Drug inhibition of whole blood aspirin esterase.

Esterase inhibition attribute of grapefruit juice leading to a new drug interaction.

This report describes a newly identified potential of grapefruit juice (GFJ) in mediating pharmacokinetic drug interactions due to its capability to inhibit esterase. The study demonstrates that GFJ inhibits purified porcine esterase activity toward p-nitrophenyl acetate and the prodrugs lovastatin and enalapril. In rat and human hepatic or gut S9 fractions and rat gut lumen, GFJ inhibited the ...

Dmd #13268 1 Esterase Inhibition Attribute of Grapefruit Juice Leading to a New Drug Interaction

Determination of aspirin responsiveness by use of whole blood platelet aggregometry.

BACKGROUND Insufficient platelet inhibition is associated with an increased cardiovascular risk in up to 30% of patients taking regular doses of aspirin. We describe an assay to study aspirin responsiveness. METHODS We performed impedance aggregometry on diluted whole blood with 1 mg/L collagen and 0.5 mmol/L arachidonic acid (AA). We measured thromboxane B(2) (TXB(2)) by RIA. We examined 66 ...

Cl . the Phosphoric - Esterase of Blood

IN a previous communication [Martland and Robison, 1924] it was shown that after blood has been laked with distilled water a rapid increase in the amount of inorganic phosphate occurs even at room temperature. The change is still more rapid at 370 but is entirely inhibited when the blood is laked with 1 00 trichloroacetic acid, which indicates that it is due to the enzymic hydrolysis of phospho...

Esterase inhibition by grapefruit juice flavonoids leading to a new drug interaction.

Our previous studies described a newly identified potential of grapefruit juice (GFJ) in mediating pharmacokinetic drug interactions due to its capability of esterase inhibition. The current study identifies the active components in GFJ responsible for its esterase-inhibitory effect. The esterase-inhibitory potential of 10 constitutive flavonoids and furanocoumarins toward p-nitrophenylacetate ...