U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C7H8N4O2.C6H5NO2
Molecular Weight 303.2734
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of THEOPHYLLINE NICOTINATE

SMILES

OC(=O)C1=CC=CN=C1.CN2C3=C(NC=N3)C(=O)N(C)C2=O

InChI

InChIKey=FWZBHOANBPBKHU-UHFFFAOYSA-N
InChI=1S/C7H8N4O2.C6H5NO2/c1-10-5-4(8-3-9-5)6(12)11(2)7(10)13;8-6(9)5-2-1-3-7-4-5/h3H,1-2H3,(H,8,9);1-4H,(H,8,9)

HIDE SMILES / InChI

Description
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

Curator's Comment: Albert Kossel discovered theophylline as a component of the tea leaf

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
THEOPHYLLINE AND DEXTROSE 5% IN PLASTIC CONTAINER

Approved Use

Theophylline 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 Date

1982
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7.3 μg/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
95.5 μg × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
8.51 h
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

Funbound

ValueDoseCo-administeredAnalytePopulation
41%
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

Doses

DosePopulationAdverse 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%)
Supraventricular tachycardia (grade 3, 16.7%)
Other AEs:
Tremor (16.7%)
Nervousness (16.7%)
Dysrhythmias (grade 1, 16.7%)
Sources: Page: p.149
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)
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)
Sources:
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%)
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%)
Sources:
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%)
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%)
Sources:
10 mg/kg single, oral (min)
Overdose
unknown
n = 14
Other AEs: Abdominal pain, Rhabdomyolysis...
Other AEs:
Abdominal pain (21%)
Rhabdomyolysis (7%)
Hypotension (21%)
Nervousness (64%)
Disorientation (7%)
Sources:
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Other AEs: Vomiting, Hypokalemia...
Other AEs:
Vomiting (73%)
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%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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
unknown
n = 14
Hypotension 21%
10 mg/kg single, oral (min)
Overdose
unknown
n = 14
Nervousness 64%
10 mg/kg single, oral (min)
Overdose
unknown
n = 14
Disorientation 7%
10 mg/kg single, oral (min)
Overdose
unknown
n = 14
Rhabdomyolysis 7%
10 mg/kg single, oral (min)
Overdose
unknown
n = 14
Atrial flutter/ fibrillation 1%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Sinus tachycardia 100%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Supraventricular tachycardia 2%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Premature ventricular ectopic beats 3%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Acid-base balance abnoraml 34%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Tremor 38%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Seizures 5%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Hemodynamic instability 7%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Vomiting 73%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Hypokalemia 85%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Hyperglycemia 98%
10 mg/kg single, oral (min)
Overdose
unknown
n = 157
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Beta-adrenergic modulation of NNK-induced lung carcinogenesis in hamsters.
2000 Nov
Theophylline administration markedly reduces hepatic and pulmonary implantation of B16-F10 melanoma cells in mice.
2000 Oct
Computerised advice on drug dosage to improve prescribing practice.
2001
Oral methyl-xanthines for bronchiectasis.
2001
Methyl-xanthines for exacerbations of chronic obstructive pulmonary disease.
2001
Doxofylline: a new generation xanthine bronchodilator devoid of major cardiovascular adverse effects.
2001
Time dependence of elastic recovery for characterization of tableting materials.
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
Creatinine clearance overestimated glomerular filtration rate in a heavy tea-drinker.
2001 Apr
Differential effects of fluvoxamine and other antidepressants on the biotransformation of melatonin.
2001 Apr
Antiasthmatic effect of YM976, a novel PDE4 inhibitor, in guinea pigs.
2001 Apr
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
Myocardial perfusion imaging findings and the role of adenosine in the warm-up angina phenomenon.
2001 Feb
Theophylline metabolism after cardiac surgery.
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
Therapeutic options for the management of patients with cardiac syndrome X.
2001 Feb
Effects of A-134974, a novel adenosine kinase inhibitor, on carrageenan-induced inflammatory hyperalgesia and locomotor activity in rats: evaluation of the sites of action.
2001 Feb
Anti-inflammatory effects of ABT-702, a novel non-nucleoside adenosine kinase inhibitor, in rat adjuvant arthritis.
2001 Feb
Age-related differences in messenger ribonucleic acid expression of key proteins involved in adipose cell differentiation and metabolism.
2001 Feb
Distinct modulation of evoked and spontaneous EPSCs by purinoceptors in the nucleus tractus solitarii of the rat.
2001 Feb 1
Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells.
2001 Feb 15
Hepatic arteriolo-portal venular shunting guarantees maintenance of nutritional microvascular supply in hepatic arterial buffer response of rat livers.
2001 Feb 15
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
Role of adenosine and glycogen in ischemic preconditioning of rat hearts.
2001 Feb 23
[Cerebral infarction in a patient consuming MaHuang extract and guarana].
2001 Feb 3
Development of heart failure in bradycardic sick sinus syndrome.
2001 Jan
Clinical correlations in infants in the neonatal intensive care unit with varying severity of gastroesophageal reflux.
2001 Jan
Calculation of the dimensions of dosage forms with release controlled by diffusion for in vivo use.
2001 Jan
A novel transverse push-pull microprobe: in vitro characterization and in vivo demonstration of the enzymatic production of adenosine in the spinal cord dorsal horn.
2001 Jan
Relaxant effect of Pimpinella anisum on isolated guinea pig tracheal chains and its possible mechanism(s).
2001 Jan
[Rhabdomyolysis as a rare complication of theophylline poisoning].
2001 Jan 15
Severe hyponatremia induced by theophylline and trimethoprim.
2001 Jan 22
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
Newer and alternative non-steroidal treatments for asthmatic inflammation.
2001 Jan-Feb
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
Plasma adenosine levels and P-selectin expression on platelets in preeclampsia.
2001 Mar
Adenosine inhibits norepinephrine release in the postischemic rat heart: the mechanism of neuronal stunning.
2001 Mar
Antiarrhythmic effects of adenosine on ischemia-induced ventricular fibrillation.
2001 Mar
Study of in vitro and in vivo dissolution of theophylline from film-coated pellets.
2001 Mar
New combination therapies for asthma.
2001 Mar
Refractory seizure with hypokalaemia.
2001 Mar
Purinergic contribution to circulatory, metabolic, and adrenergic responses to acute hypoxemia in fetal sheep.
2001 Mar
Adenosine induces initial hypoxic-ischemic depression of synaptic transmission in the rat hippocampus in vivo.
2001 Mar
Alkylxanthine-induced recovery of respiratory function following cervical spinal cord injury in adult rats.
2001 Mar
Novel identification of pseudopolymorphic changes of theophylline during wet granulation using near infrared spectroscopy.
2001 Mar
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
1 mM theophylline inhibited histamine release from human skin mast cells
Name Type Language
THEOPHYLLINE NICOTINATE
Common Name English
NSC-142642
Code English
3-PYRIDINECARBOXYLIC ACID, COMPD. WITH 3,9-DIHYDRO-1,3-DIMETHYL-1H-PURINE-2,6-DIONE (1:1)
Common Name English
NICOTINIC ACID, COMPD. WITH THEOPHYLLINE (1:1)
Common Name English
Code System Code Type Description
NSC
142642
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY
FDA UNII
LS5I9ST4B9
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY
CAS
32059-19-1
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY
EPA CompTox
DTXSID50301372
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY
PUBCHEM
285621
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY
SMS_ID
100000076970
Created by admin on Sat Dec 16 16:05:17 GMT 2023 , Edited by admin on Sat Dec 16 16:05:17 GMT 2023
PRIMARY