Investigational Drug Details
| Drug ID: | D251 |
| Drug Name: | Guaifenesin |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00874 |
| DrugBank Description: | Guaifenesin possesses a storied history, having been originally formally approved by the US FDA in 1952 and continues to be one of very few - if not perhaps the only drug that is readily available and used as an expectorant [F4525]. Since that time the agent has been a combination component of various prescription and non-prescription over-the-counter cough and cold products and is currently a widely available over-the-counter generic medication [F4525]. Although it is principally believed that guaifenesin elicits an action to facilitate productive cough to manage chest congestion [A177661, L6100, F4516, F4522, F4525], it is not known whether the agent can reliably mitigate coughing. Regardless, on March 1, 2007, the FDA received a petition asking the FDA to notify the public that some antitussives, expectorants, decongestants, antihistamines, and cough/cold combinations are not known to be safe and effective in children under the age of 6 years [F4525]. After the negotiation between FDA and major manufacturers, a voluntary transition of labels for not using guaifenesin in children under the age of 4 years was endorsed by FDA in 2008 [F4525]. Furthermore, there has also been contemporary research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist [A177652]. |
| PubChem ID: | 3516 |
| CasNo: | 93-14-1 |
| Repositioning for NAFLD: | Yes |
| SMILES: | COC1=CC=CC=C1OCC(O)CO |
| Structure: |
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| InChiKey: | HSRJKNPTNIJEKV-UHFFFAOYSA-N |
| Molecular Weight: | 198.2158 |
| DrugBank Targets: | NMDA receptor |
| DrugBank MoA: | Although the exact mechanism of action of guaifenesin may not yet be formally or totally elucidated, it is believed that expectorants like guaifenesin function by increasing mucus secretion [A177661]. Moreover, it is also further proposed that such expectorants may also act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that can elicit glandular exocytosis that is comprised of a less viscous mucus mixture [A177661]. Subsequently, these actions may provoke coughing that can ultimately flush difficult to access, congealed mucopurulent material from obstructed small airways to facilitate a temporary improvement for the individual [A177661]. Consequently, while it is generally proposed that guaifenesin functions as an expectorant by helping to loosen phlegm (mucus) and thin bronchial secretions to rid the bronchial passageways of bothersome mucus and make coughs more productive, there has also been research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist [A177652]. |
| DrugBank Pharmacology: | Guaifenesin is categorized as an expectorant that acts by enhancing the output of phlegm (sputum) and bronchial secretions via decreasing the adhesiveness and surface tension of such material [F4516]. Furthermore, guaifenesin elicits an increased flow of less viscous gastric secretions that subsequently promote ciliary action - all actions that ultimately change dry, unproductive coughing to coughs that are more productive and less frequent [F4516]. Essentially, by decreasing the viscosity and adhesiveness of such secretions, guaifenesin enhances the efficacy of mucociliary activity in removing accumulated secretions from the upper and lower airway [F4516]. |
| DrugBank Indication: | Guaifenesin is an expectorant that is indicated for providing temporary symptomatic relief from congested chests and coughs which may be due to a cold, bronchitis, and/or other breathing illnesses [FDA Label, F4510, L6079]. |
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