Sodium Channel Blockers

A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.
DrugDrug NameDrug Indication
DB00243RanolazineRanolazine is approved as a second-line agent in the management of chronic stable angina pectoris that is refractory to conventional anti-ischemic therapy.[A174913] Ranolazine has also been used off-label for the treatment of some arrhythmias such as ventricular tachycardia, however, this use does not have a lot of supporting evidence.[A174940] The use of ranolazine has been researched in the treatment of acute coronary syndrome, microvascular coronary dysfunction, arrhythmia, and glycemic control.[A174898]
DB00252PhenytoinFor the control of generalized tonic-clonic (grand mal) and complex partial (psychomotor, temporal lobe) seizures and prevention and treatment of seizures occurring during or following neurosurgery.
DB00280DisopyramideFor the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, ventricular pre-excitation and cardiac dysrhythmias. It is a Class Ia antiarrhythmic drug.
DB00281LidocaineLidocaine is an anesthetic of the amide group indicated for production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks [F4349, L5930].
DB00379MexiletineFor the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
DB00384TriamtereneTriamterene is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and the nephrotic syndrome; also in steroid-induced edema, idiopathic edema, and edema due to secondary hyperaldosteronism.[Label] Triamterene in combination with hydrochlorothiazide is indicated for the managment of hypertension or treatment of edema in patients who develop hypokalemia following hydrochlorothiazide monotherapy, and in patients who require thiazide diuretic and in whom the development of hypokalemia cannot be risked.[L6169] Triamterene allows the maintenance of potassium balance when given in combination with loop diuretics and thiazides.[T28]
DB00555LamotrigineIndicated as adjunctive therapy for the following seizure types in patients ≥2 years of age: partial seizures/primary generalized tonic-clonic seizures/generalized seizures of Lennox-Gastaut syndrome [FDA Label]. Indicated for conversion to monotherapy in adults (≥16 years of age) with partial seizures who are receiving treatment with carbamazepine, phenytoin, phenobarbital, primidone, or valproate as the single antiepileptic drug (AED)[FDA Label]. Indicated for the maintenance treatment of Bipolar I Disorder to delay the time to occurrence of mood episodes (depression, mania, hypomania, mixed episodes) in adults (≥18 years of age) treated for acute mood episodes with standard therapy [FDA Label].
DB00594AmilorideFor use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
DB00680MoricizineUsed to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.
DB00776OxcarbazepineFor use as monotherapy or adjunctive therapy in the treatment of partial seizures in adults with epilepsy and as adjunctive therapy in the treatment of partial seizures in children ages 4-16 with epilepsy.
DB00908QuinidineFor the treatment of ventricular pre-excitation and cardiac dysrhythmias
DB01035ProcainamideFor the treatment of life-threatening ventricular arrhythmias.
DB01056TocainideFor the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening.
DB01118AmiodaroneIntravenously, for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Orally, for the treatment of life-threatening recurrent ventricular arrhythmias such as recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia.
DB01182PropafenoneUsed to prolong the time to recurrence of paroxysmal atrial fibrillation/flutter (PAF) associated with disabling symptoms in patients without structural heart disease. Also used for the treatment of life-threatening documented ventricular arrhythmias, such as sustained ventricular tachycardia.
DB01195FlecainideFlecainide 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.
DB01228EncainideEncainide is a class Ic antiarrhythmic agent which was used for management of irregular heartbeats, such as atrial fibrillation, atrial flutter, ventricular tachycardia, and ventricular fibrillation.
DB01426AjmalineFor use as an antiarrhythmic agent.
DB01429AprindineNot Available
DB05232TetrodotoxinFor the treatment of chronic and breakthrough pain in advanced cancer patients as well as for the treatment of opioid dependence.
DB09119Eslicarbazepine acetateEslicarbazepine acetate is indicated as adjunctive therapy in the treatment of partial-onset seizures that are not adequately controlled with conventional therapy in epileptic patients.
DB12712PilsicainideNot Available
DB14575EslicarbazepineNot Available
DrugDrug NameTargetType
DB00243RanolazineCytochrome P450 3A4enzyme
DB00243RanolazineCytochrome P450 2D6enzyme
DB00243RanolazineBile salt export pumptransporter
DB00243RanolazineMultidrug resistance protein 1transporter
DB00243RanolazineSerum albumincarrier
DB00243RanolazineVoltage gated sodium channeltarget
DB00243RanolazineInward rectifier potassium channeltarget
DB00243RanolazineVoltage-dependent L-type calcium channeltarget
DB00243RanolazineAlpha-1 adrenergic receptorstarget
DB00243RanolazineBeta-1 adrenergic receptortarget
DB00243RanolazineFatty acidtarget
DB00243RanolazineAlpha-1-acid glycoprotein 1carrier
DB00252PhenytoinSodium channel protein type 5 subunit alphatarget
DB00252PhenytoinSodium channel protein type 1 subunit alphatarget
DB00252PhenytoinCytochrome P450 2C8enzyme
DB00252PhenytoinCytochrome P450 2C19enzyme
DB00252PhenytoinCytochrome P450 2C9enzyme
DB00252PhenytoinCytochrome P450 2B6enzyme
DB00252PhenytoinCytochrome P450 3A5enzyme
DB00252PhenytoinSerum albumincarrier
DB00252PhenytoinCytochrome P450 3A4enzyme
DB00252PhenytoinSolute carrier organic anion transporter family member 1C1transporter
DB00252PhenytoinMultidrug resistance protein 1transporter
DB00252PhenytoinCanalicular multispecific organic anion transporter 1transporter
DB00252PhenytoinCytochrome P450 11B1, mitochondrialenzyme
DB00252PhenytoinCytochrome P450 2C18enzyme
DB00252PhenytoinCytochrome P450 3A7enzyme
DB00252PhenytoinNuclear receptor subfamily 1 group I member 2target
DB00252PhenytoinSodium channel subunit beta-1target
DB00252PhenytoinSodium channel protein type 3 subunit alphatarget
DB00252PhenytoinUDP-glucuronosyltransferase 1-1enzyme
DB00252PhenytoinUDP-glucuronosyltransferase 1-6enzyme
DB00252PhenytoinUDP-glucuronosyltransferase 1-9enzyme
DB00252PhenytoinCytochrome P450 2D6enzyme
DB00252PhenytoinThyroxine-binding globulincarrier
DB00280DisopyramideSodium channel protein type 5 subunit alphatarget
DB00280DisopyramideAlpha-1-acid glycoprotein 1carrier
DB00280DisopyramideCytochrome P450 3A4enzyme
DB00280DisopyramideMuscarinic acetylcholine receptor M1target
DB00280DisopyramideMuscarinic acetylcholine receptor M2target
DB00280DisopyramideMuscarinic acetylcholine receptor M3target
DB00280DisopyramidePotassium voltage-gated channel subfamily D member 2target
DB00280DisopyramidePotassium voltage-gated channel subfamily D member 3target
DB00280DisopyramideSolute carrier family 22 member 2transporter
DB00280DisopyramideSolute carrier family 22 member 1transporter
DB00280DisopyramidePotassium voltage-gated channel subfamily H member 2target
DB00280DisopyramideAlpha-1-acid glycoprotein 2target
DB00280DisopyramideCytochrome P450 1A2enzyme
DB00281LidocaineSodium channel protein type 5 subunit alphatarget
DB00281LidocaineSodium channel protein type 10 subunit alphatarget
DB00281LidocaineEpidermal growth factor receptortarget
DB00281LidocaineSodium channel protein type 9 subunit alphatarget
DB00281LidocaineCytochrome P450 1A2enzyme
DB00281LidocaineCytochrome P450 2D6enzyme
DB00281LidocaineCytochrome P450 3A4enzyme
DB00281LidocaineCytochrome P450 3A5enzyme
DB00281LidocaineCytochrome P450 3A7enzyme
DB00281LidocaineSolute carrier family 22 member 5transporter
DB00281LidocaineMultidrug resistance protein 1transporter
DB00281LidocaineCytochrome P450 2A6enzyme
DB00281LidocaineCytochrome P450 2B6enzyme
DB00281LidocaineCytochrome P450 2C18enzyme
DB00281LidocaineCytochrome P450 2C8enzyme
DB00281LidocaineCytochrome P450 2C9enzyme
DB00281LidocaineSodium channel protein type 4 subunit alphatarget
DB00281LidocaineAlpha-1-acid glycoprotein 1target
DB00281LidocaineAlpha-1-acid glycoprotein 2target
DB00379MexiletineSodium channel protein type 5 subunit alphatarget
DB00379MexiletineCytochrome P450 1A2enzyme
DB00379MexiletineCytochrome P450 2D6enzyme
DB00379MexiletineCytochrome P450 2B6enzyme
DB00379MexiletineCytochrome P450 2E1enzyme
DB00379MexiletineCytochrome P450 3A4enzyme
DB00379MexiletineAryl hydrocarbon receptortarget
DB00384TriamtereneAmiloride-sensitive sodium channel subunit gammatarget
DB00384TriamtereneAmiloride-sensitive sodium channel subunit alphatarget
DB00384TriamtereneAmiloride-sensitive sodium channel subunit betatarget
DB00384TriamtereneAmiloride-sensitive sodium channel subunit deltatarget
DB00384TriamtereneCytochrome P450 1A2enzyme
DB00555LamotrigineSodium channel protein type 2 subunit alphatarget
DB00555LamotrigineUDP-glucuronosyltransferase 1-4enzyme
DB00555LamotrigineMultidrug resistance protein 1transporter
DB00555LamotrigineUDP-glucuronosyltransferase 1-3enzyme
DB00555LamotrigineDihydrofolate reductaseenzyme
DB00555Lamotrigine5-hydroxytryptamine receptor 3Atarget
DB00555LamotrigineVoltage-dependent R-type calcium channel subunit alpha-1Etarget
DB00555LamotrigineAdenosine receptor A1target
DB00555LamotrigineAdenosine receptor A2atarget
DB00555LamotrigineAlpha-1A adrenergic receptortarget
DB00555LamotrigineAlpha-2A adrenergic receptortarget
DB00555LamotrigineBeta-1 adrenergic receptortarget
DB00555LamotrigineD(1) dopamine receptortarget
DB00555LamotrigineD(2) dopamine receptortarget
DB00555LamotrigineGABA-A receptor (anion channel)target
DB00555LamotrigineGABA-A receptor (benzodiazepine site)target
DB00555LamotrigineHistamine H1 receptortarget
DB00555LamotrigineKappa-type opioid receptortarget
DB00555LamotrigineMuscarinic acetylcholine receptortarget
DB00555Lamotrigine5-hydroxytryptamine receptor 2Atarget
DB00555LamotrigineUDP-glucuronosyltransferase 1-1enzyme
DB00555LamotrigineSolute carrier family 22 member 2transporter
DB00594AmilorideAmiloride-sensitive sodium channel subunit betatarget
DB00594AmilorideAcid-sensing ion channel 1target
DB00594AmilorideAmiloride-sensitive amine oxidase [copper-containing]target
DB00594AmilorideAmiloride-sensitive sodium channel subunit alphatarget
DB00594AmilorideAmiloride-sensitive sodium channel subunit gammatarget
DB00594AmilorideSodium/hydrogen exchanger 1target
DB00594AmilorideAcid-sensing ion channel 2target
DB00594AmilorideAmiloride-sensitive sodium channel subunit deltatarget
DB00594AmilorideUrokinase-type plasminogen activatortarget
DB00594AmilorideSolute carrier family 22 member 2transporter
DB00594AmilorideSolute carrier family 22 member 4transporter
DB00594AmilorideAmiloride-sensitive amine oxidase [copper-containing]enzyme
DB00594AmilorideAmiloride-sensitive amine oxidase [copper-containing]enzyme
DB00680MoricizineSodium channel protein type 5 subunit alphatarget
DB00776OxcarbazepineSodium channel protein type 5 subunit alphatarget
DB00776OxcarbazepineCytochrome P450 2C19enzyme
DB00776OxcarbazepineCytochrome P450 3A4enzyme
DB00776OxcarbazepineCytochrome P450 3A5enzyme
DB00776OxcarbazepineSerum albumincarrier
DB00776OxcarbazepineUDP-glucuronosyltransferase 1-1enzyme
DB00776OxcarbazepineMultidrug resistance protein 1transporter
DB00908QuinidineSodium channel protein type 5 subunit alphatarget
DB00908QuinidineAlpha-1-acid glycoprotein 1carrier
DB00908QuinidinePotassium voltage-gated channel subfamily H member 2target
DB00908QuinidinePotassium channel subfamily K member 1target
DB00908QuinidinePotassium channel subfamily K member 6target
DB00908QuinidineCytochrome P450 1A2enzyme
DB00908QuinidineCytochrome P450 2E1enzyme
DB00908QuinidineCytochrome P450 1A1enzyme
DB00908QuinidineCytochrome P450 2D6enzyme
DB00908QuinidineCytochrome P450 3A4enzyme
DB00908QuinidineCytochrome P450 3A7enzyme
DB00908QuinidineSolute carrier family 22 member 2transporter
DB00908QuinidineSolute carrier family 22 member 1transporter
DB00908QuinidineSolute carrier family 22 member 5transporter
DB00908QuinidineMultidrug resistance protein 1transporter
DB00908QuinidineSolute carrier organic anion transporter family member 1A2transporter
DB00908QuinidineSolute carrier family 22 member 8transporter
DB00908QuinidineCanalicular multispecific organic anion transporter 1transporter
DB00908QuinidineSolute carrier family 22 member 4transporter
DB00908QuinidineSolute carrier organic anion transporter family member 1B1transporter
DB00908QuinidineCytochrome P450 2B6enzyme
DB00908QuinidineCytochrome P450 2C9enzyme
DB00908QuinidineAlpha-1A adrenergic receptortarget
DB00908QuinidineAlpha-1B adrenergic receptortarget
DB00908QuinidineAlpha-1D adrenergic receptortarget
DB00908QuinidineBile salt export pumptransporter
DB00908QuinidineCytochrome P450 2C8enzyme
DB01035ProcainamideSodium channel protein type 5 subunit alphatarget
DB01035ProcainamideDNA (cytosine-5)-methyltransferase 1target
DB01035ProcainamideCytochrome P450 2D6enzyme
DB01035ProcainamideCholinesteraseenzyme
DB01035ProcainamideSolute carrier family 22 member 2transporter
DB01035ProcainamideSolute carrier family 22 member 1transporter
DB01035ProcainamideSolute carrier family 22 member 3transporter
DB01035ProcainamideSolute carrier family 22 member 5transporter
DB01035ProcainamideSolute carrier family 22 member 4transporter
DB01035ProcainamidePotassium voltage-gated channel subfamily H member 2target
DB01035ProcainamideMultidrug and toxin extrusion protein 1transporter
DB01035ProcainamideMultidrug and toxin extrusion protein 2transporter
DB01056TocainideSodium channel protein type 5 subunit alphatarget
DB01056TocainideSerum albumincarrier
DB01056TocainideCytochrome P450 1A2enzyme
DB01118AmiodaroneBeta-1 adrenergic receptortarget
DB01118AmiodaronePotassium voltage-gated channel subfamily H member 2target
DB01118AmiodaroneCytochrome P450 2C8enzyme
DB01118AmiodaroneCytochrome P450 2C9enzyme
DB01118AmiodaroneCytochrome P450 2D6enzyme
DB01118AmiodaroneVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01118AmiodaroneVoltage-dependent calcium channel subunit alpha-2/delta-2target
DB01118AmiodaroneCytochrome P450 3A4enzyme
DB01118AmiodaroneCytochrome P450 1A2enzyme
DB01118AmiodaroneCytochrome P450 3A5enzyme
DB01118AmiodaroneCytochrome P450 3A7enzyme
DB01118AmiodaroneCytochrome P450 1A1enzyme
DB01118AmiodaroneMultidrug resistance protein 1transporter
DB01118AmiodaroneCytochrome P450 2C19enzyme
DB01118AmiodaroneCytochrome P450 2A6enzyme
DB01118AmiodaroneThyroid hormone receptor alphatarget
DB01118AmiodaroneThyroid hormone receptor betatarget
DB01118AmiodaronePeroxisome proliferator-activated receptor gammatarget
DB01118AmiodaroneBile salt export pumptransporter
DB01118AmiodaroneSolute carrier family 22 member 2transporter
DB01182PropafenoneSodium channel protein type 5 subunit alphatarget
DB01182PropafenonePotassium voltage-gated channel subfamily H member 2target
DB01182PropafenoneCytochrome P450 1A2enzyme
DB01182PropafenoneCytochrome P450 2D6enzyme
DB01182PropafenoneCytochrome P450 2C8enzyme
DB01182PropafenoneCytochrome P450 3A4enzyme
DB01182PropafenoneMultidrug resistance protein 1transporter
DB01182PropafenoneBeta-1 adrenergic receptortarget
DB01182PropafenoneBeta-2 adrenergic receptortarget
DB01195FlecainideSodium channel protein type 5 subunit alphatarget
DB01195FlecainideCytochrome P450 2D6enzyme
DB01195FlecainideSodium channel protein type 4 subunit alphatarget
DB01195FlecainideCytochrome P450 2C9enzyme
DB01195FlecainidePotassium voltage-gated channel subfamily H member 2target
DB01228EncainideSodium channel protein type 5 subunit alphatarget
DB01228EncainideCytochrome P450 2D6enzyme
DB01426AjmalineAlpha-1-acid glycoprotein 1carrier
DB01426AjmalineSodium channel protein type 5 subunit alphatarget
DB01429AprindineAlpha-1-acid glycoprotein 1carrier
DB01429AprindineCalmodulintarget
DB01429AprindineSodium channel protein type 5 subunit alphatarget
DB01429AprindineCytochrome P450 2D6enzyme
DB05232TetrodotoxinSodium channel protein type 1 subunit alphatarget
DB05232TetrodotoxinSodium channel protein type 2 subunit alphatarget
DB05232TetrodotoxinSodium channel protein type 3 subunit alphatarget
DB05232TetrodotoxinSodium channel protein type 8 subunit alphatarget
DB09119Eslicarbazepine acetateCytochrome P450 2C19enzyme
DB09119Eslicarbazepine acetateCytochrome P450 3A4enzyme
DB09119Eslicarbazepine acetateP2X purinoceptor 4target
DB09119Eslicarbazepine acetateUDP-glucuronosyltransferase 1-1enzyme
DB12712PilsicainideBile salt export pumptransporter
DB14575EslicarbazepineUDP-glucuronosyltransferase 1-1enzyme
DB14575EslicarbazepineCytochrome P450 2C19enzyme
DB14575EslicarbazepineCytochrome P450 3A4enzyme
DB14575EslicarbazepineP2X purinoceptor 4target