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Identification
NameAminophylline
Accession NumberDB01223  (APRD00329)
TypeSmall Molecule
GroupsApproved
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
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.1993-12-31Not applicableCanada
Phyllocontintablet (extended-release)225 mgoralPurdue Pharma1993-12-312011-08-04Canada
Phyllocontin-350tablet (extended-release)350 mgoralPurdue Pharma1993-12-312011-08-04Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aminophyllinetablet100 mg/1oralWest ward Pharmaceutical Corp1975-11-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousGeneral Injectables & Vaccines, Inc2010-07-01Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousHospira, Inc.1983-10-26Not 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/mLintravenousCardinal Health2011-02-11Not applicableUs
Aminophyllinetablet200 mg/1oralWest ward Pharmaceutical Corp1976-05-28Not applicableUs
Aminophyllineinjection, solution25 mg/mLintravenousGeneral Injectables & Vaccines, Inc.2009-01-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MinomalNot Available
SomophyllinNot Available
TruphyllineNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Aminophylline dihydrate
ThumbNot applicableDBSALT001739
Categories
UNII27Y3KJK423
CAS number317-34-0
WeightAverage: 420.4264
Monoisotopic: 420.198199306
Chemical FormulaC16H24N10O4
InChI KeyInChIKey=FQPFAHBPWDRTLU-UHFFFAOYSA-N
InChI
InChI=1S/2C7H8N4O2.C2H8N2/c2*1-10-5-4(8-3-9-5)6(12)11(2)7(10)13;3-1-2-4/h2*3H,1-2H3,(H,8,9);1-4H2
IUPAC Name
bis(1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione); ethane-1,2-diamine
SMILES
NCCN.CN1C2=C(NC=N2)C(=O)N(C)C1=O.CN1C2=C(NC=N2)C(=O)N(C)C1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alkaloids and derivatives. These are naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and more rarely other elements such as chlorine, bromine, and phosphorus.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassNot Available
Sub ClassNot Available
Direct ParentAlkaloids and derivatives
Alternative Parents
Substituents
  • Alkaloid or derivatives
  • Xanthine
  • Purinone
  • 6-oxopurine
  • Purine
  • Imidazopyrimidine
  • Pyrimidone
  • Pyrimidine
  • Heteroaromatic compound
  • Vinylogous amide
  • Imidazole
  • Azole
  • Urea
  • Lactam
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
PharmacodynamicsAminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion.
Mechanism of actionAminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 0.3 to 0.7 L/kg
Protein binding60%
MetabolismNot Available
Route of eliminationNot Available
Half life7-9 hours
Clearance
  • 0.29 mL/kg/min [postnatal age 3-15 days]
  • 0.64 mL/kg/min [postnatal age 25-57 days]
  • 1.7 mL/kg/min [ 1-4 years]
  • 1.6 mL/kg/min [4-12 years]
  • 0.9 mL/kg/min [13-15 years]
  • 1.4 mL/kg/min [16-17 years]
  • 0.65 mL/kg/min [Adults (16-60 years), non-smoking asthmatics]
  • 0.41 mL/kg/min [Elderly (>60 years). liver, and renal function]
  • 0.33 mL/kg/min [Acute pulmonary edema]
  • 0.54 mL/kg/min [COPD→60 years, stable non-smoker >1 year]
  • 0.48 mL/kg/min [COPD with cor pulmonale]
  • 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
  • 0.31 mL/kg/min [Liver disease -cholestasis]
  • 0.35 mL/kg/min [cirrhosis]
  • 0.65 mL/kg/min [acute hepatitis]
  • 0.47 mL/kg/min [Sepsis with multi-organ failure]
  • 0.38 mL/kg/min [hypothyroid]
  • 0.8 mL/kg/min [hyperthyroid]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9778
Blood Brain Barrier+0.5908
Caco-2 permeable-0.6802
P-glycoprotein substrateSubstrate0.7341
P-glycoprotein inhibitor INon-inhibitor0.9164
P-glycoprotein inhibitor IINon-inhibitor0.9673
Renal organic cation transporterNon-inhibitor0.7935
CYP450 2C9 substrateNon-substrate0.8073
CYP450 2D6 substrateNon-substrate0.8093
CYP450 3A4 substrateSubstrate0.5482
CYP450 1A2 substrateNon-inhibitor0.8726
CYP450 2C9 inhibitorNon-inhibitor0.9332
CYP450 2D6 inhibitorNon-inhibitor0.9633
CYP450 2C19 inhibitorNon-inhibitor0.9184
CYP450 3A4 inhibitorNon-inhibitor0.8031
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8858
