Pharmacology
Mechanism of Action
Causes bronchodilatation, through phosphodiesterase inhibition which increases concentrations of cyclic adenine monophosphate (cAMP) and produces relaxation of bronchial smooth muscle.
Pharmacokinetics/Pharmacodynamics
Absorption
Rapid
Metabolism
Not converted to free theophylline in vivo
Excretion
Urine (88% as unchanged drug)
Time to Peak
Plasma: ~45 minutes; Anuric patients: may be increased 3 to 4 times normal
Half-Life Elimination
~2 hours (may be increased in renal impairment)
Use in Specific Populations
Special Populations: Renal Function Impairment
Clearance would be correspondingly reduced in patients with impaired renal function.
Use: Labeled Indications
Bronchodilator in reversible airway obstruction due to asthma, chronic bronchitis, or emphysema
Contraindications
Hypersensitivity to dyphylline, xanthine compounds, or any component of the formulation
Dosage and Administration
Dosing: Adult
Bronchoconstriction (asthma, COPD): Oral: Up to 15 mg/kg 4 times daily, individualize dosage
Dosing: Geriatric
Refer to adult dosing.
Storage
Store at 20°C to 25°C (68°F to 77°F).
Drug Interactions
Acebrophylline: May enhance the stimulatory effect of Theophylline Derivatives. Avoid combination
Adenosine: Theophylline Derivatives may diminish the therapeutic effect of Adenosine. Consider therapy modification
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Benzodiazepines: Theophylline Derivatives may diminish the therapeutic effect of Benzodiazepines. Consider therapy modification
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Theophylline Derivatives. Management: Monitor for reduced theophylline efficacy during concomitant use with any beta-blocker. Beta-1 selective agents are less likely to antagonize theophylline than nonselective agents, but selectivity may be lost at higher doses. Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Theophylline Derivatives. Monitor therapy
Cambendazole: May increase the serum concentration of Theophylline Derivatives. Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification
Doxofylline: Theophylline Derivatives may enhance the adverse/toxic effect of Doxofylline. Avoid combination
Formoterol: Theophylline Derivatives may enhance the adverse/toxic effect of Formoterol. Theophylline Derivatives may enhance the hypokalemic effect of Formoterol. Monitor therapy
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy
Indacaterol: Theophylline Derivatives may enhance the adverse/toxic effect of Indacaterol. Theophylline Derivatives may enhance the hypokalemic effect of Indacaterol. Monitor therapy
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Lithium: Theophylline Derivatives may decrease the serum concentration of Lithium. Monitor therapy
Methotrexate: May increase the serum concentration of Theophylline Derivatives. Monitor therapy
Olodaterol: Theophylline Derivatives may enhance the adverse/toxic effect of Olodaterol. Theophylline Derivatives may enhance the hypokalemic effect of Olodaterol. Monitor therapy
Pancuronium: Theophylline Derivatives may enhance the adverse/toxic effect of Pancuronium. Theophylline Derivatives may diminish the neuromuscular-blocking effect of Pancuronium. Management: Pancuronium dosage adjustment may be necessary to induce paralysis in patients receiving concomitant theophylline derivatives. Monitor closely for adverse effects (e.g., cardiac effects) with concomitant use of these agents. Consider therapy modification
Probenecid: May increase the serum concentration of Theophylline Derivatives. Monitor therapy
QuiNINE: May increase the serum concentration of Theophylline Derivatives. Monitor therapy
Riociguat: Theophylline Derivatives may enhance the hypotensive effect of Riociguat. Avoid combination
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Adverse Reactions
Frequency not defined. Reactions reported with other xanthine derivatives and may be dose-related.
Cardiovascular: Circulatory shock, extrasystoles, flushing, hypotension, palpitations, tachycardia, ventricular arrhythmia
Central nervous system: Agitation, headache, hyperexcitability, insomnia, irritability, restlessness, seizure
Endocrine & metabolic: Albuminuria, hyperglycemia, SIADH
Gastrointestinal: Diarrhea, epigastric pain, hematemesis, nausea, vomiting
Genitourinary: Diuresis, hematuria
Neuromuscular & skeletal: Muscle twitching
Respiratory: Tachypnea
Warnings/Precautions
Disease-related concerns:
- Cardiovascular disease: Use with caution in patients with severe cardiac disease including, acute myocardial injury, hypertension, and heart failure.
- Hyperthyroidism: Use with caution in patients with hyperthyroidism.
- Peptic ulcer disease: Use with caution in patient with peptic ulcer disease.
- Renal impairment: Use with caution in patients with renal impairment; dose adjustment may be required.
- Status asthmaticus: Xanthine derivatives, including dyphylline, are not indicated for the management of status asthmaticus.
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal reproduction studies have not been conducted.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience agitation. Have patient report immediately to prescriber fast heartbeat, abnormal heartbeat, fast breathing, severe dizziness, passing out, severe anxiety, severe nausea, severe vomiting, severe diarrhea, severe headache, confusion, trouble sleeping, seizures, tremors, vomiting blood, or blood in the urine (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
