Perospiron is an atypical antipsychotic of the azapiron family [1] . It was first introduced in 2001 by the Japanese pharmaceutical company Dainippon Sumitomo Pharma as a cure for schizophrenia and acute manic psychosis [3] [4] .
| Perospiron | |
|---|---|
| Perospironum | |
 | |
 | |
| Chemical compound | |
| IUPAC | (3a S , 7a R ) -2- [4- [4- (1,2-benzothiazol-3-yl) piperazin-1-yl] butyl] -3a, 4,5,6,7,7a-hexahydroisoindole- 1,3-dion |
| Gross formula | C 23 H 30 N 4 O 2 S |
| Molar mass | 426.57 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| Farmakol. Group | Antipsychotics |
| ICD-10 | |
| Pharmacokinetics | |
| Metabolism | hepatic |
| The half-life. | 1.9-2.5 hours [1] [2] |
| Excretion | renal (0.4% of the starting material) [1] |
| Dosage Forms | |
| pills | |
| Route of administration | |
| orally | |
| Other names | |
| Lullan | |
Pharmacology
Perospiron is associated with high affinity with receptors (as an antagonist , unless otherwise indicated) [5] [6] [7] [5] [8] [9] [10] :
- 5-HT 1A (partial agonist; K i = 2.9 nM)
- 5-HT 2A (inverse agonist; K i = 1.3 nM)
- D 2 (K i = 0.6 nM)
with high receptor affinity : [6]
- H 1 (inverse agonist)
with moderate receptor affinity: [6]
- D 4
- α 1 adrenergic receptor
and with low affinity for the receptor: [6]
- D 1
Side Effects
It can cause more severe extrapyramidal disorders than other atypical antipsychotics, but easier than typical (classical) ones [1] [11] .
Notes
- ↑ 1 2 3 4 Onrust, SV; McClellan, K. Perospirone (Eng.) // Drugs : journal. - Adis International , 2001. - Vol. 15 , no. 4 . - P. 329—337 . - DOI : 10.2165 / 00023210-200115040-00006 . - PMID 11463136 .
- ↑ Yasui-Furukori, N; Furukori, H; Nakagami, T; Saito, M; Inoue, Y; Kaneko, S; Tateishi, T. Steady-State Pharmacokinetics of a New Antipsychotic Agent Perospirone and Its Active Metabolite, and Its Relationship // Therapeutic Drug Monitoring: journal. - 2004 .-- August ( vol. 26 , no. 4 ). - P. 361-365 . - DOI : 10.1097 / 00007691-200408000-00004 . - PMID 15257064 .
- ↑ de Paulis, T. Perospirone (Sumitomo Pharmaceuticals) (neopr.) // Current Opinion in Investigational Drugs. - 2002. - January ( t. 3 , No. 1 ). - S. 121-129 . - PMID 12054062 .
- ↑ Sumitomo Pharmaceuticals 2001 | News Release | Dainippon Sumitomo Pharma (Link not available) . Archived February 24, 2006.
- ↑ 1 2 Hirose, A; Kato, T; Ohno, Y; Shimizu, H; Tanaka, H; Nakamura, M; Katsube, J. Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions (Eng.) // Japanese Journal of Pharmacology: journal. - 1990 .-- July ( vol. 53 , no. 3 ). - P. 321-329 . - DOI : 10.1254 / jjp.53.321 . - PMID 1975278 .
- ↑ 1 2 3 4 Kishi, T; Iwata, N. Efficacy and Tolerability of Perospirone in Schizophrenia: A Systematic Review and Meta-Analysis of Randomized Controlled Trials (Eng.) // Drugs : journal. - Adis International 2013 .-- September ( vol. 27 , no. 9 ). - P. 731-741 . - DOI : 10.1007 / s40263-013-0085-7 . - PMID 23812802 .
- ↑ Roth, BL; Driscol, J. PDSP K i Database . Psychoactive Drug Screening Program (PDSP) . University of North Carolina at Chapel Hill and the United States National Institute of Mental Health (January 12, 2011). Archived on November 8, 2013.
- ↑ Kato, T; Hirose, A; Ohno, Y; Shimizu, H; Tanaka, H; Nakamura, M. Binding profile of SM-9018, a novel antipsychotic candidate (Eng.) // Japanese Journal of Pharmacology: journal. - 1990 .-- December ( vol. 54 , no. 4 ). - P. 478-481 . - DOI : 10.1254 / jjp.54.478 . - PMID 1982326 .
- ↑ Odagaki, Y; Toyoshima, R. 5-HT1A receptor agonist properties of antipsychotics determined by [35S] GTPgammaS binding in rat hippocampal membranes (Eng.) // Clinical and Experimental Pharmacology & Physiology : journal. - 2007. - Vol. 34 , no. 5-6 . - P. 462-466 . - DOI : 10.1111 / j.1440-1681.2007.04595.x . - PMID 17439416 .
- ↑ Seeman, P; Tallerico, T. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors (Eng.) // Molecular Psychiatry : journal. - 1998 .-- March ( vol. 3 , no. 2 ). - P. 123-134 . - DOI : 10.1038 / sj.mp.4000336 . - PMID 9577836 .
- ↑ Perospirone Hydrochloride . - The Royal Pharmaceutical Society of Great Britain, September 23, 2011.