Each bisected, blue Guaifenex® PSE 60 capsule shaped extended-release tablet provides 60 mg pseudoephedrine hydrochloride and 600 mg guaifenesin in an extended-release formulation intended for oral administration. Inactive ingredients: calcium phosphate dibasic, hydroxypropyl methylcellulose, lactose, lake blue No. 1 FD&C, magnesium stearate, povidone, silicon dioxide colloidal, and stearic acid.

Guaifenesin is an expectorant. Chemically, it is 3-(2-methoxyphe-noxy)-1, 2-propanediol and has the following structural formula:

Pseudoephedrine hydrochloride is a nasal decongestant. Chemically, it is [S-(R*,R*)]-α-[1-(methylamino)ethyl] benzen-emethanol hydrochloride and has the following structural formula:

Guaifenex® PSE 60 Extended-release Tablets are indicated for the temporary relief of nasal congestion and cough associated with respiratory tract infections and related conditions such as sinusitis, pharyngitis, bronchitis, and asthma, when these conditions are complicated by tenacious mucous and/or mucous plugs and congestion. The product is effective in productive as well as non-productive cough, but is of particular value in dry, non-productive cough which tends to injure the mucous membrane of the air passages.

Adults and pediatric patients over 12 years of age: One or two tablets every 12 hours not to exceed 4 tablets in 24 hours. Pediatric patients 6 to 12 years: 1 tablet every 12 hours not to exceed 2 tablets in 24 hours. Pediatric patients 2 to 6 years: ½ tablet every 12 hours not to exceed 1 tablet in 24 hours.

Guaifenex® PSE 60 Extended-release Tablets are available as bisected, capsule shaped blue tablets, debossed “ETHEX/214”. Bottles of 100 tablets (NDC 58177-214-04).

Store at controlled room temperature, 15°-30°C (59°-86°F).

Dispense in tight, light-resistant containers as defined in the USP .

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

Manufactured by : KV Pharmaceutical Co. for ETHEX Corporation, St. Louis, MO 63043-2413. 8/98. FDA revision date: n/a

Hyper-reactive individuals may display ephedrine-like reactions such as tachycardia, palpitations, headache, dizziness, or nausea. Sympathomimetics have been associated with certain untoward reactions including fear, anxiety, nervousness, restlessness, tremor, weakness, pallor, respiratory difficulty, dysuria, insomnia, hallucinations, convulsions, CNS depression, arrhythmias, and cardiovascular collapse with hypotension. No serious side effects have been reported with the use of guaifenesin.

Do not prescribe this product for use in patients that are now taking a prescription MAOI (certain drugs for depression, psychiatric or emotional conditions, or Parkinson's disease), or for 14 days after stopping the MAOI drug therapy. Beta-adrenergic blockers and MAOI inhibitors may potentiate the pressor effect of pseudoephedrine. Concurrent use of digitalis glycosides may increase the possibility of cardiac arrhythmias. Sympathomimetics may reduce the hypotensive effects of guanethidine, mecamylamine, methyldopa, reserpine and veratrum alkaloids. Concurrent use of tricyclic antidepressants may antagonize the effects of pseudoephedrine.

Drug/Laboratory Test Interactions: Guaifenesin may increase renal clearance for urate and thereby lower serum uric acid levels. Guaifenesin may produce an increase in urinary 5-hydroxy-indoleacetic 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.

Sympathomimetic amines should be used with caution in patients with hypertension, ischemic heart disease, diabetes mellitus, increased intraocular pressure, hyperthyroidism, or prostatic hypertrophy. Sympathomimetics may produce central nervous system stimulation with convulsions or cardiovascular collapse with accompanying hypotension. Do not exceed recommended dosage.

Hypertensive crisis can occur with concurrent use of pseudoephedrine or phenylephrine and monoamine oxidase (MAO) inhibitors, indomethacin, or with beta-blockers and methyl-dopa. If a hypertensive crisis occurs, these drugs should be discontinued immediately and therapy to lower blood pressure should be instituted. Fever should be managed by means of external cooling.

General: Use with caution in patients with diabetes, hypertension, cardiovascular disease and hyper-reactivity to ephedrine.

Before prescribing medication to suppress or modify cough, it is important to ascertain that the underlying cause of cough is identified, that modification of cough does not increase the risk of clinical or physiologic complications, and that appropriate therapy for the primary disease is instituted.

Pediatric Use: Safety and effectiveness in pediatric patients below the age of 2 years has not been established. This product is not recommended for use in pediatric patients under 2 years of age.

Geriatric Use: The elderly (60 years and older) are more likely to experience adverse reactions to sympathomimetics. Overdosage of sympathomimetics in this age group may cause hallucinations, convulsions, CNS depression, and death. Clinical studies of Guaifenex® PSE 60 Extended-release Tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Carcinogenesis, Mutagenesis, Impairment of Fertility: No data are available on the long-term potential of the components of this product for carcinogenesis, mutagenesis, or impairment of fertility in animals or humans.

