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Theophylline

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Immediate-release capsules, tablets: Bronkodyl, Elixophyllin, Quibron-T, Dividose, Slo-Phyllin, Theolair
Timed-release capsules: Aerolate, Elixophyllin SR, Slo-bid Gyrocaps,
Slo-Phyllin Gyrocaps, Theo-24, Theobid, Theoclear L.A., Theo-Dur Sprinkle, Theospan-SR, Theovent Long-Acting
Timed-release tablets: Constant-T, Quibron-T/SR Dividose, Respbid,
Theochron, Theo-Dur, Theolair-SR, Uniphyl
Liquids: Accurbron, Aerolate, Aquaphyllin, Asmalix, Elixomin, Elixophyllin, Lanophyllin, Slo-Phyllin, Theoclear-80, Theolair, Theostat 80, theophylline sodium glycinate

Pregnancy Category C

Drug classes

Bronchodilator
Xanthine

Mechanism of action

Relaxes bronchial smooth muscle, causing bronchodilation and increasing vital capacity that has been impaired by bronchospasm and air trapping; actions may be mediated by inhibition of phosphodiesterase, which increases the concentration of cyclic adenosine monophosphate; in concentrations that may be higher than those reached clinically, it also inhibits the release of slow-reacting substance of anaphylaxis and histamine.

Indications

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

Unlabeled uses:

1. Use of 2 mg/kg per day to maintain serum concentrations between
   3 and 5 ęg/ml in the treatment of apnea and bradycardia of prematurity

Contraindications

1. Hypersensitivity to any xanthines,
2. peptic ulcer,
3. active gastritis,
4. status asthmaticus,
5. pregnancy (tachycardia, jitteriness, and withdrawal apnea have been observed in neonates whose mothers received xanthines up until delivery).

Use caution in the presence of

1. cardiac arrhythmias
2. acute myocardial injury
3. CHF
4. cor pulmonale
5. severe hypertension
6. severe hypoxemia
7. renal or hepatic disease
8. hyperthyroidism
9. alcoholism
10. labor (may inhibit uterine contractions)
11. lactation

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Adverse effects

- Serum theophylline levels 20-25 ęg/ml: nausea, vomiting, diarrhea, headache, insomnia, irritability (75% of patients)
- Serum theophylline levels 30-35 ęg/ml: hyperglycemia, hypotension, cardiac arrhythmias, tachycardia ( 10 ęg/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, elevated SGOT.
   

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