Cetirizine is preferred over diphenhydramine for chronic urticaria in outpatients because it has which pharmacological advantage?
- A It is a selective H1 antagonist that does not cross the blood-brain barrier significantly, causing minimal sedation ✓
- B It has a faster onset of action due to parenteral administration
- C It also blocks H2 receptors providing combined gastric acid suppression
- D It inhibits leukotriene synthesis in addition to H1 blockade
Explanation
Cetirizine is a second-generation H1 antihistamine; its zwitterionic structure and P-glycoprotein-mediated efflux at the blood-brain barrier limit CNS penetration, resulting in minimal sedation compared to first-generation agents like diphenhydramine (which freely enter the CNS and block muscarinic, alpha-adrenergic and histamine receptors centrally). This non-sedating property makes cetirizine suitable for daytime chronic urticaria management. Neither H2 blockade nor leukotriene inhibition is a property of cetirizine.
Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.
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