Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H22NO5.C7H7N4O2 |
Molecular Weight | 511.5271 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C([N-]C=N2)C(=O)N(C)C1=O.COC3=C4OC(C)=CC(=O)C4=C(OCC[N+](C)(C)C)C5=C3OC=C5
InChI
InChIKey=YFPYRJKHCCQDNQ-UHFFFAOYSA-M
InChI=1S/C18H22NO5.C7H8N4O2/c1-11-10-13(20)14-15(23-9-7-19(2,3)4)12-6-8-22-16(12)18(21-5)17(14)24-11;1-10-5-4(8-3-9-5)6(12)11(2)7(10)13/h6,8,10H,7,9H2,1-5H3;3H,1-2H3,(H,8,9,12)/q+1;/p-1
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9676340 | https://www.ncbi.nlm.nih.gov/pubmed/27713276
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9676340 | https://www.ncbi.nlm.nih.gov/pubmed/27713276
Since its discovery as component of the tea leaf by Albert Kossel in 1888, the history of theophylline (CAS 58-55-9) has been a long and successful one. At the turn of the century, theophylline became less expensive due to chemical synthesis and was primarily used as diuretic in subsequent years. It was Samuel Hirsch who discovered the bronchospasmolytic effect of theophylline in 1992, however, despite this pioneering discovery theophylline continued to be used primarily as diuretic and cardiac remedy. The molecular mechanism of bronchodilatation is inhibition of phosphodiesterase(PDE)3 and PDE4, but the anti-inflammatory effect may be due to histone deacetylase (HDAC) activation, resulting in switching off of activated inflammatory genes.
Theophylline is indicated for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9676340
Curator's Comment: Albert Kossel discovered theophylline as a component of the tea leaf
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094125 |
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Target ID: CHEMBL2093863 |
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Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | THEOPHYLLINE AND DEXTROSE 5% IN PLASTIC CONTAINER Approved UseTheophylline is indicated for the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis. Launch Date1982 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7332727/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
THEOPHYLLINE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
95.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7332727/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
THEOPHYLLINE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.51 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7332727/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
THEOPHYLLINE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
41% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7332727/ |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
THEOPHYLLINE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
20 mg/mL steady, intravenous Highest studied dose Dose: 20 mg/mL Route: intravenous Route: steady Dose: 20 mg/mL Sources: Page: p.500 |
unhealthy, 39 years (51 % < 40 years) n = 87 Health Status: unhealthy Condition: COPD|asthma Age Group: 39 years (51 % < 40 years) Sex: M+F Population Size: 87 Sources: Page: p.500 |
Disc. AE: Vomiting... Other AEs: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (grade 3, 5.75%) Other AEs:Vomiting (12.64%) Sources: Page: p.500 |
1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Disc. AE: Gastrointestinal discomfort, Supraventricular tachycardia... Other AEs: Tremor, Nervousness... AEs leading to discontinuation/dose reduction: Gastrointestinal discomfort (grade 3, 16.7%) Other AEs:Supraventricular tachycardia (grade 3, 16.7%) Tremor (16.7%) Sources: Page: p.149Nervousness (16.7%) Dysrhythmias (grade 1, 16.7%) |
800 mg single, oral Recommended Dose: 800 mg Route: oral Route: single Dose: 800 mg Sources: Page: p.146 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M Population Size: 6 Sources: Page: p.146 |
|
800 mg 1 times / day steady, oral Recommended Dose: 800 mg, 1 times / day Route: oral Route: steady Dose: 800 mg, 1 times / day Sources: Page: p.148 |
unhealthy, 66 ± 9 n = 16 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 16 Sources: Page: p.148 |
|
1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
Other AEs: Generalized epileptic seizure, Cardiac arrhythmias... Other AEs: Generalized epileptic seizure (grade 4-5) Sources: Cardiac arrhythmias (grade 4-5) Calcium increased serum Creatine kinase increased Blood myoglobin increased Leukocyte count increased Serum phosphate decreased Magnesium serum decreased Acute myocardial infarction Obstructive uropathy Cardio-respiratory arrest (grade 5) Hypoxic encephalopathy (grade 5) |
1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Other AEs: Vomiting, Abdominal pain... Other AEs: Vomiting (61%) Sources: Abdominal pain (12%) Diarrhea (14%) Hematemesis (2%) Hypokalemia (43%) Acid-base balance abnoraml (9%) Sinus tachycardia (62%) Supraventricular tachycardia (14%) Premature ventricular ectopic beats (19%) Hypotension (8%) Nervousness (21%) Tremor (14%) Disorientation (11%) Seizures (5%) |
