Identification

Name
Lamotrigine
Accession Number
DB00555
Description

Lamotrigine is an antiepileptic drug belonging in the phenyltriazine class. It is used in the treatment of both epilepsy and as a mood stabilizer in bipolar disorder. Lamotrigine is the first medication since lithium granted Food and Drug Administration (FDA) approval for the maintenance treatment of bipolar type I. It is approved for use in more than 30 countries.10

Lamotrigine has relatively few side-effects and does not require laboratory monitoring. While it is indicated for epilepsy and bipolar disorders, there is evidence that lamotrigine could have some clinical efficacy in certain neuropathic pain states.3,4

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 256.091
Monoisotopic: 255.007850663
Chemical Formula
C9H7Cl2N5
Synonyms
  • 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
  • Lamotrigina
  • Lamotrigine
  • Lamotriginum
External IDs
  • BW 430 C
  • BW 430C
  • BW-430C
  • GW 273293

Pharmacology

Indication

Lamotrigine is indicated as adjunctive therapy for the following seizure types in patients ≥2 years of age: partial seizures, primary generalized tonic-clonic seizures, and generalized seizures due to Lennox-Gastaut syndrome.14

It is also indicated for the process of conversion to drug monotherapy for those at least 16 years of age or older with partial seizures and currently are receiving treatment with carbamazepine, phenytoin, phenobarbital, primidone, or valproate as the single antiepileptic drug (AED).14

In addition to the above, lamotrigine is also indicated for the maintenance treatment of bipolar I disorder, delaying the time to mood episodes (which may include mania, hypomania, depression, mixed episodes) in adults at least 18 years or older, who have been treated for acute mood symptoms with standard therapy.14

Limitations of use

It is important to note that lamotirigine should not be used in the treatment of acute mood episodes, as efficacy has not been established in this context.14

Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Lamotrigine likely prevents seizures and prevents mood symptoms via stabilizing presynaptic neuronal membranes and preventing the release of excitatory neurotransmitters such as glutamate, which contribute to seizure activity.10,14

A note on cardiovascular effects

The metabolite of lamotrigine, 2-N-methyl metabolite (formed by glucuronidation), is reported to cause dose-dependent prolongations of the PR interval, widening of the QRS complex, and at higher doses, complete AV block. Although this harmful metabolite is only found in trace amounts in humans, plasma concentrations may increase in conditions that cause decreased drug glucuronidation, such as liver disease.7,14,15

Mechanism of action

The exact mechanism of action of lamotrigine is not fully elucidated, as it may exert cellular activities that contribute to its efficacy in a range of conditions. Although chemically unrelated, lamotrigine actions resemble those of phenytoin and carbamazepine, inhibiting voltage-sensitive sodium channels, stabilizing neuronal membranes, thereby modulating the release of presynaptic excitatory neurotransmitters.7,10,14

Lamotrigine likely acts by inhibiting sodium currents by selective binding to the inactive sodium channel, suppressing the release of the excitatory amino acid, glutamate. The mechanism of action of lamotrigine in reducing anticonvulsant activity is likely the same in managing bipolar disorder. Studies on lamotrigine have identified its binding to sodium channels in a fashion similar to local anesthetics, which could explain the demonstrated clinical benefit of lamotrigine in some neuropathic pain states.13

Lamotrigine displays binding properties to several different receptors. In laboratory binding assays, it demonstrates weak inhibitory effect on the serotonin 5-HT3 receptor. Lamotrigine also weakly binds to Adenosine A1/A2 receptors, α1/α2/β adrenergic receptors, dopamine D1/D2 receptors, GABA A/B receptors, histamine H1 receptors, κ-opioid receptor (KOR), mACh receptors and serotonin 5-HT2 receptors with an IC50>100 µM. Weak inhibitory effects were observed at sigma opioid receptors.14 An in vivo study revealed evidence that lamotrigine inhibits Cav2.3 (R-type) calcium currents, which may also contribute to its anticonvulsant effects.6

TargetActionsOrganism
AVoltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E)
inhibitor
Humans
AVoltage-gated sodium channel alpha subunit
inhibitor
Humans
UAdenosine receptor A1
inhibitor
Humans
UAdenosine receptor A2a
inhibitor
Humans
UAlpha-1A adrenergic receptor
inhibitor
Humans
UAlpha-2A adrenergic receptor
inhibitor
Humans
UBeta-1 adrenergic receptor
inhibitor
Humans
UD(1) dopamine receptor
inhibitor
Humans
UDopamine D2 receptor
agonist
inhibitor
Humans
UGABA(A) Receptor
antagonist
inducer
Humans
UGABA(A) Receptor Benzodiazepine Binding Site
inhibitor
Humans
UHistamine H1 receptor
antagonist
Humans
UKappa-type opioid receptor
inhibitor
Humans
UAcetylcholine receptor subunit alpha
inhibitor
Humans
U5-hydroxytryptamine receptor 2A
inhibitor
Humans
U5-hydroxytryptamine receptor 3A
inhibitor
Humans
UGlutamate receptor 1
inhibitor
Humans
Absorption

