Schedule H

Oral

• Tablets: 5 mg

• Oral Solution/Syrup: 2.5 mg/5 mL

• Fixed-Dose Combinations: Levocetirizine 5 mg + Montelukast 10 mg tablets (available)

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Allergic Rhinitis (Seasonal and Perennial)

Adults:

Parameter Recommendation

Starting dose 5 mg once daily, preferably in the evening

Titration Not required

Usual maintenance dose 5 mg once daily

Maximum dose 5 mg/day

Clinical Notes:

• Symptom relief typically begins within 1 hour of administration

• Duration of action approximately 24 hours

• Reassess need periodically; consider intermittent use for seasonal symptoms

• Evening dosing preferred due to circadian variation in histamine release and potential mild sedation

1. Chronic Idiopathic Urticaria (Chronic Spontaneous Urticaria)

Adults:

Parameter Recommendation

Starting dose 5 mg once daily

Titration Not usually required at standard doses

Usual maintenance dose 5 mg once daily

Maximum dose 5 mg/day (licensed); up to 10 mg/day under specialist care

Clinical Notes:

• Assess disease activity and continued need every 3–6 months

• Minimum 2–4 weeks trial before assessing efficacy

• May be used in combination with other antihistamines under dermatologist guidance

Secondary Indications – Adults Only (Off-label)

Indication Dose Duration Notes Evidence Basis

Refractory Chronic Urticaria Up to 10 mg/day (may divide into 5 mg twice daily) Individualised; reassess every 4–6 weeks OFF-LABEL; Specialist only International consensus guidelines (EAACI); Indian dermatology specialist practice

Allergic Pruritus (non-urticarial) 5 mg once daily Symptomatic; short-term preferred OFF-LABEL Indian physician experience; symptomatic management

Atopic Dermatitis (adjunctive for pruritus) 5 mg once daily As needed for symptom control OFF-LABEL; Adjunctive only Limited evidence; used in Indian dermatology practice for nocturnal pruritus relief

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Indications: Allergic Rhinitis and Chronic Urticaria

6 months – 2 years 1.25 mg once daily Oral solution (2.5 mL of 2.5 mg/5 mL) Minimum approved age in India; use calibrated measuring device

2 – 5 years 1.25 mg twice daily OR 2.5 mg once daily Oral solution preferred Administer in evening if once daily

6 – 11 years 2.5 mg once daily; may increase to 5 mg once daily based on response Oral solution or tablet (if able to swallow) Assess severity before dose escalation

≥12 years 5 mg once daily Tablet or oral solution Adult dosing applies

Safety Monitoring in Children:

• Monitor for sedation, paradoxical excitation, or behavioural changes

• Assess renal function in children with known renal impairment before initiating

• Watch for irritability or sleep disturbances, particularly in infants

Age Restriction Statement:

Not recommended below 6 months of age. Use in infants 6 months to 2 years should be under specialist supervision only.

Secondary Indications – Paediatrics (Off-label)

Not routinely used off-label in Indian paediatric practice beyond approved indications.

Notes:

• Approximately 85% excreted unchanged via kidneys

• Not significantly removed by haemodialysis; supplemental dosing not required post-dialysis

• Paediatric renal dosing: reduce proportionally; specialist input recommended

Notes:

• Levocetirizine undergoes minimal hepatic metabolism

• Formal pharmacokinetic studies lacking in severe hepatic disease

• Monitor for increased sedation in patients with hepatic encephalopathy

• Known hypersensitivity to levocetirizine, cetirizine, hydroxyzine, or any formulation excipients

• End-stage renal disease (eGFR <10 mL/min/1.73 m²)

• Patients on dialysis

• Children under 6 months of age

• Paediatric patients with significant renal impairment (use contraindicated due to lack of appropriate dosing data)

• Moderate renal impairment (CKD Stage 3): requires dose reduction

• History of urinary retention or prostatic hypertrophy: may exacerbate symptoms

• Pre-existing seizure disorders: rare reports of seizure exacerbation

• Concurrent use of CNS depressants: additive sedation risk

• Elderly patients: increased sensitivity to sedation and anticholinergic-like effects

• Occupational hazard: advise caution when driving or operating machinery until individual response known

Parameter Details

Risk Category Not formally classified in India; limited human data available

Overall Safety Animal studies show no teratogenicity; human data insufficient for definitive safety

Recommendation Use only if clearly needed and benefit outweighs potential risk

Preferred Alternatives Chlorpheniramine (first-generation; more safety data in pregnancy), Loratadine

Trimester Considerations Avoid in first trimester if possible; may use in second/third trimester if necessary

Monitoring Monitor for maternal sedation; no specific fetal monitoring required unless high doses used

Parameter Details

Breastfeeding Compatibility Likely compatible; excreted in breast milk in low concentrations

