Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index

DrugDrug NameDrug Description
DB01418AcenocoumarolAn anticoagulant drug used in the prevention of thromboembolic diseases in infarction and transient ischemic attacks, as well as management of deep vein thrombosis and myocardial infarction.
DB01223AminophyllineA bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
DB01118AmiodaroneA class III antiarrhythmic indicated for the treatment of recurrent hemodynamically unstable ventricular tachycardia and recurrent ventricular fibrillation.
DB00321AmitriptylineA tricyclic antidepressant indicated in the treatment of depressive illness, either endogenous or psychotic, and to relieve depression associated anxiety.
DB00564CarbamazepineAn anticonvulsant used to treat various types of seizures and pain resulting from trigeminal neuralgia.
DB01242ClomipramineA tricyclic antidepressant used in the treatment of obsessive-compulsive disorder and disorders with an obsessive-compulsive component, such as depression, schizophrenia, and Tourette’s disorder.
DB00575ClonidineAn alpha-2 adrenergic agonist used to treat hypertension and severe cancer pain, among other conditions, and to treat withdrawal symptoms from various substances. It is also used to aid in the diagnosis of pheochromocytoma and to prevent migraines.
DB00924CyclobenzaprineA skeletal muscle relaxant that works on the brainstem to treat muscle spasms of local origin.
DB01151DesipramineA tricyclic antidepressant used in the treatment of depression.
DB01142DoxepinA psychotropic agent used for the treatment of depression, anxiety, manic-depressive disorder, and insomnia.
DB00458ImipramineA tricyclic antidepressant indicated for the treatment of depression and to reduce childhood enuresis.
DB00532MephenytoinA phenylhydantoin used to treat refractory partial epilepsy.
DB00540NortriptylineA tricyclic antidepressant used in the treatment of depression.
DB01100PimozideAn antipsychotic used to manage debilitating motor and phonic tics in patients with Tourette's Disorder.
DB00277TheophyllineA xanthine used to manage the symptoms of asthma, COPD, and other lung conditions caused by reversible airflow obstruction.
DB00682WarfarinA vitamin K antagonist used to treat venous thromboembolism, pulmonary embolism, thromboembolism with atrial fibrillation, thromboembolism with cardiac valve replacement, and thromboembolic events post myocardial infarction.
DB00697TizanidineAn alpha-2 adrenergic agonist used for the short-term treatment of muscle spasticity.
DrugDrug NameTargetType
DB01418AcenocoumarolVitamin K epoxide reductase complex subunit 1target
DB01418AcenocoumarolCytochrome P450 2C9enzyme
DB01418AcenocoumarolCytochrome P450 1A2enzyme
DB01418AcenocoumarolSerum albumincarrier
DB01418AcenocoumarolAlpha-1-acid glycoprotein 1carrier
DB01418AcenocoumarolCytochrome P450 2C19enzyme
DB01418AcenocoumarolCytochrome P450 3A4enzyme
DB01418AcenocoumarolP-glycoprotein 1transporter
DB01223AminophyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
DB01223AminophyllineAdenosine receptor A3target
DB01223AminophyllineAdenosine receptor A1target
DB01223AminophyllineCytochrome P450 1A2enzyme
DB01223AminophyllineCytochrome P450 2E1enzyme
DB01223AminophyllineCytochrome P450 3A4enzyme
DB01223AminophyllineHistone deacetylase 2target
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 1A1enzyme
DB01118AmiodaroneP-glycoprotein 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
DB01118AmiodaroneCytochrome P450 2J2enzyme
DB00321AmitriptylineSodium-dependent serotonin transportertarget
DB00321AmitriptylineSodium-dependent noradrenaline transportertarget
