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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 release225 mgOralPurdue Pharma1993-12-312011-08-04Canada
Phyllocontin-350Tablet, extended release350 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 KeyFQPFAHBPWDRTLU-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
Pharmacology
IndicationFor the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
cGMP-inhibited 3',5'-cyclic phosphodiesterase AProteinyes
inhibitor
HumanQ14432 details
Adenosine receptor A1Proteinyes
antagonist
HumanP30542 details
Adenosine receptor A3Proteinyes
antagonist
HumanP0DMS8 details
Histone deacetylase 2Proteinyes
activator
HumanQ92769 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Aminophylline can be decreased when it is combined with 1,10-Phenanthroline.Experimental
3,4-DichloroisocoumarinThe serum concentration of Aminophylline can be decreased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe serum concentration of Aminophylline can be decreased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.Experimental
AbirateroneThe serum concentration of Aminophylline can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may decrease the bronchodilatory activities of Aminophylline.Approved
AdalimumabThe serum concentration of Aminophylline can be decreased when it is combined with Adalimumab.Approved
AdenosineThe therapeutic efficacy of Adenosine can be decreased when used in combination with Aminophylline.Approved, Investigational
Albumin-interferon alphaThe metabolism of Aminophylline can be decreased when combined with Albumin-interferon alpha.Investigational
AllopurinolThe serum concentration of Aminophylline can be increased when it is combined with Allopurinol.Approved
AlogliptinThe serum concentration of Aminophylline can be decreased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Aminophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlprazolamThe therapeutic efficacy of Alprazolam can be decreased when used in combination with Aminophylline.Approved, Illicit, Investigational
AlprenololAlprenolol may decrease the bronchodilatory activities of Aminophylline.Approved, Withdrawn
AmiodaroneThe metabolism of Aminophylline can be decreased when combined with Amiodarone.Approved, Investigational
AmobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Amobarbital.Approved, Illicit
AmprenavirThe serum concentration of Aminophylline can be decreased when it is combined with Amprenavir.Approved
Antithrombin III humanThe serum concentration of Aminophylline can be decreased when it is combined with Antithrombin III human.Approved
ApixabanThe serum concentration of Aminophylline can be decreased when it is combined with Apixaban.Approved
AprepitantThe serum concentration of Aminophylline can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Aminophylline can be decreased when it is combined with Aprotinin.Approved, Withdrawn
ArgatrobanThe serum concentration of Aminophylline can be decreased when it is combined with Argatroban.Approved, Investigational
AsunaprevirThe serum concentration of Aminophylline can be decreased when it is combined with Asunaprevir.Approved, Investigational
AtazanavirThe metabolism of Aminophylline can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may decrease the bronchodilatory activities of Aminophylline.Approved
AtomoxetineThe metabolism of Aminophylline can be decreased when combined with Atomoxetine.Approved
AzithromycinThe metabolism of Aminophylline can be decreased when combined with Azithromycin.Approved
BarbexacloneThe serum concentration of Aminophylline can be decreased when it is combined with Barbexaclone.Experimental
BarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Barbital.Illicit
BatimastatThe serum concentration of Aminophylline can be decreased when it is combined with Batimastat.Experimental
BazedoxifeneThe serum concentration of Aminophylline can be increased when it is combined with Bazedoxifene.Approved, Investigational
BenazeprilThe serum concentration of Aminophylline can be decreased when it is combined with Benazepril.Approved, Investigational
BenzamidineThe serum concentration of Aminophylline can be decreased when it is combined with Benzamidine.Experimental
BetaxololBetaxolol may decrease the bronchodilatory activities of Aminophylline.Approved
BexaroteneThe serum concentration of Aminophylline can be decreased when it is combined with Bexarotene.Approved, Investigational
Bi201335The serum concentration of Aminophylline can be decreased when it is combined with Bi201335.Investigational
BisoprololBisoprolol may decrease the bronchodilatory activities of Aminophylline.Approved
BivalirudinThe serum concentration of Aminophylline can be decreased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Aminophylline can be decreased when combined with Boceprevir.Approved
BopindololBopindolol may decrease the bronchodilatory activities of Aminophylline.Approved
BortezomibThe metabolism of Aminophylline can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Aminophylline can be decreased when it is combined with Bosentan.Approved, Investigational
BromazepamThe therapeutic efficacy of Bromazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
BupranololBupranolol may decrease the bronchodilatory activities of Aminophylline.Approved
CaffeineThe metabolism of Aminophylline can be decreased when combined with Caffeine.Approved
CamazepamThe therapeutic efficacy of Camazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
CandoxatrilThe serum concentration of Aminophylline can be decreased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Aminophylline can be decreased when it is combined with Candoxatrilat.Experimental
CaptoprilThe serum concentration of Aminophylline can be decreased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Aminophylline can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbimazoleThe serum concentration of Aminophylline can be increased when it is combined with Carbimazole.Approved
CarbomycinThe metabolism of Aminophylline can be decreased when combined with Carbomycin.Vet Approved
CarteololCarteolol may decrease the bronchodilatory activities of Aminophylline.Approved
CeliprololCeliprolol may decrease the bronchodilatory activities of Aminophylline.Approved, Investigational
CeritinibThe serum concentration of Aminophylline can be increased when it is combined with Ceritinib.Approved
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Aminophylline.Approved, Illicit
ChlorotrianiseneThe serum concentration of Aminophylline can be increased when it is combined with Chlorotrianisene.Withdrawn
ChymostatinThe serum concentration of Aminophylline can be decreased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Aminophylline can be decreased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Aminophylline can be decreased when it is combined with Cilazapril.Approved
CimetidineThe metabolism of Aminophylline can be decreased when combined with Cimetidine.Approved
CinoxacinThe metabolism of Aminophylline can be decreased when combined with Cinoxacin.Approved, Withdrawn
CiprofloxacinThe metabolism of Aminophylline can be decreased when combined with Ciprofloxacin.Approved, Investigational
CitalopramThe metabolism of Aminophylline can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Aminophylline can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Aminophylline can be decreased when combined with Clemastine.Approved
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
ClorazepateThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Aminophylline.Approved, Illicit
ClotrimazoleThe metabolism of Aminophylline can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Aminophylline can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Aminophylline can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Aminophylline can be increased when it is combined with Conjugated Equine Estrogens.Approved
CrizotinibThe metabolism of Aminophylline can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Aminophylline can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Aminophylline can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of Aminophylline can be decreased when it is combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Aminophylline can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Aminophylline can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Aminophylline can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Aminophylline can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Aminophylline can be decreased when combined with Delavirdine.Approved
DelorazepamThe therapeutic efficacy of Delorazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
DexamethasoneThe serum concentration of Aminophylline can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Aminophylline.Approved, Illicit, Vet Approved
DienestrolThe serum concentration of Aminophylline can be increased when it is combined with Dienestrol.Approved
DiethylstilbestrolThe serum concentration of Aminophylline can be increased when it is combined with Diethylstilbestrol.Approved
DihydroergotamineThe metabolism of Aminophylline can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Aminophylline can be decreased when combined with Diltiazem.Approved
DisulfiramThe serum concentration of Aminophylline can be increased when it is combined with Disulfiram.Approved
DoxofyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Doxofylline.Approved
DoxycyclineThe metabolism of Aminophylline can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Aminophylline can be decreased when combined with Dronedarone.Approved
EcabetThe serum concentration of Aminophylline can be decreased when it is combined with Ecabet.Approved, Investigational
EdoxabanThe serum concentration of Aminophylline can be decreased when it is combined with Edoxaban.Approved
EfavirenzThe serum concentration of Aminophylline can be decreased when it is combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Aminophylline can be decreased when it is combined with Elafin.Investigational
EnalaprilThe serum concentration of Aminophylline can be decreased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Aminophylline can be decreased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Aminophylline can be decreased when it is combined with Enalkiren.Experimental
EnoxacinThe metabolism of Aminophylline can be decreased when combined with Enoxacin.Approved
EnzalutamideThe serum concentration of Aminophylline can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Aminophylline can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Aminophylline can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmololEsmolol may decrease the bronchodilatory activities of Aminophylline.Approved
