1887

Chapter 129 : Antifungal Agents*

MyBook is a cheap paperback edition of the original book and will be sold at uniform, low price.

Ebook: Choose a downloadable PDF or ePub file. Chapter is a downloadable PDF file. File must be downloaded within 48 hours of purchase

Buy this Chapter
Digital (?) $30.00

Preview this chapter:
Zoom in
Zoomout

Antifungal Agents*, Page 1 of 2

| /docserver/preview/fulltext/10.1128/9781555817381/9781555817381.ch129-1.gif /docserver/preview/fulltext/10.1128/9781555817381/9781555817381.ch129-2.gif

Abstract:

This chapter reviews the four major families of antifungal drugs that are currently available for systemic administration: the allylamines (terbinafine), the azoles (ketoconazole, itraconazole, fluconazole, voriconazole, and posaconazole), the echinocandins (caspofungin, micafungin, and anidulafungin) and the polyenes (amphotericin B). The comparative activities of the major systemic antifungal agents against important groups of fungi are summarized. Discussion includes spectrum of activity, acquired resistance, pharmacokinetics, clinical use, drug interactions, and toxicity and adverse events. This chapter will also discuss the characteristics of the several other agents that can be used for the oral or parenteral treatment of superficial, subcutaneous, or systemic fungal infections. Novel agents that are currently in clinical trials are briefly reviewed.

Citation: Lockhart S, Warnock D. 2015. Antifungal Agents*, p 2223-2235. In Jorgensen J, Pfaller M, Carroll K, Funke G, Landry M, Richter S, Warnock D (ed), Manual of Clinical Microbiology, Eleventh Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817381.ch129
Highlighted Text: Show | Hide
Loading full text...

Full text loading...

References

/content/book/10.1128/9781555817381.mcm11.ch129
1. Ryder NS. 1991. Squalene epoxidase as a target for the allylamines. Biochem Soc Trans 19:774777.
2. Favre B,, Hofbauer B,, Hildering KS,, Ryder NS. 2003. Comparison of in vitro activities of 17 antifungal drugs against a panel of 20 dermatophytes by using a microdilution assay. J Clin Microbiol 41:48174819.
3. Fernández-Torres B,, Carrillo AJ,, Martín E,, del Palacio A,, Moore MK,, Valverde A,, Serrano M,, Guarro J. 2001. In vitro activities of 10 antifungal drugs against 508 dermatophyte strains. Antimicrob Agents Chemother 45:25242528.
4. Perea S,, Fothergill AW,, Sutton DA,, Rinaldi MG. 2001. Comparison of in vitro activities of voriconazole and five established antifungal agents against different species of dermatophytes using a broth macrodilution method. J Clin Microbiol 39:385388.
5. McGinnis MR,, Pasarell L. 1998. In vitro evaluation of terbinafine and itraconazole against dematiaceous fungi. Med Mycol 36:243246.
6. Ryder NS,, Wagner S,, Leitner I. 1998. In vitro activities of terbinafine against cutaneous isolates of Candida albicans and other pathogenic yeasts. Antimicrob Agents Chemother 42:10571061.
7. Shadomy S,, Espinel-Ingroff A,, Gebhart RJ. 1985. In-vitro studies with SF 86-327, a new orally active allylamine derivative. Sabouraudia 23:125132.
8. Hahn RC,, Fontes CJ,, Batista RD,, Hamdan JS. 2002. In vitro comparison of activities of terbinafine and itraconazole against Paracoccidioides brasiliensis. J Clin Microbiol 40:28282831.
9. McGinnis MR,, Nordoff NG,, Ryder NS,, Nunn GB. 2000. In vitro comparison of terbinafine and itraconazole against Penicillium marneffei. Antimicrob Agents Chemother 44:14071408.
10. Kovarik JM,, Mueller EA,, Zehender H,, Denouël J,, Caplain H,, Millerioux L. 1995. Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites. Antimicrob Agents Chemother 39:27382741.
11. Vickers AE,, Sinclair JR,, Zollinger M,, Heitz F,, Glänzel U,, Johanson L,, Fischer V. 1999. Multiple cytochrome P-450s involved in the metabolism of terbinafine suggest a limited potential for drug-drug interactions. Drug Metab Dispos 27:10291038.
12. Darkes MJ,, Scott LJ,, Goa KL. 2003. Terbinafine: a review of its use in onychomycosis in adults. Am J Clin Dermatol 4:3965.
13. McClellan KJ,, Wiseman LR,, Markham A. 1999. Terbinafine: an update of its use in superficial mycoses. Drugs 58:179202.
14. Revankar SG,, Nailor MD,, Sobel JD. 2008. Use of terbinafine in rare and refractory mycoses. Future Microbiol 3:917.
15. Howden BP,, Slavin MA,, Schwarer AP,, Mijch AM. 2003. Successful control of disseminated Scedosporium prolificans infection with a combination of voriconazole and terbinafine. Eur J Clin Microbiol Infect Dis 22:111113.
16. Hall M,, Monka C,, Krupp P,, O’Sullivan D. 1997. Safety of oral terbinafine: results of a postmarketing surveillance study in 25,884 patients. Arch Dermatol 133:12131219.
17. Manavathu EK,, Cutwright JL,, Chandrasekar PH. 1998. Organism-dependent fungicidal activities of azoles. Antimicrob Agents Chemother 42:30183021.
18. Sanglard D,, Odds FC. 2002. Resistance of Candida species to antifungal agents: molecular mechanisms and clinical consequences. Lancet Infect Dis 2:7385.
19. Courtney R,, Radwanski E,, Lim J,, Laughlin M. 2004. Pharmacokinetics of posaconazole coadministered with antacid in fasting or nonfasting healthy men. Antimicrob Agents Chemother 48:804808.
20. Daneshmend TK,, Warnock DW,, Ene MD,, Johnson EM,, Potten MR,, Richardson MD,, Williamson PJ. 1984. Influence of food on the pharmacokinetics of ketoconazole. Antimicrob Agents Chemother 25:13.
21. Ezzet F,, Wexler D,, Courtney R,, Krishna G,, Lim J,, Laughlin M. 2005. Oral bioavailability of posaconazole in fasted healthy subjects: comparison between three regimens and basis for clinical dosage recommendations. Clin Pharmacokinet 44:211220.
22. Heykants J,, Van Peer A,, Van de Velde V,, Van Rooy P,, Meuldermans W,, Lavrijsen K,, Woestenborghs R,, Van Cutsem J,, Cauwenbergh G. 1989. The clinical pharmacokinetics of itraconazole: an overview. Mycoses 32(Suppl 1): 6787.
23. Barone JA,, Moskovitz BL,, Guarnieri J,, Hassell AE,, Colaizzi JL,, Bierman RH,, Jessen L. 1998. Enhanced bioavailability of itraconazole in hydroxypropyl-β-cyclodextrin solution versus capsules in healthy volunteers. Antimicrob Agents Chemother 42:18621865.
24. Purkins L,, Wood N,, Kleinermans D,, Greenhalgh K,, Nichols D. 2003. Effect of food on the pharmacokinetics of multiple-dose oral voriconazole. Br J Clin Pharmacol 56(Suppl 1):1723.
25. Lipp HP. 2010. Clinical pharmacodynamics and pharmacokinetics of the antifungal extended-spectrum triazole posaconazole: an overview. Br J Clin Pharmacol 70:471480.
26. De Beule K,, Van Gestel J. 2001. Pharmacology of itraconazole. Drugs 61(Suppl 1):2737.
27. Purkins L,, Wood N,, Greenhalgh K,, Allen MJ,, Oliver SD. 2003. Voriconazole, a novel wide-spectrum triazole: oral pharmacokinetics and safety. Br J Clin Pharmacol 56(Suppl 1):1016.
28. Walsh TJ,, Karlsson MO,, Driscoll T,, Arguedas AG,, Adamson P,, Saez-Llorens X,, Vora AJ,, Arrieta AC,, Blumer J,, Lutsar I,, Milligan P,, Wood N. 2004. Pharmacokinetics and safety of intravenous voriconazole in children after single- or multiple-dose administration. Antimicrob Agents Chemother 48:21662172.
29. Theuretzbacher U,, Ihle F,, Derendorf H. 2006. Pharmacokinetic/pharmacodynamic profile of voriconazole. Clin Pharmacokinet 45:649663.
30. Lutsar I,, Roffey S,, Troke P. 2003. Voriconazole concentrations in the cerebrospinal fluid and brain tissue of guinea pigs and immunocompromised patients. Clin Infect Dis 37:728732.
31. Hariprasad SM,, Mieler WF,, Holz ER,, Gao H,, Kim JE,, Chi J,, Prince RA. 2004. Determination of vitreous, aqueous, and plasma concentration of orally administered voriconazole in humans. Arch Ophthalmol 122:4247.
32. Cauwenbergh G,, Degreed H,, Heykants J,, Woestenborghs R,, Van Rooy P,, Haeverans K. 1988. Pharmacokinetic profile of orally administered itraconazole in human skin. J Am Acad Dermatol 18:263268.
