Chemical Properties
White Solid
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.
Uses
Allergic rhinitis;Blocking H1 receptors
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.
Originator
Synthelabo (France)
Definition
ChEBI: Mizolastine is a member of benzimidazoles.
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)
Metabolism
Mainly metabolised by glucuronidation although other
metabolic pathways are involved, including metabolism
by the cytochrome P450 isoenzyme CYP3A4, with the
formation of inactive hydroxylated metabolites
