Loxapine

• 产品号: DB00408
• CAS号: 1977-10-2
• 分子式: C18H18ClN3O
• 分子量: 327.80802

产品别名

• 标题: Loxapine
• IUPAC标准名: 13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene
• IUPAC传统名: loxapine
• 商标名: Loxapina [INN-Spanish]; Loxitane C; Loxepine; Dibenzacepin; Cloxazepine; Dibenzoazepine; Hydrofluoride 3170; Lossapina [Dcit]; Loxapac; Loxapin; Loxapine [Usan:Ban:Inn]; Loxapinum [INN-Latin]; Loxitane Im; Oxilapine

产品登记号

• CAS号: 1977-10-2
• PubChem CID: 3964
• PubChem SID: 46505047

产品性质

• 疏水性(logP): 3.6

产品详细信息

详细说明 (English)

• Drug Groups: approved
• Description: An antipsychotic agent used in schizophrenia. [PubChem]
• Indication: For the management of the manifestations of psychotic disorders such as schizophrenia
• Pharmacology: Loxapine, a dibenzoxazepine compound, represents a subclass of tricyclic antipsychotic agents, chemically distinct from the thioxanthenes, butyrophenones, and phenothiazines. Pharmacologically, Loxapine is a tranquilizer for which the exact mode of action has not been established, however, it is believed that by antagonising dopamine and serotonin receptors, there is a marked cortical inhibition which can manifest as tranquilization and suppression of aggression.
• Toxicity: LD₅₀=65 mg/kg (Orally in mice)
• Affected Organisms: Humans and other mammals
• Biotransformation: Hepatic
• Absorption: Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers
• Half Life: Oral-4 hours
• Elimination: Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.
• References: Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6. [Pubmed] ; Cheung SW, Tang SW, Remington G: Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Mar 8;564(1):213-21. [Pubmed]
• External Links: Wikipedia; RxList; Drugs.com

参考文献

• Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6. Pubmed
• Cheung SW, Tang SW, Remington G: Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Mar 8;564(1):213-21. Pubmed