Aptiom by Sunovion Pharmaceuticals Inc

Pharmacy Times, September 2014 Oncology, Volume 80, Issue 9

Aptiom (eslicarbazepine acetate) by Sunovion Pharmaceuticals Inc has been approved by the FDA as an adjunctive treatment of partial-onset seizures in adult patients. An estimated 2.2 million Americans are affected by epilepsy, with partial-onset seizures accounting for 60% of new epilepsy diagnoses. Aptiom is not classified as a controlled substance.1,2

Pharmacology and Pharmacokinetics

The exact mechanism of Aptiom is unknown, but the drug is believed to exert its anticonvulsant effect through the inhibition of voltage-gated sodium channels.

Aptiom reaches peak plasma concentrations 1 to 4 hours after oral administration. Food does not affect its pharmacokinetics. Aptiom is rapidly and extensively metabolized to its major active metabolite by hydrolytic first-pass metabolism. Its elimination is primarily renal. Age, gender, and race do not affect the pharmacokinetics of Aptiom.1

Dosage and Administration

Treatment with Aptiom should be initiated at a dosage of 400 mg once daily. After 1 week, the dosage should be increased to 800 mg once daily, which is the recommended maintenance dose. Some patients may benefit from the maximum maintenance dose of 1200 mg once daily; however, this dose is associated with an increase in adverse reactions and should only be initiated after the patient has tolerated the 800-mg dose for 1 week.

Patients with a creatinine clearance less than 50 mL/min should begin treatment at a dosage of 200 mg once daily for 2 weeks. Then the dosage should be increased to 400 mg once daily, which is the recommended maintenance dosage. The maximum maintenance dosage for these patients is 600 mg once daily.

No dosage adjustments are necessary in patients with mild to moderate hepatic impairment. Aptiom has not been studied in patients with severe hepatic impairment and should not be used in these patients.

Discontinuation of Aptiom should be gradual to minimize the risk of increased epileptic activity. Aptiom should not be used concurrently with oxcarbazepine.1

Clinical Trials

Aptiom was evaluated in 3 randomized, double-blind, placebo-controlled multicenter trials of more than 1400 adult patients with partial-onset epilepsy that was not adequately controlled with 1 to 3 antiepileptic drugs. The studies found statistically significant reductions in standardized seizure frequency in patients using Aptiom compared with patients using placebo, with the Aptiom group experiencing a reduction of 50% or more in seizure frequency.1,2

Contraindications, Warnings, and Precautions

The use of Aptiom is contraindicated in patients with a hypersensitivity to eslicarbazepine acetate or oxcarbazepine.

Antiepileptic drugs, including Aptiom, increase the risk of suicidal thoughts or behavior; therefore, patients should be monitored accordingly. Patients should be monitored for serious dermatologic reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis. Aptiom should be discontinued immediately if a dermatologic reaction develops. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), anaphylaxis, and angioedema have been reported during treatment with Aptiom. Hyponatremia may develop during Aptiom use. Neurologic changes (eg, dizziness, gait or coordination disturbance, somnolence, fatigue, cognitive dysfunction, visual changes) may also occur. Patients taking Aptiom should exercise caution when operating machinery or driving. Aptiom should be discontinued if jaundice or liver injury occurs.

Concurrent use of carbamazepine may require dose adjustments of Aptiom or carbamazepine. Concurrent use of phenytoin may require a higher dose of Aptiom and a dose adjustment of phenytoin, based on clinical response and the serum level of phenytoin. When Aptiom is used concurrently with phenobarbital or primidone, a higher dose of Aptiom may be necessary. Aptiom may decrease the effectiveness of hormonal contraceptives.

Aptiom is a Pregnancy Category C medication. It should not be used in women who are breast-feeding. It is not approved for patients younger than 18 years.

The most common adverse reactions during the use of Aptiom were dizziness, somnolence, nausea, headache, diplopia, vomiting, fatigue, vertigo, ataxia, blurred vision, and tremor.

Dr. Holmberg earned her PharmD from the University of Connecticut and completed an ambulatory care residency at the Phoenix VA Healthcare System. Her practice has also included pediatrics and inpatient mental health. She resides in Phoenix, Arizona.

References

  • Aptiom [package insert]. Marlborough, MA: Sunovion Pharmaceuticals Inc; 2013. www.aptiom.com/Aptiom-Prescribing-Information.pdf. Accessed August 2014.
  • Sunovion Pharmaceuticals Inc announces FDA approval of Aptiom (eslicarbazepine acetate) as once-daily adjunctive treatment of partial-onset seizures. Sunovion Pharmaceuticals Inc website. www.sunovion.com/news/aptiom-press-room.html. Accessed June 2014.