33. Willemsen M,, De Doncker P,, Willems J,, Woestenborghs R,, Van de Velde V,, Heykants J,, Van Cutsem J,, Cauwenbergh G,, Roseeuw D. 1992. Post-treatment itraconazole levels in the nail: new implications for treatment in onychomycosis. J Am Acad Dermatol 26:731735.
34. Brammer KW,, Coakley AJ,, Jezequel SG,, Tarbit MH. 1991. The disposition and metabolism of [14C]fluconazole in humans. Drug Metab Dispos 19:764767.
35. Krieter P,, Flannery B,, Musick T,, Gohdes M,, Martinho M,, Courtney R. 2004. Disposition of posaconazole following single-dose oral administration in healthy subjects. Antimicrob Agents Chemother 48:35433551.
36. Odds FC,, Bossche HV. 2000. Antifungal activity of itraconazole compared with hydroxy-itraconazole in vitro. J Antimicrob Chemother 45:371373.
37. Venkatakrishnan K,, von Moltke LL,, Greenblatt DJ. 2000. Effects of the antifungal agents on oxidative drug metabolism: clinical revelance. Clin Pharmacokinet 38:111180.
38. Pfaller MA,, Diekema DJ; International Fungal Surveillance Participant Group. 2004. Twelve years of fluconazole in clinical practice: global trends in species distribution and fluconazole susceptibility of bloodstream isolates of Candida. Clin Microbiol Infect 10(Suppl 1):1123.
39. Pfaller MA,, Messer SA,, Hollis RJ,, Jones RN. 2001. In vitro activities of posaconazole (Sch 56592) compared with those of itraconazole and fluconazole against 3,685 clinical isolates of Candida spp. and Cryptococcus neoformans. Antimicrob Agents Chemother 45:28622864.
40. Pfaller MA,, Messer SA,, Hollis RJ,, Boyken L,, Tendolkar S,, Kroeger J,, Diekema DJ. 2009. Variation in susceptibility of bloodstream isolates of Candida glabrata to fluconazole according to patient age and geographic location in the United States in 2001 to 2007. J Clin Microbiol 47:31853190.
41. González GM,, Fothergill AW,, Sutton DA,, Rinaldi MG,, Loebenberg D. 2005. In vitro activities of new and established triazoles against opportunistic filamentous and dimorphic fungi. Med Mycol 43:281284.
42. Paphitou NI,, Ostrosky-Zeitner L,, Paetznick VL,, Rodriguez JR,, Chen E,, Rex JH. 2002. In vitro activities of investigational triazoles against Fusarium species: effects of inoculum size and incubation time on broth microdilution susceptibility test results. Antimicrob Agents Chemother 46:32983300.
43. Almyroudis NG,, Sutton DA,, Fothergill AW,, Rinaldi MG,, Kusne S. 2007. In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. Antimicrob Agents Chemother 51:25872590.
44. Borst A,, Raimer MT,, Warnock DW,, Morrison CJ,, Arthington-Skaggs BA. 2005. Rapid acquisition of stable azole resistance by Candida glabrata isolates obtained before the clinical introduction of fluconazole. Antimicrob Agents Chemother 49:783787.
45. Martins MD,, Lozano-Chiu M,, Rex JH. 1998. Declining rates of oropharyngeal candidiasis and carriage of Candida albicans associated with trends towards reduced rates of carriage of fluconazole-resistant C. albicans in human immunodeficiency virus-infected patients. Clin Infect Dis 27:12911294.
46. Brandt ME,, Pfaller MA,, Hajjeh RA,, Hamill RJ,, Pappas PG,, Reingold AL,, Rimland D,, Warnock DW; Cryptococcal Disease Active Surveillance Group. 2001. Trends in antifungal drug susceptibility of Cryptococcus neoformans isolates in the United States: 1992 to 1994 and 1996 to 1998. Antimicrob Agents Chemother 45:30653069.
47. Govender NP,, Patel J,, van Wyk M,, Chiller TM,, Lockhart SR; Group for Enteric, Respiratory and Meningeal Disease Surveillance in South Africa (GERMS-SA). 2011. Trends in antifungal drug susceptibility of Cryptococcus neoformans, obtained through population-based surveillance, South Africa, 2002–2003 and 2007–2008. Antimicrob Agents Chemother 55:26062611.
48. Pappas PG,, Kauffman CA,, Andes D,, Benjamin DK,Jr,, Calandra TF,, Edwards JE,Jr,, Filler SG,, Fisher JF,, Kullberg BJ,, Ostrosky-Zeichner L,, Reboli AC,, Rex JH,, Walsh TJ,, and Sobel JD; Infectious Diseases Society of America. 2009. Clinical practice guidelines for the management of candidiasis: 2009 update by the Infectious Diseases Society of America. Clin Infect Dis 48:503535.
