Itraconazole is a recently developed triazole antifungal agent that inhibits cell membrane sterol biosynthesis. Itraconazole, in a dose-dependent manner, enhanced intracellular accumulation of daunorubicin and reversed the drug resistance in murine leukemia P388/ADR cells. In addition, itraconazole corrected the altered plasma membrane potentials of P388/ADR cells. The concentrations of itracon...

Comparison of itraconazole (R51,211) and ketoconazole in the treatment of experimental candidal vaginitis in rats on schedules of 3 and 5 days revealed significantly superior results with itraconazole at all dosages (1.0 to 7.5 mg/kg) studied, but was particularly evident at 1.0 and 2.5 mg/kg. A single 25-mg/kg dose of itraconazole was as effective as 5 daily 5-mg/kg doses of itraconazole.

Although there is a presumed drug-drug interaction between itraconazole and nonnucleoside reverse-transcriptase inhibitors, the medical literature lacks such documentation. We describe a drug-drug interaction between itraconazole and efavirenz in a patient with disseminated histoplasmosis and acquired immunodeficiency syndrome (AIDS). The drug combination resulted in persistently elevated urina...

BACKGROUND We call attention to the assumed association between itraconazole and pancreatitis by presentation of four Dutch case reports. METHODS AND RESULTS The Netherlands Pharmacovigilance Centre Lareb received four reports of pancreatitis associated with the use of itraconazole, all reported by health professionals. The diagnosis of pancreatitis was confirmed by diagnostic tests. All four...

Sir, Systemic mycoses, such as invasive aspergillosis, are usually treated with antifungal drugs such as iv amphotericin B or itraconazole capsules. The plasma concentrations of itraconazole observed in patients are sometimes much higher than the minimal therapeutic level (1000 ng/mL), and the potential hepatic toxicity of the drug needs to be evaluated. A retrospective study on the effect of i...

Oral corticosteroids are first-line therapy for allergic bronchopulmonary aspergillosis (ABPA), however, itraconazole has been recognized as an adjunctive treatment. This paper describes the prolonged use of itraconazole in an asthmatic patient with a diagnosis of ABPA. This case report features a patient who showed benefit with a longer duration of itraconazole therapy without demonstrating ad...

Itraconazole is a new orally active triazole antifungal agent with enhanced activity against Candida species. In the clinical trial described in this paper, we compared the efficacy and safety of itraconazole capsules with those of clotrimazole vaginal tablets and placebo oral capsules for women with acute vulvovaginal candidiasis. Ninety-five patients were randomized in a 2:1:1 fashion to rece...

The antiporliferative effect induced in vitro by two antifungal compounds, the azole itraconazole and the allylamine terbinafine on Leishmania major promastigotes are reported. Treatment of promastigote cultures with itraconazole or with terbinafine induced growth arrest. Concentrations of 0.75 μ/l or more of itraconazole induced cell lysis after 72 hours. However, even relatively large concent...

Choroidal neovascularization (CNV) is a major cause of severe visual loss in patients with age-related macular degeneration (AMD). Recently, itraconazole has shown potent and dose-dependent inhibition of tumor-associated angiogenesis. We evaluated the anti-angiogenic effect of itraconazole in a rat model of laser-induced CNV. After laser photocoagulation in each eye to cause CNV, right eyes wer...

Invasive aspergillosis is an increasingly frequent opportunistic infection in immunocompromised patients. Only two agents, amphotericin B and itraconazole, are licensed for therapy. Itraconazole acts through inhibition of a P-450 enzyme undertaking sterol 14alpha demethylation. In vitro resistance in Aspergillus fumigatus to itraconazole correlated with in vivo outcome has not been previously d...