Aminophylline - DrugBank

ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy

Targets (4)Enzymes (3)

Targets (4)Enzymes (3)Biointeractions (8)

Identification

Name

Aminophylline

Accession Number

DB01223 (APRD00329)

Type

Small Molecule

Groups

Approved

Description

Aminophylline 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

MOL SDF PDB SMILES InChI

Synonyms

Aminophyllin

Somophyllin

Theophylline ethylenediamine

External IDs

Not Available

Product Ingredients

Ingredient	UNII	CAS	InChI Key	Details
Aminophylline dihydrate	C229N9DX94	5897-66-5	FXNJPZOEDHBGEY-UHFFFAOYSA-N	Details

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Aminophylline Inj 25mg/ml	Liquid	25 mg	Intravenous	Abbott	1985-12-31	1997-08-18	Canada
Aminophylline Inj 25mg/ml	Solution	25 mg	Intravenous	Omega Laboratories Ltd	1984-12-31	Not applicable	Canada
Aminophylline Inj 50mg/ml	Solution	50 mg	Intravenous	Omega Laboratories Ltd	1984-12-31	Not applicable	Canada
Aminophylline Injection 50mg/ml	Solution	50 mg	Intravenous	Hospira, Inc.	1981-12-31	2012-08-03	Canada
Aminophylline Tab 0.1gm	Tablet	100 mg	Oral	Lederle Cyanamid Canada Inc.	1951-12-31	2000-08-02	Canada
Aminophylline Tab 100mg	Tablet	97.5 mg	Oral	Stanley Pharmaceuticals, A Division Of Vita Health Products Inc.	1957-12-31	2002-07-31	Canada
Jaa Aminophylline Tab 100mg	Tablet	100 mg	Oral	Jaapharm Canada Inc.	1993-12-31	2016-08-10	Canada
Phyllocontin	Tablet, extended release	225 mg	Oral	Purdue Pharma	1993-12-31	2011-08-04	Canada
Phyllocontin-350	Tablet, extended release	350 mg	Oral	Purdue Pharma	1993-12-31	2011-08-04	Canada

Approved Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Hospira, Inc.	1983-10-26	Not applicable	US
Aminophylline	Tablet	100 mg/1	Oral	West Ward Pharmaceutical	1975-11-26	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	General Injectables & Vaccines	2009-01-01	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Hospira, Inc.	1983-10-26	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Hospira, Inc.	1983-10-26	Not applicable	US
Aminophylline	Tablet	200 mg/1	Oral	West Ward Pharmaceutical	1976-05-28	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Cardinal Health	2011-02-11	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Hospira, Inc.	1983-10-26	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	General Injectables & Vaccines	2010-07-01	Not applicable	US
Aminophylline	Injection, solution	25 mg/mL	Intravenous	Cardinal Health	2011-02-11	Not applicable	US

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International Brands

Name	Company
Minomal	Not Available
Somophyllin	Not Available
Truphylline	Not Available

Brand mixtures

Not Available

Categories

UNII

27Y3KJK423

CAS number

317-34-0

Weight

Average: 420.4264
Monoisotopic: 420.198199306

Chemical Formula

C₁₆H₂₄N₁₀O₄

InChI Key

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

Pharmacology

Indication

For the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.

Structured Indications

Pharmacodynamics

Aminophylline 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 action

Aminophylline 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.

Target	Kind	Pharmacological action	Actions	Organism	UniProt ID
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Protein	yes	inhibitor	Human	Q14432	details
Adenosine receptor A1	Protein	yes	antagonist	Human	P30542	details
Adenosine receptor A3	Protein	yes	antagonist	Human	P0DMS8	details
Histone deacetylase 2	Protein	yes	activator	Human	Q92769	details

Absorption

Not Available

Volume of distribution

0.3 to 0.7 L/kg

Protein binding

60%

Metabolism

Not Available

Route of elimination

Not Available

Half life

7-9 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]