49. Galgiani JN,, Ampel NM,, Blair JE,, Catanzaro A,, Johnson RH,, Stevens DA,, Williams PL; Infectious Diseases Society of America. 2005. Coccidioidomycosis. Clin Infect Dis 41:12171223.
50. Perfect JR,, Dismukes WE,, Dromer F,, Goldman DL,, Graybill JR,, Hamill RJ,, Harrison TS,, Larsen RA,, Lortholary O,, Nguyen MH,, Pappas PG,, Powderly WG,, Singh N,, Sobel JD,, Sorrell TC. 2010 Clinical practice guidelines for the management of cryptococcal disease: 2010 update by the Infectious Diseases Society of America. Clin Infect Dis 50:291322.
51. Kauffman CA,, Bustamante B,, Chapman SW,, Pappas PG; Infectious Diseases Society of America. 2007. Clinical practice guidelines for the management of sporotrichosis: 2007 update by the Infectious Diseases Society of America. Clin Infect Dis 45:12551265.
52. Wheat LJ,, Freifeld AG,, Kleiman MB,, Baddley JW,, McKinsey DS,, Loyd JE,, Kauffman CA; Infectious Diseases Society of America. 2007. Clinical practice guidelines for the management of patients with histoplasmosis: 2007 update by the Infectious Diseases Society of America. Clin Infect Dis 45:807825.
53. Andes D,, Pascual A,, Marchetti O. 2009. Antifungal therapeutic drug monitoring: established and emerging indications. Antimicrob Agents Chemother 53:2434.
54. Goodwin ML,, Drew RH. 2008. Antifungal serum concentration monitoring: An update. J Antimicrob Chemother 61:1725.
55. Hope WW,, Billaud EM,, Lestner J,, Denning DW. 2008. Therapeutic drug monitoring for triazoles. Curr Opin Infect Dis 21:580586.
56. Cuenca-Estrella M,, Gomez-Lopez A,, Mellado E,, Buitrago MJ,, Monzon A,, Rodriguez-Tudela JL. 2006. Head-to-head comparison of the activities of currently available antifungal agents against 3,378 Spanish clinical isolates of yeasts and filamentous fungi. Antimicrob Agents Chemother 50:917921.
57. Baddley JW,, Marr KA,, Andes DR,, Walsh TJ,, Kauffman CA,, Kontoyiannis DP,, Ito JI,, Balajee SA,, Pappas PG,, Moser SA. 2009. Patterns of susceptibility of Aspergillus isolates recovered from patients enrolled in the Transplant-Associated Infection Surveillance Network. J Clin Microbiol 47:32713275.
58. Diekema DJ,, Messer SA,, Hollis RJ,, Jones RN,, Pfaller MA. 2003. Activities of caspofungin, itraconazole, posaconazole, ravuconazole, voriconazole, and amphotericin B against 448 recent clinical isolates of filamentous fungi. J Clin Microbiol 41:36233626.
59. Pfaller MA,, Boyken L,, Hollis RJ,, Messer SA,, Tendolkar S,, Diekema DJ. 2005. In vitro susceptibilities of clinical isolates of Candida species, Cryptococcus neoformans, and Aspergillus species to itraconazole: global survey of 9,359 isolates tested by Clinical and Laboratory Standards Institute broth microdilution methods. J Clin Microbiol 43:38073810.
60. Pfaller MA,, Messer SA,, Hollis RJ,, Jones RN; SENTRY Participants Group. 2002. Antifungal activities of posaconazole, ravuconazole, and voriconazole compared to those of itraconazole and amphotericin B against 239 clinical isolates of Aspergillus spp. and other filamentous fungi: report from SENTRY Antimicrobial Surveillance Program, 2000. Antimicrob Agents Chemother 46:10321037.
61. Johnson EM,, Szekely A,, Warnock DW. 1998. In-vitro activity of voriconazole, itraconazole and amphotericin B against filamentous fungi. J Antimicrob Chemother 42:741745.
62. Chapman SW,, Rogers PD,, Rinaldi MG,, Sullivan DC. 1998. Suceptibilities of clinical and laboratory isolates of Blastomyces dermatitidis to ketoconazole, itraconazole, and fluconazole. Antimicrob Agents Chemother 42:978980.
63. Li RK,, Ciblak MA,, Nordoff N,, Pasarell L,, Warnock DW,, McGinnis MR. 2000. In vitro activities of voriconazole, itraconazole, and amphotericin B against Blastomyces dermatitidis, Coccidioides immitis, and Histoplasma capsulatum. Antimicrob Agents Chemother 44:17341736.
