Supernus Pharmaceuticals received approval from the FDA for Oxtellar XR (oxcarbazepine extended-release tablets) for use as adjunctive therapy in the treatment of partial seizures in adults and in children 6–17 years of age. Supernus制药公司获得FDA批准Oxtellar XR（奥卡西平缓释片）用于治疗成人和儿童部分性癫痫发作的辅助治疗6-17岁。

Oxtellar XR is a novel once-daily extended release formulation of oxcarbazepine (formerly known as SPN-804). Oxtellar XR是一种新的每日一次的缓释配方的奥卡西平（前身为SPN-804）。

The product will be available as 150mg, 300mg and 600mg extended-release tablets in 100-count bottles.该产品将提供150毫克，300毫克和600毫克缓释片在100数瓶。 Oxtellar XR is expected to launch in the first quarter of 2013. Oxtellar XR预计将在2013年第一季度推出。
 

OXTELLAR XR Rx

Pharmacological Class:
Dibenzazepine.

Active Ingredient(s):
Oxcarbazepine 150mg, 300mg, 600mg; extended-release tablets.

Company
Supernus Pharmaceuticals

Indication(s):

Adjunctive therapy in the treatment of partial seizures in adults and in children 6–17 years of age.

Pharmacology:

The precise mechanism by which oxcarbazepine and 10-monohydroxy metabolite (MHD) exert their antiseizure effect is unknown; however, in vitro studies indicate that they produce blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and diminution of propagation of synaptic impulses. In addition, increased potassium conductance and modulation of high-voltage activated calcium channels may contribute to the anticonvulsant effects of oxcarbazepine.

Clinical Trials:

The safety and efficacy of Oxtellar XR was eva luated in a multicenter, randomized, double-blind, placebo-controlled, three-arm parallel-group study (Study 1) in adult patients with refractory partial epilepsy aged 18–65 years (n=366). The study included an 8-week baseline period, followed by a treatment period (4-week titration phase followed by a 12-week maintenance phase). The primary endpoint was median percentage change from baseline in seizure frequency per 28 days during treatment period relative to the baseline period. The criterion for statistical significance was p<0.05. Patients were randomized to one of three treatment groups and were given Oxtellar XR 1.2g/day (n=122), Oxtellar XR 2.4g/day (n=123), or placebo (n=121). The primary efficacy results demonstrated a median percent change in seizure frequency of -38.2% (p<0.078) and -42.9% (p<0.003) in the Oxtellar XR 1.2g/day and 2.4g/day treatment groups, respectively vs. -28.7% in the placebo group. Although the 1.2g/day vs. placebo contrast did not reach statistical significance, concentration-response analyses reveal that the 1.2g/day dose is an effective dose.

Legal Classification:

Rx

Adults:

Take on empty stomach. Swallow whole. >17yrs: Initially 600mg once daily for 1 week, then may increase by 600mg/day increments at weekly intervals; usual range 1.2g–2.4g/day. Concomitant antiepileptics: consider initiating at 900mg once daily. Severe renal impairment (CrCl <30mL/min): initially 300mg/day; may increase by 300–450mg/day increments at weekly intervals. ESRD on dialysis: use oxcarbazepine immediate-release. Elderly: initially 300mg or 450mg once daily; may increase by 300–450mg/day increments at weekly intervals. Conversion from oxcarbazepine immediate-release: may need higher doses.

Children:

<6yrs: not recommended. 6–17yrs: initially 8–10mg/kg once daily; max 600mg/day in the 1st week, then may increase by 8–10mg/kg/day increments at weekly intervals; usual max 600mg/day. Target maintenance doses (attain over 2–3 weeks): 20–29kg: 900mg/day; 29.1–39kg: 1.2g/day; >39kg: 1.8g/day.

Warnings/Precautions:

Risk of hyponatremia; monitor if signs/symptoms occur. Severe hepatic impairment: not recommended. Carbamazepine hypersensitivity. Suicidal behavior and ideation; monitor. Discontinue if multi-organ hypersensitivity occurs; use alternative treatment. Avoid abrupt withdrawal. Elderly. Pregnancy (Cat.C): risk of seizures; monitor during and postpartum. Nursing mothers: not recommended.

Interaction(s)

Antagonized by phenytoin, carbamazepine, phenobarbital, valproic acid; monitor and adjust dose. May decrease effectiveness of hormonal contraceptives (ethinyl estradiol, levonorgestrel), other oral or implant contraceptives; use additional non-hormonal forms. Caution with other drugs known to decrease serum sodium. May affect thyroid (T4) tests.

Adverse Reaction(s)

Dizziness, somnolence, headache, balance disorder, tremor, vomiting, diplopia, asthenia, fatigue; hyponatremia, serious skin reactions (eg, Stevens-Johnson syndrome and toxic epidermal necrolysis); rare: anaphylactic reactions, angioedema, hematological reactions; discontinue if occurs.

How Supplied:

Tabs—100

LAST UPDATED:

2/14/2013