Peringatan Keamanan

In pre-marketing clinical trials, an accidental acute overdosage (48 mg/day) was reported in one patient who experienced orthostasis and sedation. The patient fully recovered the same day. As there are no specific antidotes for cariprazine, supportive care, including close medical supervision and monitoring, is advised to manage overdose. The possibility of multiple drug involvement should also be considered.L40198

Cariprazine

DB06016

small molecule approved investigational

Deskripsi

Cariprazine is an atypical antipsychotic agent and a piperazine derivative that was first developed in Hungary.A247100 It works as a partial agonist at central dopamine D2, dopamine D3, and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors.L40198 Cariprazine has been investigated in a variety of psychiatric disorders, including schizophrenia, bipolar disorders, and major depressive disorder. Cariprazine gained its first global approval in the US in September 2015 A3941 and was later approved by Health Canada in April 2022.L41670 It is currently used to treat schizophrenia, and manic or mixed episodes and depressive episodes associated with bipolar I disorder.L41655,L40198

Struktur Molekul 2D

Berat 427.41
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Cariprazine and its active metabolites have long half lives.[A247095] Terminal half-lives of cariprazine, DCAR, and DDCAR ranged from 31.6 to 68.4, 29.7 to 37.5, and 314 to 446 hours, respectively. The effective half-life, calculated from time to steady state, or the functional half-life of total active moieties was approximately one week.[A247060]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The most clinically relevant drug concentration equates to the combined systemic concentration of cariprazine plus desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR), the two main pharmacologically active metabolites of cariprazine.A3941 After single dose administration of cariprazine, the peak plasma cariprazine concentration occurred in approximately three to six hours.L40198 In healthy volunteers, the Tmax following oral administration was 3.6 hours for cariprazine, 6.5 hours for DCAR, and 18.1 hours for DDCAR. The steady-state was reached dose-proportionally within three weeks for cariprazine, DCAR, and DDCAR in patients with schizophrenia.A3941 Administration of a single dose of 1.5 mg cariprazine capsule with a high-fat meal did not significantly affect the Cmax and AUC of cariprazine or its metabolite, desmethyl cariprazine (DCAR).L40198

Metabolisme

Cariprazine is extensively metabolized by CYP3A4 and, to a lesser extent, by CYP2D6 to form two major metabolites, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR). DCAR and DDCAR are pharmacologically active metabolites with in vitro receptor binding profiles similar to the parent drug. DCAR is further metabolized into DDCAR by CYP3A4 and CYP2D6. DDCAR can be metabolized by CYP3A4 to form a hydroxylated metabolite.A3940,A3941,L40198

Rute Eliminasi

Following administration of 12.5 mg/day cariprazine to patients with schizophrenia for 27 days, about 21% of the daily dose was found in urine, with approximately 1.2% of the daily dose being excreted in urine as unchanged parent drug.L40198

Interaksi Makanan

4 Data
  • 1. Avoid excessive or chronic alcohol consumption. Given the primary central nervous system effects of cariprazine, cariprazine should be used with caution in combination with alcohol.
  • 2. Avoid grapefruit products. Grapefruit is a known CYP3A4 inhibitor. It may increase drug levels and elevate the risk of drug adverse effects.
  • 3. Avoid St. John's Wort. St John’s Wort is a known CYP3A4 inducer. It may significantly decrease drug exposure and alter drug efficacy.
  • 4. Take with or without food. A high-fat, high-calorie meal may delay Tmax, but food generally has no significant effect on drug exposure.

