Topic
Dimethindene
About: Dimethindene is a research topic. Over the lifetime, 58 publications have been published within this topic receiving 452 citations.
Papers published on a yearly basis
Papers
TL;DR: It is considered that some antihistamines loose their effectiveness under long-term treatment and that patients may complain about the sedative side-effects, so for maximum benefit it sometimes appears necessary to change the preparation before a choice for the individual dose is finally made.
Abstract: H1-antihistamines have been used in treatment of allergic disorders for more than 30 years. However, many of them have been employed in a less than systematic fashion. Most of the antihistamines show an apparent dual mechanism of action on isolated organs, consisting of a competitive and a non-competitive component. To induce non-competitive antagonism, higher concentrations are usually required, but for dimethindene the dose ratios for competitive and non-competitive activities differed only by less than one log unit. For therapeutic guidelines it should be considered that some antihistamines loose their effectiveness under long-term treatment and that patients may complain about the sedative side-effects. Thus, for maximum benefit it sometimes appears necessary to change the preparation before a choice for the individual dose is finally made. Under this condition they will cause relief from many allergic symptoms. Nevertheless, the classical antihistamines are without effect in bronchial asthma. The search for new drugs has been successful in this direction, as it has shown the antihistaminic/antiallergic drug Ketotifen to be able to prevent and control bronchial asthma. Many commercial preparations used in the treatment of common cold, vomitus or rhinitis contain an additive in combination with the antihistamines. Some of the additives appear to be of some value since they are used to reduce the side-effects of antihistamines. Secondary pharmacological properties of the antihistamines however provide also additional uses. This holds especially for effects on the CNS. Together with the search for the role played by histamine in the central cell-to-cell communication, new drugs might be found which will inhibit more selectively the action of histamine in the CNS.
38 citations
TL;DR: Although plasma concentrations of histamine increased significantly in three patients in the placebo group given low-dose mivacurium, the mean value for the group was unchanged, and there was no consistent correlation between haemodynamic changes, cutaneous manifestations and histamine concentrations.
Abstract: In this randomized, double-blind, placebo-controlled study, we have examined histamine release, haemodynamic and cutaneous effects of mivacurium administered in low (0.105 mg kg-1 = 1.5 x ED95) and high (0.21 mg kg-1 = 3 x ED95) doses and assessed if oral pretreatment with H1/H2 antagonists would blunt the effects of mivacurium-induced histamine release. Patients received either ranitidine 300 mg and dimethindene 0.1 mg kg-1 (H1 blocker) or placebo, orally 1 h before induction of anaesthesia. Twelve patients were allocated to each group. Although plasma concentrations of histamine increased significantly in three patients in the placebo group given low-dose mivacurium, the mean value for the group was unchanged. Plasma concentrations of histamine increased significantly in five patients in the placebo group after high-dose mivacurium and the mean value was increased. There was no consistent correlation between haemodynamic changes, cutaneous manifestations and histamine concentrations. Significant cardiovascular reactions occurred in six patients in the placebo groups and in only one patient treated with antihistamines.
31 citations
TL;DR: The determination of very low concentrations of dimethindene and N-demethyl-dimethindenes in human urine was possible using sample stacking conditions to increase the amount of analyte in the capillary with good peak forms and resolutions.
29 citations
TL;DR: The house-dust mite model in the Vienna challenge chamber proved to be a useful tool for drug investigations in mite allergies and led to a statistically significant reduction of the nasal response at both concentrations tested.
Abstract: The aim of the study was to develop a laboratory system to challenge mite allergic patients with physiological concentrations of Der p I in order to evaluate the efficacy of antiallergic drugs in mite allergic patients. A double-blind, placebo-controlled, cross-over study was designed with three consecutive sessions. Twelve patients with proven sensitivity to dust mite were treated with a single dose of dimethindene maleate in a FOAD formulation (4 and 8 mg vs. placebo) 12 h before a long-term challenge with mite allergen Der p I in the Vienna challenge chamber. Challenge was performed with a constant concentration of 40 ng Der p I per cubic meter of air for 4 h. Nasal parameters were recorded at 15 min intervals during long-term challenge. In comparison to placebo, dimethindene leads to a statistically significant reduction (p<0.05) of the nasal response at both concentrations tested. The house-dust mite model in the Vienna challenge chamber thus proved to be a useful tool for drug investigations in mite allergies
16 citations
TL;DR: The oedema disk technique was used to study the effects of orally administered H1-receptor antagonists on the inflammation induced with capsaicin or croton oil in the mouse ear, and the effect of topically applied dimethindene maleate gel on theinflammation induced with crotonOil in the mice ear.
Abstract: The oedema disk technique was used to study the effects of orally administered H1-receptor antagonists (cetirizine, chloropyramine, clemastine, cyproheptadine, dimethindene, loratadine, mequitazine and terfenadine) on the inflammation induced with capsaicin or croton oil in the mouse ear, and the effect of topically applied dimethindene maleate gel on the inflammation induced with croton oil in the mouse ear. In rats of the Wistar strain, oedema was induced in the hind paw by the subplantar injection of dextran or compound 48/80. Preliminary antihistamine treatment inhibited the development of oedema in the mouse ear, and of oedema in the rat paw, to statistically significant extents, in a dose-dependent manner. In all experiments, the most potent drugs were loratadine and cyproheptadine.
15 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2017 | 1 |
| 2014 | 1 |
| 2013 | 1 |
| 2011 | 1 |
| 2009 | 1 |
| 2008 | 1 |