Mizolastine

Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.

Development of a CZE method for the determination of mizolastine and its impurities in pharmaceutical preparations using response surface methodology.[Pubmed:17195261]

Electrophoresis. 2007 Feb;28(3):395-405.

A fast and selective CZE method for the determination of Mizolastine and related impurities is described. Response surface methodology was applied to study the influence of phosphate/triethanolamine (TEA) buffer concentration, heptakis(2,3,6-tri-O-methyl)-beta-CD (TMbetaCD) concentration, voltage and temperature. The optimum conditions were: 105 mM phosphate/TEA buffer (pH 3.0) containing 10 mM TMbetaCD, temperature 19 degrees C and voltage 30 kV. Validation of the method was performed in drug substance and drug product. Robustness was evaluated using a Plackett-Burman design, including pH among the considered factors. Applying the optimal conditions, the nine peaks were baseline separated in about 10 min. The method was applied to the quality control of Mizolastine in controlled-release tablets.

[Efficacy and safety of Mizolastine in the treatment of perennial allergic rhinitis].[Pubmed:17674763]

Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2007 Jun;21(11):491-3.

OBJECTIVE: To investigate the efficacy and safety of Mizolastine in the treatment of perennial allergic rhinitis. METHOD: Multicentric random Double-blind parallel-controlled study was adopted, and compared with placebo and Cetirizine. Patients (n = 177) were grouped, seventy-two in Mizolastine group, sixty-nine in Cetirizine and thirty-six in placebo group. RESULT: In the seventh curative day symptomatic and sign marks in Mizolastine group and Cetirizine group were lower, but the mark in Mizolastine group reduced more than in Cetirizine group and placebo group. Mizolastine group is better than Cetirizine group in improvement of nasal obstruction and itching with Visual analogue scale. In the twenty first curative day reduction of symptomatic and sign marks in Mizolastine group was lower than Cetirizine group, but no statistic difference. There were 27 adverse events, no serious adverse events in 177 patients during experimental period. Most adverse events were headache and dryness in mouth and eyes. There were 10 cases adverse events in Mizolastine group, one case was related with experiment and four cases might be related with experiment. There were 14 cases adverse events in Cetirizine group, one case was related with experiment and four cases might be related with experiment. There were three cases adverse events in placebo group. CONCLUSION: Generally speaking the efficacy of Mizolastine in treatment of perennial allergic rhinitis is better than Cetirizine, Bad events are less. It is safe.

Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria.[Pubmed:18020585]

BioDrugs. 1998 Jul;10(1):41-63.

UNLABELLED: Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H(1) receptors. Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials have shown Mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with chronic idiopathic urticaria. Available data also suggest that prophylactic administration of Mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis. Mizolastine 10 mg/day is generally well tolerated, with the most common adverse events being drowsiness (7%), fatigue (2%), increased appetite (2%) and dry mouth (2%). In volunteers and patients the incidence of prolonged QT(c) interval was similar in Mizolastine and placebo recipients, although Mizolastine is contraindicated in those with cardiac disease or hepatic impairment or in those receiving erythromycin, ketoconazole or class I or III antiarrhythmic agents. Tests of psychomotor function in volunteers revealed no impairment after single doses of Mizolastine Mizolastine is a second generation antihistamine agent administered at a dosage of 10mg once daily. Unlike terfenadine and astemizole, Mizolastine has not been shown to increase the QT(c) interval in volunteers and patients. Mizolastine may be considered an effective alternative to other second generation antihistamine agents in the management of allergic rhinitis and chronic idiopathic urticaria.

Reversible anti-settlement activity against Amphibalanus (=Balanus) amphitrite, Bugula neritina, and Hydroides elegans by a nontoxic pharmaceutical compound, mizolastine.[Pubmed:20183132]

Biofouling. 2009 Nov;25(8):739-47.

Mizolastine, an antihistamine pharmaceutical, was found to significantly inhibit larval settlement of the barnacle Amphibalanus (=Balanus) amphitrite, the bryozoan Bugula neritina, and the polychaete Hydroides elegans with EC(50) values of 4.2, 11.2, and 4.1 microg ml(-1), respectively. No toxicity against the larvae of these three species was observed at the concentration range tested during incubations with Mizolastine. To determine whether the anti-settlement activity of Mizolastine is reversible, recovery bioassays using these three species were conducted. More than 70% of the larvae that had been exposed for 4 h to Mizolastine at concentrations four-fold greater than their respective EC(50) values completed normal metamorphosis. The results of the recovery bioassay provide evidence that the anti-settlement effect of Mizolastine is reversible in addition to being nontoxic. The anti-settlement activities of several intermediates of the synthesis process of Mizolastine were also examined. One of the intermediates, 2-chloro-1-(4-fluorobenzyl)-1H-benzo[d]imidazole, inhibited larval settlement and metamorphosis with low toxicity. These results may improve the understanding of the key functional group responsible for the anti-settlement activity of Mizolastine.

Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.

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