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Showing papers on "Antitussive Agent published in 1992"


Patent
24 Mar 1992
TL;DR: In this paper, the authors describe pharmaceutical compositions for use in the treatment of pain and inflammation and the relief of cough and cold symptoms in a mammalian organism, said composition comprising: (i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ib uprofen; and (ii) an antitussively effective amounts of at least one antitussive agent selected from codeine, hydrocodone, caramiphen, carabetapentane, or dextrometh
Abstract: This invention relates to pharmaceutical compositions for use in the treatment of pain and inflammation and the relief of cough and cold symptoms in a mammalian organism, said composition comprising: (i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ibuprofen; and (ii) an antitussively effective amount of at least one antitussive agent selected from codeine, hydrocodone, caramiphen, carbetapentane, or dextromethorphan, or a therapeutically active stereoisomer thereof substantially free of its other stereoisomers and optionally (iii) a therapeutically effective amount of at least one expectorant selected from guaicolsulfonate, guaifenesin, guaiacol, or terpin; or a pharmaceutically acceptable salt thereof.

60 citations


Journal ArticleDOI
TL;DR: It is suggested that Ca2+ channels play an important role in the regulation of the cough reflex and markedly increased the antitussive effects of morphine, dihydrocodeine and dextromethorphan.

34 citations


Patent
28 May 1992
TL;DR: In this paper, a method for increasing the effectiveness of dextromethorphan (DM) as an antitussive agent (i.e., as a cough suppressant) is described.
Abstract: This invention discloses a method for increasing the effectiveness of dextromethorphan (DM) as an antitussive agent (i.e., as a cough suppressant). This method involves the concurrent administration of DM and a second agent which inhibits the oxidative activity of debrisoquin hydroxylase, a cytochrome P450 oxidase enzyme. Effective anti-oxidant compounds include quinidine, yohimbine, and fluoxetine.

32 citations



Journal Article
TL;DR: The results suggest that the effect of central acting antitussive drugs were mediated by increase of 5-HT release in the brainstem, particularly in the NTS.
Abstract: The effects of antitussive drugs on the release of [3H]5-hydroxytryptamine ([3H]5-HT) were investigated in slices prepared from rat nucleus of the solitary tract (NTS) and depolarized with 30 mM KCl under superfusion conditions. Dihydrocodeine and dextromethorphan, both central acting antitussive drugs, significantly increased the release of [3H]5-HT from slices of the rat NTS. Furthermore, these antitussive drugs significantly increased the rate of turnover of the 5-HT in the brainstem. These results suggest that the effect of central acting antitussive drugs were mediated by increase of 5-HT release in the brainstem, particularly in the NTS.

27 citations


Journal ArticleDOI
TL;DR: The results suggest that haloperidol-sensitive σ-sites may be involved in the regulation of coughs.

15 citations


Patent
20 Jul 1992
TL;DR: In this article, a method of treating or preventing motion sickness is disclosed which comprises administering an anti-motion sickness effective amount of anticonvulsant compound such as phenytoin, ethotoin, primidone, ethosuximide or carbamazepine, in combination with a potentiating amount of an antitussive or cough suppressant agent such as dextromethorphan, levopropoxyphene, muscaphene, pholocodeine, or carbetapentene.
Abstract: A method of treating or preventing motion sickness is disclosed which comprises administering an anti-motion sickness effective amount of an anticonvulsant compound such as phenytoin, ethotoin, primidone, ethosuximide or carbamazepine, in combination with a potentiating amount of an antitussive or cough suppressant agent such as dextromethorphan, levopropoxyphene, muscaphene, pholocodeine, or carbetapentene. The antitussive compounds of the present invention act as potentiating agents so as to enable effective treatment or prevention of motion sickness using a reduced amount of the anticonvulsant compound normally used in such treatment. The method of the present invention reduces the potential for various side effects and thus provides a safer and more effective method of treatment for motion sickness than prior art methods.

