Molecular Formula | C28H30N2O8 |
Molar Mass | 522.5464 |
Melting Point | 152-154° |
Solubility | DMSO 105 mg/mL Water 105 mg/mL Ethanol <1 mg/mL |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | Sealed in dry,Room Temperature |
Use | An antihistaminic. |
In vitro study | 95% Azatadine bioconverted to two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine, within 72 hours in Sabouraud glucose broth. |
In vivo study | Azatadine delayed the onset of nebulization histamine, acetylcholine and serotonin induction by Dyspnea in conscious guinea pigs with PD50 of 0.01 mg/kg,0.739 mg/kg and 0.86 mg/kg. Azatadine protects against histamine-induced death by intravenous administration with oral PD50 of 0.009 mg/kg and 0.22 mg/kg in conscious guinea pigs and mice, respectively. In fasted volunteers, 4.2 hours after a single oral dose of Azatadine (4 mg), RIA 4.2 measurements showed a C max of 3 μg/L. Azatadine is almost completely metabolized by hydroxylation, demethylation, and formation of the zwitterion isomer upon opening of the oxidative ring. The Csub>max in healthy volunteers after 8.8 hours of treatment with Azatadine (5.3 mg orally) was 5.9 μg/L with a bioavailability of 80%. Azatadine (1 mg twice daily for 14 days) is effective in reducing symptoms of histamine-mediated seasonal allergic rhinitis. |
HS Code | 2933399090 |