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Active ingredient: Theophylline - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Vasodilator Agents
  • Bronchodilator Agents
  • Respiratory Smooth Muscle Relaxants

Dosage Forms

  • Capsule (sustained-release)
  • Elixir
  • Liquid
  • Tablet
  • Tablet (extended-release)

Brands / Synonyms

Accurbron; Acet-Theocin; Aerobin; Aerolate; Aerolate III; Aerolate SR; Afonilm; Afonilum; Aminophylline; Aquaphyllin; Armophylline; Asbron; Asmalix; Asmax; Austyn; Bilordyl; Bronchoretard; Bronkodyl; Bronkodyl SR; Cetraphylline; Choledyl SA; Chronophyllin; Constant T; Diffumal; Dimethylxanthine; Diphyllin; Doraphyllin; Duraphyl; Duraphyllin; Dyspne-Inhal; Egifilin; Elan; Elixex; Elixicon; Elixomin; Elixophyllin; Elixophyllin SR; Elixophylline; Etheophyl; Euphyllin; Euphylline; Euphylong; Labid; Lanophyllin; Lasma; Liquophylline; Liquorice; Maphylline; Medaphyllin; Nuelin; Optiphyllin; Parkophyllin; Physpan; Pro-Vent; Pseudotheophylline; Pulmidur; Pulmo-Timelets; Quibron; Quibron T; Quibron T / SR; Quibron-T; Quibron-T/SR; Respbid; Respicur; Respid; Slo-Bid; Slo-Phyllin; Solosin; Somophyllin CRT; Somophyllin T; Somophyllin-CRT; Somophyllin-DF; Somophyllin-T; Spophyllin Retard; Sustaire; Synophylate; Synophylate-L.A. Cenules; T-Phyl; Talotren; Tefamin; Telb-DS; Telbans Dry Syrup; Teocen 200; Teofilina; Teofyllamin; Teolair; Teonova; Teosona; Tesona; Theacitin; Theal Tablets; Theo 24; Theo-11; Theo-24; Theo-DS; Theo-Dur; Theo-Nite; Theo-Sav; Theobid; Theobid Duracap; Theobid Jr.; Theochron; Theocin; Theoclair-SR; Theoclear; Theoclear 80; Theoclear L.A.-130; Theoclear LA; Theoclear-200; Theoclear-80; Theocontin; Theodel; Theodrip; Theodur Dry Syrup; Theofol; Theograd; Theolair; Theolair-SR; Theolix; Theolixir; Theon; Theona P; Theopek; Theophyl; Theophyl-225; Theophyl-SR; Theophyline; Theophyllin; Theophylline Anhydrous; Theophylline, Anhydrous; Theophylline-SR; Theoplus; Theospan; Theostat; Theostat 80; Theotard; Theovent; Uni-Dur; Unifyl; Unilong; Uniphyl; Uniphyllin; Xanthium; Xantivent


For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis.


Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).

Mechanism of Action

Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction.


Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.


Symptoms of overdose include seizures, arrhythmias, and GI effects.

Biotrnasformation / Drug Metabolism

Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity.


This product is contraindicated in individuals who have shown hypersensitivity to its components. It is also contraindicated in patients with active peptic ulcer disease, and in individuals with underlying seizure disorders (unless receiving appropriate anti-convulsant medication).

Drug Interactions

Theophylline interacts with a wide variety of drugs. The interaction may be pharmacodynamic, i.e., alterations in the therapeutic response to theophylline or another drug or occurrence of adverse effects without a change in serum theophylline concentration. More frequently, however, the interaction is pharmacokinetic, i.e., the rate of theophylline clearance is altered by another drug resulting in increased or decreased serum theophylline concentrations. Theophylline only rarely alters the pharmacokinetics of other drugs.

The drugs listed in TABLES 2A and 2B have the potential to produce clinically significant pharmacodynamic or pharmacokinetic interactions with theophylline. The information in the "Effect" column of TABLES 2A and 2B assumes that the interacting drug is being added to a steady-state theophylline regimen. If theophylline is being initiated in a patient who is already taking a drug that inhibits theophylline clearance (e.g., cimetidine, erythromycin), the dose of theophylline required to achieve a therapeutic serum theophylline concentration will be smaller. Conversely, if theophylline is being initiated in a patient who is already taking a drug that enhances theophylline clearance (e.g., rifampin), the dose of theophylline required to achieve a therapeutic serum theophylline concentration will be larger. Discontinuation of a concomitant drug that increases theophylline clearance will result in accumulation of theophylline to potentially toxic levels, unless the theophylline dose is appropriately reduced. Discontinuation of a concomitant drug that inhibits theophylline clearance will result in decreased serum theophylline concentrations, unless the theophylline dose is appropriately increased.

