Cariprazinum

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Cariprazinum
Cognitores
ChemSpider 25999972
PubChem 11154555
DrugBank DB06016
Natura chemica
Cariprazinum
Cariprazinum
Formula chemica C
21
H
32
Cl
2
N
4
O
Massa molaris 427.411 g/mol
Natura pharmacologica
Codex ATC N05AX15 (WHO)
Tempus semivitae biologicum 2-5 d
desmethyl~: 2-3 hebd.
Metabolismus iecore (hepaticus): CYP3A4
Metaboliti Desmethylo-Cariprazinum
(DCAR)
Didesmethylo-Cariprazinum
(DDCAR)
Excretio renibus (21%), faecibus
Ad usum therapeuticum
Applicatio per os

Cariprazinum est substantia antipsychotica, agonista dopamini partialis (D3 > D2), ad schizophreniam tractandam[1]. In senectute periculum apoplexiae cerebri auctum est. Neque valor prolactini auctus neque intervallum QT prolongatum observantur.

Historia[recensere | fontem recensere]

Ante annum 2008 grex Hungaricus societatis Richter Gedeon Nyrt. varias substantias receptoria dopamini D3 et minus D2 inhibentes investigavit[2]. Paulo post sub nomen Cariprazini pristinum RGH-188 inventum erat[3] et anno 2012 Cariprazinum praesentatum est[4].

Natura Cariprazini[recensere | fontem recensere]

Natura chemica[recensere | fontem recensere]

Cariprazinum est piperazinum. Nomen chemicum (IUPAC) est 3-[4-[2-[4-(2,3-dichloro-phenyl)-piperazino-1-yl]-aethyl]-cyclohexyl]-1,1-dimethyl-urea. Massa molaris est 427.411 g/mol.

Natura pharmacologica[recensere | fontem recensere]

Cariprazinum est medicamentum cum virtutibus antipsychoticis et antidepressivis. Codex ATC est N05AX15 (WHO).

Pharmacodynamica[recensere | fontem recensere]

Cariprazinum potissime receptoria dopamini D3, paulo minus receptoria D2 obsidet[5].

Receptorium Cariprazini
affinitas ligandi,
Ki (nM)[6]
Actio
dopamini D2L 0.49 agonista partialis
dopamini D2S 0.69 agonista partialis
dopamini D3 0.085 agonista partialis
serotonini 5-HT1A 2.6 agonista partialis
serotonini 5-HT2A 18.8 antagonista
serotonini 5-HT2B 0.58 antagonista
serotonini 5-HT2C 134 agonista inversa
serotonini 5-HT7 111 antagonista
adrenergicum α1A 155 antagonista
histamini H1 23.2 antagonista
muscarinicum acetylcholini > 1,000 antagonista

Pharmacocinetica[recensere | fontem recensere]

Tempus semivitae biologicum Cariprazini est duo dies usque ad quinque dies. Cariprazinum substratum Cytochromatis P450 CYP3A4 (minus CYP2D6) est.
Metaboliti sunt Desmethylo-Cariprazinum (DCAR) et Di-Desmethylo-Cariprazinum (DDCAR)[7]. Tempora semivitae biologica metabolitorum Cariprazino magis longiora sunt, ita Desmethylo-Cariprazino 2-3 hebdomades est.

Metaboliti[recensere | fontem recensere]

Cytochromatis CYP3A4 ope in duo gradus primo DCAR deinde DDCAR oriuntur.

Notae[recensere | fontem recensere]

  1. Ceskova E., Silhan P. (2018). "Novel treatment options in depression and psychosis". Neuropsychiatr Dis Treat 14: 741-7 
  2. Kiss B., Laszlovszky I., Horváth A., Némethy Z., Schmidt E., Bugovics G., Fazekas K., Gyertyán I., Agai-Csongor E., Domány G., Szombathelyi Z. (2008). "Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: I. neurochemical characterisation of RG-15". Naunyn Schmiedebergs Arch Pharmacol 378 (5): 515-28 
  3. Mészáros G. P., Agai-Csongor E., Kapás M. (2008). "Sensitive LC-MS/MS methods for the quantification of RGH-188 and its active metabolites, desmethyl- and didesmethyl-RGH-188 in human plasma and urine". J Pharm Biomed Anal 48 (2): 388-97 
  4. Agai-Csongor E., Domány G., Nógrádi K., Galambos J., Vágó I., Keserű G. M., Greiner I., Laszlovszky I., Gere A., Schmidt E., Kiss B., Vastag M., Tihanyi K., Sághy K., Laszy J., Gyertyán I., Zájer-Balázs M., Gémesi L., Kapás M., Szombathelyi Z. (2012). "Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors". Bioorg Med Chem Lett 22 (10): 3437-40 
  5. Kiss B., Horváth A., Némethy Z., Schmidt E., Laszlovszky I., Bugovics G., Fazekas K., Hornok K., Orosz S., Gyertyán I., Agai-Csongor E., Domány G., Tihanyi K., Adham N., Szombathelyi Z. (2010). "Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile". J Pharmacol Exp Ther 333 (1): 328-40 
  6. http://pdsp.med.unc.edu/pdsp.php
  7. Nakamura T., Kubota ., Iwakaji A., Imada M., Kapás M., Morio Y. (2016). "Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week Treatment)". Drug design, development and treatment 10: 327-38 

Nexus interni

Nexus externi[recensere | fontem recensere]

  • Situs interretialis fabricatoris Cariprazini (divulgationibus) (Anglice)