Search results for "anticholinergic"

Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole

1988

Abstract The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. 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. 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. The potency of mequitazine and clemizole as H1-histamine blockers is similar, but only mequitazine at highest concentration used showed anticholinergic a…

Aclidinium inhibits human lung fibroblast to myofibroblast transition

2011

Background Fibroblast to myofibroblast transition is believed to contribute to airway remodelling in lung diseases such as asthma and chronic obstructive pulmonary disease. This study examines the role of aclidinium, a new long-acting muscarinic antagonist, on human fibroblast to myofibroblast transition. Methods Human bronchial fibroblasts were stimulated with carbachol (10 −8 to 10 −5  M) or transforming growth factor-β1 (TGF-β1; 2 ng/ml) in the presence or absence of aclidinium (10 −9 to 10 −7  M) or different drug modulators for 48 h. Characterisation of myofibroblasts was performed by analysis of collagen type I and α-smooth muscle actin (α-SMA) mRNA and protein expression as well as α…

Alterations on AChE Activity of the Fish Anguilla anguilla as Response to Herbicide-Contaminated Water

2000

Abstract The inhibition of both total and specific acetylcholinesterase activities was measured in the whole eyes of the yellow eel Anguilla anguilla after exposure to the carbamate thiobencarb. In vivo assays were conducted under a constant flow-through system of thiobencarb-contaminated water (1/60 LC50 96 h=0.22 ppm for 96 h) followed by a recovery period in clean water (192 h more). The results indicated a measurable level of AChE activity on eyes of control eels, which resulted in a sensitive indicator of the presence of thiobencarb in the water. The pesticide induced significant inhibitory effects on AChE activity ranging from 35% in total AChE activity to 75% in specific AChE activit…

Tiotropium - ein langwirksames, inhalatives Anticholinergikum zur Therapie der chronisch-obstruktiven Lungenerkrankung (COPD)

2003

Anticholinergics are agents of first choice for the symptomatic treatment of patients with COPD. Tiotropium (Ba 679 BR, Spiriva) is a long-acting inhaled anticholinergic designed for once-daily bronchodilator treatment of COPD. Tiotropium is a selective antagonist of pulmonary M1 and M3 muscarinic receptor subtypes, that produces a long-lasting (24 hours), dose-dependent bronchodilation and bronchoprotection against constrictive stimuli, e. g. methacholine, following inhalation of single doses. Clinical trials with tiotropium in COPD patients over a maximum treatment duration of one year have confirmed a persisting bronchodilator effect of tiotropium compared with placebo and ipratropium, a…

Antimuscarinic action of quinidine on the heart? A study in myocardial preparations from cat hearts

1984

Quinidine exerts anticholinergic effects which have been ascribed to atropine-like properties of the drug. We have examined the effects of acetylcholine on the force of contraction in isolated heart muscle preparations from cats and compared the inhibitory effects of atropine with those of quinidine. The effects of acetylcholine were antagonized competitively in the presence of atropine. The Schild-plot yielded a straight line; the slope was not significantly different from unity. In the presence of quinidine, the concentration-response curve of acetylcholine was shifted to the right as with atropine, however, the Schild-plot yielded a regression line which was not linear; the slope was sta…

Enzephalopathie nach Intoxikation mit einem Anticholinergikum

2008

A 55-year-old chemical laboratory technician developed mydriasis and ocular hypertension, which lasted for 6 weeks, after synthesizing several kilograms of a scopolamine-related test agent with anticholinergic action and then decanting a powdery intermediary substance, the dust of which he may have inhaled. Six weeks later he suddenly had symptoms of an acute intoxication while synthesizing a scopolamine-related substance. The anticholinergic delirium regressed completely within one day requiring no treatment. But subsequently he developed symptoms of a toxic encephalopathy. This only partially regressed over the following 3 years. Its probable cause is thought to have been either the manif…

β₂ long-acting and anticholinergic drugs control TGF-β1-mediated neutrophilic inflammation in COPD.

2012

Effects of aclidinium on determinants of COPD severity: symptoms and quality of life

2016

Marco Contoli,1 Paolo Solidoro,2 Fabiano Di Marco,3,4 Nicola Scichilone,5 Angelo Corsico,6 Fulvio Braido,7 Pierachille Santus4,8 1Research Centre on Asthma and COPD, Department of Medical Sciences, University of Ferrara, Ferrara, Italy; 2Cardiovascular and Thoracic Department, Città della Salute, Turin, Italy; 3Department of Health Sciences, University of Milan, Milan, Italy; 4Respiratory Unit, San Paolo Hospital, Milan, Italy; 5Department of Internal Medicine, Section of Pulmonology (DIBIMIS), University of Palermo, Palermo, Italy; 6Department of Molecular Medicine, Fondazione IRCCS Policlinico San Matteo, Pavia, Italy; 7Allergy and Respiratory Diseases Clinic, DIMI, University of G…

1012 – Evaluation of a risk-scale for anticholinergic side-effects in elderly psychiatric inpatients

2013

Introduction Many commonly prescribed drugs have anticholinergic properties which can induce side-effects e.g. delirium, especially in an ageing brain with increased sensitivity. Risk-assessment before starting therapy may prevent such sideeffects. Objectives We rated anticholinergic pharmacological properties of prescribed medication and compared the theoretical risk with side-effects in clinical practice. Aims The scale should improve the safety of pharmacotherapy in gerontopsychiatry. Methods Based on five publications that considered anticholinergic properties of drugs, a risk-scale was established. Riskpoints for all drugs were summarized to a total score. Patients were selected from T…

Alternative mechanisms for tiotropium

2009

Tiotropium is commonly used in the treatment of chronic obstructive pulmonary disease. Although largely considered to be a long-acting bronchodilator, its demonstrated efficacy in reducing the frequency of exacerbations and preliminary evidence from early studies indicating that it might slow the rate of decline in lung function suggested mechanisms of action in addition to simple bronchodilation. This hypothesis was examined in the recently published UPLIFT study and, although spirometric and other clinical benefits of tiotropium treatment extended to four years, the rate of decline in lung function did not appear to be reduced by the addition of tiotropium in this study. This article summ…