[Drug-drug interaction and drug-induced interference with clinical laboratory test procedures--drug interaction in biopharmaceutics (author's transl)].
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Concomitant administration of grapefruit juice can increase the plasma concentration of numerous drugs in humans and decrease the concentration of a few others. Such elevations of drug plasma concentrations have, on occasion, resulted in adverse clinical effects. Increased concentrations are primarily mediated by chemicals in grapefruit juice, which inhibit the CYP 3A4 drug-metabolizing enzyme in the small intestines. This inhibition decreases the first-pass metabolism of drugs using the CYP 3A4 intestinal system and increases the bioavailability and maximal plasma drug concentrations (Cmax) of the CYP 3A4 substrates. The effect of grapefruit juice on drug metabolism is most pronounced in drugs with a high first-pass metabolism (eg, felodipine, amiodarone), in which it inhibits the first-pass metabolism of the CYP 3A4 substrates leading to an increase in Cmax and area under the concentration time curve (AUC). The use of grapefruit juice with a few specific drugs (eg, fexofenadine, digoxin) may lower plasma drug concentrations by inhibiting drug absorption catalyzed by the organic anion transporting polypeptide (OATP).
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Twenty antacid mixtures of six quality groups containing Al(OH)3, gel, Mg(OH)2, Mg2Si3O8, CaCO3 and NaAl(OH)2CO3 at different ratios were prepared and stored for 150 days at 20 degrees C in the form of aqueous suspensions. Changes of pH in the suspensions were measured, and the accompanying structural changes were examined by IR spectrometry and X-ray diffraction analysis. Hydrotalcite was found to be formed during storage of aqueous suspensions of mixtures of Al(OH)3 Mg(OH)2; Al(OH)3: Mg(OH)2: CaCO3; Al(OH)3: Mg(OH)2: NaAl(OH)2CO3 and Mg(OH)2: NaAl(OH)2CO3. Initial neutralization activities of the suspensions and those found after the storage were compared.
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