Paper
Chlophedianol Hydrochloride: A New Antitussive Agent.
Published Dec 17, 1960 · E. M. Boyd, C. E. Boyd
Canadian Medical Association journal
4
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Abstract
DURING THE past several years, methods have been devised for the evaluation of potential antitussive agents by measuring their ability to inhibit cough induced experimentally in animals and man.' In these screening techniques, cough is produced in man and animals by devices such as inhalation of standardized irritant vapours, e.g. citric acid aerosols. Cough or cough-like movements can be produced in animals also by mechanical or electrical stimulation of the tracheobronchial mucosa or by stimulation of the superior laryngeal nerve. These impulses are carried to the cough centre, which was located in the dorsolateral region of the medulla oblongata by Borison and his associates of Salt Lake City, Utah, in 1956.2 By these screening methods, several agents have been found to have antitussive properties and at the same time to be free of narcotic effects. Of these, benzonatate (Tessalon), carbetapentane citrate (Toclase), dextromethorphan hydrobromide (Romilar), and noscapine (Nectadon) have beeni accepted for inclusion in N.N.D. 1960 by the Council on Drugs of the American Medical Association.3 Chlophedianol hydrochloride is an antitussive agent of this type. Chlophedianol hydrochloride may be described chemically as 1-phenyl-l-(o-chlorophenyl)-3-dimethylamino-propanol-1 hydrochloride. It has the structure shown in Fig. 1. The structure-activity relationships were reported in 1958 by Gosswald,4 who found chlophedianol to have the greatest antitussive effect (against cough induced in guinea pigs by inhalation of citric acid spray) of a series of substituted diphenylaminopropanols. Structurally, chlophedianol is somewhat related to diphenhydramine (Benadryl). It is a white crystalline powder, soluble in water and alcohol. It was introduced in Germany by Farbenfabriken Bayer as Detigon, an alcoholic solution containing 50 mg. of chlophedianol hydrochloride per ml.t The antitussive dosage recommended for adults by zur Linden5 is equivalent to 25 mg. of chlophedianol hydrochloride every four to eight hours. It has been used in tablet form by Schwerdtfeger.6 Therapeutic doses are absorbed when taken by mouth and broken down in the body over a period of about six to eight hours. The general pharmacological actions of chlophedianol have been reported by Gosswald4 and bv Chen and Biller.7 These investigators found the
Chlophedianol hydrochloride effectively inhibits cough-induced movements in animals and humans, with no known narcotic effects.
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