Mizolastine

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.

Chemical properties

White Solid

Originator

Synthelabo (France)

The Uses of Mizolastine

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.

The Uses of Mizolastine

Allergic rhinitis;Blocking H1 receptors

Background

Mizolastine is under investigation in clinical trial NCT01928316 (A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers).

Definition

ChEBI: Mizolastine is a member of benzimidazoles.

brand name

Mizollen

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

Not Available

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