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 It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel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).[2][3]
^Matsumoto S, Yamazoe Y (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. 51 (2): 133–142. doi:10.1046/j.1365-2125.2001.01292.x. PMC 2014443. PMID 11259984.
^Zhou Z, Vorperian VR, Gong Q, Zhang S, January CT (June 1999). "Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole". Journal of Cardiovascular Electrophysiology. 10 (6): 836–843. doi:10.1111/j.1540-8167.1999.tb00264.x. PMID 10376921. S2CID 25655101.
^Charles O, Onakpoya I, Benipal S, Woods H, Bali A, Aronson JK, et al. (2019). "Withdrawn medicines included in the essential medicines lists of 136 countries". PLOS ONE. 14 (12): e0225429. Bibcode:2019PLoSO..1425429C. doi:10.1371/journal.pone.0225429. PMC 6887519. PMID 31791048.
Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action...
QT interval. Other examples include terfenadine (Seldane, Seldane-D), astemizole (Hismanal), cisapride (Propulsid, withdrawn in many countries for prolonging...
of clarithromycin with the following medications: cisapride, pimozide, astemizole, terfenadine, ergotamine, ticagrelor, ranolazine or dihydroergotamine...
histamine H1-receptors (Ki=64 nM) with an affinity comparable to that of astemizole and diphenhydramine, and superior than that of cetirizine by three-fold...
Sánchez-Pedreño P, Aliaga A (1997). "Treatment of aquagenic urticaria with PUVA and astemizole". Journal of the American Academy of Dermatology. 36 (1): 118–9. doi:10...
selectively binding and depolymerising their tubulins. Antihistamines such as astemizole, bilastine, clemizole, emedastine, mizolastine, and oxatomide. Benzimidazole...
delavirdine fluvoxamine iron salts voriconazole aminophylline and theophylline astemizole It is a racemic 1:1 mixture of the enantiomers dexlansoprazole and levolansoprazole...
In some cases, this can lead to a fatal interaction with drugs like astemizole or terfenadine. The effect of grapefruit juice with regard to drug absorption...
government removed two second generation antihistamines, terfenadine and astemizole, from the market based on evidence that they could cause heart problems...
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