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Identification
NameDisopyramide
Accession NumberDB00280  (APRD00507)
TypeSmall Molecule
GroupsApproved
DescriptionA class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties. [PubChem]
Structure
Thumb
Synonyms
Disopiramida
Disopyramidum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Norpacecapsule, gelatin coated100 mg/1oralG.D. Searle LLC Division of Pfizer Inc1982-07-20Not applicableUs
Norpacecapsule, gelatin coated100 mg/1oralCarilion Materials Management1982-07-20Not applicableUs
Norpacecapsule, gelatin coated150 mg/1oralG.D. Searle LLC Division of Pfizer Inc1982-07-20Not applicableUs
Norpacecapsule, gelatin coated150 mg/1oralCarilion Materials Management1982-07-20Not applicableUs
Norpacecapsule, gelatin coated100 mg/1oralG.D. Searle LLC Division of Pfizer Inc1977-09-01Not applicableUs
Norpacecapsule, gelatin coated150 mg/1oralG.D. Searle LLC Division of Pfizer Inc1977-09-01Not applicableUs
Norpace Cap 100mgcapsule100 mgoralRoberts Pharmaceutical Canada Inc.1994-12-311999-08-11Canada
Norpace Cap 150mgcapsule150 mgoralRoberts Pharmaceutical Canada Inc.1994-12-311999-08-11Canada
Norpace CR 150mgtablet (extended-release)150 mgoralShire Biochem Inc1994-12-312004-04-30Canada
Rythmodancapsule150 mgoralSanofi Aventis Canada Inc2003-09-152012-05-24Canada
Rythmodancapsule100 mgoralSanofi Aventis Canada Inc2003-09-12Not applicableCanada
Rythmodan Cap 100mgcapsule100 mgoralRoussel Canada Inc.1977-12-311999-08-11Canada
Rythmodan Cap 150mgcapsule150 mgoralRoussel Canada Inc.1978-12-312000-07-28Canada
Rythmodan Capsules 100mgcapsule100 mgoralHoechst Roussel Canada Inc.1997-03-032007-07-31Canada
Rythmodan Capsules 150mgcapsule150 mgoralHoechst Roussel Canada Inc.1996-05-312005-08-01Canada
Rythmodan LA Tab 250mgtablet (extended-release)250 mgoralRoussel Canada Inc.1984-12-311997-08-05Canada
Rythmodan-LAtablet (extended-release)250 mgoralSanofi Aventis Canada Inc1999-04-302009-10-29Canada
Rythmodan-LA 250mgtablet (extended-release)250 mgoralHoechst Roussel Canada Inc.1995-12-312001-07-20Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Disopyramide Phosphatecapsule100 mg/1oralCarilion Materials Management1990-09-30Not applicableUs
Disopyramide Phosphatecapsule100 mg/1oralTeva Pharmaceuticals USA Inc1990-09-30Not applicableUs
Disopyramide Phosphatecapsule100 mg/1oralAv Kare, Inc.2014-01-03Not applicableUs
Disopyramide Phosphatecapsule150 mg/1oralTeva Pharmaceuticals USA Inc1990-09-30Not applicableUs
Disopyramide Phosphatecapsule150 mg/1oralAv Kare, Inc.2014-01-03Not applicableUs
Disopyramide Phosphatecapsule100 mg/1oralActavis Pharma, Inc.1985-05-31Not applicableUs
Disopyramide Phosphatecapsule150 mg/1oralCarilion Materials Management1990-09-30Not applicableUs
Disopyramide Phosphatecapsule150 mg/1oralActavis Pharma, Inc.1985-05-31Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DicorantilSanofi
IsorythmSERP
LispineSawai Seiyaku
RitmodanSanofi
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Disopyramide phosphate
ThumbNot applicableDBSALT000899
Categories
UNIIGFO928U8MQ
CAS number3737-09-5
WeightAverage: 339.4745
Monoisotopic: 339.231062565
Chemical FormulaC21H29N3O
InChI KeyInChIKey=UVTNFZQICZKOEM-UHFFFAOYNA-N
InChI
InChI=1/C21H29N3O/c1-16(2)24(17(3)4)15-13-21(20(22)25,18-10-6-5-7-11-18)19-12-8-9-14-23-19/h5-12,14,16-17H,13,15H2,1-4H3,(H2,22,25)
IUPAC Name
4-[bis(propan-2-yl)amino]-2-phenyl-2-(pyridin-2-yl)butanamide
SMILES
CC(C)N(CCC(C(N)=O)(C1=CC=CC=C1)C1=NC=CC=C1)C(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as pheniramines. These are compounds containing a pheniramine moiety, which is structurally characterized by the presence of a 2-benzylpyridine linked to an dimethyl(propyl)amine to form a dimethyl[3-phenyl-3-(pyridin-2-yl)propyl]amine skeleton.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassPheniramines
Direct ParentPheniramines
Alternative Parents
Substituents
  • Pheniramine
  • Phenylacetamide
  • Phenylpropylamine
  • Aralkylamine
  • Fatty acyl
  • Benzenoid
  • Fatty amide
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Primary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, ventricular pre-excitation and cardiac dysrhythmias. It is a Class Ia antiarrhythmic drug.