Pregnancy: Teratogenic Effects: Pregnancy Category C. Animal reproduction studies have not been conducted with the components of this product. It is also not known whether these drugs can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Accordingly, this product should be given to a pregnant woman only if clearly needed.

Nursing Mothers: Pseudoephedrine is excreted in breast milk. Use of this product by nursing mothers is not recommended because of the higher than usual risk for infants from sympathomimetic amines.

Since Guaifenex® PSE 60 Extended-release Tablets contain two pharmacologically different compounds, treatment of overdosage should be based upon the symptomatology of the patient as it relates to the individual ingredients. Treatment of acute overdosage would probably be based upon treating the patient for pseudoephedrine toxicity which may manifest itself as excessive CNS stimulation resulting in excitement, tremor, restlessness, and insomnia. Other effects may include tachycardia, hypertension, pallor, mydriasis, hyperglycemia and urinary retention. Severe overdosage may cause tachypnea or hyperpnea, hallucinations, convulsions or delirium, but in some individuals there may be CNS depression with somnolence, stupor or respiratory depression. Arrhythmias (including ventricular fibrillation) may lead to hypotension and circulatory collapse. Severe hypokalemia can occur, probably due to a compartmental shift rather than a depletion of potassium. No organ damage or significant metabolic derangement is associated with pseudoephedrine overdosage. Overdosage with guaifenesin is unlikely to produce toxic effects since its toxicity is much lower than that of pseudoephedrine.

The LD₅₀ of pseudoephedrine (single oral dose) has been reported to be 726 mg/kg in the mouse, 2206 mg/kg in the rat and 1177 mg/kg in the rabbit. The toxic and lethal concentrations in human biologic fluids are not known. Urinary excretion increases with acidification and decreases with alkalinization of the urine. There are few published reports of toxicity due to pseudoephedrine and no case of fatal overdosage has been reported. Guaifenesin, when administered by stomach tube to test animals in doses up to 5 grams/kg, produced no signs of toxicity.

Since the action of extended-release products may continue for as long as 12 hours, treatment of overdosage should be directed toward reducing further absorption and supporting the patient for at least that length of time. Gastric emptying (Syrup of Ipecac) and/or lavage is recommended as soon as possible after ingestion, even if the patient has vomited spontaneously. Either isotonic or half-isotonic saline may be used for lavage. Administration of an activated charcoal slurry is beneficial after lavage and/or emesis if less than 4 hours have passed since ingestion. Saline cathartics, such as Milk of Magnesia, are useful for hastening the evacuation of unreleased medication.

Adrenergic receptor blocking agents are antidotes to pseudoephedrine. In practice, the most useful is the beta-blocker propranolol which is indicated when there are signs of cardiac toxicity. Theoretically, pseudoephedrine is dialyzable but procedures have not been clinically established.

In severe cases of overdosage, it is essential to monitor both the heart (by electrocardiograph) and plasma electrolytes, and to give intravenous potassium as indicated. Vasopressors may be used to treat hypotension. Excessive CNS stimulation may be counteracted with parenteral diazepam. Stimulants should not be used.

This product is contraindicated in patients with hypersensitivity to guaifenesin, or with hypersensitivity or idiosyncrasy to sympathomimetic amines which may be manifested by insomnia, dizziness, weakness, tremor or arrhythmias.

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

Pseudoephedrine hydrochloride is an orally indirect acting sympathomimetic amine and exerts a decongestant action on the nasal mucosa. It does this by vasocon-striction which results in reduction of tissue hyperemia, edema, nasal congestion, and an increase in nasal airway patency. The vasoconstriction action of pseudoephedrine is similar to that of ephedrine. In the usual dose it has minimal vasopressor effects. Pseudoephedrine is rapidly and almost completely absorbed from the gastrointestinal tract. It has a plasma half-life of 6 to 8 hours. Acidic urine is associated with faster elimination of the drug. The drug is distributed to body tissues and fluids, including the fetal tissue, breast milk and the central nervous system (CNS). Approximately 50% to 75% of the 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.

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.

Patients should be instructed to check with physician if symptoms do not improve within 5 days or if fever is present.

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

GUAIFENESIN/PSEUDOEPHEDRINE SUSTAINED-RELEASE - ORAL

(gweye-FEN-eh-sin/sue-doh-eff-ED-rin)

USES: Guaifenesin/pseudoephedrine is used for the temporary relief of nose/sinus/ear congestion and cough with phlegm caused by the common cold, allergies, or infection. Pseudoephedrine is called a sympathomimetic and works by decreasing the swelling of nose and ear tissues and opening nose passages. Guaifenesin is called an expectorant. It works by making phlegm in the breathing tubes more liquid. This helps the cough to clear phlegm better.

