Astemizol Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Astemizole belongs to the second-generation class of non-sedating, non-anticholinergic
antihistamines. Its non-sedating properties appear to result from its
poor penetration of the blood brain barrier. As a result it shows no potentiation
of CNS depressants, including alcohol. Its long half-life allows once-daily dosing.
Chemische Eigenschaften
Crystalline Solid
Verwenden
Astemizole is used for preventing and treating severe seasonal and chronic allergic rhinitis,
allergic conjunctivitis, hives, Quinke’s edema, other allergic conditions and dermatitis.
Synonyms of this drug are hismanal, histazol, and others.
Definition
ChEBI: A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.
Weltgesundheitsorganisation (WHO)
The first clinically interesting histamine ti-antagonists were
introduced in the late forties and early fifties. Several histamine ti-antagonists have
a similar cardiac effect to that seen with astemizole and terfenadine. Serious
cardiovascular adverse reactions have been reported when used concomitantly with
imidazole antifungals and macrolide antibiotics.
Biologische Aktivität
Orally active, potent histamine H 1 antagonist (IC 50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC 50 = 227 - 734 nM). Also potent hERG K + channel blocker (IC 50 = 0.9 nM) that displays cardiotoxicity in vivo .
Sicherheitsprofil
Poison by subcutaneous andintravenous routes. Moderately toxic by ingestion. Humansystemic effects by ingestion: arrhythmias, coma, nauseaor vomiting, somnolence. When heated to decompositionit emits toxic fumes of F?? and NOx.
Astemizol Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