Interaksi Obat

1229 Data
Valsartan Cariprazine may decrease the antihypertensive activities of Valsartan.
Ramipril Cariprazine may decrease the antihypertensive activities of Ramipril.
Remikiren Cariprazine may decrease the antihypertensive activities of Remikiren.
Torasemide Cariprazine may decrease the antihypertensive activities of Torasemide.
Guanadrel Cariprazine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Cariprazine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Cariprazine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Cariprazine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Cariprazine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Cariprazine may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Cariprazine may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Cariprazine may decrease the antihypertensive activities of Prazosin.
Fosinopril Cariprazine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Cariprazine may decrease the antihypertensive activities of Trandolapril.
Metolazone Cariprazine may decrease the antihypertensive activities of Metolazone.
Benazepril Cariprazine may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Cariprazine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Cariprazine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Cariprazine may decrease the antihypertensive activities of Mecamylamine.
Moexipril Cariprazine may decrease the antihypertensive activities of Moexipril.
Lisinopril Cariprazine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Cariprazine may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Cariprazine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Cariprazine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Cariprazine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Cariprazine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Cariprazine may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Cariprazine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Cariprazine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Cariprazine may decrease the antihypertensive activities of Quinapril.
Telmisartan Cariprazine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Cariprazine may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Cariprazine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Cariprazine may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Cariprazine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Cariprazine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Cariprazine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Cariprazine may decrease the antihypertensive activities of Diazoxide.
Bretylium Cariprazine may decrease the antihypertensive activities of Bretylium.
Terazosin Cariprazine may decrease the antihypertensive activities of Terazosin.
Epoprostenol Cariprazine may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Cariprazine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Cariprazine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Cariprazine may decrease the antihypertensive activities of Saprisartan.
Spirapril Cariprazine may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Cariprazine may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Cariprazine may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Cariprazine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Cariprazine may decrease the antihypertensive activities of Temocapril.
Trimazosin Cariprazine may decrease the antihypertensive activities of Trimazosin.
Nicorandil Cariprazine may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Cariprazine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Cariprazine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Cariprazine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Cariprazine may decrease the antihypertensive activities of Imidapril.
BQ-123 Cariprazine may decrease the antihypertensive activities of BQ-123.
Cicletanine Cariprazine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Cariprazine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Cariprazine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Cariprazine may decrease the antihypertensive activities of Guanoxan.
Delapril Cariprazine may decrease the antihypertensive activities of Delapril.
Vincamine Cariprazine may decrease the antihypertensive activities of Vincamine.
Linsidomine Cariprazine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Cariprazine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Cariprazine may decrease the antihypertensive activities of Tolonidine.
Endralazine Cariprazine may decrease the antihypertensive activities of Endralazine.
Cadralazine Cariprazine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Cariprazine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Cariprazine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Cariprazine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Cariprazine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Cariprazine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Cariprazine may decrease the antihypertensive activities of Muzolimine.
Xipamide Cariprazine may decrease the antihypertensive activities of Xipamide.
Candesartan Cariprazine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Cariprazine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Cariprazine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Cariprazine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Cariprazine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Cariprazine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Cariprazine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Cariprazine may decrease the antihypertensive activities of Furosemide.
Enalapril Cariprazine may decrease the antihypertensive activities of Enalapril.
Captopril Cariprazine may decrease the antihypertensive activities of Captopril.
Amlodipine Cariprazine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Cariprazine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Cariprazine may decrease the antihypertensive activities of Nisoldipine.
Bosentan The metabolism of Cariprazine can be increased when combined with Bosentan.
Propranolol Cariprazine may decrease the antihypertensive activities of Propranolol.
Doxazosin Cariprazine may decrease the antihypertensive activities of Doxazosin.
Bisoprolol Cariprazine may decrease the antihypertensive activities of Bisoprolol.
Losartan Cariprazine may decrease the antihypertensive activities of Losartan.
Eplerenone Cariprazine may decrease the antihypertensive activities of Eplerenone.
Indapamide Cariprazine may decrease the antihypertensive activities of Indapamide.
Tadalafil Cariprazine may decrease the antihypertensive activities of Tadalafil.
Irbesartan Cariprazine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Cariprazine may decrease the antihypertensive activities of Nitrendipine.
Carvedilol Cariprazine may decrease the antihypertensive activities of Carvedilol.
Guanethidine Cariprazine may decrease the antihypertensive activities of Guanethidine.
Hydralazine Cariprazine may decrease the antihypertensive activities of Hydralazine.

Target Protein

D(3) dopamine receptor DRD3
D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 2A HTR2A
Histamine H1 receptor HRH1
5-hydroxytryptamine receptor 2C HTR2C
Alpha-1A adrenergic receptor ADRA1A

Referensi & Sumber

Synthesis reference: Agai-Csongor E, Domany G, Nogradi K, Galambos J, Vago I, Keseru GM, Greiner I, Laszlovszky I, Gere A, Schmidt E, Kiss B, Vastag M, Tihanyi K, Saghy K, Laszy J, Gyertyan I, Zajer-Balazs M, Gemesi L, Kapas M, Szombathelyi Z: Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104. Epub 2012 Apr 4. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/22537450)
Artikel (PubMed)
  • PMID: 23320989
    Citrome L: Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206. doi: 10.1517/17425255.2013.759211.
  • PMID: 26510944
    McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7.
  • PMID: 32303028
    Cooper H, Mishriky R, Reyad AA: Efficacy and Safety of Cariprazine in Acute Management of Psychiatric Disorders: a Meta-Analysis of Randomized Controlled Trials. Psychiatr Danub. 2020 Spring;32(1):36-45. doi: 10.24869/psyd.2020.36.
  • PMID: 26834462
    Nakamura T, Kubota T, Iwakaji A, Imada M, Kapas M, Morio Y: Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment). Drug Des Devel Ther. 2016 Jan 14;10:327-38. doi: 10.2147/DDDT.S95100. eCollection 2016.
  • PMID: 26956157
    Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9.
  • PMID: 27524901
    Roberts RJ, Findlay LJ, El-Mallakh PL, El-Mallakh RS: Update on schizophrenia and bipolar disorder: focus on cariprazine. Neuropsychiatr Dis Treat. 2016 Jul 25;12:1837-42. doi: 10.2147/NDT.S97616. eCollection 2016.
  • PMID: 24904434
    Brisch R, Saniotis A, Wolf R, Bielau H, Bernstein HG, Steiner J, Bogerts B, Braun K, Jankowski Z, Kumaratilake J, Henneberg M, Gos T: The role of dopamine in schizophrenia from a neurobiological and evolutionary perspective: old fashioned, but still in vogue. Front Psychiatry. 2014 May 19;5:47. doi: 10.3389/fpsyt.2014.00047. eCollection 2014.
  • PMID: 28289283
    Ashok AH, Marques TR, Jauhar S, Nour MM, Goodwin GM, Young AH, Howes OD: The dopamine hypothesis of bipolar affective disorder: the state of the art and implications for treatment. Mol Psychiatry. 2017 May;22(5):666-679. doi: 10.1038/mp.2017.16. Epub 2017 Mar 14.

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