BIA 2-093 Struktur

BIA 2-093

Bezeichnung:BIA 2-093

CAS-Nr236395-14-5

Englisch Name:BIA 2-093

CBNumberCB5503197

SummenformelC17H16N2O3

Molgewicht296.32

MOL-Datei236395-14-5.mol

BIA 2-093 physikalisch-chemischer Eigenschaften

Schmelzpunkt	183-185°C
Siedepunkt	427.4±55.0 °C(Predicted)
Dichte	1.32
storage temp.	Sealed in dry,2-8°C
Löslichkeit	H₂O: insoluble
Aggregatzustand	solid
pka	13.97±0.40(Predicted)
Farbe	white
InChIKey	QIALRBLEEWJACW-INIZCTEOSA-N

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36
WGK Germany	3
HS Code	2934.99.3000

Gefahreninformationscode (GHS)

BIA 2-093 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Although epilepsy is a neurological disorder with varying etiology and severity, the common feature is unprovoked, recurring seizures. Even when traditional AEDs, such as phenobarbital, phenytoin, carbamazepine, and valproate, control seizure activity, their effectiveness is hampered by considerable side effects and the tendency for drug-drug interactions. Designed for improved efficacy and safety, eslicarbazepine acetate is a third-generation AED that has been approved as adjunctive therapy for partial-onset seizures with or without secondary generalization. As a member of the carbamazepine family (first generation), it is the prodrug of eslicarbazepine and the active metabolite of oxcarbazepine (second generation). .
Beschreibung
Eslicarbazepine acetate is a sodium channel blocker (IC₅₀ = 138 nM in a radioligand binding assay). It inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes at concentrations ranging from 30-300 μM. In vivo, oral and i.p. administration of eslicarbazepine acetate is protective against seizures induced by maximal electroshock (MES) in mice with ED₅₀ values of 4.7 and 6.3 mg/kg, respectively, which are well below the median toxic dose (TD₅₀) values of 358.7 and 78.6 mg/kg for oral and i.p. administration respectively. High-dose administration (30 mg/kg) of eslicarbazepine acetate prevents picrotoxin-induced seizures in rats. Low-dose administration (10 mg/kg) does not suppress picrotoxin-induced seizures, however, it reduces seizure number and duration. Formulations containing eslicarbazepine acetate have been used for the treatment of partial-onset seizures.
Chemische Eigenschaften
White to Off-White Solid
Originator
BIAL Group (Spain)
Verwenden
Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine. Neuroprotective & Neuroresearch product.
Definition
ChEBI: The acetate ester, with S configuration, of licarbazepine. An anticonvulsant, it is approved for use in Europe and the United States as an adjunctive therapy for epilepsy.
Trademarks
Zebinix; Exalief, Stedesa
Nebenwirkungen
The most common adverse events occurring with an incidence of >2% were dizziness, somnolence, nausea, diplopia, headache, vomiting, abnormal coordination, blurred vision, vertigo, and fatigue. While most of these side effects appeared to be mild to moderate, they did display a dose dependency. Although eslicarbazepine acetate is only contraindicated in patients with a known hypersensitivity to the carbamazepine family of AEDs, caution should be exercised in patients with cardiac conduction abnormalities (potential for prolongations in PR intervals), renal impairment, and in patients of Han Chinese and Thai origin since the presence of HLA-B*1502 allele in these individuals has been shown to be strongly associated with the risk of developing Stevens-Johnson syndrome. Regarding drug interactions, eslicarbazepine acetate may decrease the effectiveness of hormonal contraceptives, so alternative or additional methods of contraception should be considered.

BIA 2-093 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

236395-14-5, BIA 2-093 Verwandte Suche:

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