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 It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects (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]
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[4][5] have shown high permeability and high binding to protein folds associated with
Alzheimer's.
^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.
PMID10376921.
S2CID25655101.
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 It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects (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]
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[4][5] have shown high permeability and high binding to protein folds associated with
Alzheimer's.
^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.
PMID10376921.
S2CID25655101.