Peringatan Keamanan

There is limited information regarding acute toxicity and human overdosage with brexpiprazole. Management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers. Oral activated charcoal and sorbitol (50 g/240 mL), administered one hour after ingesting oral brexpiprazole, decreased brexpiprazole Cmax and area under the curve (AUC) by approximately 5% to 23% and 31% to 39% respectively; however, there is insufficient information available on the therapeutic potential of activated charcoal in treating an overdose with brexpiprazole. There is no information on the effect of hemodialysis in treating an overdose with brexpiprazole; hemodialysis is unlikely to be useful because brexpiprazole is highly bound to plasma proteins.L46417

Brexpiprazole

DB09128

small molecule approved investigational

Deskripsi

Brexpiprazole is an atypical antipsychotic and a novel D2 dopamine and serotonin 1A partial agonist called serotonin-dopamine activity modulator (SDAM). It has a high affinity for serotonin, dopamine and alpha (?)-adrenergic receptors.L46417 Although it is structurally similar to aripiprazole, brexpiprazole has different binding affinities for dopamine and serotonin receptors. Compared to aripiprazole, brexpiprazole has less potential for partial agonist-mediated adverse effects such as extrapyramidal symptoms, which is attributed to lower intrinsic activity at the D2 receptor. It also displays stronger antagonism at the 5-HT1A and 5-HT2A receptors.A182186, A38385, A259661

Brexpiprazole was first approved by the FDA on July 10, 2015.A182186 Currently approved for the treatment of depression, schizophrenia, and agitation associated with dementia due to Alzheimer’s disease, brexpiprazole has also been investigated in other psychiatric disorders, such as post-traumatic stress disorder.A7782

Struktur Molekul 2D

Berat 433.57
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) After multiple once-daily administrations, the terminal elimination half-lives of brexpiprazole and its major metabolite, DM-3411, were 91 hours and 86 hours, respectively.[L46417]
Volume Distribusi The volume of distribution of brexpiprazole following intravenous administration is 1.56 ± 0.42 L/kg, indicating extravascular distribution.[L46417]
Klirens (Clearance) Apparent oral clearance of brexpiprazole after once-daily administration is 19.8 (±11.4) mL/h/kg.[L46417]

Absorpsi

After a single-dose administration, the Tmax was four hours and the absolute oral bioavailability was 95%. Brexpiprazole steady-state concentrations were attained within 10 to 12 days of dosing. After single and multiple once-daily dose administration, the Cmax and AUC increased dose-proportionally.L46417 A high-fat meal did not significantly affect the Cmax or AUC of brexpiprazole.L46417

Metabolisme

According to in vitro studies, brexpiprazole is mainly metabolized by CYP3A4 and CYP2D6. Brexpiprazole and its major metabolite, DM-3411, were the predominant drug moieties in the systemic circulation following single and multiple dose administration. At steady-state, DM-3411 represented 23% to 48% of brexpiprazole exposure (AUC) in plasma. DM-3411 is considered not to be pharmacologically active.L46417

Rute Eliminasi

Following a single oral dose of radiolabeled brexpiprazole, approximately 25% and 46% of radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged brexpiprazole was excreted in the urine, and approximately 14% of the oral dose was recovered unchanged in the feces.L46417

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces the CYP3A metabolism of brexpiprazole and may reduce its serum concentration. The dose of Brexpiprazole should be doubled if administered with St. John's wort.
  • 2. Drink plenty of fluids.
  • 3. Take with or without food. Food does not significantly affect brexpiprazole exposure.

