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Identification
NameAminophylline
Accession NumberDB01223  (APRD00329)
TypeSmall Molecule
GroupsApproved
DescriptionAminophylline is a drug combination that contains theophylline and ethylenediamine in a 2:1 ratio. Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Similar to other theophyllines, aminophylline is indicated for the treatment of lung diseases such as asthma, chronic bronchitis, and COPD. The majority of aminophylline medications are discontinued and the remaining medications on the market are in short supply.
Structure
Thumb
Synonyms
Aminophyllin
Somophyllin
Theophylline ethylenediamine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aminophylline Inj 25mg/mlsolution25 mgintravenousOmega Laboratories Ltd1984-12-31Not applicableCanada
Aminophylline Inj 50mg/mlsolution50 mgintravenousOmega Laboratories Ltd1984-12-31Not applicableCanada
Aminophylline Injection 25mg/mlsolution25 mgintravenousHospira Healthcare Corporation1981-12-31Not applicableCanada
Aminophylline Injection 50mg/mlsolution50 mgintravenousHospira Healthcare Corporation1981-12-312012-08-03Canada
Aminophylline Tab 0.1gmtablet100 mgoralLederle Cyanamid Canada Inc.1951-12-312000-08-02Canada
Aminophylline Tab 100mgtablet97.5 mgoralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1957-12-312002-07-31Canada
Jaa Aminophylline Tab 100mgtablet100 mgoralJaapharm Canada Inc.1993-12-312016-08-10Canada
Phyllocontintablet (extended-release)225 mgoralPurdue Pharma1993-12-312011-08-04Canada
Phyllocontin-350tablet (extended-release)350 mgoralPurdue Pharma1993-12-312011-08-04Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aminophyllineinjection, solution25 mg/mLintravenousGeneral Injectables & Vaccines, Inc.2009-01-01Not applicableUs
Aminophyllinetablet100 mg/1oralWest ward Pharmaceutical Corp1975-11-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousCardinal Health2011-02-11Not applicableUs
Aminophyllinetablet200 mg/1oralWest ward Pharmaceutical Corp1976-05-28Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousCardinal Health2011-02-11Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousGeneral Injectables & Vaccines, Inc2010-07-01Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MinomalNot Available
SomophyllinNot Available
TruphyllineNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Aminophylline dihydrate
ThumbNot applicableDBSALT001739
Categories
UNII27Y3KJK423
CAS number317-34-0
WeightAverage: 420.4264
Monoisotopic: 420.198199306
Chemical FormulaC16H24N10O4
InChI KeyInChIKey=FQPFAHBPWDRTLU-UHFFFAOYSA-N
InChI
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
IUPAC Name
bis(1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione); ethane-1,2-diamine
SMILES
NCCN.CN1C2=C(NC=N2)C(=O)N(C)C1=O.CN1C2=C(NC=N2)C(=O)N(C)C1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alkaloids and derivatives. These are naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and more rarely other elements such as chlorine, bromine, and phosphorus.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassNot Available
Sub ClassNot Available
Direct ParentAlkaloids and derivatives
Alternative Parents
Substituents
  • Alkaloid or derivatives
  • Xanthine
  • Purinone
  • 6-oxopurine
  • Purine
  • Imidazopyrimidine
  • Pyrimidone
  • Pyrimidine
  • Heteroaromatic compound
  • Vinylogous amide
  • Imidazole
  • Azole
  • Urea
  • Lactam
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
PharmacodynamicsAminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion.
