Identification

Name
Flecainide
Accession Number
DB01195  (APRD00129)
Type
Small Molecule
Groups
Approved, Withdrawn
Description

A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial arrhythmias and tachycardias. Paradoxically, however, in myocardial infarct patients with either symptomatic or asymptomatic arrhythmia, flecainide exacerbates the arrhythmia and is not recommended for use in these patients.

Structure
Thumb
Synonyms
  • (±)-flecainide
  • Flecaine
  • Flecainida
  • Flecainide
  • Flécaïnide
  • Flecainidum
  • N-(2-Piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
External IDs
CCRIS 313
Product Ingredients
IngredientUNIICASInChI Key
Flecainide acetateM8U465Q1WQ54143-56-5RKXNZRPQSOPPRN-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Flecainide AcetateTablet50 mg/1OralMylan Pharmaceuticals2011-08-022011-11-30Us
Flecainide acetateTablet100 mg/1OralCounty Line Pharmaceuticals, LLC2016-11-04Not applicableUs
Flecainide AcetateTablet150 mg/1OralMylan Pharmaceuticals2011-08-022011-11-30Us
Flecainide AcetateTablet100 mg/1OralMylan Pharmaceuticals2011-08-022012-03-31Us
Flecainide acetateTablet50 mg/1OralCounty Line Pharmaceuticals, LLC2016-11-04Not applicableUs
Flecainide acetateTablet150 mg/1OralCounty Line Pharmaceuticals, LLC2016-11-04Not applicableUs
TambocorTablet50 mgOralValeant Canada Lp Valeant Canada S.E.C.1988-12-31Not applicableCanada
TambocorTablet50000 ug/1Oral3M Company1985-10-312006-12-29Us
TambocorTablet50 mg/1OralMedicis Pharmaceutical Corporation2011-11-282013-04-30Us
TambocorTablet150000 ug/1Oral3M Company1985-10-312006-12-29Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-flecainideTablet50 mgOralApotex Corporation2006-05-08Not applicableCanada
Apo-flecainideTablet100 mgOralApotex Corporation2006-05-08Not applicableCanada
Auro-flecainideTablet50 mgOralAuro Pharma Inc2017-02-27Not applicableCanada
Auro-flecainideTablet100 mgOralAuro Pharma Inc2017-02-27Not applicableCanada
Flecainide AcetateTablet100 mg/1OralAmneal Pharmaceuticals of New York Llc2009-12-01Not applicableUs
Flecainide AcetateTablet150 mg/1OralAvPAK2015-02-12Not applicableUs
Flecainide AcetateTablet150 mg/1OralRising Health, Llc2015-07-08Not applicableUs
Flecainide AcetateTablet100 mg/1OralApotex Corp.2009-07-09Not applicableUs
Flecainide AcetateTablet50 mg/1OralBarr Laboratories2002-11-182017-07-31Us00555 0859 02 nlmimage10 512f2899
Flecainide AcetateTablet150 mg/1OralPhysicians Total Care, Inc.2008-09-30Not applicableUs
International/Other Brands
Almarytm / Apocard
Categories
UNII
K94FTS1806
CAS number
54143-55-4
Weight
Average: 414.3427
Monoisotopic: 414.137811746
Chemical Formula
C17H20F6N2O3
InChI Key
DJBNUMBKLMJRSA-UHFFFAOYSA-N
InChI
InChI=1S/C17H20F6N2O3/c18-16(19,20)9-27-12-4-5-14(28-10-17(21,22)23)13(7-12)15(26)25-8-11-3-1-2-6-24-11/h4-5,7,11,24H,1-3,6,8-10H2,(H,25,26)
IUPAC Name
N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
SMILES
FC(F)(F)COC1=CC(C(=O)NCC2CCCCN2)=C(OCC(F)(F)F)C=C1

Pharmacology

Indication

Flecainide is is a class Ic antiarrhythmic agent and as such, it is used for the prevention of paroxysmal supraventricular tachycardias (PSVT), including atrioventricular nodal reentrant tachycardia, atrioventricular reentrant tachycardia and other supraventricular tachycardias of unspecified mechanism associated with disablin.

Associated Conditions
Pharmacodynamics

Flecainide has local anesthetic activity and belongs to the membrane stabilizing (Class 1) group of antiarrhythmic agents; it has electrophysiologic effects characteristic of the IC class of antiarrhythmics.

Mechanism of action

Flecainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. Flecainide is a sodium channel blocker, binding to voltage gated sodium channels. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole.

TargetActionsOrganism
ASodium channel protein type 5 subunit alpha
inhibitor
Human
ASodium channel protein type 4 subunit alpha
inhibitor
Human
UPotassium voltage-gated channel subfamily H member 2
inhibitor
Human
Absorption

Nearly complete following oral administration.

