Sodium aurothiomalate hydrate | 39377-38-3

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: Sodium aurothiomalate hydrate
• 英文别名: disodium;gold(1+);2-sulfidobutanedioate;hydrate
• CAS: 39377-38-3；74916-57-7
• 化学式: C4H5AuNa2O5S
• 分子量: 408.09
• InChiKey: YLQOAPBVYJCTPW-UHFFFAOYSA-K

计算性质

• 辛醇/水分配系数(LogP)：
  -10.03
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  82.3
• 氢给体数：
  1
• 氢受体数：
  6

ADMET

代谢

对于接受金钠硫代苹果酸盐治疗的病人来说，尿液中主要的金物种是[Au(CN)2]-，这也出现在血液中的低分子量浸润中。

For a patient receiving gold sodium thiomalate the principal gold species in the urine is [Au(CN)2]-, which is also seen in a low molecular weight infiltrate of the blood

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用概述：金钠硫代苹果酸治疗后金进入乳汁的情况尚未经过严格研究。病例报告表明，乳汁中出现了少量金，至少有少量被吸收，因为可以在婴儿的尿液中检测到。没有报告出令人信服的毒性案例。综述文章的作者意见不一，有的建议避免使用，有的则允许使用。[1][2][3][4][5] 监测母乳喂养婴儿可能的副作用似乎是谨慎的。 ◉ 对母乳喂养婴儿的影响：据报道，有四名婴儿在母亲接受金疗法期间（包括金钠硫代苹果酸和金金硫葡萄糖）进行了母乳喂养。[6][8][9][10] 一名18个月大的婴儿在母亲治疗停止后3个月出现了暂时性面部水肿。[6] 这种反应可能是由于婴儿摄入了母亲乳汁中的金。 ◉ 对泌乳和母乳的影响：截至修订日期，没有找到相关的已发布信息。

◉ Summary of Use during Lactation:Excretion of gold into milk after gold sodium thiomalate has not been rigorously studied. Case reports indicate that gold appears in milk in small quantities and at least a little of it is absorbed because it is detectable in the infant's urine. No convincing cases of toxicity have been reported. Opinions of authors of review articles vary from recommending avoidance to allowing use.[1][2][3][4][5] Monitoring for possible adverse effects in the breastfed infant would seem prudent. ◉ Effects in Breastfed Infants:Four infants reportedly have been breastfed during maternal gold therapy (including gold sodium thiomalate and gold aurothioglucose).[6][8][9][10] Transient facial edema occurred in an 18-month-old infant, 3 months after the mother's treatment stopped.[6] The reaction was possibly due to gold in the mother's milk ingested by the infant. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 解毒与急救

当对金出现严重反应时，可能会给予皮质类固醇、二巯基丙醇（一种螯合剂）或青霉胺以帮助恢复。推荐使用泼尼松……来管理对金严重肾脏、血液、肺或肠结肠反应。当单独使用皮质类固醇治疗无效时，可以使用二巯基丙醇与皮质类固醇一起促进金的移除。

When severe reactions to gold occur, corticosteroids, dimercaprol (a chelating agent), or penicillamine may be given to aid recovery. Prednisone ... is recommended to manage severe renal, hematologic, pulmonary, or enterocolic reactions to gold. Dimercaprol may be used together with corticosteroids to facilitate removal of the gold when corticosteroid treatment alone is ineffective.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

当出现毒性反应时，应立即停止使用黄色素钠/金硫代马酸盐/的治疗。诸如局部皮炎、轻度口腔炎或轻微蛋白尿等轻微并发症通常不需要其他治疗，随着黄色素钠/金硫代马酸盐/的停用会自行解决。中重度皮肤和粘膜反应通常可以通过局部使用皮质类固醇、口服抗组胺药以及舒缓或麻醉乳膏来改善。

Treatment with myochrysine /gold sodium thiomalate/ should be discontinued immediately when toxic reactions occur. Minor complications such as localized dermatitis, mild stomatitis or slight proteinuria generally require no other therapy and resolve spontaneously with suspension of myochrysine /gold sodium thiomalate/. Moderately severe skin and mucous membrane reactions often benefit from topical corticosteroids, oral antihistaminics, and soothing or anesthetic lotions.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

对于严重的肾脏、血液、肺和肠炎并发症，建议使用大剂量的系统性皮质类固醇。皮质类固醇治疗的最佳持续时间因个别患者的反应而异。当不良反应异常严重或进展时，可能需要数月的治疗。

For serious renal, hematologic, pulmonary, and enterocolitic complications, high doses of systemic corticosteroids are recommended. The optimum duration of corticosteroid treatment varies with response of the individual patient. Therapy may be required for many months when adverse effects are unusually severe or progressive.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

在那些并发症在高剂量皮质类固醇治疗下没有改善的患者中，或者那些出现显著类固醇相关不良反应的患者中，可以给予螯合剂以增强金排泄。二巯基丙醇（BAL）已成功使用，但必须仔细监测患者，因为其使用可能会伴随许多不良反应。皮质类固醇和螯合剂可以同时使用。

In patients whose complications do not improve with high dose corticosteroid treatment, or who develop significant steroid related adverse reactions, a chelating agent may be given to enhance gold excretion. Dimercaprol (BAL) has been used successfully, but patients must be monitored carefully as numerous untoward reactions may attend it use. Corticosteroids and chelating agents may be used concomitantly.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

更高组织水平出现在使用注射金盐的情况下，平均稳态血浆水平为1至5微克/毫升。药物广泛分布于全身，包括淋巴结、骨髓、肾脏、肝脏、脾脏和各组织。大约85%至90%的药物与蛋白质结合。

Higher tissue levels occur with parenteral gold salts, with a mean steady state plasma level of 1 to 5 ug/ml. Drug is distributed widely throughout the body in lymph nodes, bone marrow, kidneys, liver, spleen, and tissues. About 85% to 90% is protein-bound.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

金钠硫代苹果酸盐在孕妇体内的金已被证明可以穿过胎盘。在接受金钠硫代苹果酸盐的妇女中，已经证明有少量金分布到乳汁中。

Gold has been shown to cross the placenta in pregnant women receiving gold sodium thiomalate. Small amounts of gold have been shown to be distributed into milk in women receiving ... gold sodium thiomalate.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

金钠硫代硫酸盐溶液在肌内注射后迅速被吸收，血清浓度在3-6小时内达到峰值。

Gold sodium thiomalate solutions are rapidly absorbed following IM injection, with peak serum concentrations occurring in 3-6 hours.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在给予单次10毫克金钠硫代硫酸盐剂量后，血清金浓度显示出双相下降，有一个相对快速的早期阶段（血清半衰期大约43小时）和一个缓慢的晚期阶段（血清半衰期大约6天）。下降的缓慢阶段可能是由于排泄，而快速下降阶段可能是由于组织分布。金化合物，包括金钠硫代硫酸盐的真实累积潜力尚未明确界定，但很明显，在给予parenteral金化合物治疗期间，比给予auranofin治疗期间，身体中保留的金量要大得多。

Following single 10-mg doses of gold sodium thiomalate, serum gold concentrations showed a biphasic decline with a relatively rapid early phase (serum half-life about 43 hours) and a slow late phase (serum half-life about 6 days). The slow phase of decline may result from excretion and the rapid phase of decline may result from tissue distribution. The true potential of gold compounds, including ... gold sodium thiomalate, to cumulate has not been clearly defined, but it is clear that substantially larger amounts of gold are retained in the body during therapy with parenteral gold compounds than during therapy with auranofin.

来源:Hazardous Substances Data Bank (HSDB)