Mechanism of actionAminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 0.3 to 0.7 L/kg
Protein binding60%
MetabolismNot Available
Route of eliminationNot Available
Half life7-9 hours
Clearance
  • 0.29 mL/kg/min [postnatal age 3-15 days]
  • 0.64 mL/kg/min [postnatal age 25-57 days]
  • 1.7 mL/kg/min [ 1-4 years]
  • 1.6 mL/kg/min [4-12 years]
  • 0.9 mL/kg/min [13-15 years]
  • 1.4 mL/kg/min [16-17 years]
  • 0.65 mL/kg/min [Adults (16-60 years), non-smoking asthmatics]
  • 0.41 mL/kg/min [Elderly (>60 years). liver, and renal function]
  • 0.33 mL/kg/min [Acute pulmonary edema]
  • 0.54 mL/kg/min [COPD→60 years, stable non-smoker >1 year]
  • 0.48 mL/kg/min [COPD with cor pulmonale]
  • 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
  • 0.31 mL/kg/min [Liver disease -cholestasis]
  • 0.35 mL/kg/min [cirrhosis]
  • 0.65 mL/kg/min [acute hepatitis]
  • 0.47 mL/kg/min [Sepsis with multi-organ failure]
  • 0.38 mL/kg/min [hypothyroid]
  • 0.8 mL/kg/min [hyperthyroid]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9778
Blood Brain Barrier+0.5908
Caco-2 permeable-0.6802
P-glycoprotein substrateSubstrate0.7341
P-glycoprotein inhibitor INon-inhibitor0.9164
P-glycoprotein inhibitor IINon-inhibitor0.9673
Renal organic cation transporterNon-inhibitor0.7935
CYP450 2C9 substrateNon-substrate0.8073
CYP450 2D6 substrateNon-substrate0.8093
CYP450 3A4 substrateSubstrate0.5482
CYP450 1A2 substrateNon-inhibitor0.8726
CYP450 2C9 inhibitorNon-inhibitor0.9332
CYP450 2D6 inhibitorNon-inhibitor0.9633
CYP450 2C19 inhibitorNon-inhibitor0.9184
CYP450 3A4 inhibitorNon-inhibitor0.8031
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8858
Ames testNon AMES toxic0.6724
CarcinogenicityNon-carcinogens0.8696
BiodegradationNot ready biodegradable0.9149
Rat acute toxicity2.4979 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7876
hERG inhibition (predictor II)Inhibitor0.6143
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous25 mg/mL
Tabletoral100 mg/1
Tabletoral200 mg/1
Solutionintravenous50 mg
Solutionintravenous25 mg
Tabletoral100 mg
Tabletoral97.5 mg
Tablet (extended-release)oral225 mg
Tablet (extended-release)oral350 mg
Prices
Unit descriptionCostUnit
Aminophylline 250 mg/10 ml vial0.48USD ml
Aminophylline 25 mg/ml0.41USD ml
Phyllocontin-350 350 mg Sustained-Release Tablet0.31USD tablet
Aminophylline 100 mg tablet0.26USD tablet
Phyllocontin 225 mg Sustained-Release Tablet0.24USD tablet
Aminophylline powder0.17USD g
Aminophylline 200 mg tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility2E+005 mg/LMERCK INDEX (1996)
logP-3.03Not Available
Predicted Properties
PropertyValueSource
logP-0.77ChemAxon
pKa (Strongest Acidic)7.82ChemAxon
pKa (Strongest Basic)-0.78ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area69.3 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity44.93 m3·mol-1ChemAxon
Polarizability16.86 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR03DA05R03DB05R03DA55
AHFS Codes
  • 86:16.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.7 KB)
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe serum concentration of Aminophylline can be decreased when it is combined with 1,10-Phenanthroline.
3,4-DichloroisocoumarinThe serum concentration of Aminophylline can be decreased when it is combined with 3,4-Dichloroisocoumarin.
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe serum concentration of Aminophylline can be decreased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.
AbirateroneThe serum concentration of Aminophylline can be increased when it is combined with Abiraterone.
AcebutololAcebutolol may decrease the bronchodilatory activities of Aminophylline.
AdalimumabThe serum concentration of Aminophylline can be decreased when it is combined with Adalimumab.
AdenosineThe therapeutic efficacy of Adenosine can be decreased when used in combination with Aminophylline.
Albumin-interferon alphaThe metabolism of Aminophylline can be decreased when combined with Albumin-interferon alpha.
AllopurinolThe serum concentration of Aminophylline can be increased when it is combined with Allopurinol.
AlogliptinThe serum concentration of Aminophylline can be decreased when it is combined with Alogliptin.
Alpha-1-proteinase inhibitorThe serum concentration of Aminophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.
AlprazolamThe therapeutic efficacy of Alprazolam can be decreased when used in combination with Aminophylline.
AlprenololAlprenolol may decrease the bronchodilatory activities of Aminophylline.
AmiodaroneThe metabolism of Aminophylline can be decreased when combined with Amiodarone.
AmobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Amobarbital.
AmprenavirThe serum concentration of Aminophylline can be decreased when it is combined with Amprenavir.
Antithrombin III humanThe serum concentration of Aminophylline can be decreased when it is combined with Antithrombin III human.
ApixabanThe serum concentration of Aminophylline can be decreased when it is combined with Apixaban.
AprepitantThe serum concentration of Aminophylline can be increased when it is combined with Aprepitant.
AprotininThe serum concentration of Aminophylline can be decreased when it is combined with Aprotinin.
ArgatrobanThe serum concentration of Aminophylline can be decreased when it is combined with Argatroban.
AsunaprevirThe serum concentration of Aminophylline can be decreased when it is combined with Asunaprevir.
AtazanavirThe serum concentration of Aminophylline can be decreased when it is combined with Atazanavir.
AtenololAtenolol may decrease the bronchodilatory activities of Aminophylline.
AtomoxetineThe metabolism of Aminophylline can be decreased when combined with Atomoxetine.
AzithromycinThe metabolism of Aminophylline can be decreased when combined with Azithromycin.
BarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Barbital.
BatimastatThe serum concentration of Aminophylline can be decreased when it is combined with Batimastat.
BazedoxifeneThe serum concentration of Aminophylline can be increased when it is combined with Bazedoxifene.
BenazeprilThe serum concentration of Aminophylline can be decreased when it is combined with Benazepril.
BenzamidineThe serum concentration of Aminophylline can be decreased when it is combined with Benzamidine.
BetaxololBetaxolol may decrease the bronchodilatory activities of Aminophylline.
BexaroteneThe serum concentration of Aminophylline can be decreased when it is combined with Bexarotene.
BisoprololBisoprolol may decrease the bronchodilatory activities of Aminophylline.
BivalirudinThe serum concentration of Aminophylline can be decreased when it is combined with Bivalirudin.
BoceprevirThe serum concentration of Aminophylline can be decreased when it is combined with Boceprevir.
BopindololBopindolol may decrease the bronchodilatory activities of Aminophylline.
BortezomibThe metabolism of Aminophylline can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Aminophylline can be decreased when it is combined with Bosentan.
BromazepamThe therapeutic efficacy of Bromazepam can be decreased when used in combination with Aminophylline.
BupranololBupranolol may decrease the bronchodilatory activities of Aminophylline.
CaffeineThe metabolism of Aminophylline can be decreased when combined with Caffeine.
CandoxatrilThe serum concentration of Aminophylline can be decreased when it is combined with Candoxatril.
CaptoprilThe serum concentration of Aminophylline can be decreased when it is combined with Captopril.
CarbamazepineThe serum concentration of Aminophylline can be decreased when it is combined with Carbamazepine.
CarbimazoleThe serum concentration of Aminophylline can be increased when it is combined with Carbimazole.
CarteololCarteolol may decrease the bronchodilatory activities of Aminophylline.
CeliprololCeliprolol may decrease the bronchodilatory activities of Aminophylline.
CeritinibThe serum concentration of Aminophylline can be increased when it is combined with Ceritinib.
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Aminophylline.
ChlorotrianiseneThe serum concentration of Aminophylline can be increased when it is combined with Chlorotrianisene.
ChymostatinThe serum concentration of Aminophylline can be decreased when it is combined with Chymostatin.
CilastatinThe serum concentration of Aminophylline can be decreased when it is combined with Cilastatin.
CilazaprilThe serum concentration of Aminophylline can be decreased when it is combined with Cilazapril.
CimetidineThe metabolism of Aminophylline can be decreased when combined with Cimetidine.
CitalopramThe metabolism of Aminophylline can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Aminophylline can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Aminophylline can be decreased when combined with Clemastine.
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Aminophylline.
ClorazepateThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Aminophylline.
ClotrimazoleThe metabolism of Aminophylline can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Aminophylline can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Aminophylline can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Aminophylline can be increased when it is combined with Conjugated Equine Estrogens.
CrizotinibThe metabolism of Aminophylline can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Aminophylline can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Aminophylline can be decreased when it is combined with Cyproterone acetate.
Dabigatran etexilateThe serum concentration of Aminophylline can be decreased when it is combined with Dabigatran etexilate.
