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Current Options in Antifungal Pharmacotherapy

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Current Options in Antifungal Pharmacotherapy Current Options in Antifungal Pharmacotherapy John Mohr, Pharm.D., Melissa Johnson, Pharm.D., Travis Cooper, Pharm.D., James S. Lewis, II, Pharm.D., and Luis Ostrosky-Zeichner, M.D. Infections caused by yeasts and molds continue to be associated with high rates of morbidity and mortality in both immunocompromised and immuno- competent patients. Many antifungal drugs have been developed over the past 15 years to aid in the management of these infections. However, treatment is still not optimal, as the epidemiology of the fungal infections continues to change and the available antifungal agents have varying toxicities and drug- interaction potential. Several investigational antifungal drugs, as well as nonantifungal drugs, show promise for the management of these infections. Key Words: antifungal drugs, invasive fungal infection, amphotericin B, polyenes, invasive aspergillosis, liposomal amphotericin B, L-AmB. (Pharmacotherapy 2008;28(5):614–645) OUTLINE Icofungipen Polyenes Conclusion Mechanism of Action Invasive fungal infections continue to be asso- Clinical Efficacy ciated with high rates of morbidity and mortality Safety in both immunocompromised and immuno- Azoles competent hosts. Amphotericin B deoxycholate Mechanism of Action (AmBd) has been the cornerstone for treatment Clinical Efficacy of invasive fungal infections since the early Safety 1950s. However, new agents have emerged to Echinocandins manage these infections over the past 15 years Mechanism of Action (Figure 1). Although Candida species remain the Clinical Efficacy most common pathogens associated with fungal Safety disease, infections caused by Aspergillus and Investigational Antifungal Drugs and Other Cryptococcus sp, Zygomycetes, and the endemic Nonantifungal Agents fungi (Histoplasma, Blastomyces, and Coccidioides Monoclonal Antibody Against Heat Shock Protein 90 sp) also account for many fungal infections. Interferon-␥ Candida species have been associated with a Aminocandin wide spectrum of invasive disease, from catheter- Ravuconazole associated infections to widespread disseminated BAL8557 disease; reported attributable mortality rates are Other Azoles 10–70% in patients with nosocomial candidemia.1–3 From the Division of Infectious Diseases, Department of Empiric antifungal therapy delayed by as little as Internal Medicine, University of Texas Health Science 12 hours has been associated with increased Center, Houston, Texas (Drs. Mohr and Ostrosky-Zeichner); 4, 5 the Division of Infectious Diseases, Duke University Medical mortality. The term invasive candidiasis has Center, Durham, North Carolina (Dr. Johnson); the been used to collectively describe the severe Department of Pharmacy, Methodist Dallas Medical Center, forms of disease, excluding uncomplicated Dallas, Texas (Dr. Cooper); and the Department of Clinical candiduria and oropharyngeal and esophageal Pharmacy and Pharmacology, University of Texas Health 6 Science Center, San Antonio, Texas (Dr. Lewis). candidiasis. Address reprint requests to John Mohr, Pharm.D., Cubist Identifying patients at risk for development of Pharmaceuticals, 65 Hayden Avenue, Lexington, MA Candida infections is an important step in 02421; e-mail: [email protected]. deciding which patients should receive treatment.7 CURRENT OPTIONS IN ANTIFUNGAL PHARMACOTHERAPY Mohr et al 615 This treatment may include strategies that are In addition, C. parapsilosis, which typically either presumptive (index of suspicion is high demonstrates higher minimum inhibitory due to many risk factors) or prophylactic (aimed concentrations (MICs) in vitro than other Candida at disease prevention in high-risk patients).8 species against echinocandins, accounted for 20% Prolonged stay in the intensive care unit (ICU), of the isolates causing bloodstream infections. placement of central venous catheters, prolonged Aspergillus, a genus of mold ubiquitous in the treatment with broad-spectrum antibiotics, environment, can cause invasive fungal infections receipt of parenteral nutrition, recent surgery in nearly every organ in the immunocompromised (particularly intraabdominal), hemodialysis, and host, but the pulmonary system is most commonly a diagnosis of diabetes mellitus or pancreatitis affected.15 The true attributable mortality rate for have been identified as risk factors for invasive invasive aspergillosis is not known. However, candidiasis.9 historical data reporting a crude mortality rate of Selection of antifungal therapy for invasive 90% clearly no longer represent the current rate candidiasis may be influenced by changes in local in the era of allogeneic hematopoietic stem cell epidemiology. Over the past 10 years, a shift in transplantation (HSCT), in