The listing of drugs in TABLES 2A and 2B is current as of April 3, 1995. New interactions are continuously being reported for theophylline, especially with new chemical entities. The clinician should not assume that a drug does not interact with theophylline if it is not listed in TABLES 2A and 2B.Before addition of a newly available drug in a patient receiving theophylline, the package insert of the new drug and/or the medical literature should be consulted to determine if an interaction between the new drug and theophylline has been reported.

TABLE 2A - Clinically significant drug interactions with theophylline*

Drug Type of Interaction Effect**
Adenosine Theophylline blocks adenosine receptors. Higher doses of adenosine may be required to achieve desired effect.
Alcohol A single large dose of alcohol (3 ml/kg of whiskey) decreases theophylline clearance for up to 24 hours. 30% increase
Allopurinol Decreases theophylline clearance at allopurinol doses ³600 mg/day. 25% increase
Aminoglutethimide Increases theophylline clearance by induction of microsomal enzyme activity. 25% decrease
Carbamazepine Similar to aminoglutethimide. 30% decrease
Cimetidine Decreases theophylline clearance by inhibiting cytochrome P450 1A2. 70% increase
Ciprofloxacin Similar to cimetidine. 40% increase
Clarithromycin Similar to erythromycin. 25% 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% increase
Enoxacin Similar to cimetidine. 300% increase
Ephedrine Synergistic CNS effects Increased frequency of nausea, nervousness, and insomnia.
Erythromycin Erythromycin metabolite decreases theophylline clearance by inhibiting cytochrome P450 3A3. 35% increase.
Erythromycin steady-state serum concentrations decreased 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% increase
Flurazepam Similar to diazepam. Similar to diazepam.
Fluvoxamine Similar to cimetidine myocardium to catecholamines, theophylline increases release of endogenous catecholamines. Similar to cimetidine ventricular arrhythmias.
Interferon, human recombinant alpha-A Decreases theophylline clearance. 100% increase
Isoproterenol (IV) Increases theophylline clearance. 20% decrease
Ketamine Pharmacologic May lower theophylline seizure threshold.
Lithium Theophylline increases renal lithium clearance. Lithium dose required to achieve a therapeutic serum concentration increased an average of 60%.
Lorazepam Similar to diazepam. Similar to diazepam.

TABLE 2B - Clinically significant drug interactions with theophylline*

Drug Type of Interaction Effect**
Methotrexate (MTX) Decreases theophylline clearance. 20% increase after low dose MTX, higher dose MTX may have a greater effect.
Mexiletine Similar to disulfiram. 80% increase
Midazolam Similar to diazepam. Similar to diazepam.
Moricizine Increases theophylline clearance. 25% decrease
Pancuronium Theophylline may antagonize non-depolarizing neuromuscular blocking effects; possibly due to phosphodiesterase inhibition. Larger dose of pancuronium may be required to achieve neuromuscular blockade.
Pentoxifylline Decreases theophylline clearance. 30% increase
Phenobarbital (PB) Similar to aminoglutethimide. 25% decrease after two weeks of concurrent PB.
Phenytoin Phenytoin increases theophylline clearance by increasing microsomal enzyme activity. Theophylline decreases phenytoin absorption. Serum theophylline and phenytoin concentrations decrease about 40%.
Propafenone Decreases theophylline clearance and pharmacologic interaction. 40% increase. Beta-2 blocking effect may decrease efficacy of theophylline.
Propranolol Similar to cimetidine and pharmacologic interaction. 100% increase. Beta-2 blocking effect may decrease efficacy of theophylline.
Rifampin Increases theophylline clearance by increasing cytochrome P450 1A2 and 3A3 activity. 20-40% decrease
Sulfinpyrazone Increases theophylline clearance by increasing demethylation and hydroxylation. 20% decrease
Decreases renal clearance of theophylline.
Tacrine Similar to cimetidine, also increases renal clearance of theophylline. 90% increase
Thiabendazole Decreases theophylline clearance. 190% increase
Ticlopidine Decreases theophylline clearance. 60% increase
Troleandomycin Similar to erythromycin. 33-100% increase depending on troleandomycin dose.
Verapamil Similar to disulfiram. 20% increase
* Refer to for further information regarding table.
** Average effect on steady state theophylline concentration or other clinical effect for pharmacologic interactions. Individual patients may experience larger changes in serum theophylline concentration than the value listed.

The Effect of Other Drugs on Theophylline Serum Concentration Measurements: Most serum theophylline assays in clinical use are immunoassays which are specific for theophylline. Other xanthines such as caffeine, dyphylline, and pentoxifylline are not detected by these assays. Some drugs (e.g., cefazolin, cephalothin), however, may interfere with certain HPLC techniques. Caffeine and xanthine metabolites in neonates or patients with renal dysfunction may cause the reading from some dry reagent office methods to be higher than the actual serum theophylline concentration.

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