Mizolastine
Latin: Mizolastinum
R06AX25
Systemic antihistamines
Antagonist at histamine H1 receptors
Template: Infobox chemical / molecular formula search available
Mizolastine is a drug which is used as a H1 - antihistamine especially for symptomatic treatment of allergic rhinitis, allergic conjunctivitis and urticaria application.
Chemistry
Mizolastine is a benzimidazole derivative and structurally it resembles the astemizole. This drug is a specific antagonist which blocks the histamine H1 - receptors. It does not affect adrenaline, acetylcholine still serotonin receptors. Mizolastine was developed in 1998 by the pharmaceutical company sanofi -aventis, which, however, sold the patent rights also at Schwarz Pharma.
Effect
Mizolastine is intended for oral ingestion, is relatively rapidly absorbed, so that after about 60 to 90 minutes, a peak plasma level is reached and the effect lasts thanks to the relatively long elimination half-life of about 24 hours. The affinity of mizolastine to the H1 receptors is 10 times greater than that of cetirizine and about 20 times higher than that of loratadine.
Due to the lack of potential to cross the blood -brain barrier, it acts only on peripheral H1 - receptors, has so unlike other antihistamines almost no sedative effect, although still temporary fatigue can occur.
Obviously has mizolastine and the ability to inhibit the synthesis of leukotrienes, which is why it ascribes antiinflammatory properties. Chance of influences on the QT interval were observed, but so far could be detected neither definite effects on the QT interval, nor arrhythmias associated with Mizolastine be observed.
Since cytochrome P450 isoenzymes involved in the metabolism of Mizolastine, it comes to interactions with simultaneous administration of CYP3A4 inhibitors, ketoconazole and erythromycin are contraindicated.
Pharmacy
In clinical trials Mizolastine showed roughly comparable efficacy with cetirizine and loratadine. It is available in tablets of 10 mg and prescription in Germany. An application in children and pregnant and lactating women is not provided due to lack of studies.
The present lower number of prescription Mizolastine preparations is probably due to comparatively higher price and the fact that patent protection is still active and thus Generic drugs can be approved in the future only. The two original preparations are under the name Mizollen ( Synthelabo ) and Zolim sold ( Schwarz Pharma ).