which nonmyeloablative species distribution has favored non-albicans chemotherapy and antifungal prophylaxis are Candida species.10, 11 Some evidence indicates administered.16 More recent studies have that fluconazole use has driven this shift12; suggested a shift of aspergillosis to late-onset however, other evidence has not been able to link infection with a more indolent course and previous fluconazole use with the emergence of significantly lower all-cause and attributable non-albicans species.13 In an antifungal suscep- mortality rates.17, 18 tibility survey of over 2000 bloodstream isolates A definitive diagnosis of invasive aspergillosis of Candida species, C. glabrata, which is less requires either a positive culture from a sterile susceptible to fluconazole in vitro than other site or, in the absence of a positive culture, species, accounted for 23% of the Candida histologic or radiologic evidence in a patient at bloodstream isolates; C. krusei, which is completely high risk with compatible clinical findings.19 resistant to fluconazole, accounted for 3%.14 When the organism is ultimately identified in However, such findings may vary by institution. tissues, the disease may be too advanced for Anidulafungin, posaconazole Micafungin Voriconazole Caspofungin Terbinafine ABCD, L-AmB ABLC Itraconazole Fluconazole Ketoconazole Miconazole Griseofulvin Flucytosine Amphotericin B Nystatin 1950 1955 1960 1965 1970 1975 1980 1985 1990 1995 2000 2005 Year Figure 1. Development of antifungal drugs from 1954–2007. ABCD = amphotericin B colloidal dispersion; L-AmB = liposomal amphotericin B; ABLC = amphotericin B lipid complex. 616 PHARMACOTHERAPY Volume 28, Number 5, 2008 successful treatment.20 Thus, tools for early Although infections caused by endemic mycoses diagnosis, preventive strategies, and new agents are not required to be reported to authorities, for treatment of the disease are needed to reduce estimates are that approximately 100,000 cases of overall mortality in patients with invasive coccidioidomycosis30 and 1–2 cases of blasto- aspergillosis.21 mycosis/100,000 persons in the general population Cryptococcus neoformans is an encapsulated occur annually in the geographic areas where the yeast that causes disease primarily of the central organisms are endemic.31 In addition, an estimated nervous system (CNS) and respiratory system.22 10–25% of patients with human immunodeficiency The incidence of disease is 0.4–1.3 cases/100,000 virus (HIV) infection develop disseminated persons in the general population and 2–7 histoplasmosis; however, environmental exposure cases/1000 patients with acquired immuno- and primary antifungal prophylaxis may affect deficiency syndrome (AIDS).23 In addition, prevalence.26 patients who have undergone organ transplan- Many antifungal agents are used to treat patients tation and are receiving high-dose corticosteroids with known or presumed invasive fungal infec- are at increased risk for development of tions and those at high risk for such infections. cryptococcosis.24 Overall mortality in patients In addition, several investigational antifungal with cryptococcal meningitis may be as high as drugs as well as nonantifungal drugs are being 30%, and even after an initial cure, 40% of studied for their management of these infections. patients have residual neurologic deficits.25 This article focuses on the use of these agents as Patients with AIDS, in whom the cryptococcal monotherapy because combination antifungal infection may never be cured, may require therapy has been reviewed in detail elsewhere.32 prolonged secondary prophylaxis.26 Zygomycosis is a group of fungal infections Polyenes caused by organisms such as Rhizopus, Absidia, Although more than 200 polyene antibiotics and Mucor. Zygomycetes can cause disseminated have been identified, amphotericin B and nystatin disease; however, disease of the pulmonary are the only polyenes used routinely in the system and paranasal sinuses with extension to clinical setting. In 1957, amphotericin B was the the brain are the most common.27 Diabetes and first antifungal agent approved by the United immunosuppression (e.g., hematologic malignancies States Food and Drug Administration (FDA) for with profound neutropenia) are the primary risk systemic administration. This agent was the factors for patients with zygomycosis.28 A definitive mainstay of antifungal treatment for invasive diagnosis of zygomycosis is made by demonstration fungal infections until triazoles and echinocandins of tissue invasion on histopathologic examination became available in recent years. Three commer- at the infection site with or without microbiologic cially available lipid formulations of amphotericin evidence of the fungus from the same site. The B—amphotericin B lipid complex (ABLC), prognosis for patients with zygomycosis
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