Eslicarbazepine

Actions

• Blocks voltage-dependent Na+ channels at high firing frequencies.
• Exerts effect on K+ channels.

Metabolism

Hepatic

Enzymes involved

• CYP3A4
• CYP2C19

Elimination

Renal

Enzyme induction

• CYP3A4
• CYP3A5
• UGT

Enzyme inhibition

• CYP2C19

Half-life

10–20 hours

Plasma protein binding

~30%

Important side-effects

Serious dermatologic reactions including Stevens-Johnson syndrome and TEN. As with carbamazepine, the risk is especially high in patients of Chinese ancestry that are carriers of the HLA-B*1502 allele. Moderate high risk of dermatologic reactions is also found in patients of European, Japanese or Korean ancestry that are carriers of the HLA-A*3101 allele.

Hyponatremia. Risk is higher in patients treated with diuretics or drugs associated with inappropriate ADH secretion, elderly and patients with renal disease associated with low sodium levels

Suicidal behaviour and ideation

Indications

Focal seizures with or without generalisation

May aggravate myoclonic and absence seizures.

Dosing recommendation

Start with 400 mg/day.

Increase to target dose after 1–2 weeks.

Target dose: 800–1200 mg/day in a simgle dose.

Renal impairment

Dose reduction might be necessary in patients with moderately impaired renal function (creatinine clearance 30-60 ml/min). Eslicarbazepine is not recommended in patients with severely impaired renal function.

Hepatic impairment

No dose reduction is necessary in patients with mildly or moderately impaired hepatic function. Insufficient data exist for patients with severely impaired hepatic function.