Lamotrigine is rapidly and entirely absorbed with minimal first-pass metabolism effects, with a bioavailability estimated at 98%. Cmax is reached in the range of 1.4 to 4.8 hours post-dose, but this depends on the dose administered, concomitant medications, and epileptic status. The rate and extent of lamictal absorption is considered equivalent between the compressed tablet form taken with water to that of the chewable dispersible tablets, taken with or without water.14,15

Volume of distribution

The mean apparent volume of distribution (Vd/F) of lamotrigine following oral administration ranges from 0.9 to 1.3 L/kg and is independent of dose administered. Lamotrigine accumulated in the kidney of the male rat, and likely behaves in a similar fashion in humans. Lamotrigine also binds to tissues containing melanin, such as the eyes and pigmented skin.14,15

Protein binding

The plasma protein binding of lamotrigine is estimated at 55%.11,14 This drug is not expected to undergo clinically significant interactions with other drugs via competition for protein binding sites due its lower protein binding.14,15

Metabolism

Lamotrigine is mainly glucuronidated, forming 2-N-glucuronide conjugate, a pharmacologically inactive metabolite.12 The total radioactivity detected after a 240mg radiolabeled dose of lamotrigine during clinical trials were as follows: lamotrigine as unchanged drug(10%), a 2-N-glucuronide (76%), a 5-N-glucuronide (10%), a 2-N-methyl metabolite (0.14%), as well as various other minor metabolites (4%).14

Hover over products below to view reaction partners

Route of elimination

Lamotrigine is excreted in both the urine and feces.12 Following oral administration of 240 mg radiolabelled lamotrigine, about 94% of total drug and its metabolites administered is recovered in the urine and 2% is recovered in the feces.14 One pharmacokinetic study recovered 43 to 87% of a lamotrigine dose in the urine mainly as glucuronidated metabolites.11 2-N-glucuronide is mainly excreted in the urine.12

Half-life

The average elimination half-life of lamotrigine ranges from approximately 14-59 hours. The value is dependent on the dose administered, concomitant drug therapy, as well as disease status.11,15 One pharmacokinetic study revealed a half-life of 22.8 to 37.4 hours in healthy volunteers. It also reported that enzyme-inducing antiepileptic drugs such as pheobarbital, phenytoin, or carbamazepine decrease the half-life of lamotrigine. On the other hand, valproic acid increases the half-life of lamotrigine (in the range of 48-59 hours).11

Clearance

The mean apparent plasma clearance (Cl/F) ranges from 0.18 to 1.21 mL/min/kg. The values vary depending on dosing regimen, concomitant antiepileptic medications, and disease state of the individual.14 In one study, healthy volunteers on lamictal monotherapy showed a clearance of about 0.44 mL/min/kg after a single dose.14

Adverse Effects
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Toxicity

The oral LD50 in mouse and rat is 205 mg/kg and 245 mg/kg, respectively.MSDS

Fatal cases of overdose of up to 15g of lamotrigine have been reported. Overdose with lamotrigine has been manifested by ataxia, nystagmus, increased seizures, decreased level of consciousness, coma, and intraventricular conduction delay. Though no known antidote exists for lamotrigine, hospitalization and general supportive measures should be employed in the case of a suspected lamotrigine overdose. Gastric lavage and emesis may be warranted with simultaneous protection of the airway. It is uncertain at this time whether hemodialysis is an effective means of removing lamotrigine from the sytemic circulation.15,14

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirThe metabolism of Abacavir can be increased when combined with Lamotrigine.
AbametapirThe serum concentration of Lamotrigine can be increased when it is combined with Abametapir.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Lamotrigine.
AcebutololThe risk or severity of bradycardia can be increased when Lamotrigine is combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Lamotrigine which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Lamotrigine which could result in a higher serum level.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Lamotrigine.
AcetazolamideThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Acetazolamide.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Lamotrigine is combined with Acetohexamide.
AcetophenazineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Acetophenazine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

