Eslicarbazepine acetate

(S )-10- acetoxy -10 ,11 -dihydro -5H- dibenz [b, f] azepine -5 -carboxamide

N03AF04

Antiepileptic

Blockade of sodium channels

Attention

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Eslicarbazepine acetate is a chemical compound that is used as a drug for long-term treatment of certain forms of epilepsy. Chemically, it is a derivative of carbamazepine, a carboxamide from the class of dibenzazepines. Eslicarbazepine was developed in the 1990s by the Portuguese pharmaceutical company Bial and is approved in Europe since 2009.

Pharmacokinetics

The prodrug of eslicarbazepine acetate is rapidly absorbed after oral administration and about 95 % by hepatic esterases hydrolytically cleaved ( first-pass metabolism ) to the active metabolite eslicarbazepine [( S)- Licarbazepin, 10,11- dihydro -10 - hydroxycarbamazepin ]. It only small amounts of the (less effective ) enantiomer R- Licarbazepin. This could be compared with the antiepileptic oxcarbazepine, after its metabolism, the ratio of S- to R- Licarbazepin Licarbazepin is 4:1, have a higher clinical efficacy of eslicarbazepine result. Approximately 30% of eslicarbazepine is bound to plasma proteins. The half-life is 8 to 17 hours after a single dose and 20 to 24 hours when taken regularly. Eslicarbazepine is almost completely excreted via the kidneys.

Operation

Eslicarbazepine has basically the same effect as the related carbamazepine. Inhibit voltage-gated sodium channels in the axons of the nerve cells and thus prevents the release of sodium channel -dependent neurotransmitter. Eslicarbazepine stabilizes the inactive form of the sodium channels and thus suppresses particular repititive excitations.

Range of applications

According to the spectrum of action of carbamazepine and oxcarbazepine eslicarbazepine is displayed in the combination therapy in epilepsy with partial and secondarily generalized seizures in adults.

Adverse effects

In placebo- controlled trials of patients treated with eslicarbazepine acetate subjects occurred in 45.3 % of unwanted effects (compared with 24.4% in placebo-treated subjects). Adverse effects were mild to moderate in intensity and occurred predominantly during the first weeks. Eslicarbazepine particular can lead to dizziness and drowsiness. It may come to the onset of headaches, coordination and attention disorders. Other adverse effects are skin rash (1.1%), tremor, nausea, vomiting, diarrhea. Hyponatremia ( reducing the content of sodium ions in the blood ) has been reported in less than 1 % of users ( compared to 23 % - 73 % for oxcarbazepine )

Eslicarbazepine may decrease the effectiveness of hormonal contraceptives. In the application of eslicarbazepine an additional non-hormonal method of contraception is recommended.