多年来，某些类型的类风湿性关节炎，包括类风湿性关节炎 (RA)，一直用硫酸羟氯喹治疗，这是一种由 4-喹啉衍生物开发的合成抗疟药物 [1]。虽然这些剂量可以阻断 DNA 或 RNA 配体诱导的 TLR9 或 7 信号传导，但氯喹同样对细胞内 pH 值没有明显影响 [2]。

硫酸股市缺线及其对应的硫酸股市缺线均值回撤TLR7和9信号，均用于治疗狼疮[2]。

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Infants exposed to hydroxychloroquine during breastfeeding receive only small amounts of the drug in breastmilk. In infants up to at least 1 year of age, careful follow-up found no adverse effects on growth, vision or hearing. International experts indicate that hydroxychloroquine is acceptable during breastfeeding.
When given once weekly for malaria prophylaxis, the amount of drug is not sufficient to harm the infant nor is the quantity sufficient to protect the child from malaria. Breastfeeding infants should receive the recommended dosages of hydroxychloroquine for malaria prophylaxis.
◉ Effects in Breastfed Infants
No adverse effects were reported in one 9-month-old breastfed infant whose mother was taking 310 mg hydroxychloroquine base daily for 6 weeks.
Five mothers took hydroxychloroquine 200 mg daily during pregnancy and breastfeeding, one for 30 months. Flash electroretinograms performed on the infants were normal.
Another group of investigators have reported numerous infants whose mother took hydroxychloroquine during pregnancy and were breastfed during maternal hydroxychloroquine use. An abstract reported 16 infants breastfed for 1 to 19 months and followed up at an average of 24 months (range 1 to 86 months) with no evidence of visual or hearing deficits. In a letter they reported 8 breastfed infants followed up at 1, 6 and 12 months of age who had normal growth and development and who had thorough, normal eye examinations at 1 and 12 months of age. In a case series, 13 mothers taking hydroxychloroquine sulfate 200 mg daily breastfed their infants for an average of 2.8 months (range 1 to 6 months). None had evidence of retinal, motor or growth abnormalities during 12 months of follow-up. The authors conclude that the benefits of breastfeeding outweigh the risk of hydroxychloroquine. It appears that the 8 infants reported in the letter were included among the 13 infants in the case series, but it is unclear whether the 16 infants reported in the abstract were part of the case series.
Thirty-three women who had been taking hydroxychloroquine for at least one year and exclusively breastfeeding had hydroxychloroquine milk levels determined over a 12-hour period. Two-thirds of the women were also taking a corticosteroid. Dosages ranged from 200 mg once every two days to 200 mg twice daily. Follow-up at 1 year of the infants did not find ocular toxicity or growth abnormalities.
In a cohort study, over a 10-year period 130 nursing mothers with a rheumatic disease took hydroxychloroquine during partial or exclusive breastfeeding. No mention was made of adverse effects in their infants.
A woman with nephrotic syndrome took hydroxychloroquine, cyclosporine, and prednisone during pregnancy and lactation. While breastfeeding she took hydroxychloroquine 200 mg, cyclosporine 125 mg in the morning and 100 mg at night (total of 3 mg/kg daily), daily and prednisone 30 mg daily. Her twin infants began partially breastfeeding (70 to 80% breastmilk) on day 7 postpartum and she continued to breastfeed for several months. The infants gained weight normally at one month of age and had no adverse reactions in the first three months postpartum.
A retrospective study was performed on data from patients with lupus erythematosus from 10 hospitals in the United Kingdom who received or did not receive hydroxychloroquine during pregnancy and lactation. One hundred fifty infants whose mothers took hydroxychloroquine during pregnancy and/or breastfeeding and were compared to 134 infants who were not exposed. Infants were followed for a median of 2.21 years. No differences in outcomes were seen between the two groups of infants, although the percentage of infants who were breastfed was not stated.
◉ Effects on Lactation and Breastmilk
A study of 43 women with systemic lupus erythematosus and their 57 pregnancies found that the use of hydroxychloroquine to treat the disease was associated with an increased duration of breastfeeding. Among mothers taking hydroxychloroquine, 88% breastfed for more than 6 months compared to 54% of women who did not take hydroxychloroquine.

[1]. Manzo C, et al. Psychomotor Agitation Following Treatment with Hydroxychloroquine. Drug Saf Case Rep. 2017 Dec;4(1):6.
[2]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40.
[3]. Yao X, et al. In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Clin Infect Dis. 2020 Mar 9. pii: ciaa237

Hydroxychloroquine Sulfate is a synthetic derivative of quinolyl with chemotherapeutic and antibiotic properties, Hydroxychloroquine Sulfate acts against erythrocytic malarial parasites (Plasmodium vivax, ovale, and malariae) by concentrating in food vacuoles. It inhibits plasmodial heme polymerase and acts through other unknown mechanisms. Hydroxychloroquine also has anti-inflammatory properties and is used in the treatment of rheumatoid arthritis and lupus erythematosus. (NCI04)
A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970)
See also: Hydroxychloroquine (has active moiety).

C18H28CLN3O5S

433.948

433.143

747-36-4

Hydroxychloroquine;118-42-3;(S)-Hydroxychloroquine;137433-24-0;(R)-Hydroxychloroquine;137433-23-9;Hydroxychloroquine sulfate (Standard);747-36-4;Hydroxychloroquine-d4 sulfate;1854126-45-6

12947

White to off-white solid powder

516.7ºC at 760 mmHg

240 °C

266.3ºC

4.284

131.37

4

8

9

28

413

0

JCBIVZZPXRZKTI-UHFFFAOYSA-N

InChI=1S/C18H26ClN3O.H2O4S/c1-3-22(11-12-23)10-4-5-14(2)21-17-8-9-20-18-13-15(19)6-7-16(17)181-5(2,3)4/h6-9,13-14,23H,3-5,10-12H2,1-2H3,(H,20,21)(H2,1,2,3,4)

2-((4-((7-chloroquinolin-4-yl)amino)pentyl)(ethyl)amino)ethan-1-ol sulfate

Ercoquin Plaquinol Toremonil Oxychlorochin Oxychloroquine Plaquenil

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~110 mg/mL (~253.49 mM)
DMF : 1.4 mg/mL (~3.23 mM)
DMSO :< 1 mg/mL

配方 1 中的溶解度: 100 mg/mL (230.44 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。