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction	Drug group
1,10-Phenanthroline	The serum concentration of Aminophylline can be decreased when it is combined with 1,10-Phenanthroline.	Experimental
3,4-Dichloroisocoumarin	The serum concentration of Aminophylline can be decreased when it is combined with 3,4-Dichloroisocoumarin.	Experimental
4-(2-Aminoethyl)Benzenesulfonyl Fluoride	The serum concentration of Aminophylline can be decreased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.	Experimental
Abiraterone	The serum concentration of Aminophylline can be increased when it is combined with Abiraterone.	Approved
Acebutolol	Acebutolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Adalimumab	The serum concentration of Aminophylline can be decreased when it is combined with Adalimumab.	Approved
Adenosine	The therapeutic efficacy of Adenosine can be decreased when used in combination with Aminophylline.	Approved, Investigational
Albinterferon Alfa-2B	The metabolism of Aminophylline can be decreased when combined with Albumin-interferon alpha.	Investigational
Allopurinol	The serum concentration of Aminophylline can be increased when it is combined with Allopurinol.	Approved
Alogliptin	The serum concentration of Aminophylline can be decreased when it is combined with Alogliptin.	Approved
Alpha-1-proteinase inhibitor	The serum concentration of Aminophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.	Approved
Alprazolam	The therapeutic efficacy of Alprazolam can be decreased when used in combination with Aminophylline.	Approved, Illicit, Investigational
Alprenolol	Alprenolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Withdrawn
Amiodarone	The metabolism of Aminophylline can be decreased when combined with Amiodarone.	Approved, Investigational
Amobarbital	The serum concentration of Aminophylline can be decreased when it is combined with Amobarbital.	Approved, Illicit
Amprenavir	The serum concentration of Aminophylline can be decreased when it is combined with Amprenavir.	Approved
Antithrombin III human	The serum concentration of Aminophylline can be decreased when it is combined with Antithrombin III human.	Approved
Apixaban	The serum concentration of Aminophylline can be decreased when it is combined with Apixaban.	Approved
Aprepitant	The serum concentration of Aminophylline can be increased when it is combined with Aprepitant.	Approved, Investigational
Aprotinin	The serum concentration of Aminophylline can be decreased when it is combined with Aprotinin.	Approved, Withdrawn
Argatroban	The serum concentration of Aminophylline can be decreased when it is combined with Argatroban.	Approved, Investigational
Atazanavir	The metabolism of Aminophylline can be decreased when combined with Atazanavir.	Approved, Investigational
Atenolol	Atenolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Atomoxetine	The metabolism of Aminophylline can be decreased when combined with Atomoxetine.	Approved
Azithromycin	The metabolism of Aminophylline can be decreased when combined with Azithromycin.	Approved
Barbexaclone	The serum concentration of Aminophylline can be decreased when it is combined with Barbexaclone.	Experimental
Barbital	The serum concentration of Aminophylline can be decreased when it is combined with Barbital.	Illicit
Batimastat	The serum concentration of Aminophylline can be decreased when it is combined with Batimastat.	Experimental
Bazedoxifene	The serum concentration of Aminophylline can be increased when it is combined with Bazedoxifene.	Approved, Investigational
Benazepril	The serum concentration of Aminophylline can be decreased when it is combined with Benazepril.	Approved, Investigational
Benzamidine	The serum concentration of Aminophylline can be decreased when it is combined with Benzamidine.	Experimental
Betaxolol	Betaxolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Bexarotene	The serum concentration of Aminophylline can be decreased when it is combined with Bexarotene.	Approved, Investigational
Bisoprolol	Bisoprolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Bivalirudin	The serum concentration of Aminophylline can be decreased when it is combined with Bivalirudin.	Approved, Investigational
Boceprevir	The metabolism of Aminophylline can be decreased when combined with Boceprevir.	Approved, Investigational
Bopindolol	Bopindolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Bortezomib	The metabolism of Aminophylline can be decreased when combined with Bortezomib.	Approved, Investigational
Bosentan	The serum concentration of Aminophylline can be decreased when it is combined with Bosentan.	Approved, Investigational
Bromazepam	The therapeutic efficacy of Bromazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Bupranolol	Bupranolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Caffeine	The metabolism of Aminophylline can be decreased when combined with Caffeine.	Approved
Camazepam	The therapeutic efficacy of Camazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Candoxatril	The serum concentration of Aminophylline can be decreased when it is combined with Candoxatril.	Experimental
Candoxatrilat	The serum concentration of Aminophylline can be decreased when it is combined with Candoxatrilat.	Experimental
Captopril	The serum concentration of Aminophylline can be decreased when it is combined with Captopril.	Approved
Carbamazepine	The serum concentration of Aminophylline can be decreased when it is combined with Carbamazepine.	Approved, Investigational
Carbimazole	The serum concentration of Aminophylline can be increased when it is combined with Carbimazole.	Approved
Carteolol	Carteolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Celiprolol	Celiprolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Investigational
