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Theophylline Uses

Uses Dosage Side effects Pregnancy Overdose Actions

What is Theophylline?

Theophylline injection is used together with other medicines to treat the acute symptoms of asthma, bronchitis, emphysema, and other lung diseases in a hospital setting.

Theophylline belongs to a group of medicines known as bronchodilators. Bronchodilators are medicines that relax the muscles in the bronchial tubes (air passages) of the lungs. They relieve cough, wheezing, shortness of breath, and troubled breathing by increasing the flow of air through the bronchial tubes.

Theophylline is available only with your doctor’s prescription.

Theophylline indications

An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.

Adult: 300-1,000 mg in divided doses 6-8 hrly. As modified-release preparation: 175-500 mg 12 hrly.

Child: <6 yr Not recommended; 6-12 yr 20-35 kg: 120-250 mg bid; >12 yr 250-500 mg bid.

Elderly: Lower doses should be used.

Hepatic impairment: Reduce dose.Intravenous

Acute severe bronchospasm

Adult: Patients not taking Theophylline or other xanthine medication: Loading dose: 4-5 mg/kg by infusion over 20-30 min. Maintenance dose: 0.4-0.6 mg/kg/hr.

Child: Patients not taking Theophylline or other xanthine medication: Loading dose: 4-5 mg/kg by infusion over 20-30 min. Maintenance dose: 1-9 yr Initially, 0.8-1 mg/kg/hr; >9-12 yr Initially, 0.7-0.77 mg/kg/hr.

Elderly: Lower doses should be used.

Hepatic impairment: Reduce dose.

Incompatibility: Y-site: Cefepime, hetastarch in normal saline, phenytoin, ceftazidime. Syringe: Ceftriaxone.

Special Populations: Reduce dose in patients w/ cor pulmonale, heart failure, liver disease and fever. Smokers and those who consume alcohol may require higher maintenance dose.

How should I use Theophylline?

Use Theophylline sustained-release capsules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

  • Some foods may change the effectiveness or increase the side effects of Theophylline sustained-release capsules. Talk to your doctor about how you should take Theophylline sustained-release capsules with regard to food. Do not suddenly change your diet or eating habits without first checking with your doctor.
  • Swallow Theophylline sustained-release capsules whole. Do not break, crush, or chew before swallowing.
  • Take Theophylline sustained-release capsules at about the same time(s) each day. If you are using more than 1 dose per day, try to take the second dose 10 to 12 hours after your first dose and before the evening meal. Check with your doctor or pharmacist if you have questions about how to take Theophylline sustained-release capsules.
  • If you are using 1 dose per day, take Theophylline sustained-release capsules in the morning unless your doctor tells you otherwise.
  • Continue to take Theophylline sustained-release capsules even if you feel well. Do not miss any doses.
  • If you miss a dose of Theophylline sustained-release capsules, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Theophylline sustained-release capsules.

Uses of Theophylline in details

There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.

Theophylline is used to treat lung diseases such as asthma and COPD (bronchitis, emphysema). It must be used regularly to prevent wheezing and shortness of breath. This medication belongs to a class of drugs known as xanthines. It works in the airways by relaxing muscles, opening breathing passages, and decreasing the lungs’ response to irritants. Controlling symptoms of breathing problems can decrease time lost from work or school.

This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden breathing problems. If sudden shortness of breath occurs, use your quick-relief inhaler as prescribed.

How to use Theophylline

Take this medication by mouth as directed by your doctor, usually once or twice daily. Since different manufacturers have different ways to take this medication, ask your doctor or pharmacist about the best time(s) to take your brand of Theophylline and if you should take the drug with or without food.

Do not crush or chew the capsules or tablets. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split the tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.

The dosage is based on your medical condition, response to treatment, age, weight, lab tests (Theophylline blood levels), and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor’s instructions carefully.

Certain diets (such as high protein/low carbohydrate or high carbohydrate/low protein) may change the effect of Theophylline. Tell your doctor if you have any major changes in your diet. Your doctor may need to adjust your dose.

Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day. Keep taking this medication even if you feel well. Do not increase your dose, take this drug more often, or stop taking it without first consulting your doctor.

Get medical help right away if your asthma symptoms worsen or if you are using your quick-relief inhaler more than usual or more often than prescribed.

Theophylline description

Theophylline is a chiral compound. The racemic mixture can be divided into its optical antipodes: levo- and dextro-amphetamine. Theophylline is the parent compound of its own structural class, comprising a broad range of psychoactive derivatives, e.g., MDMA (Ecstasy) and the N-methylated form, methamphetamine. Theophylline is a homologue of phenethylamine.