DB00321AmitriptylinePotassium voltage-gated channel subfamily KQT member 2target
DB00321AmitriptylineAlpha-2A adrenergic receptortarget
DB00321AmitriptylineCytochrome P450 1A2enzyme
DB00321AmitriptylineCytochrome P450 2C19enzyme
DB00321AmitriptylineCytochrome P450 2D6enzyme
DB00321AmitriptylineSerum albumincarrier
DB00321AmitriptylineAlpha-1-acid glycoprotein 1carrier
DB00321AmitriptylineHistamine H1 receptortarget
DB00321Amitriptyline5-hydroxytryptamine receptor 2Atarget
DB00321Amitriptyline5-hydroxytryptamine receptor 1Atarget
DB00321AmitriptylineAlpha-1A adrenergic receptortarget
DB00321AmitriptylineCytochrome P450 3A4enzyme
DB00321AmitriptylineCytochrome P450 3A5enzyme
DB00321AmitriptylinePotassium voltage-gated channel subfamily A member 1target
DB00321AmitriptylineAlpha-1D adrenergic receptortarget
DB00321AmitriptylineDelta-type opioid receptortarget
DB00321AmitriptylineKappa-type opioid receptortarget
DB00321AmitriptylineHigh affinity nerve growth factor receptortarget
DB00321AmitriptylineBDNF/NT-3 growth factors receptortarget
DB00321AmitriptylineCytochrome P450 2C9enzyme
DB00321AmitriptylineCytochrome P450 2B6enzyme
DB00321AmitriptylineCytochrome P450 2C8enzyme
DB00321AmitriptylineHistamine H2 receptortarget
DB00321AmitriptylineHistamine H4 receptortarget
DB00321AmitriptylineSigma non-opioid intracellular receptor 1target
DB00321Amitriptyline5-hydroxytryptamine receptor 2Ctarget
DB00321AmitriptylineAlpha-1B adrenergic receptortarget
DB00321Amitriptyline5-hydroxytryptamine receptor 7target
DB00321Amitriptyline5-hydroxytryptamine receptor 1Dtarget
DB00321AmitriptylineMu-type opioid receptortarget
DB00321Amitriptyline5-hydroxytryptamine receptor 1Btarget
DB00321Amitriptyline5-hydroxytryptamine receptor 6target
DB00321AmitriptylinePotassium voltage-gated channel subfamily KQT member 3target
DB00321AmitriptylineUDP-glucuronosyltransferase 2B10enzyme
DB00321Amitriptyline5-hydroxytryptamine receptor 1Ctarget
DB00321AmitriptylineMuscarinic acetylcholine receptortarget
DB00321AmitriptylineHERG human cardiac K+ channeltarget
DB00321AmitriptylineP-glycoprotein 1transporter
DB00321AmitriptylineUDP-glucuronosyltransferase 1-4enzyme
DB00564CarbamazepineVoltage-gated sodium channel alpha subunittarget
DB00564CarbamazepineCytochrome P450 2C8enzyme
DB00564CarbamazepineCytochrome P450 2B6enzyme
DB00564CarbamazepineCytochrome P450 3A4enzyme
DB00564CarbamazepineCytochrome P450 1A2enzyme
DB00564CarbamazepineCytochrome P450 2C19enzyme
DB00564CarbamazepineCytochrome P450 2C9enzyme
DB00564CarbamazepineP-glycoprotein 1transporter
DB00564CarbamazepineCytochrome P450 3A5enzyme
DB00564CarbamazepineUDP-glucuronosyltransferase 2B7enzyme
DB00564CarbamazepineRalA-binding protein 1transporter
DB00564CarbamazepineCanalicular multispecific organic anion transporter 1transporter
DB00564CarbamazepineNeuronal acetylcholine receptor subunit alpha-4target
DB00564CarbamazepineNuclear receptor subfamily 1 group I member 2target
DB00564CarbamazepineUDP-glucuronosyltransferase 1-1enzyme
DB00564CarbamazepineUDP-glucuronosyltransferase 1-6enzyme
DB00564CarbamazepineUDP-glucuronosyltransferase 1-7enzyme
DB01242ClomipramineSodium-dependent serotonin transportertarget
DB01242ClomipramineSodium-dependent noradrenaline transportertarget
DB01242ClomipramineGlutathione S-transferase Ptarget
DB01242Clomipramine5-hydroxytryptamine receptor 2Atarget
DB01242ClomipramineCytochrome P450 1A2enzyme
DB01242ClomipramineCytochrome P450 2D6enzyme
DB01242ClomipramineCytochrome P450 2C19enzyme
DB01242ClomipramineP-glycoprotein 1transporter
DB01242ClomipramineCytochrome P450 3A4enzyme
DB01242Clomipramine5-hydroxytryptamine receptor 2Btarget
