Clinical Information

Lamotrigine (Lamictal) is approved for therapy of bipolar I disorder and a wide variety of seizure disorders including Lennox-Gastaut syndrome, primary generalized tonic-clonic seizures, and partial seizures. Its many off-label uses include treatment of migraine, trigeminal neuralgia, and treatment-refractory depression. Lamotrigine inhibits glutamate release (an excitatory amino acid) and voltage-sensitive sodium channels to stabilize neuronal membranes; it also weakly inhibits the 5-HT3 (serotonin) receptor.

Lamotrigine oral bioavailability is very high (approximately 98%).The drug is metabolized by glucuronic acid conjugation to inactive metabolites. The half-life is 25 to 33 hours in adults, but decreases with concurrent use of phenytoin or carbamazepine (13-14 hours), and increases with concomitant valproic acid therapy (59-70 hours), renal dysfunction, or hepatic impairment. The therapeutic range is relatively wide, 2.5 to 15 mcg/mL for most individuals. Common adverse effects are dizziness, ataxia, blurred or double vision, nausea, or vomiting.