Identification
- Summary
Lamotrigine is a phenyltriazine antiepileptic used to treat some types of epilepsy and bipolar I disorder.
- Brand Names
- Lamictal
- Generic Name
- Lamotrigine
- DrugBank Accession Number
- DB00555
- Background
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
Structure for Lamotrigine (DB00555)
- 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
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Bipolar 1 disorder •••••••••••• ••••• ••••••• ••••••• ••••••••• ••••••• •••••• •••••••••••••• Adjunct therapy in management of Partial seizures •••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• ••••••• Adjunct therapy in management of Partial seizures •••••••••••• ••••••• ••••••• ••••••••• ••••••• •••••• •••••••••••••• Prevention of Partial-onset seizures •••••••••••• Adjunct therapy in management of Primary generalized tonic-clonic seizures •••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• ••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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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
Target Actions Organism AVoltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E) inhibitorHumans AVoltage-gated sodium channel alpha subunit inhibitorHumans UAdenosine receptor A1 inhibitorHumans UAdenosine receptor A2a inhibitorHumans UAlpha-1A adrenergic receptor inhibitorHumans UAlpha-2A adrenergic receptor inhibitorHumans UBeta-1 adrenergic receptor inhibitorHumans UD(1) dopamine receptor inhibitorHumans UDopamine D2 receptor agonistinhibitorHumans UGABA(A) Receptor antagonistinducerHumans UGABA(A) Receptor Benzodiazepine Binding Site inhibitorHumans UHistamine H1 receptor antagonistHumans UKappa-type opioid receptor inhibitorHumans UAcetylcholine receptor subunit alpha inhibitorHumans U5-hydroxytryptamine receptor 2A inhibitorHumans U5-hydroxytryptamine receptor 3A inhibitorHumans UGlutamate receptor 1 inhibitorHumans - 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
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- 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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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
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Lamotrigine is combined with 1,2-Benzodiazepine. Abacavir The metabolism of Abacavir can be increased when combined with Lamotrigine. Acebutolol Lamotrigine may increase the arrhythmogenic activities of Acebutolol. Aceclofenac The risk or severity of hyperkalemia can be increased when Lamotrigine is combined with Aceclofenac. Acemetacin The risk or severity of hyperkalemia can be increased when Lamotrigine is combined with Acemetacin. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- 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
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Lamictal Tablet, for suspension 25 mg/1 Oral GlaxoSmithKline LLC 1998-09-03 Not applicable US 
Lamictal Tablet 2 mg Oral Glaxosmithkline Inc 2001-09-13 Not applicable Canada 
Lamictal Tablet 200 mg/1 Oral Lake Erie Medical &Surgical Supply Dba Quality Care Products Llc 2012-02-29 2017-06-01 US Lamictal Tablet 100 mg Oral Glaxosmithkline Inc 1995-12-31 Not applicable Canada Lamictal Tablet 25 mg/1 Oral Lake Erie Medical &Surgical Supply Dba Quality Care Products Llc 2012-02-29 2017-06-01 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ag-lamotrigine Tablet 150 mg Oral Angita Pharma Inc. Not applicable Not applicable Canada Ag-lamotrigine Tablet 100 mg Oral Angita Pharma Inc. Not applicable Not applicable Canada Ag-lamotrigine Tablet 25 mg Oral Angita Pharma Inc. Not applicable Not applicable Canada Apo-lamotrigine Tablet 150 mg Oral Apotex Corporation 2002-03-18 Not applicable Canada Apo-lamotrigine Tablet 100 mg Oral Apotex Corporation 2002-03-18 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Lamictal Lamotrigine (100 mg/1) + Lamotrigine (25 mg/1) Kit; Tablet Oral GlaxoSmithKline LLC 2003-09-29 Not applicable US Lamictal Lamotrigine (100 mg/1) + Lamotrigine (25 mg/1) Kit; Tablet Oral GlaxoSmithKline LLC 2003-09-29 Not applicable US Lamictal Lamotrigine (100 mg/1) + Lamotrigine (25 mg/1) Kit; Tablet Oral GlaxoSmithKline LLC 2003-09-29 Not applicable US Lamictal Lamotrigine (100 mg/1) + Lamotrigine (25 mg/1) Kit; Tablet Oral GlaxoSmithKline LLC 2003-09-29 Not applicable US Lamictal ODT Lamotrigine (50 mg/1) + Lamotrigine (100 mg/1) Kit; Tablet, orally disintegrating Oral GlaxoSmithKline LLC 2009-06-05 Not applicable US