1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Other AEs: Vomiting, Hypokalemia... Other AEs: Vomiting (30%) Sources: Hypokalemia (44%) Hyperglycemia (18%) Acid-base balance abnoraml (9%) Sinus tachycardia (100%) Supraventricular tachycardia (12%) Premature ventricular ectopic beats (10%) Atrial flutter/ fibrillation (12%) Multifocal atrial tachycardia (2%) Hemodynamic instability (40%) Tremor (16%) Seizures (14%) |
10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Other AEs: Abdominal pain, Rhabdomyolysis... Other AEs: Abdominal pain (21%) Sources: Rhabdomyolysis (7%) Hypotension (21%) Nervousness (64%) Disorientation (7%) |
10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Other AEs: Vomiting, Hypokalemia... Other AEs: Vomiting (73%) Sources: Hypokalemia (85%) Hyperglycemia (98%) Acid-base balance abnoraml (34%) Sinus tachycardia (100%) Supraventricular tachycardia (2%) Premature ventricular ectopic beats (3%) Atrial flutter/ fibrillation (1%) Hemodynamic instability (7%) Tremor (38%) Seizures (5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Vomiting | 12.64% | 20 mg/mL steady, intravenous Highest studied dose Dose: 20 mg/mL Route: intravenous Route: steady Dose: 20 mg/mL Sources: Page: p.500 |
unhealthy, 39 years (51 % < 40 years) n = 87 Health Status: unhealthy Condition: COPD|asthma Age Group: 39 years (51 % < 40 years) Sex: M+F Population Size: 87 Sources: Page: p.500 |
Vomiting | grade 3, 5.75% Disc. AE |
20 mg/mL steady, intravenous Highest studied dose Dose: 20 mg/mL Route: intravenous Route: steady Dose: 20 mg/mL Sources: Page: p.500 |
unhealthy, 39 years (51 % < 40 years) n = 87 Health Status: unhealthy Condition: COPD|asthma Age Group: 39 years (51 % < 40 years) Sex: M+F Population Size: 87 Sources: Page: p.500 |
Nervousness | 16.7% | 1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Tremor | 16.7% | 1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Dysrhythmias | grade 1, 16.7% | 1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Gastrointestinal discomfort | grade 3, 16.7% Disc. AE |
1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Supraventricular tachycardia | grade 3, 16.7% Disc. AE |
1200 mg 1 times / day steady, oral Recommended Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: Page: p.149 |
unhealthy, 66 ± 9 n = 6 Health Status: unhealthy Condition: COPD Age Group: 66 ± 9 Sex: M+F Population Size: 6 Sources: Page: p.149 |
Acute myocardial infarction | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Blood myoglobin increased | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Calcium increased serum | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Creatine kinase increased | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Leukocyte count increased | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Magnesium serum decreased | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Obstructive uropathy | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Serum phosphate decreased | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
|
Cardiac arrhythmias | grade 4-5 | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
Generalized epileptic seizure | grade 4-5 | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
Cardio-respiratory arrest | grade 5 | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
Hypoxic encephalopathy | grade 5 | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Sources: |
Disorientation | 11% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Abdominal pain | 12% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Diarrhea | 14% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Supraventricular tachycardia | 14% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Tremor | 14% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Premature ventricular ectopic beats | 19% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Hematemesis | 2% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Nervousness | 21% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Hypokalemia | 43% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Seizures | 5% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Vomiting | 61% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Sinus tachycardia | 62% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Hypotension | 8% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Acid-base balance abnoraml | 9% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 102 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 102 Sources: |
Premature ventricular ectopic beats | 10% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Sinus tachycardia | 100% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Atrial flutter/ fibrillation | 12% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Supraventricular tachycardia | 12% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Seizures | 14% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Tremor | 16% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Hyperglycemia | 18% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Multifocal atrial tachycardia | 2% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Vomiting | 30% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Hemodynamic instability | 40% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Hypokalemia | 44% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Acid-base balance abnoraml | 9% | 1600 mg 1 times / day multiple, oral (max) Overdose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: |