Interaksi Obat

1488 Data
Valsartan Brexpiprazole may decrease the antihypertensive activities of Valsartan.
Ramipril Brexpiprazole may decrease the antihypertensive activities of Ramipril.
Remikiren Brexpiprazole may decrease the antihypertensive activities of Remikiren.
Torasemide Brexpiprazole may decrease the antihypertensive activities of Torasemide.
Guanadrel Brexpiprazole may decrease the antihypertensive activities of Guanadrel.
Olmesartan Brexpiprazole may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Brexpiprazole may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Brexpiprazole may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Brexpiprazole may decrease the antihypertensive activities of Minoxidil.
Treprostinil Brexpiprazole may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Brexpiprazole may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Brexpiprazole may decrease the antihypertensive activities of Fosinopril.
Trandolapril Brexpiprazole may decrease the antihypertensive activities of Trandolapril.
Metolazone Brexpiprazole may decrease the antihypertensive activities of Metolazone.
Benazepril Brexpiprazole may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Brexpiprazole may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Brexpiprazole may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Brexpiprazole may decrease the antihypertensive activities of Mecamylamine.
Moexipril Brexpiprazole may decrease the antihypertensive activities of Moexipril.
Lisinopril Brexpiprazole may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Brexpiprazole may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Brexpiprazole may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Brexpiprazole may decrease the antihypertensive activities of Cryptenamine.
Perindopril Brexpiprazole may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Brexpiprazole may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Brexpiprazole may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Brexpiprazole may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Brexpiprazole may decrease the antihypertensive activities of Quinapril.
Telmisartan Brexpiprazole may decrease the antihypertensive activities of Telmisartan.
Hydrochlorothiazide Brexpiprazole may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Brexpiprazole may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Brexpiprazole may decrease the antihypertensive activities of Deserpidine.
Pentolinium Brexpiprazole may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Brexpiprazole may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Brexpiprazole may decrease the antihypertensive activities of Diazoxide.
Bretylium Brexpiprazole may decrease the antihypertensive activities of Bretylium.
Epoprostenol Brexpiprazole may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Brexpiprazole may decrease the antihypertensive activities of Polythiazide.
Cilazapril Brexpiprazole may decrease the antihypertensive activities of Cilazapril.
Saprisartan Brexpiprazole may decrease the antihypertensive activities of Saprisartan.
Spirapril Brexpiprazole may decrease the antihypertensive activities of Spirapril.
Tienilic acid Brexpiprazole may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Brexpiprazole may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Brexpiprazole may decrease the antihypertensive activities of Temocapril.
Nicorandil Brexpiprazole may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Brexpiprazole may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Brexpiprazole may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Brexpiprazole may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Brexpiprazole may decrease the antihypertensive activities of Imidapril.
BQ-123 Brexpiprazole may decrease the antihypertensive activities of BQ-123.
Cicletanine Brexpiprazole may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Brexpiprazole may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Brexpiprazole may decrease the antihypertensive activities of Zofenopril.
Guanoxan Brexpiprazole may decrease the antihypertensive activities of Guanoxan.
Delapril Brexpiprazole may decrease the antihypertensive activities of Delapril.
Vincamine Brexpiprazole may decrease the antihypertensive activities of Vincamine.
Linsidomine Brexpiprazole may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Brexpiprazole may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Brexpiprazole may decrease the antihypertensive activities of Tolonidine.
Endralazine Brexpiprazole may decrease the antihypertensive activities of Endralazine.
Cadralazine Brexpiprazole may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Brexpiprazole may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Brexpiprazole may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Brexpiprazole may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Brexpiprazole may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Brexpiprazole may decrease the antihypertensive activities of Guanoclor.
Muzolimine Brexpiprazole may decrease the antihypertensive activities of Muzolimine.
Xipamide Brexpiprazole may decrease the antihypertensive activities of Xipamide.
Candesartan Brexpiprazole may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Brexpiprazole may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Brexpiprazole may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Brexpiprazole may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Brexpiprazole may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Brexpiprazole may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Brexpiprazole may decrease the antihypertensive activities of Quinaprilat.
Furosemide Brexpiprazole may decrease the antihypertensive activities of Furosemide.
Enalapril Brexpiprazole may decrease the antihypertensive activities of Enalapril.
Captopril Brexpiprazole may decrease the antihypertensive activities of Captopril.
Bosentan Brexpiprazole may decrease the antihypertensive activities of Bosentan.
Losartan Brexpiprazole may decrease the antihypertensive activities of Losartan.
Eplerenone Brexpiprazole may decrease the antihypertensive activities of Eplerenone.
Indapamide Brexpiprazole may decrease the antihypertensive activities of Indapamide.
Irbesartan Brexpiprazole may decrease the antihypertensive activities of Irbesartan.
Guanethidine Brexpiprazole may decrease the antihypertensive activities of Guanethidine.
Hydralazine Brexpiprazole may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Brexpiprazole may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Brexpiprazole may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Brexpiprazole may decrease the antihypertensive activities of Pinacidil.
Riociguat Brexpiprazole may decrease the antihypertensive activities of Riociguat.
Macitentan Brexpiprazole may decrease the antihypertensive activities of Macitentan.
Aliskiren Brexpiprazole may decrease the antihypertensive activities of Aliskiren.
Selexipag Brexpiprazole may decrease the antihypertensive activities of Selexipag.
Levamlodipine Brexpiprazole may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Brexpiprazole may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Brexpiprazole may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Brexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.
Hydrocodone Brexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.

Target Protein

5-hydroxytryptamine receptor 1A HTR1A
D(2) dopamine receptor DRD2
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 7 HTR7
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
Alpha-2C adrenergic receptor ADRA2C
Histamine H1 receptor HRH1
Muscarinic acetylcholine receptor M1 CHRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26310190
    Greig SL: Brexpiprazole: First Global Approval. Drugs. 2015 Sep;75(14):1687-97. doi: 10.1007/s40265-015-0462-2.
  • PMID: 26913177
    Das S, Barnwal P, Winston A B, Mondal S, Saha I: Brexpiprazole: so far so good. Ther Adv Psychopharmacol. 2016 Feb;6(1):39-54. doi: 10.1177/2045125315614739.
  • PMID: 29955525
    Diefenderfer LA, Iuppa C: Brexpiprazole: A review of a new treatment option for schizophrenia and major depressive disorder. Ment Health Clin. 2018 Mar 23;7(5):207-212. doi: 10.9740/mhc.2017.09.207. eCollection 2017 Sep.
  • PMID: 36979900
    Brasso C, Colli G, Sgro R, Bellino S, Bozzatello P, Montemagni C, Villari V, Rocca P: Efficacy of Serotonin and Dopamine Activity Modulators in the Treatment of Negative Symptoms in Schizophrenia: A Rapid Review. Biomedicines. 2023 Mar 16;11(3):921. doi: 10.3390/biomedicines11030921.
  • PMID: 27408517
    Eaves S, Rey JA: Brexpiprazole (Rexulti): A New Monotherapy for Schizophrenia and Adjunctive Therapy for Major Depressive Disorder. P T. 2016 Jul;41(7):418-22.
  • PMID: 26899451
    Stahl SM: Mechanism of action of brexpiprazole: comparison with aripiprazole. CNS Spectr. 2016 Feb;21(1):1-6. doi: 10.1017/S1092852915000954.

Contoh Produk & Brand

Produk: 51 • International brands: 0
Produk
  • Brexpiprazole
    Tablet, film coated • 0.25 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet, film coated • 0.5 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet, film coated • 1 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet, film coated • 2 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet, film coated • 3 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet, film coated • 4 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet • 0.25 mg/1 • Oral • US • Generic • Approved
  • Brexpiprazole
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 51 produk.

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