Astemizole is a second generation antihistamine used to treat allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice.
- Mechanism
- Curator reviewed
Astemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H1 receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H3-receptors, producing adverse effects.
- Primary indication
- Astemizole was indicated for use in the relieving allergy symptoms, particularly rhinitis and conjunctivitis.Curator reviewed
- Formula / weight
- C28H31FN4O · 458.5703 g/mol (avg)
- First approval
- Canada, 1984
- Code names
- BRN 4830190 · R 42512 · R 43,512
Resolves to
GXDALQBWZGODGZ-UHFFFAOYSA-NSMILESCOC1=CC=C(CCN2CCC(CC2)NC2=NC3=CC=CC=C3N2CC2=CC=C(F)C=C2)C=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Astemizole, and which of those have an active Phase 3 trial?
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