Guaifenesin

Guaifenesin
Clinical data
Trade names Mucinex
AHFS/Drugs.com Monograph
MedlinePlus a682494
License data
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
ATC code R05CA03 (WHO) QM03BX90 (WHO)
Legal status
Legal status
Pharmacokinetic data
Metabolism Renal
Biological half-life 1-5 hours[1]
Identifiers
CAS Number 93-14-1 YesY
PubChem (CID) 3516
IUPHAR/BPS 7617
DrugBank DB00874 YesY
ChemSpider 3396 YesY
UNII 495W7451VQ YesY
KEGG D00337 YesY
ChEMBL CHEMBL980 YesY
ECHA InfoCard 100.002.021
Chemical and physical data
Formula C10H14O4
Molar mass 198.216 g/mol
3D model (Jmol) Interactive image
Chirality Racemic mixture
  (verify)

Guaifenesin INN /ɡwaɪˈfɛnᵻsɪn/ or guaiphenesin (former BAN), also glyceryl guaiacolate,[2] is an expectorant drug sold over the counter and usually taken orally to assist the bringing up (expectoration) of phlegm from the airways in acute respiratory tract infections.

History

Similar medicines derived from the guaiac tree were in use as a generic remedy by American indigenous peoples when explorers reached North America in the 16th century. The Spanish encountered guaiacum wood "when they conquered Santo Domingo; it was soon brought back to Europe, where it acquired an immense reputation in the sixteenth century as a cure for syphilis and certain other diseases..."[3]

The 1955 edition of the Textbook of Pharmacognosy states: "Guaiacum has a local stimulant action which is sometimes useful in sore throat. The resin is used in chronic gout and rheumatism, whilst the wood is an ingredient in the compound concentrated solution of sarsaparilla, which was formerly much used as an alternative in syphilis."[3]

Guaifenesin was first approved by the Food and Drug Administration (FDA) in 1952. Although previously deemed "Generally Regarded as Safe" in its original approval, the drug received a New Drug Application for the extended-release version, which won approval on July 12, 2002. Because of this, the FDA then issued letters to other manufacturers of timed-release guaifenesin to stop marketing their unapproved versions, leaving Adams Respiratory Therapeutics in control of the market. Adams was subsequently acquired by Reckitt Benckiser, based on the strength of the marketing generated by Adams' Mucinex brand.[4][5]

Availability

Guaifenesin is sold as pills or syrups under many brand names. Single-ingredient formulations of guaifenesin are available, and it is also included in many other over-the-counter cough and cold remedy combinations (usually in conjunction with dextromethorphan, paracetamol (acetaminophen), ephedrine, pseudoephedrine, or phenylephrine).

Medical uses

Cough

The principal use of guaifenesin is in the treatment of coughing. A Cochrane Collaboration meta-analysis of over-the-counter medicines for acute cough in children and adults concluded that there was not enough high-quality clinical data to prove or disprove the effectiveness of any examined drug including guaifenesin.[6] Guaifenesin is sometimes combined with dextromethorphan, an antitussive, such as in Mucinex DM or Robitussin DM.[7]

Other uses

The guaifenesin protocol uses guaifenesin as an unapproved fibromyalgia treatment, despite the fact that a one-year double-blind study indicates that the treatment performs no better than placebo.[8][9] Guaifenesin has not been approved by the FDA for the treatment of fibromyalgia.

Based on a small, non-blinded study,[10] guaifenesin has been promoted to facilitate conception, by thinning and increasing cervical mucus, during the few days before ovulation.[11]

Anecdotal uses include thinning of the mucus in sinuses allowing drainage through the nose relieving sinus pressure in the face.

Mechanism of action

Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. It has been said to aid in the flow of respiratory tract secretions, allowing ciliary movement to carry the loosened secretions upward toward the pharynx.[12] Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions.

