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Details

Stereochemistry ACHIRAL
Molecular Formula 2C7H8N4O2.C2H8N2.H2O
Molecular Weight 438.4416
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMINOPHYLLINE MONOHYDRATE

SMILES

O.NCCN.CN1C2=C(NC=N2)C(=O)N(C)C1=O.CN3C4=C(NC=N4)C(=O)N(C)C3=O

InChI

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

HIDE SMILES / InChI

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

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

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
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
Treatment options for sleep apnoea.
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
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
Antiasthmatic effect of YM976, a novel PDE4 inhibitor, in guinea pigs.
2001 Apr
Preparation of controlled release systems by free-radical UV polymerizations in the presence of a drug.
2001 Apr 2
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
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
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
K(ATP)(+) channels, nitric oxide, and adenosine are not required for local metabolic coronary vasodilation.
2001 Feb
Age-related differences in messenger ribonucleic acid expression of key proteins involved in adipose cell differentiation and metabolism.
2001 Feb
[Use of the paraxanthine/caffeine ratio in the saliva of patients with liver cirrhosis].
2001 Feb 1
Distinct modulation of evoked and spontaneous EPSCs by purinoceptors in the nucleus tractus solitarii of the rat.
2001 Feb 1
Breakage and fusion of the TEL (ETV6) gene in immature B lymphocytes induced by apoptogenic signals.
2001 Feb 1
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
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
Caffeine increases paragigantocellularis neuronal firing rate and induces withdrawal signs in morphine-dependent rats.
2001 Feb 2
[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
[Rhabdomyolysis as a rare complication of theophylline poisoning].
2001 Jan 15
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
Severe hyponatremia induced by theophylline and trimethoprim.
2001 Jan 22
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
Drug treatment of airway inflammation in asthma.
2001 Mar
Plasma adenosine levels and P-selectin expression on platelets in preeclampsia.
2001 Mar
Antiarrhythmic effects of adenosine on ischemia-induced ventricular fibrillation.
2001 Mar
New combination therapies for asthma.
2001 Mar
Purinergic contribution to circulatory, metabolic, and adrenergic responses to acute hypoxemia in fetal sheep.
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
A multiparticulate drug-delivery system based on pellets incorporated into congealable polyethylene glycol carrier materials.
2001 Mar 23
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 Dec 15 17:02:57 UTC 2023
Edited
by admin
on Fri Dec 15 17:02:57 UTC 2023
Record UNII
Y7E0LU9ZMS
Record Status Validated (UNII)
Record Version
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Name Type Language
AMINOPHYLLINE MONOHYDRATE
WHO-DD  
Common Name English
AMINOPHYLLINE HYDRATE [JAN]
Common Name English
1H-PURINE-2,6-DIONE, 3,9-DIHYDRO-1,3-DIMETHYL-, COMPD. WITH 1,2-ETHANEDIAMINE, HYDRATE (2:1:1)
Systematic Name English
THEOPHYLLINE-ETHYLENEDIAMINE MONOHYDRATE [EP MONOGRAPH]
Common Name English
AMINOPHYLLINE MONOHYDRATE [USP MONOGRAPH]
Common Name English
Aminophylline monohydrate [WHO-DD]
Common Name English
Code System Code Type Description
CAS
76970-41-7
Created by admin on Fri Dec 15 17:02:57 UTC 2023 , Edited by admin on Fri Dec 15 17:02:57 UTC 2023
PRIMARY
FDA UNII
Y7E0LU9ZMS
Created by admin on Fri Dec 15 17:02:57 UTC 2023 , Edited by admin on Fri Dec 15 17:02:57 UTC 2023
PRIMARY
CAS
72487-55-9
Created by admin on Fri Dec 15 17:02:57 UTC 2023 , Edited by admin on Fri Dec 15 17:02:57 UTC 2023
NON-SPECIFIC STOICHIOMETRY
EPA CompTox
DTXSID40227754
Created by admin on Fri Dec 15 17:02:57 UTC 2023 , Edited by admin on Fri Dec 15 17:02:57 UTC 2023
PRIMARY
PUBCHEM
16218860
Created by admin on Fri Dec 15 17:02:57 UTC 2023 , Edited by admin on Fri Dec 15 17:02:57 UTC 2023
PRIMARY
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ACTIVE MOIETY