Schedule H

Oral

• Tablets: 5 mg, 10 mg, 20 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Essential Hypertension

Parameter Details

Starting dose 5–10 mg once daily (preferably after meals)

Titration Increase by 5–10 mg at intervals of 2–4 weeks based on BP response

Usual maintenance dose 10–20 mg once daily

Maximum dose 20 mg once daily

Key clinical notes Lower starting dose (5 mg) preferred in elderly, volume-depleted, or patients on concomitant antihypertensives. Dual L-type and N-type calcium channel blockade reduces reflex sympathetic activation. Particularly suitable in hypertension with proteinuric CKD or diabetes — evidence suggests reduced urinary albumin excretion compared to amlodipine.

Secondary Indications — Adults (Off-label)

Hypertension with Benign Prostatic Hyperplasia (OFF-LABEL)

• Dose: 10 mg once daily

• Duration: Chronic use with regular review

• Specialist only: Urology/Cardiology consultation advised

• Evidence basis: Small Indian trials suggest modest improvement in lower urinary tract symptoms (LUTS) in hypertensive men with BPH; N-type channel blockade may reduce sympathetic tone to prostatic smooth muscle

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Not applicable — Cilnidipine is not approved for use in patients below 18 years of age. Safety and efficacy data in the paediatric population are not established.

Secondary Indications — Paediatrics (Off-label)

Not applicable — No standardised paediatric dosing available. Use in children not recommended.

Age restriction statement: Not recommended below 18 years except under paediatric cardiologist or nephrologist supervision in exceptional circumstances.

Clinical note: Cilnidipine is preferred in CKD with proteinuria in Indian nephrology practice due to N-type channel blockade reducing efferent arteriolar tone and potentially lowering intraglomerular pressure.

• Known hypersensitivity to cilnidipine or other dihydropyridine calcium channel blockers

• Severe hypotension (systolic BP <90 mmHg)

• Cardiogenic shock

• Acute myocardial infarction with haemodynamic instability

• Severe aortic stenosis

• Unstable angina

• Heart failure with reduced ejection fraction — may worsen oedema; use with caution

• Hepatic impairment — increased risk of hypotension

• Elderly patients — increased susceptibility to orthostatic hypotension

• Patients on multiple antihypertensives — cumulative hypotensive effect

• Peripheral oedema — may require dose reduction or switch to alternative agent

• Concurrent use with strong CYP3A4 inhibitors or inducers

Parameter Details

Safety status Not established; avoid unless clearly necessary

Risk Animal studies suggest potential fetal risk; human data insufficient

Preferred alternatives Labetalol, nifedipine (extended-release), methyldopa — extensively studied in pregnancy hypertension

When may be used Only if alternatives contraindicated and benefit clearly outweighs risk; specialist obstetric input required

Monitoring Maternal BP, fetal growth (serial ultrasound), uteroplacental Doppler if prolonged use

Parameter Details

Compatibility Unknown; use with caution

Expected levels in milk Likely low (based on lipophilicity and protein binding), but no specific human data

Preferred alternatives Amlodipine or nifedipine (more safety data available in breastfeeding)

Infant monitoring If used, monitor infant for adequate feeding, sedation, weight gain, and signs of hypotension

• Recommended starting dose: 5 mg once daily

• Titration: Slow; increase at 4-week intervals based on BP response

• Additional risks: Increased risk of orthostatic hypotension, dizziness, falls, and syncope. May have reduced hepatic metabolism.

• Monitoring: Regular BP monitoring (including orthostatic BP); assess for ankle oedema and dizziness at each visit

Interacting Drug Effect / Mechanism Recommendation

Potent CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir) Increased cilnidipine plasma levels — excessive hypotension Avoid combination or reduce cilnidipine dose significantly; monitor BP closely

Strong CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital) Reduced cilnidipine efficacy Monitor BP; may require dose increase or alternative antihypertensive

Beta-blockers Additive negative chronotropic and hypotensive effects Use with caution; monitor HR and BP

Grapefruit juice CYP3A4 inhibition — increased drug levels Avoid concurrent consumption

Interacting Drug Effect / Mechanism Recommendation

NSAIDs (chronic use) May attenuate antihypertensive effect via sodium and water retention Monitor BP; avoid prolonged NSAID use

Diuretics Additive hypotensive effect; volume depletion Monitor for symptomatic hypotension

Simvastatin (>20 mg) Potential CYP3A4 interaction increasing statin levels Prefer atorvastatin or rosuvastatin

Other antihypertensives Cumulative BP lowering Monitor for excessive hypotension

Digoxin Possible increase in digoxin levels Monitor digoxin levels if used concomitantly

Cimetidine CYP3A4 inhibition — mild increase in cilnidipine levels Monitor BP

• Headache

• Dizziness

• Flushing

• Peripheral oedema (less frequent than amlodipine)

• Palpitations

• Fatigue

• Nausea

• Severe hypotension or syncope — usually with overdose or rapid dose escalation; requires discontinuation

• Symptomatic bradycardia (rare; related to N-type channel effect)

• Elevated hepatic transaminases — discontinue if significant

• Gingival hyperplasia (rare with long-term use)

• Hypersensitivity reactions including rash, angioedema (rare)

After initiation/dose change BP monitoring weekly for 2–4 weeks; assess for oedema and dizziness

Long-term BP and heart rate at each visit; renal function and LFTs every 6–12 months; ankle oedema assessment

Single-ingredient formulations:

• Cilacar® (J.B. Chemicals / Jubilant)

• Cilday® (Zydus Cadila)

• Cinod® (Ajanta Pharma)

• Cilnidip® (Micro Labs)

• Cilnikem® (Alkem)

• Cilaheart® (Lupin)

Common Fixed-Dose Combinations (FDCs):

• Not currently listed under NLEM; prices not NPPA-controlled

• Wide price variation across brands

1. Dual channel blockade advantage: Cilnidipine inhibits both L-type (vascular) and N-type (neuronal) calcium channels, resulting in less reflex tachycardia and reduced sympathetic overactivity compared to amlodipine.

1. Lower oedema incidence: Indian comparative studies indicate cilnidipine causes significantly less pedal oedema than amlodipine — consider switching from amlodipine in patients with troublesome ankle swelling.

1. CKD preference: Useful in hypertensive patients with proteinuria or diabetic nephropathy — N-type blockade may reduce efferent arteriolar pressure and urinary albumin excretion.

1. Timing of administration: Administer after meals for optimal absorption.

1. Avoid abrupt discontinuation: In patients on long-term therapy, gradual dose reduction preferred to prevent rebound hypertension.

1. Not for acute BP lowering: Onset of action is gradual; not suitable for hypertensive emergencies.

hypertension; calcium channel blocker; CCB; L/N-type blocker; CKD-friendly; low oedema; cilnidipine India; diabetic nephropathy; proteinuria

RxIndia v1.0 — 11 Jun 2025

• CDSCO approved product inserts (Cilacar®, Cinod®)

• Indian Pharmacopoeia 2018

• API Textbook of Medicine, 10th & 11th Editions

• ICMR Guidelines on Hypertension Management (2021)

• AIIMS Hypertension Treatment Protocol

• Indian Society of Nephrology — CKD management recommendations

• Indian RCTs: cilnidipine vs amlodipine in diabetic nephropathy and essential hypertension (supportive evidence for oedema and proteinuria outcomes)