PharmacodynamicsDisopyramide is an antiarrhythmic drug indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia that are life-threatening. In man, Disopyramide at therapeutic plasma levels shortens the sinus node recovery time, lengthens the effective refractory period of the atrium, and has a minimal effect on the effective refractory period of the AV node. Little effect has been shown on AV-nodal and His-Purkinje conduction times or QRS duration. However, prolongation of conduction in accessory pathways occurs.
Mechanism of actionDisopyramide is a Type 1A antiarrhythmic drug (ie, similar to procainamide and quinidine). It inhibits the fast sodium channels. In animal studies Disopyramide decreases the rate of diastolic depolarization (phase 4) in cells with augmented automaticity, decreases the upstroke velocity (phase 0) and increases the action potential duration of normal cardiac cells, decreases the disparity in refractoriness between infarcted and adjacent normally perfused myocardium, and has no effect on alpha- or beta-adrenergic receptors.
Related Articles
AbsorptionNearly complete
Volume of distributionNot Available
Protein binding50%-65%
Metabolism

Hepatic

SubstrateEnzymesProduct
Disopyramide
mono-isopropyl-disopyramideDetails
Route of eliminationIn healthy men, about 50% of a given dose of disopyramide is excreted in the urine as the unchanged drug, about 20% as the mono-N-dealkylated metabolite and 10% as the other metabolites.
Half life6.7 hours (range 4-10 hours)
ClearanceNot Available
ToxicityLD50=580 mg/kg in rats
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Disopyramide Action PathwayDrug actionSMP00325
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9529
Blood Brain Barrier+0.9508
Caco-2 permeable+0.557
P-glycoprotein substrateSubstrate0.5492
P-glycoprotein inhibitor INon-inhibitor0.8677
P-glycoprotein inhibitor IINon-inhibitor0.8535
Renal organic cation transporterInhibitor0.5702
CYP450 2C9 substrateNon-substrate0.7975
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6906
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8236
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8626
Ames testNon AMES toxic0.8258
CarcinogenicityNon-carcinogens0.8873
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9764 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.996
hERG inhibition (predictor II)Inhibitor0.6168
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Kv pharmaceutical co
  • Gd searle llc
  • Interpharm inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral100 mg/1
Capsuleoral150 mg/1
Capsule, gelatin coatedoral100 mg/1
Capsule, gelatin coatedoral150 mg/1
Capsuleoral150 mg
Tablet (extended-release)oral150 mg
Capsuleoral100 mg
Tablet (extended-release)oral250 mg
Prices
Unit descriptionCostUnit
Norpace CR 150 mg 12 Hour Capsule2.35USD capsule
Norpace cr 150 mg capsule2.26USD capsule
Norpace CR 100 mg 12 Hour Capsule1.98USD capsule
Norpace 150 mg capsule1.94USD capsule
Norpace cr 100 mg capsule1.91USD capsule
Norpace 100 mg capsule1.62USD capsule
Disopyramide Phosphate 150 mg capsule0.96USD capsule
Disopyramide 150 mg capsule0.82USD capsule
Disopyramide Phosphate 100 mg capsule0.72USD capsule
Disopyramide 100 mg capsule0.69USD capsule
Rythmodan 150 mg Capsule0.43USD capsule
Rythmodan 100 mg Capsule0.3USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point94.5-95 °CCusic, J.W. and Sause, H.W.; U.S. Patent 3,225,054; December 21,1965; assigned to G.D. Searle & Co.
water solubility44.9 mg/LNot Available
logP2.58MANNHOLD,R ET AL. (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.0493 mg/mLALOGPS
logP3.21ALOGPS
logP3.47ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)16.19ChemAxon
pKa (Strongest Basic)10.42ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area59.22 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity102.3 m3·mol-1ChemAxon
Polarizability38.82 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Cusic, J.W. and Sause, H.W.; U.S. Patent 3,225,054; December 21,1965; assigned to G.D. Searle & Co.

