LUFYLLIN (dyphylline), a xanthine derivative, is a bronchodilator available for oral administration as tablets containing 200 mg and 400 mg of dyphylline. Other ingredients: magnesium stearate, microcrystalline cellulose.

Chemically, dyphylline is 7-(2,3-dihydroxypropyl)-theophylline, a white, extremely bitter, amorphous powder that is freely soluble in water and soluble in alcohol to the extent of 2 g/100 mL. Dyphylline forms a neutral solution that is stable in gastrointestinal fluids over a wide range of pH.

The molecular formula for dyphylline is C ₁₀ H ₁₄ N ₄ O ₄ with a molecular weight of 254.25. The structual formula is:

Last updated on RxList: 1/20/2005

For relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema.

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

Usual adult dosage:   Up to 15 mg/kg every six hours.

Appropriate dosage adjustments should be made in patients with impaired renal function (see Clinical PHARMACOLOGY ).

LUFYLLIN Tablets contain 200 mg dyphylline and are white, rectangular, scored on one side and imprinted WALLACE 521 on the other side. The tablets are available in bottles of 100 (NDC 0037-0521-92), 1000 (NDC 0037-0521-97), and 5000 (NDC 0037-0521-98).

LUFYLLIN-400 Tablets contain 400 mg dyphylline and are white, capsule-shaped, scored on one side and imprinted WALLACE 731 on the other side. The tablets are available in bottles of 100 (NDC 0037-0731-92), 1000 (NDC 0037-0731-97), and 2500 (NDC 0037-0731-99).

Storage:   Store at controlled room temperature 20°-25°C (68°-77°F).

Dispense in a tight container.

WALLACE LABORATORIES
Division of
Carter-Wallace, Inc.
Cranbury, New Jersey 08512

Last updated on RxList: 1/20/2005

Adverse reactions with the use of LUFYLLIN have been infrequent, relatively mild, and rarely required reduction in dosage or withdrawal of therapy.

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, 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, ventricular arrhythmias.

Respiratory:   tachypnea.

Renal:   albuminuria, gross and microscopic hematuria, diuresis.

Other:   hyperglycemia, inappropriate ADH syndrome.

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 (see Clinical PHARMACOLOGY ).

Last updated on RxList: 1/20/2005

LUFYLLIN 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.

General:   Use LUFYLLIN with caution in patients with severe cardiac disease, hypertension, hyperthyroidism, acute myocardial injury, or peptic ulcer.

Carcinogenesis, mutagenesis, impairment of fertility:   No long-term animal studies have been performed with LUFYLLIN.

Pregnancy:   Teratogenic effects Pregnancy Category C. Animal reproduction studies have not been conducted with LUFYLLIN. It is also not known if LUFYLLIN can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. LUFYLLIN 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 LUFYLLIN is administered to a nursing woman.

Pediatric use:   Safety and effectiveness in children have not been established.

Geriatric Use: Clinical studies of LUFYLLIN did not include sufficient numbers of subjects age 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

Last updated on RxList: 1/20/2005

There have been no reports, in the literature, of overdosage with LUFYLLIN. However, the following information based on reports of theophylline overdosage are 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 a 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.

Hypersensitivity to dyphylline or related xanthine compounds.

Last updated on RxList: 1/20/2005

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.

LUFYLLIN 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 LUFYLLIN.

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, congestive heart failure, 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 range of plasma levels within which dyphylline can be expected to produce effective bronchodilation has not been determined.

Dyphylline plasma concentrations can be accurately determined using high pressure liquid chromatography (HPLC) * or gas-liquid chromatography (GLC).

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* See Valia, et al., J. Chromatogr. 221 : 170 (1980). Small quantities of pure dyphylline powder may be obtained from Wallace Laboratories, Cranbury, N.J. The internal standard, (beta)-hydroxyethyl-theophylline, may be obtained from companies supplying analytical chemicals.

 

Last updated on RxList: 1/20/2005

No Information Provided.

See WARNINGS and PRECAUTIONS sections

Last updated on RxList: 1/20/2005

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.

DYPHYLLINE - ORAL

(DYE-fill-in)

COMMON BRAND NAME(S): Dilor, Lufyllin

USES: This medication is used to treat and prevent wheezing and trouble breathing caused by ongoing lung disease (e.g., asthma, emphysema, chronic bronchitis). Dyphylline belongs to a class of drugs known as xanthines. It works in the airways by relaxing muscles, opening air passages to improve breathing, and decreasing the lungs' response to irritants. Controlling symptoms of breathing problems can decrease time lost from work or school.

HOW TO USE: Take this medication by mouth with or without food, usually 4 times daily or as directed by your doctor. If this medication upsets your stomach, you may take it with food.

If you are taking a liquid form, use a medication-measuring device to carefully measure the prescribed dose. Do not use a household spoon.

If you are taking a tablet scored with a line, you may break it before swallowing.

Dosage is based on your medical condition and response to therapy.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: Stomach pain/cramping, nausea, vomiting, diarrhea, loss of appetite, headache, trouble sleeping, irritability, restlessness, nervousness, shaking, flushing, and increased urination may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because 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: confusion, dizziness, mental/mood changes, muscle twitching/pain/tenderness, weakness, rapid breathing.

Tell your doctor immediately if any of these rare but very serious side effects occur: fainting, fast/slow/irregular heartbeat, vomit that looks like coffee grounds, dark/tarry stools, blood in urine, seizures.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, red/scaly skin, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact 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 using dyphylline, tell your doctor or pharmacist if you are allergic to it; or to theophylline, theobromine or caffeine; or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: glaucoma, diabetes, heart problems (e.g., angina, irregular heartbeat), high blood pressure, kidney disease, seizures, stomach/intestinal ulcer, overactive thyroid (hyperthyroidism).

This drug may make you dizzy. Use caution while driving, using machinery, or doing any activity that requires alertness. Limit alcoholic beverages.

Liquid preparations of this product may contain sugar and/or alcohol. Caution is advised if you have diabetes, alcohol dependence, or liver disease. Ask your doctor or pharmacist about using this product safely.

Before having surgery, tell your doctor or dentist that you are using this medication.

Kidney function declines as you grow older. This medication is removed by the kidneys. Therefore, caution is advised when using this drug in the elderly because they may be more sensitive to its effects.

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

This drug passes into breast milk and may have undesirable effects on a nursing infant (e.g., irritability). Consult your doctor before breast-feeding.

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

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: adenosine, adrenaline-like drugs (e.g., ephedrine, phenylephrine, pseudoephedrine), certain antiarrhythmic drugs (e.g., mexiletine, propafenone), benzodiazepines (e.g., diazepam, flurazepam), certain beta blockers (e.g., propranolol), digoxin, isoproterenol, lithium, probenecid.

Check the labels on all your medicines (e.g., cough-and-cold products, diet aids) because they may contain ingredients that could increase the side effects of this medication. Ask your pharmacist about using those products safely.

Caffeine and alcohol can increase the side effects of this medication. Avoid drinking large amounts of beverages containing alcohol or caffeine (e.g., coffee, tea, colas), or eating large amounts of chocolate.

This medication may interfere with certain medical/laboratory tests (e.g., dipyridamole-thallium imaging tests), 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: agitation, nausea, frequent vomiting, trouble sleeping, unusual thirst, fever, ringing in the ears, fast/irregular heartbeat, seizures, confusion, chest pain.

NOTES: Do not share this medication with others.

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 in a tightly closed container at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. Do not freeze liquid forms of this medication. 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.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-800-854-1166 (USA) or 1-800-668-1507 (Canada).

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