Product Images
International/Other Brands
Convulsan (Actavis) / Crisomet (Juste) / Dafex (Phoenix) / Daksol (Pharmavita) / Danoptin (Pliva) / Dezepil (Rafarm) / Elmendos (GlaxoSmithKline) / Epilepax (Ivax) / Epimil (Ivax) / Epiral (Zentiva) / Epitec (Cipla Medpro) / Epitrigine (Actavis) / Labileno (GlaxoSmithKline) / Lambipol (GlaxoSmithKline) / Lamect (PharmaSwiss) / Lameptil (Sandoz) / Lameptil S (Sandoz) / Lametec (Vitalchem) / Lamez (Intas) / Lamictal CD (GlaxoSmithKline) / Lamictin (GlaxoSmithKline) / Lamotrix (Glenmark) / Larig (Rowex) / Medotrigin (Medochemie) / Mogine (Douglas) / Trimolep (Psicofarma) / Trogine (Ranbaxy) / Xebarin (Dr Reddys)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LamictalTablet100 mgOralGlaxosmithkline Inc1995-12-31Not applicableCanada flag
LamictalTablet100 mg/1OralGlaxoSmithKline LLC1995-01-17Not applicableUS flag00173 0642 55 nlmimage10 c518e287
LamictalTablet, for suspension25 mg/1OralGlaxoSmithKline LLC1998-09-03Not applicableUS flag00173 0527 00 nlmimage10 b518daa6
LamictalTablet150 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-292014-12-31US flag
LamictalTablet100 mg/1OralREMEDYREPACK INC.2016-12-092020-03-31US flag
LamictalTablet200 mg/1OralGlaxoSmithKline LLC1995-01-18Not applicableUS flag00173 0644 60 nlmimage10 b218d956
LamictalTablet100 mg/1OralPhysicians Total Care, Inc.2008-05-09Not applicableUS flag54868 467520180907 15195 1xrimtk
LamictalTablet5 mgOralGlaxosmithkline Inc1999-06-02Not applicableCanada flag
LamictalTablet100 mg/1OralRebel Distributors1995-01-17Not applicableUS flag
LamictalTablet25 mg/1OralRemedy Repack2007-10-242018-10-16US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-lamotrigineTabletOralApotex Corporation2002-03-18Not applicableCanada flag
Apo-lamotrigineTabletOralApotex Corporation2002-03-18Not applicableCanada flag
Apo-lamotrigineTabletOralApotex Corporation2002-03-18Not applicableCanada flag
Auro-lamotrigineTabletOralAuro Pharma Inc2012-06-13Not applicableCanada flag
Auro-lamotrigineTabletOralAuro Pharma Inc2012-06-13Not applicableCanada flag
Auro-lamotrigineTabletOralAuro Pharma Inc2012-06-13Not applicableCanada flag
Dom-lamotrigineTabletOralDominion PharmacalNot applicableNot applicableCanada flag
Dom-lamotrigineTabletOralDominion PharmacalNot applicableNot applicableCanada flag
Dom-lamotrigineTabletOralDominion PharmacalNot applicableNot applicableCanada flag
LamotrigineTablet25 mg/1OralPhysicians Total Care, Inc.2009-12-09Not applicableUS flag54868 607820180907 15195 1r4idaw
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
LamictalLamotrigine (100 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2003-09-29Not applicableUS flag
LamictalLamotrigine (100 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2003-09-29Not applicableUS flag
LamictalLamotrigine (100 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2003-09-29Not applicableUS flag
LamictalLamotrigine (100 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2003-09-29Not applicableUS flag
Lamictal ODTLamotrigine (50 mg/1) + Lamotrigine (100 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag
Lamictal ODTLamotrigine (25 mg/1) + Lamotrigine (50 mg/1) + Lamotrigine (100 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag00173 0778 61 nlmimage10 ec19764b
Lamictal ODTLamotrigine (50 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag
Lamictal ODTLamotrigine (25 mg/1) + Lamotrigine (50 mg/1) + Lamotrigine (100 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag00173 0778 61 nlmimage10 ec19764b
Lamictal ODTLamotrigine (50 mg/1) + Lamotrigine (100 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag
Lamictal ODTLamotrigine (50 mg/1) + Lamotrigine (25 mg/1)OralGlaxoSmithKline LLC2009-06-05Not applicableUS flag

Categories

ATC Codes
N03AX09 — Lamotrigine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dichlorobenzenes. These are compounds containing a benzene with exactly two chlorine atoms attached to it.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Halobenzenes
Direct Parent
Dichlorobenzenes
Alternative Parents
Aminotriazines / Imidolactams / Aryl chlorides / 1,2,4-triazines / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
1,2,4-triazine / 1,2-dichlorobenzene / Amine / Aminotriazine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Heteroaromatic compound / Hydrocarbon derivative
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
dichlorobenzene, primary arylamine, 1,2,4-triazines (CHEBI:6367)

Chemical Identifiers

UNII
U3H27498KS
CAS number
84057-84-1
InChI Key
PYZRQGJRPPTADH-UHFFFAOYSA-N
InChI
InChI=1S/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16)
IUPAC Name
6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine
SMILES
NC1=NC(N)=C(N=N1)C1=C(Cl)C(Cl)=CC=C1

References

Synthesis Reference

Grahame Roy Lee, "Process for the preparation of lamotrigine." U.S. Patent US5925755, issued January, 1981.