US3225054
General ReferencesNot Available
External Links
ATC CodesC01BA03
AHFS Codes
  • 24:04.04.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Disopyramide.
AcarboseAcarbose may increase the hypoglycemic activities of Disopyramide.
AcebutololDisopyramide may increase the bradycardic activities of Acebutolol.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Disopyramide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Disopyramide.
AicarAicar may increase the hypoglycemic activities of Disopyramide.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Disopyramide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Disopyramide.
AlprenololDisopyramide may increase the bradycardic activities of Alprenolol.
AmantadineAmantadine may increase the QTc-prolonging activities of Disopyramide.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Disopyramide.
AmiodaroneAmiodarone may increase the QTc-prolonging activities of Disopyramide.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Disopyramide.
AmoxapineAmoxapine may increase the hypoglycemic activities of Disopyramide.
AnagrelideAnagrelide may increase the QTc-prolonging activities of Disopyramide.
ApomorphineApomorphine may increase the QTc-prolonging activities of Disopyramide.
AprepitantThe serum concentration of Disopyramide can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Disopyramide.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Disopyramide.
ArotinololDisopyramide may increase the bradycardic activities of Arotinolol.
Arsenic trioxideDisopyramide may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherDisopyramide may increase the QTc-prolonging activities of Artemether.
AsenapineDisopyramide may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe metabolism of Disopyramide can be decreased when combined with Atazanavir.
AtenololDisopyramide may increase the bradycardic activities of Atenolol.
AtomoxetineThe metabolism of Disopyramide can be decreased when combined with Atomoxetine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Disopyramide.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Disopyramide.
BefunololDisopyramide may increase the bradycardic activities of Befunolol.
BenmoxinBenmoxin may increase the hypoglycemic activities of Disopyramide.
BetaxololDisopyramide may increase the bradycardic activities of Betaxolol.
BevantololDisopyramide may increase the bradycardic activities of Bevantolol.
BexaroteneThe serum concentration of Disopyramide can be decreased when it is combined with Bexarotene.
BisoprololDisopyramide may increase the bradycardic activities of Bisoprolol.
BoceprevirThe metabolism of Disopyramide can be decreased when combined with Boceprevir.
BopindololDisopyramide may increase the bradycardic activities of Bopindolol.
BortezomibThe metabolism of Disopyramide can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Disopyramide can be decreased when it is combined with Bosentan.
BuforminBuformin may increase the hypoglycemic activities of Disopyramide.
BufuralolDisopyramide may increase the bradycardic activities of Bufuralol.
BupranololDisopyramide may increase the bradycardic activities of Bupranolol.
BuserelinBuserelin may increase the QTc-prolonging activities of Disopyramide.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Disopyramide.
CarbamazepineThe metabolism of Disopyramide can be increased when combined with Carbamazepine.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Disopyramide.
CarteololDisopyramide may increase the bradycardic activities of Carteolol.
CarvedilolDisopyramide may increase the bradycardic activities of Carvedilol.
CastanospermineCastanospermine may increase the hypoglycemic activities of Disopyramide.
CeliprololDisopyramide may increase the bradycardic activities of Celiprolol.
CeritinibCeritinib may increase the QTc-prolonging activities of Disopyramide.
ChloroquineChloroquine may increase the QTc-prolonging activities of Disopyramide.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Disopyramide.
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Disopyramide.
CiglitazoneCiglitazone may increase the hypoglycemic activities of Disopyramide.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Disopyramide.
CisaprideDisopyramide may increase the QTc-prolonging activities of Cisapride.
CitalopramCitalopram may increase the QTc-prolonging activities of Disopyramide.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Disopyramide.
ClemastineThe metabolism of Disopyramide can be decreased when combined with Clemastine.
ClomipramineClomipramine may increase the hypoglycemic activities of Disopyramide.
ClotrimazoleThe metabolism of Disopyramide can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Disopyramide.
CobicistatThe metabolism of Disopyramide can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Disopyramide can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Disopyramide.
CyclosporineThe metabolism of Disopyramide can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Disopyramide can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the hypoglycemic activities of Disopyramide.
DarunavirThe metabolism of Disopyramide can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Disopyramide can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Disopyramide can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Disopyramide.
DelavirdineThe metabolism of Disopyramide can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Disopyramide.