EstazolamThe therapeutic efficacy of Estazolam can be decreased when used in combination with Aminophylline.Approved, Illicit
EstradiolThe serum concentration of Aminophylline can be increased when it is combined with Estradiol.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Aminophylline can be increased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Aminophylline can be increased when it is combined with Estrone.Approved
EthanolThe serum concentration of Aminophylline can be increased when it is combined with Ethanol.Approved
Ethinyl EstradiolThe serum concentration of Aminophylline can be increased when it is combined with Ethinyl Estradiol.Approved
EtizolamThe therapeutic efficacy of Etizolam can be decreased when used in combination with Aminophylline.Approved
EtravirineThe serum concentration of Aminophylline can be decreased when it is combined with Etravirine.Approved
FebuxostatThe serum concentration of the active metabolites of Aminophylline can be increased when Aminophylline is used in combination with Febuxostat.Approved
FleroxacinThe metabolism of Aminophylline can be decreased when combined with Fleroxacin.Approved
FluconazoleThe metabolism of Aminophylline can be decreased when combined with Fluconazole.Approved
FludiazepamThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
FlumazenilThe therapeutic efficacy of Flumazenil can be decreased when used in combination with Aminophylline.Approved
FlumequineThe metabolism of Aminophylline can be decreased when combined with Flumequine.Withdrawn
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
FlurazepamThe therapeutic efficacy of Flurazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
FluvoxamineThe metabolism of Aminophylline can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.Approved, Investigational
FosamprenavirThe metabolism of Aminophylline can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Aminophylline can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Aminophylline can be decreased when it is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Aminophylline can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Aminophylline can be decreased when it is combined with Gabexate.Investigational
GarenoxacinThe metabolism of Aminophylline can be decreased when combined with Garenoxacin.Investigational
GatifloxacinThe metabolism of Aminophylline can be decreased when combined with Gatifloxacin.Approved, Investigational
GeldanamycinThe serum concentration of Aminophylline can be decreased when it is combined with Geldanamycin.Experimental
GemifloxacinThe metabolism of Aminophylline can be decreased when combined with Gemifloxacin.Approved, Investigational
GenisteinThe serum concentration of Aminophylline can be increased when it is combined with Genistein.Investigational
GM6001The serum concentration of Aminophylline can be decreased when it is combined with GM6001.Experimental
GrepafloxacinThe metabolism of Aminophylline can be decreased when combined with Grepafloxacin.Withdrawn
HexestrolThe serum concentration of Aminophylline can be increased when it is combined with Hexestrol.Withdrawn
HexobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Hexobarbital.Approved
HirulogThe serum concentration of Aminophylline can be decreased when it is combined with Hirulog.Experimental
IdelalisibThe serum concentration of Aminophylline can be increased when it is combined with Idelalisib.Approved
idraparinuxThe serum concentration of Aminophylline can be decreased when it is combined with idraparinux.Investigational
IFNaThe metabolism of Aminophylline can be decreased when combined with IFNa.Investigational
ImatinibThe metabolism of Aminophylline can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Aminophylline can be decreased when it is combined with Imidapril.Investigational
IndacaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Indacaterol.Approved
IndinavirThe metabolism of Aminophylline can be decreased when combined with Indinavir.Approved
Interferon Alfa-2a, RecombinantThe metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2a, Recombinant.Approved
Interferon Alfa-2b, RecombinantThe metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.Approved
Interferon alfa-n1The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n1.Approved
Interferon alfa-n3The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n3.Approved, Investigational
Interferon alfacon-1The metabolism of Aminophylline can be decreased when combined with Interferon alfacon-1.Approved
Interferon beta-1aThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1a.Approved, Investigational
Interferon beta-1bThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1b.Approved
Interferon gamma-1bThe metabolism of Aminophylline can be decreased when combined with Interferon gamma-1b.Approved, Investigational
IsavuconazoniumThe metabolism of Aminophylline can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe serum concentration of Aminophylline can be decreased when it is combined with Isoflurophate.Approved, Withdrawn
IsoniazidThe serum concentration of Aminophylline can be increased when it is combined with Isoniazid.Approved
IsoprenalineThe serum concentration of Aminophylline can be decreased when it is combined with Isoprenaline.Approved
