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Guaifenesin (Systemic)


VA CLASSIFICATION
Primary: RE302

Commonly used brand name(s): Anti-Tuss; Balminil Expectorant; Benylin-E; Breonesin; Calmylin Expectorant; Diabetic Tussin EX; Fenesin; Gee-Gee; Genatuss; Glycotuss; Glytuss; Guiatuss; Halotussin; Humibid L.A; Humibid Sprinkle; Hytuss; Hytuss-2X; Naldecon Senior EX; Organidin NR; Pneumomist; Resyl; Robitussin; Scot-tussin Expectorant; Sinumist-SR; Touro EX; Uni-tussin.

Another commonly used name is
glyceryl guaiacolate .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Expectorant—

Indications

Accepted

Cough (treatment)—Guaifenesin is indicated as an expectorant in the temporary symptomatic management of cough due to minor upper respiratory infections and related conditions, such as sinusitis, pharyngitis, and bronchitis, when these conditions are complicated by viscous mucus and congestion {09} {11}. However, because supporting data are very limited, there is some controversy about its effectiveness {10} {12} {13} {14} {15} {16}.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    198.22 {06}

Mechanism of action/Effect:

Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions {01} {02} {03}; however, objective evidence for this is limited {09} {17} and conflicting. {10}

Absorption:

Readily absorbed from gastrointestinal tract {02}.

Elimination:
    Renal, as inactive metabolites {02}.


Precautions to Consider

Carcinogenicity/Tumorigenicity/Mutagenicity

Studies to determine the carcinogenicity, tumorigenicity, or mutagenicity of guaifenesin in animals have not been conducted {01} {02}.

Pregnancy/Reproduction

Pregnancy—
Although adequate and well-controlled studies in pregnant women have not been done, the Collaborative Perinatal Project monitored 197 mother-child pairs exposed to guaifenesin during the first trimester. An increased occurrence of inguinal hernias was found in the neonates. However, congenital defects were not strongly associated with guaifenesin use during pregnancy in 2 large groups of mother-child pairs. {07}

Studies have not been done in animals {01} {02}.

FDA Pregnancy Category C {01} {02}.

Breast-feeding

It is not known whether guaifenesin is distributed into breast milk. However, problems in humans have not been documented. {01} {07}

Pediatrics

Appropriate studies on the relationship of age to the effects of guaifenesin have not been performed in the pediatric population. However, no pediatrics-specific problems have been documented to date.

Caution is recommended in children up to 12 years of age with persistent or chronic cough, such as occurs with asthma, or if the cough is accompanied by excessive phlegm (mucus). The condition of these children may need a physician's evaluation before guaifenesin is administered. {04} {05}

Guaifenesin should not be given to children younger than 2 years of age unless recommended by a physician {04}.


Geriatrics


Appropriate studies on the relationship of age to the effects of guaifenesin have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date.


Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With diagnostic test results
5-hydroxyindoleacetic acid (5-HIAA), urine    (urinary determinations may be falsely increased when nitrosonaphthol reagent is used because of color interference by guaifenesin metabolites; guaifenesin should be discontinued 48 hours before collection of urine for this test {01} {02} {03})


Vanillylmandelic acid (VMA), urine    (guaifenesin or its metabolites may cause color interference with urinary determinations and may falsely elevate VMA test for catechols; guaifenesin should be discontinued 48 hours before collection of urine for this test {01} {02} {03})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problem exists
Sensitivity to guaifenesin


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Less frequent or rare
    
Diarrhea {01}{02}
    
dizziness {01}
    
headache {01}
    
nausea or vomiting {01}{02}
    
skin rash {01}
    
stomach pain {02}
    
urticaria {01}(hives)





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Guaifenesin (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to guaifenesin

Pregnancy—Increased incidence of inguinal hernias in the babies of one group of women taking guaifenesin during pregnancy; however, this did not occur in other groups





Use in children—For self-medication, caution if cough is persistent or occurs with excessive phlegm; not administering to children younger than 2 years of age unless directed by a physician


Proper use of this medication

Proper administration
Importance of maintaining adequate fluid intake

» For extended-release dosage forms



• Swallowing capsules whole or opening capsules and sprinkling contents on soft food, then swallowing without crushing or chewing


• Not breaking (unless scored for breakage), crushing, or chewing tablets; swallowing tablet whole


» Proper dosing
Missed dose (if on a scheduled dosing regimen): Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
Checking with physician if cough persists after medication has been used for 7 days or if fever, skin rash, continuing headache, or sore throat is present with cough {04}


General Dosing Information
Before prescribing or recommending medication to suppress or modify cough, it is important that the underlying cause of the cough be assessed {02} {08}.

For self-medication, guaifenesin should not be taken for chronic cough unless directed by a physician {04}.

Patient should be advised to maintain adequate hydration {18}.


Oral Dosage Forms

GUAIFENESIN CAPSULES USP

Usual adult and adolescent dose
Expectorant
Oral, 200 to 400 mg every four hours, not to exceed 2400 mg a day {04}.


Usual pediatric dose
Expectorant
Children 2 to 6 years of age: The liquid or extended-release capsule dosage forms may be preferable for children in this age group.

Children 6 to 12 years of age: Oral, 100 to 200 mg every four hours, not to exceed 1200 mg a day. {01}


Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


200 mg (OTC) [Breonesin] [Hytuss-2X]

Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container.


GUAIFENESIN EXTENDED-RELEASE CAPSULES

Usual adult and adolescent dose
Expectorant
Oral, 600 to 1200 mg every twelve hours, not to exceed 2400 mg a day {03}.


Usual pediatric dose
Expectorant
Children 2 to 6 years of age: Oral, 300 mg every twelve hours, not to exceed 600 mg a day {03}.