Theophylline dosage

General Considerations

Theophylline (Theophylline capsule) ®, like other extended-release Theophylline products, is intended for patients with relatively continuous or recurring symptoms who have a need to maintain therapeutic serum levels of Theophylline. It is not intended for patients experiencing an acute episode of bronchospasm (associated with asthma, chronic bronchitis, or emphysema). Such patients require rapid relief of symptoms and should be treated with an immediate-release or intravenous Theophylline preparation (or other bronchodilators) and not with extended-release products.

Patients who metabolize Theophylline at a normal or slow rate are reasonable candidates for once-daily dosing with Theophylline (Theophylline capsule) ®. Patients who metabolize Theophylline rapidly (e.g., the young, smokers, and some nonsmoking adults) and who have symptoms repeatedly at the end of a dosing interval, will require either increased doses given once a day or preferably, are likely to be better controlled by a schedule of twice-daily dosing. Those patients who require increased daily doses are more likely to experience relatively wide peak-trough differences and may be candidates for twice-a-day dosing with Theophylline (Theophylline capsule) ®.

Patients should be instructed to take this medication each morning at approximately the same time and not to exceed the prescribed dose.

Recent studies suggest that dosing of extended-release Theophylline products at night (after the evening meal) results in serum concentrations of Theophylline which are not identical to those recorded during waking hours and may be characterized by early trough and delayed peak levels. This appears to occur whether the drug is given as an immediate-release, extended-release, or intravenous product. To avoid this phenomenon when two doses per day are prescribed, it is recommended that the second dose be given 10 to 12 hours after the morning dose and before the evening meal.

Food and posture, along with changes associated with circadian rhythm, may influence the rate of absorption and/or clearance rates of Theophylline from extended-release dosage forms administered at night. The exact relationship of these and other factors to nighttime serum concentrations and the clinical significance of such findings require additional study. Therefore, it is not recommended that

Theophylline (Theophylline capsule) ® (when used as a once-a-day product) be administered at night.

Patients who require a relatively high dose of Theophylline (i.e., a dose equal to or greater than 900 mg or 13 mg/kg, whichever is less) should not take Theophylline (Theophylline capsule) ® less than 1 hour before a high-fat-content meal since this may result in a significant increase in peak serum level and in the extent of absorption of Theophylline as compared to administration in the fasted state.

The steady-state peak serum Theophylline concentration is a function of the dose, the dosing interval, and the rate of Theophylline absorption and clearance in the individual patient. Because of marked individual differences in the rate of Theophylline clearance, the dose required to achieve a peak serum Theophylline concentration in the 10-20 mcg/mL range varies fourfold among otherwise similar patients in the absence of factors known to alter Theophylline clearance (e.g., 400-1600 mg/day in adults < 60 years old and 10-36 mg/kg/day in children 1-9 years old). For a given population there is no single Theophylline dose that will provide both safe and effective serum concentrations for all patients. Administration of the median Theophylline dose required to achieve a therapeutic serum Theophylline concentration in a given population may result in either sub-therapeutic or potentially toxic serum Theophylline concentrations in individual patients. For example, at a dose of 900 mg/day in adults < 60 years or 22 mg/kg/day in children 1-9 years, the steady-state peak serum Theophylline concentration will be < 10 mcg/mL in about 30% of patients, 10-20 mcg/mL in about 50% and 20-30 mcg/mL in about 20% of patients. The dose of Theophylline must be individualized on the basis of peak serum Theophylline concentration measurements in order to achieve a dose that will provide maximum potential benefit with minimal risk of adverse effects.

Transient caffeine-like adverse effects and excessive serum concentrations in slow metabolizers can be avoided in most patients by starting with a sufficiently low dose and slowly increasing the dose, if judged to be clinically indicated, in small increments. Dose increases should only be made if the previous dosage is well tolerated and at intervals of no less than 3 days to allow serum Theophylline concentrations to reach the new steady state. Dosage adjustment should be guided by serum Theophylline concentration measurement. Health care providers should instruct patients and care givers to discontinue any dosage that causes adverse effects, to withhold the medication until these symptoms are gone and to then resume therapy at a lower, previously tolerated dosage.

If the patient’s symptoms are well controlled, there are no apparent adverse effects, and no intervening factors that might alter dosage requirements, serum Theophylline concentrations should be monitored at 6 month intervals for rapidly growing children and at yearly intervals for all others. In acutely ill patients, serum Theophylline concentrations should be monitored at frequent intervals, e.g., every 24 hours.

Theophylline distributes poorly into body fat, therefore, mg/kg dose should be calculated on the basis of ideal body weight. Table V contains Theophylline dosing titration schema recommended for patients in various age groups and clinical circumstances. Table VI contains recommendations for Theophylline dosage adjustment based upon serum Theophylline concentrations. Application of these general dosing recommendations to individual patients must take into account the unique clinical characteristics of each patient. In general, these recommendations should serve as the upper limit for dosage adjustments in order to decrease the risk of potentially serious adverse events associated with unexpected large increases in serum Theophylline concentration.