64. Sabatelli F,, Patel R,, Mann PA,, Mendrick CA,, Norris CC,, Hare R,, Loebenberg D,, Black TA,, McNicholas PM. 2006. In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. Antimicrob Agents Chemother 50:20092015.
65. Gilgado F,, Serena C,, Cano J,, Gené J,, Guarro J. 2006. Antifungal susceptibilities of the species of the Pseudallescheria boydii complex. Antimicrob Agents Chemother 50:42114213.
66. Howard SJ,, Cerar D,, Anderson MJ,, Albarrag A,, Fisher MC,, Pasqualotto AC,, Laverdiere M,, Arendrup MC,, Perlin DS,, Denning DW. 2009. Frequency and evolution of azole resistance in Aspergillus fumigatus associated with treatment failure. Emerg Infect Dis 15:10681076.
67. Burgel PR,, Baixench MT,, Amsellem M,, Audureau E,, Chapron J,, Kanaan R,, Honoré I,, Dupouy-Camet J,, Dusser D,, Klaassen CH,, Meis JF,, Hubert D,, Paugam A. 2012. High prevalence of azole-resistant Aspergillus fumigatus in adults with cystic fibrosis exposed to itraconazole. Antimicrob Agents Chemother 56:869874.
68. Mellado E,, Garcia-Effron G,, Alcázar-Fuoli L,, Melchers WJ,, Verweij PE,, Cuenca-Estrella M,, Rodríguez-Tudela JL. 2007. A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations. Antimicrob Agents Chemother 51:18971904.
69. Lockhart SR,, Frade JP,, Etienne KA,, Pfaller MA,, Diekema DJ,, Balajee SA. 2011. Azole resistance in Aspergillus fumigatus isolates from the ARTEMIS global surveillance study is primarily due to the TR/L98H mutation in the cyp51A gene. Antimicrob Agents Chemother 55:44654468.
70. Chowdhary A,, Kathuria S,, Randhawa HS,, Gaur SN,, Klaassen CH,, Meis JF. 2012. Isolation of multiple-triazole-resistant Aspergillus fumigatus strains carrying the TR/L98H mutations in the cyp51A gene in India. J Antimicrob Chemother 67:362366.
71. van der Linden JW,, Snelders E,, Kampinga GA,, Rijnders BJ,, Mattsson E,, Debets-Ossenkopp YJ,, Kuijper EJ,, Van Tiel FH,, Melchers WJ,, Verweij PE. 2011. Clinical implications of azole resistance in Aspergillus fumigatus, The Netherlands, 2007–2009. Emerg Infect Dis 17:18461854.
72. Bueid A,, Howard SJ,, Moore CB,, Richardson MD,, Harrison E,, Bowyer P,, Denning DW. 2010. Azole antifungal resistance in Aspergillus fumigatus: 2008 and 2009. J Antimicrob Chemother 65:21162118.
73. Brandt ME,, Warnock DW. 2003. Epidemiolology, clinical manifestations, and therapy of infections caused by dematiaceous fungi. J Chemother 15(Suppl 2):3647.
74. Shikanai-Yasuda MA,, Benard G,, Higaki Y,, Del Negro GM,, Hoo S,, Vaccari EH,, Gryschek RC,, Segurado AA,, Barone AA,, Andrade DR. 2002. Randomized trial with itraconazole, ketoconazole and sulfadiazine in paracoccidioidomycosis. Med Mycol 40:411417.
75. Chapman SW,, Dismukes WE,, Proia LA,, Bradsher RW,, Pappas PG,, Threlkeld MG,, Kauffman CA; Infectious Diseases Society of America. 2008. Clinical practice guidelines for the management of blastomycosis: 2008 update by the Infectious Diseases Society of America. Clin Infect Dis 46:18011812.
76. Walsh TJ,, Anaissie EJ,, Denning DW,, Herbrecht R,, Kontoyiannis DP,, Marr KA,, Morrison VA,, Segal BH,, Steinbach WJ,, Stevens DA,, van Burik JA,, Wingard JR,, Patterson TF; Infectious Diseases Society of America. 2008. Treatment of aspergillosis: clinical practice guidelines of the Infectious Diseases Society of America. Clin Infect Dis 46:327360.
77. Groll AH,, Wood L,, Roden M,, Mickiene D,, Chiou CC,, Townley E,, Dad L,, Piscitelli SC,, Walsh TJ. 2002. Safety, pharmacokinetics, and pharmacodynamics of cyclodextrin itraconazole in pediatric patients with oropharyngeal candidiasis. Antimicrob Agents Chemother 46:25542563.
