
- exposure pathway: 口服给药后从胃肠道缓慢但完全吸收。
- Toxicity summary: 马普替林通过抑制突触前儿茶酚胺的摄取发挥其抗抑郁作用,从而增加其在脑突触间隙的浓度。在单次剂量下,马普替林对脑电图的影响表现为α波密度上升,α波频率降低,α波幅度增加。然而,与其他三环类抗抑郁药一样,马普替林降低惊厥阈值。马普替林作为中枢突触前α<sub>2</sub>肾上腺素能抑制性自受体和异受体的拮抗剂,这种作用据推测会导致中枢去甲肾上腺素和血清素活性增加。马普替林也是一种中等强度的外周α<sub>1</sub>肾上腺素能拮抗剂,这可能解释了其偶尔...
- Regulatory information: 新西兰EPA化学品清单状态:马普替林:没有单独批准,但可在适当的团体标准下使用
- Toxicity Data: LD50: 900 mg/kg (口服,大鼠) (A308) LD50: 90 mg/kg (口服,人类) (A308)
- Symptoms and Signs: 过量的体征包括运动不安、肌肉抽搐和强直、震颤、共济失调、惊厥、高热、眩晕、瞳孔放大、呕吐、发绀、低血压、休克、心动过速、心律失常、心脏传导障碍、呼吸抑制,以及意识障碍直至深度昏迷。
- Carcinogen Classification: 对人类无致癌性迹象(未被IARC列出)。
- Drug Induced Liver Injury: 参考: DOI:10.1016/j.drudis.2011.05.007
- Effects During Pregnancy and Lactation: 在1999年至2008年对80,882对挪威母婴的研究中,392名女性报告了产后新使用抗抑郁药,201名报告她们在怀孕期间继续使用抗抑郁药。与未暴露对照组相比,怀孕晚期使用抗抑郁药与母乳喂养 initiation可能性降低7%相关,但对母乳喂养持续时间或 exclusivity 无影响。与未暴露对照组相比,新开始或重新使用抗抑郁药与6个月时主要母乳喂养可能性降低63%,以及任何母乳喂养可能性降低51%相关,同时母乳喂养突然停止的风险增加2.6倍。未提及特定的抗抑郁药。
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