DabrafenibThe serum concentration of Aminophylline can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Aminophylline can be decreased when it is combined with Darunavir.
DasatinibThe serum concentration of Aminophylline can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Aminophylline can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Aminophylline can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Aminophylline can be decreased when it is combined with Dexamethasone.
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Aminophylline.
DienestrolThe serum concentration of Aminophylline can be increased when it is combined with Dienestrol.
DiethylstilbestrolThe serum concentration of Aminophylline can be increased when it is combined with Diethylstilbestrol.
DihydroergotamineThe metabolism of Aminophylline can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Aminophylline can be decreased when combined with Diltiazem.
DisulfiramThe serum concentration of Aminophylline can be increased when it is combined with Disulfiram.
DoxofyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Doxofylline.
DoxycyclineThe metabolism of Aminophylline can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Aminophylline can be decreased when combined with Dronedarone.
EcabetThe serum concentration of Aminophylline can be decreased when it is combined with Ecabet.
EdoxabanThe serum concentration of Aminophylline can be decreased when it is combined with Edoxaban.
EfavirenzThe serum concentration of Aminophylline can be decreased when it is combined with Efavirenz.
ElafinThe serum concentration of Aminophylline can be decreased when it is combined with Elafin.
EnalaprilThe serum concentration of Aminophylline can be decreased when it is combined with Enalapril.
EnalaprilatThe serum concentration of Aminophylline can be decreased when it is combined with Enalaprilat.
EnalkirenThe serum concentration of Aminophylline can be decreased when it is combined with Enalkiren.
EnzalutamideThe serum concentration of Aminophylline can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Aminophylline can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Aminophylline can be decreased when it is combined with Eslicarbazepine acetate.
EsmololEsmolol may decrease the bronchodilatory activities of Aminophylline.
EstazolamThe therapeutic efficacy of Estazolam can be decreased when used in combination with Aminophylline.
EstradiolThe serum concentration of Aminophylline can be increased when it is combined with Estradiol.
EstriolThe serum concentration of Aminophylline can be increased when it is combined with Estriol.
EstroneThe serum concentration of Aminophylline can be increased when it is combined with Estrone.
EthanolThe serum concentration of Aminophylline can be increased when it is combined with Ethanol.
Ethinyl EstradiolThe serum concentration of Aminophylline can be increased when it is combined with Ethinyl Estradiol.
EtravirineThe serum concentration of Aminophylline can be decreased when it is combined with Etravirine.
FebuxostatThe serum concentration of the active metabolites of Aminophylline can be increased when Aminophylline is used in combination with Febuxostat.
FluconazoleThe metabolism of Aminophylline can be decreased when combined with Fluconazole.
FlumazenilThe therapeutic efficacy of Flumazenil can be decreased when used in combination with Aminophylline.
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Aminophylline.
FlurazepamThe therapeutic efficacy of Flurazepam can be decreased when used in combination with Aminophylline.
FluvoxamineThe metabolism of Aminophylline can be decreased when combined with Fluvoxamine.
FormoterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.
FosamprenavirThe metabolism of Aminophylline can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Aminophylline can be increased when it is combined with Fosaprepitant.
FosinoprilThe serum concentration of Aminophylline can be decreased when it is combined with Fosinopril.
FosphenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Aminophylline can be increased when it is combined with Fusidic Acid.
GeldanamycinThe serum concentration of Aminophylline can be decreased when it is combined with Geldanamycin.
GenisteinThe serum concentration of Aminophylline can be increased when it is combined with Genistein.
GM6001The serum concentration of Aminophylline can be decreased when it is combined with GM6001.
HexestrolThe serum concentration of Aminophylline can be increased when it is combined with Hexestrol.
HexobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Hexobarbital.
HirulogThe serum concentration of Aminophylline can be decreased when it is combined with Hirulog.
IdelalisibThe serum concentration of Aminophylline can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Aminophylline can be decreased when combined with Imatinib.
IndacaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Indacaterol.
IndinavirThe serum concentration of Aminophylline can be decreased when it is combined with Indinavir.
Interferon Alfa-2a, RecombinantThe metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2a, Recombinant.
Interferon Alfa-2b, RecombinantThe metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.
Interferon alfa-n1The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n1.
