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LAMOTRIGINE Drug Record

  • Summary
  • Interactions
  • Claims
  • LAMOTRIGINE chembl:CHEMBL741 Approved

    Alternate Names:

    LAMICTAL CD
    LAMOTRIGINE
    BW-430C
    LAMICTAL ODT
    LAMICTAL
    LAMICTAL XR
    LAMOTRIGINUM
    QÍN
    LAMICTAL®
    LAMOTRIGINA
    3,5-DIAMINO-6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZINE
    GIZORD
    QIN
    drugbank:00555
    pubchem.compound:3878
    chembl:CHEMBL741
    rxcui:28439
    chemidplus:84057-84-1

    Drug Info:

    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications anticonvulsant
    Drug Categories agents causing hyperkalemia
    Drug Categories agents producing tachycardia
    Drug Categories anti-epileptic agent
    Drug Categories antiarrhythmic agents
    Drug Categories anticholinergic agents
    Drug Categories bradycardia-causing agents
    Drug Categories calcium-regulating hormones and agents
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 substrates
    Drug Categories cytochrome p-450 substrates
    Drug Categories decreased central nervous system disorganized electrical activity
    Drug Categories drugs causing inadvertant photosensitivity
    Drug Categories drugs that are mainly renally excreted
    Drug Categories miscellaneous anticonvulsants
    Drug Categories mood stabilizer
    Drug Categories muscarinic antagonists
    Drug Categories oct1 substrates
    Drug Categories oct2 inhibitors
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories photosensitizing agents
    Drug Categories potential qtc-prolonging agents
    Drug Categories psychotropic drugs
    Drug Categories qtc prolonging agents
    Drug Categories tranquilizing agents
    Drug Categories triazines
    Drug Categories ugt1a1 inducers
    Drug Categories ugt1a1 substrates
    Drug Categories ugt1a3 substrates
    Drug Categories ugt1a4 substrates
    (4 More Sources)

    Publications:

    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Zhou Y et al., 2015, Polymorphisms of ABCG2, ABCB1 and HNF4α are associated with Lamotrigine trough concentrations in epilepsy patients., Drug Metab Pharmacokinet
    Inoue K et al., 2016, Factors that influence the pharmacokinetics of lamotrigine in Japanese patients with epilepsy., Eur J Clin Pharmacol
    Milosheska D et al., 2016, Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters., Br J Clin Pharmacol
    Singkham N et al., 2013, Influence of the UGT2B7 -161C>T polymorphism on the population pharmacokinetics of lamotrigine in Thai patients., Eur J Clin Pharmacol
    Kwan P et al., 2008, Multidrug resistance in epilepsy and polymorphisms in the voltage-gated sodium channel genes SCN1A, SCN2A, and SCN3A: correlation among phenotype, genotype, and mRNA expression., Pharmacogenet Genomics
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Lipkind et al., 2005, Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels., Mol. Pharmacol.
    Ma CL et al., 2014, Association of SCN1A, SCN2A and ABCC2 gene polymorphisms with the response to antiepileptic drugs in Chinese Han patients with epilepsy., Pharmacogenomics
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Shen CH et al., 2016, Specific OCT1 and ABCG2 polymorphisms are associated with Lamotrigine concentrations in Chinese patients with epilepsy., Epilepsy Res
    Aberg et al., 1997, Lamotrigine therapy in infantile neuronal ceroid lipofuscinosis (INCL)., Neuropediatrics
    Kazeem GR et al., 2009, High-resolution HLA genotyping and severe cutaneous adverse reactions in lamotrigine-treated patients., Pharmacogenet Genomics
    Klarica Domjanović I et al., 2018, Interaction between ABCG2 421C>A polymorphism and valproate in their effects on steady-state disposition of lamotrigine in adults with epilepsy., Br J Clin Pharmacol
    Chang Y et al., 2014, Correlation of the UGT1A4 gene polymorphism with serum concentration and therapeutic efficacy of lamotrigine in Han Chinese of Northern China., Eur J Clin Pharmacol
    Zhou J et al., 2011, Functional analysis of UGT1A4(P24T) and UGT1A4(L48V) variant enzymes., Pharmacogenomics
    Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics
    Kumari R et al., 2011, Pharmacogenomic association study on the role of drug metabolizing, drug transporters and drug target gene polymorphisms in drug-resistant epilepsy in a north Indian population., Indian J Hum Genet
    Bertok S et al., 2017, The association of SCN1A p.Thr1067Ala polymorphism with epilepsy risk and the response to antiepileptic drugs in Slovenian children and adolescents with epilepsy., Seizure
    Yang B et al., 2008, Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides., Bioorg Med Chem
    Meldrum BS, 1996, Update on the mechanism of action of antiepileptic drugs., Epilepsia
    Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
    Braga MF et al., 2002, Lamotrigine reduces spontaneous and evoked GABAA receptor-mediated synaptic transmission in the basolateral amygdala: implications for its effects in seizure and affective disorders., Neuropharmacology
    Wang JF et al., 2002, Lamotrigine increases gene expression of GABA-A receptor beta3 subunit in primary cultured rat hippocampus cells., Neuropsychopharmacology
    Lapidus KA et al., 2013, Novel glutamatergic drugs for the treatment of mood disorders., Neuropsychiatr Dis Treat
    Leng Y et al., 2013, Neuroprotective effects of the mood stabilizer lamotrigine against glutamate excitotoxicity: roles of chromatin remodelling and Bcl-2 induction., Int J Neuropsychopharmacol
    Chartoff EH et al., 2014, It's MORe exciting than mu: crosstalk between mu opioid receptors and glutamatergic transmission in the mesolimbic dopamine system., Front Pharmacol
    Vinod KY et al., 2002, Lamotrigine induced selective changes in 5-HT(1A) receptor mediated response in rat brain., Neurochem Int
    Bourin M et al., 2005, Evidence for the activity of lamotrigine at 5-HT(1A) receptors in the mouse forced swimming test., J Psychiatry Neurosci
    Kotwal A et al., 2015, Serotonin Syndrome in the Setting of Lamotrigine, Aripiprazole, and Cocaine Use., Case Rep Med
    Dibué-Adjei M et al., 2017, Cav2.3 (R-Type) Calcium Channels are Critical for Mediating Anticonvulsive and Neuroprotective Properties of Lamotrigine In Vivo., Cell Physiol Biochem
    Kaur S et al., 1996, Motor effects of lamotrigine in naive and dopamine-depleted mice., Eur J Pharmacol
    Vallés AS et al., 2007, Lamotrigine is an open-channel blocker of the nicotinic acetylcholine receptor., Neuroreport
    Zheng C et al., 2010, The anticonvulsive drug lamotrigine blocks neuronal {alpha}4{beta}2 nicotinic acetylcholine receptors., J Pharmacol Exp Ther
  • LAMOTRIGINE   PPT1