DB01242Clomipramine5-hydroxytryptamine receptor 2Ctarget
DB01242ClomipramineSerum albumincarrier
DB00575ClonidineAlpha-2A adrenergic receptortarget
DB00575ClonidineCytochrome P450 2D6enzyme
DB00575ClonidineAlpha-2B adrenergic receptortarget
DB00575ClonidineAlpha-2C adrenergic receptortarget
DB00575ClonidineSolute carrier family 22 member 3transporter
DB00575ClonidineSolute carrier family 22 member 5transporter
DB00575ClonidineSolute carrier family 22 member 4transporter
DB00575ClonidineP-glycoprotein 1transporter
DB00575ClonidineCytochrome P450 1A2enzyme
DB00575ClonidineCytochrome P450 3A4enzyme
DB00575ClonidineCytochrome P450 1A1enzyme
DB00575ClonidineCytochrome P450 3A5enzyme
DB00575ClonidineAlpha-1A adrenergic receptortarget
DB00575ClonidineAlpha-1B adrenergic receptortarget
DB00575ClonidineAlpha-1D adrenergic receptortarget
DB00575ClonidineSerum albumincarrier
DB00924Cyclobenzaprine5-hydroxytryptamine receptor 2Atarget
DB00924CyclobenzaprineCytochrome P450 1A2enzyme
DB00924CyclobenzaprineCytochrome P450 3A4enzyme
DB00924CyclobenzaprineCytochrome P450 2D6enzyme
DB00924CyclobenzaprineSerum albumincarrier
DB00924CyclobenzaprineUDP-glucuronosyltransferase 1-4enzyme
DB00924CyclobenzaprineUDP-glucuronosyltransferase 2B10enzyme
DB00924Cyclobenzaprine5-hydroxytryptamine receptor 2Btarget
DB00924Cyclobenzaprine5-hydroxytryptamine receptor 2Ctarget
DB00924Cyclobenzaprine5-hydroxytryptamine receptor 7target
DB00924Cyclobenzaprine5-hydroxytryptamine receptor 6target
DB00924CyclobenzaprineSodium-dependent serotonin transportertarget
DB00924CyclobenzaprineSodium-dependent noradrenaline transportertarget
DB00924CyclobenzaprineToll-like receptor 4target
DB00924CyclobenzaprineAldehyde oxidasetarget
DB01151DesipramineMuscarinic acetylcholine receptor M1target
DB01151DesipramineSodium-dependent noradrenaline transportertarget
DB01151DesipramineBeta-2 adrenergic receptortarget
DB01151DesipramineMuscarinic acetylcholine receptor M2target
DB01151DesipramineSodium-dependent serotonin transportertarget
DB01151DesipramineHistamine H1 receptortarget
DB01151DesipramineBeta-1 adrenergic receptortarget
DB01151DesipramineCytochrome P450 2D6enzyme
DB01151DesipramineMuscarinic acetylcholine receptor M3target
DB01151DesipramineMuscarinic acetylcholine receptor M4target
DB01151DesipramineMuscarinic acetylcholine receptor M5target
DB01151DesipramineAlpha-1 adrenergic receptorstarget
DB01151Desipramine5-hydroxytryptamine receptor 2Atarget
DB01151DesipramineAlpha-1-acid glycoprotein 1carrier
DB01151DesipramineCytochrome P450 2B6enzyme
DB01151DesipramineCytochrome P450 3A4enzyme
DB01151DesipramineSolute carrier family 22 member 2transporter
DB01151DesipramineSolute carrier family 22 member 1transporter
DB01151DesipramineSolute carrier family 22 member 3transporter
DB01151DesipramineSolute carrier family 22 member 5transporter
DB01151DesipramineP-glycoprotein 1transporter
DB01151DesipramineSolute carrier family 22 member 4transporter
DB01151DesipramineCytochrome P450 1A2enzyme
DB01151DesipramineCytochrome P450 2E1enzyme
DB01151DesipramineSphingomyelin phosphodiesterasetarget
DB01151Desipramine5-hydroxytryptamine receptor 1Atarget
DB01151Desipramine5-hydroxytryptamine receptor 2Ctarget
DB01151DesipramineDopamine D2 receptortarget
DB01151DesipramineAlpha-2 adrenergic receptorstarget
DB01142DoxepinSodium-dependent serotonin transportertarget
DB01142DoxepinSodium-dependent noradrenaline transportertarget
DB01142DoxepinHistamine H1 receptortarget
DB01142DoxepinHistamine H2 receptortarget
DB01142DoxepinCytochrome P450 2D6enzyme
DB01142DoxepinMuscarinic acetylcholine receptor M1target
DB01142DoxepinMuscarinic acetylcholine receptor M2target
DB01142DoxepinMuscarinic acetylcholine receptor M3target
DB01142DoxepinMuscarinic acetylcholine receptor M4target
DB01142DoxepinMuscarinic acetylcholine receptor M5target
DB01142DoxepinAlpha-1A adrenergic receptortarget
DB01142Doxepin5-hydroxytryptamine receptor 1Atarget
DB01142Doxepin5-hydroxytryptamine receptor 2Atarget
DB01142DoxepinCytochrome P450 2C19enzyme
DB01142DoxepinCytochrome P450 2C9enzyme
DB01142DoxepinCytochrome P450 1A2enzyme
DB01142DoxepinP-glycoprotein 1transporter
DB01142Doxepin5-hydroxytryptamine receptor 2Btarget
DB01142Doxepin5-hydroxytryptamine receptor 2Ctarget
DB01142DoxepinAlpha-1B adrenergic receptortarget
DB01142DoxepinAlpha-1D adrenergic receptortarget
DB01142DoxepinCytochrome P450 3A4enzyme
DB01142Doxepin5-hydroxytryptamine receptor 6target
DB01142DoxepinHistamine H4 receptortarget
DB01142DoxepinPotassium voltage-gated channel subfamily H member 2target
DB01142DoxepinSerum albumincarrier
DB01142DoxepinAlpha-1-acid glycoprotein 1carrier
DB00458ImipramineSodium-dependent noradrenaline transportertarget
DB00458ImipramineSodium-dependent serotonin transportertarget
DB00458ImipramineCytochrome P450 1A2enzyme
DB00458ImipramineCytochrome P450 2C19enzyme
DB00458ImipramineCytochrome P450 2D6enzyme
DB00458ImipramineHistamine H1 receptortarget
DB00458ImipramineAlpha-1A adrenergic receptortarget
DB00458Imipramine5-hydroxytryptamine receptor 2Atarget
DB00458ImipramineMuscarinic acetylcholine receptor M1target
DB00458ImipramineMuscarinic acetylcholine receptor M2target
DB00458ImipramineMuscarinic acetylcholine receptor M3target
DB00458ImipramineMuscarinic acetylcholine receptor M4target
DB00458ImipramineMuscarinic acetylcholine receptor M5target
DB00458ImipraminePotassium voltage-gated channel subfamily D member 2target
DB00458ImipraminePotassium voltage-gated channel subfamily D member 3target
DB00458ImipramineAlpha-1D adrenergic receptortarget
DB00458ImipramineAlpha-1-acid glycoprotein 1carrier
DB00458ImipramineSolute carrier family 22 member 2transporter
DB00458ImipramineSolute carrier family 22 member 3transporter
DB00458ImipramineP-glycoprotein 1transporter
DB00458ImipramineSolute carrier family 22 member 4transporter
DB00458ImipramineCytochrome P450 3A4enzyme
DB00458ImipramineCytochrome P450 2B6enzyme
DB00458ImipramineCytochrome P450 2C18enzyme
DB00458ImipramineCytochrome P450 2E1enzyme
DB00458ImipramineCytochrome P450 3A7enzyme
DB00458Imipramine5-hydroxytryptamine receptor 2Ctarget
DB00458ImipramineAlpha-1B adrenergic receptortarget
DB00458Imipramine5-hydroxytryptamine receptor 7target
DB00458ImipramineD(1) dopamine receptortarget
DB00458ImipramineDopamine D2 receptortarget
DB00458ImipraminePotassium voltage-gated channel subfamily H member 2target
DB00458ImipramineSodium-dependent dopamine transportertarget
DB00458Imipramine5-hydroxytryptamine receptor 1Atarget
DB00458Imipramine5-hydroxytryptamine receptor 6target
DB00458ImipraminePotassium voltage-gated channel subfamily H member 1target
DB00458ImipramineSerum albumincarrier
DB00458ImipramineAlpha-1-acid glycoprotein 2target
DB00532MephenytoinSodium channel protein type 5 subunit alphatarget
DB00532MephenytoinCytochrome P450 2B6enzyme
DB00532MephenytoinCytochrome P450 2C9enzyme
DB00532MephenytoinCytochrome P450 2C19enzyme
DB00532MephenytoinCytochrome P450 1A2enzyme
DB00532MephenytoinCytochrome P450 2D6enzyme
DB00532MephenytoinCytochrome P450 2C8enzyme
DB00532MephenytoinNuclear receptor subfamily 1 group I member 2target
DB00532MephenytoinThyroxine-binding globulincarrier
DB00540NortriptylineSodium-dependent serotonin transportertarget
DB00540NortriptylineSodium-dependent noradrenaline transportertarget
DB00540NortriptylineCytochrome P450 1A2enzyme
DB00540NortriptylineCytochrome P450 2D6enzyme
DB00540NortriptylineSerum albumincarrier
DB00540NortriptylineAlpha-1-acid glycoprotein 1carrier
DB00540NortriptylineHistamine H1 receptortarget
DB00540NortriptylineMuscarinic acetylcholine receptor M1target
DB00540NortriptylineMuscarinic acetylcholine receptor M2target
DB00540NortriptylineMuscarinic acetylcholine receptor M3target
DB00540NortriptylineMuscarinic acetylcholine receptor M4target
DB00540NortriptylineMuscarinic acetylcholine receptor M5target
DB00540Nortriptyline5-hydroxytryptamine receptor 2Atarget
DB00540NortriptylineAlpha-1A adrenergic receptortarget
DB00540Nortriptyline5-hydroxytryptamine receptor 1Atarget
DB00540NortriptylineCytochrome P450 3A4enzyme
DB00540NortriptylineCytochrome P450 3A5enzyme
DB00540NortriptylineAlpha-1D adrenergic receptortarget
DB00540NortriptylineCytochrome P450 2C19enzyme
DB00540NortriptylineProstaglandin G/H synthase 1enzyme
DB00540NortriptylineCytochrome P450 2E1enzyme
DB00540Nortriptyline5-hydroxytryptamine receptor 2Ctarget
DB00540Nortriptyline5-hydroxytryptamine receptor 6target
DB00540NortriptylineAlpha-1B adrenergic receptortarget
DB00540NortriptylineAlpha-2 adrenergic receptorstarget
DB00540NortriptylineBeta adrenergic receptortarget
DB00540NortriptylineDopamine D2 receptortarget
DB00540NortriptylineSigma receptortarget
DB00540Nortriptyline5-hydroxytryptamine receptor 1Ctarget
DB01100PimozideDopamine D2 receptortarget
DB01100PimozideCalmodulintarget
DB01100PimozidePotassium voltage-gated channel subfamily H member 2target
DB01100PimozideCytochrome P450 3A4enzyme
DB01100PimozideCytochrome P450 1A2enzyme
DB01100PimozideCytochrome P450 3A5enzyme
DB01100PimozideCytochrome P450 3A7enzyme
DB01100PimozideP-glycoprotein 1transporter
DB01100PimozideDopamine D3 receptortarget
DB01100PimozideCytochrome P450 2D6enzyme
DB00277TheophyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
DB00277TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
DB00277TheophyllineAdenosine receptor A2btarget
DB00277TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
DB00277TheophyllinecGMP-specific 3',5'-cyclic phosphodiesterasetarget
DB00277TheophyllineAdenosine receptor A1target
DB00277TheophyllineAdenosine receptor A2atarget
DB00277TheophyllineCytochrome P450 1A2enzyme
DB00277TheophyllineAdenosine deaminaseenzyme
DB00277TheophyllineCytochrome P450 2E1enzyme
DB00277TheophyllineCytochrome P450 3A4enzyme
DB00277TheophyllineSolute carrier family 22 member 7transporter
DB00277TheophyllineCytochrome P450 1A1enzyme
DB00277TheophyllineCytochrome P450 1B1enzyme
DB00277TheophyllineCytochrome P450 2D6enzyme
DB00277TheophyllineHistone deacetylase 2target
DB00277TheophyllineCopine-1target
DB00277TheophyllineMinor histocompatibility antigen H13target
DB00277TheophyllineNodal modulator 1target
DB00277TheophyllinePoly [ADP-ribose] polymerase 1target
DB00277TheophyllineProtein RIC-3target
DB00277TheophyllineTubulin monoglycylase TTLL3target
DB00682WarfarinVitamin K epoxide reductase complex subunit 1target
DB00682WarfarinCytochrome P450 2C8enzyme
DB00682WarfarinCytochrome P450 1A2enzyme
DB00682WarfarinCytochrome P450 2C9enzyme
DB00682WarfarinAlpha-1-acid glycoprotein 1carrier
DB00682WarfarinSerum albumincarrier
DB00682WarfarinCytochrome P450 2C19enzyme
DB00682WarfarinCytochrome P450 3A4enzyme
DB00682WarfarinCytochrome P450 2C18enzyme
DB00682WarfarinNuclear receptor subfamily 1 group I member 2target
DB00697TizanidineAlpha-2 adrenergic receptorstarget
DB00697TizanidineCytochrome P450 1A2enzyme
DB00697TizanidineNischarintarget
DB00697TizanidineAlpha-1 adrenergic receptorstarget