Product: Vimpat
Company: UCB
Pharmacologic class: Anti-epileptic (sodium channel inactivator)
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Active ingredient: Lacosamide 50 mg, 100 mg, 150 mg, 200 mg; tabs.
Indication: Adjunct in partial-onset seizures.
Also: Vimpat injection
Active ingredient: Lacosamide 10 mg/mL; solution for IV infusion.
Indication: Adjunct in partial-onset seizures, when oral administration is not feasible.
Pharmacology: Lacosamide selectively enhances the slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing. It also binds to collapsin response mediator protein-2, which is involved in neuronal differentiation and control of axonal growth. The exact mechanism of action of lacosamide in treating epilepsy is not known.
Lacosamide has been shown to have no significant pharmacokinetic interactions with carbamazepine or valproate. Steady-state plasma levels of concomitant antiepileptic drugs (AEDs) were unaffected by lacosamide.
Lacosamide is completely absorbed after oral administration. It has a bioavailability of about 100%. The 30- and 60-minute IV infusions are bioequivalent to the oral tabs.
Clinical trials: Three 12-week trials were conducted to establish the efficacy of lacosamide. These studies enrolled approximately 1,300 patients with partial-onset seizures with or without generalization who were not adequately controlled with one to three concomitant AEDs. In each study, an eight-week baseline phase was followed by randomization and a titration phase, then a maintenance phase that lasted 12 weeks during which patients remained on a stable dose of lacosamide. Study 1 compared lacosamide 200 mg, 400 mg, and 600 mg/day with placebo; Study 2 compared lacosamide 400 mg and 600 mg/day with placebo, and Study 3 compared lacosamide 200 mg and 400 mg/day with placebo. The reduction in 28-day seizure frequency (baseline to maintenance phase) compared with placebo was the primary efficacy variable in each study.
At doses of 200 mg, 400 mg, and 600 mg daily, lacosamide was shown to be significantly superior to placebo in reducing seizure frequency. The 600-mg/day dose was not more effective than the 400-mg/day dose.
Adults: Injection: may give without diluting, or mix in appropriate diluent and give by IV infusion over 30-60 minutes. For oral and injection: >17 years: initially 50 mg twice daily; may increase at weekly intervals by 100 mg/day in two divided doses. Maintenance dose: 200-400 mg/day. Renal impairment (cretinine clearance >30 mL/min), end-stage renal disease, mild-to-moderate hepatic impairment: maximum 300 mg/day. Consider supplemental dose (50%) after hemodialysis. Avoid abrupt cessation.
Children: <17 years: not recommended.
Precautions: Severe hepatic impairment: not recommended. Cardiac conduction disturbances (e.g., second-degree atrioventricular block). Severe cardiac disease (e.g., myocardial ischemia, heart failure). Monitor for suicidal ideation, depression. Diabetic neuropathy. Elderly. Pregnancy (Cat. C). Nursing mothers: not recommended.
Interactions: Caution with other drugs that cause PR prolongation.
Adverse reactions: Dizziness, ataxia, diplopia, headache, GI upset, syncope; rare: multi-organ hypersensitivity reaction.
Note: To enroll in the UCB AED Pregnancy Registry call 888.537.7734.
How supplied: Tabs—60, 180 Single-use vials (20 mL)—10
For more information, call 800.477.7877 or visit www.Vimpat.com.
