Dyphylline and Guaifenesin Tablets

Dosage Form: tablet

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Dyphylline and Guaifenesin
Tablets, USP

Rx Only

Dyphylline and Guaifenesin Tablets Description

Dyphylline and Guaifenesin Tablets are a bronchodilator/expectorant combination available for oral administration.

Each tablet contains:

Dyphylline 200 mg
Guaifenesin 200 mg

Dyphylline is a bronchodilator which occurs as a white, odorless, extremely bitter, amorphous or crystalline solid. It is freely soluble in water; sparingly soluble in alcohol and in chloroform; practically insoluble in ether. The chemical name is 1H-Purine-2,6-dione, 7-(2,3-dihydroxypropyl)-3,7-dihydro-1,3-dimethyl-, (±)-. Its structural formula is as follows:

C10H14N4O4      M.W. 254.24

Guaifenesin is an expectorant which occurs as 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. The chemical name is 1,2-Propanediol, 3-(2-methoxyphenoxy)-, (±)-. Its structural formula is as follows:

C10H14O4      M.W. 198.22

INACTIVE INGREDIENTS: Magnesium Stearate, Maltodextrin, Microcrystalline Cellulose, Povidone, Silica and Stearic Acid.

Dyphylline and Guaifenesin Tablets - Clinical Pharmacology

Dyphylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree. The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle.

Dyphylline is well tolerated and produces less nausea than aminophylline and other alkaline theophylline compounds when administered orally. Unlike the hydrolyzable salts of theophylline, dyphylline is not converted to free theophylline in vivo. It is absorbed rapidly in therapeutically active form and in healthy volunteers reaches a mean peak plasma concentration of 17.1 mcg/mL in approximately 45 minutes following a single oral dose of 1000 mg of dyphylline.

Dyphylline exerts its bronchodilatory effects directly and, unlike theophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Because of this, dyphylline pharmacokinetics and plasma levels are not influenced by various factors that affect liver function and hepatic enzyme activity, such as smoking, age, or concomitant use of drugs which affect liver function.

The elimination half-life of dyphylline is approximately two hours (1.8-2.1 hr.) and approximately 88% of a single oral dose can be recovered from the urine unchanged. The renal clearance would be correspondingly reduced in patients with impaired renal function. In anuric patients, the half-life may be increased 3 to 4 times normal.

Dyphylline plasma levels are dose-related and generally predictable. The therapeutic range of plasma levels within which dyphylline can be expected to produce effective bronchodilation has not been determined.

Guaifenesin is an expectorant which increases respiratory tract fluid secretions and helps to loosen phlegm and bronchial secretions. By reducing the viscosity of secretions, guaifenesin increases the efficiency of the cough reflex and of ciliary action in removing accumulated secretions from the trachea and bronchi. Guaifenesin is readily absorbed from the gastrointestinal tract and is rapidly metabolized and excreted in the urine. Guaifenesin has a plasma half-life of one hour. The major urinary metabolite is β-(2-methoxyphenoxy) lactic acid.

Indications and Usage for Dyphylline and Guaifenesin Tablets

Dyphylline and Guaifenesin is indicated as a bronchodilator-expectorant for treating bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Dyphylline and Guaifenesin acts to dilate bronchioles and liquefy mucus, giving relief from dyspnea, non-productive cough and tracheobronchial irritation.

Contraindications

Hypersensitivity to any of the ingredients or related compounds.

Warnings

This product is not indicated in the management of status asthmaticus, which is a serious medical emergency. Although the relationship between plasma levels of dyphylline and appearance of toxicity is unknown, excessive doses may be expected to be associated with an increased risk of adverse effects.

Do not use this product unless a diagnosis of asthma has been made by a doctor. Do not use this product if you have heart disease, high blood pressure, thyroid disease, diabetes, or difficulty in urination due to enlargement of the prostate gland unless directed by a doctor. Do not use this product if you have ever been hospitalized for asthma or if you are taking any prescription drug for asthma unless directed by a doctor.

Precautions

General

Use Dyphylline and Guaifenesin with caution in patients with severe cardiac disease, hypertension, hyperthyroidism, acute myocardial injury or peptic ulcer. Before prescribing medication to suppress or modify cough, it is important to ascertain that the underlying cause of the cough is identified, that modification of the cough does not increase the risk of clinical or physiological complications, and that appropriate therapy for the primary disease is instituted.

Drug/Laboratory Test Interactions

Synergism between xanthine bronchodilators (e.g., theophylline), ephedrine, and other sympathomimetic bronchodilators has been reported. This should be considered whenever these agents are prescribed concomitantly. Concurrent administration of dyphylline and probenecid, which competes for tubular secretion, has been shown to increase the plasma half-life of dyphylline. Guaifenesin may increase renal clearance for urate and thereby lower serum uric acid levels. Guaifenesin may produce an increase in urinary 5- hydroxyindoleacetic acid and may therefore interfere with the interpretation of this test for the diagnosis of carcinoid syndrome. It may also falsely elevate the VMA test for catechols. Administration of this drug should be discontinued 48 hours prior to the collection of urine specimens for such tests.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term animal studies have been performed with this product.

