Pseudodine C

PSEUDODINE C- triprolidine hydrochloride, pseudoephedrine hydrochloride and codeine phosphate syrup
Wockhardt USA, Inc.

CV

Rx Only

DESCRIPTION

Each 5 mL (teaspoonful) of Pseudodine™ C Cough Syrup for oral administration contains:

Triprolidine Hydrochloride, USP ………….1.25 mg
Pseudoephedrine Hydrochloride, USP…..30 mg
Codeine Phosphate, USP ……………………10 mg
Alcohol ……………………………………………4.4%

In addition, the following inactive ingredients are present: Artificial Fruit Flavor; Artificial Raspberry Flavor; Liquid Sugar; Menthol, USP; Methylparaben, NF; Propylene Glycol, USP; Purified Water, USP; Sodium Benzoate, NF; Sodium Citrate, USP and Sorbitol Solution, USP. It may also contain Citric Acid, USP.

Pseudodine™ C Cough Syrup has antitussive, antihistaminic and nasal decongestant effects. The components of this product have the following chemical names and structural formulas:

Codeine Phosphate, USP:
7,8-Didehydro-4,5α-epoxy-3-methoxy-17-methylmorphinan-6α-ol phosphate (1:1) (salt) hemihydrate.

Chemical Structure
(click image for full-size original)

C18 H21 NO3 •H3 PO4 •½ H2 O M.W. 406.37

Triprolidine Hydrochloride, USP:
(E)-2-[3-(1-Pyrrolidinyl)-1-p -tolylpropenyl]pyridine monohydrochloride monohydrate.

Chemical Structure
(click image for full-size original)

C19 H22 N2 •HCl•H2 O M.W. 332.87

Pseudoephedrine Hydrochloride, USP:
Benzenemethanol, α-[1-(methylamino)ethyl]-, [S-(R*,R*)]-, hydrochloride.

Chemical Structure

C10 H15 NO•HCl M.W. 201.69

CLINICAL PHARMACOLOGY

Codeine

Codeine probably exerts its antitussive activity by depressing the medullary (brain) cough center, thereby raising its threshold for incoming cough impulses.

Codeine is readily absorbed from the gastrointestinal tract, with a therapeutic dose reaching peak antitussive effectiveness in about 2 hours and persisting for 4 to 6 hours. Codeine is rapidly distributed from blood to body tissues and taken up preferentially by parenchymatous organs such as liver, spleen and kidney. It passes the blood brain barrier and is found in fetal tissue and breast milk.

The drug is not bound by plasma proteins nor is it accumulated in body tissues. Codeine is metabolized in the liver to morphine and norcodeine, each representing about 10 percent of the administered codeine dose. About 90 percent of the dose is excreted within 24 hours, primarily through the kidneys. Urinary excretion products are free and glucuronide-conjugated codeine (about 70%), free and conjugated norcodeine (about 10%), free and conjugated morphine (about 10%), normorphine (under 4%) and hydrocodone (<1%). The remainder of the dose appears in the feces.

Triprolidine

Antihistamines such as triprolidine hydrochloride act as antagonists of the H1 histamine receptor. Consequently, they prevent histamine from eliciting typical immediate hypersensitivity responses in the nose, eyes, lungs and skin.

Animal distribution studies have shown localization of triprolidine in lung, spleen and kidney tissue. Liver microsome studies have revealed the presence of several metabolites with an oxidized product of the toluene methyl group predominating.

Pseudoephedrine

Pseudoephedrine acts as an indirect sympathomimetic agent by stimulating sympathetic (adrenergic) nerve endings to release norepinephrine. Norepinephrine in turn stimulates alpha and beta receptors throughout the body. The action of pseudoephedrine hydrochloride is apparently more specific for the blood vessels of the upper respiratory tract and less specific for the blood vessels of the systemic circulation. The vasoconstriction elicited at these sites results in the shrinkage of swollen tissues in the sinuses and nasal passages.

