theophylline


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theophylline

 [the-of€´ĭ-lin]
an alkaloid derived from tea or produced synthetically; it is a smooth muscle relaxant used chiefly for its bronchodilator effect in the treatment of chronic obstructive pulmonary disease, emphysema, bronchial asthma, chronic bronchitis, and bronchospastic distress. It also has myocardial stimulant, coronary vasodilator, diuretic, and respiratory center stimulant effects.
theophylline cholinate oxtriphylline.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.

theophylline

Apo-Theo LA, Elixophyllin, Novo-Theophyl SR, Nuelin SA, PMS-Theophylline, Pulmophyllin ELX, Ratio-Theo-Bronc, Slo-Phyllin, Theo-24, Theochron, Theolair, Theo-Time, Uniphyl, Uniphyllin Continus

Pharmacologic class: Xanthine derivative

Therapeutic class: Bronchodilator, spasmolytic

Pregnancy risk category C

Action

Relaxes bronchial smooth muscles, suppressing airway response to stimuli. Also inhibits phosphodiesterase and release of slow-reacting substance of anaphylaxis and histamine.

Availability

Capsules (immediate-release): 100 mg, 200 mg

Capsules (extended-release, 8 to 12 hours): 50 mg, 60 mg, 65 mg, 75 mg, 100 mg, 125 mg, 130 mg

Capsules (extended-release, 12 hours): 50 mg, 125 mg, 130 mg, 250 mg, 260 mg

Capsules (extended-release, 24 hours): 100 mg, 200 mg, 300 mg, 400 mg

Elixir: 80 mg/15 ml

Injection (with dextrose): 0.4 mg/ml, 0.8 mg/ml, 1.6 mg/ml, 2 mg/ml, 3.2 mg/ml, 4 mg/ml

Syrup (cherry): 80 mg/15 mg, 150 mg/15 ml

Tablets (immediate-release): 100 mg, 125 mg, 200 mg, 250 mg, 300 mg

Tablets (extended-release, 12 to 24 hours): 100 mg, 200 mg, 300 mg, 400 mg, 450 mg, 600 mg

Tablets (extended-release, 24 hours): 400 mg, 600 mg

Indications and dosages

Acute bronchospasm in patients not receiving theophylline

Adults (otherwise healthy nonsmokers): Initially, 6 mg/kg P.O., followed in next 12 to 16 hours by 3 mg/kg P.O. q 6 hours for two doses, then a maintenance dosage of 3 mg/kg P.O. q 8 hours

Children ages 9 to 16; young adult smokers: Initially, 6 mg/kg P.O., followed in next 12 to 16 hours by 3 mg/kg P.O. q 4 hours for three doses, then a maintenance dosage of 3 mg/kg P.O. q 6 hours

Children ages 1 to 9: Initially, 6 mg/kg P.O., followed in next 12 to 16 hours by 4 mg/kg P.O. q 4 hours for three doses, then a maintenance dosage of 4 mg/kg P.O. q 6 hours

Acute bronchospasm in patients receiving theophylline

Adults and children: Loading dose based partly on time, amount, and administration route of last dose and on expectation that each 0.5 mg/kg will produce 1 mcg/ml rise in theophylline blood level. In significant respiratory distress, loading dose may be 2.5 mg/kg P.O. or I.V. to increase theophylline level by approximately 5 mcg/ml.

Chronic bronchospasm

Adults and children: Immediate-release forms-16 mg/kg or 400 mg P.O. daily (whichever is lower) in three to four divided doses q 6 to 8 hours. Timed-release forms-12 mg/kg or 400 mg P.O. daily (whichever is lower) in three to four divided doses q 8 to 12 hours. May increase dosage of either immediate- or timed-release form at 2- to 3-day intervals, to a maximum of 13 mg/kg or 900 mg daily (whichever is lower) in patients older than age 16, 18 mg/kg daily in children ages 12 to 16, 20 mg/kg daily in children ages 9 to 12, or 24 mg/kg daily in children up to age 9.

Dosage adjustment

• Cor pulmonale or heart failure

• Elderly patients

• Young adults

Off-label uses

• Essential tremor

• Apnea and bradycardia in premature infants

Contraindications

• Hypersensitivity to drug or other xanthines (such as coffee, theobromine)

• Active peptic ulcer

• Seizure disorder

Precautions

Use cautiously in:

• alcoholism; heart failure or other cardiac or circulatory impairment; hypertension; renal or hepatic disease; COPD; hypoxemia; hyperthyroidism; diabetes mellitus; glaucoma; peptic ulcer disease

• elderly patients

• children younger than age 1.