Ceritinib	The serum concentration of Aminophylline can be increased when it is combined with Ceritinib.	Approved
Chlordiazepoxide	The therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Aminophylline.	Approved, Illicit
Chlorotrianisene	The serum concentration of Aminophylline can be increased when it is combined with Chlorotrianisene.	Withdrawn
Chymostatin	The serum concentration of Aminophylline can be decreased when it is combined with Chymostatin.	Experimental
Cilastatin	The serum concentration of Aminophylline can be decreased when it is combined with Cilastatin.	Approved
Cilazapril	The serum concentration of Aminophylline can be decreased when it is combined with Cilazapril.	Approved
Cimetidine	The metabolism of Aminophylline can be decreased when combined with Cimetidine.	Approved
Cinoxacin	The metabolism of Aminophylline can be decreased when combined with Cinoxacin.	Approved, Withdrawn
Ciprofloxacin	The metabolism of Aminophylline can be decreased when combined with Ciprofloxacin.	Approved, Investigational
Citalopram	The metabolism of Aminophylline can be decreased when combined with Citalopram.	Approved
Clarithromycin	The metabolism of Aminophylline can be decreased when combined with Clarithromycin.	Approved
Clemastine	The metabolism of Aminophylline can be decreased when combined with Clemastine.	Approved
Clonazepam	The therapeutic efficacy of Clonazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Clorazepate	The therapeutic efficacy of Clorazepate can be decreased when used in combination with Aminophylline.	Approved, Illicit
Clotrimazole	The metabolism of Aminophylline can be decreased when combined with Clotrimazole.	Approved, Vet Approved
Cobicistat	The metabolism of Aminophylline can be decreased when combined with Cobicistat.	Approved
Conivaptan	The serum concentration of Aminophylline can be increased when it is combined with Conivaptan.	Approved, Investigational
Conjugated estrogens	The serum concentration of Aminophylline can be increased when it is combined with Conjugated Equine Estrogens.	Approved
Crizotinib	The metabolism of Aminophylline can be decreased when combined with Crizotinib.	Approved
Cyclosporine	The metabolism of Aminophylline can be decreased when combined with Cyclosporine.	Approved, Investigational, Vet Approved
Cyproterone acetate	The serum concentration of Aminophylline can be decreased when it is combined with Cyproterone acetate.	Approved, Investigational
Dabigatran etexilate	The serum concentration of Aminophylline can be decreased when it is combined with Dabigatran etexilate.	Approved
Dabrafenib	The serum concentration of Aminophylline can be decreased when it is combined with Dabrafenib.	Approved
Darexaban	The serum concentration of Aminophylline can be decreased when it is combined with Ym150.	Investigational
Darunavir	The metabolism of Aminophylline can be decreased when combined with Darunavir.	Approved
Dasatinib	The serum concentration of Aminophylline can be increased when it is combined with Dasatinib.	Approved, Investigational
Deferasirox	The serum concentration of Aminophylline can be decreased when it is combined with Deferasirox.	Approved, Investigational
Delavirdine	The metabolism of Aminophylline can be decreased when combined with Delavirdine.	Approved
Delorazepam	The therapeutic efficacy of Delorazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Dexamethasone	The serum concentration of Aminophylline can be decreased when it is combined with Dexamethasone.	Approved, Investigational, Vet Approved
Diazepam	The therapeutic efficacy of Diazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit, Vet Approved
Dienestrol	The serum concentration of Aminophylline can be increased when it is combined with Dienestrol.	Approved
Diethylstilbestrol	The serum concentration of Aminophylline can be increased when it is combined with Diethylstilbestrol.	Approved
Dihydroergotamine	The metabolism of Aminophylline can be decreased when combined with Dihydroergotamine.	Approved
Diltiazem	The metabolism of Aminophylline can be decreased when combined with Diltiazem.	Approved
Disulfiram	The serum concentration of Aminophylline can be increased when it is combined with Disulfiram.	Approved
Doxofylline	The risk or severity of adverse effects can be increased when Aminophylline is combined with Doxofylline.	Approved
Doxycycline	The metabolism of Aminophylline can be decreased when combined with Doxycycline.	Approved, Investigational, Vet Approved
Dronedarone	The metabolism of Aminophylline can be decreased when combined with Dronedarone.	Approved
Ecabet	The serum concentration of Aminophylline can be decreased when it is combined with Ecabet.	Approved, Investigational
Edoxaban	The serum concentration of Aminophylline can be decreased when it is combined with Edoxaban.	Approved
Efavirenz	The serum concentration of Aminophylline can be decreased when it is combined with Efavirenz.	Approved, Investigational
Elafin	The serum concentration of Aminophylline can be decreased when it is combined with Elafin.	Investigational
Enalapril	The serum concentration of Aminophylline can be decreased when it is combined with Enalapril.	Approved, Vet Approved
Enalaprilat	The serum concentration of Aminophylline can be decreased when it is combined with Enalaprilat.	Approved
Enalkiren	The serum concentration of Aminophylline can be decreased when it is combined with Enalkiren.	Experimental
Enoxacin	The metabolism of Aminophylline can be decreased when combined with Enoxacin.	Approved
Enzalutamide	The serum concentration of Aminophylline can be decreased when it is combined with Enzalutamide.	Approved
Equol	The serum concentration of Aminophylline can be increased when it is combined with S Equol.	Investigational
Erythromycin	The metabolism of Aminophylline can be decreased when combined with Erythromycin.	Approved, Vet Approved
