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At least 19 recordsLinked to original sources
PubMed1977

Studies on the potency of various antitussive agents.

Several antitussive agents were assessed for their cough-suppressant activity. Cough responses were obtained by electrically stimulating the lower brainstem, in cats lightly anesthetized with sodium pentobarbital or in unanesthetized midcollicular decerebrate preparations. Cough sounds were recorded with the aid of a microphone. The cough reactive region was concentrated in an area dorsomedial to the trigeminal tract and nucleus. The potency of these antitussive agents (dextromethorphan, RO 21-4790-001, codeine, clonazepam, diazepam and caramiphen) were determined by studying their effect on the centrally induced cough responses. Each of these agents was administered in graded doses intravenously to determine the minimal effective doses for suppressing the cough responses. They are 0.57, 2.55, 1.71, 0.048, 0.28 and 3.18 mg/kg for the above listed drugs. The results indicate that clonazepam was found to be the most potent antitussive among these agents, the mean effective dose being about 1/35 of that of codeine. The antitussive potency of benzodiazepines is not well correlated with their muscle relaxant activity. For instance, clonazepam and diazepam have the same potency in depressing polysynaptic spinal reflexes, whereas the former is six times more potent than diazepam as an antitussive. This finding indicates that clonazepam has a high specificity as an antitussive.

Animals↗
PubMed2004

Levocloperastine in the treatment of chronic nonproductive cough: comparative efficacy versus standard antitussive agents.

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.

Adolescent↗
PubMed1982

A comparative randomized double-blind clinical trial of isoaminile citrate and chlophedianol hydrochloride as antitussive agents.

The efficacy and safety of a new centrally acting antitussive agent, isoaminile citrate, was compared with that of chlophedianol hydrochloride in a double-blind, randomized interpatient study. A total of 66 patients participated, two and four patients were lost to follow-up with isoaminile and chlophedianol, respectively. In the experimentally induced cough in 12 normal human subjects, isoaminile (40 mg) was as effective as chlophedianol (20 mg), but its duration of action was somewhat longer. One subject developed allergic skin rash with chlophedianol and was withdrawn from the study. In 60 patients with cough associated with chest diseases, isoaminile (40 mg, 3 x daily) was as effective as chlophedianol (20 mg, 3 x daily) in suppressing cough as judged from the 3-h and 24-h cough counts. The increase in PEFR at day 7 of treatment was somewhat more marked with chlophedianol as compared with isoaminile. None of the drugs interfered with the expectoration process. The side effects observed were few, mild in nature, and did not require a decrease in dose or withdrawal of treatment in any of the patients. Isoaminile citrate was concluded to be an effective and relatively safe antitussive agent. Isoaminile citrate, alpha(isopropyl)-alpha-(beta-dimethylaminoproyl) phenylacetonitrile citrate, is a centrally acting antitussive agent. In animal experiments this drug was as efficacious as codeine but was devoid of any respiratory depressant effect [Krause 1958, Kuroda et al. 1971]. This controlled double-randomized interpatient study was designed to test the comparative efficacy and safety of isoaminile and chlophedianol, another centrally acting antitussive, in humans.

Acetonitriles↗
PubMed2005

Effects of antitussive agents administered before bronchoalveolar lavage in horses.

