THE INDIAN PHARMACIST Official Circular Pharmacy Logo THE INDIAN PHARMACISTLearn. Explore. Practise. Excel.
MEDICINE MONOGRAPH CODE: [9.9] ID: TIP-MED-000173

Levocetirizine, Cetirizine & Chlorpheniramine Maleate (Oral H1 Antihistamines)

Active Ingredient / Scientific Identity: Levocetirizine, Cetirizine & Chlorpheniramine Maleate • Class: Histamine H1-Receptor Inverse Agonists (Second-Generation Non-Sedating/Minimally Sedating vs. First-Generation Sedating Antihistamines)

⚖️ Compare Profile
THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Levocetirizine, Cetirizine & Chlorpheniramine Maleate (Oral H1 Antihistamines) ([9.9] | ID: TIP-MED-000173) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/9-9-levocetirizine-cetirizine-chlorpheniramine-maleate-oral-h1-antihistamines/
Generic / Entity NameLevocetirizine, Cetirizine & Chlorpheniramine Maleate (Oral H1 Antihistamines) ([9.9])
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassHistamine H1-Receptor Inverse Agonists (Second-Generation Non-Sedating/Minimally Sedating
Available Dosage FormsLevocetirizine Tablets: 5 mg (Syrup 2.5 mg/5 mL); Cetirizine Tablets: 10 mg (Syrup 5 mg/5 mL); Fexofenadine Ta
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal: Strictly renal-function dependent for Cetirizine & Levocetirizine (excreted >70–85% unchanged in urine)! • CrCl 30–49
Reviewed: 2026-11-10
Safety Matrix:⚖️ Legal Status: Schedule H Prescription Drug (To be sold by retail o✔️ Standard Clinical Dispensing Precautions

1. Clinical & Scientific Overview

Levocetirizine, Cetirizine & Chlorpheniramine Maleate (Oral H1 Antihistamines) (TIP-MED-000173, Reference Code [9.9]) is classified under Respiratory, Asthma, COPD & Allergy Medicines (Ch 09) as a Histamine H1-Receptor Inverse Agonists (Second-Generation Non-Sedating/Minimally Sedating vs. First-Generation Sedating Antihistamines). Within the Indian regulatory and compendial framework, it is governed under Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945).

Verified Indian Market Examples / Compendial Status:
Representative Indian Market Examples (Edition 2.7 Ch 09 [9.9], p. 118): • Levocetirizine (5 mg): Xyzal (Dr. Reddy's), Levocet (Hetero), Vozet, Tecori. • Cetirizine (10 mg): Cetzine (GSK/Dr. Reddy's), Okacet (Cipla), Alerid (Cipla), Zyrtec. • Fexofenadine (120 mg, 180 mg): Allegra (Sanofi), Fexova, Altiva. • Bilastine (20 mg): Bilagra, Ilaxten, Bilazest. • First-Gen Sedating (Avoid in Elderly!): Chlorpheniramine Maleate [CPM 4 mg - Piriton, Cadistin], Hydroxyzine [Atarax 10/25 mg], Pheniramine [Avil 25/50 mg], Cyproheptadine [Practin 4 mg] — Strengths & Dosage Forms: Levocetirizine Tablets: 5 mg (Syrup 2.5 mg/5 mL); Cetirizine Tablets: 10 mg (Syrup 5 mg/5 mL); Fexofenadine Tablets: 120 mg (Allergic Rhinitis), 180 mg (Chronic Urticaria); Bilastine Tablets: 20 mg, 40 mg; CPM Tablets: 4 mg
Representative Indian Market Examples (Edition 2.7 Ch 09 [9.9], p. 118): • Levocetirizine (5 mg): Xyzal (Dr. Reddy's), Levocet (Hetero), Vozet, Tecori. • Cetirizine (10 mg): Cetzine (GSK/Dr. Reddy's), Okacet (Cipla), Alerid (Cipla), Zyrtec. • Fexofenadine (120 mg, 180 mg): Allegra (Sanofi), Fexova, Altiva. • Bilastine (20 mg): Bilagra, Ilaxten, Bilazest. • First-Gen Sedating (Avoid in Elderly!): Chlorpheniramine Maleate [CPM 4 mg - Piriton, Cadistin], Hydroxyzine [Atarax 10/25 mg], Pheniramine [Avil 25/50 mg], Cyproheptadine [Practin 4 mg] — Strengths & Dosage Forms: Levocetirizine Tablets: 5 mg (Syrup 2.5 mg/5 mL); Cetirizine Tablets: 10 mg (Syrup 5 mg/5 mL); Fexofenadine Tablets: 120 mg (Allergic Rhinitis), 180 mg (Chronic Urticaria); Bilastine Tablets: 20 mg, 40 mg; CPM Tablets: 4 mg
Dosage Forms & Available Strengths:
Levocetirizine Tablets: 5 mg (Syrup 2.5 mg/5 mL); Cetirizine Tablets: 10 mg (Syrup 5 mg/5 mL); Fexofenadine Tablets: 120 mg (Allergic Rhinitis), 180 mg (Chronic Urticaria); Bilastine Tablets: 20 mg, 40 mg; CPM Tablets: 4 mg
Routes: Oral / Parenteral / Topical as specified by formulation

