Theophylline

DEA Class; Rx

Common Brand Names; Theo 24, Theochron, Elixophyllin, aminophylline, Uniphyl

Oral and intravenous methylxanthine
Used primarily for maintenance treatment of COPD or asthma but is not a preferred agent in either disease; also used in apnea of prematurity not responding to other therapies
Aminophylline is converted to theophylline systemically; 1 mg aminophylline = 0.8 mg theophylline

Indicated for the treatment of asthma exacerbation or for asthma maintenance treatment; or for maintenance treatment or exacerbations due to chronic obstructive pulmonary disease (COPD) (e.g., emphysema or chronic bronchitis).

Hypersensitivity

Peak serum concentration <20 mcg/mL

• Central nervous system excitement, headache, insomnia, irritability, restlessness, seizure
• Diarrhea, nausea, vomiting
• Diuresis (transient)
• Exfoliative dermatitis
• Skeletal muscle tremors
• Tachycardia, flutter
• Hypercalcemia (with concomitant hyperthyroid disease)
• Difficulty urinating (elderly males with prostatism)

Peak serum concentration >30 mcg/mL

• Acute myocardial infarction
• Seizures (resistant to anticonvulsants)
• Urinary retention

Patients, who develop CNS abnormalities, reported (rarely) to experience nonconvulsive status epilepticus

Theophylline clearance may decrease in patients with congestive heart failure, acute pulmonary edema, hepatic disease, cor pulmonale, acute hepatitis, hypothyroidism, cirrhosis, fever, or sepsis with multiorgan failure and shock; severe and potentially fatal toxicity may occur if reduced theophylling clearance occurs

Avoid extravasation; vesicant; ensure proper placement of catherer prior to and during infusion

Use with caution in patients with hyperthyroidism, seizure disorder, peptic ulcer, or cardiovascular disease

Some dosage forms may contain propylene glycol; use caution; seizures, hyperosmolality, lactic acidosis, and respiratory depression reported associated with use of large amounts of propylene glycol

Measure serum levels and withhold subsequent doses if patient develops signs and symptoms of theophylline toxicity

Use caution in patients with cardiac arrhythmia, excluding bradyarrhythmia; use may exacerbate arrhythmia

Use with caution in patients with cystic fibrosis; increased theophylline clearance may occur

Use with caution in patients with seizure disorders; use may exacerbate seizure disorder

Do not increase dose in response to acute exacerbation of symptoms unless steady state serum theophylline concentration of <10 mcg//mL

Pregnancy category: C

Lactation: Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants; serious adverse effects in infant are unlikely unless mother has toxic serum theophylline concentration