IsradipineThe metabolism of Aminophylline can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Aminophylline can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Aminophylline can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Aminophylline can be decreased when it is combined with Ixazomib.Approved
JosamycinThe metabolism of Aminophylline can be decreased when combined with Josamycin.Approved
KetoconazoleThe metabolism of Aminophylline can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe metabolism of Aminophylline can be decreased when combined with Kitasamycin.Experimental
LepirudinThe serum concentration of Aminophylline can be decreased when it is combined with Lepirudin.Approved
LevofloxacinThe metabolism of Aminophylline can be decreased when combined with Levofloxacin.Approved, Investigational
LevothyroxineThe metabolism of Aminophylline can be increased when combined with Levothyroxine.Approved
LidocaineThe metabolism of Aminophylline can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Linagliptin.Approved
LiothyronineThe metabolism of Aminophylline can be increased when combined with Liothyronine.Approved, Vet Approved
LiotrixThe metabolism of Aminophylline can be increased when combined with Liotrix.Approved
LisinoprilThe serum concentration of Aminophylline can be decreased when it is combined with Lisinopril.Approved, Investigational
LithiumThe serum concentration of Lithium can be decreased when it is combined with Aminophylline.Approved
LomefloxacinThe metabolism of Aminophylline can be decreased when combined with Lomefloxacin.Approved
LopinavirThe metabolism of Aminophylline can be decreased when combined with Lopinavir.Approved
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Aminophylline.Approved
LovastatinThe metabolism of Aminophylline can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Aminophylline can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Aminophylline can be increased when combined with Lumacaftor.Approved
MestranolThe serum concentration of Aminophylline can be increased when it is combined with Mestranol.Approved
MethallenestrilThe serum concentration of Aminophylline can be increased when it is combined with Methallenestril.Experimental
MethimazoleThe serum concentration of Aminophylline can be increased when it is combined with Methimazole.Approved
MethohexitalThe serum concentration of Aminophylline can be decreased when it is combined with Methohexital.Approved
MethotrexateThe serum concentration of Aminophylline can be increased when it is combined with Methotrexate.Approved
MethylphenobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Methylphenobarbital.Approved
MetoprololMetoprolol may decrease the bronchodilatory activities of Aminophylline.Approved, Investigational
MexiletineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.Approved
MidazolamThe therapeutic efficacy of Midazolam can be decreased when used in combination with Aminophylline.Approved, Illicit
MifepristoneThe serum concentration of Aminophylline can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Aminophylline can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Aminophylline can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Aminophylline can be decreased when it is combined with Moexipril.Approved
MoxifloxacinThe metabolism of Aminophylline can be decreased when combined with Moxifloxacin.Approved, Investigational
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.Experimental
NadololNadolol may decrease the bronchodilatory activities of Aminophylline.Approved
NafamostatThe serum concentration of Aminophylline can be decreased when it is combined with Nafamostat.Investigational
NafcillinThe serum concentration of Aminophylline can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidThe metabolism of Aminophylline can be decreased when combined with Nalidixic Acid.Approved
Natural alpha interferonThe metabolism of Aminophylline can be decreased when combined with Natural alpha interferon.Approved, Investigational
NCX 4016The serum concentration of Aminophylline can be decreased when it is combined with NCX 4016.Investigational
NebivololNebivolol may decrease the bronchodilatory activities of Aminophylline.Approved, Investigational
NefazodoneThe metabolism of Aminophylline can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Aminophylline can be decreased when combined with Nelfinavir.Approved
NemonoxacinThe metabolism of Aminophylline can be decreased when combined with Nemonoxacin.Investigational
NetazepideThe therapeutic efficacy of Netazepide can be decreased when used in combination with Aminophylline.Investigational
NetupitantThe serum concentration of Aminophylline can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Aminophylline can be increased when combined with Nevirapine.Approved
NicotineThe metabolism of Aminophylline can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Aminophylline can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Aminophylline.Approved
NitroaspirinThe serum concentration of Aminophylline can be decreased when it is combined with Nitroaspirin.Investigational
NorfloxacinThe metabolism of Aminophylline can be decreased when combined with Norfloxacin.Approved
OfloxacinThe metabolism of Aminophylline can be decreased when combined with Ofloxacin.Approved
OlaparibThe metabolism of Aminophylline can be decreased when combined with Olaparib.Approved
OleandomycinThe metabolism of Aminophylline can be decreased when combined with Oleandomycin.Vet Approved
OlodaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Olodaterol.Approved
OmapatrilatThe serum concentration of Aminophylline can be decreased when it is combined with Omapatrilat.Investigational
OsimertinibThe serum concentration of Aminophylline can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Aminophylline can be decreased when it is combined with Otamixaban.Investigational
OxazepamThe therapeutic efficacy of Oxazepam can be decreased when used in combination with Aminophylline.Approved
OxprenololOxprenolol may decrease the bronchodilatory activities of Aminophylline.Approved
PalbociclibThe serum concentration of Aminophylline can be increased when it is combined with Palbociclib.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Aminophylline is combined with Pancuronium.Approved
PazufloxacinThe metabolism of Aminophylline can be decreased when combined with Pazufloxacin.Investigational
PefloxacinThe metabolism of Aminophylline can be decreased when combined with Pefloxacin.Approved
Peginterferon alfa-2aThe metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.Approved
Peginterferon beta-1aThe metabolism of Aminophylline can be decreased when combined with Peginterferon beta-1a.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Aminophylline.Approved, Investigational
PentobarbitalThe metabolism of Aminophylline can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoxifyllineThe serum concentration of Aminophylline can be increased when it is combined with Pentoxifylline.Approved, Investigational
PerindoprilThe serum concentration of Aminophylline can be decreased when it is combined with Perindopril.Approved
Pf 00477736The therapeutic efficacy of Pf 00477736 can be decreased when used in combination with Aminophylline.Investigational
PhenobarbitalThe metabolism of Aminophylline can be increased when combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Aminophylline can be decreased when it is combined with Phosphoramidon.Experimental
PindololPindolol may decrease the bronchodilatory activities of Aminophylline.Approved
PirenzepineThe therapeutic efficacy of Pirenzepine can be decreased when used in combination with Aminophylline.Approved
Polyestradiol phosphateThe serum concentration of Aminophylline can be increased when it is combined with Polyestradiol phosphate.Approved
PosaconazoleThe metabolism of Aminophylline can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrazepamThe therapeutic efficacy of Prazepam can be decreased when used in combination with Aminophylline.Approved, Illicit
PrimidoneThe metabolism of Aminophylline can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Aminophylline can be decreased when it is combined with Prinomastat.Investigational
ProbenecidThe serum concentration of Aminophylline can be increased when it is combined with Probenecid.Approved
PromestrieneThe serum concentration of Aminophylline can be increased when it is combined with Promestriene.Investigational
PropafenoneThe serum concentration of Aminophylline can be increased when it is combined with Propafenone.Approved
PropranololPropranolol may decrease the bronchodilatory activities of Aminophylline.Approved, Investigational
PropylthiouracilThe serum concentration of Aminophylline can be increased when it is combined with Propylthiouracil.Approved
PrulifloxacinThe metabolism of Aminophylline can be decreased when combined with Prulifloxacin.Investigational
QuinaprilThe serum concentration of Aminophylline can be decreased when it is combined with Quinapril.Approved, Investigational
QuinestrolThe serum concentration of Aminophylline can be increased when it is combined with Quinestrol.Approved
QuinineThe serum concentration of Aminophylline can be increased when it is combined with Quinine.Approved
RacecadotrilThe serum concentration of Aminophylline can be decreased when it is combined with Racecadotril.Investigational
RamiprilThe serum concentration of Aminophylline can be decreased when it is combined with Ramipril.Approved
RanolazineThe metabolism of Aminophylline can be decreased when combined with Ranolazine.Approved, Investigational
RegadenosonAminophylline may decrease the vasodilatory activities of Regadenoson.Approved
RemikirenThe serum concentration of Aminophylline can be decreased when it is combined with Remikiren.Approved
RifabutinThe metabolism of Aminophylline can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Aminophylline can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Aminophylline can be increased when combined with Rifapentine.Approved
RiociguatAminophylline may increase the hypotensive activities of Riociguat.Approved
RitonavirThe metabolism of Aminophylline can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Aminophylline can be decreased when it is combined with Rivaroxaban.Approved
RopiniroleThe metabolism of Aminophylline can be decreased when combined with Ropinirole.Approved, Investigational
RosoxacinThe metabolism of Aminophylline can be decreased when combined with Rosoxacin.Approved
S EquolThe serum concentration of Aminophylline can be increased when it is combined with S Equol.Investigational
SaquinavirThe metabolism of Aminophylline can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Saxagliptin.Approved
SecobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Secobarbital.Approved, Vet Approved
SecoisolariciresinolThe serum concentration of Aminophylline can be increased when it is combined with Secoisolariciresinol.Investigational
