Drug |
Type of interaction |
Effect on theophylline serum
concentrations or pharmacologic effect |
Adenosine |
Theophylline blocks adenosine receptors |
Higher doses of adenosine may be required to achieve
desired anti-arrhythmic effect |
Alcohol |
A single large dose of alcohol (3 ml/kg of whiskey)
decreases theophylline clearance for up to 24 hours |
33 percent increase |
Allopurinol |
Decreases theophylline clearance at allopurinol doses ≥600 mg/day |
25 percent increase |
Aminoglutethimide |
Increases theophylline clearance by induction of
microsomal enzyme activity |
25 percent decrease |
Carbamazepine |
Similar to aminoglutethimide |
30 percent decrease |
Cimetidine |
Decreases theophylline clearance by inhibiting
cytochrome P450 1A2 |
70 percent increase |
Ciprofloxacin |
Similar to cimetidine |
40 percent increase |
Clarithromycin |
Similar to erythromycin |
25 percent increase |
Diazepam |
Benzodiazepines increase CNS concentrations of
adenosine, a potent CNS depressant, while theophylline blocks adenosine
receptors |
Larger diazepam doses may be required to produce
desired level of sedation |
Discontinuation of theophylline without reduction of
diazepam dose may result in respiratory depression |
Disulfiram |
Decreases theophylline clearance by inhibiting
hydroxylation and demethylation |
50 percent increase |
Enoxacin |
Similar to cimetidine |
300 percent increase |
Ephedrine |
Synergistic CNS effects |
Increased frequency of nausea, nervousness, and insomnia |
Erythromycin |
Erythromycin metabolite decreases theophylline
clearance by inhibiting cytochrome P450 3A3 |
35 percent increase. Erythromycin steady-state serum
concentrations decrease by a similar amount |
Estrogen |
Estrogen-containing oral contraceptives decrease
theophylline clearance in a dose-dependent fashion. The effect of
progesterone on theophylline clearance is unknown |
30 percent increase |
Flurazepam |
Similar to diazepam |
Similar to diazepam |
Fluvoxamine |
Similar to cimetidine |
Similar to cimetidine |
Halothane |
Halothane sensitizes the myocardium to catecholamines;
theophylline increases release of endogenous catecholamines |
Increased risk of
ventricular arrhythmias |