US5925755
General References
  1. Backonja M: Neuromodulating drugs for the symptomatic treatment of neuropathic pain. Curr Pain Headache Rep. 2004 Jun;8(3):212-6. [PubMed:15115640]
  2. Barbosa L, Berk M, Vorster M: A double-blind, randomized, placebo-controlled trial of augmentation with lamotrigine or placebo in patients concomitantly treated with fluoxetine for resistant major depressive episodes. J Clin Psychiatry. 2003 Apr;64(4):403-7. [PubMed:12716240]
  3. Jensen TS: Anticonvulsants in neuropathic pain: rationale and clinical evidence. Eur J Pain. 2002;6 Suppl A:61-8. [PubMed:11888243]
  4. Pappagallo M: Newer antiepileptic drugs: possible uses in the treatment of neuropathic pain and migraine. Clin Ther. 2003 Oct;25(10):2506-38. [PubMed:14667954]
  5. Tehrani SP, Daryaafzoon M, Bakhtiarian A, Ejtemaeemehr S, Sahraei H: The effects of lamotrigine on the acquisition and expression of morphine-induced place preference in mice. Pak J Biol Sci. 2009 Jan 1;12(1):33-9. [PubMed:19579915]
  6. Dibue-Adjei M, Kamp MA, Alpdogan S, Tevoufouet EE, Neiss WF, Hescheler J, Schneider T: Cav2.3 (R-Type) Calcium Channels are Critical for Mediating Anticonvulsive and Neuroprotective Properties of Lamotrigine In Vivo. Cell Physiol Biochem. 2017;44(3):935-947. doi: 10.1159/000485361. Epub 2017 Nov 24. [PubMed:29176325]
  7. Goa KL, Ross SR, Chrisp P: Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs. 1993 Jul;46(1):152-76. doi: 10.2165/00003495-199346010-00009. [PubMed:7691504]
  8. Garnett WR: Lamotrigine: pharmacokinetics. J Child Neurol. 1997 Nov;12 Suppl 1:S10-5. doi: 10.1177/0883073897012001041. [PubMed:9429124]
  9. Polepally AR, Brundage RC, Remmel RP, Leppik IE, Pennell PB, White JR, Ramsay RE, Kistner BM, Birnbaum AK: Lamotrigine pharmacokinetics following oral and stable-labeled intravenous administration in young and elderly adult epilepsy patients: Effect of age. Epilepsia. 2018 Sep;59(9):1718-1726. doi: 10.1111/epi.14519. Epub 2018 Aug 12. [PubMed:30101556]
  10. Prabhavalkar KS, Poovanpallil NB, Bhatt LK: Management of bipolar depression with lamotrigine: an antiepileptic mood stabilizer. Front Pharmacol. 2015 Oct 23;6:242. doi: 10.3389/fphar.2015.00242. eCollection 2015. [PubMed:26557090]
  11. Rambeck B, Wolf P: Lamotrigine clinical pharmacokinetics. Clin Pharmacokinet. 1993 Dec;25(6):433-43. doi: 10.2165/00003088-199325060-00003. [PubMed:8119045]
  12. Milosheska D, Lorber B, Vovk T, Kastelic M, Dolzan V, Grabnar I: Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters. Br J Clin Pharmacol. 2016 Aug;82(2):399-411. doi: 10.1111/bcp.12984. Epub 2016 May 29. [PubMed:27096250]
  13. 44. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 544, 549). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
  14. Lamictal FDA Label [Link]
  15. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Human Metabolome Database
HMDB0014695
KEGG Drug
D00354
PubChem Compound
3878
PubChem Substance
46505408
ChemSpider
3741
BindingDB
50031299
RxNav
28439
ChEBI
6367
ChEMBL
CHEMBL741
ZINC
ZINC000000013156
Therapeutic Targets Database
DAP000039
PharmGKB
PA450164
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lamotrigine
AHFS Codes
  • 28:12.92 — Miscellaneous Anticonvulsants
FDA label
Download (1.12 MB)
MSDS
Download (24.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableHippocampal Atrophy Due to Corticosteroid / Hypomania Due to Corticosteroid Use / Memory Impairment Due to Corticosteroid Use1
4CompletedBasic ScienceEpilepsies2
4CompletedBasic ScienceHealthy Volunteers1
4CompletedHealth Services ResearchMemory Disturbances1
4CompletedPreventionBipolar Disorder (BD)1
4CompletedSupportive CareCerebral Palsy (CP) / Crying1
4CompletedTreatmentAlcohol Dependence / Bipolar Disorder (BD) / Depression / Mania / Psychosis1
4CompletedTreatmentBipolar Disorder (BD)7
4CompletedTreatmentBipolar Disorder (BD) / Dependence, Cocaine1
4CompletedTreatmentBipolar Disorder (BD) / Depression1