Interferon alfacon-1The metabolism of Aminophylline can be decreased when combined with Interferon alfacon-1.
Interferon beta-1aThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1a.
Interferon beta-1bThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1b.
IsavuconazoniumThe metabolism of Aminophylline can be decreased when combined with Isavuconazonium.
IsoflurophateThe serum concentration of Aminophylline can be decreased when it is combined with Isoflurophate.
IsoniazidThe serum concentration of Aminophylline can be increased when it is combined with Isoniazid.
IsoprenalineThe serum concentration of Aminophylline can be decreased when it is combined with Isoprenaline.
IsradipineThe metabolism of Aminophylline can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Aminophylline can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Aminophylline can be increased when it is combined with Ivacaftor.
IxazomibThe serum concentration of Aminophylline can be decreased when it is combined with Ixazomib.
KetoconazoleThe metabolism of Aminophylline can be decreased when combined with Ketoconazole.
LepirudinThe serum concentration of Aminophylline can be decreased when it is combined with Lepirudin.
LevothyroxineThe metabolism of Aminophylline can be increased when combined with Levothyroxine.
LidocaineThe metabolism of Aminophylline can be decreased when combined with Lidocaine.
LinagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Linagliptin.
LiothyronineThe metabolism of Aminophylline can be increased when combined with Liothyronine.
LiotrixThe metabolism of Aminophylline can be increased when combined with Liotrix.
LisinoprilThe serum concentration of Aminophylline can be decreased when it is combined with Lisinopril.
LithiumThe serum concentration of Lithium can be decreased when it is combined with Aminophylline.
LopinavirThe serum concentration of Aminophylline can be decreased when it is combined with Lopinavir.
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Aminophylline.
LovastatinThe metabolism of Aminophylline can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Aminophylline can be increased when it is combined with Luliconazole.
MestranolThe serum concentration of Aminophylline can be increased when it is combined with Mestranol.
MethimazoleThe serum concentration of Aminophylline can be increased when it is combined with Methimazole.
MethohexitalThe serum concentration of Aminophylline can be decreased when it is combined with Methohexital.
MethotrexateThe serum concentration of Aminophylline can be increased when it is combined with Methotrexate.
MethylphenobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Methylphenobarbital.
MetoprololMetoprolol may decrease the bronchodilatory activities of Aminophylline.
MexiletineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.
MidazolamThe therapeutic efficacy of Midazolam can be decreased when used in combination with Aminophylline.
MifepristoneThe metabolism of Aminophylline can be decreased when combined with Mifepristone.
MitotaneThe serum concentration of Aminophylline can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Aminophylline can be decreased when it is combined with Modafinil.
MoexiprilThe serum concentration of Aminophylline can be decreased when it is combined with Moexipril.
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Aminophylline can be decreased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.
NadololNadolol may decrease the bronchodilatory activities of Aminophylline.
NafcillinThe serum concentration of Aminophylline can be decreased when it is combined with Nafcillin.
Natural alpha interferonThe metabolism of Aminophylline can be decreased when combined with Natural alpha interferon.
NCX 4016The serum concentration of Aminophylline can be decreased when it is combined with NCX 4016.
NebivololNebivolol may decrease the bronchodilatory activities of Aminophylline.
NefazodoneThe metabolism of Aminophylline can be decreased when combined with Nefazodone.
NelfinavirThe serum concentration of Aminophylline can be decreased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Aminophylline can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Aminophylline can be decreased when combined with Nevirapine.
NicotineThe metabolism of Aminophylline can be decreased when combined with Nicotine.
NilotinibThe metabolism of Aminophylline can be decreased when combined with Nilotinib.
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Aminophylline.
OlaparibThe metabolism of Aminophylline can be decreased when combined with Olaparib.
OlodaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Olodaterol.
OmapatrilatThe serum concentration of Aminophylline can be decreased when it is combined with Omapatrilat.
OsimertinibThe serum concentration of Aminophylline can be increased when it is combined with Osimertinib.
OtamixabanThe serum concentration of Aminophylline can be decreased when it is combined with Otamixaban.
OxazepamThe therapeutic efficacy of Oxazepam can be decreased when used in combination with Aminophylline.
OxprenololOxprenolol may decrease the bronchodilatory activities of Aminophylline.
