Alprazolam grapefruit juice

Yasui N, Kondo T, Furukori H, et al. Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam. Psychopharmacology (Berl) 2000 150(2) 185-190. 

There have been two studies of the effects of repeated ingestion of grapefruit juice on the pharmacokinetics and pharmacodynamics of both single and multiple oral doses of alprazolam in a total of 19 subjects (38). Grapefruit juice altered neither the steady-state plasma concentration of alprazolam nor its clinical effects. 

ALPRAZOLAM, DIAZEPAM, MIDAZOLAM-ORAL GRAPEFRUIT JUICE Possibly t efficacy and t adverse effects, e.g. sedation, CNS depression Possibly t bioavailability, 1 presystemic metabolism. Constituents of grapefruit juice irreversibly inhibit intestinal CYP3A4. Transport via P-gp and MRP-2 efflux pumps is also inhibited Avoid concomitant use. Be particularly vigilant in elderly patients or those with impaired liver function. Consider alternative, e.g. temazepam... 

Increased depressive effects when taken with other CNS depressants Inhibitors of CYP450 3A, such as nefazodone, fluvoxamine, fluoxetine, and even grapefruit juice, may decrease clearance of alprazolam and thereby raise alprazolam plasma levels and enhance sedative side effects alprazolam dose may need to be lowered... 

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,... 

CYP3A4 alprazolam, calcium channel blockers, cisapride, clarithromycin, cyclosporin A, erythromycin, HIV protease inhibitors, lidocaine, midazolam, simvastatin, terfenadine carbamazepine, dexamethsone, phenobarbital, phenytoin, rifampicin, St John s wort cimetidine, erythromycin, grapefruit juice, HIV protease inhibitors, itraconazole, ketoconazole... 

Alprazolam Is probably the BZD least affected by grapefruit juice, although many consider that the effect of grapefruit juice on midazolam Is unlikely to be clinically Important with 300 mL of juice, t plasma concentrations of diazepam are considered to be clinically insignificant - be aware of impaired cognition... 

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