4,9-Dihydro-4-(1-methylpiperidin-4-yliden)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-onfumarat Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
Ketotifen is a histamine H
1 receptor antagonist (K
i = 1.3 nM) and mast cell stabilizer. It is selective for H
1 receptors over H
2 and H
3 receptors (K
is = 987 and 2,500 nM, respectively). Ketotifen (50 and 100 μM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 . It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg. Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model. Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.
Chemische Eigenschaften
Off-White Solid
Verwenden
Ketotifen fumarate salt has been used: for mast cell product antagonism, as a positive control in β-hexosaminidase release assay, as mast cell stabilizer to treat pregnant dams added to ad libitum drinking water
Allgemeine Beschreibung
Ketotifen fumarate, 4-(1-methyl-4-piperidylidene)-4Hbenzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one hydrogenfumarate (Zaditor), is a fine crystalline powder.Ketotifen is a ketothiophene isostere analog of the dibenzocycloheptaneantihistamines. The solution contains0.345 mg of ketotifen fumarate, which is equivalent to0.25 mg of ketotifen. The solution also contains the preservativebenzalkonium chloride (0.01%) as well as glycerol,sodium hydroxide and/or hydrochloric acid (to adjust pH),and purified water. It has a pH of 4.4 to 5.8 and an osmolalityof 210 to 300 mOsm/kg.
The recommended dose of ketotifen solution is 1 drop instilledinto each affected eye every 8 to 12 hours. The mostfrequently reported adverse reactions are conjunctival infection,headaches, and rhinitis. This drug product is for ocularadministration only and not for injection or oral use.Ketotifen solution should be used with caution during pregnancyor while nursing, because its safety has not been studiedunder these circumstances.
Biologische Aktivität
An H 1 receptor antagonist.
4,9-Dihydro-4-(1-methylpiperidin-4-yliden)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-onfumarat Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
