
- Treatment: 应采用一般症状性和支持性措施,并立即进行胃灌洗。应监测呼吸、脉搏和血压,如同所有药物过量的情况一样。尚无丁螺环酮的特异性解毒剂,且丁螺环酮的可透析性尚未确定。(L1712)
- exposure pathway: 口服。在人体中迅速吸收。由于广泛的首过代谢,生物利用度低且可变(约5%)。
- Harmful effect: 临床医生可以通过继续治疗和逐渐调整至最佳治疗剂量来减轻这些不良药物反应。值得注意的是,丁螺环酮具有最小的性副作用。它甚至被证明在作为增效剂给药时有助于减轻SSRIs的不良性作用。患者应收到关于中枢神经系统抑制可能性的警告。此外,临床医生应告知患者静坐不能(可能是由于中枢多巴胺拮抗作用)和血清素综合征的罕见可能性。上市后监测报告了与丁螺环酮相关的梦游症病例。然而,也应考虑精神疾病导致的神经生物学改变。QT延长也在有预先存在心脏疾病的患者中有报道...
- Toxicity summary: 丁螺环酮结合到背缝核前突触神经元和海马体后突触神经元上的5-HT型1A血清素受体,从而抑制背缝核含5-HT神经元的放电率。丁螺环酮还结合多巴胺D2型(DA2)受体,阻断前突触多巴胺受体。丁螺环酮增加蓝斑核的放电,这是大脑中高浓度去甲肾上腺素细胞体所在的区域。丁螺环酮作用的净结果是血清素能活性受到抑制,而去甲肾上腺素能和多巴胺能细胞放电增强。
- Regulatory information: REACH注册物质:状态:活跃 更新:2020-09-01 https://echa.europa.eu/registration-dossier/-/registered-dossier/31319
- Toxicity Data: LD50: 136 mg/kg (口服,大鼠)
- Hepatotoxicity: 药物类别:镇静剂和催眠药,杂类
- Symptoms and Signs: 过量的症状包括头晕、嗜睡、恶心或呕吐、严重的胃部不适和异常小的瞳孔。
- Hazard categories and classifications: 急性毒性 3 (100%)
- Carcinogen Classification: 对人类无致癌性迹象(未被IARC列出)。
- Drug Induced Liver Injury: 参考文献:DOI:10.1016/j.drudis.2019.09.022
- Effects During Pregnancy and Lactation: 目前尚不清楚丁螺环酮是否会影响男性生育能力(使伴侣怀孕的能力)或增加高于背景风险的出生缺陷风险。制造商的报告称性欲降低(性欲减少)、射精延迟和勃起功能障碍(无法获得和维持勃起)。这些问题可能影响男性生育能力。通常,父亲或精子捐献者的暴露不太可能增加妊娠风险。有关更多信息,请参阅MotherToBaby信息表父系暴露,网址为https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/。
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Research chemical 1g; ≥95%
Research chemical 1g; ≥95%; supplied for laboratory research, analysis, inspection, and scientific procurement use; specifications: 1g; ≥95%.
1g




