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QuickView for Lamotrigine (compound)


PubChem
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 ...
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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...
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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 sodiumValproic acid increases the effect of lamotrigine
EthotoinPhenytoin may reduce levels of lamotrigine
Valproic AcidValproic 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.
NorethindroneThe oral contraceptive decreases the effect of lamotrigine
Ethinyl EstradiolThe oral contraceptive decreases the effect of lamotrigine
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