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357336-20-0 Usage

Definition

ChEBI: A non-proteinogenic amino acid derivative that is butanamide in which the pro-S hydrogen at position 2 is replaced by a (4R)-2-oxo-4-propylpyrrolidin-1-yl. Used for treatment of partial onset seizures related to epilepsy.

Precaution

You should not use brivaracetam if you are allergic to it[4, 11, 12].
Brivaracetam may become habit-forming for people administrate. Therefore, it is of risk to share brivaracetam with another person, especially avoid sharing with someone with a history of drug abuse or addiction. You should keep the medication in a place where others cannot get to it. Selling or giving away this medicine is against the law.
Before administrate the brivaracetam, tell your doctor if you have ever had one or several of the following symptom for your own safety: Depression or a mood disorder; Suicidal thoughts or actions; liver disease; or alcoholism or drug addiction.
Follow your doctor's instructions about taking seizure medication if you are pregnant. Seizure control is very important during pregnancy, and having a seizure could harm both mother and baby. Do not start or stop taking this medicine without your doctor's advice, and tell your doctor right away if you become pregnant. If you are pregnant, your name may be listed on a pregnancy registry. This is to track the outcome of the pregnancy and to evaluate any effects of brivaracetam on the baby.
It is not known whether brivaracetam passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.
Brivaracetam is not approved for use by anyone younger than 16 years old[4].
Patients of hepatic impairment should subject to dose adjustment[4].

References

  1. https://www.ncbi.nlm.nih.gov/pubmed/21575627
  2. https://www.ucb.com/stories-media/press-releases/article/U-S-FDA-approves-UCB-s-new-epilepsy-treatment-BRIVIACT-for-patients-with-partial-onset-seizures
  3. https://www.drugbank.ca/drugs/DB05541
  4. https://www.briviact.com/briviact-PI.pdf
  5. https://www.ucb.com/stories-media/Press-Releases/article/New-indication-for-BRIVIACT-brivaracetam-UCB-s-newest-antiepileptic-drug-approved-by-FDA-as-monotherapy-treatment-of-partial-onset-seizures-in-adults
  6. Gillard, Michel, et al. "Binding characteristics of brivaracetam, a selective, high affinity SV2A ligand in rat, mouse and human brain: Relationship to anti-convulsant properties." European Journal of Pharmacology664.1(2011]:36-44.
  7. Yang, X., et al. "Brivaracetam augments short-term depression and slows vesicle recycling. " Epilepsia 56.12(2016]:1899-1909.
  8. Nicolas, J. M., et al. "Brivaracetam, a selective high-affinity synaptic vesicle protein 2A[SV2A] ligand with preclinical evidence of high brain permeability and fast onset of action. " Epilepsia 57.2(2016]:201-209.
  9. Vogl, Christian, et al. "The SV2A Ligand Levetiracetam Inhibits Presynaptic Ca2+ Channels Via an Intracellular Pathway."[2012].
  10. Briviact® US Prescribing Information. Brussels, Belgium: UCB, 2016.
  11. https://www.rxlist.com/briviact-side-effects-drug-center.htm
  12. https://www.everydayhealth.com/drugs/brivaracetam

Uses

Treatment ofTreatment of epilepsy, neuropathic pain and essential tremor.

Description

Brivaracetam, a chemical analog of Levetiracetam, is a racetam derivative with anticonvulsant effect. It is used for the treatment of partial-onset seizures with or without secondary generalisation, in combination with other antiepileptic drugs. The exact mechanism of brivaracetam's anti-epileptogenic activity is unknown. What is known is thatbrivaracetam 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 can also inhibit Na+ channels which may also contribute to its anti-epileptogenic action.

Application

Brivaracetam is indicated for the treatment of partial-onset seizures in patients 4 years of age and older[4,5]. It provides a new monotherapy treatment option for epilepsy patients 16 years of age and older who suffering partial-onset[focal] seizures, which can be initiated at a therapeutic dose at day one[5].

Mode of action

The accurate mode of action of brivaracetam remains unclear. It is known that Brivaracetam can strongly bind to SV2A[6-8], which 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[6-8]. It may access the luminal side of recycling synaptic vesicles during vesicular endocytosis, which may reduce excitatory neurotransmitter release and enhance synaptic depression during trains of high-frequency activity, such as is believed to occur during epileptic activity. Brivaracetam is also known to inhibit Na+ channels which may also contribute to its anti-epileptogenic action[9].

Warning

It is possible that BRIVIACT can cause the following severe adverse effects, special attention should pay immediately once those following cases occur[4, 10, 11].
Suicidal Behavior and Ideation: Antiepileptic drugs can increase the risk of suicidal behavior and ideation. Monitor patients taking BRIVIACT for the emergence or worsening of depression; unusual changes in mood or behavior; or suicidal thoughts, behavior, or self-harm. Advise patients, their caregivers, and/or families to be alert for these behavioral changes and report them immediately to a healthcare provider[4].
Psychiatric Adverse Reactions: BRIVIACT can also cause psychiatric adverse reactions, including non-psychotic and psychotic symptoms. These events were reported in approximately 13% of patients taking at least 50 mg per day of BRIVIACT compared to 8% of patients taking placebo. A total of 1.7% of adult patients taking BRIVIACT discontinued treatment due to psychiatric reactions compared to 1.3% of patients taking placebo. Advise patients to report these symptoms immediately to a healthcare provider[10].
Hypersensitivity: BRIVIACT can cause hypersensitivity reactions such as bronchospasm and angioedema. The patients should discontinue BRIVIACT if a he/she develops a hypersensitivity reaction after treatment. BRIVIACT should not be applied in patients with a prior hypersensitivity reaction to brivaracetam or any of the inactive ingredients[10].
Neurological Adverse Reactions: BRIVIACT causes somnolence, fatigue, dizziness, and disturbance in coordination. Somnolence and fatigue-related adverse reactions were reported in 25% of patients taking at least 50 mg per day of BRIVIACT compared to 14% of patients taking placebo. Dizziness and disturbance in gait and coordination were reported in 16% of patients taking at least 50 mg per day of BRIVIACT compared to 10% of patients taking placebo. The risk is greatest early in treatment but can occur at any time. Monitor patients for these signs and symptoms and advise them not to drive or operate machinery until they have gained sufficient experience on BRIVIACT[4].
Withdrawal of Antiepileptic Drugs: BRIVIACT should generally be withdrawn gradually because of the risk of increased seizure frequency and status epilepticus[4].

Adverse reactions

The most common adverse reactions[at least 5% for BRIVIACT and at least 2% more frequently than placebo] are somnolence and sedation, dizziness, fatigue, and nausea and vomiting symptoms, drowsiness, and loss of balance of coordination, irritability and constipation[4, 10,11].

Overview and History

Brivaracetam is an orally bioavailable levetiracetam derivative, with anticonvulsant activity. It can be used in the treatment of partial-onset seizures[1-3]. Brivaracetam binds SV2A with 20 times higher affinity than levetiracetam. It is available under the brand name Briviact made by UCB. It was approved by the federal drug administration of USA[FDA] on Feb 19th 2016[1-3].

357336-20-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name Brivaracetam

1.2 Other means of identification

Product number -
Other names (2S)-2-[(4R)-2-oxo-4-propylpyrrolidin-1-yl]butanamide

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:357336-20-0 SDS

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