Astemizole

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Astemizole
Clinical data
AHFS/Drugs.comMultum Consumer Information
MedlinePlusa600034
Pregnancy
category
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • Withdrawn
Fecal
Identifiers
  • 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidyl]benzoimidazol-2-amine
JSmol)
  • Fc1ccc(cc1)Cn2c5ccccc5nc2NC4CCN(CCc3ccc(OC)cc3)CC4
  • InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) checkY
  • Key:GXDALQBWZGODGZ-UHFFFAOYSA-N checkY
  (verify)

Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation

arrhythmias due to hERG channel blockade).[2][3]

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

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.

Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed]

Astemizole does also act as FIASMA (functional inhibitor of acid sphingomyelinase).[6]

Astemizole has been researched as a treatment for Creutzfeldt-Jakob Disease (CJD).[7]

Toxicity

Astemizole has an oral

LD50
of approximately 2052 mg/kg (in mice).

References

  1. PMID 11259984
    .
  2. S2CID 25655101
    .
  3. PMID 31791048
    .
  4. PMID 20110603
    .
  5. PMID 12667689
    .
  6. PMID 21909365
    .
  7. PMID 23576755
    .

External links