Tags: Voriconazole

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A white or almost white, hygroscopic, crystalline powder. It exhibits polymorphism. Slightly soluble in water freely soluble in methyl alcohol soluble in acetone.


Candida albicans and related species cause a variety of infections. Cutaneous candidiasis syndromes include erosio interdigitalis blastomycetica, folliculitis, balanitis, intertrigo paronychia, onychomycosis, diaper rash, perianal candidiasis, and the syndromes of chronic mucocutaneous candidiasis. Mucous membrane infections include oral candidiasis (thrush), esophagitis, and vaginitis.

Intestinal Helminths

Infections are often asymptomatic. In the immuno-compromised host, Strongyloides can progress to a fatal hyperinfection syndrome. Helminths include the roundworms (nematodes), flukes (trematodes), and tapeworms (cestodes). These parasites are large, ranging in size from 1 cm to 10 m, and they often live in the human gastrointestinal tract without causing symptoms.

Antifungal Agents

Fungi are eukaryotes, and they share many of the structural and metabolic characteristics of human cells. As a result, designing agents that affect fungi without harming human cells has proved difficult. One major difference between the two cell types is the primary sterol building block used to form the plasma membrane. The fungal plasma membrane consists of ergosterols; the major sterol component of the human plasma membrane is cholesterol.

Fungal Infections, Invasive

Systemic mycoses, such as histoplasmosis, coccidioidomycosis, cryptococcosis, blastomycosis, paracoccidioidomycosis, and sporotrichosis, are caused by primary or “pathogenic” fungi that can cause disease in both healthy and immunocompromised individuals. In contrast, mycoses caused by opportunistic fungi such as Candida albicans, Aspergillus spp., Trichosporon, Torulopsis (Candida) glabrata, Fusarium, Alternaria, and Mucor are generally found only in the immunocompromised host.

Antimicrobial Regimen Selection

A generally accepted systematic approach to the selection and evaluation of an antimicrobial regimen is shown in Table Systematic Approach for Selection of Antimicrobials. An «empiric» antimicrobial regimen is begun before the offending organism is identified, while a «definitive» regimen is instituted when the causative organism is known. The use of combinations to prevent the emergence of resistance is widely applied but not often realized. The only circumstance where this has been clearly effective is in the treatment of tuberculosis.


Efficacy has been demonstrated in clinical studies in patients for primary therapy of invasive aspergillosis, for primary and salvage therapy of invasive aspergillosis, and for treatment of invasive aspergillosis in patients whose disease was refractory to, or who were intolerant of, other antifungal therapy. Aspergillus fumigatus was the most frequent isolate in patients with aspergillosis participating in clinical trials with the drug. A complete or partial response was achieved in 48% of patients in this study, with lower response rates observed in patients with definite disease (38%) than in those with probable disease (58%).

Voriconazole: Drug Interactions

Voriconazole, a triazole antifungal agent, is a synthetic derivative of fluconazole. Like other azole antifungal agents, voriconazole presumably exerts its antifungal activity by altering cellular membranes, resulting in increased permeability, secondary metabolic effects, and growth inhibition. Although the exact mechanism of action of voriconazole has not been fully determined, the drug inhibits cytochrome P-450-dependent sterol 14-a-demethylase in susceptible fungi, which leads to accumulation of C-14-methylated sterols (e.g., lanosterol) and decreased concentrations of ergosterol. Voriconazole is active in vitro against Aspergillus fumigatus, A. flavus, A. niger, and A. terreus.