unhealthy n = 92 Health Status: unhealthy Condition: asthma|emphysema|chronic bronchitis Population Size: 92 Sources: |
Abdominal pain | 21% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Hypotension | 21% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Nervousness | 64% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Disorientation | 7% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Rhabdomyolysis | 7% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 14 Health Status: unknown Population Size: 14 Sources: |
Atrial flutter/ fibrillation | 1% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Sinus tachycardia | 100% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Supraventricular tachycardia | 2% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Premature ventricular ectopic beats | 3% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Acid-base balance abnoraml | 34% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Tremor | 38% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Seizures | 5% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Hemodynamic instability | 7% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Vomiting | 73% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Hypokalemia | 85% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
Hyperglycemia | 98% | 10 mg/kg single, oral (min) Overdose Dose: 10 mg/kg Route: oral Route: single Dose: 10 mg/kg Sources: |
unknown n = 157 Health Status: unknown Population Size: 157 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Computerised advice on drug dosage to improve prescribing practice. | 2001 |
|
Oral methyl-xanthines for bronchiectasis. | 2001 |
|
Doxofylline: a new generation xanthine bronchodilator devoid of major cardiovascular adverse effects. | 2001 |
|
A novel method for measuring gel strength of controlled release hydrogel tablets using a cone/plate rheometer. | 2001 |
|
Rat ventral prostate xanthine oxidase bioactivation of ethanol to acetaldehyde and 1-hydroxyethyl free radicals: analysis of its potential role in heavy alcohol drinking tumor-promoting effects. | 2001 |
|
Caffeine citrate: a review of its use in apnoea of prematurity. | 2001 |
|
Differential effects of fluvoxamine and other antidepressants on the biotransformation of melatonin. | 2001 Apr |
|
Evaluation of absorption kinetics of orally administered theophylline in rats based on gastrointestinal transit monitoring by gamma scintigraphy. | 2001 Apr |
|
How to safeguard delivery of high-alert i.v. drugs. | 2001 Feb |
|
Caffeine metabolism before and after liver transplantation. | 2001 Feb |
|
Metabolism of 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline in human hepatocytes: 2-amino-3-methylimidazo[4,5-f]quinoxaline-8-carboxylic acid is a major detoxification pathway catalyzed by cytochrome P450 1A2. | 2001 Feb |
|
High-throughput cytochrome P450 (CYP) inhibition screening via a cassette probe-dosing strategy. V. Validation of a direct injection/on-line guard cartridge extraction--tandem mass spectrometry method for CYP1A2 inhibition assessment. | 2001 Feb |
|
Effect of coadministered drugs and ethanol on the binding of therapeutic drugs to human serum in vitro. | 2001 Feb |
|
Advair: combination treatment with fluticasone propionate/salmeterol in the treatment of asthma. | 2001 Feb |
|
Rapid modulation of Na+/K+-ATPase activity in osmoregulatory tissues of a salmonid fish. | 2001 Feb |
|
Screening of beta-2 agonists and confirmation of fenoterol, orciprenaline, reproterol and terbutaline with gas chromatography-mass spectrometry as tetrahydroisoquinoline derivatives. | 2001 Feb 10 |
|
Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells. | 2001 Feb 15 |
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Hepatic arteriolo-portal venular shunting guarantees maintenance of nutritional microvascular supply in hepatic arterial buffer response of rat livers. | 2001 Feb 15 |
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The calcium-dependent [3H]acetylcholine release from synaptosomes of brown trout (Salmo trutta) optic tectum is inhibited by adenosine A1 receptors: effects of enucleation on A1 receptor density and cholinergic markers. | 2001 Feb 16 |
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Caffeine increases paragigantocellularis neuronal firing rate and induces withdrawal signs in morphine-dependent rats. | 2001 Feb 2 |
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Role of adenosine and glycogen in ischemic preconditioning of rat hearts. | 2001 Feb 23 |
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[Cerebral infarction in a patient consuming MaHuang extract and guarana]. | 2001 Feb 3 |
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[Theophylline in the treatment of sleep-related breathing disorders]. | 2001 Jan |
