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Back to Xanthine derivatives


  Asthma News

Xolair reduced the rate of hospital emergency visits by 44% in patients with inadequately controlled asthma.


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Theophylline ethylenediamine
Amoline, Phyllocontin, Truphylline

Pregnancy Category C

Drug classes


Mechanism of action

Relaxes bronchial smooth muscle, causing bronchodilation and increasing vital capacity, which has been impaired by bronchospasm and air trapping; in higher concentrations, it also inhibits the release of slow-reacting substance of anaphylaxis (SRS-A) and histamine.


  1. Symptomatic relief or prevention of bronchial asthma and reversible bronchospasm associated with chronic bronchitis and emphysema

Unlabeled uses:

  1. Respiratory stimulant in Cheyne-Stokes respiration
  2. Treatment of apnea and bradycardia in premature babies


  1. Hypersensitivity to any xanthine or to ethylenediamine,
  2. Peptic ulcer
  3. Active gastritis
  4. Rectal or colonic irritation or infection (use of the rectal preparations)

Use caution in the presence of cardiac arrhythmias, acute myocardial injury, CHF, cor pulmonale, severe hypertension, severe hypoxemia, renal or hepatic disease, hyperthyroidism, alcoholism, labor, lactation.

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Adverse effects

- Serum theophylline levels 20-25 ?/ml: nausea, vomiting, diarrhea, headache, insomnia, irritability (75% of patients)
- Serum theophylline levels 30-35 ?/ml: hyperglycemia, hypotension, cardiac arrhythmias, tachycardia ( 10 ?/ml in premature newborns); seizures, brain damage, death

  • CNS: Irritability (especially children); restlessness, dizziness, muscle twitching, convulsions, severe depression, stammering speech; abnormal behavior characterized by withdrawal, mutism andunresponsiveness alternating with hyperactive periods
  • GI: Loss of appetite, hematemesis, epigastric pain, gastroesophageal reflux during sleep, increased SGOT
  • CV: Palpitations, sinus tachycardia, ventricular tachycardia, life-threatening ventricular arrhythmias, circulatory failure
    Respiratory: Tachypnea, respiratory arrest
  • GU: Proteinuria, increased excretion of renal tubular cells & RBCs; diuresis (dehydration), urinary retention in men with prostate enlargement
  • Other: Fever, flushing, hyperglycemia, SIADH, rash

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