Disease relevance of Dimetindene

• Cutaneous responses to substance P and calcitonin gene-related peptide in chronic urticaria: the effect of cetirizine and dimethindene [1].
• Contact dermatitis from a gel containing dimethindene maleate [2].
• Efficacy of topical dimetindene in experimentally induced pruritus and weal and flare reactions [3].
• Two allergic reactions that occurred within minutes after start of the 5- and 10-g hydroxocobalamin infusions were successfully managed with dexamethasone and/or dimethindene maleate [4].
• Following dimethpyrindene all animals showed arterial hypotension, pulmonal hypertension, decrease in peripheral resistance and hyperventilation [5].

Psychiatry related information on Dimetindene

• Effects of dimethindene maleate on psychomotor performance in the oculodynamic test compared with placebo and loratadine [6].

High impact information on Dimetindene

• Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists [7].
• This second-generation dimethindene analogue might also be the starting point for the development of M(2)-selective muscarinic antagonists useful for quantifying M(2) receptors in the central nervous system with positron emission tomography imaging [7].
• Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene [8].
• The PRL increase caused by Fe (0.2 mg/70 kg) was not altered by pretreatment with the H1-antagonist Di, the H2-antagonist Ci, or the combination of both [9].
• In anaesthetized rats methylhistaprodifen and compounds 1-4 induced almost the same fall in blood pressure as in pithed and vagotomized animals; the effects were sensitive to blockade by dimetindene (1 micromol/kg) [10].

Chemical compound and disease context of Dimetindene

• Dimetindene maleate (DMM, Fenistil, CAS 3614-69-5) a specific H1-receptor antagonist, is therapeutically used for the treatment of respiratory allergies, urticaria, itching dermatoses and generally pruritic sensations occurring with various diseases [11].
• The topical application of a 0.1% dimetindene maleate gel on the forearms of 11 subjects reduces the areas of both erythema and wheal produced by the intradermal injection of 0.025 mg of histamine hydrochloride to a statistically greater degree than 1% d-chlorpheniramine maleate cream (p less than 0.005 and p less than 0.0005, respectively) [12].

Biological context of Dimetindene

• The effect of dimethindene (DMI) on transmembrane potentials and contractile force was studied in atrial and ventricular myocardium of guinea-pigs [13].
• Maximal W and F, area under curve (AUC), and time of W and F disappearance were calculated at baseline and 4 h after a single dose of 20 mg cetirizine (Ce), 4 mg dimethindene (Di), or placebo (P), in a double-blind, placebo-controlled (DBPC), crossover, randomized study [1].
• Enantioselective biotransformation of the chiral antihistaminic drug dimethindene in humans and rats [14].
• Pharmacokinetics of dimetindene after intravenous and oral administration to healthy volunteers [15].
• Identification of the molecular structure of the phenolic primary metabolite of dimetindene in animals and man [16].

Anatomical context of Dimetindene

• Action of dimethindene on the electrophysiological and mechanical properties of atrial and ventricular myocardium of guinea-pig [13].
• All drugs except for dimethindene, which only minimally passes across the blood-brain barrier, suppressed muricide [17].
• Using large volumes of in vitro incubations of rat microsomes with dimetindene and cofactors, 1.15 mg of pure primary metabolite were first produced and then extensively purified [16].
• The effects on transepithelial ion transports of chloropyramine, dimetindene and diphenhydramine, which are three antagonists of H1-receptors of histamine, were examined in bovine tracheal epithelium and in frog skin [18].

Associations of Dimetindene with other chemical compounds

• We conclude that dimethindene maleate is a moderately potent H1-receptor antagonist, and that the inhibition of the 48/80 and house dust mite induced weals is accounted for by the antihistaminic effect of dimethindene maleate [19].
• The treated group of 20 patients was premedicated with the H1 antagonist dimetindene (0.2 mg/kg) and the H2 antagonist ranitidine (1.25 mg/kg); the control group of 20 patients received saline [20].
• The concentration-response curve of histamine was shifted to the right by the H3 receptor antagonists thioperamide, impromidine and burimamide (apparent pA2 8.37, 6.86 and 7.05, respectively), by the H2 receptor antagonist ranitidine (apparent pA2 4.27) and was not affected by the H1 receptor antagonist dimetindene (32 mumols/l) [21].
• Tissue oxygenation was ameliorated by the H1-antagonist treatment, as demonstrated by plasma lactate levels and base excess values (p < .05, control group versus dimethindene group) [22].
• 12 h before a 4-h-lasting continuous challenge with permanent 1000 dactylis grass pollen in the VCC, administration of dimetindene (Fenistil R Pellets) in doses of 4 mg, 8 mg or identically appearing placebo was scheduled in three sessions [23].

Gene context of Dimetindene

• Although the histamine H1 receptor antagonist, dimethindene (0.1 mg/kg, i.p.), attenuated the hypothermic effect of morphine (10 mg/kg), a histamine H2 receptor antagonist, ranitidine (100 mg/kg, i.p.), had no effect [24].
• Rauwolscine also unmasked a vasodepressor response to R-(-)-alpha-methylhistamine not affected by the H3 receptor antagonist thioperamide, but counteracted by the H1 receptor antagonist dimetindene or the H2 receptor antagonist ranitidine [25].
• It is concluded from these results that dimetindene 0.1% nasal spray solution is a safe and efficient treatment option for children under 14 years suffering from seasonal allergic rhinitis [26].
• The aim of this study was to investigate the efficacy and tolerability of intranasally applied dimetindene (CAS 3614-69-5) 0.1% spray in children suffering from seasonal allergic rhinitis [26].

Analytical, diagnostic and therapeutic context of Dimetindene

• The urinary data for nine volunteers after oral administration of racemic dimethindene are presented [27].
• Mechanistic study of opposite migration order of dimethindene enantiomers in capillary electrophoresis in the presence of native beta-cyclodextrin and heptakis(2,3,6-tri-O-methyl)-beta-cyclodextrin [28].
• In comparison to placebo, dimethindene leads to a statistically significant reduction (p < 0.05) in nasal response and clinical symptoms for at least 16 h after treatment [29].
• Eight healthy male volunteers were treated i.v. with 4 mg dimetindene maleate or sodium chloride solution in a double blind, cross over study [30].
• The determination of dimethindene in human serum by enzyme-linked immunosorbent assay (EIA) [31].

References