Note: The liquid dosage forms may be preferable for children 2 to 6 years of age, who cannot always be relied upon to swallow the contents of the capsule without chewing.


Children 6 to 12 years of age: Oral, 600 mg every twelve hours, not to exceed 1200 mg a day {03}.


Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


300 mg (Rx) [Humibid Sprinkle]

Canada—
Not commercially available.

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container.

Additional information:
Extended-release capsules may be swallowed whole or opened and the contents sprinkled on soft food immediately prior to ingestion, then swallowed without crushing or chewing. Capsule contents should not be subdivided. {03}


GUAIFENESIN ORAL SOLUTION

Usual adult and adolescent dose
See Guaifenesin Capsules USP .

Usual pediatric dose
Expectorant
Children 6 months to 2 years of age—Dosage must be individualized by physician. A commonly used regimen is 25 to 50 mg every four hours, not to exceed 300 mg a day {01}.

Children 2 to 6 years of age—Oral, 50 to 100 mg every four hours, not to exceed 600 mg a day {01}.

Children 6 to 12 years to age—See Guaifenesin Capsules USP.


Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


100 mg per 5 mL (OTC) [Diabetic Tussin EX (alcohol free) (sugar free)] [Scot-tussin Expectorant (alcohol 3.5%) (sugar free)]


100 mg per 5 mL (Rx) [Organidin NR (sorbitol) (alcohol free)]


200 mg per 5 mL (OTC) [Naldecon Senior EX (alcohol free) (sugar free)]

Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from freezing.


GUAIFENESIN SYRUP USP

Usual adult and adolescent dose
See Guaifenesin Capsules USP .

Usual pediatric dose
See Guaifenesin Oral Solution.

Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


100 mg per 5 mL (OTC) [Anti-Tuss (alcohol 3.5%)] [Genatuss (alcohol 3.5%)] [Guiatuss] [Halotussin ( alcohol 3.5%)] [Robitussin (alcohol 3.5%)] [Uni-tussin (alcohol 3.5%)][Generic]

Canada—


100 mg per 5 mL (OTC) [Balminil Expectorant] [Benylin-E (alcohol 5%)] [Calmylin Expectorant (sorbitol ) (alcohol free)] [Robitussin (alcohol 3.5%)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from freezing.


GUAIFENESIN TABLETS USP

Usual adult and adolescent dose
See Guaifenesin Capsules USP .

Usual pediatric dose
See Guaifenesin Capsules USP.

Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


100 mg (OTC) [Glycotuss] [Hytuss (scored) (sugar free)]


200 mg (OTC) [Gee-Gee] [Glytuss]


200 mg (Rx) [Organidin NR (scored)]

Canada—


100 mg (OTC) [Resyl]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container.


GUAIFENESIN EXTENDED-RELEASE TABLETS

Usual adult and adolescent dose
See Guaifenesin Extended-release Capsules .

Usual pediatric dose
See Guaifenesin Extended-release Capsules {02} .

Strength(s) usually available
U.S.—


600 mg (Rx) [Fenesin (scored)] [Humibid L.A (scored)] [Pneumomist ( scored)] [Sinumist-SR (scored)] [Touro EX (scored)][Generic]

Canada—
Not commercially available.

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container.



Revised: 06/27/2000



References
  1. Organidin NR package insert (Carter-Wallace—US), Rev 1994.
  1. Fenesin package insert (Dura Pharmaceuticals—US), Rev 1993.
  1. Humibid LA/Humibid Sprinkles package insert (Adams—US).
  1. Robitussin package (A. H. Robins—US), Rev 3/94.
  1. OTC expectorant drugs label warning. Weekly Pharmacy Reports. The Green Sheet, 1992 May; 41(27): 1.
  1. The United States pharmacopeia. The national formulary. USP 23rd revision (January 1, 1995). NF 18th ed (January 1, 1995). Rockville, MD: The United States Pharmacopeial Convention, Inc., 1994.
  1. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. A reference guide to fetal and neonatal risk. 3rd ed. Baltimore: Williams & Wilkins, 1990: 597-9.
  1. Irwin RS, Curley FJ, Bennett FM. Appropriate use of antitussives and protussives. Drugs 1993; 46(1): 80-91.
  1. Anon. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; expectorant drug products for over-the-counter human use; final monograph. Fed Regist, 1989; 54(38): 8494-509.
  1. Hirsch SR, Viernes PF, Kory RC. The expectorant effect of glyceryl guaiacolate in patients with chronic bronchitis. Chest 1973; 63: 9-14.
  1. Kuhn JJ, Hendley JO, Adams KF, et al. Antitussive effect of guaifenesin in young adults with natural colds. Chest 1982; 82: 713-8.
  1. Irwin RS, Pratter MR. Treatment of cough. Chest 1982; 82: 662-3.
  1. Witek TJ, Schachter EN. Respiratory care drugs. In: Pharmacology and therapeutics in respiratory care. Philadelphia: W. B. Saunders Company, 1994: 242-3.
  1. Ziment I. Hydration, humidification, and mucokinetic therapy. In: Weiss EB, Stein M, editors. Bronchial asthma. Mechanisms and therapeutics. Boston: Little, Brown and Company, 1993: 917-33.
  1. Hendeles L. Efficacy and safety of antihistamines and expectorants in nonprescription cough and cold preparations. Pharmacotherapy 1993; 13: 154-8.
  1. Reviewers' responses to monograph revision of 5/95.
  1. Chodosh S, Medici TC, Enslein K. Objective sputum changes associated with glyceryl guaiacolate in chronic bronchial diseases. Bull Physiopathol Respir 1973; 9: 315-24.
  1. Reviewers' responses to monograph revision of 5/95.
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