Disease relevance of Instotal

• In several large controlled comparative clinical studies, loratadine was superior to placebo, faster acting than astemizole and as effective as azatadine, cetirizine, chlorpheniramine (chlorphenamine), clemastine, hydroxyzine, mequitazine and terfenadine in patients with allergic rhinitis and chronic urticaria [1].
• These data clearly suggest that mequitazine has potential to treat allergic conjunctivitis [2].
• 4 Mequitazine and terfenadine did not affect salivary flow, heart rate or pilocarpine-induced miosis [3].
• Autonomic dysfunction in perennial vasomotor rhinitis and the effect of mequitazine [4].
• Mequitazine in the treatment of hayfever [5].

Psychiatry related information on Instotal

• Divided attention performance was also affected by Treatment. Reaction time (RT) during mequitazine treatments increased in a dose-related manner and significantly differed from placebo at the highest dose [6].
• OBJECTIVE: The present study compares the sedative effects of three doses of mequitazine on actual driving, psychomotor performance and memory with those of a first- and a second-generation antihistamine [6].

High impact information on Instotal

• Double-blind placebo-controlled study of loratadine, mequitazine, and placebo in the symptomatic treatment of seasonal allergic rhinitis [7].
• To obtain this model, the bioactive conformations of several (semi-)rigid classical histamine H1-receptor antagonists have been investigated (cyproheptadine, phenindamine, triprolidine, epinastine, mequitazine, IBF28145, and mianserine) [8].
• Microsomes from genetically engineered human B-lymphoblastoid cells expressing cytochrome P450 2D6 (CYP2D6) efficiently metabolized mequitazine to the hydroxylated and S-oxidized metabolites [9].
• Inhibition of CYP3A-catalyzed midazolam 1'-hydroxylase by various histamine H1 antagonists, including mequitazine, suggested that mequitazine and some other histamine H1 antagonists could also be inhibitors of CYP3A in human liver microsomes [9].
• In addition, we also examined the excitatory responses of SAR activity to right atrial injections of histamine at 10 and 60 micrograms/kg before and after topical administration of atropine (0.1 ml, 1%, n = 6) or mequitazine (0.1 ml, 1%, n = 6) in 12 SAR preparations [10].

Chemical compound and disease context of Instotal

• Randomised double masked trial comparing the efficacy and tolerance of 0.05% mequitazine eye drops versus 0.05% levocabastine and placebo in allergic conjunctivitis induced by a conjunctival provocation test with Dermatophagoides pteronyssinus [11].
• A double-blind comparison of terfenadine and mequitazine in the symptomatic treatment of acute pollinosis [12].
• In controlling perennial rhinitis symptoms mequitazine was markedly inferior to dexchlorpheniramine and only slightly better than placebo [13].
• RESULTS: The sum of the scores for hyperemia and itching, and total composite score were lower after 0.05% mequitazine than after 2% disodium cromoglycate (p < 0.0001 in each case) [14].
• A new type of antiallergic drug, oxatomide (60 mg daily), was compared with the antihistaminic, mequitazine (10 mg daily), in a 5-week double-blind randomized study involving 26 patients with chronic urticaria [15].

Biological context of Instotal

• To realized the role of H1 receptor involved in TF-induced apoptosis, different H1 receptor antagonists including promethazine, mequitazine, and chlorpheniramin (50-100 microM) were administered and demonstrated that these chemicals cannot induced apoptosis through the H1 receptor signaling pathway [16].
• Effect of mequitazine on the pharmacokinetics of theophylline in asthmatic patients [17].
• Mequitazine (5 mg) impaired visuo-motor coordination 7.5 h after ingestion (considered to be a chance result), but there was no effect on digit symbol substitution, critical flicker fusion threshold or dynamic visual acuity [18].
• The effects of single oral doses of mequitazine (5 and 10 mg), terfenadine (60 mg) and triprolidine (10 mg) as active controls, and placebo were evaluated on visuo-motor coordination, digit symbol substitution, critical flicker fusion and dynamic visual acuity, and on subjective assessments of mood and well-being in six normal female volunteers [18].
• The objective of this study was to develop an assay for mequitazine (MQZ) for the study of the bioavailability of the drug in human subjects [19].

Anatomical context of Instotal

• The interaction of mequitazine with phospholipid model membranes [20].
• Indomethacin or removal of endothelium did not affect the inhibitory effect of mequitazine on the responses to PE [21].
• When membrane and cytosol fractions were incubated with each drug, epinastine, ketotifen and mequitazine prevented O2- generation [22].
• These data show that: a) diphenhydramine and mequitazine appear to produce CNS effects by altering basic processes within the brain; b) astemizole and terfenadine seem to cross the blood-brain barrier at high doses only; c) loratadine has the lowest liability to produce central side effects [23].
• Mequitazine at 10(-7) M produced a parallel shift of the dose-response curve to acetylcholine in the rat duodenum, clemizole and the lower doses of mequitazine failed to modify the effect of acetylcholine [24].

Associations of Instotal with other chemical compounds

• 1 The anticholinergic effects of atropine and two antihistamines (terfenadine and mequitazine) were investigated vs placebo in a double-blind study [3].
• Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plot were 9.95 +/- 0.44 for mequitazine and 10.54 +/- 0.44 for clemizole [24].
• If dexchlorpheniramine induces a significant sleep distortion (slowed REM sleep cycle and decreased amount of REM sleep), no similar trend occured with mequitazine, a result that could be dose or time related [25].
• Disodium cromoglycate and tranilast with inhibitory actions on mediator release inhibited PCA specifically, whereas antihistaminics, including ketotifen, azelastine, mequitazine and diphenhydramine, inhibited histamine- and serotonin-induced cutaneous reactions as well as PCA [26].
• The bronchodilating activity of mequitazine (MQ) (10-[3- quinuclidynilmethyl ]-phenothiazine) has been investigated in the guinea-pig using various spasmogens such as acetylcholine, histamine and leukotriene-C4 (LTC4) [27].

Analytical, diagnostic and therapeutic context of Instotal

• The first procedure is based on determination of mequitazine by HPLC with UV detection at 256 nm [28].
• The results suggested that after the oral administration only low mequitazine concentrations appeared in serum, most of the drug seemed to be deactivated by the extrarenal route, and the kinetic properties of the drug resembled those of several phenothiazines used for psychiatric therapy [29].
• In order to achieve a better tolerance, patients are protected with antihistamines on the days they are administered the immunotherapy (mequitazine 5 mg every 12 hours) and also, doses equal or over 40 micrograms are given fractionally, injecting half dose in each arm [30].
• The suppressive activity of mequitazine (MQZ) on histamine skin reactivity was evaluated in 29 healthy subjects (age 22-25 years) in a single-blind study [31].
• Determination of mequitazine in human plasma by gas-chromatography/mass spectrometry with ion-trap detector and its pharmacokinetics after oral administration to volunteers [19].

References