Volume of distribution
Not Available
Protein binding

40%

Metabolism

Hepatic. Flecainide does not undergo any consequential presystemic biotransformation. The two major urinary metabolites are meta-O-dealkylated flecainide (active, but about one-fifth as potent) and the meta-O-dealkylated lactam of flecainide (non-active metabolite).

Route of elimination

In healthy subjects, about 30% of a single oral dose (range, 10 to 50%) is excreted in urine as unchanged drug. Several minor metabolites (3% of the dose or less) are also found in urine; only 5% of an oral dose is excreted in feces. In patients, free (unconjugated) plasma levels of the two major metabolites are very low (less than 0.05 μg/mL).

Half life

20 hours (range 12-27 hours)

Clearance
Not Available
Toxicity

Oral LD50 is 50-498 mg/kg in rat. Symptoms of overdose include nausea and vomiting, convulsions, hypotension, bradycardia, syncope, extreme widening of the QRS complex, widening of the QT interval, widening of the PR interval, ventricular tachycardia, AV nodal block, asystole, bundle branch block, cardiac failure, and cardiac arrest.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Flecainide Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Flecainide.
4-MethoxyamphetamineThe metabolism of Flecainide can be decreased when combined with 4-Methoxyamphetamine.
AbataceptThe metabolism of Flecainide can be increased when combined with Abatacept.
AbexinostatThe risk or severity of QTc prolongation can be increased when Flecainide is combined with Abexinostat.
AbirateroneThe metabolism of Flecainide can be decreased when combined with Abiraterone.
AcebutololThe metabolism of Flecainide can be decreased when combined with Acebutolol.
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Flecainide.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Flecainide.
AceprometazineThe risk or severity of QTc prolongation can be increased when Flecainide is combined with Aceprometazine.
AcetaminophenThe metabolism of Flecainide can be decreased when combined with Acetaminophen.
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Bmitt, E.H. and Brown, W.R.; U.S. Patent 3,900,481; August 19,1975; assigned to Riker Laboratories, Inc.

