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Dyphylline

Pronunciation

(DYE fi lin)

Index Terms

  • Dihydroxypropyl Theophylline

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Elixir, Oral:

Dylix: 100 mg/15 mL (473 mL [DSC]) [contains alcohol, usp]

Tablet, Oral:

Lufyllin: 200 mg [DSC], 400 mg [scored]

Brand Names: U.S.

  • Dylix [DSC]
  • Lufyllin

Pharmacologic Category

  • Phosphodiesterase Enzyme Inhibitor, Nonselective

Pharmacology

Causes bronchodilatation, through phosphodiesterase inhibition which increases concentrations of cyclic adenine monophosphate (cAMP) and produces relaxation of bronchial smooth muscle.

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)

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

Dosing: Adult

Bronchoconstriction (asthma, COPD): Oral: Up to 15 mg/kg 4 times daily, individualize dosage

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; primarily undergoes renal elimination and an increase in systemic exposure is likely. The following adjustments have been recommended (Aronoff, 2007):

CrCl >50 mL/minute: Administer 75% of normal dose

CrCl 10-50 mL/minute: Administer 50% of normal dose

CrCl <10 mL/minute: Administer 25% of normal dose

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling.

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. Consider therapy modification

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy

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

Indacaterol: Theophylline Derivatives may enhance the adverse/toxic effect of Indacaterol. Theophylline Derivatives may enhance the hypokalemic effect of Indacaterol. Monitor therapy

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination

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

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 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 akathisia or headache. Have patient report immediately to prescriber tachycardia, arrhythmia, tachypnea, severe dizziness, syncope, considerable anxiety, significant nausea, intolerable diarrhea, severe headache, illogical thinking, insomnia, tremors, hematemesis, or hematuria (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.

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