Table V. Dosing initiation and titration (as anhydrous Theophylline).*A. Children (12-15 years) and adults (16-60 years) without risk factors for impaired clearance. Titration Step Children > 45 kg and adults 1. Starting Dosage 12-14 mg/kg/day up to a maximum of 300 mg/day divided Q 24 hrs* 300-400 mg/day Dose reduction and/or serum Theophylline concentration measurement is indicated whenever adverse effects are present, physiologic abnormalities that can reduce Theophylline clearance occur (e.g., sustained fever), or a drug that interacts with Theophylline is added or discontinued.

How supplied

Theophylline (Theophylline capsule) ® (Theophylline) is supplied in extended-release capsules containing 100, 200, 300 or 400 mg of anhydrous Theophylline.

Theophylline (Theophylline capsule) ® 100 mg capsules are yellow-orange and clear, with markings Theophylline (Theophylline capsule), 100 mg, ucb, and 2832, supplied as: NDC NumberStorage

Store below 77 °F (25 °C).

FOR MEDICAL INFORMATION Contact: Medical Affairs Department Phone: (800) 477-7877, Fax: (770) 970-8859. Manufactured for: UCB Pharma, Inc. Smyrna, GA 30080. by Pfizer Pharmaceuticals LLC Caguas, PR 00725. 04/2005.

Theophylline interactions

What other drugs will affect Theophylline

Theophylline interacts with a wide variety of drugs. The interaction may be pharmacodynamic, i.e., alterations in the therapeutic response to Theophylline or another drug or occurrence of adverse effects without a change in serum Theophylline concentration. More frequently, however, the interaction is pharmacokinetic, i.e., the rate of Theophylline clearance is altered by another drug resulting in increased or decreased serum Theophylline concentrations. Theophylline only rarely alters the pharmacokinetics of other drugs.

The drugs listed in Table II have the potential to produce clinically significant pharmacodynamic or pharmacokinetic interactions with Theophylline. The information in the “Effect” column of Table II assumes that the interacting drug is being added to a steady-state Theophylline regimen. If Theophylline is being initiated in a patient who is already taking a drug that inhibits Theophylline clearance (e.g., cimetidine, erythromycin), the dose of Theophylline required to achieve a therapeutic serum Theophylline concentration will be smaller. Conversely, if Theophylline is being initiated in a patient who is already taking a drug that enhances Theophylline clearance (e.g., rifampin), the dose of Theophylline required to achieve a therapeutic serum Theophylline concentration will be larger. Discontinuation of a concomitant drug that increases Theophylline clearance will result in accumulation of Theophylline to potentially toxic levels, unless the Theophylline dose is appropriately reduced. Discontinuation of a concomitant drug that inhibits Theophylline clearance will result in decreased serum Theophylline concentrations, unless the Theophylline dose is appropriately increased.

The drugs listed in Table III have either been documented not to interact with Theophylline or do not produce a clinically significant interaction (i.e., < 15% change in Theophylline clearance).

The listing of drugs in Table II and III are current as of February 9, 1995. New interactions are continuously being reported for Theophylline, especially with new chemical entities. The clinician should not assume that a drug does not interact with Theophylline if it is not listed in Table II. Before addition of a newly available drug in a patient receiving Theophylline, the package insert of the new drug and/or the medical literature should be consulted to determine if an interaction between the new drug and Theophylline has been reported.

Table II: Clinically significant drug interactions with Theophylline*.Drug*Refer to PRECAUTIONS: DRUG INTERACTIONS for information regarding table.The Effect Of Other Drugs On Theophylline Serum Concentration Measurements

Most serum Theophylline assays in clinical use are immunoassays which are specific for Theophylline. Other xanthines such as caffeine, dyphylline, and pentoxifylline are not detected by these assays. Some drugs (e.g., cefazolin, cephalothin), however, may interfere with certain HPLC techniques. Caffeine and xanthine metabolites in neonates or patients with renal dysfunction may cause the reading from some dry reagent office methods to be higher than the actual serum Theophylline concentration.

Theophylline side effects

What are the possible side effects of Theophylline?