Pharmacoeconomics

Manufacturers
  • Glaxosmithkline
  • Aurobindo pharma ltd
  • Dr reddys laboratories ltd
  • Glenmark generics ltd
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Taro pharmaceutical industries ltd
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Zydus pharmaceuticals usa inc
  • Smithkline beecham corp
  • Smithkline beecham corp dba glaxosmithkline
  • Apotex inc
  • Cadista pharmaceuticals inc
  • Lupin ltd
  • Matrix laboratories ltd
  • Roxane laboratories inc
  • Torrent pharmaceuticals ltd
  • Upsher smith laboratories inc
  • Wockhardt ltd
Packagers
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • Atlantic Biologicals Corporation
  • Aurobindo Pharma Ltd.
  • Cadila Healthcare Ltd.
  • Cadista Pharmaceuticals Inc.
  • Cardinal Health
  • Caremark LLC
  • Cobalt Pharmaceuticals Inc.
  • Compass Pharma Services LLC
  • Comprehensive Consultant Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • DSM Corp.
  • GlaxoSmithKline Inc.
  • Glenmark Generics Ltd.
  • Greenstone LLC
  • Heartland Repack Services LLC
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pharmacy Service Center
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Sandoz
  • Stat Rx Usa
  • Taro Pharmaceuticals USA
  • Teva Pharmaceutical Industries Ltd.
  • Torrent Pharmaceuticals
  • UDL Laboratories
  • Vangard Labs Inc.
  • Zydus Pharmaceuticals
Dosage Forms
FormRouteStrength
Tablet, for suspensionOral100 MG
Tablet, for suspensionOral200 MG
Tablet, for suspensionOral25 MG
Tablet, for suspensionOral5 MG
Tablet, for suspensionOral50 MG
TabletOral
Tablet, coatedOral750 mg
Tablet
Tablet, solubleOral5 mg
Tablet, chewableOral100 mg
Tablet, chewableOral200 mg
Tablet, chewableOral25 mg
Tablet, chewableOral5 mg
Tablet, chewableOral50 mg
Tablet, solubleOral100 mg
Tablet, solubleOral200 mg
TabletOral100 mg
TabletOral200 mg
TabletOral50 mg
TabletOral25 mg
Tablet, solubleOral50 mg
Tablet, solubleOral25 mg
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral150 mg
TabletOral2 MG
TabletOral5 MG
Tablet, for suspensionOral2 mg/1
Tablet, solubleOral
Tablet, chewableOral2 mg
Tablet2 MG
Tablet5 mg
Tablet, for solution; tablet, for suspensionOral5 MG
Tablet, film coated, extended releaseOral250 mg/1
Tablet, film coated, extended releaseOral300 mg/1
Tablet, coatedOral100 mg
Tablet, coatedOral25 mg
Tablet, coatedOral50 mg
Tablet100 MG
Tablet50 MG
Tablet200 MG
Tablet25 MG
Tablet, for solution; tablet, for suspensionOral200 MG
Tablet, for solution; tablet, for suspensionOral25 MG
Tablet, for solution; tablet, for suspensionOral100 MG
Tablet, for solution; tablet, for suspensionOral
Tablet, for solution; tablet, for suspensionOral50 MG
KitOral
SuspensionOral1 mg/1mL
TabletOral200 mg/1
TabletOral25 mg/1
Tablet, chewableOral2 mg/1
Tablet, chewableOral25 mg/1
Tablet, chewableOral5 mg/1
Tablet, extended releaseOral100 mg/1
Tablet, extended releaseOral200 mg/1
Tablet, extended releaseOral25 mg/1
Tablet, extended releaseOral250 mg/1
Tablet, extended releaseOral300 mg/1
Tablet, extended releaseOral50 mg/1
Tablet, film coated, extended releaseOral100 mg/1
Tablet, film coated, extended releaseOral200 mg/1
Tablet, film coated, extended releaseOral25 mg/1
Tablet, film coated, extended releaseOral50 mg/1
Tablet, for suspensionOral25 mg/1
Tablet, for suspensionOral5 mg/1
Tablet, orally disintegratingOral100 mg/1
Tablet, orally disintegratingOral200 mg/1
Tablet, orally disintegratingOral25 mg/1
Tablet, orally disintegratingOral50 mg/1
TabletOral250 mg/1
TabletOral300 mg/1
TabletOral50 mg/1
Prices
Unit descriptionCostUnit
LaMICtal Starter 98 25 (84)-100(14)mg Kit Box556.69USD box
LaMICtal XR 200 mg 24 Hour tablet12.11USD tablet
Lamictal xr 200 mg tablet11.65USD tablet
LaMICtal XR 100 mg 24 Hour tablet11.36USD tablet
Lamictal xr 100 mg tablet10.92USD tablet
Lamictal xr 50 mg tablet10.2USD tablet
Lamictal 200 mg tablet7.44USD tablet
Lamictal odt start kt (orange)7.28USD tablet
Lamictal xr start kit (orange)7.28USD tablet
Lamictal odt 200 mg tablet6.95USD tablet
Lamictal odt 100 mg tablet5.82USD tablet
Lamotrigine 200 mg tablet5.78USD tablet
LaMICtal 25 mg Chew Tabs5.63USD tab
Lamictal odt 50 mg tablet5.46USD tablet
Lamictal tab start kit (green)5.46USD tablet
Lamictal 150 mg tablet5.38USD tablet
Lamictal odt 25 mg tablet5.1USD tablet
Lamictal xr 25 mg tablet5.1USD tablet
Lamictal 100 mg tablet4.72USD tablet
Lamotrigine tablet starter kit4.24USD tablet
Lamotrigine 150 mg tablet3.98USD tablet
Lamictal 25 mg tablet3.78USD tablet
Lamotrigine 100 mg tablet3.52USD tablet
LamoTRIgine 25 mg Chew Tabs3.33USD tab
LamoTRIgine 5 mg Chew Tabs3.18USD tab
Lamotrigine 25 mg tablet2.9USD tablet
Apo-Lamotrigine 150 mg Tablet1.31USD tablet
Mylan-Lamotrigine 150 mg Tablet1.31USD tablet
Novo-Lamotrigine 150 mg Tablet1.31USD tablet
Pms-Lamotrigine 150 mg Tablet1.31USD tablet
Ratio-Lamotrigine 150 mg Tablet1.31USD tablet
Apo-Lamotrigine 100 mg Tablet0.88USD tablet
Mylan-Lamotrigine 100 mg Tablet0.88USD tablet
Novo-Lamotrigine 100 mg Tablet0.88USD tablet
Pms-Lamotrigine 100 mg Tablet0.88USD tablet
Ratio-Lamotrigine 100 mg Tablet0.88USD tablet
Apo-Lamotrigine 25 mg Tablet0.22USD tablet
Mylan-Lamotrigine 25 mg Tablet0.22USD tablet
Novo-Lamotrigine 25 mg Tablet0.22USD tablet
Pms-Lamotrigine 25 mg Tablet0.22USD tablet
Ratio-Lamotrigine 25 mg Tablet0.22USD tablet
Lamictal 5 mg Chewable Tablet0.18USD tablet
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Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5698226No1997-12-162012-07-29US flag
CA2277722No2001-03-272012-01-29Canada flag
US9144547No2015-09-292023-09-22US flag
US8637512No2014-01-282028-06-14US flag
US8840925No2014-09-232028-07-02US flag
US7919115No2011-04-052029-01-04US flag
US9339504No2016-05-172028-07-02US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)177-181https://www.chemicalbook.com/ChemicalProductProperty_US_CB4166704.aspx
boiling point (°C)503.1±60.0https://www.chemicalbook.com/ChemicalProductProperty_US_CB4166704.aspx
water solubility0.17 mg/mLFDA label
logP1.93http://www.t3db.ca/toxins/T3D2570
pKa5.7FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.488 mg/mLALOGPS
logP1.87ALOGPS
logP1.93ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)14.98ChemAxon
pKa (Strongest Basic)5.87ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area90.71 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity66.62 m3·mol-1ChemAxon
Polarizability23.1 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9382
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.7155
P-glycoprotein inhibitor INon-inhibitor0.911
P-glycoprotein inhibitor IINon-inhibitor0.9604
Renal organic cation transporterNon-inhibitor0.8176
CYP450 2C9 substrateNon-substrate0.9162
CYP450 2D6 substrateNon-substrate0.9055
CYP450 3A4 substrateNon-substrate0.6862
CYP450 1A2 substrateNon-inhibitor0.611
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.7007
CYP450 2C19 inhibitorNon-inhibitor0.8594
CYP450 3A4 inhibitorNon-inhibitor0.7678
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5515
Ames testNon AMES toxic0.8202
CarcinogenicityNon-carcinogens0.7895
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7556 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9168
hERG inhibition (predictor II)Non-inhibitor0.8735
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
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-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-0090000000-0ca7be847ef73a25032b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0c09-0890000000-f7244245bf6816d03dc7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-97d10d3ad5d45edcaeba
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-b2dbf89c13423bc1b59f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-d26cb5886894916aa1d8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0590000000-528845465e0a140f6b60
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0930000000-9a68c83a3573a48cf6c2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0kmi-0900000000-bb97e1aecda1747cbf29
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-97d10d3ad5d45edcaeba
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-97d10d3ad5d45edcaeba
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0090000000-1e756e80b9a7d4b0dd18
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0490000000-a29a09ef58e19c7e62e1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0940000000-85279d67921a0106c4e2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0kmi-0900000000-eba38744d927d1c39a74
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0ab9-0790000000-036c53ed1835e3d33348
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0290000000-26664a56093e292ec551
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0190000000-33187897c9fb0b0a178f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-2940000000-1a4f3a098b426ac4febb

