theophylline (redirected from Theophylline-sr)

theophylline /the·oph·yl·line/ (the-of´ĭ-lin) a xanthine derivative found in tea leaves and prepared synthetically; its salts and derivatives act as smooth muscle relaxants, central nervous system and cardiac muscle stimulants, and bronchodilators; used as a bronchodilator in asthma and in bronchitis, emphysema, or other chronic obstructive pulmonary disease. Its choline salt is oxtriphylline.

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the·oph·yl·line (th-f-ln, th-fln)

n.

A colorless crystalline alkaloid derived from tea leaves or made synthetically, used as a cardiac stimulant and diuretic.

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theophylline

[thē·əfil′ēn]

Etymology: L, thea, tea; Gk, phyllon, leaf

a bronchodilator.

indications It can be prescribed for oral administration to relax the smooth muscle of the bronchial passages in the treatment of bronchospasm in bronchial asthma, bronchitis, and emphysema. Its use has tapered sharply because of the availability of safer and more effective asthma medications that can be administered by inhalation.

contraindications Hypertension, cardiac disease, liver disease, renal disease, or concurrent treatment with other xanthines may prohibit its use.

adverse effects Among the most serious adverse effects are hypersensitivity, GI bleeding, palpitations, and seizures.

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theophylline

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 emphysema, bronchial asthma, chronic bronchitis and bronchospastic distress. It also has myocardial stimulant, coronary vasodilator, diuretic and respiratory center stimulant effects.

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theophylline cholinate

oxtriphylline, a smooth muscle relaxant, myocardial stimulant and diuretic.

theophylline ethylenediamine

a smooth muscle relaxant, myocardial stimulant and diuretic. Called also aminophylline.

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theophylline

Apo-Theo LA (CA), Elixophyllin, Nuelin (UK), Pulmophyllin ELX (CA), Slo-Phyllin (UK), Theochron, Theolair (CA), Uniphyl, Uniphyllin Continus (UK)

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

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

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

Solution: 80 mg/15 ml, 150 mg/15 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 (timed-release, 8 to 12 hours): 100 mg, 200 mg, 250 mg, 300 mg, 500 mg

Tablets (timed-release, 8 to 24 hours): 100 mg, 200 mg, 300 mg, 450 mg

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

Tablets (timed-release, 24 hours): 200 mg, 250 mg, 260 mg, 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.

Route	Onset	Peak	Duration
P.O.	Rapid	1-2 hr	6 hr
P.O. (timed)	Delayed	4-8 hr	8-24 hr
I.V.	Rapid	End of infusion	6-8 hr

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.

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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.