PalbociclibThe serum concentration of Aminophylline can be increased when it is combined with Palbociclib.
PancuroniumThe risk or severity of adverse effects can be increased when Aminophylline is combined with Pancuronium.
Peginterferon alfa-2aThe metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.
Peginterferon alfa-2bThe serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.
Peginterferon beta-1aThe metabolism of Aminophylline can be decreased when combined with Peginterferon beta-1a.
PenbutololPenbutolol may decrease the bronchodilatory activities of Aminophylline.
PentobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Pentobarbital.
PentoxifyllineThe serum concentration of Aminophylline can be increased when it is combined with Pentoxifylline.
PerindoprilThe serum concentration of Aminophylline can be decreased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Phenytoin.
PhosphoramidonThe serum concentration of Aminophylline can be decreased when it is combined with Phosphoramidon.
PindololPindolol may decrease the bronchodilatory activities of Aminophylline.
PirenzepineThe therapeutic efficacy of Pirenzepine can be decreased when used in combination with Aminophylline.
Polyestradiol phosphateThe serum concentration of Aminophylline can be increased when it is combined with Polyestradiol phosphate.
PosaconazoleThe metabolism of Aminophylline can be decreased when combined with Posaconazole.
PrazepamThe therapeutic efficacy of Prazepam can be decreased when used in combination with Aminophylline.
PrimidoneThe serum concentration of Aminophylline can be decreased when it is combined with Primidone.
PrinomastatThe serum concentration of Aminophylline can be decreased when it is combined with Prinomastat.
ProbenecidThe serum concentration of Aminophylline can be increased when it is combined with Probenecid.
PropafenoneThe serum concentration of Aminophylline can be increased when it is combined with Propafenone.
PropranololPropranolol may decrease the bronchodilatory activities of Aminophylline.
PropylthiouracilThe serum concentration of Aminophylline can be increased when it is combined with Propylthiouracil.
QuinaprilThe serum concentration of Aminophylline can be decreased when it is combined with Quinapril.
QuinestrolThe serum concentration of Aminophylline can be increased when it is combined with Quinestrol.
QuinineThe serum concentration of Aminophylline can be increased when it is combined with Quinine.
RamiprilThe serum concentration of Aminophylline can be decreased when it is combined with Ramipril.
RanolazineThe metabolism of Aminophylline can be decreased when combined with Ranolazine.
RegadenosonAminophylline may decrease the vasodilatory activities of Regadenoson.
RemikirenThe serum concentration of Aminophylline can be decreased when it is combined with Remikiren.
RifabutinThe metabolism of Aminophylline can be increased when combined with Rifabutin.
RifampicinThe metabolism of Aminophylline can be increased when combined with Rifampicin.
RifapentineThe metabolism of Aminophylline can be increased when combined with Rifapentine.
RiociguatAminophylline may increase the hypotensive activities of Riociguat.
RitonavirThe serum concentration of Aminophylline can be decreased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Aminophylline can be decreased when it is combined with Rivaroxaban.
RopiniroleThe metabolism of Aminophylline can be decreased when combined with Ropinirole.
SaquinavirThe serum concentration of Aminophylline can be decreased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Saxagliptin.
SecobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Secobarbital.
SildenafilThe metabolism of Aminophylline can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Aminophylline can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Aminophylline can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Sitagliptin.
SotalolSotalol may decrease the bronchodilatory activities of Aminophylline.
SpiraprilThe serum concentration of Aminophylline can be decreased when it is combined with Spirapril.
St. John's WortThe serum concentration of Aminophylline can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Aminophylline can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Aminophylline can be decreased when combined with Sulfisoxazole.
Synthetic Conjugated Estrogens, AThe serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, A.
Synthetic Conjugated Estrogens, BThe serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, B.
TelaprevirThe serum concentration of Aminophylline can be decreased when it is combined with Telaprevir.
TelithromycinThe metabolism of Aminophylline can be decreased when combined with Telithromycin.
TemazepamThe therapeutic efficacy of Temazepam can be decreased when used in combination with Aminophylline.
TemocaprilThe serum concentration of Aminophylline can be decreased when it is combined with Temocapril.
TenofovirThe metabolism of Aminophylline can be decreased when combined with Tenofovir.