Administration

• For I.V. delivery, use infusion solution designed for drug, or mix with dextrose 5% in water. Administer by controlled infusion pump.

• Know that for acute bronchospasm, theophylline preferably is given I.V. as 20 mg/ml of theophylline (or 25 mg/ml of aminophylline).

• Don't give timed-release form to patient with acute bronchospasm.

Adverse reactions

CNS: irritability, dizziness, nervousness, restlessness, headache, insomnia, reflex hyperexcitability, seizures

CV: palpitations, marked hypotension, sinus tachycardia, extrasystole, circulatory failure, ventricular arrhythmias

GI: nausea, vomiting, diarrhea, hematemesis, gastroesophageal reflux

GU: increased diuresis, proteinuria

Metabolic: hyperglycemia, syndrome of inappropriate antidiuretic hormone secretion

Musculoskeletal: muscle twitching

Respiratory: tachypnea, respiratory arrest

Skin: urticaria, rash, alopecia, flushing

Other: fever, hypersensitivity reaction

Interactions

Drug-drug. Allopurinol, calcium channel blockers, cimetidine, corticosteroids, disulfiram, ephedrine, hormonal contraceptives, influenza virus vaccine, interferon, macrolides, mexiletine, nonselective beta-adrenergic blockers, quinolones, thiabendazole: increased theophylline blood level, greater risk of toxicity

Aminoglutethimide, barbiturates, ketoconazole, rifampin, sulfinpyrazone, sympathomimetics: decreased theophylline blood level and effects

Carbamazepine, isoniazid, loop diuretics: increased or decreased theophylline blood level

Halothane: increased risk of arrhythmias

Hydantoins: decreased hydantoin blood level

Lithium: decreased therapeutic effect of lithium

Nondepolarizing muscle relaxants: reversal of neuromuscular blockade

Propofol: antagonism of propofol's sedative effects

Tetracyclines: increased risk of adverse reactions to theophylline

Drug-diagnostic tests. Glucose: increased level

Drug-food. Any food: altered bioavailability and absorption of some timed-release theophylline forms, causing rapid release and possible toxicity

Caffeine- or xanthine-containing foods and beverages: increased theophylline blood level and greater risk of adverse CNS and cardiovascular reactions

Diet high in protein and charcoal-broiled beef and low in carbohydrates: increased theophylline elimination, decreased efficacy

High-carbohydrate, low-protein diet: decreased theophylline elimination, increased risk of adverse reactions

Drug-herbs. Caffeine-containing herbs (such as cola nut, guarana, maté): increased theophylline blood level, greater risk of adverse CNS and cardiovascular reactions

Ephedra (ma huang): increased stimulant effect

St. John's wort: decreased theophylline blood level and efficacy

Drug-behaviors. Nicotine (in cigarettes, gum, transdermal patches): increased theophylline metabolism, decreased efficacy

Patient monitoring

• Monitor for signs and symptoms of hypersensitivity reaction, including rash and fever.

• Assess respiratory status. Monitor pulmonary function tests to gauge drug efficacy and identify adverse effects.

• Monitor cardiovascular and neurologic status carefully.

• Assess glucose level in diabetic patient.

Patient teaching

• Advise patient to take oral form with 8 oz of water 1 hour before or 2 hours after meals.

• Tell patient not to crush or chew timed-release form.

• Caution patient not to use different drug brands interchangeably.

Instruct patient to immediately report worsening dyspnea and other respiratory problems.

• Teach patient to recognize and report adverse neurologic reactions.

• Tell patient that all nicotine forms (including cigarettes, patches, and gum) decrease drug efficacy. Discourage nicotine use.

• Advise patient that a diet high in protein and charcoal-broiled beef and low in carbohydrates makes drug less effective.

• Tell patient that a high-carbohydrate, low-protein diet increases risk of adverse reactions, as do products containing caffeine.

• Caution patient to avoid herbs, especially ephedra and St. John's wort.

