Topic
Antitussive Agent
About: Antitussive Agent is a research topic. Over the lifetime, 380 publications have been published within this topic receiving 5776 citations.
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TL;DR: The results indicate that the antitussive effect of WIN 55212-2 is mediated by the activation of cannabinoid CB(1) receptors and mu(2) (naloxonazine-insensitive)-opioid receptors, but not mu (1) ( nalox onazine-sensitive)- or kappa-opioids receptors.
16 citations
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TL;DR: Findings suggested that CA-Ver deserved attention for its potent antitussive effects related to the central opioid receptors, but without addiction, and had a good development perspective.
Abstract: The purpose of this work was to search for potential drugs with potent antitussive and expectorant activities as well as a low toxicity, but without addictive properties. Cholic acid-verticinone ester (CA-Ver) was synthesized based on the clearly elucidated antitussive and expectorant activities of verticinone in bulbs of Fritillaria and different bile acids in Snake Bile. In our previous study, CA-Ver showed a much more potent activity than codeine phosphate. This study was carried out to investigate the central antitussive mechanism and the addictive evaluation of CA-Ver. Testing on a capsaicin-induced cough model of mice pretreated with naloxone, a non-selective opioid receptor antagonist, was performed for the observation of CA-Ver's central antitussive mechanism. We then took naloxone-induced withdrawal tests of mice for the judgment of CA-Ver's addiction. Lastly, we determined the opioid dependence of CA-Ver in the guinea pig ileum. The test on the capsaicin-induced cough model showed that naloxone could block the antitussive effect of CA-Ver, suggesting the antitussive mechanism of CA-Ver was related to the central opioid receptors. The naloxone-urged withdrawal tests of the mice showed that CA-Ver was not addictive, and the test of the opioid dependence in the guinea pig ileum showed that CA-Ver had no withdrawal response. These findings suggested that CA-Ver deserved attention for its potent antitussive effects related to the central opioid receptors, but without addiction, and had a good development perspective.
16 citations
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30 Apr 1985TL;DR: In this paper, N-monosubstituted and N,N-disubstitized amides of the 1-methyl-5-p-toluoylpyrrole-2-acetic acid, which are active as antiinflammatory, analgesic, antipyretic, antisecretive and antitussive agents, are disclosed.
Abstract: N-monosubstituted and N,N-disubstituted amides of the 1-methyl-5-p-toluoylpyrrole-2-acetic acid, which are active as antiinflammatory, analgesic, antipyretic, antisecretive and antitussive agents, are disclosed. These amides are prepared by reacting an amine with an activated derivative of the 1-methyl-5-p-toluoylpyrrole-2-acetic acid of formula ##STR1## wherein X is an activating group suitable for promoting the formation of an amide bond.
16 citations
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TL;DR: Some of the new synthetic compounds discussed in this review have demonstrated antitussive activity equivalent to that of codeine and are replacing the older narcotic preparations in the symptomatic management of cough.
Abstract: The cough reflex as part of an integrated protective mechanism for adequate bronchoelimination is vital in maintaining the integrity of the pulmonary parenchyma. While it is undoubtedly true that more patients have died from an inability to cough effectively than from the act of coughing itself, adequate control of useless cough is often necessary in order to preserve the health and wellȁbeing of the patient. Until recently, cough mixtures were compounded empirically and assessed clinically on the basis of subjective response. Based upon physiologic and pharmacologic studies on the mechanics and regulation of the cough reflex together with the development of new techniques for eliciting a reproducible cough with graded stimuli in animals and man, quantitative objective studies of antitussive activity are now possible. This has stimulated the search for new compounds devoid of the analgesic and narcotic properties of the opium derivatives. Some of the new synthetic compounds discussed in this review have demonstrated antitussive activity equivalent to that of codeine and are replacing the older narcotic preparations in the symptomatic management of cough.
16 citations
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TL;DR: Levocloperastine is an effective antitussive agent for the treatment of cough in patients of all ages with a more rapid onset of action than standard agents with an improved tolerability profile.
Abstract: The medical and social impact of cough is substantial. Current antitussive agents at effective doses have adverse events such as drowsiness, nausea and constipation that limit their use. There is also recent evidence that standard antitussive agents, such as codeine, may not reduce cough during upper respiratory infections. Therefore, there is a need for more effective and better-tolerated agents. The efficacy of levocloperastine, a novel antitussive, which acts both centrally on the cough center and on peripheral receptors in the tracheobronchial tree in treating chronic cough, was compared with that of other standard antitussive agents (codeine, levodropropizine and DL-cloperastine) in six open clinical trials. The studies enrolled patients of all ages with cough associated with various respiratory disorders including bronchitis, asthma, pneumonia and chronic obstructive pulmonary disease. Levocloperastine significantly improved cough symptoms (intensity and frequency of cough) in all trials, and improvements were observed after the first day of treatment. In children, levocloperastine reduced nighttime awakenings and irritability, and in adults it was effective in treating cough induced by angiotensin-converting enzyme inhibitors. When compared with other antitussive agents, levocloperastine had improved or comparable efficacy, with a more rapid onset of action. Importantly, no evidence of central adverse events was recorded with levocloperastine, whereas drowsiness was reported by a significant number of patients receiving codeine. Levocloperastine is an effective antitussive agent for the treatment of cough in patients of all ages. It has a more rapid onset of action than standard agents with an improved tolerability profile.
16 citations