| Disease | IN A RANDOMIZED, FOUR-PHASE, CROSSOVER STUDY, 12 HEALTHY VOLUNTEERS RECEIVED 0.25 MG TRIAZOLAM WITH WATER, WITH 200 ML NORMAL-STRENGTH OR DOUBLE-STRENGTH GRAPEFRUIT JUICE OR, ON THE THIRD DAY OF MULTIPLE-DOSE [THREE TIMES DAILY (T.I.D.)]
ADMINISTRATION OF DOUBLE-STRENGTH GRAPEFRUIT JUICE. TIMED BLOOD SAMPLES WERE COLLECTED UP TO 23 H AFTER DOSING, AND THE EFFECTS OF TRIAZOLAM WERE MEASURED WITH FOUR PSYCHOMOTOR TESTS UP TO 10 H AFTER DOSING. THE AREA UNDER THE PLASMA TRIAZOLAM
CONCENTRATION-TIME CURVE (AUC 0-INF) WAS INCREASED BY 53%, 49% AND 143% BY A SINGLE DOSE OF NORMAL-STRENGTH, A SINGLE DOSE OF DOUBLE-STRENGTH AND MULTIPLE-DOSE ADMINISTRATION OF DOUBLE-STRENGTH GRAPEFRUIT JUICE, RESPECTIVELY. ONE GLASS OF
GRAPEFRUIT JUICE INCREASES PLASMA TRIAZOLAM CONCENTRATIONS, BUT REPEATED CONSUMPTION OF GRAPEFRUIT JUICE PRODUCES A SIGNIFICANTLY GREATER INCREASE IN TRIAZOLAM CONCENTRATIONS THAN ONE GLASS OF JUICE. |