• Advise patient not to take over-the-counter drugs without prescriber's approval. Tell him to inform all prescribers he's taking drug, because it interacts with many other drugs.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved

the·oph·yl·line

(thē-of'i-lin),
An alkaloid found with caffeine in tea leaves (commercial theophylline is prepared synthetically); shares chemical and pharmacologic properties with caffeine and theobromine.
Farlex Partner Medical Dictionary © Farlex 2012

theophylline

(thē-ŏf′ə-lĭn)
n.
A colorless crystalline alkaloid, C7H8N4O2, derived from tea leaves or made synthetically, used as a bronchodilator primarily to treat asthma and chronic obstructive pulmonary disease.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.

theophylline

Therapeutics A xanthine derivative used in asthmatics, which relaxes smooth muscle; its effect is ↓ in smokers and in barbiturates and phenytoin therapy Action Relaxes smooth muscle of bronchial airways and pulmonary blood vessels, resulting in broncho- and vasodilation; it is also a diuretic, coronary vasodilator, cardiac and cerebral stimulant Adverse effects GI irritation-anorexia, N&V, epigastric pain, restlessness, insominia, headache Contraindications Acute peptic ulcer disease, untreated seizure disorder; theophylline accumulates in organ failure–eg, heart–CHF, liver, lungs, and kidney, by interfering with drug metabolism–eg, allopurinol, cimetidine, erythromycin, propranolol; theophylline may cause seizures and arrhythmias. See Aminophylline.
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.

the·oph·yl·line

(thē-of'i-lin)
An alkaloid found with caffeine in tea leaves; shares chemical and pharmacologic properties with caffeine and theobromine.
Medical Dictionary for the Health Professions and Nursing © Farlex 2012

theophylline

A bronchodilator drug used to treat asthma and to assist in the treatment of HEART FAILURE by increasing the heart rate and reducing OEDEMA by promoting excretion of urine. The drug is on the WHO official list. Brand names are Nuelin SA, Slo-Phyllin and Uniphyllin Continus. Franol is a theophylline preparation with EPHEDRINE.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005

the·oph·yl·line

(thē-of'i-lin)
Alkaloid found with caffeine in tea leaves; shares chemical and pharmacologic properties with caffeine and theobromine.
Medical Dictionary for the Dental Professions © Farlex 2012
References in periodicals archive ?
The R1 reagent formulation used was 100 mmol/L Tris, 100 mmol/L KCl, 80 mmol/L IMP, 4 mmol/L TCEP, 6 mmol/L EDTA, 1.47 /.mol/L theophylline-MPA, 4 mmol/L Suttocide A, 0.1 g/L (theophylline) monoclonal antibody, IMPDH-II (adjusted to rate), final pH 8.0.
Study participants were given inhaled beclomethasone, four puffs three times daily, or oral theophylline titrated to a target serum level of 8-12 [micro]g/mL.
Fortunately, not all quinolones cause a rise in serum theophylline concentrations.
Sustained-release theophylline is indicated as an alternative for maintenance in steps 2-4 in patients older than 5 years of age.
This observation is based on a limited amount of data.10 As such, the objective of the study was to make a comparison between theophylline and caffeine when used in standard doses in order to treat and prevent AOP in pre-term neonates to determine any differences in regards to (i) the episodes of apnea (ii) the relationship between serum concentration of methylxanthines and related apneic episodes and (iii) the requirement for monitoring of drug.
The aim is to test the theory that low doses of theophylline will act on the airways, helping the inhaled steroids already used widely in COPD today to work far more effectively.
The kit covers a wide range of drugs, including acetylcysteine, ampicillin Na, cefoxitin Na, doxycycline HCl, theophylline, levodopa, methyldopa, metronidazole, acetylsalicylic acid, ibuprofen, phenylbutazone, rifampicin, cyclosporine, acetaminophen and heparin.
There have been few studies comparing the efficacy of theophylline and caffeine in managing AOP in the West, [2-8] but practically none in the Indian pediatric population.
An Emirates Racing Authority (ERA) press release issued on Monday states that prohibited substances caffeine and theophylline were detected in the post-race urine sample taken from Journalistic following the Commercial Bank of Dubai handicap at Jebel Ali on December 13, 2013.
Theophylline is an agent used in the treatment of obstructive airway diseases.
These interactions included angiotensin-converting enzyme (ACE) inhibitors and potassium-sparing diuretics; ACE inhibitors or angiotensin receptor blockers and sulfamethoxazole/trimethoprim (SMX/ TMP); benzodiazepines or zolpidem and other medications; calcium channel blockers and macrolide antibiotics; digoxin and macrolide antibiotics; lithium and loop diuretics or ACE inhibitors; phenytoin and SMX/TMP; sulfonylureas and antimicrobial agents; theophylline and ciprofloxacin; and warfarin and antimicrobial agents or non-steroidal antiinflammatory drags.