Atorvastatin Grapefruit juice

Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. Clin Pharmacol Ther 1999 66(2) 118-127. 

Fukazawa I, Uchida N, Uchida E, Yasuhara H. Effects of grapefruit juice on pharmacokinetics of atorvastatin and pravastatin in Japanese. Br J Clin Pharmacol 2004 57(4) 448 55. 

Grapefruit juice inhibits CYP3A4, and serum concentrations of atorvastatin, but not of pravastatin, increased after administration of double-strength grapefruit juice 200 ml tds for 2 days (109). 

STATINS GRAPEFRUIT JUICE t levels with simvastatin slight rise with atorvastatin. t risk of adverse effects such as myopathy Constituent of grapefruit juice inhibits CYP3A4-mediated metabolism of simvastatin Patients taking simvastatin and atorvastatin should avoid grapefruit juice... 

Clinically important, potentially hazardous interactions with alfuzosin, alprazolam, amphotericin B, anisindione, antacids, aprepitant, astemizole, atorvastatin, bosentan, ciclesonide, cimetidine, clorazepate, conivaptan, cyproterone, dasatinib, dexamethasone, dicumarol, didanosine, eplerenone, erythromycin, ethotoin, fentanyl, fesoterodine, fosamprenavir, fosphenytoin, grapefruit juice, HMG-CoA reductase inhibitors, imatinib, ixabepilone, lapatinib, lopinavir, lovastatin, mephenytoin, methylprednisolone, micafungin, midazolam, nilotinib, pimozide, prednisolone, prednisone, quinidine, rifampin, rimonabant, rivaroxaban, sildenafil, silodosin, simvastatin, sirolimus, solifenacin, temsirolimus, terfenadine, tolvaptan, triazolam, vardenafil, vinblastine, vincristine, warfarin... 

Active components in grapefruit juice include furanocoumarins capable of inhibiting the metabolism of many drugs, including alprazolam, atorvastatin, cisapride, cyclosporine, and midazolam. Such compounds may also enhance oral bioavailability by inhibiting drug transporters in the Gl tract responsible for intestinal efflux of drugs,... 

Large amounts of grapefruit juice markediy increase the plasma ieveis of iovastatin and simvastatin, but only modestly affect the plasma levels of atorvastatin. Pravastatin seems not to interact The clinical signiflcance of the possible effects of pomegranate juice on rosuvastatin, and orange juice on pravastatin are unclear. 

Ando H, Tsuruoka S, Yanagihara H, Sugimoto K, Miyata M, Yamazoe Y, Takamura T, Kaneko S, Fujimura A. Effects of grapefruit juice on the pharmacddnetics of pitavastatin and atorvastatin. BrJ Clin Pharmacol (2005) 60,494-7. 

Especially the inhibition or induction of cytochrome P450 subtype 3A4 (CYP 3A4) is clinically relevant, because a variety of active substances and food substances (e.g. grapefruit juice) are able to affect this enzyme. Substances inhibiting CYP 3A4 include ciclosporin, dihydropyridines, verapamil, midazolam, paclitaxel, simvastatin, lovastatin, atorvastatin, cimetidine, erythromycin, troleandomycin, ketoconazole (and other azoles). Substances inducing CYP 3A4 include steroids, rifampicin, phenobarbital and St John s wort. 

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