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Data regarding this target action are limited in the literature.
General Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1E gives rise to R-type calcium currents. R-type calcium channels belong to the 'high-voltage activated' (HVA) group and are blocked by nickel, and partially by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to dihydropyridines (DHP), omega-conotoxin-GVIA (omega-CTx-GVIA), and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing alpha-1E subunit could be involved in the modulation of firing patterns of neurons which is important for information processing.
Specific Function
Calcium channel activity
Gene Name
CACNA1E
Uniprot ID
Q15878
Uniprot Name
Voltage-dependent R-type calcium channel subunit alpha-1E
Molecular Weight
261729.05 Da
References
  1. Dibue-Adjei M, Kamp MA, Alpdogan S, Tevoufouet EE, Neiss WF, Hescheler J, Schneider T: Cav2.3 (R-Type) Calcium Channels are Critical for Mediating Anticonvulsive and Neuroprotective Properties of Lamotrigine In Vivo. Cell Physiol Biochem. 2017;44(3):935-947. doi: 10.1159/000485361. Epub 2017 Nov 24. [PubMed:29176325]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity
Specific Function
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 protein forms a...

Components:
References
  1. Lipkind GM, Fozzard HA: Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels. Mol Pharmacol. 2005 Dec;68(6):1611-22. Epub 2005 Sep 20. [PubMed:16174788]
  2. Rang, H. P. and Dale, M. M. (2012). Rang and Dale's Pharmacology (7th ed.). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
  3. Lamictal FDA Label [Link]
  4. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Purine nucleoside binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
ADORA1
Uniprot ID
P30542
Uniprot Name
Adenosine receptor A1
Molecular Weight
36511.325 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Identical protein binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
ADORA2A
Uniprot ID
P29274
Uniprot Name
Adenosine receptor A2a
Molecular Weight
44706.925 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
Molecular Weight
51322.1 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.

Components:
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM. The agonist action on the D2 receptor was demonstrated only in an in vivo study in mice.
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Kaur S, Starr M: Motor effects of lamotrigine in naive and dopamine-depleted mice. Eur J Pharmacol. 1996 May 23;304(1-3):1-6. doi: 10.1016/0014-2999(96)00134-3. [PubMed:8813577]
  3. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Inducer
Curator comments
Weak inhibitor with an IC50>100 µM. Induction of GABA receptor expression has been observed in rats.
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Braga MF, Aroniadou-Anderjaska V, Post RM, Li H: Lamotrigine reduces spontaneous and evoked GABAA receptor-mediated synaptic transmission in the basolateral amygdala: implications for its effects in seizure and affective disorders. Neuropharmacology. 2002 Mar;42(4):522-9. doi: 10.1016/s0028-3908(01)00198-8. [PubMed:11955522]
  3. Meldrum BS: Update on the mechanism of action of antiepileptic drugs. Epilepsia. 1996;37 Suppl 6:S4-11. doi: 10.1111/j.1528-1157.1996.tb06038.x. [PubMed:8941036]
  4. Wang JF, Sun X, Chen B, Young LT: Lamotrigine increases gene expression of GABA-A receptor beta3 subunit in primary cultured rat hippocampus cells. Neuropsychopharmacology. 2002 Apr;26(4):415-21. doi: 10.1016/S0893-133X(01)00385-2. [PubMed:11927166]
  5. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Braga MF, Aroniadou-Anderjaska V, Post RM, Li H: Lamotrigine reduces spontaneous and evoked GABAA receptor-mediated synaptic transmission in the basolateral amygdala: implications for its effects in seizure and affective disorders. Neuropharmacology. 2002 Mar;42(4):522-9. doi: 10.1016/s0028-3908(01)00198-8. [PubMed:11955522]
  3. Meldrum BS: Update on the mechanism of action of antiepileptic drugs. Epilepsia. 1996;37 Suppl 6:S4-11. doi: 10.1111/j.1528-1157.1996.tb06038.x. [PubMed:8941036]
  4. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Bourin M, Masse F, Hascoet M: Evidence for the activity of lamotrigine at 5-HT(1A) receptors in the mouse forced swimming test. J Psychiatry Neurosci. 2005 Jul;30(4):275-82. [PubMed:16049571]
  3. Vinod KY, Subhash MN: Lamotrigine induced selective changes in 5-HT(1A) receptor mediated response in rat brain. Neurochem Int. 2002 Apr;40(4):315-9. doi: 10.1016/s0197-0186(01)00088-2. [PubMed:11792461]
  4. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Chartoff EH, Connery HS: It's MORe exciting than mu: crosstalk between mu opioid receptors and glutamatergic transmission in the mesolimbic dopamine system. Front Pharmacol. 2014 May 27;5:116. doi: 10.3389/fphar.2014.00116. eCollection 2014. [PubMed:24904419]
  3. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name
CHRNA1
Uniprot ID
P02708
Uniprot Name
Acetylcholine receptor subunit alpha
Molecular Weight
54545.235 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. Zheng C, Yang K, Liu Q, Wang MY, Shen J, Valles AS, Lukas RJ, Barrantes FJ, Wu J: The anticonvulsive drug lamotrigine blocks neuronal {alpha}4{beta}2 nicotinic acetylcholine receptors. J Pharmacol Exp Ther. 2010 Nov;335(2):401-8. doi: 10.1124/jpet.110.171108. Epub 2010 Aug 5. [PubMed:20688974]
  3. Valles AS, Garbus I, Barrantes FJ: Lamotrigine is an open-channel blocker of the nicotinic acetylcholine receptor. Neuroreport. 2007 Jan 8;18(1):45-50. doi: 10.1097/01.wnr.0000246323.66438.94. [PubMed:17259859]
  4. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Weak inhibitor with an IC50>100 µM.
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Abelaira HM, Reus GZ, Ribeiro KF, Zappellini G, Cipriano AL, Scaini G, Streck EL, Quevedo J: Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats. Pharmacol Biochem Behav. 2012 May;101(3):348-53. doi: 10.1016/j.pbb.2012.01.019. Epub 2012 Jan 27. [PubMed:22306746]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
IC50 = 18 µM
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Kotwal A, Cutrona SL: Serotonin Syndrome in the Setting of Lamotrigine, Aripiprazole, and Cocaine Use. Case Rep Med. 2015;2015:769531. doi: 10.1155/2015/769531. Epub 2015 Aug 2. [PubMed:26339247]
  2. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Lamotrigine inhibits the release of glutamate from cerebral nerve terminals.
General Function
Pdz domain binding
Specific Function
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a co...
Gene Name
GRIA1
Uniprot ID
P42261
Uniprot Name
Glutamate receptor 1
Molecular Weight
101505.245 Da
References
  1. Lapidus KA, Soleimani L, Murrough JW: Novel glutamatergic drugs for the treatment of mood disorders. Neuropsychiatr Dis Treat. 2013;9:1101-12. doi: 10.2147/NDT.S36689. Epub 2013 Aug 7. [PubMed:23976856]
  2. Leng Y, Fessler EB, Chuang DM: Neuroprotective effects of the mood stabilizer lamotrigine against glutamate excitotoxicity: roles of chromatin remodelling and Bcl-2 induction. Int J Neuropsychopharmacol. 2013 Apr;16(3):607-20. doi: 10.1017/S1461145712000429. Epub 2012 May 8. [PubMed:22564541]
  3. FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]

