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PubMed1985

[The anti-inflammatory effect of a combination of dimethindene maleate and betamethasone in topical formulations].

The antiinflammatory activity of three preparations (cream, ointment, jelly) of Fenistil Plus (betamethasone + dimethindene maleate) was shown by means of reflection densitometry, a new pharmacodynamic model. The three preparations led to restitution of the Tesafilm-stripped skin within 4 h. There was no significant difference in the efficacy of the preparations. After application of 10 g of the ointment the plasma levels of betamethasone remained within the limits of identification of the analytical method. An influence of the drug on the endogenous plasma hydrocortisone (cortisol) levels could not be found.

Administration, Topical↗
PubMed1999

Cutaneous responses to substance P and calcitonin gene-related peptide in chronic urticaria: the effect of cetirizine and dimethindene.

BACKGROUND: Neuropeptides appear to participate in the pathogenesis of chronic urticaria. The purpose of this study was to investigate the cutaneous responses to substance P (SP) and calcitonin gene-related peptide (CGRP) in delayed pressure urticaria patients (DPUpt) and chronic idiopathic urticaria patients (CIUpt) compared to healthy adults (HA), and also to evaluate the effect of H1-antagonists on these responses. METHODS: Wheal (W) and flare (F) reactions to intradermally (ID) injected SP, CGRP, histamine (H), and diluent controls were evaluated in nine CIUpt, nine DPUpt, and nine HA at 3, 7, 15, 30, 60, and 120 min after injection. 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. RESULTS: CIUpt exhibited enhanced and longer lasting W reactions to SP and CGRP (AUC: P<0.05) than HA; SP- and CGRP-induced F (at maximal concentration) were larger and longer lasting in CIUpt than in HA (P<0.003 and P = 0.004, respectively). In the DPU group, SP-induced W and F responses were intermediate in magnitude compared to CIUpt and HA. In HA, SP-induced flares were significantly suppressed only by Ce (P<0.020), while both Ce and Di affected SP-induced W and F in the two patient groups (P<0.05). CGRP-induced flare inhibition by the two H1-antagonists was also greater in the urticaria patient groups than in HA. CONCLUSIONS: CIUpt and, to a lesser extent, DPUpt showed enhanced SP- and CGRP-induced W and F reactions. CGRP elicited an immediate W and F response, followed by prolonged erythema. H1-antagonists partially affected W and F reactions to SP and only the F response induced by CGRP; this effect was more pronounced in the urticaria patient groups than in HA. Overall, W and F cutaneous responses to SP were suppressed to a greater extent by Ce than Di.

Adult↗
PubMed1986

Effects of chloropyramine, dimethindene and diphenhydramine on transepithelial ion transport: studies in bovine tracheal epithelium and frog skin.

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. The short-circuit current I0 across bovine tracheal epithelium is the sum of active secretion of Cl- and absorption of Na+. In this tissue, all three drugs induced a reversible, dose-related inhibition of I0, up to 100%. The concentrations giving 50% of maximal effect were 1.4 X 10(-4) M for chloropyramine, 2.0 X 10(-4) M for dimetindene and 2.5 X 10(-4) M for diphenhydramine. The effect was unrelated to the agonist binding site of H1-receptors of histamine, since it was not altered in the presence of 10(-3) M histamine. Experiments in which Na+ transport was selectively reduced by 5 X 10(-5) M amiloride, or in which Cl- transport was selectively abolished by 10(-3) M furosemide, 10(-4) M bumetanide or Cl- removal, indicated that Na+ and Cl- transports were equally affected by the drugs. The action of chloropyramine was composed of an early inhibition of Na+ and Cl- movements, followed by a slow recovery of Cl- secretion. In frog skin, each one of the three H1-antagonists modified the I0, following two main patterns of response, a stimulation at the lower concentrations tested, or an inhibition at higher concentrations. Dose-response relationships were obscured by a large variability in response of individual skins. These observations in bovine tracheal epithelium and frog skin suggest that H1-antagonists might alter the functioning of other epithelia as well.

Animals↗
PubMed1996

[Decongestant nasal spray. Results of a rhinomanometric double-blind study].

Between november 1993 and july 1995 60 patients with a common cold underwent randomized and double-blind testing of 3 commercial nasal sprays-benzydamine, xylometazoline combined with the secretolytic S-carboxymethylcysteine, and phenylephrine combined with the antihistaminic dimethindene maleate. After prior active rhinomanometric measurement of the untreated nose, the test substance was applied. The change of nasal patency was registered after 3 and 10 minutes and then after 2, 4, 6 and 8 hours. At the end the patient gave a subjective evaluation of the used spray. There was no change in nasal obstruction following application of NaCl or benzydamine. Xylometazoline/S-carboxymethylcysteine (+87%) or phenylephrine/ dimethindene maleate (+113%) augmented nasal patency within minutes. Using phenylephrine/dimethindene maleate the effect lasted less than 2 hours, while after xylometazoline/S-carboxymethylcysteine decongestion lasted more than 6 hours. The patients also subjectively reported an increase in nasal patency after the use of benzydamine and placebo. But only phenylephrine/ dimethindene maleate or xylometazoline/S-carboxymethylcysteine were judged good. Using benzydamine or phenylephrine + dimethindene maleate, more side-effects (mainly dryness and burning) were mentioned. Considering the subjective assessment of side-effects and duration of action, as well as objective parameters, derivatives of imidazole (oxymetazoline and xylometazoline) are first choice in treatment of the common cold.

