From Surf Wiki (app.surf) — the open knowledge base

Astemizole

Antihistamine drug

| Drugs.com =

| elimination_half-life = 24 hours

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 It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel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 has been researched as a treatment for Creutzfeldt-Jakob Disease (CJD).

Like many carbendazim-derived benzimidazoles, it has been reported to interact with tubulin and inhibit its polymerization.

Toxicity

Astemizole has an oral LD50 of approximately 2052 mg/kg (in mice).

References

(February 2001). "Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine". British Journal of Clinical Pharmacology.
(June 1999). "Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole". Journal of Cardiovascular Electrophysiology.
(2019). "Withdrawn medicines included in the essential medicines lists of 136 countries". PLOS ONE.
(2010). "Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease". IOS Press.
(March 2003). "High throughput artificial membrane permeability assay for blood-brain barrier". European Journal of Medicinal Chemistry.
(2011). "Identification of novel functional inhibitors of acid sphingomyelinase". PLOS ONE.
(April 2013). "Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents". Proceedings of the National Academy of Sciences of the United States of America.
(2025). "NanoDSF Screening for Anti-tubulin Agents Uncovers New Structure–Activity Insights". Journal of Medicinal Chemistry.

Info: Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

phenethylamines belgian-inventions benzimidazoles 4-fluorophenyl-compounds h1-receptor-antagonists herg-blocker janssen-pharmaceutica 4-methoxyphenyl-compounds piperidines withdrawn-drugs

Want to explore this topic further?

Ask Mako anything about Astemizole — get instant answers, deeper analysis, and related topics.

Research with Mako

Free with your Surf account

Content sourced from Wikipedia, available under CC BY-SA 4.0.

This content may have been generated or modified by AI. CloudSurf Software LLC is not responsible for the accuracy, completeness, or reliability of AI-generated content. Always verify important information from primary sources.

Report