9 citations


Journal Article
TL;DR: Since the comparative antitussive potency of the two drugs in clinical experimental models has not been evaluated, the authors performed a randomized, double blind, cross over investigation in which the effects of single oral doses of levodroPropizine and dropropizine were assessed by using the citric acid-induced cough model.
Abstract: Levodropropizine is the levo-rotatory (S)-enantiomer of dropropizine, a racemic non-opiate antitussive agent which has been used clinically for many years. Compared with the racemic drug, levodropropizine exhibits in animal models similar antitussive activity but considerably lower central nervous system (CNS) depressant effects. It is also less likely to cause sedation in treated patients. Since the comparative antitussive potency of the two drugs in clinical experimental models has not been evaluated, the authors performed a randomized, double blind, cross over investigation in which the effects of single oral doses (60 and 90 mg) of levodropropizine and dropropizine were assessed by using the citric acid-induced cough model in eight normal volunteers. Stimulation tests involved inhalation of individual cumulative doses of citric acid (6.3 to 53.3 mg) which at pre-study assessment had been found to induce reproducibly at least ten coughs over a 30 sec period. Each subject was studied by repeating the citric acid stimulation test four times (0 h, 1 h, 2 h and 6 h) on each of five different days separated by intervals of at least three days. In the absence of drug administration (control session), cough response to citric inhalation was remarkably reproducible throughout the 6 h period of observation. A marked and statistically significant reduction in cough response (to about one third--one sixth of the pre-drug values) was observed 1 h after intake for both compounds. At subsequent testing 2 h and 6 h after dosing, cough response was still depressed and did not differ significantly from that observed at 1 h.(ABSTRACT TRUNCATED AT 250 WORDS)

8 citations


Journal Article
TL;DR: When co-administered intracisternally, the selective delta-opioid agonist DPDPE consistently and significantly decreased the antitussive potencies of kappa-receptor agonists, U-50,488H and U-62,066E.
Abstract: When co-administered intracisternally, the selective delta-opioid agonist [D-Pen2,5]enkephalin (DPDPE), which had no significant effect on the cough reflex, consistently and significantly decreased the antitussive potencies of kappa-receptor agonists, U-50,488H and U-62,066E. The decrease in the antitussive effects of these kappa-receptor agonists caused by DPDPE were prevented by selective delta receptor antagonist, naltrindole. These results suggest that delta receptors may play an inhibitory role in antitussive processes that are mediated by the kappa-receptors.

5 citations



Patent
10 Jun 1992
TL;DR: A powdery pharmaceutical preparation for the nasal cavity is obtained by dispersing and comprising one or two or more of an antiphlogistic steroidal agent, an analgesic and antiph logistic agent, antitussive agents, an antihistaminic agent and a medicine having antiallergic actions.
Abstract: PURPOSE:To obtain a powdery pharmaceutical preparation for the nasal cavity capable of sticking and staying in a nasal mucous membrane for a prescribed time and efficiently releasing a medicine by blending tamarind gum or xanthan gum with the medicine. CONSTITUTION:This powdery pharmaceutical preparation for the nasal cavity is obtained by dispersing and comprising one or two or more of an antiphlogistic steroidal agent, an analgesic and antiphlogistic agent, antitussive agents, an antihistaminic agent and a medicine having antiallergic actions, etc., in tamarind gum or xanthan gum and preparing the resultant dispersion into a powdery form. The administration thereof is carried out by scattering the pharmaceutical preparation in the form of a powder, a fine granule or a granule on a lesion or a mucous membrane in the nasal cavity or spraying the pharmaceutical preparation by using a suitable tool. Although a conventional ointment or jelly for the nasal cavity is difficult to administer into the depth in the nasal cavity and a nasal drop or a spray is difficult to retain the medicine in the nasal cavity for a prescribed time, this pharmaceutical preparation is suitable for administration into the nasal cavity. The medicine is blended in an amount of 0.001-10wt.% in the pharmaceutical preparation in the case of the medicine which is the antiphlogistic steroidal agent and 0.01-80wt.% in the pharmaceutical preparation in the case of the medicine that is the analgesic and antiphlogistic agent, the antitussive agent, the antihistaminic agent or the medicine having the antiallergic actions.