Prednisolone Itraconazole

Itraconazole, given orally increased oral prednisolone concentrations by only 24% (481) but increased intravenous dexamethasone concentrations 3.3-fold and oral dexamethasone 3.7-fold (482). 

Varis T, Kivisto KT, Neuvonen PJ. The effect of itraconazole on the pharmacokinetics and pharmacodynamics of oral prednisolone. Eur J Clin Pharmacol 2000 56(l) 57-60. 

The effects of oral itraconazole (400 mg on the first day then 200 mg/day for 3 days) on the pharmacokinetics of a single oral dose of prednisolone 60 mg or methylprednisolone 48 mg have been studied in 14 healthy men in a two-period, crossover study (97). Plasma cortisol concentrations were determined as a pharmacodjmamic index. The disposition of prednisolone was unchanged. 

The effects of itraconazole on the pharmacokinetics and pharmacodynamics of oral prednisolone have been investigated in a double-blind, randomized, crossover study (98). Ten healthy subjects took either oral itraconazole 200 mg od or placebo for 4 days. On day 4 they took oral prednisolone 20 mg. Itraconazole increased the plasma AUC of prednisolone by 24% and its half-hfe by 29% compared with placebo. The peak plasma concentration and time to the peak of prednisolone were not affected. Itraconazole reduced the mean morning plasma cortisol concentration, measured 23 hours after prednisolone, by 27%. 

The minor interaction of itraconazole with oral prednisolone is probably of limited clinical significance. The susceptibility of prednisolone to interact with CYP3A4 inhibitors is considerably smaller than that of methylprednisolone, and itraconazole and probably also other inhibitors of CYP3A4 can be used concomitantly with prednisolone without marked interaction. 

Lebrun-Vignes B, Archer VC, Diquet B, Levron JC, Chosidow O, Puech AJ, Warot D. Effect of itraconazole on the pharmacokinetics of prednisolone and methylprednisolone and cortisol secretion in healthy subjects. Br J Clin Pharmacol 2001 51(5) 443-50. 

Clinically important, potentially hazardous interactions with amprenavir, aprepitant, bedomethasone, buprenorphine, calcium, chloramphenicol, cimetidine, dobazam, clorazepate, cyclosporine, cyproterone, darunavir, dasatinib, delavirdine, dexamethasone, diazoxide, disulfiram, dopamine, fesoterodine, fluconazole, flunisolide, fluoxetine, fosamprenavir, ginkgo biloba, hydrocortisone, imatinib, indinavir, influenza vaccines, isoniazid, isradipine, itraconazole, lacosamide, lapatinib, lopinavir, meperidine, methylprednisolone, midazolam, mivacurium, nelfinavir, nilotinib, nilutamide, phenylbutazone, piracetam, posaconazole, prednisolone, prednisone, primrose, ritonavir, rivaroxaban, sage, saquinavir, solifenacin, St John s wort, sucralfate, telithromycin, temsirolimus, teniposide, ticlopidine, tizanidine, tolvaptan, triamcinolone, uracil/tegafur, vigabatrin... 

There is some evidence to surest that itraconazole can increase the ieveis and/or effects of inhaled budesonide, the active metab-oiite of ciclesonide, deflazacort, dexamethasone and methylpred-nisoione, and, to a lesser extent, prednisolone and prednisone. A few case reports describe the development of secondary Cnsh-ing s syndrome in patients taking itraconazole and bndesonide, fluticasone and deflazacort... 

A study in 10 hedthy subjects found that itraconazole 200 mg daily for 4 days increased the AUC of a single 20-mg oral dose of prednisolone by 24%, but this was eonsidered to be of limited clinical significance. ... 

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