Ames testNon AMES toxic0.6724
CarcinogenicityNon-carcinogens0.8696
BiodegradationNot ready biodegradable0.9149
Rat acute toxicity2.4979 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7876
hERG inhibition (predictor II)Inhibitor0.6143
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous25 mg/mL
Tabletoral100 mg/1
Tabletoral200 mg/1
Solutionintravenous50 mg
Solutionintravenous25 mg
Tabletoral97.5 mg
Tabletoral100 mg
Tablet (extended-release)oral225 mg
Tablet (extended-release)oral350 mg
Prices
Unit descriptionCostUnit
Aminophylline 250 mg/10 ml vial0.48USD ml
Aminophylline 25 mg/ml0.41USD ml
Phyllocontin-350 350 mg Sustained-Release Tablet0.31USD tablet
Aminophylline 100 mg tablet0.26USD tablet
Phyllocontin 225 mg Sustained-Release Tablet0.24USD tablet
Aminophylline powder0.17USD g
Aminophylline 200 mg tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility2E+005 mg/LMERCK INDEX (1996)
logP-3.03Not Available
Predicted Properties
PropertyValueSource
logP-0.77ChemAxon
pKa (Strongest Acidic)7.82ChemAxon
pKa (Strongest Basic)-0.78ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area69.3 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity44.93 m3·mol-1ChemAxon
Polarizability16.86 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR03DA05R03DA55R03DB05
AHFS Codes
  • 86:16.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.7 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Aminophylline can be increased when it is combined with Abiraterone.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Aminophylline.
AdalimumabThe serum concentration of Aminophylline can be decreased when it is combined with Adalimumab.
AdenosineThe therapeutic efficacy of Adenosine can be decreased when used in combination with Aminophylline.
AllopurinolThe serum concentration of Aminophylline can be increased when it is combined with Allopurinol.
AlprazolamThe therapeutic efficacy of Alprazolam can be decreased when used in combination with Aminophylline.
AmphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Aminophylline.
AprepitantThe serum concentration of Aminophylline can be increased when it is combined with Aprepitant.
AtomoxetineAtomoxetine may increase the hypertensive activities of Aminophylline.
BatimastatThe serum concentration of Aminophylline can be decreased when it is combined with Batimastat.
BenzphetamineThe risk or severity of adverse effects can be increased when Benzphetamine is combined with Aminophylline.
BexaroteneThe serum concentration of Aminophylline can be decreased when it is combined with Bexarotene.
BortezomibThe metabolism of Aminophylline can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Aminophylline can be decreased when it is combined with Bosentan.
BromazepamThe therapeutic efficacy of Bromazepam can be decreased when used in combination with Aminophylline.
ButabarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Butabarbital.
ButethalThe serum concentration of Aminophylline can be decreased when it is combined with Butethal.
CalcidiolThe serum concentration of Aminophylline can be increased when it is combined with Calcidiol.
CalcitriolThe serum concentration of Aminophylline can be increased when it is combined with Calcitriol.
CamazepamThe therapeutic efficacy of Camazepam can be decreased when used in combination with Aminophylline.
CarbamazepineThe serum concentration of Aminophylline can be decreased when it is combined with Carbamazepine.
CarbimazoleThe serum concentration of Aminophylline can be increased when it is combined with Carbimazole.
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Aminophylline.
ChlormezanoneThe therapeutic efficacy of Chlormezanone can be decreased when used in combination with Aminophylline.
ChlorotrianiseneThe serum concentration of Aminophylline can be increased when it is combined with Chlorotrianisene.
ChlorphentermineThe risk or severity of adverse effects can be increased when Chlorphentermine is combined with Aminophylline.
CholecalciferolThe serum concentration of Aminophylline can be increased when it is combined with Cholecalciferol.
CimetidineThe metabolism of Aminophylline can be decreased when combined with Cimetidine.
CinolazepamThe therapeutic efficacy of Cinolazepam can be decreased when used in combination with Aminophylline.
ClarithromycinThe metabolism of Aminophylline can be decreased when combined with Clarithromycin.
ClenbuterolThe risk or severity of adverse effects can be increased when Clenbuterol is combined with Aminophylline.
ClobazamThe therapeutic efficacy of Clobazam can be decreased when used in combination with Aminophylline.
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Aminophylline.
ClotiazepamThe therapeutic efficacy of Clotiazepam can be decreased when used in combination with Aminophylline.
CloxazolamThe therapeutic efficacy of Cloxazolam can be decreased when used in combination with Aminophylline.
ConivaptanThe serum concentration of Aminophylline can be increased when it is combined with Conivaptan.
Cyproterone acetateThe serum concentration of Aminophylline can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Aminophylline can be decreased when it is combined with Dabrafenib.
DasatinibThe serum concentration of Aminophylline can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Aminophylline can be decreased when it is combined with Deferasirox.
DihydrotachysterolThe serum concentration of Aminophylline can be increased when it is combined with Dihydrotachysterol.
DisulfiramThe serum concentration of Aminophylline can be increased when it is combined with Disulfiram.
DobutamineThe risk or severity of adverse effects can be increased when Dobutamine is combined with Aminophylline.
DopamineThe risk or severity of adverse effects can be increased when Dopamine is combined with Aminophylline.
DoxofyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Doxofylline.
DronabinolDronabinol may increase the tachycardic activities of Aminophylline.
EpinephrineThe risk or severity of adverse effects can be increased when Epinephrine is combined with Aminophylline.
ErgocalciferolThe serum concentration of Aminophylline can be increased when it is combined with Ergocalciferol.
EsmololEsmolol may decrease the activities of Aminophylline.
EthanolThe serum concentration of Aminophylline can be increased when it is combined with Ethanol.
FebuxostatThe serum concentration of the active metabolites of Aminophylline can be increased when Aminophylline is used in combination with Febuxostat.
FenoterolThe risk or severity of adverse effects can be increased when Fenoterol is combined with Aminophylline.
FluconazoleThe metabolism of Aminophylline can be decreased when combined with Fluconazole.
FludiazepamThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Aminophylline.
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Aminophylline.
FluvoxamineThe metabolism of Aminophylline can be decreased when combined with Fluvoxamine.
FormoterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.
FosaprepitantThe serum concentration of Aminophylline can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Aminophylline can be increased when it is combined with Fusidic Acid.
HalazepamThe therapeutic efficacy of Halazepam can be decreased when used in combination with Aminophylline.
HeptabarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Heptabarbital.
HexobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Hexobarbital.
IdelalisibThe serum concentration of Aminophylline can be increased when it is combined with Idelalisib.
IndacaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Indacaterol.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Aminophylline.
IsoflurophateThe serum concentration of Aminophylline can be decreased when it is combined with Isoflurophate.
IsoniazidThe serum concentration of Aminophylline can be increased when it is combined with Isoniazid.
IsoprenalineThe serum concentration of Aminophylline can be decreased when it is combined with Isoprenaline.
IvacaftorThe serum concentration of Aminophylline can be increased when it is combined with Ivacaftor.
KetazolamThe therapeutic efficacy of Ketazolam can be decreased when used in combination with Aminophylline.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Aminophylline.
LinezolidLinezolid may increase the hypertensive activities of Aminophylline.
LiothyronineThe metabolism of Aminophylline can be increased when combined with Liothyronine.
LithiumThe serum concentration of Lithium can be decreased when it is combined with Aminophylline.
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Aminophylline.
LuliconazoleThe serum concentration of Aminophylline can be increased when it is combined with Luliconazole.
MephentermineThe risk or severity of adverse effects can be increased when Mephentermine is combined with Aminophylline.
MetaraminolThe risk or severity of adverse effects can be increased when Metaraminol is combined with Aminophylline.
MethamphetamineThe risk or severity of adverse effects can be increased when Methamphetamine is combined with Aminophylline.
MethimazoleThe serum concentration of Aminophylline can be increased when it is combined with Methimazole.
MethohexitalThe serum concentration of Aminophylline can be decreased when it is combined with Methohexital.
MethotrexateThe serum concentration of Aminophylline can be increased when it is combined with Methotrexate.
MethoxamineThe risk or severity of adverse effects can be increased when Methoxamine is combined with Aminophylline.
MexiletineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.
MidodrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Aminophylline.
MifepristoneThe serum concentration of Aminophylline can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Aminophylline can be decreased when it is combined with Mitotane.
NadololNadolol may decrease the activities of Aminophylline.
NaphazolineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Aminophylline.
NelfinavirThe metabolism of Aminophylline can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Aminophylline can be increased when it is combined with Netupitant.
NorepinephrineThe risk or severity of adverse effects can be increased when Norepinephrine is combined with Aminophylline.
OlodaterolThe risk or severity of adverse effects can be increased when Aminophylline is combined with Olodaterol.
OrciprenalineThe risk or severity of adverse effects can be increased when Orciprenaline is combined with Aminophylline.
OxymetazolineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with Aminophylline.
PalbociclibThe serum concentration of Aminophylline can be increased when it is combined with Palbociclib.
PancuroniumThe risk or severity of adverse effects can be increased when Aminophylline is combined with Pancuronium.
Peginterferon alfa-2aThe metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.
Peginterferon alfa-2bThe serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Pentobarbital.
PentoxifyllineThe serum concentration of Aminophylline can be increased when it is combined with Pentoxifylline.
PhenmetrazineThe risk or severity of adverse effects can be increased when Phenmetrazine is combined with Aminophylline.
PhentermineThe risk or severity of adverse effects can be increased when Phentermine is combined with Aminophylline.
PhenylephrineThe risk or severity of adverse effects can be increased when Phenylephrine is combined with Aminophylline.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Aminophylline.
PhenytoinThe serum concentration of Aminophylline can be decreased when it is combined with Phenytoin.
PrimidoneThe serum concentration of Aminophylline can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Aminophylline can be increased when it is combined with Propafenone.
PropylthiouracilThe serum concentration of Aminophylline can be increased when it is combined with Propylthiouracil.
QuazepamThe therapeutic efficacy of Quazepam can be decreased when used in combination with Aminophylline.
QuinineThe serum concentration of Aminophylline can be increased when it is combined with Quinine.
RegadenosonAminophylline may decrease the vasodilatory activities of Regadenoson.
RiociguatAminophylline may increase the hypotensive activities of Riociguat.
RitodrineThe risk or severity of adverse effects can be increased when Ritodrine is combined with Aminophylline.
SalmeterolThe risk or severity of adverse effects can be increased when Salmeterol is combined with Aminophylline.
SecobarbitalThe serum concentration of Aminophylline can be decreased when it is combined with Secobarbital.
SiltuximabThe serum concentration of Aminophylline can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Aminophylline can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Aminophylline can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Aminophylline can be increased when it is combined with Stiripentol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Aminophylline.
TemazepamThe therapeutic efficacy of Temazepam can be decreased when used in combination with Aminophylline.
TerbutalineThe risk or severity of adverse effects can be increased when Terbutaline is combined with Aminophylline.
TeriflunomideThe serum concentration of Aminophylline can be decreased when it is combined with Teriflunomide.
ThiabendazoleThe metabolism of Aminophylline can be decreased when combined with Thiabendazole.
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Aminophylline.
TiclopidineThe metabolism of Aminophylline can be decreased when combined with Ticlopidine.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Aminophylline.
TocilizumabThe serum concentration of Aminophylline can be decreased when it is combined with Tocilizumab.
TofisopamThe therapeutic efficacy of Tofisopam can be decreased when used in combination with Aminophylline.
TriazolamThe therapeutic efficacy of Triazolam can be decreased when used in combination with Aminophylline.
VemurafenibThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.
ZafirlukastThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.
Food Interactions
  • Limit caffeine intake.
  • Take with food.
  • Vitamin B6 needs increased, supplement recommended.

Targets

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

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on April 05, 2016 16:04