II. Precautions
- Theophylline is listed here for completeness, not for recommended use
- In the developed world, Theophylline and its adverse effects are largely supplanted by better agents
- Limited roles may be found in refractory cases under specialty care, and in underdeveloped world regions
III. Indications
- Limited utility where standard of care Asthma Management is available
- Theophylline and Aminophylline were replaced by Inhaled Beta Adrenergic Agonists (e.g. Albuterol) and Ipratropium Bromide
IV. Preparations: Methylxanthines
- Theophylline
- Oral administration only
- Aminophylline
- IV form of Theophylline
- Water soluble salt of Theophylline
- Aminophylline has higher solubility allows for IV administration
- Other Methylxanthines
V. Mechanism
- Xanthines are isolated from plants Camellia sinensis and Coffea arabica
- Activity: Xanthines and Methylxanthines in general
- Xanthines at high dose inhibit phosphodiesterase (PDE) and Prostaglandin production
- PDE catalyzes cAMP, with increased cAMP levels when PDE is inhibited
- cAMP mediates adrenergic induced bronchodilation
- Block Adenosine
- Results in CNS and cardiac stimulation
- Moderate cellular Calcium
- Xanthines at high dose inhibit phosphodiesterase (PDE) and Prostaglandin production
- Effects: Theophylline
- Bronchial Smooth Muscle relaxation (high doses of Theophylline)
- Peripheral vasodilation (not central)
- CNS and cardiac stimulant
- Diuretic
- Anti-inflammatory (at low doses of Theophylline)
VI. Dosing
- Theophylline 150 to 300 mg orally twice daily
- Patients should not modify dose from prescribed (even for missed dosing)
- Doubling dose for a missed dose may result in Theophylline toxicity
VII. Pharmacokinetics: Oral Theophylline
VIII. Adverse Effects
IX. Drug Interactions
- Agents that increase Theophylline half life and serum concentrations
- Alcohol
- Cimetidine
- Ciprofloxacin
- Diltiazem
- Erythromycin
- Oral Contraceptives
- Propranolol (very strong effect, doubles the Theophylline concentration)
- Verapamil
- Agents that decrease Theophylline half life and serum concentrations
-
Sympathomimetics
- Increased CNS and cardiac toxicity
X. Resources
- Theophylline XR Tablet (DailyMed)
- Aminophylline Intravenous Solution (DailyMed)
XI. References
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 90
- Falk (2016) Am Fam Physician 94(6): 454-62 [PubMed]
Images: Related links to external sites (from Bing)
Related Studies
| theophylline (on 3/15/2023 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| THEOPHYLLINE ER 300 MG TAB | Generic | $2.38 each |
| THEOPHYLLINE ER 300 MG TABLET | Generic | $2.54 each |
| THEOPHYLLINE ER 400 MG TABLET | Generic | $0.64 each |
| THEOPHYLLINE ER 600 MG TABLET | Generic | $0.96 each |
Ontology: Aminophylline (C0002575)
| Definition (NCI) | A methylxanthine and derivative of theophylline. Aminophylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Aminophylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart. |
| Definition (MSH) | A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications. |
| Definition (CSP) | drug combination that contains theophylline and ethylenediamine; its most common use is in bronchial asthma, but it has been investigated for several other applications. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D000628 |
| SnomedCT | 391758000, 373508009, 55867006 |
| English | Aminophylline, Ethylenediamine, Theophylline, Theophyllamine, Theophylline Ethylenediamine, 1H-Purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-, compd. with 1,2-ethanediamine (2:1), Ammophyllin, Theophyline Ethylenediamine, 1H-Purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-, compound with 1,2-Ethanediamine(2:1), aminophylline, theophylline ethylenediamine, aminophylline (medication), Aminophylline [Chemical/Ingredient], aminophyllin, theophyllamine, Aminophylline - chemical, Aminophylline - chemical (substance), AMINOPHYLLINE, Aminophylline (product), Aminophylline (substance) |
| Swedish | Aminofyllin |
| Czech | aminofylin |
| Finnish | Teofyllamiini |
| German | Theophyllin-Ethylendiamin, Theophyllamin, Aminophyllin |
| Russian | AMINOFILLIN, EUFILLIN, АМИНОФИЛЛИН, ЭУФИЛЛИН |
| Japanese | アミノフィリン, テオフィリンエチレンジアミン |
| French | Théophylline éthylène-diamine, Théophyllamine, Aminophylline, Théophylline éthylènediamine, Théophylline-éthylènediamine |
| Croatian | AMINOFILIN |
| Polish | Aminofilina |
| Spanish | aminofilina (producto), aminofilina (sustancia), aminofilina, Aminofilina |
| Italian | Amminofillina |
| Portuguese | Aminofilina |
Ontology: Theophylline (C0039771)
| Definition (CHV) | a drug used to prevent and treat wheezing and shortness of breath caused by respiratory diseases such as asthma |
| Definition (CHV) | a drug used to prevent and treat wheezing and shortness of breath caused by respiratory diseases such as asthma |
| Definition (NCI) | A natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. (NCI04) |
| Definition (NCI_NCI-GLOSS) | A drug used to improve breathing in people who are short of breath. It belongs to the family of drugs called bronchodilators or respiratory smooth muscle relaxants. |
| Definition (MSH) | A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLATE CYCLASE and cyclic AMP. |
| Definition (CSP) | 1,3-dimethylxanthine; methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. |
| Definition (PDQ) | A natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41340&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41340&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C872" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Biologically Active Substance (T123) , Organic Chemical (T109) |
| MSH | D013806 |
| SnomedCT | 255657001, 372810006, 66493003 |
| LNC | LP16288-0, MTHU004269 |
| English | 1,3 Dimethylxanthine, 1,3-Dimethylxanthine, Theophylline, 1H-Purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-, 3,7-Dihydro-1,3-dimethyl-1H-purine-2,6-dione, theophylline, theophylline (medication), aminophylline (as theophylline), Theophylline [Chemical/Ingredient], THEOPHYLLINE, theophyllines, Theophylline product, Theophylline (product), Theophylline (substance) |
| Swedish | Teofyllin |
| Czech | theofylin |
| Finnish | Teofylliini |
| Russian | TEOFILLIN, 1,3-DIMETILKSANTIN, 1,3-ДИМЕТИЛКСАНТИН, ТЕОФИЛЛИН |
| Japanese | テオチン, 1,3-ジメチルキサンチン, テオフィリン |
| Croatian | TEOFILIN |
| Polish | Teofilina |
| Spanish | teofilina (producto), teofilina (sustancia), teofilina, Teofilina |
| French | Théophylline |
| German | Theophyllin |
| Italian | Teofillina |
| Portuguese | Teofilina |
Ontology: methylxanthine (C0066447)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C008514 |
| SnomedCT | 259553003 |
| Spanish | derivado xantínico metilado, metilxantina (sustancia), metilxantina |
| English | Methylated xanthine derivative, methylxanthine [Chemical/Ingredient], methylxanthine, methyl xanthine, methyl xanthines, methylxanthines, Methyl xanthine, METHYLXANTHINES, Methyl xanthine (substance), Methylated xanthine derivative (substance), Methylxanthines, Methylxanthine |
