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Guaifenesin

Guaifenesin (gwi fen' ə sin) (INN) or guaiphenesin (former BAN) is an expectorant drug usually taken orally to assist the expectoration ("bringing up") of phlegm from the airways in acute respiratory tract infections. Guaifenesin works by drawing water into the bronchi. The water both thins mucous and lubricates the airway, facilitating the removal of mucous by coughing. It is sold under several brand names such as Humibid, Mucinex, Benylin and Robitussin, and it also is included in many over-the-counter cough and cold remedies. more...

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Guaifenesin's molecular formula is C10H14O4, and its chemical name is 3-(2-methoxyphenoxy)-1,2-propanediol. Its CAS number is 93-14-1. It was first approved by the FDA in 1952.

Guaifenesin is also used in the experimental guaifenesin protocol in the treatment of fibromyalgia.

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Effectiveness of Guaifenesin in the treatment of cough
From American Family Physician, 7/15/04 by Karl E. Miller

Cough results from a complex interaction between receptors in the airway and the central nervous system; this interaction is poorly understood. Glyceryl ether of guaiacol, commonly known as guaifenesin, is present in multiple cough and cold preparations. This compound has been labeled an expectorant because it is thought to relieve cough by thinning sputum and increasing its production. Guaifenesin is the only expectorant that has been considered effective by the U.S. Food and Drug Administration. Despite its broad use in the treatment of cough, multiple studies have found inconsistent results supporting the effectiveness of guaifenesin as an expectorant or cough suppressant. Little information is available concerning the impact of guaifenesin on the sensitivity of the cough reflex. Dicpinigaitis and Gayle conducted a randomized, placebo-controlled, double-blind study to assess the efficacy of a single dose of guaifenesin on cough reflex sensitivity.

The trial involved a group of persons with acute viral upper respiratory tract infection (URI) and a group of healthy persons. The participants were nonsmokers, did not have a history of pulmonary disorders, and had no symptoms suggestive of gastroesophageal reflux disease. Within the previous four weeks, the healthy participants had no URI symptoms, seasonal allergies, or postnasal drip. Participants with URI took no medications to control symptoms within at least 24 hours of the study.

Each participant received a single 400-mg dose of guaifenesin or placebo one to two hours before undergoing a capsaicin challenge to induce cough. The capsaicin challenge was performed with incremental increases in concentration until it induced five or more coughs within 15 seconds of inhalation. Spirometry data were collected before the challenge. The main outcome was the concentration of capsaicin required to induce five or more coughs. The results included comparing the effects of guaifenesin and placebo among the patients with URI and the healthy participants.

The URI and healthy groups each contained 14 persons. All participants were induced to cough during the capsaicin challenge test. The spirometry results did not differ between persons who received guaifenesin and persons who received placebo. Among patients with URI, those who received guaifenesin required significantly higher concentrations of capsaicin to induce cough compared with the placebo group. In seven of the 14 participants who received guaifenesin, the concentration needed to induce cough was double that of the placebo group. Among the healthy persons, no differences occurred between the placebo and guaifenesin groups with regard to the concentration of capsaicin that induced five or more coughs.

The authors conclude that guaifenesin inhibits the cough reflex in patients with URI. This action occurs because the cough receptors are transiently hypersensitive secondary to the URI. They add that this effect was not present in healthy persons.

KARL E. MILLER, M.D.

Dicpinigaitis PV, Gayle YE. Effect of guaifenesin on cough reflex sensitivity. Chest December 2003;124:2178-81.

EDITOR'S NOTE: Over the past few years, there has been an increased emphasis on evidence-based medicine. Because of this emphasis, the efficacy of some of the older, more established medications has been questioned. One of these medications is guaifenesin. Included in a significant number of cough and cold preparations, guaifenesin functions mainly as an expectorant. Studies have shown that this medication is an effective expectorant. The study by Dicpinigaitis and Gayle adds to this body of literature by demonstrating that guaifenesin also suppresses cough in patients with URI symptoms. This study provides physicians with a proven medication that can control the symptoms of URIs and provide supportive care for patients with URIs.--K.E.M.

COPYRIGHT 2004 American Academy of Family Physicians
COPYRIGHT 2004 Gale Group

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