Last reviewed · How we verify
Zyrtec® (cetirizine)
Zyrtec® (cetirizine) is a H1-receptor antagonist (second-generation antihistamine) Small molecule drug developed by Organon and Co. It is currently FDA-approved for Seasonal and perennial allergic rhinitis, Chronic urticaria (hives).
Cetirizine is a selective H1-receptor antagonist that blocks histamine binding to H1 receptors on cells, preventing allergic symptoms.
Cetirizine is a selective H1-receptor antagonist that blocks histamine binding to H1 receptors on cells, preventing allergic symptoms. Used for Seasonal and perennial allergic rhinitis, Chronic urticaria (hives).
At a glance
| Generic name | Zyrtec® (cetirizine) |
|---|---|
| Sponsor | Organon and Co |
| Drug class | H1-receptor antagonist (second-generation antihistamine) |
| Target | H1 receptor |
| Modality | Small molecule |
| Therapeutic area | Allergy/Immunology |
| Phase | FDA-approved |
Mechanism of action
Cetirizine competitively inhibits histamine at peripheral H1 receptors, reducing the release and effects of histamine that cause itching, sneezing, rhinorrhea, and urticaria. As a second-generation antihistamine, it is highly selective for H1 receptors and has minimal central nervous system penetration due to its hydrophilic nature and poor blood-brain barrier crossing, resulting in reduced sedation compared to first-generation antihistamines.
Approved indications
- Seasonal and perennial allergic rhinitis
- Chronic urticaria (hives)
Common side effects
- Headache
- Somnolence/drowsiness
- Fatigue
- Dry mouth
- Pharyngitis
Key clinical trials
- Fasting Study of Cetirizine HCl Tablets 10 mg and Zyrtec® Tablets 10 mg (PHASE1)
- Food Study of Cetirizine HCl Tablets 10 mg and Zyrtec® 10 mg (PHASE1)
- Phase 2 Study IV QUZYTTIR™ (Cetirizine Hydrochloride Injection) vs V Diphenhydramine (PHASE2)
- Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03180) (PHASE4)
- Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03182) (PHASE4)
- Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03181) (PHASE4)
- Multi-Center, Pediatric, Open-Label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec ® 5.0 mg Chewable Tablet Medications (Study P04573) (Completed) (PHASE4)
- Multi-center, Pediatric, Open-label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec 5.0 mg Chewable Tablet Medications (Study P04574)(COMPLETED) (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Zyrtec® (cetirizine) CI brief — competitive landscape report
- Zyrtec® (cetirizine) updates RSS · CI watch RSS
- Organon and Co portfolio CI
Frequently asked questions about Zyrtec® (cetirizine)
What is Zyrtec® (cetirizine)?
How does Zyrtec® (cetirizine) work?
What is Zyrtec® (cetirizine) used for?
Who makes Zyrtec® (cetirizine)?
What drug class is Zyrtec® (cetirizine) in?
What development phase is Zyrtec® (cetirizine) in?
What are the side effects of Zyrtec® (cetirizine)?
What does Zyrtec® (cetirizine) target?
Related
- Drug class: All H1-receptor antagonist (second-generation antihistamine) drugs
- Target: All drugs targeting H1 receptor
- Manufacturer: Organon and Co — full pipeline
- Therapeutic area: All drugs in Allergy/Immunology
- Indication: Drugs for Seasonal and perennial allergic rhinitis
- Indication: Drugs for Chronic urticaria (hives)
- Compare: Zyrtec® (cetirizine) vs similar drugs
- Pricing: Zyrtec® (cetirizine) cost, discount & access