Adverse reactions associated with Theophylline are generally mild when peak serum Theophylline concentrations are < 20 mcg/mL and mainly consist of transient caffeine-like adverse effects such as nausea, vomiting, headache, and insomnia. When peak serum Theophylline concentrations exceed 20 mcg/mL, however, Theophylline produces a wide range of adverse reactions including persistent vomiting, cardiac arrhythmias, and intractable seizures which can be lethal. The transient caffeinelike adverse reactions occur in about 50% of patients when Theophylline therapy is initiated at doses higher than recommended initial doses (e.g., > 300 mg/day in adults and > 12 mg/kg/day in children beyond > 1 year of age). During the initiation of Theophylline therapy, caffeine-like adverse effects may transiently alter patient behavior, especially in school age children, but this response rarely persists. Initiation of Theophylline therapy at a low dose with subsequent slow titration to a predetermined age-related maximum dose will significantly reduce the frequency of these transient adverse effects. In a small percentage of patients ( < 3% of children and < 10% of adults) the caffeine-like adverse effects persist during maintenance therapy, even at peak serum Theophylline concentrations within the therapeutic range (i.e., 10-20 mcg/mL). Dosage reduction may alleviate the caffeine-like adverse effects in these patients, however, persistent adverse effects should result in a reevaluation of the need for continued Theophylline therapy and the potential therapeutic benefit of alternative treatment.

Other adverse reactions that have been reported at serum Theophylline concentrations < 20 mcg/mL include diarrhea, irritability, restlessness, fine skeletal muscle tremors, and transient diuresis. In patients with hypoxia secondary to COPD, multifocal atrial tachycardia and flutter have been reported at serum Theophylline concentrations ≥ 15 mcg/mL. There have been a few isolated reports of seizures at serum Theophylline concentrations < 20 mcg/mL in patients with an underlying neurological disease or in elderly patients. The occurrence of seizures in elderly patients with serum Theophylline concentrations < 20 mcg/mL may be secondary to decreased protein binding resulting in a larger proportion of the total serum Theophylline concentration in the pharmacologically active unbound form. The clinical characteristics of the seizures reported in patients with serum Theophylline concentrations < 20 mcg/mL have generally been milder than seizures associated with excessive serum Theophylline concentrations resulting from an overdose (i.e., they have generally been transient, often stopped without anticonvulsant therapy, and did not result in neurological residua).

TABLE IV. Manifestations of Theophylline toxicity. *Percentage of patients reported with sign or symptomAcute Overdose10 4*These data are derived from two studies in patients with serum Theophylline concentrations > 30 mcg/mL. In the first study (Study #1—Shanon, Ann Intern Med 1993;119:1161-67), data were prospectively collected from 249 consecutive cases of Theophylline toxicity referred to a regional poison center for consultation. In the second study (Study #2—Sessler, Am J Med 1990;88:567-76), data were retrospectively collected from 116 cases with serum Theophylline concentrations > 30 mcg/mL among 6000 blood samples obtained for measurement of serum Theophylline concentrations in three emergency departments. Differences in the incidence of manifestations of Theophylline toxicity between the two studies may reflect sample selection as a result of study design (e.g., in Study #1, 48% of the patients had acute intoxications versus only 10% in Study #2) and different methods of reporting results.

**NR = Not reported in a comparable manner.

Theophylline contraindications

What is the most important information I should know about Theophylline?

Do not take Theophylline in larger or smaller amounts or for longer than recommended. Theophylline overdose can occur if you accidentally take too much at one time, or if your daily doses are too high. To be sure you are using the correct dose, your blood will need to be tested often.

Do not start or stop smoking without first talking to your doctor. Smoking changes the way your body uses Theophylline, and you may need to use a different dose.

Sometimes it is not safe to use certain drugs at the same time. Many drugs can interact with Theophylline. Tell your doctor about all other medicines you use. Also tell your doctor if you start or stop using any of your other medications.

Stop using Theophylline and call your doctor at once if you have severe or continued vomiting, rapid heartbeats, confusion, tremors, or seizure.

Active ingredient matches for Theophylline:

Theophylline1 consumer reported useful Was the Theophylline drug useful in terms of decreasing the symptom or the disease?According to the reports released by website users, the below mentioned percentages of users say the drug is useful / not useful to them in decreasing their symptoms/disease. The usefulness of the drug depends on many factors, like severity of the disease, perception of symptom, or disease by the patient, brand name used [matters only to a certain extent], other associated conditions of the patient. If the drug is not effective or useful in your case, you need to meet the doctor to get re-evaluated about your symptoms/disease, and he will prescribe an alternative drug. Users No survey data has been collected yet Report price estimates »1 consumer reported time for results To what extent do I have to use Theophylline before I begin to see changes in my health conditions?As part of the reports released by website users, it takes > 3 month and a few days before you notice an improvement in your health conditions.Please note, it doesn’t mean you will start to notice such health improvement in the same time frame as other users. There are many factors to consider, and we implore you to visit your doctor to know how long before you can see improvements in your health while taking Theophylline. To get the time effectiveness of using Theophylline drug by other patients, please click here. Users

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