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Non-Sedating H₁ Antihistamine
Allergic Rhinitis:
Symptomatic relief of seasonal/perennial allergic rhinitis
Chronic Urticaria:
Treatment of uncomplicated skin manifestations
Allergen-Induced Asthma:
Adjunctive symptomatic management
(Use under registered physician's guidance)
Potent selective H₁-receptor antagonist:
Inhibits histamine-mediated early-phase allergic response
Reduces inflammatory cell migration and mediator release (late-phase)
No significant anticholinergic effects
Minimal CNS penetration → low sedation potential
| Parameter | Profile |
|---|---|
| Absorption | Rapid; Tₘₐₓ: 0.5-1 hr (adults) • Food delays but does not reduce absorption |
| Distribution | Vd: 0.5 L/kg • Protein binding: 93% |
| Metabolism | Minimal hepatic metabolism (CYP-independent) |
| Elimination | Renal excretion (60-70% unchanged) • t½: 8-11 hr (adults) |
| Dialysis | Not removed by hemodialysis |
| Patient Group | Dosage Regimen |
|---|---|
| Adults & Children ≥6 yrs | 10 mg once daily OR 5 mg twice daily |
| Children 2-5 yrs | 5 mg once daily OR 2.5 mg twice daily |
| Children 1-2 yrs | 2.5 mg twice daily (max 5 mg/day) |
| Infants 6-11 mos | 2.5 mg once daily |
| Patient Group | Dosage | Administration |
|---|---|---|
| Adults & ≥12 yrs | 10 mg every 24 hr | IV push over 1-2 min |
| Children 6-11 yrs | 5-10 mg* every 24 hr | IV push over 1-2 min |
| Children 6 mos-5 yrs | 2.5 mg every 24 hr | IV push over 1-2 min |
*Dose based on symptom severity
Contraindicated in children <6 yrs with renal/hepatic impairment
(Follow registered physician's advice)
Hypersensitivity to cetirizine, hydroxyzine, or any component
Severe renal impairment (CrCl <10 mL/min) without dose adjustment
Common (≥1%):
Somnolence (mild) • Headache • Dry mouth • Fatigue
Rare (<0.1%):
Hypersensitivity reactions • Paradoxical excitation (children)
Transient hepatic transaminase elevation
No clinically significant interactions with:
Theophylline • Azithromycin • Pseudoephedrine • Ketoconazole • Erythromycin
Pregnancy (Category B):
Use only if benefit justifies risk (limited human data)
Lactation:
Excreted in breast milk; avoid or discontinue nursing
Renal/Hepatic Impairment:
Reduce dose by 50% in moderate impairment (CrCl 30-49 mL/min)
Avoid IV in severe impairment
CNS Effects:
Caution when driving/operating machinery (individual susceptibility)
Asthma Use:
Not for acute bronchospasm; use as adjunct only
| Group | Pharmacokinetics | Dosing Guidance |
|---|---|---|
| Elderly | ↓ Clearance proportional to ↓ CrCl | Adjust based on renal function |
| Renal Impairment | ↑ t½ (20 hr) • ↑ AUC (3-fold in dialysis | ↓ Dose by 50% if CrCl 30-49 mL/min |
| Hepatic Impairment | ↑ t½ (2-3 fold) | ↓ Dose by 50% |
Second-Generation H₁ Antihistamine (Non-Sedating)
Conditions: Below 30°C • Protect from light/moisture
IV Stability: Use immediately after reconstitution
Keep out of children's reach
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