DesipramineDesipramine may increase the QTc-prolonging activities of Disopyramide.
DexamethasoneThe serum concentration of Disopyramide can be decreased when it is combined with Dexamethasone.
DiflunisalDiflunisal may increase the hypoglycemic activities of Disopyramide.
DihydroergotamineThe metabolism of Disopyramide can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Disopyramide.
DiltiazemThe metabolism of Disopyramide can be decreased when combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Disopyramide.
DofetilideDofetilide may increase the QTc-prolonging activities of Disopyramide.
DolasetronDolasetron may increase the QTc-prolonging activities of Disopyramide.
DomperidoneDisopyramide may increase the QTc-prolonging activities of Domperidone.
DoxepinDoxepin may increase the QTc-prolonging activities of Disopyramide.
DoxycyclineThe metabolism of Disopyramide can be decreased when combined with Doxycycline.
DronedaroneDisopyramide may increase the QTc-prolonging activities of Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Disopyramide.
DulaglutideDulaglutide may increase the hypoglycemic activities of Disopyramide.
EfavirenzThe serum concentration of Disopyramide can be decreased when it is combined with Efavirenz.
EliglustatDisopyramide may increase the QTc-prolonging activities of Eliglustat.
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Disopyramide.
EnzalutamideThe serum concentration of Disopyramide can be decreased when it is combined with Enzalutamide.
EribulinEribulin may increase the QTc-prolonging activities of Disopyramide.
ErythromycinErythromycin may increase the QTc-prolonging activities of Disopyramide.
EscitalopramDisopyramide may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Disopyramide can be decreased when it is combined with Eslicarbazepine acetate.
EsmololDisopyramide may increase the bradycardic activities of Esmolol.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Disopyramide.
EtravirineThe serum concentration of Disopyramide can be decreased when it is combined with Etravirine.
ExenatideExenatide may increase the hypoglycemic activities of Disopyramide.
EzogabineEzogabine may increase the QTc-prolonging activities of Disopyramide.
FamotidineFamotidine may increase the QTc-prolonging activities of Disopyramide.
FelbamateFelbamate may increase the QTc-prolonging activities of Disopyramide.
FenfluramineFenfluramine may increase the hypoglycemic activities of Disopyramide.
FingolimodFingolimod may increase the arrhythmogenic activities of Disopyramide.
FlecainideFlecainide may increase the QTc-prolonging activities of Disopyramide.
FluconazoleThe metabolism of Disopyramide can be decreased when combined with Fluconazole.
FluoxetineDisopyramide may increase the QTc-prolonging activities of Fluoxetine.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Disopyramide.
FlupentixolDisopyramide may increase the QTc-prolonging activities of Flupentixol.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Disopyramide.
FormoterolFormoterol may increase the QTc-prolonging activities of Disopyramide.
FosamprenavirThe metabolism of Disopyramide can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Disopyramide can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Disopyramide.
FosphenytoinDisopyramide may increase the QTc-prolonging activities of Fosphenytoin.
FosphenytoinThe metabolism of Disopyramide can be increased when combined with Fosphenytoin.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Disopyramide.
Fusidic AcidThe serum concentration of Disopyramide can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Disopyramide.
GalantamineGalantamine may increase the QTc-prolonging activities of Disopyramide.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Disopyramide.
GlibornurideGlibornuride may increase the hypoglycemic activities of Disopyramide.
GliclazideGliclazide may increase the hypoglycemic activities of Disopyramide.
GlimepirideGlimepiride may increase the hypoglycemic activities of Disopyramide.
GlipizideGlipizide may increase the hypoglycemic activities of Disopyramide.
GliquidoneGliquidone may increase the hypoglycemic activities of Disopyramide.
GlyburideGlyburide may increase the hypoglycemic activities of Disopyramide.
GoserelinGoserelin may increase the QTc-prolonging activities of Disopyramide.
GranisetronGranisetron may increase the QTc-prolonging activities of Disopyramide.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Disopyramide.
HistrelinHistrelin may increase the QTc-prolonging activities of Disopyramide.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Disopyramide.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Disopyramide.
IbandronateIbandronate may increase the QTc-prolonging activities of Disopyramide.
IbutilideDisopyramide may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Disopyramide can be increased when it is combined with Idelalisib.
IloperidoneDisopyramide may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Disopyramide can be decreased when combined with Imatinib.
ImipramineImipramine may increase the QTc-prolonging activities of Disopyramide.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Disopyramide.
IndalpineIndalpine may increase the hypoglycemic activities of Disopyramide.