Eslicarbazepine acetate	The serum concentration of Aminophylline can be decreased when it is combined with Eslicarbazepine acetate.	Approved
Esmolol	Esmolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Estazolam	The therapeutic efficacy of Estazolam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Estradiol	The serum concentration of Aminophylline can be increased when it is combined with Estradiol.	Approved, Investigational, Vet Approved
Estriol	The serum concentration of Aminophylline can be increased when it is combined with Estriol.	Approved, Vet Approved
Estrone	The serum concentration of Aminophylline can be increased when it is combined with Estrone.	Approved
Ethanol	The serum concentration of Aminophylline can be increased when it is combined with Ethanol.	Approved
Ethinyl Estradiol	The serum concentration of Aminophylline can be increased when it is combined with Ethinyl Estradiol.	Approved
Etizolam	The therapeutic efficacy of Etizolam can be decreased when used in combination with Aminophylline.	Approved
Etravirine	The serum concentration of Aminophylline can be decreased when it is combined with Etravirine.	Approved
Faldaprevir	The serum concentration of Aminophylline can be decreased when it is combined with Bi201335.	Investigational
Febuxostat	The serum concentration of the active metabolites of Aminophylline can be increased when Aminophylline is used in combination with Febuxostat.	Approved
Fleroxacin	The metabolism of Aminophylline can be decreased when combined with Fleroxacin.	Approved
Fluconazole	The metabolism of Aminophylline can be decreased when combined with Fluconazole.	Approved
Fludiazepam	The therapeutic efficacy of Fludiazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Flumazenil	The therapeutic efficacy of Flumazenil can be decreased when used in combination with Aminophylline.	Approved
Flumequine	The metabolism of Aminophylline can be decreased when combined with Flumequine.	Withdrawn
Flunitrazepam	The therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Flurazepam	The therapeutic efficacy of Flurazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Fluvoxamine	The metabolism of Aminophylline can be decreased when combined with Fluvoxamine.	Approved, Investigational
Formoterol	The risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.	Approved, Investigational
Fosamprenavir	The metabolism of Aminophylline can be decreased when combined with Fosamprenavir.	Approved
Fosaprepitant	The serum concentration of Aminophylline can be increased when it is combined with Fosaprepitant.	Approved
Fosinopril	The serum concentration of Aminophylline can be decreased when it is combined with Fosinopril.	Approved
Fosphenytoin	The serum concentration of Aminophylline can be decreased when it is combined with Fosphenytoin.	Approved
Fusidic Acid	The serum concentration of Aminophylline can be increased when it is combined with Fusidic Acid.	Approved
Gabexate	The serum concentration of Aminophylline can be decreased when it is combined with Gabexate.	Investigational
Gatifloxacin	The metabolism of Aminophylline can be decreased when combined with Gatifloxacin.	Approved, Investigational
Geldanamycin	The serum concentration of Aminophylline can be decreased when it is combined with Geldanamycin.	Experimental
Gemifloxacin	The metabolism of Aminophylline can be decreased when combined with Gemifloxacin.	Approved, Investigational
Genistein	The serum concentration of Aminophylline can be increased when it is combined with Genistein.	Investigational
GM6001	The serum concentration of Aminophylline can be decreased when it is combined with GM6001.	Experimental
Grepafloxacin	The metabolism of Aminophylline can be decreased when combined with Grepafloxacin.	Withdrawn
Hexestrol	The serum concentration of Aminophylline can be increased when it is combined with Hexestrol.	Withdrawn
Hexobarbital	The serum concentration of Aminophylline can be decreased when it is combined with Hexobarbital.	Approved
Idelalisib	The serum concentration of Aminophylline can be increased when it is combined with Idelalisib.	Approved
Imatinib	The metabolism of Aminophylline can be decreased when combined with Imatinib.	Approved
Imidapril	The serum concentration of Aminophylline can be decreased when it is combined with Imidapril.	Investigational
Indacaterol	The risk or severity of adverse effects can be increased when Aminophylline is combined with Indacaterol.	Approved
Indinavir	The metabolism of Aminophylline can be decreased when combined with Indinavir.	Approved
Interferon Alfa-2a, Recombinant	The metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2a, Recombinant.	Approved
Interferon Alfa-2b, Recombinant	The metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.	Approved
Interferon alfa-n1	The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n1.	Approved
Interferon alfa-n3	The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n3.	Approved, Investigational
Interferon alfacon-1	The metabolism of Aminophylline can be decreased when combined with Interferon alfacon-1.	Approved
Interferon beta-1a	The metabolism of Aminophylline can be decreased when combined with Interferon beta-1a.	Approved, Investigational
Interferon beta-1b	The metabolism of Aminophylline can be decreased when combined with Interferon beta-1b.	Approved
Interferon gamma-1b	The metabolism of Aminophylline can be decreased when combined with Interferon gamma-1b.	Approved, Investigational
Isavuconazonium	The metabolism of Aminophylline can be decreased when combined with Isavuconazonium.	Approved, Investigational
Isoflurophate	The serum concentration of Aminophylline can be decreased when it is combined with Isoflurophate.	Approved, Withdrawn
Isoniazid	The serum concentration of Aminophylline can be increased when it is combined with Isoniazid.	Approved