Milk Levels Low (based on cetirizine data; levocetirizine is the active enantiomer)

Preferred Alternatives Loratadine or cetirizine (more breastfeeding safety data available)

Infant Monitoring Observe for drowsiness, irritability, poor feeding, or changes in sleep pattern

Recommendation May use if antihistamine required; prefer single evening dose to minimise infant exposure

Parameter Recommendation

Starting dose 2.5 mg once daily

Titration Increase to 5 mg only if tolerated and required

Special Considerations Assess renal function before prescribing; eGFR-based dosing mandatory

Monitoring Monitor for sedation, dizziness, confusion, urinary retention

Fall Risk Increased; counsel patient and caregivers

Cognitive Effects Less anticholinergic burden than first-generation antihistamines; still monitor

Interacting Drug/Class Effect Management

Alcohol Enhanced CNS depression; increased sedation and impaired psychomotor function Avoid concurrent use

Benzodiazepines and other CNS depressants Additive sedation Avoid combination or use with extreme caution; dose reduction may be needed

Opioid analgesics Potentiation of sedation and respiratory depression Monitor closely; consider dose adjustment

Interacting Drug/Class Effect Management

Anticholinergic drugs (e.g., tricyclic antidepressants, antimuscarinics) Increased risk of urinary retention, dry mouth, constipation Monitor symptoms, especially in elderly

Ritonavir May modestly increase levocetirizine levels via reduced renal clearance Monitor for increased side effects

Theophylline (high doses) Slight reduction in levocetirizine clearance reported Clinical significance minimal; monitor if concerns

Other antihistamines Additive effects without additional benefit at standard doses Avoid unnecessary combination except under specialist guidance

• Somnolence (more common in first few days of treatment)

• Dry mouth

• Fatigue

• Headache

• Pharyngitis/nasopharyngitis (particularly in paediatric patients)

• Abdominal pain (children)

Adverse Effect Notes

Hypersensitivity reactions (including anaphylaxis) Very rare; discontinue immediately if suspected

Seizures Rare; reported mainly in paediatric patients or those with predisposition

Acute urinary retention Rare; more likely in elderly males with prostatic hypertrophy

Aggressive behaviour, agitation, hallucinations Rare; mainly reported in children; discontinue if occurs

Fixed drug eruption Rare; documented in case reports

Suicidal ideation Very rare; monitor in susceptible individuals

Timing Parameter

Baseline Serum creatinine and eGFR (mandatory in elderly, renal disease, children with suspected renal impairment)

After initiation Assess for sedation, dizziness, and symptom control at 1–2 weeks

Long-term use Reassess need for continued therapy every 3–6 months; annual renal function in elderly or those at risk

Paediatric Monitor growth, behaviour, and sleep patterns

• Xyzal (UCB)

• Levocet (Cipla)

• LCZ (Torrent)

• Lezyncet (Sun Pharma)

• Vozet (Lupin)

• Livozit (FDC Ltd)

• Cetcip-L (Cipla)

• Alerid-L (Aristo)

• Okacet-L (Zydus)

Fixed-Dose Combinations:

NLEM Status: Cetirizine (racemic form) included in NLEM 2022; price ceiling under NPPA applicable to cetirizine formulations. Levocetirizine not directly listed but market pricing remains competitive.

1. Evening administration is preferred as it aligns with peak nocturnal histamine release and mitigates any residual sedation during waking hours.

1. Renal function assessment is essential before prescribing, particularly in elderly patients where age-related decline in GFR is common but often unrecognised.

1. Dose escalation to 10 mg/day in refractory urticaria is an established off-label practice in dermatology; always document rationale and obtain informed consent.

1. Safer long-term profile compared to first-generation antihistamines due to minimal anticholinergic activity and lower CNS penetration.

1. Paradoxical reactions in children (excitation, irritability, insomnia) are uncommon but recognised; counsel parents and consider dose reduction or alternative if this occurs.

1. Not interchangeable with cetirizine on a milligram-for-milligram basis; levocetirizine 5 mg is therapeutically equivalent to cetirizine 10 mg.

levocetirizine; antihistamine; H1-blocker; allergic rhinitis; chronic urticaria; non-sedating antihistamine; renal adjustment; paediatric-safe; dermatology; NLEM India

RxIndia v1.1 — 10 Jan 2025

• CDSCO approved product inserts (Indian manufacturers)

• Indian Pharmacopoeia 2022

• National List of Essential Medicines (NLEM) 2022

• API Textbook of Medicine (24th Edition)

• IAP Drug Formulary 2021

• AIIMS Standard Treatment Guidelines

• IADVL (Indian Association of Dermatologists, Venereologists and Leprologists) treatment recommendations

• WHO Model Formulary (supportive reference for paediatric dosing)