Brivaracetam

703.83

212.29

1592732-453-0

U863JGG2IA

2710

C65270

N03AX23|N - Nervous system

2933990090

63.4

0.88

1.062

76.38°

409.3±28.0 °C at 760 mmHg

201.3±24.0 °C

1.494

D25 -60.57° (c = 1 in methanol)

P264, P270, P301+P312, P330, P501

H302

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 2 companies from 1 notifications to the ECHA C&L Inventory.

No carcinogenesis or fertility impairment found. Overdose is associated with somnolence and dizziness.

Prospective studies reported that chronic brivaracetam therapy was not accompanied by significant elevations in serum aminotransferase levels and clinically apparent liver injury was not observed. Brivaracetam has had limited general use, but has not been linked to instances of clinically apparent liver injury. Levetiracetam, an anticonvulsant with similar structure and mechanism of action, has been linked to rare instances of acute liver injury, generally arising within 1 to 20 weeks and presenting with a hepatocellular pattern of injury without immunoallergic or autoimmune features. Whether similar cases will be linked to brivaracetam is not known.

<20% bound to plasma proteins.

Used as adjunctive therapy for partial-onset seizures in patients 16 years of age or older.|FDA Label|Briviact is indicated as adjunctive therapy in the treatment of partial-onset seizures with or without secondary generalisation in adult and adolescent patients from 16 years of age with epilepsy.|Treatment of epilepsy with partial-onset seizures, Treatment of neonatal seizures|Treatment of paediatric epilepsy syndromes

Brivaracetam is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Brivaracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and is suspected of causing rare cases of clinically apparent drug induced liver disease.

Anticonvulsants

Brivaracetam binds SV2A with high affinity. SV2A is known to play a role in epileptogenesis through modulation of synaptic GABA release. It is thought that brivaracetam exerts its anti-epileptogenic effects through its binding to SV2A. Brivaracetam is also known to inhibit Na+ channels which may also contribute to its anti-epileptogenic action.

Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)

Nearly 100% oral bioavailability.|\>95% excreted in urine with <10% of the parent compound unchanged. <1% excreted in feces.|0.5L/kg.|CL/F of 0.7-1.07 mL/min kg. Clearance is primarily metabolic with less than 10% of the parent drug excreted unchanged.

Primarily metabolized by hydrolysis of the acetamide moeity to form a carboxylic acid metabolite. Another metabolite is created via oxidation of the propyl side chain by CYP2C8 as well as CYP3A4, CYP2C19, and CYP2B6. Some conjugation with glucuronic acid and taurine account for a small amount of metabolism.

7-8h.

The precise mechanism of brivaracetam's anti-epileptogenic activity is unknown.

(2S)-2-((4R)-2-oxo-4-propylpyrrolidin-1-yl)butanamide

Brivaracetam|BRV, UCB-34714, Briviact, ((2S)-2-[(4R)-2-oxo-4-propylpyrrolidin-1-yl] butanamide)|2710|Schedule V - Substances in the DEA Schedule V have a low potential for abuse relative to substances listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotics.|No

Human drugs -> Briviact (in Italy: Nubriveo) -> EMA Drug Category|Antiepileptics -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients