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Identification
NameTerfenadine
Accession NumberDB00342  (APRD00606)
TypeSmall Molecule
GroupsWithdrawn
DescriptionIn the U.S., Terfenadine was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation.
Structure
Thumb
Synonyms
(RS)-1-(4-tert-butylphenyl)-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}-butan-1-ol
Terfenadin
Terfenadina
Terfénadine
Terfenadine
Terfenadinum
External Identifiers
  • RMI 9918
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Allergy Relieftablet60 mgoralJcp Laboratories Inc.1994-12-311998-08-12Canada
Novo-terfenadine Tab 60mgtablet60 mgoralNovopharm Limited1993-12-311999-11-15Canada
Safeway Once A Day Allergy Caplet 120mgtablet120 mgoralJcp Laboratories Inc.1991-12-311997-01-13Canada
Seldane - Sus 30mg/5mlsuspension30 mgoralHoechst Marion Roussel Canada Inc.1995-12-311998-08-12Canada
Seldane - Tab 60mgtablet60 mgoralHoechst Marion Roussel Canada Inc.1996-10-071998-08-12Canada
Seldane 120mg Once-A-day Capletstablet120 mgoralHoechst Marion Roussel Canada Inc.1995-12-311998-08-12Canada
Seldane Sus 6mg/mlsuspension6 mgoralMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1985-12-311996-09-09Canada
Seldane Tab 120mgtablet120 mgoralMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1988-12-311997-08-05Canada
Seldane Tab 60mgtablet60 mgoralMerrell Pharms Inc., Division Of Merrell Dow (Can)1983-12-311997-08-05Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-terfenadine Tab 120mgtablet120 mgoralApotex Inc1993-12-311999-12-08Canada
Apo-terfenadine Tablets 60mgtablet60 mgoralApotex Inc1993-12-311999-12-08Canada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BronalGalenika
DaylertMicro Labs
SeldaneNot Available
ServininNovartis
TeldaneNot Available
TerfedCipla
Terfenadin ALAliud
Terfenadine FLXAccord Healthcare
TerfinInterbat
TernadinDunar
TrexylRanbaxy
TriludanNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7BA5G9Y06Q
CAS number50679-08-8
WeightAverage: 471.6734
Monoisotopic: 471.313729561
Chemical FormulaC32H41NO2
InChI KeyInChIKey=GUGOEEXESWIERI-UHFFFAOYSA-N
InChI
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
IUPAC Name
1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol
SMILES
CC(C)(C)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylbutylamine
  • Phenylpropane
  • Aralkylamine
  • Piperidine
  • Tertiary alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary alcohol
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
PharmacodynamicsTerfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. The active metabolite of terfenadine is fexofenadine.
Mechanism of actionTerfenadine competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of terfenadine to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier, CNS depression is minimal.
Related Articles
AbsorptionOn the basis of a mass balance study using 14C labeled terfenadine the oral absorption of terfenadine was estimated to be at least 70%
Volume of distributionNot Available
Protein binding70%
Metabolism

Hepatic

SubstrateEnzymesProduct
Terfenadine
fexofenadineDetails
Route of eliminationNot Available
Half life3.5 hours
ClearanceNot Available
ToxicityMild (e.g., headache, nausea, confusion), but adverse cardiac events including cardiac arrest, ventricular arrhythmias including torsades de pointes and QT prolongation have been reported. LD50=mg/kg (orally in mice)
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+0.9535
Blood Brain Barrier+0.5319
Caco-2 permeable+0.6691
P-glycoprotein substrateSubstrate0.8338
P-glycoprotein inhibitor IInhibitor0.7145
P-glycoprotein inhibitor IIInhibitor0.5515
Renal organic cation transporterInhibitor0.5731
CYP450 2C9 substrateNon-substrate0.8286
CYP450 2D6 substrateSubstrate0.7689
CYP450 3A4 substrateSubstrate0.6664
CYP450 1A2 substrateInhibitor0.5553
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorInhibitor0.5229
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9627
Ames testNon AMES toxic0.8907
CarcinogenicityNon-carcinogens0.8443
BiodegradationNot ready biodegradable0.9683
Rat acute toxicity2.0063 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5556
hERG inhibition (predictor II)Inhibitor0.8014
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Veratex Corp.
Dosage forms
FormRouteStrength
Tabletoral60 mg
Tabletoral120 mg
Suspensionoral30 mg
Suspensionoral6 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point147 °CPhysProp
water solubility0.0963 mg/L (at 25 °C)MCFARLAND,JW ET AL. (2001)
logP7.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000458 mg/mLALOGPS
logP5.89ALOGPS
logP6.48ChemAxon
logS-6ALOGPS
pKa (Strongest Acidic)13.2ChemAxon
pKa (Strongest Basic)9.02ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area43.7 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity146.27 m3·mol-1ChemAxon
Polarizability56.45 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
MSMass Spectrum (Electron Ionization)splash10-001i-8890000000-2c6ad1195e498f463cbfView in MoNA
References
Synthesis Reference

Timothy G. Fawcett, Christian T. Goralski, David W. Ziettlow, “Preparation of polymorphically pure terfenadine.” U.S. Patent US4742175, issued April, 1975.

US4742175
General ReferencesNot Available
External Links
ATC CodesR06AX12
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.9 KB)
Interactions
Drug Interactions
Drug
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Terfenadine.
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Terfenadine.
AbirateroneThe metabolism of Terfenadine can be decreased when combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Terfenadine.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Terfenadine.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Terfenadine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Terfenadine.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Terfenadine.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Terfenadine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Terfenadine.
AmiodaroneThe serum concentration of Terfenadine can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Terfenadine.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Terfenadine.
AmphetamineAmphetamine may decrease the sedative activities of Terfenadine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Terfenadine.
AprepitantThe serum concentration of Terfenadine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Terfenadine.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Terfenadine.
ArtemetherThe metabolism of Terfenadine can be decreased when combined with Artemether.
AtazanavirThe serum concentration of Terfenadine can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Terfenadine.
AtomoxetineThe metabolism of Terfenadine can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Terfenadine.
BenzphetamineBenzphetamine may decrease the sedative activities of Terfenadine.
Benzylpenicilloyl PolylysineTerfenadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Terfenadine.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Terfenadine.
BetaxololThe metabolism of Terfenadine can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Terfenadine can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Terfenadine can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Terfenadine can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Terfenadine can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Terfenadine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Terfenadine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Terfenadine.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Terfenadine.
BupropionThe metabolism of Terfenadine can be decreased when combined with Bupropion.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Terfenadine.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Terfenadine.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Terfenadine.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Terfenadine.
CapecitabineThe metabolism of Terfenadine can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Terfenadine can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Terfenadine.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Terfenadine.
CelecoxibThe metabolism of Terfenadine can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Terfenadine can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Terfenadine.
ChloroquineThe metabolism of Terfenadine can be decreased when combined with Chloroquine.
ChlorphentermineChlorphentermine may decrease the sedative activities of Terfenadine.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Terfenadine.
ChlorpromazineThe metabolism of Terfenadine can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Terfenadine can be decreased when combined with Cholecalciferol.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Terfenadine.
CimetidineThe metabolism of Terfenadine can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Terfenadine can be decreased when combined with Cinacalcet.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Terfenadine.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Terfenadine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Terfenadine.
CitalopramThe metabolism of Terfenadine can be decreased when combined with Citalopram.
ClarithromycinThe serum concentration of Terfenadine can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Terfenadine can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Terfenadine.
ClobazamThe metabolism of Terfenadine can be decreased when combined with Clobazam.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Terfenadine.
ClomipramineThe metabolism of Terfenadine can be decreased when combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Terfenadine.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Terfenadine.
ClotrimazoleThe metabolism of Terfenadine can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Terfenadine.
ClozapineThe metabolism of Terfenadine can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Terfenadine can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Terfenadine.
CocaineThe metabolism of Terfenadine can be decreased when combined with Cocaine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Terfenadine.
ConivaptanThe serum concentration of Terfenadine can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Terfenadine.
CrizotinibThe metabolism of Terfenadine can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Terfenadine.
CyclosporineThe metabolism of Terfenadine can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Terfenadine.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Terfenadine.
DabrafenibThe serum concentration of Terfenadine can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Terfenadine.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Terfenadine.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Terfenadine.
DarifenacinThe metabolism of Terfenadine can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Terfenadine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Terfenadine can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Terfenadine.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Terfenadine.
DeferasiroxThe serum concentration of Terfenadine can be decreased when it is combined with Deferasirox.
DelavirdineDelavirdine may increase the arrhythmogenic activities of Terfenadine.
DesipramineThe metabolism of Terfenadine can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Terfenadine can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Terfenadine.
DextroamphetamineDextroamphetamine may decrease the sedative activities of Terfenadine.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Terfenadine.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Terfenadine.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Terfenadine.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Terfenadine.
DihydroergotamineThe metabolism of Terfenadine can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Terfenadine.
DiltiazemThe metabolism of Terfenadine can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Terfenadine.
DiphenhydramineThe metabolism of Terfenadine can be decreased when combined with Diphenhydramine.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Terfenadine.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Terfenadine.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Terfenadine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Terfenadine.
DoxycyclineThe metabolism of Terfenadine can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Terfenadine can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Terfenadine can be decreased when combined with Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Terfenadine.
EfavirenzThe serum concentration of Terfenadine can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Terfenadine.
EliglustatThe metabolism of Terfenadine can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Terfenadine can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Terfenadine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Terfenadine.
ErythromycinThe metabolism of Terfenadine can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Terfenadine.
Eslicarbazepine acetateThe serum concentration of Terfenadine can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Terfenadine.
EstriolThe serum concentration of Estriol can be increased when it is combined with Terfenadine.
EstroneThe serum concentration of Estrone can be increased when it is combined with Terfenadine.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Terfenadine.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Terfenadine.
EtravirineThe serum concentration of Terfenadine can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Terfenadine.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Terfenadine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Terfenadine.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Terfenadine.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Terfenadine.
FloxuridineThe metabolism of Terfenadine can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Terfenadine can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Terfenadine can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Terfenadine can be decreased when combined with Fluoxetine.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Terfenadine.
FluvastatinThe metabolism of Terfenadine can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Terfenadine can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Terfenadine can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Terfenadine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Terfenadine can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Terfenadine can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Terfenadine.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Terfenadine.
GemfibrozilThe metabolism of Terfenadine can be decreased when combined with Gemfibrozil.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Terfenadine.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Terfenadine.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Terfenadine.
HaloperidolThe metabolism of Terfenadine can be decreased when combined with Haloperidol.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Terfenadine.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Terfenadine.
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Terfenadine.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Terfenadine.
IdelalisibThe serum concentration of Terfenadine can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Terfenadine can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Terfenadine.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Terfenadine.
ImipramineThe metabolism of Terfenadine can be decreased when combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Terfenadine.
IndinavirThe serum concentration of Terfenadine can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Terfenadine.
IrbesartanThe metabolism of Terfenadine can be decreased when combined with Irbesartan.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Terfenadine.
IsavuconazoniumThe metabolism of Terfenadine can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Terfenadine can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Terfenadine can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Terfenadine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Terfenadine can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Terfenadine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Terfenadine.
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Terfenadine.
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Terfenadine.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Terfenadine.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Terfenadine.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Terfenadine.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Terfenadine.
LeflunomideThe metabolism of Terfenadine can be decreased when combined with Leflunomide.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Terfenadine.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Terfenadine.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Terfenadine.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Terfenadine.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Terfenadine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Terfenadine.
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Terfenadine.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Terfenadine.
LopinavirThe serum concentration of Terfenadine can be increased when it is combined with Lopinavir.
LorcaserinThe metabolism of Terfenadine can be decreased when combined with Lorcaserin.
LosartanThe serum concentration of Losartan can be increased when it is combined with Terfenadine.
LosartanThe metabolism of Terfenadine can be decreased when combined with Losartan.
LovastatinThe metabolism of Terfenadine can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Terfenadine can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Terfenadine can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Terfenadine can be decreased when combined with Lumefantrine.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Terfenadine.
MephentermineMephentermine may decrease the sedative activities of Terfenadine.
MethadoneThe metabolism of Terfenadine can be decreased when combined with Methadone.
MethamphetamineMethamphetamine may decrease the sedative activities of Terfenadine.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Terfenadine.
MethotrimeprazineThe metabolism of Terfenadine can be decreased when combined with Methotrimeprazine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Terfenadine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Terfenadine.
MetoprololThe metabolism of Terfenadine can be decreased when combined with Metoprolol.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Terfenadine.
MifepristoneThe metabolism of Terfenadine can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Terfenadine.
MirabegronThe metabolism of Terfenadine can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Terfenadine can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Terfenadine.
ModafinilThe serum concentration of Terfenadine can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Terfenadine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Terfenadine.
NadololThe serum concentration of Nadolol can be increased when it is combined with Terfenadine.
NafcillinThe serum concentration of Terfenadine can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Terfenadine.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Terfenadine.
NefazodoneThe serum concentration of Terfenadine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Terfenadine can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Terfenadine can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Terfenadine can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Terfenadine.
NicardipineThe metabolism of Terfenadine can be decreased when combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Terfenadine.
NilotinibThe metabolism of Terfenadine can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Terfenadine.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Terfenadine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Terfenadine.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Terfenadine.
OlaparibThe metabolism of Terfenadine can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Terfenadine.
OmeprazoleThe metabolism of Terfenadine can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Terfenadine can be increased when it is combined with Osimertinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Terfenadine.
PalbociclibThe serum concentration of Terfenadine can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Terfenadine.
PanobinostatThe metabolism of Terfenadine can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Terfenadine can be decreased when combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Terfenadine.
Peginterferon alfa-2bThe serum concentration of Terfenadine can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Terfenadine can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Terfenadine can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Terfenadine.
PhenterminePhentermine may decrease the sedative activities of Terfenadine.
PhenytoinThe metabolism of Terfenadine can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Terfenadine.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Terfenadine.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Terfenadine.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Terfenadine.
PosaconazoleThe serum concentration of Terfenadine can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Terfenadine.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Terfenadine.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Terfenadine.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Terfenadine.
PrimidoneThe metabolism of Terfenadine can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Terfenadine.
PromazineThe metabolism of Terfenadine can be decreased when combined with Promazine.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Terfenadine.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Terfenadine.
PyrimethamineThe metabolism of Terfenadine can be decreased when combined with Pyrimethamine.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Terfenadine.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Terfenadine.
QuinidineThe metabolism of Terfenadine can be decreased when combined with Quinidine.
QuinineThe serum concentration of Quinine can be increased when it is combined with Terfenadine.
QuinineThe metabolism of Terfenadine can be decreased when combined with Quinine.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Terfenadine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Terfenadine.
RanolazineThe metabolism of Terfenadine can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Terfenadine.
RifabutinThe metabolism of Terfenadine can be increased when combined with Rifabutin.
RifampicinThe metabolism of Terfenadine can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Terfenadine.
RifapentineThe metabolism of Terfenadine can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Terfenadine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Terfenadine.
RitonavirThe serum concentration of Terfenadine can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Terfenadine.
RolapitantThe metabolism of Terfenadine can be decreased when combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Terfenadine.
RopiniroleThe metabolism of Terfenadine can be decreased when combined with Ropinirole.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Terfenadine.
SaquinavirThe serum concentration of Terfenadine can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Terfenadine.
SecobarbitalThe metabolism of Terfenadine can be increased when combined with Secobarbital.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Terfenadine.
SertralineThe metabolism of Terfenadine can be decreased when combined with Sertraline.
SildenafilThe metabolism of Terfenadine can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Terfenadine.
SiltuximabThe serum concentration of Terfenadine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Terfenadine can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Terfenadine.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Terfenadine.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Terfenadine.
SorafenibThe metabolism of Terfenadine can be decreased when combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Terfenadine.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Terfenadine.
St. John's WortThe serum concentration of Terfenadine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Terfenadine can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Terfenadine can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Terfenadine can be decreased when combined with Sulfamethoxazole.
SulfisoxazoleThe metabolism of Terfenadine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Terfenadine.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Terfenadine.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Terfenadine.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Terfenadine.
TelaprevirThe serum concentration of Terfenadine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Terfenadine can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Terfenadine.
TerbinafineThe metabolism of Terfenadine can be decreased when combined with Terbinafine.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Terfenadine.
ThioridazineThe metabolism of Terfenadine can be decreased when combined with Thioridazine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Terfenadine.
TicagrelorThe metabolism of Terfenadine can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Terfenadine can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Terfenadine.
TipranavirThe metabolism of Terfenadine can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Terfenadine can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Terfenadine can be decreased when combined with Tolbutamide.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Terfenadine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Terfenadine.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Terfenadine.
TranylcypromineThe metabolism of Terfenadine can be decreased when combined with Tranylcypromine.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Terfenadine.
TrimethoprimThe metabolism of Terfenadine can be decreased when combined with Trimethoprim.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Terfenadine.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Terfenadine.
Valproic AcidThe metabolism of Terfenadine can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Terfenadine can be decreased when combined with Valsartan.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Terfenadine.
VenlafaxineThe metabolism of Terfenadine can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Terfenadine.
VerapamilThe metabolism of Terfenadine can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Terfenadine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Terfenadine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Terfenadine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Terfenadine.
VoriconazoleThe serum concentration of Terfenadine can be increased when it is combined with Voriconazole.
ZafirlukastThe metabolism of Terfenadine can be decreased when combined with Zafirlukast.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Terfenadine.
ZiprasidoneThe metabolism of Terfenadine can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [PubMed:9485522 ]
  3. Salata JJ, Jurkiewicz NK, Wallace AA, Stupienski RF 3rd, Guinosso PJ Jr, Lynch JJ Jr: Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ Res. 1995 Jan;76(1):110-9. [PubMed:8001268 ]
  4. Wood-Baker R, Smith R, Holgate ST: A double-blind, placebo controlled study of the effect of the specific histamine H1-receptor antagonist, terfenadine, in chronic severe asthma. Br J Clin Pharmacol. 1995 Jun;39(6):671-5. [PubMed:7654486 ]
  5. Phillips GD, Polosa R, Holgate ST: The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma. Clin Exp Allergy. 1989 Jul;19(4):405-9. [PubMed:2569356 ]
  6. Rafferty P, Holgate ST: Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways. Am Rev Respir Dis. 1987 Jan;135(1):181-4. [PubMed:2879489 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Gessner G, Zacharias M, Bechstedt S, Schonherr R, Heinemann SH: Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents. Mol Pharmacol. 2004 May;65(5):1120-9. [PubMed:15102940 ]
  3. Testai L, Cecchetti V, Sabatini S, Martelli A, Breschi MC, Calderone V: Effects of K openers on the QT prolongation induced by HERG-blocking drugs in guinea-pigs. J Pharm Pharmacol. 2010 Jul;62(7):924-30. doi: 10.1211/jpp.62.06.0014. [PubMed:20636881 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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. Wang RW, Newton DJ, Liu N, Atkins WM, Lu AY: Human cytochrome P-450 3A4: in vitro drug-drug interaction patterns are substrate-dependent. Drug Metab Dispos. 2000 Mar;28(3):360-6. [PubMed:10681383 ]
  2. 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 ]
  3. Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [PubMed:9485522 ]
  4. Nemeroff CB, DeVane CL, Pollock BG: Newer antidepressants and the cytochrome P450 system. Am J Psychiatry. 1996 Mar;153(3):311-20. [PubMed:8610817 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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 ]
  2. Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [PubMed:9485522 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 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:
Oxygen binding
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.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 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
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible for the epoxidation of endogenous cardiac arachidonic acid pools.
Gene Name:
CYP2J2
Uniprot ID:
P51589
Molecular Weight:
57610.165 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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  2. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389 ]
  3. Hait WN, Gesmonde JF, Murren JR, Yang JM, Chen HX, Reiss M: Terfenadine (Seldane): a new drug for restoring sensitivity to multidrug resistant cancer cells. Biochem Pharmacol. 1993 Jan 26;45(2):401-6. [PubMed:8094615 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23