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Exall (Carbetapentane Citrate / Pseudoephedrine Hydrochloride / Guaifenesin) - Description and Clinical Pharmacology

 
 



Exall-D Liquid

Rx Only

Antitussive / Nasal Decongestant / Expectorant

DESCRIPTION: ExallTM-D Liquid is alcohol-free, dye-free, sugar-free, colorless liquid for oral
administration having a fruit gum odor and flavor.

Each teaspoonful (5 ml) for oral administration contains:
Carbetapentane Citrate................................ 10 mg
Pseudoephedrine Hydrochloride................... 30 mg
Guaifenesin.............................................. 100 mg

Inactive ingredients: Citric Acid, Fruit Gum Flavor, Glycerin, Propylene Glycol, Purified Water,
Sodium Citrate, Sodium Saccharin, Sorbitol.

Carbetapentane Citrate (1-Phenylcyclopentanecarboxylic acid 2- (2-diethylaminoethoxy) ethyl
ester citrate) is a white crystalline powder. It is freely soluble in water and chloroform. Its structure
is as follows:


Pseudoephedrine Hydrochloride is a nasal decongestant with the chemical name Benzenemethanol,
alpha-[1-(methylamino)ethyl]-, [S-(R*, R*)-, hydrochloride. Its structure is as follows:


Guaifenesin (1,2-Propanediol, 3-(2-methoxyphenoxy)-, (±)-) is a white to slightly gray, crystalline
powder, having a bitter taste. It may have a slight characteristic odor. It is soluble in water, alcohol,
chloroform, glycerin, and propylene glycol. Its structure is as follows:


CLINICAL PHARMACOLOGY

Antitussive, nasal decongestant, and expectorant actions.

Carbetapentane citrate is a centrally acting non-narcotic antitussive. Carbetapentane citrate
has atropine-like and local anesthetic actions, as well as temporarily controls and suppresses
the cough reflex by selective depression of the medullary cough center. It has no significant
analgesic or sedative properties, does not depress respiration or pre-dispose to addiction with
usual doses.

Pseudoephedrine hydrochloride is an oral sympathomimetic amine that acts as a nasal
decongestant to respiratory tract mucous membranes. While its vasoconstrictor action is
similar to that of ephedrine, pseudoephedrine has less pressor effect in normotensive adults.
Serum half-life for pseudoephedrine is 6 to 8 hours. Acidic urine is associated with faster
elimination of the drug. About one-half of the administered dose is excreted in the urine.
Pseudoephedrine causes vasoconstriction, which results in reduction of tissue hyperemia,
edema, nasal congestion and an increase in nasal airway patency.

Guaifenesin has an expectorant action, which increases the output of respiratory tract fluid by
reducing adhesiveness and surface tension. By increasing respiratory tract fluid, guaifenesin
reduces the viscosity of secretions, and facilitates expectoration of retained secretions.
Guaifenesin is readily absorbed from the gastrointestinal tract and is rapidly metabolized and
renally excreted. Guaifenesin has a plasma half-life of one hour. The major urinary metabolite
is beta-(2-methoxyphenoxy) lactic acid. Sinus and bronchial drainage is improved and dry,
non-productive coughs become more productive and less frequent. Guaifenesin helps loosen
phlegm (mucus) and thin bronchial secretions to rid the bronchial passageways of bothersome
mucus, drain bronchial tubes, and make coughs more productive.

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