US3900481A
General References
  1. Gill JS, Mehta D, Ward DE, Camm AJ: Efficacy of flecainide, sotalol, and verapamil in the treatment of right ventricular tachycardia in patients without overt cardiac abnormality. Br Heart J. 1992 Oct;68(4):392-7. [PubMed:1449923]
  2. Sakurada H, Hiyoshi Y, Tejima T, Yanase O, Tokuyasu Y, Watanabe K, Motomiya T, Sugiura M, Hiraoka M: [Effects of oral flecainide treatment of refractory tachyarrhythmias]. Kokyu To Junkan. 1990 May;38(5):471-6. [PubMed:2115193]
  3. Echt DS, Liebson PR, Mitchell LB, Peters RW, Obias-Manno D, Barker AH, Arensberg D, Baker A, Friedman L, Greene HL, et al.: Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial. N Engl J Med. 1991 Mar 21;324(12):781-8. [PubMed:1900101]
  4. Greenberg HM, Dwyer EM Jr, Hochman JS, Steinberg JS, Echt DS, Peters RW: Interaction of ischaemia and encainide/flecainide treatment: a proposed mechanism for the increased mortality in CAST I. Br Heart J. 1995 Dec;74(6):631-5. [PubMed:8541168]
  5. Gasparini M, Priori SG, Mantica M, Napolitano C, Galimberti P, Ceriotti C, Simonini S: Flecainide test in Brugada syndrome: a reproducible but risky tool. Pacing Clin Electrophysiol. 2003 Jan;26(1 Pt 2):338-41. [PubMed:12687841]
External Links
Human Metabolome Database
HMDB0015326
KEGG Drug
D07962
KEGG Compound
C07001
PubChem Compound
3356
PubChem Substance
46508078
ChemSpider
3239
BindingDB
50131434
ChEBI
75984
ChEMBL
CHEMBL652
Therapeutic Targets Database
DAP000518
PharmGKB
PA449646
IUPHAR
2560
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Flecainide
ATC Codes
C01BC04 — Flecainide
AHFS Codes
  • 24:04.04.12 — Class IC Antiarrythmics
MSDS
Download (77.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedSupportive CarePain NOS1
2CompletedTreatmentArrhythmia of ventricular origin / Arrythmias / Cardiovascular Disease (CVD) / Heart Diseases1
2CompletedTreatmentFailed First Radiofrequency Ablation Procedure / Paroxysmal Atrial Fibrillation (PAF)1
2RecruitingTreatmentNarcolepsy1
2RecruitingTreatmentParoxysmal Atrial Fibrillation (PAF)1
3CompletedPreventionArrhythmia of ventricular origin / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Death, Sudden,Cardiac / Heart Arrest / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
3CompletedTreatmentArrythmias / Cardiovascular Disease (CVD) / Heart Diseases / Nonvalvular Atrial Fibrillation1
3CompletedTreatmentParoxysmal Atrial Fibrillation (PAF)1
3Enrolling by InvitationTreatmentFetal Atrial Flutter Without Hydrops / Fetal Supraventricular Tachycardia With Hydrops / Fetal Supraventricular Tachycardia Without Hydrops1
3SuspendedTreatmentNonvalvular Atrial Fibrillation1
4CompletedTreatmentBrugada Syndrome / Nonvalvular Atrial Fibrillation / Ventricular Tachycardia (VT)1
4RecruitingTreatmentCarvedilol / Outflow Tract / Ventricular Premature Complexes1
4RecruitingTreatmentNonvalvular Atrial Fibrillation1
4RecruitingTreatmentParoxysmal Atrial Fibrillation (PAF)1
4TerminatedTreatmentNonvalvular Atrial Fibrillation1
4Unknown StatusDiagnosticNonvalvular Atrial Fibrillation1
4WithdrawnTreatmentNonvalvular Atrial Fibrillation1
Not AvailableActive Not RecruitingTreatmentNonvalvular Atrial Fibrillation1
Not AvailableActive Not RecruitingTreatmentNonvalvular Atrial Fibrillation / Quality of Life1
Not AvailableCompletedTreatmentCatecholaminergic Polymorphic Ventricular Tachycardia (CPVT)1
Not AvailableCompletedTreatmentNonvalvular Atrial Fibrillation2
Not AvailableRecruitingTreatmentHeart Failure, Unspecified / Recurrent Atrial Fibrillation1
Not AvailableRecruitingTreatmentNonvalvular Atrial Fibrillation1
Not AvailableTerminatedBasic ScienceBlood Pressures / Ventricular Premature Complexes1
Not AvailableUnknown StatusTreatmentPersistent Atrial Fibrillation1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • 3M Health Care
  • Alphapharm Party Ltd.
  • Amneal Pharmaceuticals
  • AQ Pharmaceuticals Inc.
  • Barr Pharmaceuticals
  • Graceway Pharmaceuticals
  • Kaiser Foundation Hospital
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Ohm Laboratories Inc.
  • Par Pharmaceuticals
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Ranbaxy Laboratories
  • Roxane Labs
  • Southwood Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral50 mg
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral50 mg/1
TabletOral100000 ug/1
TabletOral150000 ug/1
TabletOral50000 ug/1
Prices
Unit descriptionCostUnit
Tambocor 150 mg tablet5.75USD tablet
Tambocor 100 mg tablet4.27USD tablet
Flecainide acetate 150 mg tablet3.83USD tablet
Flecainide acetate 100 mg tablet2.95USD tablet
Tambocor 50 mg tablet2.72USD tablet
Flecainide acetate 50 mg tablet1.95USD tablet
Tambocor 100 mg Tablet1.19USD tablet
Apo-Flecainide 100 mg Tablet0.83USD tablet
Tambocor 50 mg Tablet0.6USD tablet
Apo-Flecainide 50 mg Tablet0.41USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)228-229Bmitt, E.H. and Brown, W.R.; U.S. Patent 3,900,481; August 19,1975; assigned to Riker Laboratories, Inc.
water solubility48.4 mg/mL at 37 °C (acetate form)Not Available
logP3.78MANNHOLD,R ET AL. (1990)
pKa9.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0324 mg/mLALOGPS
logP2.98ALOGPS
logP3.19ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)13.68ChemAxon
pKa (Strongest Basic)9.62ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area59.59 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity88.4 m3·mol-1ChemAxon
Polarizability35.92 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9856
Blood Brain Barrier+0.8605
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7773
P-glycoprotein inhibitor IInhibitor0.5307
P-glycoprotein inhibitor IINon-inhibitor0.7716
Renal organic cation transporterNon-inhibitor0.6687
CYP450 2C9 substrateNon-substrate0.8921
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.5957
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.6853
CYP450 2D6 inhibitorNon-inhibitor0.6556
CYP450 2C19 inhibitorInhibitor0.5307
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5538
Ames testNon AMES toxic0.672
CarcinogenicityNon-carcinogens0.8821
BiodegradationNot ready biodegradable0.9968
Rat acute toxicity2.5680 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9409
hERG inhibition (predictor II)Inhibitor0.8474
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-001i-9000000000-b732167df77d39193144
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00dl-0095000000-644485d209c90776a32d
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00di-0190000000-201f2152d161a1ff83e5
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00di-0790000000-928874c4b348381ad1b8
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0596-0940000000-ee7a94ba0d7bcfa2fe93
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-052g-1910000000-a32ac2f605f11fbbc5e0
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0297-1900000000-f1c49d25a6b161ff44d9
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0000900000-9820e909cb01d45fa815
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00kb-2009500000-68b872fada8afdd4e580
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f6t-5019000000-8fa5e4257c88beda0ea1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uea-8069000000-149a79cf429446ec77c2
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uei-6292000000-103ccdef98c4b6c9e408
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0pdi-8970000000-9258d139b203d6c98df0

