II. Precautions

  1. Theophylline is listed here for completeness, not for recommended use
  2. In the developed world, Theophylline and its adverse effects are largely supplanted by better agents
    1. Limited roles may be found in refractory cases under specialty care, and in underdeveloped world regions

III. Indications

  1. Limited utility where standard of care Asthma Management is available

IV. Preparations: Methylxanthines

  1. Aminophylline
  2. Caffeine
  3. Pentoxifylline (Trental)
  4. Theophylline

V. Mechanism

  1. Xanthines are isolated from plants Camellia sinensis and Coffea arabica
  2. Activity: Xanthines and Methylxanthines in general
    1. Xanthines inhibit phosphodiesterase and prostaglandin production
    2. Moderate cellular calcium
    3. Block Adenosine
  3. Effects: Theophylline
    1. Bronchial smooth muscle relaxation (high doses of Theophylline)
    2. Peripheral vasodilation (not central)
    3. CNS and cardiac stimulant
    4. Diuretic
    5. Anti-inflammatory (at low doses of Theophylline)

VI. Dosing

  1. Theophylline 150 to 300 mg twice daily

VII. Adverse Effects

  1. Serum Theophylline Level <20 mg/L
    1. Headache
    2. Insomnia
    3. Nausea
    4. Vomiting
  2. Serum Theophylline Level >20 mg/L
    1. Arrhythmias
    2. Seizures

VIII. Drug Interactions

  1. Agents that increase Theophylline serum concentrations
    1. Alcohol
    2. Ciprofloxacin
    3. Diltiazem
    4. Erythromycin
    5. Oral Contraceptives
    6. Propranolol (very strong effect, doubles the Theophylline concentration)
    7. Verapamil
  2. Agents that decrease Theophylline serum concentrations
    1. Phenytoin (Dilantin)

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Cost: Medications

theophylline (on 5/18/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
THEOPHYLLINE 80 MG/15 ML SOLN Generic $0.13 per ml
THEOPHYLLINE ER 100 MG TABLET Generic $0.30 each
THEOPHYLLINE ER 200 MG TABLET Generic $0.44 each
THEOPHYLLINE ER 300 MG TAB Generic $2.34 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