The effect of magnesium trisilicate and kaolin on the in vivo absorption of chloroquine.
An in vitro study indicated that certain antacids and adsorbents may decrease the oral availability of th two widely used antimalarial agents chloroquine and pyrimethamine. To determine if this data was applicable to the clinical (in vivo) situation, plasma levels of one of the antimalarial agents (chloroquine) were followed in six Negro--Arab volunteers both when given alone and when taken with separate doses of two of the implicated interactants (magnesium trisilicate and kaolin). This in vivo work confirmed the in vitro findings; chloroquine area under the plasma concentration-time curve data were decreased by both magnesium trisilicate (18.2%) and kaolin (28.6%). Similar results could be expected for pyrimethamine. It is suggested therefore, to avoid loss of drug, that the antimalarials should not be taken with gastrointestinal medications of this type or that their administration should be separated by at least 4 h to reduce the risk of them interacting in the gut, thus preventing drug adsorption to the antacids/adsorbents, and loss of systemic availability.
D000328:Adult; D001682:Biological Availability; D002738:Chloroquine / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D007616:Kaolin / Q000494:pharmacology*; D008274:Magnesium / Q000494:pharmacology*; D017633:Magnesium Silicates; D008297:Male; D012824:Silicic Acid / Q000494:pharmacology*; D012822:Silicon Dioxide / Q000494:pharmacology*
D017633:Magnesium Silicates; D012824:Silicic Acid; D007616:Kaolin; D012822:Silicon Dioxide; D002738:Chloroquine; C001671:magnesium trisilicate; D008274:Magnesium