Guaifenesin

R05C - Expectorants, excl. combinations with cough suppressants ATC R01BA52 Small molecule approved 2002 Oral Natural product

JFDA label: Unifed Extra Syrup

Mechanism of Action

— Unknown

Indications

Approved

Cough (expectorant)

Contraindications

Source: Lexicomp

OTC labeling: When used for self-medication, do not use extended-release tablets in children Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (3)

Not Known Dizziness · drowsiness · headache

Metabolism and nutrition disorders (1)

Not Known Hypouricemia

Gastrointestinal disorders (3)

Not Known Nausea · stomach pain · vomiting

Skin and subcutaneous tissue disorders (1)

Not Known Skin rash

Dosing

Source: Lexicomp

Cough (expectorant): Oral: Granules: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours Extended-release tablet: 600 mg to 1,200 mg every 12 hours as needed; maximum: 2,400 mg/24 hours Immediate-release tablet: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours Liquid: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours

(For additional information see "Guaifenesin: Pediatric drug information") Cough (expectorant): Oral: Granules: Children 4 years to Children 6 years to Children ≥12 years and Adolescents: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours Extended-release tablet: Children ≥12 years and Adolescents: 600 mg to 1,200 mg every 12 hours as needed; maximum: 2,400 mg/24 hours Immediate-release tablet: Children ≥12 years and Adolescents: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours Liquid: Children 2 years to Children 4 years to Children 6 years to Children ≥12 years and Adolescents: 200 to 400 mg every 4 hours as needed; maximum: 2,400 mg/24 hours

Refer to adult dosing.

There are no dosage adjustments provided in manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.

Phenylalanine

Some products may contain phenylalanine. Other warnings/precautions:

Self-medication (OTC use)

When used for self-medication (OTC), discontinue use and notify health care provider if symptoms do not improve within 7 days, or are accompanied by fever, rash, or persistent headache, or if you are hypersensitive to any component of the formulation. For persistent or chronic cough (as with smoking, asthma, chronic bronchitis, emphysema) or if cough is accompanied by excessive phlegm, consult a health care provider prior to use.

Pregnancy & Lactation

Pregnancy

When treatment for cough is needed during pregnancy, guaifenesin at standard OTC doses is generally considered acceptable. Some sources recommend use be reserved for significant maternal need; products containing alcohol should be avoided (Conover 2003; Ward 2005).

Lactation

Information related to the presence of guaifenesin in breast milk has not been located. Products containing alcohol should be avoided.

Chemistry & Properties

Formula	C10H14O4
Molecular weight	198.22 g/mol
IUPAC name	3-(2-methoxyphenoxy)propane-1,2-diol
CAS	93-14-1
PubChem CID	3516
InChIKey	`HSRJKNPTNIJEKV-UHFFFAOYSA-N`
logP	0.43 (XLogP 1.4)
Polar surface area	58.92 Å²
H-bond acceptors / donors	4 / 2
Drug-likeness (QED)	0.72
Lipinski violations	0

SMILES

COc1ccccc1OCC(O)CO

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	70.0%
Half-life	0.989 h
Volume of distribution	0.575 L/kg
Protein binding	62.2%
BBB penetrant	Yes

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP2C9	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (16)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Trifed Expectorant	Suspension 100 mg/5 ml, 1.25 mg/5 ml, 30 mg/5 ml	100 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.650
Bronchofed Expectorant	Solution 30 mg, 100 mg, 1.25 mg	100 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	0.740
Trifed Expectorant	Suspension 30 mg/5 ml, 100 mg/5 ml, 1.25 mg/5 ml	120 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.750
Cofex syrup	Syrup 33.3 mg/5 ml, (as Hcl) 1.65 mg/5 ml, 33.3 mg/5 ml, 33.3 mg/5 ml	100 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	0.800
Cofex syrup	Syrup 33.3 mg/5 ml, (as Hcl) 1.65 mg/5 ml, 33.3 mg/5 ml, 33.3 mg/5 ml	120 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	0.960
JOSWE NOCUF SYR	Syrup 100 mg/10 ml, 20 mg/10 ml, 5 mg/10 ml	120 ml	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	1.000
Unifed Expectorant Syrup	Syrup 100 mg/5 ml, 1.25 mg/5 ml, 30 mg/5 ml	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.050
Rectolyn Suppositories	Suppository 66.6 mg, 3.3 mg, 66.6 mg, 66.6 mg	10	Dar Al Dawa Development and Investment Co Ltd/Jordan	1.080
Cofex syrup	Syrup 33.3 mg/5 ml, (as Hcl) 1.65 mg/5 ml, 33.3 mg/5 ml, 33.3 mg/5 ml	150 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	1.200
Unifed Extra Syrup	Syrup 50 mg, 1.25 mg, 10 mg, 7.5 mg	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.440
Daywell syrup	Syrup 2.5 mg/5 ml, 50 mg/5 ml	120 ml	Jordan Sweden Medical & Sterilization Co.	1.630
Triaminic Chest And Nasal Congestion Syrup	Syrup 2.5 mg/5 ml, 50 mg/5 ml	118 ml	Nabulsi Drug Store	2.000
Pecosan Syrup	Syrup 100 mg/5 ml	100 ml	Sukhtian Pharma Co. (SP)	2.130
Panadol Cold and Flu All n one	Tablet 250 mg, 5 mg, 100 mg	24 tab	Sukhtian Group	2.640
Guayafen Syrup	Syrup 100 mg/5 ml	100 ml	Sukhtian Group	2.660
Mucinex 600mg ER Tab	Tablet 600 mg	20 tab	Nairoukh Drug Store	6.160