Astemizole is a second-generation H₁-antihistamine known for its non-sedating action due to limited blood-brain barrier penetration. Structurally, it features a benzoxazole ring fused to a piperazine moiety, contributing to its high receptor selectivity. It effectively treats allergic rhinitis, urticaria, and chronic idiopathic urticaria by blocking H₁ receptors and exhibiting mild anti-inflammatory properties without significant central nervous system effects.
Structure of Astemizole
- Astemizole is a non-sedating second-generation antihistamine with a benzoxazole ring fused to a piperazine moiety.
- Chemical Formula: C₂₇H₃₁NO₃
Mode of Action
- Selective H₁-receptor antagonist with minimal penetration of the blood-brain barrier, reducing sedation.
- It also exhibits anti-inflammatory properties.
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Uses
- Allergic Rhinitis: Relieves symptoms like sneezing, itching, and runny nose.
- Urticaria: Alleviates hives and skin itching.
- Chronic Idiopathic Urticaria: Effective in long-term management of hives.
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