Do not use this medication in children younger than 6 years unless specifically directed by the doctor. Some products are not recommended for use in children younger than 12 years. Consult with the doctor or pharmacist regarding your specific product. To decrease the risk for serious side effects, carefully follow all of the doctor's dosage directions. Do not give other cough and cold medication that might contain the same or similar ingredients (see also Drug Interactions section). Ask your doctor or pharmacist about other ways to relieve cough and cold symptoms (e.g., saline nose drops/spray, using a humidifier or infant nasal suction bulb).

HOW TO USE: Take this medication by mouth, usually every 12 hours with a full glass of water or as directed by your doctor. If stomach upset occurs, take with food or milk. Sustained-release products should be swallowed whole. Do not crush, chew, or split this medication. Doing so can destroy the long action of the drug and may increase side effects.

Dosage is based on your age, medical condition and response to therapy. If this medication does not require a prescription from your doctor, follow the specific dosing instructions on the packaging to find the correct dose for your age.

If your doctor directs you to take this medication daily, take it regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.

If your symptoms do not improve after 7 days, if they worsen, or if you develop a fever/chills, contact your doctor. Do not take more medication than is recommended.

SIDE EFFECTS: Mild stomach upset, trouble sleeping, dizziness, lightheadedness, headache, nervousness, fast heartbeat, loss of appetite, shaking, or unusual sweating may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

This product may reduce blood flow to your hands and feet, causing them to feel cold. Smoking may worsen this effect. Dress warmly and avoid tobacco use.

If your doctor has directed you to use this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: fast/irregular heartbeat, severe/uncontrolled shaking, difficulty urinating, decreased sexual ability.

Tell your doctor immediately if any of these rare but very serious side effects occur: seizures, mental/mood changes (e.g., anxiety, panic, hallucinations).

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, tell your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking this medication, tell your doctor or pharmacist if you are allergic to pseudoephedrine or guaifenesin; or if you have any other allergies. Also tell your doctor if you have had a negative reaction to other sympathomimetics (e.g., ephedrine, phenylephrine).

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: severe high blood pressure, heart disease (e.g., severe coronary artery disease, angina, heart failure), certain types of fast heart rhythm problems (e.g., atrial fibrillation/flutter, paroxysmal supraventricular tachycardia-PSVT), a certain slow heart rhythm problem (sinus bradycardia), closed-angle glaucoma, difficulty urinating (e.g., due to enlarged prostate).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: stroke, high blood pressure, chest pain (angina), heart attack, smoking, long-term breathing problems (e.g., asthma, chronic bronchitis, emphysema), cough with large amounts of phlegm, mental/mood disorders (e.g., anxiety, bipolar disorder, mania), epilepsy/seizure problems, certain blood vessel problems (e.g., Raynaud's disease, peripheral vascular disease), overactive thyroid (hyperthyroidism), low blood flow to the brain (cerebral insufficiency), diabetes, difficulty sleeping.

This drug may make you dizzy or lightheaded; use caution engaging in activities requiring alertness such as driving or using machinery. Limit alcoholic beverages.

Caution is advised when using this drug in the elderly because they may be more sensitive to its effects, especially dizziness and lightheadedness.

Caution is advised when using this product in children because they may be more sensitive to its side effects, especially excitation, agitation, and increased blood pressure.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

The pseudoephedrine in this product passes into breast milk. It is not known whether guaifenesin passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

This drug should not be used with the following medications because very serious interactions may occur: MAO inhibitors (e.g., furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine).

Avoid taking MAO inhibitors within 2 weeks before, during, and after treatment with this medication. In some cases a serious, possibly fatal drug interaction may occur.

If you are currently using any of these medications, tell your doctor or pharmacist before starting this product.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: other decongestants (taken by mouth or sprayed into the nose), products containing caffeine, some blood pressure medications (e.g., beta blockers, calcium channel blockers, reserpine, guanethidine, methyldopa, mecamylamine), tricyclic antidepressants (e.g., nortriptyline, amitriptyline), digoxin.

Pseudoephedrine may worsen the serious side effects of some medications used for migraine headaches (e.g., sumatriptan, naratriptan, zolmitriptan, ergotamine). Consult your pharmacist or doctor for more details.

Check the labels on all your medicines (e.g., cough-and-cold products, diet aids) because they may contain ingredients that could increase your heart rate or blood pressure. Ask your pharmacist about the safe use of those products before using them.

Pseudoephedrine and guaifenesin are available in both prescription and nonprescription products. Check the labels of all your medications carefully to make sure you are not taking more than one product containing these medications.

The guaifenesin in this product can affect the results of certain lab tests (e.g., uric acid levels, 5-hydroxyindoleacetic acid levels, vanillylmandelic acid levels), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe dizziness/fainting, severe weakness, fast irregular heartbeat, slow/shallow breathing, hallucinations, seizures, vomiting.

NOTES: Do not share this medication with others.

Drink plenty of fluids while taking this medication unless your doctor instructs you otherwise. This may help to relieve congestion. This medication is for temporary use only. Do not use for more than 7 days without first consulting your doctor.

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature at 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.