Experiment 68016
Worktypes
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Citrus paradisi (RUTACEAE) |
| Citation | ZAIDENSTEIN,R: SOBACK,S: GIPS,M: AVNI,B: DISHI,V: WEISSGARTEN,Y: GOLIK,A: SCAPA,E:. (2001). EFFECT OF GRAPEFRUIT JUICE ON THE PHARMACOKINETICS OF LOSARTAN AND ITS ACTIVE METABOLITE E3174 IN HEALTHY VOLUNTEERS.. 23(4) |
| Amount utilized | |
| Compound isolated | |
| Disease | THE EFFECT OF GJ ON LOSARTAN PHARMACOKINETICS WAS ASSESSED IN A RANDOMIZED CROSSOVER TRIAL. LOSARTAN WAS GIVEN TO 9 VOLUNTEERS WITH AND WITHOUT GJ. CONCENTRATIONS OF LOSARTAN AND ITS E3174 METABOLITE WERE DETERMINED IN SERUM BY HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD (HPLC). SIGNIFICANT DIFFERENCES WERE OBSERVED IN SOME OF THE PHARMACOKINETIC PARAMETERS OF LOSARTAN AND ITS METABOLITE E3174 AFTER LOSARTAN ADMINISTRATION WITH AND WITHOUT CO-ADMINISTERED GJ. THE LAG TIME (TIME TO DRUG APPEARANCE IN SERUM) OF LOSARTAN INCREASED SIGNIFICANTLY WITH CO-ADMINISTERED GJ. THE MEAN RESIDENCE TIME (MRT) AND HALF-LIFE (T 1/2) OF THE E3174 METABOLITE WERE SIGNIFICANTLY LONGER AND THE AREA UNDER THE CONCENTRATION-TIME CURVE (AUC) OF THE E3174 METABOLITE WAS SIGNIFICANTLY SMALLER AFTER CONCOMITANT GJ ADMINISTRATION. THE RATIO AUC LOSARTAN/AUC E3174 WAS SIGNIFICANTLY INCREASED AFTER CON-CURRENT GRAPEFRUIT JUICE INTAKE. THE INCREASED LAG TIME OF LOSARTAN AND THE INCREASED MRT AND T 1/2 AND DECREASED AUC OF E3174 WERE CONSIDERED INDICATIVE OF SIMULTANEOUS CYP 3A4 INHIBITION AND P-GLYCOPROTEIN ACTIVATION. THE SIGNIFICANTLY INCREASED AUC LOSARTAN/AUC E3174 RATIO, HOWEVER, INDICATES REDUCED LOSARTAN CONVERSION TO E3174 BY CYP 3A4 METABOLISM AS A RESULT OF CO-ADMINISTERED. |
| Dose amount | 200.0 ML |
| Number | 1 |
| Qualitative result | ACTIVE |
| Animal | HUMAN ADULT |
| Per unit | DAY |
| Dose expression | DOSE |
| Extract | BARK JUICE |
| Gender | GIVEN TO BOTH SEXES |