Enzymes

Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...

Components:
References
  1. Argikar UA, Senekeo-Effenberger K, Larson EE, Tukey RH, Remmel RP: Studies on induction of lamotrigine metabolism in transgenic UGT1 mice. Xenobiotica. 2009 Nov;39(11):826-35. doi: 10.3109/00498250903188985. [PubMed:19845433]
  2. Chen H, Yang K, Choi S, Fischer JH, Jeong H: Up-regulation of UDP-glucuronosyltransferase (UGT) 1A4 by 17beta-estradiol: a potential mechanism of increased lamotrigine elimination in pregnancy. Drug Metab Dispos. 2009 Sep;37(9):1841-7. doi: 10.1124/dmd.109.026609. Epub 2009 Jun 22. [PubMed:19546240]
  3. Argikar UA, Remmel RP: Variation in glucuronidation of lamotrigine in human liver microsomes. Xenobiotica. 2009 May;39(5):355-63. doi: 10.1080/00498250902745082. [PubMed:19387891]
  4. Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [PubMed:15304429]
  5. Milosheska D, Lorber B, Vovk T, Kastelic M, Dolzan V, Grabnar I: Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters. Br J Clin Pharmacol. 2016 Aug;82(2):399-411. doi: 10.1111/bcp.12984. Epub 2016 May 29. [PubMed:27096250]
  6. Lamictal FDA Label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Nadph binding
Specific Function
Key enzyme in folate metabolism. Contributes to the de novo mitochondrial thymidylate biosynthesis pathway. Catalyzes an essential reaction for de novo glycine and purine synthesis, and for DNA pre...
Gene Name
DHFR
Uniprot ID
P00374
Uniprot Name
Dihydrofolate reductase
Molecular Weight
21452.61 Da
References
  1. Srinivasan B, Tonddast-Navaei S, Skolnick J: Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase. Eur J Med Chem. 2015 Oct 20;103:600-14. doi: 10.1016/j.ejmech.2015.08.021. Epub 2015 Sep 5. [PubMed:26414808]
  2. Das P, Ramaswamy S, Arora M, Samuels I, Gabel TL: Lamotrigine-induced neutropenia in a woman with schizoaffective disorder. Prim Care Companion J Clin Psychiatry. 2007;9(6):471-2. doi: 10.4088/pcc.v09n0611i. [PubMed:18185836]
  3. Lamictal FDA Label [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Poureshghi F, Ghandforoushan P, Safarnejad A, Soltani S: Interaction of an antiepileptic drug, lamotrigine with human serum albumin (HSA): Application of spectroscopic techniques and molecular modeling methods. J Photochem Photobiol B. 2017 Jan;166:187-192. doi: 10.1016/j.jphotobiol.2016.09.046. Epub 2016 Nov 5. [PubMed:27951518]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Luna-Tortos C, Fedrowitz M, Loscher W: Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008 Dec;55(8):1364-75. doi: 10.1016/j.neuropharm.2008.08.032. Epub 2008 Sep 11. [PubMed:18824002]
  2. Weiss J, Kerpen CJ, Lindenmaier H, Dormann SM, Haefeli WE: Interaction of antiepileptic drugs with human P-glycoprotein in vitro. J Pharmacol Exp Ther. 2003 Oct;307(1):262-7. doi: 10.1124/jpet.103.054197. Epub 2003 Sep 3. [PubMed:12954800]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. dofetilide - Drug Summary [Link]
  2. Lamictal FDA Label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Wagner DJ, Hu T, Wang J: Polyspecific organic cation transporters and their impact on drug intracellular levels and pharmacodynamics. Pharmacol Res. 2016 Sep;111:237-246. doi: 10.1016/j.phrs.2016.06.002. Epub 2016 Jun 16. [PubMed:27317943]
  2. Dickens D, Owen A, Alfirevic A, Giannoudis A, Davies A, Weksler B, Romero IA, Couraud PO, Pirmohamed M: Lamotrigine is a substrate for OCT1 in brain endothelial cells. Biochem Pharmacol. 2012 Mar 15;83(6):805-14. doi: 10.1016/j.bcp.2011.12.032. Epub 2011 Dec 29. [PubMed:22227272]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2020 01:55

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