Guaifenesin
Tusseryl® Oral Solu-on
100 mg/ 5 mL Oral solu1on
Expectorant
PRODUCT DESCRIPTION
Guaifenesin (Tusseryl) Oral solu1on containing 100 mg
guaifenesin in every 5 mL (1 teaspoonful) of oral solu1on in
orange flavor is used as a treatment for cough through
loosening the clearance of mucus.
Chemical Name: 3-(2-methoxyphenoxy) propane-1,2-diol
Formula-on
Each 5 mL of Guaifenesin Oral Solu1on contains:
Guaifenesin . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 100 mg
Alcohol . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 4%
PHARMACOLOGIC PROPERTIES
Pharmacodynamics
Guaifenesin is an expectorant. It enhances the output of
sputum and bronchial secre1ons through decreasing the
adhesiveness and surface tension of these secre1ons.
Guaifenesin increases the flow of viscous gastric secre1ons
that promote ciliary ac1on, which can cause dry, unproduc1ve
coughing to become produc1ve and less frequent.
Pharmacokine-cs
Absorp-on
Guaifenesin is well absorbed along the gastrointes1nal tract
aTer oral administra1on.
Distribu-on
The apparent volume of distribu1on of guaifenesin in healthy
adult subjects is 116 L (CV=45.7%). Informa1on about plasma
protein binding is not readily available.
Metabolism
ATer the oral administra1on of 400 mg guaifenesin, it is
immediately hydrolyzed (>60% of the dose hydrolyzed over a
range of seven hours) with β-(2-methoxyphenoxy)-lac1c acid
found as the major urinary drug metabolite yet no parent drug
was detectable in the urine. Guaifenesin also undergoes
oxida1on as well as demethyla1on and is hepa1cally
metabolized hepa1cally through oxida1on to β-(2-
methoxyphenoxy)-lac1c acid. It is then demethylated by O-
demethylase in the liver microsomes to an extent wherein
about 40% of the administered dose is excreted in the urine
within 3 hours as the demethylated metabolite. O-
demethylase appears to be the primary metabolic enzyme of
guaifenesin. The primary metabolites of the substance are β-
(2-methoxyphenoxy)-lac1c acid and the demethylated
hydroxyguaifenesin, which are both inac1ve moie1es.
Elimina-on
ATer administra1on, guaifenesin is metabolized and then
largely excreted in the urine. The mean clearance for
guaifenesin is about 94.8 L/hr (CV=51.4%)
PRECLINICAL SAFETY DATA
Acute toxicity
The LD50 following a single oral dose of guaifenesin is 6810
mg/kg body weight in mice, 1510-3690 mg/kg body weight in
rats, 2550-3160 mg/kg in rabbits and over 10,000 mg/kg in
dogs.
Chronic and subchronic toxicity
Rats aged over 90 days survived following oral doses of up to
2,000 mg/kg body weight. The development of calculi was
observed in all organs of the urinary tract.
Mutagenic and carcinogenic poten-al
Mutagenicity and carcinogenicity studies in animals are lacking
therefore, the risk of this type of ac1vity cannot be accurately
determined.
Reproduc-ve toxicity
Insufficient reproduc1ve toxicity studies have been conducted
on guaifenesin and animal studies have shown that the drug
does not have teratogenic ac1vity. Risk of embryo-fetal
development has not been observed in humans.
INDICATIONS
Guaifenesin is an expectorant used as a remedy for cough and
conges1on caused by common colds, bronchi1s, and other
b r e a t h i n g i l l n e s s e s . I t i s u s u a l l y n o t g i v e n fo r
ongoing cough from smoking or long-term breathing problems
unless prescribed by a physician. Guaifenesin works by
loosening mucus in the airways, clearing conges1on, and
making breathing easier.
DOSAGE AND ADMINISTRATION
For short-ac1ng oral solu1ons for cough:
Adults - 200 to 400 milligrams (mg) every four hours.
Children 6 to 12 years of age - 100 to 200 mg every four hours.
Children 4 to 6 years of age - 50 to 100 mg every four hours.
Children and infants up to 4 years of age - Use is not
recommended .
Guaifenesin has an onset 1me of 30 minutes and a dura1on of
4-6 hours. Guaifenesin is intended to be taken with plenty of
fluids to help loosen the mucus in the lungs. It may be taken
without food or with food if it causes an upset stomach. Liquid
doses must be measured using a specially marked spoon or
container. If a dose is missed take it as soon as possible. Skip
the missed dose if it is almost 1me for the next dose. Do not
take double or extra doses.
CONTRAINDICATIONS
Guaifenesin is contraindicated with individuals who are allergic
to guaifenesin, sympathomime1c agents, tramadol, ephedrine
analogues as well as opioids.
WARNINGS AND PRECAUTIONS
Guaifenesin should not be taken by individuals who have an
overac1ve thyroid gland, diabetes, closed angle glaucoma,
significant uncontrolled high blood pressure, enlarged
prostate, decreased func1on of the adrenal gland, asthma, low
blood pressure, severe liver disease, acute pancrea1c
inflamma1on and/or kidney disease.
Ask a doctor before use if you have cough that occurs with too
much mucus or a chronic cough such as cases that occur with
smoking, asthma , chronic bronchi1s or emphysema.
depression. Rare reports have also proven urinary or renal
calculi in pa1ents who have consumed large quan11es of
guaifenesin for long periods of 1me. Gastric lavage and
suppor1ve and suppor1ve treatment are recommended.
INSTRUCTIONS FOR USE AND HANDLING
Use a specially marked spoon or container to measure your
dose. Do not take more than 6 doses in any 24-hour period.
Adults and children 12 years and over: (2 - 4 ) tsp every 4 hours
Children under 12 years: Consult a doctor
STORAGE
Store at temperature between 20°-25°C (68°-77°F). Keep away
from light, heat, moisture and freezing. Keep out of reach of
children.
DOSAGE FORMS AND PACKAGING AVAILABLE
Guaifenesin (Tusseryl®) Oral Solu1on is available in 1 x 60 mL
Orange Flavored Oral Solu1on
MANUFACTURED AND DISTRIBUTED BY:

PREGNANCY AND LACTATION

Pregnancy
It is not known whether Guaifenesin can harm an unborn baby
during pregnancy. Consult with your physician before taking Manufactured by ASTERĒ PHARMACEUTICALS
this medica1on if you are pregnant. 100 Tordesillas St., Salcedo Village, Maka1, Metro Manila,
Lacta-on Philippines
It is not known if guaifenesin is excreted into breast milk. Date of First Authoriza1on:
Consult a physician before taking this medicine if you are Date of Revision:
breasgeeding a baby.

ADVERSE EFFECT
Gastrointes-nal
Gastrointes1nal side effects include vomi1ng, stomachache or
aTer taking higher than recommended doses.
Rare: vomi1ng , diarrhea, abdominal pain
Nervous
Dizziness and headache were the frequently reported adverse
effects aTer intake of guaifenesin.
Rare: Dizziness, nausea, headache
Immune system disorders
Hypersensi1vity reac1ons include difficul1es in swallowing,
edema of the face, lips, tongue or throat and strong itching
with rash or swelling of the skin.

OVERDOSE AND TREATMENT

Mild or moderate overdosing can lead to dizziness,
gastrointes1nal disorders, nausea, vomi1ng or decreased
muscle tone. Very high doses on the other hand may produce
symptoms like excita1on, trouble breathing and respiratory