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QuickView for Lamotrigine (compound)

Summary
General Info

PubChem

PubChem Compound 11139949

PubChem Compound 11139949

Name:	lamotrigine
PubChem Compound ID:	11139949
Molecular formula:	C₉H₇Cl₂N₅
Molecular weight:	263.043 g/mol

DrugBank

Identification

Name:	lamotrigine
Name (isomeric):	DB00555
Drug Type:	small molecule
Synonyms:	Lamotrigina [Spanish]; GW 273293; Lamotriginum [Latin]
Brand:	Lamictal CD, Lamictal, Lamictin, Lamictal XR
Category:	Antidepressants, Calcium Channel Blockers, Analgesics, Antimanic Agents, Anticonvulsants, Excitatory Amino Acid Antagonists
CAS number:	84057-84-1

Pharmacology

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.
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 ... show more » 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. show less «
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. in vitro pharmacological studies suggest that lamotrigine inhibits voltage-sensitive sodium channels and/or calcium channels, thereby stabilizing neuronal membranes and consequently modulating pr... show more » One proposed mechanism of action of Lamotrigine, the relevance of which remains to be established in humans, involves an effect on sodium channels. in vitro pharmacological studies suggest that lamotrigine inhibits voltage-sensitive sodium channels and/or calcium channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of excitatory amino acids (e.g., glutamate and aspartate). Studies on lamotrigine show binding to sodium channels similar to local anesthetics. show less «
Absorption:	98%
Protein binding:	55%
Biotransformation:	Hepatic
Half Life:	25 +/- 10 hours (healthy individuals); 42.9 hours (chronic renal failure)
Clearance:	Apparent plasma cl=0.44 mL/min/kg [healthy volunteers taking single-dose LAMICTAL] Apparent plasma cl=0.58 mL/min/kg [healthy volunteers taking multiple-dose LAMICTAL] Apparent plasma cl=0.30 mL/min/kg [healthy volunteers taking valproate and single-dose LAMICTAL] Apparent plasma cl=0.18 mL/min/kg [healthy volunteers taking valproate and multiple-dose LAMICTAL] Apparent plasma cl=1.1 mL/min/kg [Patients with epilepsy taking carbamazepine, phenytoin, phenobarbital, or primidone plus valproate and single-dose LAMICTAL] Apparent plasma cl=1.12 mL/min/kg [Patients with epilepsy taking carbamazepine, phenytoin, phenobarbital, or primidone plus valproate and multiple-dose LAMICTAL]
Toxicity:	LD₅₀=250 (mg/kg) (in rat, mice); LD₅₀>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.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take without regard to meals.

Drug interaction:

Divalproex sodium	Valproic acid increases the effect of lamotrigine
Ethotoin	Phenytoin may reduce levels of lamotrigine
Valproic Acid	Valproic acid may increase the adverse effects of Lamotrigine by increasing Lamotrigine serum concentration. The Lamotrigine dose should be reduced by 50% during concomitant therapy. Monitor for changes in Lamotrigine therapeutic and adverse effects if Valproic acid is initiated, discontinued or dose changed.
Norethindrone	The oral contraceptive decreases the effect of lamotrigine
Ethinyl Estradiol	The oral contraceptive decreases the effect of lamotrigine

Divalproex sodium	Valproic acid increases the effect of lamotrigine
Ethotoin	Phenytoin may reduce levels of lamotrigine
Valproic Acid	Valproic acid may increase the adverse effects of Lamotrigine by increasing Lamotrigine serum concentration. The Lamotrigine dose should be reduced by 50% during concomitant therapy. Monitor for changes in Lamotrigine therapeutic and adverse effects if Valproic acid is initiated, discontinued or dose changed.
Norethindrone	The oral contraceptive decreases the effect of lamotrigine
Ethinyl Estradiol	The oral contraceptive decreases the effect of lamotrigine
Phenytoin	Phenytoin may reduce levels of lamotrigine
Mephenytoin	Phenytoin may reduce levels of lamotrigine
Mestranol	The oral contraceptive decreases the effect of lamotrigine
Fosphenytoin	Phenytoin may reduce levels of lamotrigine
Rifampin	Rifampin decreases levels of lamotrigine
Carbamazepine	Lamotrigine may increase the adverse effects of carbamazepine by increasing the concentration of its active metabolite, carbamazepine-epoxide. Carbamazepine may decrease the therapeutic effect of lamotrigine by increasing its metabolism. Lamotrigine doses should be adjusted accordingly. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinue or doses are changed.
Triprolidine	The CNS depressants, Triprolidine and Lamotrigine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Desogestrel	The oral contraceptive decreases the effect of lamotrigine
Butabarbital	Barbiturates like butabarbital may decrease the serum concentration of lamotrigine. There are separate patient management guidelines for patients age 12 and under and for patients older than 12 years of age. Monitor for decreased serum concentrations/therapeutic effects of lamotrigine if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
Thiopental	Thiopental may increase the metabolism and clearance of Lamotrigine. Monitor for decreased therapeutic effect of Lamotrigine if Thiopental is initiated.
Butalbital	Barbiturates such as butalbital may decrease the serum concentration of lamotrigine. There are separate management guidelines for patients age 12 and under and for patients older than 12 years of age. Please refer to the current approved prescribing information for additional information. Monitor for decreased serum concentrations/therapeutic effects of lamotrigine if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
Clozapine	Lamotrigine increases the effect and toxicity of clozapine
Methsuximide	Methsuximide decreases the effect of lamotrigine

Targets

Sodium channel protein type 2 subunit alpha

Enzymes

UDP-glucuronosyltransferase 1-4

UDP-glucuronosyltransferase 1-3

Transporters

Multidrug resistance protein 1