Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: Evidence for dominant presystemic elimination at the gut site

European Journal of Clinical Pharmacology

Volumn 56, Issue 9-10, 2000, Pages 643-649

  Uno, T ^a   Ohkubo, T ^a   Sugawara, K ^a   Higashiyama, A ^b   Motomura, S ^b   Ishizaki, T ^c  

^a HIROSAKI UNIVERSITY HOSPITAL   (Japan)

^b HIROSAKI UNIVERSITY   (Japan)

^c KUMAMOTO UNIVERSITY   (Japan)

Author keywords

Grapefruit juice; Intestinal drug metabolism; Nicardipine

Indexed keywords

NICARDIPINE; WATER;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL TRIAL; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG DISPOSITION; ENANTIOMER; FIRST PASS EFFECT; FOOD DRUG INTERACTION; FRUIT JUICE; GRAPE; HEMODYNAMICS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; INTESTINE ABSORPTION; JAPAN; LIVER METABOLISM; NORMAL HUMAN; PRIORITY JOURNAL; STEREOCHEMISTRY;

ADULT; AREA UNDER CURVE; BEVERAGES; BIOLOGICAL AVAILABILITY; CALCIUM CHANNEL BLOCKERS; CITRUS; CROSS-OVER STUDIES; HUMANS; INTESTINES; LIVER; MALE; NICARDIPINE; STEREOISOMERISM;

EID: 0034468612     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002280000235     Document Type: Article

References (41)

1. 'Second generation' dihydropyridine calcium antagonists. Greater vascular sensitivity and some unique applications
2. Anti-hypertensive dose-response effects of nicardipine in stable essential hypertension
3. Immediate and long-term effects of nicardipine, at rest and during exercise, in patients with coronary artery disease
4. Comparative pharmacokinetics of nicardipine hydrochloride, a new vasodilator, in various species
5. A review of the human metabolism and pharmacokinetics of nicardipine hydrochloride
6. Oxidation of dihydropyridine calcium channel blockers and analogues by human liver cytochrome P450 III A4
7. Use of in vitro and in vivo data to estimate the likelihood of metabolic pharmacokinetic interactions
8. Factors affecting the absolute bioavailability of nifedipine
9. Grapefruit juice and cimetidine inhibit stereoselective metabolism of nitrendipine in humans
10. Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics
11. Grapefruit juice-felodipine interaction: Reproducibility and characterization with the extended release drug formulation
12. Effect of grapefruit juice on the pharmacokinetics of amlodipine in health volunteers
13. Interaction of citrus juice with felodipine and nifedipine
14. Erythromycin-felodipine interaction: Magnitude, mechanism, and comparison with grapefruit juice
15. Drug interactions with grapefruit juice
16. In vitro inhibition of dihydrpyridine oxidation and aflatoxin B1 activation in human liver microsomes by naringenin and other flavonoids
17. Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavonoids found in grapefruit juice
18. Grapefruit juice-felodipine interaction: Mechanism, predictability, and effect of naringin
19. Identification of 6′, 7′-dihydroxybergamottin, a cytochrome P450 inhibitor in grapefruit juice
20. Specific CYP3A4 inhibitors in grapefruit juice: Furanocoumarin dimers as components of drug interaction
21. 6′, 7′-Dihydroxybergamottin in grapefruit juice and Seville orange juice: Effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein
22. Cytochrome P450 isoenzymes, epoxide hydrolase and glutathion transferase in rat and human hepatic and extrahepatic tissues
23. Characterisation of CYP3A gene subfamily expression in human gastrointestinal tissues
24. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism
25. First-pass metabolism of midazolam by the human intestine
26. Enantioselective high-performance iquid chromatographic determination of nicardipine in human plasma
27. Determination of (+)-and (-)-nicardipine concentration in human serum and their correlation with the antihypertensive effect after oral administration of racemic nicardipine
28. Noncompartmental determination of the steady-state volume of distribution
29. A physiological approach to hepatic drug clearance
30. Clinical pharmacokinetics: Concepts and applications
31. Enantio-selective determination of felodipine and other chiral dihydropyridine calcium entry blockers in human plasma
32. Determination of (+)- and (-)-nilvadipine in human plasma using chiral stationary-phase liquid chromatography and gas chromatography-mass spectrometry, and a preliminary pharmacokinetic study in humans
33. Simultaneous assessment of the intravenous and oral disposition of the enantiomers of racemic nimodipine by chiral stationary-phase high-performance liquid chromatography and gas chromatography/mass spectroscopy combined with a stable isotope technique
34. Stereoselective pharmacokinetics of oral and intravenous nitrendipine in healthy male subjects
35. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A4 protein expression
36. Relationship between time of intake of grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy subjects
37. The metabolism of nicardipine hydrochloride in healthy male volunteers
38. Single intravenous close and steady-state oral dose pharmacokinetics of nicardipine in healthy subjects
39. Clinical pharmacology of nicardipine in liver transplant patients
40. Effects of grapefruit juice ingestion-pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy men