Itraconazole oral solution

ETFN patients with suspected fungal infections - 200 mg IV twice daily for 4 doses, followed by 200 mg once daily for up to 14 days. Continue treatment with 200 mg itraconazole oral solution (20 ml) twice daily until resolution of clinically significant neutropenia. The safety and efficacy of itraconazole use exceeding 28 days in ETFN is not known. 

Oral solution/Injectlon The oral bioavailability is maximal when itraconazole oral solution is taken without food. Steady state is reached after 1 to 2 weeks during chronic administration. Peak plasma levels are observed 2 hours (fasting) to 5 hours (with food) following oral administration. Steady-state plasma concentrations are approximately 25% lower when the oral solution is taken with food. 

Cystic fibrosis If a patient with cystic fibrosis does not respond to itraconazole oral solution, consider switching to alternative therapy. 

Severely neutropenic patients Itraconazole oral solution as treatment for oropharyngeal and/or esophageal candidiasis was not investigated in severely neutropenic patients. Because of its pharmacokinetic properties, itraconazole oral solution is not recommended for initiation of treatment in patients at immediate risk of systemic candidiasis. 

Children Safety and efficacy have not been established. A small number of patients from 3 to 16 years of age have been treated with 100 mg/day for systemic fungal infections and no serious adverse effects have been reported. Itraconazole oral solution was given to 26 pediatric patients 6 months to 12 years of age. Itraconazole was dosed at 5 mg/kg once daily for 2 weeks, and no serious unexpected adverse events were reported. 

Gubbins PO, McConnell SA, Gurley BJ, et al. Influence of grapefruit juice on the systemic availability of itraconazole oral solution in healthy adult volunteers. Pharmacotherapy 2004 24(4) 460 67. 

Itraconazole oral solution contains 10 mg of itraconazole per milliliter, solubilized by hydroxypropyl-(beta)-cyclo-dextrin (400 mg/mL) as a molecular inclusion complex. The solution is clear and yellowish in color with a target... 

Janssen Research Foundation, Itraconazole Oral Solution, NDA 020657, Food and Drug Administration, Freedom of Information Staff (HFI-35), 5600 Fishers Lane, Rockville MD 20857, http //www.fda.gov/. 

Amphotericin and itraconazole have been compared in a multicenter, open, randomized study in 277 adults with cancer and neutropenia (54). Itraconazole oral solution (100 mg bd, n — 144) was compared with a combination of amphotericin capsules and nystatin oral suspension n — 133). Adverse events were reported in about 45% of patients in each group. The most frequent were vomiting (14 versus 12 patients), diarrhea (12 versus 9 patients), nausea (5 versus 12 patients), and rash (2 versus 13 patients). There were no differences in liver function... 

In a double-blind comparison in oropharyngeal candidiasis in 244 patients with AIDS, itraconazole oral solution and fluconazole capsules (each 100 mg/day for 14 days) were equally efficacious there were no significant differences in adverse effects (17). 

Itraconazole oral solution and fluconazole tablets have been compared in oropharyngeal candidiasis in HIV/ AIDS patients in a prospective randomized, blind, multicenter trial (18). Both regimens of itraconazole oral solution (100 mg bd for 7 days or 100 mg od for 14 days) were equivalent to fluconazole (100 mg od for 14 days). Itraconazole oral solution was well tolerated. 

Boogaerts MA, Maertens I, Van Der Geest R, Bosly A, Michaux JM, Van Hoof A, Cleeren M, Wostenborghs R, De Beule K. Pharmacokinetics and safety of a 7-day administration of intravenous itraconazole followed by a 14-day administration of itraconazole oral solution in patients with hematologic malignancy. Antimicrob Agents Chemother 2001 45(3) 981-5. 

Phillips P, De Beule K, Frechette G, Tchamouroff S, Vandercam B, Weitner L, Hoepelman A, Stingl G, Clotet B. A double-blind comparison of itraconazole oral solution and fluconazole capsules for the treatment of oropharyngeal candidiasis in patients with AIDS. Chn Infect Dis 1998 26(6) 1368-73. 

Graybill JR, Vazquez J, Darouiche RO, Morhart R, Greenspan D, Tuazon C, Wheat LJ, Carey J, Leviton I, Hewitt RG, MacGregor RR, Valenti W, Restrepo M, Moskovitz BL. Randomized trial of itraconazole oral solution for oropharyngeal candidiasis in HIV/AIDS patients. Am J Med 1998 104(l) 33-9. 

Foot AB, Veys PA, Gibson BE. Itraconazole oral solution as antifungal prophylaxis in children undergoing stem cell transplantation or intensive chemotherapy for haematological disorders. Bone Marrow Transplant 1999 24(10) 1089-93. 

Willems L, van der Geest R, de Beule K. Itraconazole oral solution and intravenous formulations a review of pharmacokinetics and pharmacodynamics. J Clin Pharm Ther 2001 Jun 26(3) 159-169. 

Systemic oral azoles should be reserved for use in the more severe episodes of OPC unresponsive to topical agents or in patients with concurrent esophageal involvement. Although clinical response in more than 80% of patients can be obtained with 50 to 200 mg/day of fluconazole, response occurs within 10 days with the 50-mg daily dose compared to within 5 days for 100- to 200-mg daily doses even for the most intractable forms of OPC. The lower dose potentially may contribute to selection of resistance. Itraconazole oral solution with an improved absorption profile compared with the capsule formulation is comparable with fluconazole with respect to clinical and mycologic response and relapse rates. A 14-day treatment course of itraconazole seems to be more effective than a 7-day course—the shorter course is associated with lower rates of mycologic cure and higher relapse rates. Itraconazole solution can be used as first-line therapy for OPC, and it may be used for cases... 

In contrast, studies with itraconazole oral solution give different results. A study in 30 healthy males given itraconazole soluhon 200 mg daily, either on an empty stomach or with a standard breakfast, found that the bi-oavailability was 29% higher when itraconazole was taken in the fasted state. ... 

Itraconazole. Itraconazole 200 mg [capsule] was given after a standard breakfast to 11 healthy subjects after 14 days pre-treatment with omeprazole 40 mg daily. The AUC and maximum serum level of itraconazole were both reduced by about 65%. In contrast, another study in 15 healthy subjects found that omeprazole 40 mg daily did not significantly affect the pharmacokinetics of single 400-mg doses of itraconazole or its metabolite hydroxyitraconazole when given as an oral solution. However, there was a large interpatient variation in mean serum levels. Another study similarly reported that omeprazole had little effect on the pharmacokinetics of itraconazole oral solution. ... 

Grapefruit juice impaired the absorption of itraconazole capsules in one study, but not in another. Grapefruit juice had no effect on the absorption of itraconazole oral solution. Orange juice impaired the absorption of itraconazole capsules in one study. 

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