OBJECTIVE: To determine whether treatment of horses with antitussive agents before bronchoalveolar lavage (BAL) reduces the frequency and intensity of the cough reflex during BAL. ANIMALS: 8 healthy horses. PROCEDURE: Standard BAL was performed on each horse weekly for 6 weeks. Detomidine was used as a general sedative, and various antitussive agents were evaluated for their suitability to suppress undesirable coughing. Treatments administered prior to BAL consisted of saline (0.9% NaCl) solution (control treatment), codeine, butorphanol tartrate, glycopyrrolate, lidocaine hydrochloride (final concentration, 0.33%), and lidocaine hydrochloride at a final concentration of 0.66% (lidocaine 0.66%). Frequency and intensity of coughing were digitally recorded throughout the BAL procedure. The volume of BAL fluid collected was measured, and the fluid was cytologically examined to assess potential effects of the medications on composition. RESULTS: Coughing frequency was significantly reduced after intratracheal administration of lidocaine 0.66%. Moreover, intratracheal administration of lidocaine 0.66% or IV administration of butorphanol resulted in a significant reduction in the intensity of coughing episodes. All other treatments failed to significantly suppress coughing frequency and intensity, compared with results for the saline treatment. Glycopyrrolate caused obvious adverse clinical effects. Treatments did not influence the volume of BAL fluid collected nor composition of the fluid. CONCLUSIONS AND CLINICAL RELEVANCE: Intratracheal administration of lidocaine (final concentration, 0.66%) proved to be the most reliable method to reduce frequency and intensity of coughing in horses during BAL.

Animals↗
PubMed1995

N-acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate.

The synthesis of a novel class of antitussive agents is described. The compounds were examined for antitussive activity in guinea pig after cough induction by electrical or chemical stimulation. Ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate (BBR 2173, moguisteine, 7) and other structurally related compounds showed a significant level of activity, comparable to that of codeine and dextromethorphan. The compounds presented in this paper are characterized by the N-acyl-2-substituted-1,3-thiazolidine moiety, which is a novel entry in the field of antitussive agents. The serendipitous discovery of the role played by the thiazolidine moiety in determining the antitussive effect promoted extensive investigations on these structures. This optimization process on N-acyl-2-substituted-1,3-thiazolidines led to the initial identification of 2-[(2-methoxypheoxy)methyl]-3-[2-(acetylthio)acetyl]- 1,3-thiazolidine (18a) as an interesting lead compound. The careful study of the rapid and very complicated metabolism of 18a provided further insights for the design of newer related derivatives. The observation that the metabolic oxidation on the lateral chain's sulfur of 18a to sulfoxide maintained the antitussive properties suggested the introduction of isosteric functional groups with respect to the sulfoxide moiety. Subsequent structural modifications showed that hydrolyzable malonic residues in the 3-position of the thiazolidine ring were able to assure high antitussive activity. This optimization ultimately led to the selection of moguisteine (7) as the most effective and safest representative of the series. Moguisteine is completely devoid of unwanted side effects (such as sedation and addiction), and its activity was demonstrated also in clinical studies.

Animals↗
PubMed1985

[Objectivation of the effect of antitussive agents using tussometry in patients with chronic cough].

The antitussive effect of several antitussive agents has been objectively evaluated in patients with chronic stable cough due to bronchial carcinoma, pulmonary tuberculosis or chronic obstructive lung disease. The patients received the active antitussive drugs or placebo in a double-blind, randomized crossover design. The preparations were administered at 10 p.m. and 2 a.m. on 7 consecutive nights and no antitussive was given for the following 20 hours. Cough frequency and intensity were recorded from 10 p.m. until 6 a.m. The active medications were noscapine (30 mg), dextromethorphan (20 mg), dihydrocodeine (30 mg) and codeine (20, 30 and 60 mg) at 10 p.m. and 2 a.m. Cough frequency and intensity were objectively assessed with a pressure transducer placed over the trachea and recorded on a chartrecorder. Statistical analysis was performed with analysis of variance and multiple range testing. Noscapine, dextromethorphan, dihydrocodeine and codeine (60 mg) significantly (p less than 0.001) reduced the cough frequency compared to placebo. They also produced a greater reduction of cough intensity than placebo, codeine (20 mg) and codeine (30 mg) (p less than 0.001). The duration of action of low-dose codeine (6 hours) was unsatisfactory. Subjective preference for dextromethorphan indicates a psychotropic central nervous action of this drug not assessed by the measuring device. Noscapine was equally well tolerated but more neutral psychologically.

Adult↗