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RX BIN: 015558
RX PCN: HT
Group ID: DDN6600
Card Holder ID: DDN6600

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2018 Price of Ezogabine

$

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Ezogabine volume of distribution

8.7 L/kg

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What is Ezogabine

Ezogabine (D23129) is a close structural analog of the centrally acting analgesic flupitrine. It is a neuronal potassium channel opener being developed as a first-in-class antiepileptic drug (AED) and is currently being studied in Phase 3 trials as an adjunctive treatment for partial-onset seizures in adult patients with refractory epilepsy. FDA approved in June 10, 2011 under the name of ezogabine.

Ezogabine mechanism of action

Ezogabine has a novel mechanism of action that involves opening of neuronal Kv7.2-7.5 (formerly KCNQ2-5) voltage activated potassium channels. These channels (primarily Kv7.2/7.3) enable generation of the M-current, a sub-threshold potassium current that serves to stabilize the membrane potential and control neuronal excitability. In addition to acting on potassium ion channels, retigabine also affects GABA neurotransmission in the GABA-A receptor, which is a key inhibitory receptor in the central nervous system and is implicated in epilepsy. Malfunctioning of the GABA-A receptor leads to hyperexcitability in the brain, which causes seizures, making this receptor an important target for antiepileptic therapeutics. Apart from increasing the concentration of GABA in the brain (by either enhancing GABA synthesis or blocking GABA metabolism), retigabine allosterically potentiates GABA-induced current in rat cortical neurons in a concentration-dependent manner. Numerous studies have demonstrated that retigabine is effective in a broad spectrum of in vivo epilepsy and seizure models.

Dosage forms of Ezogabine

FormRouteStrength
Tablet, film coatedoral200 mg/1
Tablet, film coatedoral300 mg/1
Tablet, film coatedoral400 mg/1
Prescription Generics

false

International Brands

Potiga

Synonyms

D-23129 Ethyl {2-amino-4-[(4-fluorobenzyl)amino]phenyl}carbamate

Manufacturers

Glaxo Smith Kline Llc

CAS number

150812-12-7

UNII

12G01I6BBU

State

solid

Affected organisms

Humans and other mammals

Indication of Ezogabine

Adjuvant treatment of partial-onset seizures.

Toxicity of Ezogabine

Lethal Dose, acute, oral, rat = 100 mg/kg; Lethal Dose, chronic, oral, rat = 5.1 mg/kg/day, 90-day; Most common adverse effects that lead to discontinuation of therapy include dizziness and somnolence.

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