Product Information
Registration Status: ActiveREXULTI FILM-COATED TABLETS 4MG is approved to be sold in Singapore with effective from 2019-08-05. It is marketed by LUNDBECK SINGAPORE PTE LTD, with the registration number of SIN15763P.
This product contains Brexpiprazole 4mg in the form of TABLET, FILM COATED. It is approved for ORAL use.
This product is manufactured by OTSUKA PHARMACEUTICAL CO. in FRANCE, and LTD. (TOKUSHIMA FACTORY) in JAPAN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for major depressive disorder (MDD). Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).
Indication
As an adjunctive treatment of major depressive disorder (MDD) and for treatment of schizophrenia.
Mechanism of Action
Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.
Pharmacokinetics
- Absorption
- Brexpiprazole reaches peak plasma concentration within 4 hours of administration, and steady state occurs within 10-12 days of dosing. Oral bioavailability is 95%, and can be administered with or without food.
- Distribution
- Intravenous volume of distribution is 1.56L/kg.
- Metabolism
- Metabolized mainly by CYP3A4 and CYP2D6 enzymes into its major metabolite, DM-3411. DM-3411 is not considered to contribute any therapeutic effect.
- Elimination
Clearance
19.8mL/h/kg
Toxicity
The most commonly observed adverse effects include: weight increase, akathisia, somnolence, tremor and nasopharyngitis. Neonates are at risk for extrapyramidal and/or withdrawal symptoms if exposed to an antipsychotic drug during the third trimester of development.
Active Ingredient/Synonyms
Brexpiprazole | Brexpiprazole |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.