IndapamideIndapamide may increase the QTc-prolonging activities of Disopyramide.
IndenololDisopyramide may increase the bradycardic activities of Indenolol.
IndinavirThe metabolism of Disopyramide can be decreased when combined with Indinavir.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Disopyramide.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Disopyramide.
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Disopyramide.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Disopyramide.
Insulin HumanInsulin Human may increase the hypoglycemic activities of Disopyramide.
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Disopyramide.
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Disopyramide.
IproclozideIproclozide may increase the hypoglycemic activities of Disopyramide.
IproniazidIproniazid may increase the hypoglycemic activities of Disopyramide.
IsavuconazoniumThe metabolism of Disopyramide can be decreased when combined with Isavuconazonium.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Disopyramide.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Disopyramide.
IsradipineThe metabolism of Disopyramide can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Disopyramide can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Disopyramide.
IvacaftorThe serum concentration of Disopyramide can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Disopyramide can be increased when it is combined with Ketoconazole.
LabetalolDisopyramide may increase the bradycardic activities of Labetalol.
LanreotideDisopyramide may increase the hypoglycemic activities of Lanreotide.
LapatinibLapatinib may increase the QTc-prolonging activities of Disopyramide.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Disopyramide.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Disopyramide.
LevobunololDisopyramide may increase the bradycardic activities of Levobunolol.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Disopyramide.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Disopyramide.
LidocaineDisopyramide may increase the arrhythmogenic activities of Lidocaine.
LinagliptinLinagliptin may increase the hypoglycemic activities of Disopyramide.
LiraglutideLiraglutide may increase the hypoglycemic activities of Disopyramide.
LithiumLithium may increase the QTc-prolonging activities of Disopyramide.
LopinavirDisopyramide may increase the QTc-prolonging activities of Lopinavir.
LovastatinThe metabolism of Disopyramide can be decreased when combined with Lovastatin.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Disopyramide.
LuliconazoleThe serum concentration of Disopyramide can be increased when it is combined with Luliconazole.
LumefantrineDisopyramide may increase the QTc-prolonging activities of Lumefantrine.
LurasidoneLurasidone may increase the QTc-prolonging activities of Disopyramide.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Disopyramide.
MebanazineMebanazine may increase the hypoglycemic activities of Disopyramide.
MecaserminDisopyramide may increase the hypoglycemic activities of Mecasermin.
MefloquineMefloquine may increase the QTc-prolonging activities of Disopyramide.
MesalazineMesalazine may increase the hypoglycemic activities of Disopyramide.
MetforminMetformin may increase the hypoglycemic activities of Disopyramide.
MethadoneMethadone may increase the QTc-prolonging activities of Disopyramide.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Disopyramide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Disopyramide.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Disopyramide.
MetipranololDisopyramide may increase the bradycardic activities of Metipranolol.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Disopyramide.
MetoprololDisopyramide may increase the bradycardic activities of Metoprolol.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Disopyramide.
MifepristoneMifepristone may increase the QTc-prolonging activities of Disopyramide.
MiglitolMiglitol may increase the hypoglycemic activities of Disopyramide.
MiglustatMiglustat may increase the hypoglycemic activities of Disopyramide.
MilnacipranMilnacipran may increase the hypoglycemic activities of Disopyramide.
MinaprineMinaprine may increase the hypoglycemic activities of Disopyramide.
MirabegronMirabegron may increase the QTc-prolonging activities of Disopyramide.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Disopyramide.
MitiglinideMitiglinide may increase the hypoglycemic activities of Disopyramide.
MitotaneThe serum concentration of Disopyramide can be decreased when it is combined with Mitotane.
MoclobemideMoclobemide may increase the hypoglycemic activities of Disopyramide.
ModafinilThe serum concentration of Disopyramide can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Disopyramide.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Disopyramide.
NadololDisopyramide may increase the bradycardic activities of Nadolol.
NafcillinThe serum concentration of Disopyramide can be decreased when it is combined with Nafcillin.
NateglinideNateglinide may increase the hypoglycemic activities of Disopyramide.
NefazodoneThe metabolism of Disopyramide can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Disopyramide can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Disopyramide can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Disopyramide can be decreased when combined with Nevirapine.
NialamideNialamide may increase the hypoglycemic activities of Disopyramide.
NicardipineNicardipine may increase the QTc-prolonging activities of Disopyramide.
NilotinibDisopyramide may increase the QTc-prolonging activities of Nilotinib.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Disopyramide.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Disopyramide.
OctamoxinOctamoxin may increase the hypoglycemic activities of Disopyramide.
OctreotideOctreotide may increase the hypoglycemic activities of Disopyramide.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Disopyramide.
OlanzapineOlanzapine may increase the hypoglycemic activities of Disopyramide.
OlaparibThe metabolism of Disopyramide can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Disopyramide.
OndansetronOndansetron may increase the QTc-prolonging activities of Disopyramide.
OsimertinibThe serum concentration of Disopyramide can be increased when it is combined with Osimertinib.
OxandroloneOxandrolone may increase the hypoglycemic activities of Disopyramide.
OxprenololDisopyramide may increase the bradycardic activities of Oxprenolol.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Disopyramide.
OxytocinOxytocin may increase the QTc-prolonging activities of Disopyramide.
PalbociclibThe serum concentration of Disopyramide can be increased when it is combined with Palbociclib.
PaliperidoneDisopyramide may increase the QTc-prolonging activities of Paliperidone.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Disopyramide.
PargylinePargyline may increase the hypoglycemic activities of Disopyramide.
ParoxetineParoxetine may increase the hypoglycemic activities of Disopyramide.
PasireotideDisopyramide may increase the hypoglycemic activities of Pasireotide.
PazopanibPazopanib may increase the QTc-prolonging activities of Disopyramide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Disopyramide.
PenbutololDisopyramide may increase the bradycardic activities of Penbutolol.
PentamidinePentamidine may increase the QTc-prolonging activities of Disopyramide.
PentamidineDisopyramide may increase the hypoglycemic activities of Pentamidine.
PentobarbitalThe metabolism of Disopyramide can be increased when combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Disopyramide.
PhenelzinePhenelzine may increase the hypoglycemic activities of Disopyramide.
PhenforminPhenformin may increase the hypoglycemic activities of Disopyramide.
PheniprazinePheniprazine may increase the hypoglycemic activities of Disopyramide.
PhenobarbitalThe serum concentration of Disopyramide can be decreased when it is combined with Phenobarbital.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Disopyramide.
PhenytoinThe serum concentration of Disopyramide can be decreased when it is combined with Phenytoin.
PimozideDisopyramide may increase the QTc-prolonging activities of Pimozide.
PindololDisopyramide may increase the bradycardic activities of Pindolol.
PioglitazonePioglitazone may increase the hypoglycemic activities of Disopyramide.
PirlindolePirlindole may increase the hypoglycemic activities of Disopyramide.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Disopyramide.
PosaconazoleThe metabolism of Disopyramide can be decreased when combined with Posaconazole.
PractololDisopyramide may increase the bradycardic activities of Practolol.
PramlintidePramlintide may increase the hypoglycemic activities of Disopyramide.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Disopyramide.
PrimidoneThe metabolism of Disopyramide can be increased when combined with Primidone.
ProcainamideDisopyramide may increase the QTc-prolonging activities of Procainamide.
PromazinePromazine may increase the QTc-prolonging activities of Disopyramide.
PromethazinePromethazine may increase the QTc-prolonging activities of Disopyramide.
PropafenonePropafenone may increase the arrhythmogenic activities of Disopyramide.
PropofolPropofol may increase the QTc-prolonging activities of Disopyramide.
PropranololDisopyramide may increase the bradycardic activities of Propranolol.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Disopyramide.
QuetiapineDisopyramide may increase the QTc-prolonging activities of Quetiapine.
QuinidineDisopyramide may increase the QTc-prolonging activities of Quinidine.
QuinineDisopyramide may increase the QTc-prolonging activities of Quinine.
RanolazineThe metabolism of Disopyramide can be decreased when combined with Ranolazine.
RasagilineRasagiline may increase the hypoglycemic activities of Disopyramide.
RepaglinideRepaglinide may increase the hypoglycemic activities of Disopyramide.
RifabutinThe metabolism of Disopyramide can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Disopyramide can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Disopyramide can be increased when combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Disopyramide.
RisperidoneRisperidone may increase the QTc-prolonging activities of Disopyramide.
RitonavirThe metabolism of Disopyramide can be decreased when combined with Ritonavir.
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Disopyramide.
SafrazineSafrazine may increase the hypoglycemic activities of Disopyramide.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Disopyramide.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Disopyramide.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Disopyramide.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Disopyramide.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Disopyramide.
SelegilineSelegiline may increase the hypoglycemic activities of Disopyramide.