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Caffeine metabolism in a group of 67 patients with primary biliary cirrhosis. | 2001 Jan |
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Clinical correlations in infants in the neonatal intensive care unit with varying severity of gastroesophageal reflux. | 2001 Jan |
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[Rhabdomyolysis as a rare complication of theophylline poisoning]. | 2001 Jan 15 |
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Suspected caffeine and ephedrine toxicosis resulting from ingestion of an herbal supplement containing guarana and ma huang in dogs: 47 cases (1997-1999). | 2001 Jan 15 |
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Severe hyponatremia induced by theophylline and trimethoprim. | 2001 Jan 22 |
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Facilitative effects of an adenosine A1/A2 receptor blockade on spatial memory performance of rats: selective enhancement of reference memory retention during the light period. | 2001 Jan 8 |
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Newer and alternative non-steroidal treatments for asthmatic inflammation. | 2001 Jan-Feb |
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Improvement of encapsulation efficiency of water-in-oil-in-water emulsion with hypertonic inner aqueous phase. | 2001 Jan-Feb |
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Adenosine diphosphate ribose dilates bovine coronary small arteries through apyrase- and 5'-nucleotidase-mediated metabolism. | 2001 Jan-Feb |
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The mechanism of gentisic acid-induced relaxation of the guinea pig isolated trachea: the role of potassium channels and vasoactive intestinal peptide receptors. | 2001 Mar |
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Drug treatment of airway inflammation in asthma. | 2001 Mar |
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Plasma adenosine levels and P-selectin expression on platelets in preeclampsia. | 2001 Mar |
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Adenosine inhibits norepinephrine release in the postischemic rat heart: the mechanism of neuronal stunning. | 2001 Mar |
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Antiarrhythmic effects of adenosine on ischemia-induced ventricular fibrillation. | 2001 Mar |
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Study of in vitro and in vivo dissolution of theophylline from film-coated pellets. | 2001 Mar |
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New combination therapies for asthma. | 2001 Mar |
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Refractory seizure with hypokalaemia. | 2001 Mar |
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Continuous venovenous haemofiltration for the treatment of theophylline toxicity. | 2001 Mar |
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Purinergic contribution to circulatory, metabolic, and adrenergic responses to acute hypoxemia in fetal sheep. | 2001 Mar |
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Adenosine induces initial hypoxic-ischemic depression of synaptic transmission in the rat hippocampus in vivo. | 2001 Mar |
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Alkylxanthine-induced recovery of respiratory function following cervical spinal cord injury in adult rats. | 2001 Mar |
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Novel identification of pseudopolymorphic changes of theophylline during wet granulation using near infrared spectroscopy. | 2001 Mar |
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Profile of moxifloxacin drug interactions. | 2001 Mar 15 |
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Activation of glutamate uptake by guanosine in primary astrocyte cultures. | 2001 Mar 26 |
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Inhibitory effect of theophylline on recombinant GABA(A) receptor. | 2001 Mar 5 |
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Cytosolic xanthine oxidoreductase mediated bioactivation of ethanol to acetaldehyde and free radicals in rat breast tissue. Its potential role in alcohol-promoted mammary cancer. | 2001 Mar 7 |
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Escape deficits induced by inescapable shock and metabolic stress are reversed by adenosine receptor antagonists. | 2001 May |
Patents
Sample Use Guides
For a given population there is no single theophylline dose that will provide both safe
and effective serum concentrations for all patients. The dose of theophylline must be individualized on the basis of serum theophylline concentration measurements in order to achieve a dose that will provide maximum potential benefit with minimal risk of adverse effects.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24231152
1 mM theophylline inhibited histamine release from human skin mast cells
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ACTIVE MOIETY
SUBSTANCE RECORD