Astemizole
chemical compound
Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977. It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel blockade).
Pharmacology
Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects.
Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus (caused by histamine).
Despite some earlier reports that astemizole does not cross the blood–brain barrier, several studies have shown high permeability and high binding to protein folds associated with Alzheimer's.
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.
Astemizole does also act as FIASMA (functional inhibitor of acid sphingomyelinase).
“Astemizole” enters the record as chemical compound. Crown Archives preserves that source wording while asking what Astemizole, chemical and compound can confirm, complicate or overturn.
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Stable identifiers, scientific names and standards terminology offer the best bridge between this overview and specialist evidence. The source revision retrieved here is dated Sep 22, 2026. The linked authority identifier is Q423437. None of the 0 selected statements returned an explicit reference. The first chronological checks are 1977 and 1999.
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