For many years, certain types of rheumatoid arthritis, including rheumatoid arthritis (RA), have been treated with hydroxychloroquine sulfate, a synthetic antimalarial medication developed from a 4-quinoline derivative [1]. While these dosages can block DNA or RNA ligand-induced TLR9 or 7 signaling, or chloroquine likewise has no discernible effect on intracellular pH [2].

The sulfuric acid stock market Quexian and its counterparts, the sulfuric acid stock market Quexian mean retracement TLR7 and 9 signals, are used to treat lupus [2].

Effects During Pregnancy and Lactation
◉ Overview of Lactation Use
Infants exposed to hydroxychloroquine during lactation ingest only small amounts of the drug through breast milk. Careful follow-up of infants under 1 year of age revealed no adverse effects on growth, vision, or hearing. International experts indicate that hydroxychloroquine use during lactation is acceptable.
When used weekly for malaria prevention, the dosage is insufficient to harm the infant or protect the child from malaria infection. Breastfed infants should receive the recommended dose of hydroxychloroquine for malaria prevention.
◉ Impact on Breastfed Infants
One 9-month-old breastfed infant with no reported adverse reactions had a mother who took 310 mg of hydroxychloroquine daily for 6 weeks.
Five mothers took 200 mg of hydroxychloroquine daily during pregnancy and lactation, one for up to 30 months. Flash electroretinography (FIR) results were normal in these infants. Another group of researchers reported multiple cases of infants whose mothers took hydroxychloroquine during pregnancy and who were breastfed while their mothers were taking hydroxychloroquine. An abstract reported that 16 infants were breastfed for 1 to 19 months, with a mean follow-up of 24 months (range 1 to 86 months), and no visual or hearing impairments were observed. In a letter, they reported 8 breastfed infants followed up at 1, 6, and 12 months of age; these infants showed normal growth and development and underwent comprehensive ophthalmological examinations at 1 month and 12 months of age, all with normal results. In a case series, 13 mothers who took 200 mg of hydroxychloroquine sulfate daily breastfed for an average of 2.8 months (range 1 to 6 months). During the 12-month follow-up period, none of the infants showed retinal, motor, or growth abnormalities. The authors concluded that the benefits of breastfeeding outweighed the risks of hydroxychloroquine. The 8 infants reported in the letter appear to be included in the 13 infants in the case series, but it is unclear whether the 16 infants reported in the abstract were included in the case series.
Thirty-three women who had taken hydroxychloroquine for at least one year and were exclusively breastfeeding underwent a 12-hour hydroxychloroquine concentration measurement in their breast milk. Two-thirds of the women were also taking corticosteroids. Dosage ranged from 200 mg every two days to 200 mg twice daily. Infants were followed up for one year, and no ocular toxicity or growth abnormalities were observed.
In a cohort study, 130 breastfeeding mothers with rheumatic diseases took hydroxychloroquine for 10 years while they were partially or exclusively breastfeeding. Adverse reactions in infants were not mentioned in the study.
A woman with nephrotic syndrome took hydroxychloroquine, cyclosporine, and prednisone during pregnancy and lactation. During lactation, she took 200 mg of hydroxychloroquine daily, 125 mg of cyclosporine in the morning and 100 mg in the evening (total daily dose of 3 mg/kg), and 30 mg of prednisone. Her twins were partially breastfed (70% to 80% breast milk) starting on day 7 postpartum and she continued breastfeeding for several months. The infants gained weight normally at one month of age and experienced no adverse reactions in the first three months postpartum.
A retrospective study analyzed data from 10 UK hospitals of patients with lupus who had or had not taken hydroxychloroquine during pregnancy and lactation. The study compared 150 infants whose mothers took hydroxychloroquine during pregnancy and/or lactation with 134 infants who had not been exposed to hydroxychloroquine. The median follow-up time for the infants was 2.21 years. There were no differences in outcomes between the two groups, but the proportion of breastfed infants was not specified.
◉ Effects on lactation and breast milk
A study of 43 patients with systemic lupus erythematosus and their 57 pregnancies found that hydroxychloroquine treatment for the disease was associated with prolonged breastfeeding. Among mothers who took hydroxychloroquine, 88% breastfed for more than 6 months, compared to 54% among mothers 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 quinolone derivative with chemotherapeutic and antibacterial properties. Hydroxychloroquine sulfate combats erythrocytic Plasmodium (Plasmodium vivax, Plasmodium ovale, and Plasmodium malariae) by accumulating in food vesicles. It inhibits Plasmodium heme polymerase and acts through other unknown mechanisms. Hydroxychloroquine also has anti-inflammatory properties and is used to treat rheumatoid arthritis and lupus erythematosus. (NCI04)
A chemotherapeutic drug against erythrocytic Plasmodium. Hydroxychloroquine appears to accumulate in the food vesicles of infected parasites. It inhibits Plasmodium heme polymerase. (Excerpt from Gilman et al., Pharmacological Basis of Therapeutic Drugs by Goodman and Gilman, 9th ed., p. 970)
See also: Hydroxychloroquine (with active fraction).

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

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

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

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

Solubility in Formulation 1: 100 mg/mL (230.44 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)