Pseudoephedrine is rapidly and almost completely absorbed from the gastrointestinal tract. Considerable variation in half-life has been observed (from about 4½ to 10 hours), which is attributed to individual differences in absorption and excretion. Excretion rates are also altered by urine pH, increasing with acidification and decreasing with alkalinization. As a result, mean half-life falls to about 4 hours at pH 5 and increases to 12 to 13 hours at pH 8.

After administration of a 60 mg tablet, 87 to 96% of the pseudoephedrine is cleared from the body within 24 hours. The drug is distributed to body tissues and fluids, including fetal tissue, breast milk and the central nervous system (CNS). About 55 to 75% of an administered dose is excreted unchanged in the urine; the remainder is apparently metabolized in the liver to inactive compounds by N-demethylation, parahydroxylation and oxidative deamination.

Pseudodine C Indications and Usage

Pseudodine™ C Cough Syrup is indicated for temporary relief of coughs and upper respiratory symptoms, including nasal congestion, associated with allergy or the common cold.

CONTRAINDICATIONS

Pseudodine™ C Cough Syrup is contraindicated under the following conditions:

Use in Newborn or Premature Infants

This drug should not be used in newborn or premature infants.

Use in Lower Respiratory Disease

Antihistamines should not be used to treat lower respiratory tract symptoms, including asthma.

Hypersensitivity to

(1) codeine phosphate or other narcotics; (2) triprolidine hydrochloride or other antihistamines of similar chemical structure; or (3) sympathomimetic amines, including pseudoephedrine.

Sympathomimetic amines are contraindicated in patients with severe hypertension, severe coronary artery disease and in patients on monoamine oxidase (MAO) inhibitor therapy (see PRECAUTIONS, Drug Interactions).

WARNINGS

Pseudodine™ C Cough Syrup should be used with considerable caution in patients with increased intraocular pressure (narrow angle glaucoma), stenosing peptic ulcer, pyloroduodenal obstruction, symptomatic prostatic hypertrophy, bladder neck obstruction, hypertension, diabetes mellitus, ischemic heart disease, and hyperthyroidism.

In the presence of head injury or other intracranial lesions, the respiratory depressant effects of codeine and other narcotics may be markedly enhanced, as well as their capacity for elevating cerebrospinal fluid pressure.

Narcotics also produce other CNS depressant effects, such as drowsiness, that may further obscure the clinical course of patients with head injuries.

Codeine or other narcotics may obscure signs on which to judge the diagnosis or clinical course of patients with acute abdominal conditions.

PRECAUTIONS

General

Pseudodine™ C Cough Syrup should be prescribed with caution for certain special-risk patients, such as the elderly or debilitated, and for those with severe impairment of renal or hepatic function, gallbladder disease or gallstones, respiratory impairment, cardiac arrhythmias, history of bronchial asthma, prostatic hypertrophy or urethral stricture, and in patients known to be taking other antitussive, antihistamine or decongestant medications. Patients’ self-medication habits should be investigated to determine their use of such medications. Pseudodine™ C Cough Syrup is intended for short-term use only.

Ultra-rapid Metabolizers of Codeine

Some individuals may be ultra-rapid metabolizers due to a specific CYP2D6*2×2 genotype. These individuals convert codeine into its active metabolite, morphine, more rapidly and completely than other people. This rapid conversion results in higher than expected serum morphine levels. Even at labeled dosage regiments, individuals who are ultra-rapid metabolizers may experience overdose symptoms such as extreme sleepiness, confusion or shallow breathing.

The prevalence of this CYP2D6 phenotype varies widely and has been estimated at 0.5 to 1% in Chinese and Japanese, 0.5 to 1% in Hispanics, 1 to 10% in Caucasians, 3% in African Americans, and 16 to 28% in North Africans, Ethiopians and Arabs. Data is not available for other ethnic groups.

When physicians prescribe codeine-containing drugs, they should choose the lowest effective dose for the shortest period of time and should inform their patients about these risks and the signs of morphine overdose. (See PRECAUTIONS-Nursing Mothers)

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