Administration, Intranasal↗
PubMed1995

The design and pharmacology of novel selective muscarinic agonists and antagonists.

The muscarinic pharmacology of C1-methyl-substituted chiral compounds related to McN-A-343 and of (R)- and (S)-dimethindene has been studied. Among the McN-A-343 analogues, the (S)-enantiomers were more potent and had higher affinity than the (R)-isomers. The quaternary compound (S)-BN 228 was found to be the most potent M1-selective agonist known today (pEC50: M1/rabbit vas deferens = 7.83; M2/guinea-pig atria = 6.35; M3/guinea-pig ileum = 6.29). In both the atria and ileum the tertiary carbamate, (S)-4-F-MePyMcN, was a competitive antagonist (pA2 value = 7.39 and 6.82, respectively). In contrast, in rabbit vas deferens (S)-4-F-MePyMcN was a potent partial agonist (pEC50 = 7.22; apparent efficacy = 0.83). These results indicate that (S)-4-F-MePyMcN might be a useful tool to study M1 receptor-mediated effects involved in central cholinergic function. (S)-Dimethindene was a potent M2-selective antagonist (pA2 = 7.86/atria; pKi = 7.8/rat heart) with lower affinities for the M1 (pA2 = 6.36/rat duodenum; pKi = 7.1/NB-OK 1 cells), M3 (pA2 = 6.92/guinea-pig ileum; pKi = 6.7/rat pancreas) and M4 receptors (pKi = 7.0/rat striatum). It was more potent (up to 41-fold) than the (R)-isomer. In contrast, the stereoselectivity was inverse at ileal H1 receptors (pA2: (R)-isomer = 9.42; (S)-isomer = 7.48). Thus, (S)-dimethindene could be a valuable agent to test the hypothesis that M2 antagonists show beneficial effects in the treatment of cognitive disorders. It might also become the starting point for the development of diagnostic tools for quantifying M2 receptors in the CNS with PET imaging.

(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethy↗
PubMed2005

Antimuscarinic agents exhibit local inhibitory effects on muscarinic receptors in bladder-afferent pathways.

OBJECTIVES: To investigate the potential of antimuscarinic agents for sensory mechanisms in overactive bladder using intravesical instillation. METHODS: Antimuscarinic agents were instilled intravesically in rats using two protocols. In the high-dose protocol, 5 mg atropine, oxybutynin, and dimethindene (M2-selective muscarinic receptor antagonist) were instilled into the bladder, and cystometric parameters, such as bladder capacity, intercontraction interval, pressure threshold, and maximal voiding pressure were monitored. In the low-dose protocol, 0.1 and 0.5 mug/mL oxybutynin, trospium, tolterodine, and dimethindene were continuously infused into the bladder. The doses chosen were based on the calculated urine-excreted concentrations of trospium typically achieved from human oral treatment of 40 mg/day. The effect of carbachol with and without the low-dose agents was then assessed. RESULTS: With the high-dose protocol, bladder capacity, intercontraction interval, and pressure threshold were increased when atropine and oxybutynin were instilled, but not when dimethindene was used. The maximal voiding pressure was not affected by any of the agents tested. In the low-dose protocol, none of the cystometric parameters were altered with antimuscarinic agents alone. The intercontraction interval decreased with intravesical carbachol (65% +/- 0.1% compared with baseline), but this was prevented with concomitant antimuscarinic agents. CONCLUSIONS: We have separated the local inhibitory effects of antimuscarinic agents during the storage phase from a decrease in voiding pressure. Intravesical instillation of antimuscarinic agents at clinically meaningful concentrations also suppressed carbachol-induced bladder overactivity. Antimuscarinic agents may be effective in treating overactive bladder, not only by suppression of muscarinic receptor-mediated detrusor muscle contractions, but also by blocking muscarinic receptors in bladder-afferent pathways.

Acetylcholine↗
PubMed1995

Effect of H1-antagonism on cardiovascular, pulmonary, and immunological dysfunction in porcine endotoxic shock.

The definite role of histamine in early hyperdynamic septic shock is not yet clear. Therefore a randomized, controlled, blind trial was performed to investigate the effect of the H1-antagonist dimethindene in hyperdynamic porcine shock. Lipopolysaccharide (LPS) infusion (5 micrograms/kg/h) in anesthetized pigs (n = 6) in the control-group induced a hyperdynamic shock state with a decrease in mean arterial blood pressure, and systemic vascular resistance (SVR), and an increase in mean arterial pulmonary pressure and pulmonary vascular resistance (PVR). In the verum group (n = 6) dimethindene (2 mg/kg) administered 15 min before LPS application prevented the decrease in SVR significantly (p < .05) and ameliorated the increase in MPAP and PVR. The impairment in pulmonary function, as measured by the oxygenation ratio (PaO2/FiO2) in LPS-treated animals, was reduced by the H1-antagonist (p = .01). 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). The increase in tumor necrosis factor alpha by LPS infusion was not influenced by H1-antagonist pretreatment. The early decrease in SVR did not correlate with an enhanced nitric oxide formation, as measured by nitrate/nitrite plasma levels.

Animals↗