Pregnancy

Pregnancy Category C

Animal reproduction studies have not been conducted with this formulation. It is also not known whether this product can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. This medication should be given to a pregnant woman only if clearly needed.

Nursing Mothers

Dyphylline is present in human milk at approximately twice the maternal plasma concentration. Caution should be exercised when this product is administered to a nursing woman.

Pediatric Use

This product is not indicated for use in the pediatric population.

Adverse Reactions

This formulation may cause nausea, headache, cardiac palpitation and CNS stimulation. Postprandial administration may help avoid gastric discomfort.

The following adverse reactions which have been reported with other xanthine bronchodilators, and which have most often been related to excessive drug plasma levels, should be considered as potential adverse effects when dyphylline is administered.

Gastrointestinal: nausea, vomiting, epigastric pain, hematemesis, and diarrhea.

Central Nervous System: headache, irritability, restlessness, insomnia, hyperexcitability, agitation, muscle twitching, generalized clonic and tonic convulsions.

Cardiovascular: palpitation, tachycardia, extrasystoles, flushing, hypotension, circulatory failure, and ventricular arrhythmias.

Respiratory: tachypnea.

Renal: albuminuria, gross and microscopic hematuria, diuresis.

Other: hyperglycemia, inappropriate ADH syndrome.

Overdosage

There have been no reports, in the literature, of overdosage with this product. However, the following information based on reports of theophylline overdosage is considered typical of the xanthine class of drugs and should be kept in mind.

SIGNS AND SYMPTOMS

Restlessness, anorexia, nausea, vomiting, diarrhea, insomnia, irritability, and headache. Marked overdosage with resulting severe toxicity has produced agitation, severe vomiting, dehydration, excessive thirst, tinnitus, cardiac arrhythmias, hyperthermia, diaphoresis, and generalized clonic and tonic convulsions. Cardiovascular collapse has also occurred, with some fatalities. Seizures have occurred in some cases associated with very high theophylline plasma concentrations, without any premonitory symptoms of toxicity.

TREATMENT

There is no specific antidote for overdosage with drugs of the xanthine class. Symptomatic treatment and general supportive measures should be instituted with careful monitoring and maintenance of vital signs, fluids and electrolytes. The stomach should be emptied by inducing emesis if the patient is conscious and responsive, or by gastric lavage, taking care to protect against aspiration, especially in stuporous, or comatose patients. Maintenance of an adequate airway is essential in case oxygen or assisted respiration is needed. Sympathomimetic agents should be avoided but sedatives such as short-acting barbiturates may be useful.

Dyphylline is dialyzable and, although not recommended as routine procedure in overdosage cases, hemodialysis may be of some benefit when severe intoxication is present or when the patient has not responded to general supportive and symptomatic treatment.

Dyphylline and Guaifenesin Tablets Dosage and Administration

Dosage should be individually titrated according to the severity of the condition and the response of the patient.

USUAL ADULT DOSAGE

1 tablet four times daily.

This product is not indicated for use in the pediatric population. (see PRECAUTIONS, Pediatric Use.)

How is Dyphylline and Guaifenesin Tablets Supplied

Dyphylline and Guaifenesin are round, white, compressed tablets, debossed B 375. They are packaged in bottles of 100, NDC # 51991-375-01.

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN. IN CASE OF ACCIDENTAL OVERDOSE, SEEK PROFESSIONAL ASSISTANCE OR CONTACT A POISON CONTROL CENTER IMMEDIATELY.

Dispense in a tight, light-resistant container with a child-resistant closure as defined in the USP/NF.

STORAGE

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F). See USP Controlled Room Temperature.

All prescription substitutions using this product shall be pursuant to state statutes as applicable. This is not an Orange Book product.

Distributed by: Breckenridge Pharmaceutical, Inc., Boca Raton, FL 33487

Manufactured by: Contract Pharmacal Corp., Hauppauge, NY 11788

Iss.10/03
Rev. 11/08

Made in USA

PRINCIPAL DISPLAY PANEL - 100 Tablet Bottle Label

Breckenridge
Pharmaceutical, Inc.

NDC 51991-375-01

Dyphylline
& Guaifenesin

Tablets, USP

Bronchodilator - Expectorant

Rx Only

100 Tablets

DYPHYLLINE AND GUAIFENESIN 
dyphylline and guaifenesin tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:51991-375
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Dyphylline (Dyphylline) Dyphylline 200 mg
Guaifenesin (Guaifenesin) Guaifenesin 200 mg
Inactive Ingredients
Ingredient Name Strength
Magnesium stearate  
Maltodextrin  
Cellulose, Microcrystalline  
Povidone  
Silicon Dioxide  
Stearic Acid  
Product Characteristics
Color WHITE Score 2 pieces
Shape ROUND Size 10312mm
Flavor Imprint Code B;375
Contains         
Packaging
# Item Code Package Description
1 NDC:51991-375-01 100 TABLET (TABLET) in 1 BOTTLE, PLASTIC
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
UNAPPROVED DRUG OTHER 08/01/2001 02/29/2012
Labeler - Breckenridge Pharmaceutical, Inc. (150554335)
Establishment
Name Address ID/FEI Operations
Contract Pharmacal 057795122 MANUFACTURE
Revised: 01/2011
 
Breckenridge Pharmaceutical, Inc.
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