- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
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Overview
| Generic Names: | GW 273293; Lamotrigina [Spanish]; Lamotriginum [Latin]; lamotrigine |
|---|---|
| Trade Names: | Lamictal; Lamictal CD; Lamictal XR; Lamictin |
| PharmGKB Accession Id: | PA450164 |
Description
Lamotrigine is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. For epilepsy it is used to treat partial seizures, primary and secondary tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome. Lamotrigine also acts as a mood stabilizer. It is the first medication since lithium granted Food and Drug Administration (FDA) approval for the maintenance treatment of bipolar type I. Chemically unrelated to other anticonvulsants, lamotrigine has relatively few side-effects and does not require blood monitoring. The exact way lamotrigine works is unknown. Wikipedia (source: Drug Bank)
Indication
For the adjunctive treatment of partial seizures in epilepsy and generalized seizures of Lennox-Gastaut syndrome. Also for the maintenance treatment of bipolar I disorder and depression. (source: Drug Bank)
ATC Therapeutic Category
- N03AX:Other antiepileptics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
One proposed mechanism of action of Lamotrigine, the relevance of which remains to be established in humans, involves an effect on sodium channels. <i>in vitro</i> pharmacological studies suggest that lamotrigine inhibits voltage-sensitive sodium channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of excitatory amino acids (e.g., glutamate and aspartate). (source: Drug Bank)
Pharmacology
Lamotrigine, an antiepileptic drug (AED) of the phenyltriazine class, is chemically unrelated to existing antiepileptic drugs. Lamotrigine is also used in the treatment of depression and bipolar disorder. Lamotrigine is thought to exert its anticonvulsant effect by stabilizing presynaptic neuronal membranes. Lamotrigine inhibits sodium currents by selectively binding to the inactivated state of the sodium channel and subsequently suppresses the release of the excilatory amino acid, glutamate. (source: Drug Bank)
Food Interactions
Take without regard to meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
55% (source: Drug Bank)
Absorption
98% (source: Drug Bank)
Toxicity
LD<sub>50</sub>=250 (mg/kg) (in rat, mice); LD<sub>50</sub>>640 orally (mg/kg) (in rat, mice) (Sawyer). Symptoms of overdose include decreased level of consciousness, coma, delayed heartbeat, increased seizures, lack of coordination, and rolling eyeballs. (source: Drug Bank)
Isomeric SMILES Code:
c1cc(c(c(c1)Cl)Cl)c2c(nc(nn2)N)N (source: Drug Bank)
Curated Annotations (
)
-
rs2304016
at chr2:165876749
in
SCN2A,
SCN2A2
The A allele of this SNP was associated with resistance to sodium channel-blocking anti-epileptic drugs in a Chinese patient population.- Variant Name:
- SCN2A:IVS7-32A>G
- Related Drugs:
- carbamazepine, lamotrigine, oxcarbazepine, phenytoin, topiramate
- Related Diseases:
- Epilepsy
- Evidence:
-
PMID:18784617
-
rs2032582
at chr7:86998554
in
ABCB1
This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).- Variant Name:
- ABCB1: 2677T/A>G
- Related Drugs:
- carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
- Related Diseases:
- Epilepsy
- Evidence:
-
PMID:19450124
-
rs3789243
at chr7:87058822
in
ABCB1
This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).- Related Drugs:
- carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
- Related Diseases:
- Epilepsy
- Evidence:
-
PMID:19450124
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ABCB1 |
|
Publications, Variants |
|
HLA-B |
|
Publications |
|
|
SCN2A |
|
Variants |
|
|
SCN2A2 |
|
Variants |
|
|
UGT1A4 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| carbamazepine |
|
Carbamazepine decreases the effect of lamotrigine (source: Drug Bank) |
| clozapine |
|
Lamotrigine increases the effect and toxicity of clozapine (source: Drug Bank) |
| desogestrel |
|
The oral contraceptive decreases the effect of lamotrigine (source: Drug Bank) |
| estradiol |
|
The oral contraceptive decreases the effect of lamotrigine (source: Drug Bank) |
| ethinyl estradiol |
|
The oral contraceptive decreases the effect of lamotrigine (source: Drug Bank) |
| ethotoin |
|
Phenytoin may reduce levels of lamotrigine (source: Drug Bank) |
| fosphenytoin |
|
Phenytoin may reduce levels of lamotrigine (source: Drug Bank) |
| mephenytoin |
|
Phenytoin may reduce levels of lamotrigine (source: Drug Bank) |
| mestranol |
|
The oral contraceptive decreases the effect of lamotrigine (source: Drug Bank) |
| methsuximide |
|
Methsuximide decreases the effect of lamotrigine (source: Drug Bank) |
| norethindrone |
|
The oral contraceptive decreases the effect of lamotrigine (source: Drug Bank) |
| phenytoin |
|
Phenytoin may reduce levels of lamotrigine (source: Drug Bank) |
| rifampin |
|
Rifampin decreases levels of lamotrigine (source: Drug Bank) |
| sodium |
|
Valproic acid increases the effect of lamotrigine (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Drug Hypersensitivity |
|
Publications |
|
|
Drug Toxicity |
|
Publications |
|
|
Epidermal Necrolysis, Toxic |
|
Publications |
|
|
Epilepsy |
|
Publications, Variants |
|
|
Stevens-Johnson Syndrome |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.