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Details

Stereochemistry ACHIRAL
Molecular Formula 2C7H8N4O2.C2H8N2
Molecular Weight 420.427
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMINOPHYLLINE

SMILES

Cn1c2c(c(=O)n(C)c1=O)nc[nH]2.Cn1c2c(c(=O)n(C)c1=O)nc[nH]2.C(CN)N

InChI

InChIKey=FQPFAHBPWDRTLU-UHFFFAOYSA-N
InChI=1S/2C7H8N4O2.C2H8N2/c2*1-10-5-4(8-3-9-5)6(12)11(2)7(10)13;3-1-2-4/h2*3H,1-2H3,(H,8,9);1-4H2

HIDE SMILES / InChI

Molecular Formula C2H8N2
Molecular Weight 60.0984
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C7H8N4O2
Molecular Weight 180.1643
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

3.96489589E11
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
Influence of adenosine agonists and antiepileptic drugs on theophylline-induced seizures in rats.
1998 Oct
Theophylline and cisplatin synergize in down regulation of BCL-2 induction of apoptosis in human granulosa cells transformed by a mutated p53 (p53 val135) and Ha-ras oncogene.
2000 Aug
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
Time dependence of elastic recovery for characterization of tableting materials.
2001
A comparison of reflectance and transmittance near-infrared spectroscopic techniques in determining drug content in intact tablets.
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
Antiasthmatic effect of YM976, a novel PDE4 inhibitor, in guinea pigs.
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
Age-related differences in messenger ribonucleic acid expression of key proteins involved in adipose cell differentiation and metabolism.
2001 Feb
Determination of urinary methylated purine pattern by high-performance liquid chromatography.
2001 Feb 10
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
[Theophylline in the treatment of sleep-related breathing disorders].
2001 Jan
Caffeine metabolism in a group of 67 patients with primary biliary cirrhosis.
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
Adenosine diphosphate ribose dilates bovine coronary small arteries through apyrase- and 5'-nucleotidase-mediated metabolism.
2001 Jan-Feb
Drug treatment of airway inflammation in asthma.
2001 Mar
Plasma adenosine levels and P-selectin expression on platelets in preeclampsia.
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
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
Profile of moxifloxacin drug interactions.
2001 Mar 15
Activation of glutamate uptake by guanosine in primary astrocyte cultures.
2001 Mar 26
Inhibitory effect of theophylline on recombinant GABA(A) receptor.
2001 Mar 5
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
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
1 mM theophylline inhibited histamine release from human skin mast cells
Substance Class Chemical
Created
by admin
on Fri Jun 25 20:53:52 UTC 2021
Edited
by admin
on Fri Jun 25 20:53:52 UTC 2021
Record UNII
27Y3KJK423
Record Status Validated (UNII)
Record Version
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Name Type Language
AMINOPHYLLINE
HSDB   INCI   INN   MART.   MI   ORANGE BOOK   USP   VANDF   WHO-DD   WHO-IP  
INN   INCI  
Official Name English
AMINOPHYLLINE [USP MONOGRAPH]
Common Name English
AMINOPHYLLINE [MART.]
Common Name English
AMINOPHYLLINUM [WHO-IP LATIN]
Common Name English
THEOPHYLLINE-ETHYLENEDIAMINE ANHYDROUS [EP]
Common Name English
1H-PURINE-2,6-DIONE, 3,7-DIHYDRO-1,3-DIMETHYL-, COMPD. WITH 1,2-ETHANEDIAMINE (2:1)
Systematic Name English
SOMOPHYLLIN
Brand Name English
AMINOPHYLLINE [WHO-IP]
Common Name English
THEOPHYLLINE-ETHYLENEDIAMINE ANHYDROUS
EP  
Common Name English
CARDOPHYLLIN
Common Name English
NSC-7919
Code English
AMINOPHYLLINE [VANDF]
Common Name English
TRUPHYLLINE
Brand Name English
AMINOPHYLLINE [HSDB]
Common Name English
LINAMPHETA
Common Name English
THEOPHYLLINE COMPOUND WITH ETHYLENEDIAMINE (2:1)
Systematic Name English
AMINOPHYLLIN
Brand Name English
AMINOPHYLLINE [MI]
Common Name English
THEOPHYLLINE AND ETHYLENEDIAMINE
Systematic Name English
THEOPHYLLINE-ETHYLENEDIAMINE [EP MONOGRAPH]
Common Name English
AMINOPHYLLINE [ORANGE BOOK]
Common Name English
AMINOPHYLLINE [INN]
Common Name English
THEOPHYLLINE ETHYLENEDIAMINE
Systematic Name English
AMINOPHYLLINE [INCI]
Common Name English
SYNTOPHYLLIN
Common Name English
AMINOPHYLLINE [WHO-DD]
Common Name English
PHYLLOCONTIN
Brand Name English
Classification Tree Code System Code
WHO-VATC QR03DB05
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
WHO-ATC R03DB05
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
WHO-VATC QR03DA05
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
WHO-ATC R03DA55
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
NCI_THESAURUS C744
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
WHO-VATC QR03DA55
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
LIVERTOX 41
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
WHO-ATC R03DA05
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
NCI_THESAURUS C319
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
Code System Code Type Description
DRUG BANK
DB01223
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
MERCK INDEX
M1731
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C47393
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
CAS
317-34-0
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
HSDB
221
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
PUBCHEM
9433
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
LACTMED
Aminophylline
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
INN
376
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
RXCUI
689
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY RxNorm
EVMPD
SUB05444MIG
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
ChEMBL
CHEMBL190
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
FDA UNII
27Y3KJK423
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
MESH
D000628
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
ECHA (EC/EINECS)
206-264-5
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
WIKIPEDIA
AMINOPHYLLINE
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
AMINOPHYLLINE
Created by admin on Fri Jun 25 20:53:52 UTC 2021 , Edited by admin on Fri Jun 25 20:53:52 UTC 2021
PRIMARY Description: White or slightly yellowish granules or powder; odour, slightly ammoniacal. Solubility: Freely soluble in water (the solution may become cloudy in the presence of carbon dioxide); slightly soluble in ethanol (~750 g/l) TS; practically insoluble in ether R. Category: Antispasmodic; diuretic; coronary vasodilator.Storage. Aminophylline should be kept in a tightly closed container, protected from light. Additional information: Aminophylline contains a variable quantity of water of hydration. Upon exposure to air Aminophylline gradually loses ethylenediamine and absorbs carbon dioxide with the liberation of free theophylline. Even in the absence of light, Aminophylline is gradually degraded on exposure to a humid atmosphere, the decomposition being faster at higher temperatures. Definition: Aminophylline contains not less than 78.0% and not more than 86.0% of theophylline (C7H8N4O2), and not less than 12.8% and not more than 15.0% of ethylenediamine (C2H8N2), both calculated with reference to the anhydrous substance.
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Related Record Type Details
ACTIVE MOIETY