TeriflunomideThe serum concentration of Aminophylline can be decreased when it is combined with Teriflunomide.
TheophyllineThe metabolism of Aminophylline can be decreased when combined with Theophylline.
ThiabendazoleThe metabolism of Aminophylline can be decreased when combined with Thiabendazole.
ThiamylalThe serum concentration of Aminophylline can be decreased when it is combined with Thiamylal.
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Aminophylline.
ThiopentalThe serum concentration of Aminophylline can be decreased when it is combined with Thiopental.
ThiorphanThe serum concentration of Aminophylline can be decreased when it is combined with Thiorphan.
Thyroid, porcineThe metabolism of Aminophylline can be increased when combined with Thyroid, porcine.
TiboloneThe serum concentration of Aminophylline can be increased when it is combined with Tibolone.
TiclopidineThe metabolism of Aminophylline can be decreased when combined with Ticlopidine.
TimololTimolol may decrease the bronchodilatory activities of Aminophylline.
TipranavirThe serum concentration of Aminophylline can be decreased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Aminophylline can be decreased when it is combined with Tocilizumab.
TrandolaprilThe serum concentration of Aminophylline can be decreased when it is combined with Trandolapril.
TriazolamThe therapeutic efficacy of Triazolam can be decreased when used in combination with Aminophylline.
UbenimexThe serum concentration of Aminophylline can be decreased when it is combined with Ubenimex.
VemurafenibThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Aminophylline can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Aminophylline can be decreased when combined with Verapamil.
VildagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Vildagliptin.
VoriconazoleThe metabolism of Aminophylline can be decreased when combined with Voriconazole.
XimelagatranThe serum concentration of Aminophylline can be decreased when it is combined with Ximelagatran.
ZafirlukastThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.
ZeranolThe serum concentration of Aminophylline can be increased when it is combined with Zeranol.
ZiprasidoneThe metabolism of Aminophylline can be decreased when combined with Ziprasidone.
Food Interactions
  • Limit caffeine intake.
  • Take with food.
  • Vitamin B6 needs increased, supplement recommended.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name:
PDE3A
Uniprot ID:
Q14432
Molecular Weight:
124978.06 Da
References
  1. Hirota K, Yoshioka H, Kabara S, Koizumi Y, Abe H, Sato T, Matsuki A: Spasmolytic effects of colforsin daropate on serotonin-induced pulmonary hypertension and bronchoconstriction in dogs. Acta Anaesthesiol Scand. 2002 Mar;46(3):297-302. [PubMed:11939921 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Purine nucleoside binding
Specific Function:
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
ADORA1
Uniprot ID:
P30542
Molecular Weight:
36511.325 Da
References
  1. Yamamoto S, Nakanishi O, Matsui T, Shinohara N, Kinoshita H, Lambert C, Ishikawa T: Intrathecal adenosine A1 receptor agonist attenuates hyperalgesia without inhibiting spinal glutamate release in the rat. Cell Mol Neurobiol. 2003 Apr;23(2):175-85. [PubMed:12735630 ]
  2. Lerman BB: Response of nonreentrant catecholamine-mediated ventricular tachycardia to endogenous adenosine and acetylcholine. Evidence for myocardial receptor-mediated effects. Circulation. 1993 Feb;87(2):382-90. [PubMed:8425287 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
G-protein coupled adenosine receptor activity
Specific Function:
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. Possible role in reproduction.
Gene Name:
ADORA3
Uniprot ID:
P0DMS8
Molecular Weight:
36184.175 Da
References
  1. Stella L, de Novellis V, Marabese I, Berrino L, Maione S, Filippelli A, Rossi F: The role of A3 adenosine receptors in central regulation of arterial blood pressure. Br J Pharmacol. 1998 Oct;125(3):437-40. [PubMed:9806324 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
activator
General Function:
Transcription factor binding
Specific Function:
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Forms transcriptional repressor c...
Gene Name:
HDAC2
Uniprot ID:
Q92769
Molecular Weight:
55363.855 Da
References
  1. Ito K, Lim S, Caramori G, Cosio B, Chung KF, Adcock IM, Barnes PJ: A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6. Epub 2002 Jun 17. [PubMed:12070353 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23