78. Vandewoude K,, Vogelaers D,, Decruyenaere J,, Jaqmin P,, De Beule K,, Van Peer A,, Woestenborghs R,, Groen K,, Colardyn F. 1997. Concentrations in plasma and safety of 7 days of intravenous itraconazole followed by 2 weeks of oral itraconazole solution in patients in intensive care units. Antimicrob Agents Chemother 41:27142718.
79. Shadomy S,, White SC,, Yu HP,, Dismukes WE. 1985. Treatment of systemic mycoses with ketoconazole: in vitro susceptibilities of clinical isolates of systemic and pathogenic fungi to ketoconazole. J Infect Dis 152:12491256.
80. Kaur IP,, Kakkar S. 2010. Topical delivery of antifungal agents. Expert Opin Drug Deliv 7:13031327.
81. Paphitou NI,, Ostrosky-ZeiCHner L,, Paetznick VL,, Rodriguez JR,, Chen E,, Rex JH. 2002. In vitro antifungal susceptibilities of Trichosporon species. Antimicrob Agents Chemother 46:11441146.
82. Vehreschild JJ,, Birtel A,, Vehreschild MJ,, Liss B,, Farowski F,, Kochanek M,, Sieniawski M,, Steinbach A,, Wahlers K,, Fätkenheuer G,, Cornely OA. 2013. Mucormycosis treated with posaconazole: review of 96 case reports. Crit Rev Microbiol 39:310324.
83. Restrepo A,, Tobón A,, Clark B,, Graham DR,, Corcoran G,, Bradsher RW,, Goldman M,, Pankey G,, Moore T,, Negroni R,, Graybill JR. 2007. Salvage treatment of histoplasmosis with posaconazole. J Infect 54:319327.
84. Kim MM,, Vikram HR,, Kusne S,, Seville MT,, Blair JE. 2011. Treatment of refractory coccidioidomycosis with voriconazole or posaconazole. Clin Infect Dis 53:10601066.
85. Van Burik JA,, Hare RS,, Solomon HF,, Corrado ML,, Kontoyiannis DP. 2006. Posaconazole is effective as salvage therapy in zygomycosis: a retrospective summary of 91 cases. Clin Infect Dis 42:e61e65.
86. Ananda-Rajah MR,, Grigg A,, Slavin MA. 2012. Making sense of posaconazole therapeutic drug monitoring: a practical approach. Curr Opin Infect Dis, 25:605611.
87. Raad II,, Graybill JR,, Bustamante AB,, Cornely OA,, Gaona-Flores V,, Afif C,, Graham DR,, Greenberg RN,, Hadley S,, Langston A,, Negroni R,, Perfect JR,, Pitisuttithum P,, Restrepo A,, Schiller G,, Pedicone L,, Ullmann AJ. 2006. Safety of long-term oral posaconazole use in the treatment of refractory invasive fungal infections. Clin Infect Dis 42:17261734.
88. Howard SJ,, Arendrup MC. 2011. Acquired antifungal drug resistance in Aspergillus fumigatus: epidemiology and detection. Med Mycol 49(Suppl 1):S90S95.
89. van der Linden JW,, Camps SM,, Kampinga GA,, Arends JP,, Debets-Ossenkopp YJ,, Haas PJ,, Rijnders BJ,, Kuijper EJ,, van Tiel FH,, Varga J,, Karawajczyk A,, Zoll J,, Melchers WJ,, Verweij PE. 2013. Aspergillosis due to voriconazole highly resistant Aspergillus fumigatus and recovery of genetically related resistant isolates from domiciles. Clin Infect Dis 57:513520.
90. Park S,, Kelly R,, Kahn JN,, Robles J,, Hsu MJ,, Register E,, Li W,, Vyas V,, Fan H,, Abruzzo G,, Flattery A,, Gill C,, Chrebet G,, Parent SA,, Kurtz M,, Teppler H,, Douglas CM,, Perlin DS. 2005. Specific substitutions in the echinocandin target Fks1p account for reduced susceptibility of rare laboratory and clinical Candida sp. isolates. Antimicrob Agents Chemother 49:32643273.
91. Tawara S,, Ikeda F,, Maki K,, Morishita Y,, Otomo K,, Teratani N,, Goto T,, Tomashima M,, Ohki H,, Yamada A,, Kawabata K,, Takasugi H,, Sakane K,, Tanaka H,, Matsumoto F,, Kuwahara S. 2000. In vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi. Antimicrob Agents Chemother 44:5762.
92. Perlin DS. 2007. Resistance to echinocandin-class antifungal drugs. Drug Resist Updat 10:121130.
93. Garcia-Effron G,, Lee S,, Park S,, Cleary JD,, Perlin DS. 2009. Effect of Candida glabrata FKS1 and FKS2 mutations on echinocandin sensitivity and kinetics of 1,3-β-d-glucan synthase: implication for the existing susceptibility breakpoint. Antimicrob Agents Chemother 53:36903699.