    Interaction Score: 0.69

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9151331


    Sources:
    NCI

  • LAMOTRIGINE   UGT1A4

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29791014 26790665 23263737 24820767 22047493


    Sources:
    PharmGKB

  • LAMOTRIGINE   AQP4

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18572411


    Sources:
    DTC

  • LAMOTRIGINE   UGT2B7

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26213157 26790665 27096250 23263737


    Sources:
    PharmGKB

  • LAMOTRIGINE   CACNA1E

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    29176325


    Sources:
    DrugBank

  • LAMOTRIGINE   CHRNA1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17259859 20688974 22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   HNF4A

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27610747 26213157


    Sources:
    PharmGKB

  • LAMOTRIGINE   HLA-C

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19668019


    Sources:
    PharmGKB

  • LAMOTRIGINE   HLA-DQB1

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19668019


    Sources:
    PharmGKB

  • LAMOTRIGINE   SLC22A1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27610747


    Sources:
    PharmGKB

  • LAMOTRIGINE   SCN2A

    Interaction Score: 0.18

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Lamictal
    Novel drug target Established target
    Mechanism of Interaction Sodium channel alpha subunit blocker

    PMIDs:
    18784617 17139284 16174788 25155934 17016423


    Sources:
    PharmGKB TdgClinicalTrial ChemblInteractions

  • LAMOTRIGINE   SCN1A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    23859570 21747585 28753467 16174788 25155934


    Sources:
    PharmGKB DrugBank ChemblInteractions

  • LAMOTRIGINE   GRIA1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23976856 22564541


    Sources:
    DrugBank

  • LAMOTRIGINE   HLA-DRB1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19668019


    Sources:
    PharmGKB

  • LAMOTRIGINE   ABCG2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27610747 29791014 26213157


    Sources:
    PharmGKB

  • LAMOTRIGINE   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inducer (activating)
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8941036 22306746 11955522 11927166


    Sources:
    DrugBank

  • LAMOTRIGINE   ADORA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   ADORA2A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN11A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • LAMOTRIGINE   HTR3A

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26339247


    Sources:
    DrugBank

  • LAMOTRIGINE   OPRK1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746 24904419


    Sources:
    DrugBank

  • LAMOTRIGINE   HRH1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11792461 22306746 16049571


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN7A

    Interaction Score: 0.03

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   SCN8A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   SCN3A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Sodium channel alpha subunit blocker

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   ADRB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN4A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   ADRA2A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN9A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   DRD2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    agonist (activating)
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8813577 22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN10A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Sodium channel alpha subunit blocker

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   ADRA1A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   DRD1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   SCN5A

    Interaction Score: 0.01

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LAMOTRIGINE   HTR2A

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22306746


    Sources:
    DrugBank

  • LAMOTRIGINE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LAMOTRIGINE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LAMOTRIGINE   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LAMOTRIGINE   CYP1A2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LAMOTRIGINE   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LAMOTRIGINE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DrugBank: DB00555

    • Version: 5.1.7

    Alternate Names:
    LAMOTRIGINE DrugBank Drug Name
    84057-84-1 CAS Number
    Apo-lamotrigine Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Meldrum BS, 1996, Update on the mechanism of action of antiepileptic drugs., Epilepsia
    Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
    Braga MF et al., 2002, Lamotrigine reduces spontaneous and evoked GABAA receptor-mediated synaptic transmission in the basolateral amygdala: implications for its effects in seizure and affective disorders., Neuropharmacology

  • TdgClinicalTrial: LAMOTRIGINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications anticonvulsant
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: LAMOTRIGINE

    • Version: 14-September-2017

    Alternate Names:
    C38703 NCI drug code

    Drug Info:

    Publications:
    Aberg et al., 1997, Lamotrigine therapy in infantile neuronal ceroid lipofuscinosis (INCL)., Neuropediatrics

  • DTC: LAMOTRIGINE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL741 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Yang B et al., 2008, Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides., Bioorg Med Chem

  • PharmGKB: lamotrigine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Shen CH et al., 2016, Specific OCT1 and ABCG2 polymorphisms are associated with Lamotrigine concentrations in Chinese patients with epilepsy., Epilepsy Res
    Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics
    Kumari R et al., 2011, Pharmacogenomic association study on the role of drug metabolizing, drug transporters and drug target gene polymorphisms in drug-resistant epilepsy in a north Indian population., Indian J Hum Genet

  • TTD: Lamotrigine

    • Version: 2020.06.01

    Alternate Names:
    D03FLC TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL741

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL741

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21