Guaifenesin

Guaifenesin (Glyceryl Guaiacolate)
 is an expectorant that is used to help clear mucus or phlegm (pronounced flem)

from the chest when you have congestion from a cold or flu. It works by thinning
the mucus or phlegm in the lungs.
Available Forms
 Granules: 100 mg
 Liquid: 100 mg/5 mL *, 200 mg/5 mL , 200 mg/10 mL
 Syrup: 100 mg/5 mL
 Tablets: 200 mg , 400 mg
 Tablets (extended-release) : 600 mg , 1,200 mg
Indications and Dosage Considerations – Should be Given as Follows: Cough
 Adult - 100-400 mg orally Q4H; not to exceed 2.4 g/day
 Extended-release: 1-2 tablets (600-1200 mg) orally every 12 hours; not to

exceed 4 tablets/24 hours (2.4 g/day)
 Pediatric
o Children 6 months to 2 years: 25-50 mg every 4 hours; not to exceed 300
mg/day
o Children 2-6 years: 50-100 mg orally every 4 hours; not to exceed 600
mg/day
o Children 6-11 years: 100-200 mg orally every 4 hours; not to exceed 1.2
g/day
o Children older than 12 years
 100-400 mg orally every 4 hours; not to exceed 2.4 g/day, OR
 1-2 extended-release tablets (600-1200 mg) orally every 12 hours;
not to exceed 4 tablets/24 hours (2.4 g/day)
Contraindications
 General Information
o Guaifenesin may alter some laboratory tests. It may increase renal
clearance for urate and lower serum uric acid levels.
o Guaifenesin may also falsely elevate the VMA test for catechols.
o Guaifenesin should be discontinued at least 48 hours prior to the
collection of urine specimens for such laboratory tests.
 Asthma, bronchitis, emphysema, heart failure, tobacco smoking
o Guaifenesin should not be used for a cough that is specifically associated
with heart failure or ACE inhibitor therapy.
 Fever
 Pregnancy
 Breast-feeding
 Geriatric
Brand Names
 US Brand Names
o Allfen
o Altarussin
o Amibid LA
o Antitussin
o Bidex 400
o Diabetic Siltussin DAS-Na
o Diabetic Tussin EX
o Drituss G
o Guaifenex G
o Guaifenex LA
o Mucinex
o Robitussin
 Canadian Brand Names
o Balminil Expectorant
o Balminil Expectorant Sugar-Free
o Benylin-E
o Benylin E Extra Strength Chest Congestion
o Broncho-Grippex Expectorant
o Resyl
o Robitussin Extra Strength
Pharmacodynamics
Absorption - Studies have shown that guaifenesin is well absorbed from and along the
gastrointestinal tract after oral administration
Distribution - The geometric mean apparent volume of distribution of guaifenesin determined in

healthy adult subjects is 116L
Metabolism - After the oral administration of 400 mg guaifenesin, the agent experiences rapid
hydrolysis (more than 60% of the dose hydrolyzed over a range of seven hours) with β-(2-
methoxyphenoxy)-lactic acid found as the major urinary metabolite but no parent drug
detectable in the urine 5,7. Moreover, it has been observed that guaifenesin also experiences
both oxidation and demethylation 5. In particular, the medication is quickly metabolized
hepatically by way of oxidation to β-(2-methoxyphenoxy)-lactic acid 5. Furthermore, guaifenesin
is also demethylated by O-demethylase in liver microsomes to the point where about 40% of an
administered dose is excreted as this metabolite in the urine within 3 hours 5. In fact, O-
demethylase appears to be the primary enzyme for the metabolism of guaifenesin and the
primary metabolites of the substance are β-(2-methoxyphenoxy)-lactic acid and the
demethylated hydroxyguaifenesin, both of which are themselves inactive moieties 5.
Elimination - After administration, guaifenesin is metabolized and then largely excreted in the
urine.
Half-life- approx.. 1 hour
References:
 Guaifenesin (Oral Route) Description and Brand Names - Mayo Clinic . (2022).
Retrieved 22 November 2022, from https://www.mayoclinic.org/drugs-
supplements/guaifenesin-oral-route/description/drg-
20068720#:~:text=Guaifenesin%20is%20used%20to%20help,or%20phlegm
%20in%20the%20lungs.
 (2022). Retrieved 22 November 2022, from
https://www.rxlist.com/consumer_guaifenesin_mucinex/drugs-condition.htm
 Mucinex (guaifenesin) dose, indications, adverse effects, interactions... from
PDR.net . (2022). Retrieved 22 November 2022, from https://www.pdr.net/drug-
summary/Mucinex-guaifenesin-1275#:~:text=Guaifenesin%20should%20not
%20be%20used,of%20a%20health%20care%20professional.
 Guaifenesin: Uses, Interactions, Mechanism of Action | DrugBank Online. (2022).
Retrieved 22 November 2022, from https://go.drugbank.com/drugs/DB00874


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Guaifenesin

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Guaifenesin (Glyceryl Guaiacolate)

 is an expectorant that is used to help clear mucus or phlegm (pronounced flem)

 Adult - 100-400 mg orally Q4H; not to exceed 2.4 g/day

 Extended-release: 1-2 tablets (600-1200 mg) orally every 12 hours; not to

Distribution - The geometric mean apparent volume of distribution of guaifenesin determined in

Half-life- approx.. 1 hour

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