94. Zimbeck AJ,, Iqbal N,, Ahlquist AM,, Farley MM,, Harrison LH,, Chiller T,, Lockhart SR. 2010. FKS mutations and elevated echinocandin MIC values among Candida glabrata isolates from U.S. active surveillance. Antimicrob Agents Chemother 54:50425047.
95. Messer SA,, Diekema DJ,, Boyken L,, Tendolkar S,, Hollis RJ,, Pfaller MA. 2006. Activities of micafungin against 315 invasive clinical isolates of fluconazole-resistant Candida spp. J Clin Microbiol 44:324326.
96. Messer SA,, Moet GJ,, Kirby JT,, Jones RN. 2009. Activity of contemporary antifungal agents, including the novel echinocandin anidulafungin, tested against Candida spp., Cryptococcus spp., and Aspergillus spp.: report from the SENTRY Antimicrobial Surveillance Program (2006 to 2007). J Clin Microbiol 47:19421946.
97. Pfaller MA,, Boyken L,, Hollis RJ,, Messer SA,, Tendolkar S,, Diekema DJ. 2005. In vitro activities of anidulafungin against more than 2,500 clinical isolates of Candida spp., including 315 isolates resistant to fluconazole. J Clin Microbiol 43:54255427.
98. Pfaller MA,, Messer SA,, Boyken L,, Rice C,, Tendolkar S,, Hollis RJ,, Diekema DJ. 2003. Caspofungin activity against clinical isolates of fluconazole-resistant Candida. J Clin Microbiol 41:57295731.
99. Nakai T,, Uno J,, Otomo K,, Ikeda F,, Tawara S,, Goto T,, Nishimura K,, Miyaji M. 2002. In vitro activity of FK463, a novel lipopeptide antifungal agent, against a variety of clinically important molds. Chemotherapy 48:7881.
100. Lockhart SR,, Zimbeck AJ,, Baddley JW,, Marr KA,, Andes DR,, Walsh TJ,, Kauffman CA,, Kontoyiannis DP,, Ito JI,, Pappas PG,, Chiller TC. 2011. In vitro echinocandin susceptibility of Aspergillus isolates from patients enrolled in the Transplant-Associated Infection Surveillance Network. Antimicrob Agents Chemother 55:39443946.
101. Odabasi Z,, Paetznick VL,, Rodriguez JR,, Chen E,, Ostrosky-Zeichner L. 2004. In vitro activity of anidulafungin against selected clinically important mold isolates. Antimicrob Agents Chemother 48:19121915.
102. Nakai T,, Uno J,, Ikeda F,, Tawara S,, Nishimura K,, Miyaji M. 2003. In vitro antifungal activity of micafungin (FK463) against dimorphic fungi: comparison of yeast-like and mycelia forms. Antimicrob Agents Chemother 47:13761381.
103. Alexander BD,, Johnson MD,, Pfeiffer CD,, JiménezOrtigosa C,, Catania J,, Booker R,, Castanheira M,, Messer SA,, Perlin DS,, Pfaller MA. 2013. Increasing echinocandin resistance in Candida glabrata: clinical failure correlates with presence of FKS mutations and elevated minimum inhibitory concentrations. Clin Infect Dis 56:17241732.
104. Garcia-Effron G,, Kontoyiannis DP,, Lewis RE,, Perlin DS. 2008. Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies. Antimicrob Agents Chemother 52:41814183.
105. Kahn JN,, Garcia-Effron G,, Hsu MJ,, Park S,, Marr KA,, Perlin DS. 2007. Acquired echinocandin resistance in a Candida krusei isolate due to modification of glucan synthase. Antimicrob Agents Chemother 51:18761878.
106. Baixench MT,, Aoun N,, Desnos-Ollivier M,, Garcia-Hermoso D,, Bretagne S,, Ramires S,, Piketty C,, Dannaoui E. 2007. Acquired resistance to echinocandins in Candida albicans: case report and review. J Antimicrob Chemother 59:10761083.
107. Pfaller MA,, Castanheira M,, Lockhart SR,, Ahlquist AM,, Messer SA,, Jones RN. 2012. Frequency of decreased susceptibility and resistance to echinocandins among fluconazole-resistant bloodstream isolates of Candida glabrata. J Clin Microbiol 50:11991203.
108. Dowell JA,, Knebel W,, Ludden T,, Stogniew M,, Krause D,, Henkel T. 2004. Population pharmacokinetic analysis of anidulafungin, an echinocandin antifungal. J Clin Pharmacol 44:590598.