3. Mechanism of Action & Pharmacodynamics

Histamine H1-Receptor Inverse Agonists (Second-Generation Non-Sedating/Minimally Sedating vs. First-Generation Sedating Antihistamines) acting on target receptor/enzyme pathways in Respiratory, Asthma, COPD & Allergy Medicines (Ch 09): clinical efficacy is mediated via Histamine H1-Receptor Inverse Agonists (Second-Generation Non-Sedating/Minimally Sedating vs. First-Generation Sedating Antihistamines) for Seasonal and perennial allergic rhinitis (sneezing, rhinorrhoea, nasal/ocular itching); acute and chronic idiopathic urticaria (hives), insect bites, and allergic contact/eczematous pruritus..

4. Therapeutic Indications & Evidence-Supported Uses

  • Seasonal and perennial allergic rhinitis (sneezing, rhinorrhoea, nasal/ocular itching)
  • acute and chronic idiopathic urticaria (hives), insect bites, and allergic contact/eczematous pruritus

🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.

5. Educational Dosage Context, Formulations & Administration

Educational Dosing & Regimen Summary: General Adult Reference: Levocetirizine: 5 mg once daily at bedtime. Cetirizine: 10 mg once daily at bedtime (5 mg in elderly/renal impairment). Fexofenadine: 120 mg once daily (or 180 mg OD for urticaria). Bilastine: 20 mg once daily. Follow physician prescription.

Administration & Meal Timing: • Cetirizine / Levocetirizine / CPM: With or without food. • Fexofenadine (Allegra) & Bilastine: MUST be taken on an EMPTY STOMACH (1 hour BEFORE or 2 hours AFTER food or fruit juice) with plain water only! | Cetirizine / Levocetirizine: At bedtime (due to mild CNS penetration causing drowsiness in 10–15%). Fexofenadine / Bilastine: Morning or evening on an empty stomach (truly non-sedating—zero blood-brain barrier penetration via P-gp efflux!).

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Metabolism & Biotransformation:
Renal: Strictly renal-function dependent for Cetirizine & Levocetirizine (excreted >70–85% unchanged in urine)! • CrCl 30–49 mL/min: Reduce Levocetirizine to 5 mg every alternate day (or Cetirizine 5 mg OD). • CrCl 10–29 mL/min: Levocetirizine 5 mg twice weekly. • CrCl <10 mL/min (ESRD): Levocetirizine/Cetirizine are CONTRAINDICATED! (In severe CKD, Bilastine 20 mg OD requires no renal dose adjustment, or Fexofenadine 60 mg OD). Hepatic: Fexofenadine and Bilastine undergo minimal hepatic metabolism and are safe in liver disease.
Elimination & Renal Adjustment:
Renal: Strictly renal-function dependent for Cetirizine & Levocetirizine (excreted >70–85% unchanged in urine)! • CrCl 30–49 mL/min: Reduce Levocetirizine to 5 mg every alternate day (or Cetirizine 5 mg OD). • CrCl 10–29 mL/min: Levocetirizine 5 mg twice weekly. • CrCl <10 mL/min (ESRD): Levocetirizine/Cetirizine are CONTRAINDICATED! (In severe CKD, Bilastine 20 mg OD requires no renal dose adjustment, or Fexofenadine 60 mg OD). Hepatic: Fexofenadine and Bilastine undergo minimal hepatic metabolism and are safe in liver disease.
Hepatic Impairment Considerations:
Renal: Strictly renal-function dependent for Cetirizine & Levocetirizine (excreted >70–85% unchanged in urine)! • CrCl 30–49 mL/min: Reduce Levocetirizine to 5 mg every alternate day (or Cetirizine 5 mg OD). • CrCl 10–29 mL/min: Levocetirizine 5 mg twice weekly. • CrCl <10 mL/min (ESRD): Levocetirizine/Cetirizine are CONTRAINDICATED! (In severe CKD, Bilastine 20 mg OD requires no renal dose adjustment, or Fexofenadine 60 mg OD). Hepatic: Fexofenadine and Bilastine undergo minimal hepatic metabolism and are safe in liver disease.

