Overview
11 DESCRIPTION The chemical name of eslicarbazepine acetate is (S)-10-Acetoxy-10,11-dihydro-5Hdibenz[b,f]azepine-5-carboxamide. Eslicarbazepine acetate is a dibenz[b,f]azepine-5-carboxamide derivative. Its molecular formula is C 17 H 16 N 2 O 3 and its molecular weight is 296.32. The chemical structure is: Eslicarbazepine acetate is a white to off-white crystalline powder.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Eslicarbazepine acetate is extensively converted to eslicarbazepine, which is considered to be responsible for therapeutic effects in humans. The precise mechanism(s) by which eslicarbazepine exerts anticonvulsant activity is unknown but is thought to involve inhibition of voltage-gated sodium channels. 12.2 Pharmacodynamics The effect of eslicarbazepine acetate on cardiac repolarization was evaluated in a randomized, double-blind, placebo-and active-controlled 4-period crossover trial in healthy adult men and women. Subjects received eslicarbazepine acetate 1,200 mg once daily × 5 days, eslicarbazepine acetate 2,400 mg once daily × 5 days, an active-control, moxifloxacin 400 mg × 1 dose on Day 5, and placebo once daily × 5 days.
Indications
- 1 INDICATIONS AND USAGE Eslicarbazepine acetate tablets are indicated for the treatment of partial-onset seizures in patients 4 years of age and older. Eslicarbazepine acetate tablets are indicated for the treatment of partial-onset seizures in patients 4 years of age and older. ( 1 )
Common Doses
- 400 mg
- 800 mg
- 600 mg
- 200 mg
Dosage
2 DOSAGE AND ADMINISTRATION • Adult Patients: The recommended initial dosage of eslicarbazepine acetate is 400 mg once daily. For some patients, treatment may be initiated at 800 mg once daily if the need for seizure reduction outweighs an increased risk of adverse reactions. Increase the dose in weekly increments of 400 mg to 600 mg once daily, based on clinical response and tolerability, to a recommended maintenance dosage of 800 mg to 1,600 mg once daily. ( 2.
Contraindications
- 4 CONTRAINDICATIONS Eslicarbazepine acetate tablets are contraindicated in patients with a hypersensitivity to eslicarbazepine acetate or oxcarbazepine [see Warnings and Precautions ( 5.2 , 5.3 , and 5.4 )]. Hypersensitivity to eslicarbazepine acetate or oxcarbazepine. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are described in more detail in the Warnings and Precautions section of the label: • Suicidal Behavior and Ideation [see Warnings and Precautions ( 5.1 )] • Serious Dermatologic Reactions [see Warnings and Precautions ( 5.2 )] • Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity [see Warnings and Precautions ( 5.3 )] • Anaphylactic Reactions and Angioedema [see Warnings and Precautions ( 5.4 )] • Hyponatremia [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS • Carbamazepine: May need dose adjustment for eslicarbazepine acetate or carbamazepine. ( 2.3 , 5.6 , 7.1 ) • Phenytoin: Higher dosage of eslicarbazepine acetate may be necessary and dose adjustment may be needed for phenytoin. ( 2.3 , 7.1 , 7.2 ) • Phenobarbital or Primidone: Higher dosage of eslicarbazepine acetate may be necessary. ( 2.3 , 7.1 ) • Hormonal Contraceptives: Eslicarbazepine acetate may decrease the effectiveness of hormonal contraceptives. ( 7.4 , 8.3 ) 7.1 Other Antiepileptic Drugs Several AEDs (e.g.