Chemical Property of Mizolastine
Chemical Property:
- Melting Point:217°
- Refractive Index:1.682
- PKA:9.73±0.40(Predicted)
- PSA：70.05000
- Density:1.34 g/cm3
- LogP:3.47720
- Storage Temp.:Refrigerator
- Solubility.:Chloroform (Slightly, Heated), DMSO, Methanol (Slightly, Heated)
- XLogP3:3.2
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:5
- Exact Mass:432.20738760
- Heavy Atom Count:32
- Complexity:728
- Purity/Quality:
-
99% *data from raw suppliers
Mizolastine *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5
- Recent ClinicalTrials:A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers
-
Description
Mizolastine was marketed in Germany and Switzerland as Mizollen for
the symptomatic relief of seasonal and perennial allergic rhinoconjunctivitis and
urticaria. Mizolastine is a new long-acting, orally active antihistaminic agent with
a rapid onset of action ; the two most recent H1 antagonists launched were
fexofenadine, metabolite of terfenadine (Sepracor, 1996) and Olopatadine
(Kyowa Hakko, 1997). Mizolastine can be prepared in 2 steps from 2-chloro 1-
(4-fluorobenzyl)benzimidazole by successive condensations of appropriate
amine and thioether. Mizolastine selectively blocks the peripheral H1 receptors
(but not the serotonergic, noradrenergic, muscarinic receptors) with a minimal
occupancy of brain receptors, and therefore does not elicit any sedative effects.
Moreover, Mizolastine does not produce cardiac rhythm disorders which have
been associated with certain non-sedating antihistamines in humans.
-
Uses
A highly selective histamine H1-receptor antagonist (with no anticholinergic, antiadrenergic, or antiserotonin activity) for use in the treatment of allergic disorders, especially rhinitis and urticaria. Allergic rhinitis;Blocking H1 receptors
-
Clinical Use
Antihistamine:
Symptomatic relief of allergy, e.g. hayfever, urticaria
-
Drug interactions
Potentially hazardous interactions with other drugs
Anti-arrhythmics: increased risk of ventricular
arrhythmias - avoid with amiodarone, disopyramide,
flecainide, mexiletine, procainamide and
propafenone.
Antibacterials: metabolism possibly inhibited by
macrolides - avoid; increased risk of ventricular
arrhythmias with moxifloxacin - avoid.
Antidepressants: risk of ventricular arrhythmias with
citalopram and escitalopram - avoid.
Antifungals: metabolism inhibited by itraconazole
and ketoconazole and possibly imidazoles - avoid.
Antimalarials: avoid with piperaquine with
artenimol.
Antivirals: concentration possibly increased by
ritonavir; increased risk of ventricular arrhythmias
with saquinavir - avoid.
Beta-blockers: increased risk of ventricular
arrhythmias with sotalol - avoid.
Ciclosporin: use with caution due to inhibition of
ciclosporin metabolism.
Cytotoxics: possible increased risk of ventricular
arrhythmias with vandetanib.
Avoid concomitant treatment with any drug that
could prolong QT interval.
Caution with drugs that inhibit cytochrome P450
enzymes (may elevate mizolastine levels)