SildenafilThe metabolism of Aminophylline can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Aminophylline can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Aminophylline can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Sitagliptin.Approved, Investigational
SolithromycinThe metabolism of Aminophylline can be decreased when combined with Solithromycin.Investigational
SotalolSotalol may decrease the bronchodilatory activities of Aminophylline.Approved
SparfloxacinThe metabolism of Aminophylline can be decreased when combined with Sparfloxacin.Approved
SpiraprilThe serum concentration of Aminophylline can be decreased when it is combined with Spirapril.Approved
St. John's WortThe serum concentration of Aminophylline can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Aminophylline can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Aminophylline can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
Synthetic Conjugated Estrogens, AThe serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BThe serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, B.Approved
TelaprevirThe metabolism of Aminophylline can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Aminophylline can be decreased when combined with Telithromycin.Approved
TemafloxacinThe metabolism of Aminophylline can be decreased when combined with Temafloxacin.Withdrawn
TemazepamThe therapeutic efficacy of Temazepam can be decreased when used in combination with Aminophylline.Approved
TemocaprilThe serum concentration of Aminophylline can be decreased when it is combined with Temocapril.Experimental, Investigational
TenofovirThe metabolism of Aminophylline can be decreased when combined with Tenofovir.Approved, Investigational
TeriflunomideThe serum concentration of Aminophylline can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Aminophylline can be decreased when combined with Theophylline.Approved
ThiabendazoleThe metabolism of Aminophylline can be decreased when combined with Thiabendazole.Approved, Vet Approved
ThiamylalThe serum concentration of Aminophylline can be decreased when it is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Aminophylline.Approved, Vet Approved
ThiorphanThe serum concentration of Aminophylline can be decreased when it is combined with Thiorphan.Experimental
Thyroid, porcineThe metabolism of Aminophylline can be increased when combined with Thyroid, porcine.Approved
TiboloneThe serum concentration of Aminophylline can be increased when it is combined with Tibolone.Approved
TiclopidineThe metabolism of Aminophylline can be decreased when combined with Ticlopidine.Approved
TimololTimolol may decrease the bronchodilatory activities of Aminophylline.Approved
TipranavirThe serum concentration of Aminophylline can be decreased when it is combined with Tipranavir.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Aminophylline.Approved
TocilizumabThe serum concentration of Aminophylline can be decreased when it is combined with Tocilizumab.Approved
TrandolaprilThe serum concentration of Aminophylline can be decreased when it is combined with Trandolapril.Approved
TriazolamThe therapeutic efficacy of Triazolam can be decreased when used in combination with Aminophylline.Approved
TroleandomycinThe metabolism of Aminophylline can be decreased when combined with Troleandomycin.Approved
TrovafloxacinThe metabolism of Aminophylline can be decreased when combined with Trovafloxacin.Approved, Withdrawn
TylosinThe metabolism of Aminophylline can be decreased when combined with Tylosin.Vet Approved
UbenimexThe serum concentration of Aminophylline can be decreased when it is combined with Ubenimex.Experimental
UlinastatinThe serum concentration of Aminophylline can be decreased when it is combined with Ulinastatin.Investigational
VemurafenibThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Aminophylline can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Aminophylline can be decreased when combined with Verapamil.Approved
VildagliptinThe serum concentration of Aminophylline can be decreased when it is combined with Vildagliptin.Approved, Investigational
VoriconazoleThe metabolism of Aminophylline can be decreased when combined with Voriconazole.Approved, Investigational
XimelagatranThe serum concentration of Aminophylline can be decreased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
Ym150The serum concentration of Aminophylline can be decreased when it is combined with Ym150.Investigational
ZafirlukastThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.Approved, Investigational
ZeranolThe serum concentration of Aminophylline can be increased when it is combined with Zeranol.Vet Approved
ZiprasidoneThe metabolism of Aminophylline can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Limit caffeine intake.
  • Take with food.
  • Vitamin B6 needs increased, supplement recommended.
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR03DA55R03DB05R03DA05
AHFS Codes
  • 86:16.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.7 KB)
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 releaseOral225 mg
Tablet, extended releaseOral350 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
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

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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23