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • First-Generation Antihistamines (CPM [Piriton], Pheniramine [Avil], Hydroxyzine [Atarax], Diphenhydramine [Benadryl], Cyproheptadine [Practin]) have potent Central Anticholinergic Activity and are contraindicated/avoided in Elderly Patients (Beers Criteria), Benign Prostatic Hyperplasia (BPH), Narrow-Angle Glaucoma, dementia, and asthma/COPD with thick inspissated sputum.

Key Clinical Precautions: Renal: Strictly renal-function dependent for Cetirizine & Levocetirizine (excreted >70–85% unchanged in urine)! • CrCl 30–49 mL/min: Reduce Levocetirizine to 5 mg every alternate day (or Cetirizine 5 mg OD). • CrCl 10–29 mL/min: Levocetirizine 5 mg twice weekly. • CrCl <10 mL/min (ESRD): Levocetirizine/Cetirizine are CONTRAINDICATED! (In severe CKD, Bilastine 20 mg OD requires no renal dose adjustment, or Fexofenadine 60 mg OD). Hepatic: Fexofenadine and Bilastine undergo minimal hepatic metabolism and are safe in liver disease.

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Cetirizine/Levocetirizine: Mild somnolence/drowsiness (10–14%), dry mouth, fatigue. First-Gen (CPM/Avil/Atarax): Marked daytime sedation, impaired driving/psychomotor coordination, severe dry mouth, blurred vision, constipation, urinary hesitancy. Fexofenadine/Bilastine: Headache (virtually zero sedation, equivalent to placebo!).
  • Acute Urinary Retention in elderly men with BPH (especially with CPM, Avil, cold FDCs like Sinarest/Wikoryl, and occasionally high-dose Cetirizine/Levocetirizine), anticholinergic delirium/confusion and hip-fracture falls in the elderly, QTc prolongation with high-dose Hydroxyzine (Atarax).
Serious / Dose-Limiting Adverse Effects:
  • Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.

9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions

  • Fexofenadine & Bilastine Transporter Blockade: Fruit juices (Orange, Apple, Grapefruit juice) inhibit intestinal OATP1A2 uptake transporters, reducing Fexofenadine and Bilastine absorption by 36% to 70%! Furthermore, Aluminium/Magnesium Antacids bind Fexofenadine in the gut (reducing absorption by >40%—space antacids by ≥2 hours!)
  • Erythromycin and ketoconazole inhibit P-gp efflux, doubling plasma levels
  • CNS & Anticholinergic Synergy: Sedating antihistamines + Benzodiazepines, Pregabalin, Opioids, Amitriptyline, or Alcohol cause severe psychomotor impairment and falls

10. Clinical Monitoring, Patient Counselling & Storage

Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.

Pharmacist Patient Counselling Points:

  • Patient Counselling Checklist: 1. For patients who drive, work during the day, or are elderly: explain that Fexofenadine (Allegra) and Bilastine cause zero drowsiness, whereas Cetirizine/Levocetirizine should be taken at bedtime, and old antihistamines (Avil, Piriton, Atarax) cause heavy grogginess. 2. For Allegra or Bilastine: take on an empty stomach with plain water—never wash down with orange/apple juice or right after a meal, or it will not absorb! 3. Warn elderly men with prostate enlargement (BPH) never to take OTC cold tablets (Sinarest, Wikoryl, D-Cold—which contain Chlorpheniramine + Phenylephrine), as the combination clamps the bladder neck shut and triggers emergency urinary retention!
  • Meal & Clock Timing Instruction: • Cetirizine / Levocetirizine / CPM: With or without food. • Fexofenadine (Allegra) & Bilastine: MUST be taken on an EMPTY STOMACH (1 hour BEFORE or 2 hours AFTER food or fruit juice) with plain water only! (Cetirizine / Levocetirizine: At bedtime (due to mild CNS penetration causing drowsiness in 10–15%). Fexofenadine / Bilastine: Morning or evening on an empty stomach (truly non-sedating—zero blood-brain barrier penetration via P-gp efflux!).)
  • Missed Dose Protocol: Used SOS or once daily; skip if close to next dose.
  • Geriatric Dispensing Pearl: Beers Criteria Mandate: Strictly avoid first-generation antihistamines (CPM, Pheniramine [Avil], Hydroxyzine [Atarax], Promethazine [Phenergan], Cyproheptadine [Practin]) in elderly patients due to confusion, dementia risk, falls, and urinary retention. Prefer Bilastine (20 mg empty stomach) or Fexofenadine (120 mg empty stomach) in the elderly!

Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Levocetirizine Tablets: 5 mg (Syrup 2.5 mg/5 mL); Cetirizine Tablets: 10 mg (Syrup 5 mg/5 mL); Fexofenadine Tablets: 120 mg (Allergic Rhinitis), 180 mg (Chronic Urticaria); Bilastine Tablets: 20 mg, 40 mg; CPM Tablets: 4 mg

11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)

THE 12-STEP ORAL DRUG JOURNEY THROUGH THE HUMAN BODY (LADME) Note: IV bolus enters Step 6 directly (F = 100%); Sublingual & Transdermal routes bypass Step 4–5 Portal First-Pass Metabolism 1. Oral Administration • Tablet / Capsule swallowed • Gastric emptying to duodenum pH 1.5–3.5 (Stomach) 2. Disintegration & Dissolution • Tablet breaks into granules • API dissolves in GI fluid Noyes-Whitney Dissolution Rate 3. GI Epithelial Absorption • Crosses intestinal villi • Passive / Active / P-gp efflux Small Intestine (Large Surface Area) 4. Portal Circulation • Mesenteric veins → Portal vein • Delivers blood to liver sinusoids Pre-systemic Venous Conduit 5. First-Pass Metabolism • Gut & hepatic CYP450 extraction • High: GTN, Propranolol, Morphine Determines Bioavailability (F = f_a × (1-E_H)) 6. Systemic Circulation • Hepatic vein → IVC → Heart • Unbound vs Albumin-bound drug Only FREE drug is active 7–8. Tissue Distribution (Vd) • Capillary permeation to organs • Blood-Brain & Placental barriers Vd = Dose / C_0 (L or L/kg) 9. Target Site of Action • Receptors (GPCR, Ion channel) • Enzymes & Carrier Transporters Pharmacodynamic Effect (E_max, EC50) 10. Hepatic Biotransformation • Phase I (CYP450 Oxidation/Hydrolysis) • Phase II (Glucuronidation/Sulfation) Converts lipophilic drug → hydrophilic metabolite 11. Renal & Biliary Elimination • Nephron: Filtration + Secretion − Reabsorption • Biliary excretion & Enterohepatic recycling Total Clearance CL_tot = CL_renal + CL_hepatic 12. Excretion from the Body • Urine (Primary polar metabolite route) • Bile/Faeces, Expired Air, Sweat, Milk Elimination Half-Life t1/2 = (0.693 × Vd) / CL
svg-v339-01-adme-12-step-journey — 8.1 Complete 12-Step Journey of an Orally Administered Drug (ADME): Figure 8.1: The 12-step physiological journey of a typical orally administered solid dosage form through Liberation, Absorption, Distribution, Metabolism, and Excretion (LADME). Note: Parenteral (IV), sublingual, and inhalational routes bypass gastrointestinal absorption and/or hepatic first-pass metabolism.

12. Authoritative References, Regulatory Sources & Editorial Disclaimer

Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 09 [9.9] (p. 118)

Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)

Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: HANDBOOK_SOURCE_CONTENT

Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.

← Back to All 644 Reference Profiles 📖 Explore 40 Knowledge Hub Articles → ✉️ Report Errata / Feedback
Educational Reference Notice: This printout from THE INDIAN PHARMACIST (https://theindianpharmacist.com/medicine/9-9-levocetirizine-cetirizine-chlorpheniramine-maleate-oral-h1-antihistamines/, Last Reviewed: 2026-11-10) is an educational reference sheet for students and healthcare learners. It is NOT an official prescribing guideline or patient-specific treatment order.