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzamides. These are organic compounds containing a carboxamido substituent attached to a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
Benzamides
Alternative Parents
Phenoxy compounds / Phenol ethers / Benzoyl derivatives / Alkyl aryl ethers / Piperidines / Secondary carboxylic acid amides / Amino acids and derivatives / Dialkylamines / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
Benzamide / Phenoxy compound / Benzoyl / Phenol ether / Alkyl aryl ether / Piperidine / Amino acid or derivatives / Carboxamide group / Secondary carboxylic acid amide / Carboxylic acid derivative
show 18 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
piperidines, organofluorine compound, aromatic ether, monocarboxylic acid amide (CHEBI:75984)

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 pr...
Gene Name
SCN5A
Uniprot ID
Q14524
Uniprot Name
Sodium channel protein type 5 subunit alpha
Molecular Weight
226937.475 Da
References
  1. Nagatomo T, January CT, Makielski JC: Preferential block of late sodium current in the LQT3 DeltaKPQ mutant by the class I(C) antiarrhythmic flecainide. Mol Pharmacol. 2000 Jan;57(1):101-7. [PubMed:10617684]
  2. Benhorin J, Taub R, Goldmit M, Kerem B, Kass RS, Windman I, Medina A: Effects of flecainide in patients with new SCN5A mutation: mutation-specific therapy for long-QT syndrome? Circulation. 2000 Apr 11;101(14):1698-706. [PubMed:10758053]
  3. Priori SG, Napolitano C, Schwartz PJ, Bloise R, Crotti L, Ronchetti E: The elusive link between LQT3 and Brugada syndrome: the role of flecainide challenge. Circulation. 2000 Aug 29;102(9):945-7. [PubMed:10961955]
  4. Cerrone M, Crotti L, Faggiano G, De Michelis V, Napolitano C, Schwartz PJ, Priori SG: [Long QT syndrome and Brugada syndrome: 2 aspects of the same disease?]. Ital Heart J Suppl. 2001 Mar;2(3):253-7. [PubMed:11307783]
  5. Viswanathan PC, Bezzina CR, George AL Jr, Roden DM, Wilde AA, Balser JR: Gating-dependent mechanisms for flecainide action in SCN5A-linked arrhythmia syndromes. Circulation. 2001 Sep 4;104(10):1200-5. [PubMed:11535580]
  6. Ramos E, O'leary ME: State-dependent trapping of flecainide in the cardiac sodium channel. J Physiol. 2004 Oct 1;560(Pt 1):37-49. Epub 2004 Jul 22. [PubMed:15272045]
  7. 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]
  8. Liu H, Atkins J, Kass RS: Common molecular determinants of flecainide and lidocaine block of heart Na+ channels: evidence from experiments with neutral and quaternary flecainide analogues. J Gen Physiol. 2003 Mar;121(3):199-214. [PubMed:12601084]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity
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 pr...
Gene Name
SCN4A
Uniprot ID
P35499
Uniprot Name
Sodium channel protein type 4 subunit alpha
Molecular Weight
208059.175 Da
References
  1. Desaphy JF, De Luca A, Didonna MP, George AL Jr, Camerino Conte D: Different flecainide sensitivity of hNav1.4 channels and myotonic mutants explained by state-dependent block. J Physiol. 2004 Jan 15;554(Pt 2):321-34. Epub 2003 Nov 7. [PubMed:14608015]
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 ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
Molecular Weight
126653.52 Da
References
  1. Chiu PJ, Marcoe KF, Bounds SE, Lin CH, Feng JJ, Lin A, Cheng FC, Crumb WJ, Mitchell R: Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci. 2004 Jul;95(3):311-9. [PubMed:15272206]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Enzyme inhibition data based on findings of 1 in vitro study.
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Walker DK, Alabaster CT, Congrave GS, Hargreaves MB, Hyland R, Jones BC, Reed LJ, Smith DA: Significance of metabolism in the disposition and action of the antidysrhythmic drug, dofetilide. In vitro studies and correlation with in vivo data. Drug Metab Dispos. 1996 Apr;24(4):447-55. [PubMed:8801060]

Drug created on June 13, 2005 07:24 / Updated on December 16, 2018 23:30