Isoprenaline	The serum concentration of Aminophylline can be decreased when it is combined with Isoprenaline.	Approved
Isradipine	The metabolism of Aminophylline can be decreased when combined with Isradipine.	Approved
Itraconazole	The metabolism of Aminophylline can be decreased when combined with Itraconazole.	Approved, Investigational
Ivacaftor	The serum concentration of Aminophylline can be increased when it is combined with Ivacaftor.	Approved
Ixazomib	The serum concentration of Aminophylline can be decreased when it is combined with Ixazomib.	Approved
Josamycin	The metabolism of Aminophylline can be decreased when combined with Josamycin.	Approved
Ketoconazole	The metabolism of Aminophylline can be decreased when combined with Ketoconazole.	Approved, Investigational
Kitasamycin	The metabolism of Aminophylline can be decreased when combined with Kitasamycin.	Experimental
Lepirudin	The serum concentration of Aminophylline can be decreased when it is combined with Lepirudin.	Approved
Levofloxacin	The metabolism of Aminophylline can be decreased when combined with Levofloxacin.	Approved, Investigational
Levothyroxine	The metabolism of Aminophylline can be increased when combined with Levothyroxine.	Approved
Lidocaine	The metabolism of Aminophylline can be decreased when combined with Lidocaine.	Approved, Vet Approved
Linagliptin	The serum concentration of Aminophylline can be decreased when it is combined with Linagliptin.	Approved
Liothyronine	The metabolism of Aminophylline can be increased when combined with Liothyronine.	Approved, Vet Approved
Liotrix	The metabolism of Aminophylline can be increased when combined with Liotrix.	Approved
Lisinopril	The serum concentration of Aminophylline can be decreased when it is combined with Lisinopril.	Approved, Investigational
Lithium	The serum concentration of Lithium can be decreased when it is combined with Aminophylline.	Approved
Lomefloxacin	The metabolism of Aminophylline can be decreased when combined with Lomefloxacin.	Approved
Lopinavir	The metabolism of Aminophylline can be decreased when combined with Lopinavir.	Approved
Lorazepam	The therapeutic efficacy of Lorazepam can be decreased when used in combination with Aminophylline.	Approved
Lovastatin	The metabolism of Aminophylline can be decreased when combined with Lovastatin.	Approved, Investigational
Luliconazole	The serum concentration of Aminophylline can be increased when it is combined with Luliconazole.	Approved
Lumacaftor	The metabolism of Aminophylline can be increased when combined with Lumacaftor.	Approved
Mestranol	The serum concentration of Aminophylline can be increased when it is combined with Mestranol.	Approved
Methallenestril	The serum concentration of Aminophylline can be increased when it is combined with Methallenestril.	Experimental
Methimazole	The serum concentration of Aminophylline can be increased when it is combined with Methimazole.	Approved
Methohexital	The serum concentration of Aminophylline can be decreased when it is combined with Methohexital.	Approved
Methotrexate	The serum concentration of Aminophylline can be increased when it is combined with Methotrexate.	Approved
Methylphenobarbital	The serum concentration of Aminophylline can be decreased when it is combined with Methylphenobarbital.	Approved
Metoprolol	Metoprolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Investigational
Mexiletine	The metabolism of Aminophylline can be decreased when combined with Mexiletine.	Approved
Midazolam	The therapeutic efficacy of Midazolam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Mifepristone	The serum concentration of Aminophylline can be increased when it is combined with Mifepristone.	Approved, Investigational
Mitotane	The serum concentration of Aminophylline can be decreased when it is combined with Mitotane.	Approved
Modafinil	The serum concentration of Aminophylline can be decreased when it is combined with Modafinil.	Approved, Investigational
Moexipril	The serum concentration of Aminophylline can be decreased when it is combined with Moexipril.	Approved
Moxifloxacin	The metabolism of Aminophylline can be decreased when combined with Moxifloxacin.	Approved, Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline	The serum concentration of Aminophylline can be decreased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.	Experimental
Nadolol	Nadolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Nafamostat	The serum concentration of Aminophylline can be decreased when it is combined with Nafamostat.	Approved, Investigational
Nafcillin	The serum concentration of Aminophylline can be decreased when it is combined with Nafcillin.	Approved
Nalidixic Acid	The metabolism of Aminophylline can be decreased when combined with Nalidixic Acid.	Approved
Natural alpha interferon	The metabolism of Aminophylline can be decreased when combined with Natural alpha interferon.	Approved, Investigational
NCX 4016	The serum concentration of Aminophylline can be decreased when it is combined with NCX 4016.	Investigational
Nebivolol	Nebivolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Investigational
Nefazodone	The metabolism of Aminophylline can be decreased when combined with Nefazodone.	Approved, Withdrawn
Nelfinavir	The metabolism of Aminophylline can be decreased when combined with Nelfinavir.	Approved
Netazepide	The therapeutic efficacy of Netazepide can be decreased when used in combination with Aminophylline.	Investigational
Netupitant	The serum concentration of Aminophylline can be increased when it is combined with Netupitant.	Approved
Nevirapine	The metabolism of Aminophylline can be increased when combined with Nevirapine.	Approved
Nicotine	The metabolism of Aminophylline can be decreased when combined with Nicotine.	Approved
Nilotinib	The metabolism of Aminophylline can be decreased when combined with Nilotinib.	Approved, Investigational