SertralineSertraline may increase the hypoglycemic activities of Disopyramide.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Disopyramide.
SildenafilThe metabolism of Disopyramide can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Disopyramide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Disopyramide can be increased when it is combined with Simeprevir.
SitagliptinSitagliptin may increase the hypoglycemic activities of Disopyramide.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Disopyramide.
SorafenibSorafenib may increase the QTc-prolonging activities of Disopyramide.
SotalolDisopyramide may increase the QTc-prolonging activities of Sotalol.
St. John's WortThe serum concentration of Disopyramide can be decreased when it is combined with St. John's Wort.
StanozololStanozolol may increase the hypoglycemic activities of Disopyramide.
StiripentolThe serum concentration of Disopyramide can be increased when it is combined with Stiripentol.
SulfadiazineDisopyramide may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleDisopyramide may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Disopyramide.
SulfisoxazoleDisopyramide may increase the hypoglycemic activities of Sulfisoxazole.
SulodexideSulodexide may increase the hypoglycemic activities of Disopyramide.
SunitinibDisopyramide may increase the hypoglycemic activities of Sunitinib.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Disopyramide.
TelaprevirThe metabolism of Disopyramide can be decreased when combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Disopyramide.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Disopyramide.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Disopyramide.
TestosteroneTestosterone may increase the hypoglycemic activities of Disopyramide.
TetrabenazineDisopyramide may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineDisopyramide may increase the QTc-prolonging activities of Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Disopyramide.
TiclopidineThe metabolism of Disopyramide can be decreased when combined with Ticlopidine.
TimololDisopyramide may increase the bradycardic activities of Timolol.
TizanidineTizanidine may increase the QTc-prolonging activities of Disopyramide.
TocilizumabThe serum concentration of Disopyramide can be decreased when it is combined with Tocilizumab.
TolazamideTolazamide may increase the hypoglycemic activities of Disopyramide.
TolbutamideTolbutamide may increase the hypoglycemic activities of Disopyramide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Disopyramide.
TolterodineTolterodine may increase the QTc-prolonging activities of Disopyramide.
ToremifeneDisopyramide may increase the QTc-prolonging activities of Toremifene.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Disopyramide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Disopyramide.
TrazodoneTrazodone may increase the hypoglycemic activities of Disopyramide.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Disopyramide.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Disopyramide.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Disopyramide.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Disopyramide.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Disopyramide.
VandetanibDisopyramide may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Disopyramide.
VemurafenibDisopyramide may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Disopyramide can be decreased when combined with Venlafaxine.
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Disopyramide.
VilanterolVilanterol may increase the QTc-prolonging activities of Disopyramide.
VilazodoneVilazodone may increase the hypoglycemic activities of Disopyramide.
VildagliptinVildagliptin may increase the hypoglycemic activities of Disopyramide.
VogliboseVoglibose may increase the hypoglycemic activities of Disopyramide.
VoriconazoleThe metabolism of Disopyramide can be decreased when combined with Voriconazole.
VorinostatVorinostat may increase the QTc-prolonging activities of Disopyramide.
VortioxetineVortioxetine may increase the hypoglycemic activities of Disopyramide.
ZimelidineZimelidine may increase the hypoglycemic activities of Disopyramide.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Disopyramide.
