Chloroquine in Human Milk

Abstract

Simultaneous milk and saliva samples were collected over a seven-day period from five lactating subjects after they had ingested two tablets of chloroquine sulfate (300 mg base). The samples were analyzed for chloroquine content by use of a combination of thin-layer chromatography and spectrophotometry. Regression analysis of two variables subject to error was used to determine the milk:saliva levels relationship. The Student's t test for paired data at .05 level of significance was used to evaluate the relationship between chloroquine levels in milk and saliva. The milk:saliva chloroquine concentrations ratio obtained by regression analysis was 0.89 +/- 0.08 (r = .93; P less than .05), and this compared favorably with the value of 0.99 +/- 0.07 obtained from the ratio of the AUC. There were no significant differences in the Tmax, Cmax, AUC, clearance, and elimination half-life values of chloroquine in milk and saliva (P greater than .05). Milk and saliva appear to be part of the central compartment. The amount of chloroquine estimated to be consumed by a nursling over a 24-hour period is about 0.55% of a 300-mg dose consumed by the mother. The data suggest that milk chloroquine levels can be estimated from saliva levels.

Prospective evaluation of a model for the prediction of milk:plasma drug concentrations from physicochemical characteristics.

“…The equation for predicting ln(M/P) ratios for basic drugs (equation 1) was then refined utilising the 10 new basic drugs in addition to those used to define the original model. This was performed, as previously, a Milk:plasma ratios were reported at 2.86 and 0.36 (Atkinson et al, 1990a), and 0.99 (Ette et al, 1987). Average = 1.40. b Milk:plasma ratios were reported from 2.43-5.64 (Hackett et al, 1990).…”

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

“…These results suggest that there may be effects of cimetidine on both the gastric absorption and CYP-mediated metabolism of CQ. In contrast, ranitidine does not affect the PK of CQ (Ette et al 1987b). It is possible that the lack of effects of ranitidine on CYP-mediated metabolism of CQ underlies this negative interaction.…”

Pharmacokinetics and Pharmacological Properties of Chloroquine and Hydroxychloroquine in the Context of COVID‐19 Infection

“…Chloroquine is also reported to transfer via placenta and into milk. 33,34 Hydroxychloroquine. The reported mean (± SD) blood-toplasma hydroxychloroquine concentration ratio is 7.2 (± 4.2).…”

“…suggest chloroquine protein binding is concentration independent over the range of 25–400 ng/mL and (S)‐chloroquine binds more to plasma (~ 67%) than (R)‐chloroquine (~ 49%). Chloroquine is also reported to transfer via placenta and into milk 33,34 …”