Nitrazepam	The therapeutic efficacy of Nitrazepam can be decreased when used in combination with Aminophylline.	Approved
Nitroaspirin	The serum concentration of Aminophylline can be decreased when it is combined with Nitroaspirin.	Investigational
Norfloxacin	The metabolism of Aminophylline can be decreased when combined with Norfloxacin.	Approved
Ofloxacin	The metabolism of Aminophylline can be decreased when combined with Ofloxacin.	Approved
Olaparib	The metabolism of Aminophylline can be decreased when combined with Olaparib.	Approved
Olodaterol	The risk or severity of adverse effects can be increased when Aminophylline is combined with Olodaterol.	Approved
Omapatrilat	The serum concentration of Aminophylline can be decreased when it is combined with Omapatrilat.	Investigational
Osimertinib	The serum concentration of Aminophylline can be increased when it is combined with Osimertinib.	Approved
Oxazepam	The therapeutic efficacy of Oxazepam can be decreased when used in combination with Aminophylline.	Approved
Oxprenolol	Oxprenolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Palbociclib	The serum concentration of Aminophylline can be increased when it is combined with Palbociclib.	Approved
Pancuronium	The risk or severity of adverse effects can be increased when Aminophylline is combined with Pancuronium.	Approved
Pazufloxacin	The metabolism of Aminophylline can be decreased when combined with Pazufloxacin.	Investigational
Pefloxacin	The metabolism of Aminophylline can be decreased when combined with Pefloxacin.	Approved
Peginterferon alfa-2a	The metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.	Approved, Investigational
Peginterferon alfa-2b	The serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.	Approved
Peginterferon beta-1a	The metabolism of Aminophylline can be decreased when combined with Peginterferon beta-1a.	Approved
Penbutolol	Penbutolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Investigational
Pentobarbital	The metabolism of Aminophylline can be increased when combined with Pentobarbital.	Approved, Vet Approved
Pentoxifylline	The serum concentration of Aminophylline can be increased when it is combined with Pentoxifylline.	Approved, Investigational
Perindopril	The serum concentration of Aminophylline can be decreased when it is combined with Perindopril.	Approved
PF-477736	The therapeutic efficacy of Pf 00477736 can be decreased when used in combination with Aminophylline.	Investigational
Phenobarbital	The metabolism of Aminophylline can be increased when combined with Phenobarbital.	Approved
Phenytoin	The serum concentration of Aminophylline can be decreased when it is combined with Phenytoin.	Approved, Vet Approved
Phosphoramidon	The serum concentration of Aminophylline can be decreased when it is combined with Phosphoramidon.	Experimental
Pindolol	Pindolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Pirenzepine	The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Aminophylline.	Approved
Posaconazole	The metabolism of Aminophylline can be decreased when combined with Posaconazole.	Approved, Investigational, Vet Approved
Prazepam	The therapeutic efficacy of Prazepam can be decreased when used in combination with Aminophylline.	Approved, Illicit
Primidone	The metabolism of Aminophylline can be increased when combined with Primidone.	Approved, Vet Approved
Prinomastat	The serum concentration of Aminophylline can be decreased when it is combined with Prinomastat.	Investigational
Probenecid	The serum concentration of Aminophylline can be increased when it is combined with Probenecid.	Approved
Promestriene	The serum concentration of Aminophylline can be increased when it is combined with Promestriene.	Investigational
Propafenone	The serum concentration of Aminophylline can be increased when it is combined with Propafenone.	Approved
Propranolol	Propranolol may decrease the bronchodilatory activities of Aminophylline.	Approved, Investigational
Propylthiouracil	The serum concentration of Aminophylline can be increased when it is combined with Propylthiouracil.	Approved
Prulifloxacin	The metabolism of Aminophylline can be decreased when combined with Prulifloxacin.	Investigational
Quinapril	The serum concentration of Aminophylline can be decreased when it is combined with Quinapril.	Approved, Investigational
Quinestrol	The serum concentration of Aminophylline can be increased when it is combined with Quinestrol.	Approved
Quinine	The serum concentration of Aminophylline can be increased when it is combined with Quinine.	Approved
Racecadotril	The serum concentration of Aminophylline can be decreased when it is combined with Racecadotril.	Investigational
Ramipril	The serum concentration of Aminophylline can be decreased when it is combined with Ramipril.	Approved
Ranolazine	The metabolism of Aminophylline can be decreased when combined with Ranolazine.	Approved, Investigational
Regadenoson	Aminophylline may decrease the vasodilatory activities of Regadenoson.	Approved
Remikiren	The serum concentration of Aminophylline can be decreased when it is combined with Remikiren.	Approved
Rifabutin	The metabolism of Aminophylline can be increased when combined with Rifabutin.	Approved
Rifampicin	The metabolism of Aminophylline can be increased when combined with Rifampicin.	Approved
Rifapentine	The metabolism of Aminophylline can be increased when combined with Rifapentine.	Approved
Riociguat	Aminophylline may increase the hypotensive activities of Riociguat.	Approved
Ritonavir	The metabolism of Aminophylline can be decreased when combined with Ritonavir.	Approved, Investigational
Rivaroxaban	The serum concentration of Aminophylline can be decreased when it is combined with Rivaroxaban.	Approved
Ropinirole	The metabolism of Aminophylline can be decreased when combined with Ropinirole.	Approved, Investigational
