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Showing papers on "Antitussive Agent published in 1977"


Journal ArticleDOI
TL;DR: The synthesis of a novel series of antitussive agents was described and the 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine.
Abstract: The synthesis of a novel series of antitussive agents is described. Two series of amino-substituted tetra- and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve. A significant level of activity, comparable with that of codeine, was found in the 4alpha-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine. The effects of structural modification upon antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28.

18 citations


Journal ArticleDOI
TL;DR: Clonazepam was found to be the most potent antitussive among these agents, the mean effective dose being about 1/35 of that of codeine.
Abstract: 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.

15 citations


Journal Article
TL;DR: The antitussive effect of two different drugs A (Codeine, Phenyltoloxamine) and B (Dihydrocodeine, Remedacen) was compared in a double blind clinical trial by measuring the frequency and strength of cough attacks for 7 hours.
Abstract: The antitussive effect of two different drugs A (Codeine, Phenyltoloxamine) and B (Dihydrocodeine, Remedacen) was compared in a double blind clinical trial by measuring the frequency and strength of cough attacks for 7 hours. The cough attacks were measured by a pressure-monitoring device which was externally fastened to the throat. Drug B suppressed the strenght and frequency for at least 9 hours after application while the effectiveness of drug A lasted only for about 6 hours after application. In any case the respiratory drive was unaffected.

4 citations


01 Aug 1977
TL;DR: Nine cough mixtures available on the Swiss market and randomly chosen were tested telemetrically and with the exception of Sinecod all syrups effected immediate and long-lasting pH-depressions in interdental plaque.
Abstract: Nine cough mixtures available on the Swiss market and randomly chosen were tested telemetrically. With the exception of Sinecod all syrups effected immediate and long-lasting pH-depressions in interdental plaque. Patients should be informed on the pronounced caries-promoting potential of these medications.

2 citations



Journal ArticleDOI
TL;DR: In this paper, a series of amino-substituted tetra-and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve.
Abstract: The synthesis of a novel series of antitussive agents is described. Two series of amino-substituted tetra- and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve. A significant level of activity, comparable with that of codeine, was found in the 4alpha-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine. The effects of structural modification upon antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28.