Description

Simple

A medication used to eliminate phlegm and treat chest congestions.

Clinical

An expectorant commonly found in OTC products for the symptomatic relief from congested chests and coughs associated with cold, bronchitis, and/or other breathing illnesses.

Overview

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 [11]. 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 [11]. Although it is principally believed that guaifenesin elicits an action to facilitate productive cough to manage chest congestion [4, 7, 9, Read more

Pharmacology

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, Read more

Pharmacodynamic

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 [ Read more

Mechanism of action

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 [ Read more

Absorption

Studies have shown that guaifenesin is well absorbed from and along the gastrointestinal tract after oral administration [ Read more

Protein binding

Information regarding the protein binding of guaifenesin is not readily available or accessible.

Volume of distribution

The geometric mean apparent volume of distribution of guaifenesin determined in healthy adult subjects is 116L (CV=45.7%) [ Read more

Clearance

The mean clearance recorded for guaifenesin is about 94.8 L/hr (CV=51.4%) [11].

Half life

The half-life in plasma observed for guaifenesin is approximately one hour [ Read more

Route of elimination

After administration, guaifenesin is metabolized and then largely excreted in the urine [ Read more

Toxicity

The most prevalent signs and symptoms associated with an overdose of guaifenesin have been nausea and vomiting [7].

Although adequate and well-controlled studie... Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • true
  • Sex Group: all
  • Regions: US

Food Interactions

  • Take with a full glass of water.
  • Take with or without food. The absorption is unaffected by food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
11 References
  1. 1 . Thompson GA, Solomon G, Albrecht HH, Reitberg DP, Guenin E: Guaifenesin Pharmacokinetics Following Single-Dose Oral Administration in Children Aged 2 to 17 Years. J Clin Pharmacol. 2016 Jul;56(7):894-901. doi: 10.1002/jcph.682. Epub 2016 Jan 24.PubMed: 26632082
  2. 2 . Kagan L, Lavy E, Hoffman A: Effect of mode of administration on guaifenesin pharmacokinetics and expectorant action in the rat model. Pulm Pharmacol Ther. 2009 Jun;22(3):260-5. doi: 10.1016/j.pupt.2008.12.020. Epub 2009 Jan 6.PubMed: 19166957
  3. 3 . Keshavarz M, Showraki A, Emamghoreishi M: Anticonvulsant Effect of Guaifenesin against Pentylenetetrazol-Induced Seizure in Mice. Iran J Med Sci. 2013 Jun;38(2):116-21.PubMed: 23825891
  4. 4 . Yuta A, Baraniuk JN: Therapeutic approaches to mucus hypersecretion. Curr Allergy Asthma Rep. 2005 May;5(3):243-51.PubMed: 15842963
  5. 5 . Albrecht HH, Dicpinigaitis PV, Guenin EP: Role of guaifenesin in the management of chronic bronchitis and upper respiratory tract infections. Multidiscip Respir Med. 2017 Dec 11;12:31. doi: 10.1186/s40248-017-0113-4. eCollection 2017.PubMed: 29238574
  6. 6 . MyHealth.Alberta.ca Network: Guaifenesin - Oral Profile Link
  7. 7 . Electronic Medicines Compendium: Robitussin Chesty Cough Medicine Monograph Link
  8. 8 . Australian Government Department of Health Therapeutic Goods Administration OTC Medicines Monograph: Guaifenesin File
  9. 9 . A NOVEL STABILITY INDICATING HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF GUAIPHENESIN, CHLORPHENERAMINE MALEATE & DEXTROMETHORPHAN HBr File
  10. 10 . National Pharmaceutical Regulatory Agency (NPRA) Guaiphenesin Product Information File
  11. 11 . CENTER FOR DRUG EVALUATION AND RESEARCH: CLINICAL PHARMACOLOGY AND BIOPHARMACEUTICS REVIEW(S) OF GUAIFENESIN/HYDROCODONE BITARTRATE File