Rosoxacin	The metabolism of Aminophylline can be decreased when combined with Rosoxacin.	Approved
Saquinavir	The metabolism of Aminophylline can be decreased when combined with Saquinavir.	Approved, Investigational
Saxagliptin	The serum concentration of Aminophylline can be decreased when it is combined with Saxagliptin.	Approved
Secobarbital	The serum concentration of Aminophylline can be decreased when it is combined with Secobarbital.	Approved, Vet Approved
Secoisolariciresinol	The serum concentration of Aminophylline can be increased when it is combined with Secoisolariciresinol.	Investigational
Sildenafil	The metabolism of Aminophylline can be decreased when combined with Sildenafil.	Approved, Investigational
Siltuximab	The serum concentration of Aminophylline can be decreased when it is combined with Siltuximab.	Approved
Simeprevir	The serum concentration of Aminophylline can be increased when it is combined with Simeprevir.	Approved
Sitagliptin	The serum concentration of Aminophylline can be decreased when it is combined with Sitagliptin.	Approved, Investigational
Solithromycin	The metabolism of Aminophylline can be decreased when combined with Solithromycin.	Investigational
Sotalol	Sotalol may decrease the bronchodilatory activities of Aminophylline.	Approved
Sparfloxacin	The metabolism of Aminophylline can be decreased when combined with Sparfloxacin.	Approved
Spirapril	The serum concentration of Aminophylline can be decreased when it is combined with Spirapril.	Approved
St. John's Wort	The serum concentration of Aminophylline can be decreased when it is combined with St. John's Wort.	Nutraceutical
Stiripentol	The serum concentration of Aminophylline can be increased when it is combined with Stiripentol.	Approved
Sulfisoxazole	The metabolism of Aminophylline can be decreased when combined with Sulfisoxazole.	Approved, Vet Approved
Synthetic Conjugated Estrogens, A	The serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, A.	Approved
Synthetic Conjugated Estrogens, B	The serum concentration of Aminophylline can be increased when it is combined with Synthetic Conjugated Estrogens, B.	Approved
Telaprevir	The metabolism of Aminophylline can be decreased when combined with Telaprevir.	Withdrawn
Telithromycin	The metabolism of Aminophylline can be decreased when combined with Telithromycin.	Approved
Temafloxacin	The metabolism of Aminophylline can be decreased when combined with Temafloxacin.	Withdrawn
Temazepam	The therapeutic efficacy of Temazepam can be decreased when used in combination with Aminophylline.	Approved
Temocapril	The serum concentration of Aminophylline can be decreased when it is combined with Temocapril.	Experimental, Investigational
Tenofovir disoproxil	The metabolism of Aminophylline can be decreased when combined with Tenofovir.	Approved, Investigational
Teriflunomide	The serum concentration of Aminophylline can be decreased when it is combined with Teriflunomide.	Approved
Theophylline	The metabolism of Aminophylline can be decreased when combined with Theophylline.	Approved
Thiabendazole	The metabolism of Aminophylline can be decreased when combined with Thiabendazole.	Approved, Vet Approved
Thiamylal	The serum concentration of Aminophylline can be decreased when it is combined with Thiamylal.	Approved, Vet Approved
Thiopental	The therapeutic efficacy of Thiopental can be decreased when used in combination with Aminophylline.	Approved, Vet Approved
Thiorphan	The serum concentration of Aminophylline can be decreased when it is combined with Thiorphan.	Experimental
Thyroid, porcine	The metabolism of Aminophylline can be increased when combined with Thyroid, porcine.	Approved
Tibolone	The serum concentration of Aminophylline can be increased when it is combined with Tibolone.	Approved
Ticlopidine	The metabolism of Aminophylline can be decreased when combined with Ticlopidine.	Approved
Timolol	Timolol may decrease the bronchodilatory activities of Aminophylline.	Approved
Tipranavir	The serum concentration of Aminophylline can be decreased when it is combined with Tipranavir.	Approved, Investigational
Tizanidine	The serum concentration of Tizanidine can be increased when it is combined with Aminophylline.	Approved
Tocilizumab	The serum concentration of Aminophylline can be decreased when it is combined with Tocilizumab.	Approved
Trandolapril	The serum concentration of Aminophylline can be decreased when it is combined with Trandolapril.	Approved
Triazolam	The therapeutic efficacy of Triazolam can be decreased when used in combination with Aminophylline.	Approved
Trovafloxacin	The metabolism of Aminophylline can be decreased when combined with Trovafloxacin.	Approved, Withdrawn
Ubenimex	The serum concentration of Aminophylline can be decreased when it is combined with Ubenimex.	Experimental
Ulinastatin	The serum concentration of Aminophylline can be decreased when it is combined with Ulinastatin.	Investigational
Vemurafenib	The serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.	Approved
Venlafaxine	The metabolism of Aminophylline can be decreased when combined with Venlafaxine.	Approved
Verapamil	The metabolism of Aminophylline can be decreased when combined with Verapamil.	Approved
Vildagliptin	The serum concentration of Aminophylline can be decreased when it is combined with Vildagliptin.	Approved, Investigational
Voriconazole	The metabolism of Aminophylline can be decreased when combined with Voriconazole.	Approved, Investigational
Ximelagatran	The serum concentration of Aminophylline can be decreased when it is combined with Ximelagatran.	Approved, Investigational, Withdrawn
Zafirlukast	The serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.	Approved, Investigational
Ziprasidone	The 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 Reference

Not Available

General References

Not Available

External Links

Resource	Link
Human Metabolome Database (HMDB)	HMDB15354
KEGG Drug	D00227
PubChem Compound	9433
PubChem Substance	46508784
ChemSpider	9062
ChEBI	2659
ChEMBL	CHEMBL1370561
Therapeutic Targets Database	DAP000613
PharmGKB	PA164781029
Drug Product Database	9963
Drugs.com	http://www.drugs.com/cdi/aminophylline.html
Wikipedia	Aminophylline

ATC Codes

R03DA20 — Combinations of xanthines

R03DA55 — Aminophylline, combinations

R03DB05 — Aminophylline and adrenergics

R03DA05 — Aminophylline

AHFS Codes

86:16.00

PDB Entries

Not Available

FDA label

Not Available

MSDS

Download (72.7 KB)

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Completed	Not Available	Bladder Cancers	1
0	Not Yet Recruiting	Treatment	Acute Kidney Injury (AKI)	1
1	Completed	Basic Science	Mountain Sickness	1
1	Completed	Treatment	Acute Mountain Sickness and Fatigue	1
1	Completed	Treatment	High Altitude Pulmonary Hypertension	1
1, 2	Completed	Prevention	Physiological Function in Low Oxygen Environment	1
2	Completed	Treatment	Anaesthesia	1
2	Completed	Treatment	Cardiac Arrest	1
3	Completed	Treatment	Asthma Bronchial	1
3	Completed	Treatment	Post-Dural Puncture Headache	1
4	Completed	Prevention	Acute Kidney Injury (AKI)	1
4	Completed	Prevention	Patients Being Assessed With Nuclear Stress Testing of the Heart Using the Stress Agent Regadenoson (Lexiscan ®)	1
4	Completed	Prevention	Patients With Severe Chronic Kidney Disease Being Evaluated With Nuclear Stress Testing of the Heart Using the Stress Agent Regadenoson (Lexiscan ®)	1
4	Suspended	Diagnostic	Coronary Artery Disease	1
4	Terminated	Not Available	Asthma Bronchial	1
Not Available	Completed	Treatment	Acute Kidney Injury (AKI)	1
Not Available	Unknown Status	Basic Science	Venoarteriolar Reflex	1
Not Available	Unknown Status	Treatment	Function of Renal Transplant	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Amend
C.O. Truxton Inc.
Cardinal Health
Carlisle Laboratories Inc.
Dispensing Solutions
G & W Labs
General Injectables and Vaccines Inc.
Hospira Inc.
Kaiser Foundation Hospital
Lake Erie Medical and Surgical Supply
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
PCA LLC
Pharmedix
Prescript Pharmaceuticals
West-Ward Pharmaceuticals

Dosage forms

Form	Route	Strength
Injection, solution	Intravenous	25 mg/mL
Tablet	Oral	100 mg/1
Tablet	Oral	200 mg/1
Liquid	Intravenous	25 mg
Solution	Intravenous	25 mg
Solution	Intravenous	50 mg
Tablet	Oral	100 mg
Tablet	Oral	97.5 mg
Tablet, extended release	Oral	225 mg
Tablet, extended release	Oral	350 mg

Prices

Unit description	Cost	Unit
Aminophylline 250 mg/10 ml vial	0.48USD	ml
Aminophylline 25 mg/ml	0.41USD	ml
Phyllocontin-350 350 mg Sustained-Release Tablet	0.31USD	tablet
Aminophylline 100 mg tablet	0.26USD	tablet
Phyllocontin 225 mg Sustained-Release Tablet	0.24USD	tablet
Aminophylline powder	0.17USD	g
Aminophylline 200 mg tablet	0.15USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	2E+005 mg/L	MERCK INDEX (1996)
logP	-3.03	Not Available

Predicted Properties

Property	Value	Source
logP	-0.77	ChemAxon
pKa (Strongest Acidic)	7.82	ChemAxon
pKa (Strongest Basic)	-0.78	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	3	ChemAxon
Hydrogen Donor Count	1	ChemAxon
Polar Surface Area	69.3 Å²	ChemAxon
Rotatable Bond Count	1	ChemAxon
Refractivity	44.93 m³·mol^-1	ChemAxon
Polarizability	16.86 Å³	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9778
Blood Brain Barrier	+	0.5908
Caco-2 permeable	-	0.6802
P-glycoprotein substrate	Substrate	0.7341
P-glycoprotein inhibitor I	Non-inhibitor	0.9164
P-glycoprotein inhibitor II	Non-inhibitor	0.9673
Renal organic cation transporter	Non-inhibitor	0.7935
CYP450 2C9 substrate	Non-substrate	0.8073
CYP450 2D6 substrate	Non-substrate	0.8093
CYP450 3A4 substrate	Substrate	0.5482
CYP450 1A2 substrate	Non-inhibitor	0.8726
CYP450 2C9 inhibitor	Non-inhibitor	0.9332
CYP450 2D6 inhibitor	Non-inhibitor	0.9633
CYP450 2C19 inhibitor	Non-inhibitor	0.9184
CYP450 3A4 inhibitor	Non-inhibitor	0.8031
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.8858
Ames test	Non AMES toxic	0.6724
Carcinogenicity	Non-carcinogens	0.8696
Biodegradation	Not ready biodegradable	0.9149
Rat acute toxicity	2.4979 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.7876
hERG inhibition (predictor II)	Inhibitor	0.6143

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum Type	Description	Splash Key
LC-MS/MS	LC-MS/MS Spectrum - , positive	splash10-001i-1900000000-f6d60952fa154f363515	View in MoNA
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Negative	Not Available

Taxonomy

Description

This compound belongs to the class of chemical entities known as monoalkylamines. These are organic compounds containing an primary aliphatic amine group.

Kingdom

Chemical entities

Super Class

Organic compounds

Class

Organic nitrogen compounds

Sub Class

Organonitrogen compounds

Direct Parent

Monoalkylamines

Alternative Parents

Organopnictogen compounds / Hydrocarbon derivatives

Substituents

Organopnictogen compound / Hydrocarbon derivative / Primary aliphatic amine / Aromatic heteropolycyclic compound

Molecular Framework

Not Available

External Descriptors

Not Available

Targets

Details

1. cGMP-inhibited 3',5'-cyclic phosphodiesterase A

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

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 ]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Details

2. Adenosine receptor A1

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

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 ]
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 ]

Details

3. Adenosine receptor A3

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

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 ]

Details

4. Histone deacetylase 2

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

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

Details

1. Cytochrome P450 1A2

Kind: Protein
Organism: Human
Pharmacological action: unknown
Actions: substrateinhibitor

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

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 ]

Details

2. Cytochrome P450 2E1

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

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 ]

Details

3. Cytochrome P450 3A4

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

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 ]

Drug created on June 13, 2005 07:24 / Updated on July 18, 2017 16:57

Get DrugBank to go!

Structure for DB01223 (Aminophylline)

Targets

References

References

References

References

Enzymes

References

References

References