Guaifenesin has muscle relaxant and anticonvulsant properties and may be acting as an NMDA receptor antagonist.[13]

Side-effects

Side-effects of guaifenesin include nausea, vomiting, formation of kidney stones,[14] diarrhea, and constipation.[15] Nausea and vomiting can be reduced by taking guaifenesin with meals.[2] The risk of forming kidney stones during prolonged use can be reduced by maintaining good hydration and increasing the pH of urine. Rarely, severe allergic reactions may occur, including a rash or swelling of the lips or face, which may require urgent medical assistance. Mild dry mouth or chapped lips may also occur when taking this medication. Drinking a glass of water is recommended each time one takes guaifenesin.[16]

Guaifenesin increases the analgesic effect of paracetamol (acetaminophen) and aspirin, increases the sedative effects of alcohol, tranquilisers, sleep-pills and total anesthetics. Guaifenesin increases the effects of medication that decrease muscle tone.

Veterinary use

Guaifenesin's neurological properties first became known in the late 1940s. Guaifenesin is a centrally acting muscle relaxant used routinely in large-animal veterinary surgery. Guaifenesin is used in combination with, for example, propofol, since guaifenesin does not produce analgesia nor does it produce unconsciousness.[17][18]

See also

References

  1. ↑ Aluri JB, Stavchansky S (1993). "Determination of guaifenesin in human plasma by liquid chromatography in the presence of pseudoephedrine". J Pharm Biomed Anal. 11 (9): 803–8. doi:10.1016/0731-7085(93)80072-9. PMID 8218524.
  2. 1 2 "Guaifenesin". Drugs.com. Retrieved 2008-10-29.
  3. 1 2 Wallis, Thomas E. (1955). Textbook of Pharmacognosy.
  4. ↑ "Announcements RB Press release - 10/12/2007". Retrieved 16 November 2010.
  5. ↑ Goldstein, Jacob (25 May 2007). "FDA Bumps Phlegm-Fighters From Market". The Wall Street Journal. Retrieved 16 November 2010.
  6. ↑ Smith SM, Schroeder K, Fahey T (2008). Smith SM, ed. "Over-the-counter medications for acute cough in children and adults in ambulatory settings". Cochrane Database Syst Rev (1): CD001831. doi:10.1002/14651858.CD001831.pub3. PMID 18253996.
  7. ↑ "Guaifenesin DM". webmd.com.
  8. ↑ "Consumer Alert — Guaifenesin for Fibromyalgia". Fmnetnews.com. Retrieved 2012-01-04.
  9. ↑ Bennett RM, De Garmo P, Clark SR (1996). "A Randomized, Prospective, 12 Month Study To Compare The Efficacy Of Guaifenesin Versus Placebo In The Management Of Fibromyalgia" (reprint). Arthritis and Rheumatism. 39 (Supplement9): S212. doi:10.1002/art.1780391402.
  10. ↑ Check JH, Adelson HG, Wu CH (1982). "Improvement of cervical factor with guaifenesin". Fertility and Sterility. 37: 5.
  11. ↑ Weschler, Toni (2002). Taking Charge of Your Fertility (Revised ed.). New York: HarperCollins. p. 52. ISBN 0-06-093764-5.
  12. ↑ Gutierrez, K. (2007). Pharmacotherapeutics: Clinical Reasoning in Primary Care. W.B. Saunders Co.
  13. ↑ Keshavarz M, Showraki A, Emamghoreishi M (2013). "Anticonvulsant Effect of Guaifenesin against Pentylenetetrazol-Induced Seizure in Mice". Iran J Med Sci. 38 (2): 116–21. PMC 3700057Freely accessible. PMID 23825891.
  14. ↑ Bennett S, Hoffman N, Monga M (December 2004). "Ephedrine- and guaifenesin-induced nephrolithiasis". J Altern Complement Med. 10 (6): 967–9. doi:10.1089/acm.2004.10.967. PMID 15673990.
  15. ↑ Guaifenesin Side Effects http://www.drugs.com/sfx/guaifenesin-side-effects.html
  16. ↑ Guaifenesin http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682494.html
  17. ↑ Tranquilli, W. J., Thurmon, J. C., and Grimm, K. A. 2007. Lumb and Jones’ Veterinary Anesthesia and Analgesia. Blackwell Publishing. Chapter: Centrally Acting Muscle Relaxants.
  18. ↑ Valverde A (Apr 2013). "Balanced anesthesia and constant-rate infusions in horses". Vet Clin North Am Equine Pract. 29 (1): 89–122. doi:10.1016/j.cveq.2012.11.004.
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