Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMK0GHV)

• Drug Name: Encainide Drug Info
• Synonyms: Encainida; Encainidum; Enkaid; Encainida [Spanish]; Encainide [French]; Encainidum [Latin]; No stereochem; MJ 9067; Encainide (INN); Encainide [INN:BAN]; MJ-9067; MJ-9067-1; Encainide Hydrochloride, (+-)-Isomer; (+-)-2'-[2-(1-methyl-2-piperidyl)ethyl]-p-anisanilide; (+-)-4-Methoxy-N-(2-(2-(1-methyl-2-piperidinyl)ethyl)phenyl)benzamide; (+/-)-4-Methoxy-N-[2-[2-(1-methyl-2-piperidinyl)ethyl]phenyl]benzamide; 4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide; 4-methoxy-N-[2-[2-(1-methylpiperidin-2-yl)ethyl]phenyl]benzamide; 4-methoxy-N-{2-[2-(1-methylpiperidin-2-yl)ethyl]phenyl}benzamide

Indication

Disease Entry	ICD 11	Status	REF
Heart arrhythmia	BC65	Withdrawn from market	[1]

• Therapeutic Class: Antiarrhythmic Agents
• Cross-matching ID:
  PubChem CID: 48041
  ChEBI ID: CHEBI:4788
  CAS Number: CAS 66778-36-7
  TTD Drug ID: DMK0GHV
  INTEDE Drug ID: DR0575

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated sodium channel alpha Nav1.5 (SCN5A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mephenytoin	DM5UGDK	Epilepsy	8A60-8A68	Approved	[4]
Mexiletine	DMCTE9R	Ventricular tachycardia	BC71	Approved	[5]
Fosphenytoin	DMOX3LB	Epilepsy	8A60-8A68	Approved	[4]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[5]
LOMERIZINE	DME0TC8	Migraine	8A80	Approved	[6]
Tetrodotoxin	DMWMPRG	Bacterial infection	1A00-1C4Z	Approved	[7]
Dyclonine	DMU6OFP	Pain	MG30-MG3Z	Approved	[8]
Moricizine	DMOMBJW	Arrhythmia	BC9Z	Approved	[2]
Ethotoin	DMXWOCP	Complex partial seizure	8A68.0	Approved	[9]
Prilocaine	DMI7DZ2	Pain	MG30-MG3Z	Approved	[8]

Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[10]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[11]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[12]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[13]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[14]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[15]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[16]
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[17]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[18]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.5 (SCN5A)	TTZOVE0	SCN5A_HUMAN	Blocker	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2D6 (CYP2D6) Main DME	DECB0K3	CP2D6_HUMAN	Substrate	[3]

References

• [1] New antiarrhythmic drugs: tocainide, mexiletine, flecainide, encainide, and amiodarone. Mayo Clin Proc. 1987 Nov;62(11):1033-50.
• [2] From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33.
• [3] Effects of the antifungal agents on oxidative drug metabolism: clinical relevance. Clin Pharmacokinet. 2000 Feb;38(2):111-80.
• [4] Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68.
• [5] 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.
• [6] Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37.
• [7] Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81.
• [8] Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12.
• [9] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [10] Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
• [11] Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
• [12] CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
• [13] Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
• [14] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
• [15] Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
• [16] Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
• [17] Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
• [18] Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
• [19] Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.