Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Grapefruit juice has minimal effects on plasma concentrations of lovastatin-derived 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors
Autore:
Rogers, JD; Zhao, J; Liu, LD; Amin, RD; Gagliano, KD; Porras, AG; Blum, RA; Wilson, MF; Stepanavage, M; Vega, JM;
Indirizzi:
Merck Res Labs, W Point, PA 19486 USA Merck Res Labs W Point PA USA 19486Merck Res Labs, W Point, PA 19486 USA Merck Res Labs, Rahway, NJ USA Merck Res Labs Rahway NJ USAMerck Res Labs, Rahway, NJ USA Millard Fillmore Hosp, Buffalo, NY 14209 USA Millard Fillmore Hosp Buffalo NY USA 14209 re Hosp, Buffalo, NY 14209 USA
Titolo Testata:
CLINICAL PHARMACOLOGY & THERAPEUTICS
fascicolo: 4, volume: 66, anno: 1999,
pagine: 358 - 366
SICI:
0009-9236(199910)66:4<358:GJHMEO>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
SERUM CONCENTRATIONS; SIMVASTATIN; FELODIPINE; CYCLOSPORINE; ITRACONAZOLE; MECHANISM; EFFICACY; HUMANS; ACID; RAT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Rogers, JD Merck Res Labs, WP75A-303, W Point, PA 19486 USA Merck Res LabsWP75A-303 W Point PA USA 19486 int, PA 19486 USA
Citazione:
J.D. Rogers et al., "Grapefruit juice has minimal effects on plasma concentrations of lovastatin-derived 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors", CLIN PHARM, 66(4), 1999, pp. 358-366

Abstract

Objective: To evaluate the effect of regular-strength grapefruit juice, a cytochrome P4503A4 (CYP3A4) inhibitor, on the pharmacokinetics of a commonly prescribed regimen of oral lovastatin. Methods: In a randomized crossover study, 16 healthy subjects received a single 40 mg dose of lovastatin in the evening after each consumed an 8-ounce glass of regular-strength grapefruit juice or water with breakfast for 3 consecutive days. The effect of the same grapefruit juice and water regimenon the pharmacokinetics of midazolam (2 mg oral dose given 1 hour after the third day of grapefruit juice and water) was used as a positive control in the same subjects, Plasma concentrations of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors were determined by an enzyme inhibition assay, and concentrations of lovastatin, lovastatin acid, and midazolam were determined by liquid chromatography-tandem mass spectrometry. Results: The area under the plasma concentration-time profiles (AUC) and maximum plasma concentrations (C-max) of HMG-CoA reductase inhibitors increased slightly (similar to 30% for each) after consumption of grapefruit juice. Similar effects on AUC and C-max (similar to 40% increase for each) werenoted after analysis of samples of hydrolyzed plasma (which converts inactive lactones to active hydroxy acid species). The AUC and C-max values for lovastatin approximately doubled in the presence of grapefruit juice, whereas the same parameters for lovastatin acid increased 1.6-fold. Grapefruit juice caused the AUC for midazolam to increase by a factor of similar to 2,4. Conclusions: Daily consumption of a glass of regular-strength grapefruit juice has a minimal effect on plasma concentrations of HMG-CoA reductase inhibitors (similar to 30% to 40% increase) after a 40 mg evening dose of lovastatin.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/10/20 alle ore 10:26:38