Categories
- ATC Codes
- N03AX09 — Lamotrigine
- Drug Categories
- Agents causing hyperkalemia
- Agents producing tachycardia
- Anti-epileptic Agent
- Antiarrhythmic agents
- Anticholinergic Agents
- Anticonvulsants
- Bradycardia-Causing Agents
- Calcium Channel Blockers
- Calcium-Regulating Hormones and Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Decreased Central Nervous System Disorganized Electrical Activity
- Drugs causing inadvertant photosensitivity
- Drugs that are Mainly Renally Excreted
- Membrane Transport Modulators
- Miscellaneous Anticonvulsants
- Mood Stabilizer
- Muscarinic Antagonists
- Nervous System
- OCT1 substrates
- OCT2 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Photosensitizing Agents
- Potential QTc-Prolonging Agents
- Psychotropic Drugs
- QTc Prolonging Agents
- Sodium Channel Blockers
- Tranquilizing Agents
- Triazines
- UGT1A1 Inducers
- UGT1A1 Substrates
- UGT1A3 substrates
- UGT1A4 substrates
- 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)
- Affected organisms
- Humans and other mammals
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
- Backonja M: Neuromodulating drugs for the symptomatic treatment of neuropathic pain. Curr Pain Headache Rep. 2004 Jun;8(3):212-6. [Article]
- 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. [Article]
- Jensen TS: Anticonvulsants in neuropathic pain: rationale and clinical evidence. Eur J Pain. 2002;6 Suppl A:61-8. [Article]
- Pappagallo M: Newer antiepileptic drugs: possible uses in the treatment of neuropathic pain and migraine. Clin Ther. 2003 Oct;25(10):2506-38. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Garnett WR: Lamotrigine: pharmacokinetics. J Child Neurol. 1997 Nov;12 Suppl 1:S10-5. doi: 10.1177/0883073897012001041. [Article]
- 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. [Article]
- 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. [Article]
- Rambeck B, Wolf P: Lamotrigine clinical pharmacokinetics. Clin Pharmacokinet. 1993 Dec;25(6):433-43. doi: 10.2165/00003088-199325060-00003. [Article]
- 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. [Article]
- 44. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 544, 549). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- Lamictal FDA Label [Link]
- FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
- FDA Approved Drug Products: LAMICTAL (lamotrigine) tablets [Link]
- FDA Approved Drug Products: LAMICTAL XR (lamotrigine) extended-release tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014695
- KEGG Drug
- D00354
- PubChem Compound
- 3878
- PubChem Substance
- 46505408
- ChemSpider
- 3741
- BindingDB
- 50031299
- 28439
- ChEBI
- 6367
- ChEMBL
- CHEMBL741
- ZINC
- ZINC000000013156
- Therapeutic Targets Database
- DAP000039
- PharmGKB
- PA450164
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- IYJ
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Lamotrigine
- PDB Entries
- 8thh
- FDA label
- Download (1.12 MB)
- MSDS
- Download (24.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Not Available Hippocampal Atrophy Due to Corticosteroid / Hypomania Due to Corticosteroid Use / Memory Impairment Due to Corticosteroid Use 1 4 Completed Basic Science Epilepsy 2 4 Completed Basic Science Healthy Subjects (HS) 1 4 Completed Health Services Research Memory Disturbances 1 4 Completed Prevention Bipolar Disorder (BD) 1
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
Form Route Strength Tablet, for suspension Oral 100 MG Tablet, for suspension Oral 200 MG Tablet, for suspension Oral 25 MG Tablet, for suspension Oral 5 MG Tablet, for suspension Oral 50 MG Tablet Oral 100.0 mg Tablet Oral 25.0 mg Tablet, coated Oral 750 mg Tablet, soluble Oral 50 mg Tablet Oral 10.000 mg Tablet Oral 100 mg/1 Tablet Oral 150 mg/1 Tablet Oral 150 mg Tablet Oral 2 mg Tablet, chewable Oral 100 MG Tablet, for suspension Oral 2 mg/1 Tablet, soluble Oral 5 MG Tablet Oral 200 mg Tablet, extended release Oral 200 mg Tablet, extended release Oral 300 mg Tablet, chewable Oral Tablet, chewable Oral 5 mg Tablet, for solution; tablet, for suspension Oral 5 MG Tablet, chewable Oral 50 mg Tablet Oral 5.000 mg Tablet, film coated Oral 2 mg Tablet Oral 5 mg Tablet, effervescent Oral Tablet, soluble Oral 100 mg Kit; tablet, film coated, extended release Oral Tablet, film coated, extended release Oral 250 mg/1 Tablet, film coated, extended release Oral 300 mg/1 Tablet, extended release Oral 100 mg Tablet, soluble Oral 25 mg Tablet, extended release Oral 50 mg Tablet, extended release Oral 25 mg Tablet Oral Tablet, soluble Oral Tablet, for solution; tablet, for suspension Oral 200 MG Tablet, for solution; tablet, for suspension Oral 25 MG Tablet, for solution; tablet, for suspension Oral 100 MG Tablet, for solution; tablet, for suspension Oral 50 MG Tablet, soluble Oral 2500000 mg Tablet, soluble Oral 5000000 mg Tablet, for suspension Oral Tablet, soluble Oral 200 mg Tablet, soluble Oral 10000000 mg Kit Oral Kit; tablet Oral Kit; tablet, orally disintegrating Oral Tablet Oral 200 mg/1 Tablet Oral 25 mg/1 Tablet, chewable Oral 2 mg/1 Tablet, chewable Oral 25 mg/1 Tablet, chewable Oral 5 mg/1 Tablet, extended release Oral 100 mg/1 Tablet, extended release Oral 200 mg/1 Tablet, extended release Oral 25 mg/1 Tablet, extended release Oral 250 mg/1 Tablet, extended release Oral 300 mg/1 Tablet, extended release Oral 50 mg/1 Tablet, film coated, extended release Oral 100 mg/1 Tablet, film coated, extended release Oral 200 mg/1 Tablet, film coated, extended release Oral 25 mg/1 Tablet, film coated, extended release Oral 50 mg/1 Tablet, for suspension Oral 25 mg/1 Tablet, for suspension Oral 5 mg/1 Tablet, orally disintegrating Oral 100 mg/1 Tablet, orally disintegrating Oral 200 mg/1 Tablet, orally disintegrating Oral 25 mg/1 Tablet, orally disintegrating Oral 50 mg/1 Tablet Oral 250 mg/1 Tablet Oral 300 mg/1 Tablet Oral 50 mg/1 Tablet Oral 50.0 mg Tablet, chewable Oral 200 mg Tablet, chewable Oral 25 mg Tablet Oral 100.000 mg Tablet Oral 25.000 mg Tablet, chewable Oral 2 mg Tablet Oral 100 mg Tablet Oral 25 mg Tablet Oral 50 mg Tablet, coated Oral 100 mg Tablet, coated Oral 25 mg Tablet, coated Oral 50 mg - Prices
Unit description Cost Unit LaMICtal Starter 98 25 (84)-100(14)mg Kit Box 556.69USD box LaMICtal XR 200 mg 24 Hour tablet 12.11USD tablet Lamictal xr 200 mg tablet 11.65USD tablet LaMICtal XR 100 mg 24 Hour tablet 11.36USD tablet Lamictal xr 100 mg tablet 10.92USD tablet Lamictal xr 50 mg tablet 10.2USD tablet Lamictal 200 mg tablet 7.44USD tablet Lamictal odt start kt (orange) 7.28USD tablet Lamictal xr start kit (orange) 7.28USD tablet Lamictal odt 200 mg tablet 6.95USD tablet Lamictal odt 100 mg tablet 5.82USD tablet Lamotrigine 200 mg tablet 5.78USD tablet LaMICtal 25 mg Chew Tabs 5.63USD tab Lamictal odt 50 mg tablet 5.46USD tablet Lamictal tab start kit (green) 5.46USD tablet Lamictal 150 mg tablet 5.38USD tablet Lamictal odt 25 mg tablet 5.1USD tablet Lamictal xr 25 mg tablet 5.1USD tablet Lamictal 100 mg tablet 4.72USD tablet Lamotrigine tablet starter kit 4.24USD tablet Lamotrigine 150 mg tablet 3.98USD tablet Lamictal 25 mg tablet 3.78USD tablet Lamotrigine 100 mg tablet 3.52USD tablet LamoTRIgine 25 mg Chew Tabs 3.33USD tab LamoTRIgine 5 mg Chew Tabs 3.18USD tab Lamotrigine 25 mg tablet 2.9USD tablet Apo-Lamotrigine 150 mg Tablet 1.31USD tablet Mylan-Lamotrigine 150 mg Tablet 1.31USD tablet Novo-Lamotrigine 150 mg Tablet 1.31USD tablet Pms-Lamotrigine 150 mg Tablet 1.31USD tablet Ratio-Lamotrigine 150 mg Tablet 1.31USD tablet Apo-Lamotrigine 100 mg Tablet 0.88USD tablet Mylan-Lamotrigine 100 mg Tablet 0.88USD tablet Novo-Lamotrigine 100 mg Tablet 0.88USD tablet Pms-Lamotrigine 100 mg Tablet 0.88USD tablet Ratio-Lamotrigine 100 mg Tablet 0.88USD tablet Apo-Lamotrigine 25 mg Tablet 0.22USD tablet Mylan-Lamotrigine 25 mg Tablet 0.22USD tablet Novo-Lamotrigine 25 mg Tablet 0.22USD tablet Pms-Lamotrigine 25 mg Tablet 0.22USD tablet Ratio-Lamotrigine 25 mg Tablet 0.22USD tablet Lamictal 5 mg Chewable Tablet 0.18USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5698226 No 1997-12-16 2012-07-29 US CA2277722 No 2001-03-27 2012-01-29 Canada US9144547 No 2015-09-29 2023-09-22 US US8637512 No 2014-01-28 2028-06-14 US US8840925 No 2014-09-23 2028-07-02 US US7919115 No 2011-04-05 2029-01-04 US US9339504 No 2016-05-17 2028-07-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 177-181 https://www.chemicalbook.com/ChemicalProductProperty_US_CB4166704.aspx boiling point (°C) 503.1±60.0 https://www.chemicalbook.com/ChemicalProductProperty_US_CB4166704.aspx water solubility 0.17 mg/mL FDA label logP 1.93 http://www.t3db.ca/toxins/T3D2570 pKa 5.7 FDA label - Predicted Properties
Property Value Source Water Solubility 0.488 mg/mL ALOGPS logP 1.87 ALOGPS logP 1.93 Chemaxon logS -2.7 ALOGPS pKa (Strongest Acidic) 14.98 Chemaxon pKa (Strongest Basic) 5.89 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 90.71 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 66.62 m3·mol-1 Chemaxon Polarizability 23.1 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9382 Caco-2 permeable + 0.8867 P-glycoprotein substrate Non-substrate 0.7155 P-glycoprotein inhibitor I Non-inhibitor 0.911 P-glycoprotein inhibitor II Non-inhibitor 0.9604 Renal organic cation transporter Non-inhibitor 0.8176 CYP450 2C9 substrate Non-substrate 0.9162 CYP450 2D6 substrate Non-substrate 0.9055 CYP450 3A4 substrate Non-substrate 0.6862 CYP450 1A2 substrate Non-inhibitor 0.611 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.7007 CYP450 2C19 inhibitor Non-inhibitor 0.8594 CYP450 3A4 inhibitor Non-inhibitor 0.7678 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5515 Ames test Non AMES toxic 0.8202 Carcinogenicity Non-carcinogens 0.7895 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.7556 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9168 hERG inhibition (predictor II) Non-inhibitor 0.8735
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 146.5280483 predictedDarkChem Lite v0.1.0 [M-H]- 154.19135 predictedDeepCCS 1.0 (2019) [M+H]+ 146.3922483 predictedDarkChem Lite v0.1.0 [M+H]+ 156.54933 predictedDeepCCS 1.0 (2019) [M+Na]+ 147.0034483 predictedDarkChem Lite v0.1.0 [M+Na]+ 162.64249 predictedDeepCCS 1.0 (2019)
Targets
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- 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
- 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. [Article]
- 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
- 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. [Article]
- 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]
- Lamictal FDA Label [Link]
- 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
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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. [Article]
- FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- AgonistInhibitor
- 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
- 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. [Article]
- 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. [Article]
- FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- AntagonistInducer
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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
- 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. [Article]
- 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. [Article]
- FDA Approved Products: Lamictal (lamotrigine) chewable dispersible tablets [Link]
Enzymes
- 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
- 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. [Article]
- 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. [Article]
- Lamictal FDA Label [Link]
- 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
- 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. [Article]
- 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. [Article]
- Argikar UA, Remmel RP: Variation in glucuronidation of lamotrigine in human liver microsomes. Xenobiotica. 2009 May;39(5):355-63. doi: 10.1080/00498250902745082. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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. [Article]
- 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. [Article]
- 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
- 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
- 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. [Article]
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55