milk excretion

Preferred alternatives Amlodipine, nifedipine — better established lactation safety data

Expected levels in milk Unknown in humans; likely present based on lipophilicity

Infant monitoring If unavoidable exposure, monitor infant for hypotension, poor feeding, lethargy

Recommendation Avoid breastfeeding or discontinue lercanidipine; formula feeding advised if drug essential

• Recommended starting dose: 10 mg once daily

• Titration: Increase cautiously; wait at least 2–4 weeks before considering dose escalation

• Additional risks: Increased susceptibility to hypotension, dizziness, and falls. Age-related decline in hepatic and renal function may reduce drug clearance.

• Monitoring: Orthostatic BP measurement; regular assessment for peripheral oedema and dizziness

Interacting Drug Effect / Mechanism Recommendation

Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, nelfinavir) Marked increase in lercanidipine plasma levels — risk of severe hypotension Contraindicated; avoid combination

Ciclosporin Mutual increase in plasma levels of both drugs Contraindicated; do not co-administer

Grapefruit juice CYP3A4 inhibition — substantially increases bioavailability Avoid grapefruit consumption during treatment

Other dihydropyridine CCBs Overlapping mechanism; additive effects Avoid concurrent use

Interacting Drug Effect / Mechanism Recommendation

Moderate CYP3A4 inhibitors (erythromycin, fluconazole, diltiazem) Increased lercanidipine levels Use with caution; monitor BP closely

CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital) Reduced lercanidipine efficacy Monitor BP; dose adjustment or alternative antihypertensive may be needed

Beta-blockers Additive negative inotropic and hypotensive effects Monitor for excessive BP lowering and bradycardia

Other antihypertensives Cumulative hypotensive effect Monitor BP; adjust doses as needed

Digoxin Mild increase in digoxin levels Monitor digoxin levels if high-dose digoxin used

Alcohol Enhanced hypotensive effect Counsel regarding moderation

Simvastatin Possible CYP3A4-mediated interaction Monitor for statin-related adverse effects

Midazolam Increased midazolam exposure Use lower midazolam doses; monitor for sedation

• Headache

• Flushing

• Peripheral oedema (less common than with amlodipine)

• Dizziness

• Palpitations

• Fatigue

• Asthenia

• Symptomatic hypotension or syncope — discontinue or reduce dose

• Angina exacerbation or new-onset chest pain — requires evaluation and possible discontinuation

• Significant hepatic transaminase elevation — monitor LFTs; discontinue if persistent

• Allergic skin reactions (urticaria, rash) — discontinue if severe

• Gingival hyperplasia (rare, with long-term use)

After initiation/dose change BP at 1–2 weeks; assess for peripheral oedema, dizziness, angina

Long-term BP at each visit; LFTs periodically (6–12 monthly); ankle oedema assessment; renal function annually

Single-ingredient formulations:

• Zanidip® (Menarini / Berlin Pharma)

• Lercadip® (Abbott)

• Cardilec® (USV)

• Lecardion® (Macleods)

• Lercasmart® (Micro Labs)

• Lerka® (Glenmark)

• Lernipin® (Intas)

Common Fixed-Dose Combinations (FDCs):

• Lercanidipine + Atenolol

• Not listed under NLEM; private market pricing applies

• Considerable inter-brand price variation

1. Empty stomach administration is critical: Bioavailability drops by up to 70% when taken with high-fat meals. Counsel patients to take 15–30 minutes before breakfast.

1. Lower oedema risk than amlodipine: Third-generation DHP with preferential precapillary arteriolar dilation reduces hydrostatic pressure and oedema formation — useful alternative in patients intolerant to amlodipine due to ankle swelling.

1. CYP3A4-sensitive drug: Strictly avoid concomitant strong CYP3A4 inhibitors and ciclosporin. Counsel against grapefruit juice consumption.

1. Avoid in unstable cardiac conditions: Contraindicated within 1 month of MI or in uncontrolled heart failure; may worsen angina in some patients.

1. Gradual onset: Due to high lipophilicity and membrane binding, onset is gradual and sustained — not suitable for acute BP reduction.

1. Switching from amlodipine: When switching due to oedema, can initiate lercanidipine 10 mg and titrate; oedema often resolves within 2–4 weeks.

hypertension; calcium channel blocker; dihydropyridine; third-generation CCB; low oedema; CYP3A4 substrate; hepatic-avoid; pregnancy-contraindicated; elderly-caution

RxIndia v1.0 — 11 Jun 2025

• CDSCO approved product inserts (Zanidip®, Lercadip®)

• Indian Pharmacopoeia

• National Formulary of India 2021

• API Textbook of Medicine, 11th Edition

• AIIMS Drug Formulary

• Goodman & Gilman's The Pharmacological Basis of Therapeutics, 13th Edition

• Menarini India prescribing information

• International RCTs for Raynaud's phenomenon (supportive, off-label use)