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Details

Stereochemistry ACHIRAL
Molecular Formula 2C7H8N4O2.C2H8N2.4H2O
Molecular Weight 492.4875
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMINOPHYLLINE TETRAHYDRATE

SMILES

O.O.O.O.NCCN.CN1C2=C(N=CN2)C(=O)N(C)C1=O.CN3C4=C(N=CN4)C(=O)N(C)C3=O

InChI

InChIKey=QIDMTYBNFQHLJS-UHFFFAOYSA-N
InChI=1S/2C7H8N4O2.C2H8N2.4H2O/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;4*1H2

HIDE SMILES / InChI

Molecular Formula C7H8N4O2
Molecular Weight 180.164
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C2H8N2
Molecular Weight 60.0983
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

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
Resin hemoperfusion as treatment for theophylline-induced seizures.
1979 Jun
[The effect of GM-CSF on endothelin-1 and endothelin converting enzyme gene expression in human airway smooth muscle cells with or without theophylline incubation].
1997 Oct
Epileptogenic action of caffeine during anoxia in the neonatal rat hippocampus.
1999 Jul
[A case of acute renal failure with rhabdomyolysis caused by the interaction of theophylline and clarithromycin].
1999 Jun
Effects of theophylline, dexamethasone and salbutamol on cytokine gene expression in human peripheral blood CD4+ T-cells.
1999 Nov
Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP.
1999 Nov
Theophylline as a therapy for chronic lymphocytic leukemia: a case report and review of literature.
2000
Effects of theophylline on human eosinophil functions: comparative study with neutrophil functions.
2000 Aug
Steroid hormone activity of flavonoids and related compounds.
2000 Jul
[Depression of serum pyridoxal levels in theophylline-related seizures].
2000 Jul
Beta-adrenergic modulation of NNK-induced lung carcinogenesis in hamsters.
2000 Nov
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
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
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
Mechanism of prolonged vasorelaxation to ATP in the rat isolated mesenteric arterial bed.
2001 Feb
K(ATP)(+) channels, nitric oxide, and adenosine are not required for local metabolic coronary vasodilation.
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
Hepatic arteriolo-portal venular shunting guarantees maintenance of nutritional microvascular supply in hepatic arterial buffer response of rat livers.
2001 Feb 15
Development of heart failure in bradycardic sick sinus syndrome.
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
Relationships between lipolysis induced by various lipolytic agents and hormone-sensitive lipase in rat fat cells.
2001 Jan
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
Mice with a deletion in the gene for CCAAT/enhancer-binding protein beta have an attenuated response to cAMP and impaired carbohydrate metabolism.
2001 Jan 5
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
Adenosine diphosphate ribose dilates bovine coronary small arteries through apyrase- and 5'-nucleotidase-mediated metabolism.
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
Intravenous theophylline--an alternative to temporary pacing in the management of bradycardia secondary to AV nodal block.
2001 Mar
Adenosine inhibits norepinephrine release in the postischemic rat heart: the mechanism of neuronal stunning.
2001 Mar
New combination therapies for asthma.
2001 Mar
Novel identification of pseudopolymorphic changes of theophylline during wet granulation using near infrared spectroscopy.
2001 Mar
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
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 Sat Dec 16 18:06:24 GMT 2023
Edited
by admin
on Sat Dec 16 18:06:24 GMT 2023
Record UNII
LPY3U2N8EG
Record Status Validated (UNII)
Record Version
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Name Type Language
AMINOPHYLLINE TETRAHYDRATE
Common Name English
1H-PURINE-2,6-DIONE, 3,9-DIHYDRO-1,3-DIMETHYL-, COMPD. WITH 1,2-ETHANEDIAMINE, HYDRATE (2:1:4)
Systematic Name English
1H-PURINE-2,6-DIONE, 3,7-DIHYDRO-1,3-DIMETHYL-, COMPD. WITH 1,2-ETHANEDIAMINE (2:1), TETRAHYDRATE
Systematic Name English
Code System Code Type Description
PUBCHEM
157010711
Created by admin on Sat Dec 16 18:06:24 GMT 2023 , Edited by admin on Sat Dec 16 18:06:24 GMT 2023
PRIMARY
CAS
56440-60-9
Created by admin on Sat Dec 16 18:06:24 GMT 2023 , Edited by admin on Sat Dec 16 18:06:24 GMT 2023
PRIMARY
FDA UNII
LPY3U2N8EG
Created by admin on Sat Dec 16 18:06:24 GMT 2023 , Edited by admin on Sat Dec 16 18:06:24 GMT 2023
PRIMARY
Related Record Type Details
ANHYDROUS->SOLVATE