Excretion of chloroquine, dapsone and pyrimethamine in human milk.

Edstein,; Veenendaal,; Newman, K; Hyslop, Richard M.

doi:10.1111/j.1365-2125.1986.tb02967.x

Cited by 61 publications

(19 citation statements)

References 9 publications

(9 reference statements)

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“…In a number of studies, CQ or its metabolites (Edstein et al 1986;Ogunbona et al 1987;Ette et al 1987a, b, c;Akintonwa et al 1988) as well as HCQ have been shown to be excreted in breast milk (Nation et al 1984;Østensen et al 1985). Transplacental transmission of CQ and HCQ has also been observed (Akintonwa et al 1988;CostedoatChalumeau et al 2002).…”

Section: Excretion In Breast Milk and Transplacental Passagementioning

confidence: 90%

Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

et al. 2015

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HCQ and CQ have a good reputation for being effective and relatively safe treatments in SLE, mild-moderate RA and Sjøgren's syndrome. There is need for (a) more information on their mode of action in relation to the control of these diseases, (b) scope for developing formulations that have improved pharmacokinetic and therapeutic properties and safety, and (c) further exploring their use in drug combinations not only with other disease modifying agents but also with biologics.

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Section: Excretion In Breast Milk and Transplacental Passagementioning

confidence: 90%

Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

et al. 2015

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“…The data quality is also variable because of small subject numbers in each study (1)(2)(3)(4)(5)(6)(7)(8)(9)(10), and wide variability in drug measurements per subject (13)(14)(15)(16)(17). Only three studies used AUC data to estimate milk Cavg.…”

Section: Discussionmentioning

confidence: 99%

Transfer of chloroquine and desethylchloroquine across the placenta and into milk in Melanesian mothers

Law

Ilett

Hackett

et al. 2008

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• The literature on placental and milk transfer of chloroquine and its major bioactive metabolite desethylchloroquine is sparse and incomplete. WHAT THIS STUDY ADDS• We have provided data on the transplacental transfer of chloroquine and desethylchloroquine in Melanesian women (n = 19), measured transfer of these drugs into breast milk (n = 16) and estimated absolute and relative infant doses for the breastfed infant.• The data for desethylchloroquine are novel.• In all three areas we have significantly increased both quantity and quality of the available database. AIMSTo investigate the transfer of chloroquine and its major bioactive metabolite desethylchloroquine across the placenta and into breast milk. METHODSIn Papua New Guinea, chloroquine (CQ; 25 mg base kg ) is recommended for prophylaxis of malaria during pregnancy, and at the Alexishafen Health Centre women are routinely prescribed CQ at the time of delivery. Fetal-cord and maternal serum samples were collected at delivery (n = 19) and milk samples were collected from day 3 to day 17-21 after delivery (n = 16). CQ and its primary active metabolite desethylchloroquine (DECQ) were quantified by high-performance liquid chromatography. For both CQ and DECQ cord/maternal ratios (C/M) were calculated to characterize placental transfer, and infant exposure via milk was estimated by standard methods. RESULTSThe median (interquartile range) C/M was 1.1 (0.9, 1.6) for CQ and 1.2 (0.5, 1.8) for DECQ. The average concentration in milk over the time of sampling was 167 mg l -1 (27, 340) for CQ and 54 mg l -1 (22, 106) for DECQ. Estimated absolute and relative infant doses were 34 mg kg -1 day -1 (7, 50) and 15 mg kg -1 day -1 (4, 26), and 2.3% (0.5, 3.6) and 1.0% (0.4, 2.0) for CQ and DECQ (as CQ equivalents), respectively. CONCLUSIONInfant exposure to CQ and DECQ during pregnancy will be similar to that in the maternal circulation, and dependent on maternal dose and frequency. The median CQ + DECQ relative infant dose of 3.2% (as CQ equivalents) was low, confirming that use of CQ during lactation is compatible with breastfeeding.

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“…Dapsone has also been reported to cross the blood-brain barrier and the placenta and is found in breast milk [5,6]. Hence, dapsone therapies are still associated with drawbacks of hemolysis, methemoglobinemia and patient non-compliance [7].…”

mentioning

confidence: 99%