ZuclopenthixolDisopyramide may increase the QTc-prolonging activities of Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function:
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
References
  1. Sugao M, Fujiki A, Nishida K, Sakabe M, Tsuneda T, Iwamoto J, Mizumaki K, Inoue H: Repolarization dynamics in patients with idiopathic ventricular fibrillation: pharmacological therapy with bepridil and disopyramide. J Cardiovasc Pharmacol. 2005 Jun;45(6):545-9. [PubMed:15897781 ]
  2. Fujiki A, Sugao M, Nishida K, Sakabe M, Tsuneda T, Mizumaki K, Inoue H: Repolarization abnormality in idiopathic ventricular fibrillation: assessment using 24-hour QT-RR and QaT-RR relationships. J Cardiovasc Electrophysiol. 2004 Jan;15(1):59-63. [PubMed:15028073 ]
  3. Shimizu W, Antzelevitch C, Suyama K, Kurita T, Taguchi A, Aihara N, Takaki H, Sunagawa K, Kamakura S: Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9. [PubMed:11196553 ]
  4. 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
unknown
Actions
antagonist
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. Yamamoto N, Ozaki T, Keida Y, Ohtsuka M, Goto T: A comparison of the binding characteristics of class I antiarrhythmic agents for human muscarinic m1-m3 receptors. J Cardiovasc Pharmacol. 1999 Jul;34(1):53-9. [PubMed:10413067 ]
  2. Ishida Y, Mizukami M, Taniguchi T, Satake N, Fujiwara M, Shibata S: Anticholinergic action of disopyramide in intestinal smooth muscle of the guinea pig: inhibition of muscarinic receptors (M1 and M2). Jpn J Pharmacol. 1990 Feb;52(2):363-70. [PubMed:1690310 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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. Yamamoto N, Ozaki T, Keida Y, Ohtsuka M, Goto T: A comparison of the binding characteristics of class I antiarrhythmic agents for human muscarinic m1-m3 receptors. J Cardiovasc Pharmacol. 1999 Jul;34(1):53-9. [PubMed:10413067 ]
  2. Ishida Y, Mizukami M, Taniguchi T, Satake N, Fujiwara M, Shibata S: Anticholinergic action of disopyramide in intestinal smooth muscle of the guinea pig: inhibition of muscarinic receptors (M1 and M2). Jpn J Pharmacol. 1990 Feb;52(2):363-70. [PubMed:1690310 ]
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. Yamamoto N, Ozaki T, Keida Y, Ohtsuka M, Goto T: A comparison of the binding characteristics of class I antiarrhythmic agents for human muscarinic m1-m3 receptors. J Cardiovasc Pharmacol. 1999 Jul;34(1):53-9. [PubMed:10413067 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity
Specific Function:
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain. Mediates the major part of the dendritic A-type current I(SA) in brain neurons (By similarity). This current is activated at membrane potentials that are below the threshold for action potentials. It regulates neuronal excitability, prolongs the latency before the firs...
Gene Name:
KCND2
Uniprot ID:
Q9NZV8
Molecular Weight:
70535.825 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated by interactions with other alpha subunits and with regulatory subunits.
Gene Name:
KCND3
Uniprot ID:
Q9UK17
Molecular Weight:
73450.53 Da
References
  1. Casis O, Sanchez-Chapula JA: Disopyramide, imipramine, and amitriptyline bind to a common site on the transient outward K+ channel. J Cardiovasc Pharmacol. 1998 Oct;32(4):521-6. [PubMed:9781919 ]

Enzymes

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. Echizen H, Tanizaki M, Tatsuno J, Chiba K, Berwick T, Tani M, Gonzalez FJ, Ishizaki T: Identification of CYP3A4 as the enzyme involved in the mono-N-dealkylation of disopyramide enantiomers in humans. Drug Metab Dispos. 2000 Aug;28(8):937-44. [PubMed:10901704 ]
  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. Zhang L, Fitzloff JF, Engel LC, Cook CS: Species difference in stereoselective involvement of CYP3A in the mono-N-dealkylation of disopyramide. Xenobiotica. 2001 Feb;31(2):73-83. [PubMed:11407536 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
other/unknown
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Chu JS, Kishion S, Nomura A, Miyazaki K: Serum alpha 1-acid glycoprotein, sialic acid, and protein binding of disopyramide in normal subjects and cardiac patients. Zhongguo Yao Li Xue Bao. 1997 Sep;18(5):408-10. [PubMed:10322928 ]
  2. Hanada K, Ohta T, Hirai M, Arai M, Ogata H: Enantioselective binding of propranolol, disopyramide, and verapamil to human alpha(1)-acid glycoprotein. J Pharm Sci. 2000 Jun;89(6):751-7. [PubMed:10824133 ]
  3. Nakagawa T, Kishino S, Itoh S, Sugawara M, Miyazaki K: Differential binding of disopyramide and warfarin enantiomers to human alpha(1)-acid glycoprotein variants. Br J Clin Pharmacol. 2003 Dec;56(6):664-9. [PubMed:14616427 ]
  4. Haughey DB, Steinberg I, Lee MH: Protein binding of disopyramide--displacement by mono-N-dealkyldisopyramide and variation with source of alpha-1-acid glycoprotein. J Pharm Pharmacol. 1985 Apr;37(4):285-8. [PubMed:2860235 ]
  5. Brunner F, Muller WE: Prazosin binding to human alpha 1-acid glycoprotein (orosomucoid), human serum albumin, and human serum. Further characterization of the 'single drug binding site' of orosomucoid. J Pharm Pharmacol. 1985 May;37(5):305-9. [PubMed:2862237 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880 ]
  2. Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [PubMed:11758759 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [PubMed:11758759 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23