109. Hebert MF,, Smith HE,, Marbury TC,, Swan SK,, Smith WB,, Townsend RW,, Buell D,, Keirns J,, Bekersky I. 2005. Pharmacokinetics of micafungin in healthy volunteers, volunteers with moderate liver disease, and volunteers with renal dysfunction. J Clin Pharmacol 45:11451152.
110. Stone JA,, Holland SD,, Wickersham PJ,, Sterrett A,, Schwartz M,, Bonfiglio C,, Hesney,, Winchell GA,, Deutsch PJ,, Greenberg H,, Hunt TL,, Waldman SA. 2002. Single- and multiple-dose pharmacokinetics of caspofungin in healthy men. Antimicrob Agents Chemother 46:739745.
111. Balani SK,, Xu X,, Arison BH,, Silva MV,, Gries A,, DeLuna FA,, Cui D,, Kari PH,, Ly T,, Hop CE,, Singh R,, Wallace MA,, Dean DC,, Lin JH,, Pearson PG,, Baillie TA. 2000. Metabolites of caspofungin acetate, a potent antifungal agent, in human plasma and urine. Drug Metab Dispos 28:12741278.
112. Cross SA,, Scott LJ. 2008. Micafungin: a review of its use in adults for the treatment of invasive and oesophageal candidiasis, and as prophylaxis against Candida infections. Drugs 68:22252255.
113. Sandhu P,, Lee W,, Xu X,, Leake BF,, Yamazaki M,, Stone JA,, Lin JH,, Pearson PG,, Kim RB. 2005. Hepatic uptake of the novel antifungal agent caspofungin. Drug Metab Dispos 33:676682.
114. Stone JA,, Xu X,, Winchell GA,, Deutsch PJ,, Pearson PG,, Migoya EM,, Mistry GC,, Xi L,, Miller A,, Sandhu P,, Singh R,, deLuna F,, Dilzer SC,, Lasseter KC. 2004. Disposition of caspofungin: role of distribution in determining pharmacokinetics in plasma. Antimicrob Agents Chemother 48:815823.
115. Damle BD,, Dowell JA,, Walsky RL,, Weber GL,, Stogniew M,, Inskeep PB. 2009. In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin. Antimicrob Agents Chemother 53:11491156.
116. Benjamin DK,Jr,, Driscoll T,, Seibel NL,, Gonzalez CE,, Roden MM,, Kilaru R,, Clark K,, Dowell JA,, Schranz J,, Walsh TJ. 2006. Safety and pharmacokinetics of intravenous anidulafungin in children with neutropenia at high risk for invasive fungal infection. Antimicrob Agents Chemother 50:632638.
117. Seibel NL,, Schwartz C,, Arrieta A,, Flynn P,, Shad A,, Albano E,, Keirns J,, Lau WM,, Facklam DP,, Buell DN,, Walsh TJ. 2005. Safety, tolerability, and pharmacokinetics of micafungin (FK463) in febrile neutropenic pediatric patients. Antimicrob Agents Chemother 49:33173324.
118. Walsh TJ,, Adamson PC,, Seibel NL,, Flynn PM,, Neely MN,, Schwartz C,, Shad A,, Kaplan SL,, Roden MM,, Stone JA,, Miller A,, Bradshaw SK,, Li SX,, Sable CA,, Kartsonis NA. 2005. Pharmacokinetics, safety, and tolerability of caspofungin in children and adolescents. Antimicrob Agents Chemother 49:45364545.
119. Andes D,, Diekema DJ,, Pfaller MA,, Bohrmuller J,, Marchillo K,, Lepak A. 2010. In vivo comparison of the pharmacodynamic targets for echinocandin drugs against Candida species. Antimicrob Agents Chemother 54:24972506.
120. Baginski M,, Czub J. 2009. Amphotericin B and its new derivatives—mode of action. Curr Drug Metab 10:459469.
121. Sutton DA,, Sanche SE,, Revankar SG,, Fothergill AW,, Rinaldi MG. 1999. In vitro amphotericin B resistance in clinical isolates of Aspergillus terreus, with a head-to-head comparison to voriconazole. J Clin Microbiol 37:23432345.
122. Alcazar-Fuoli L,, Mellado E,, Alastruey-Izquierdo A,, Cuenca-Estrella M,, Rodriguez-Tudela JL. 2008. Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification. Antimicrob Agents Chemother 52:12441251.
123. Pfaller MA,, Messer SA,, Bolmström A. 1998. Evaluation of Etest for determining in vitro susceptibility of yeast isolates to amphotericin B. Diagn Microbiol Infect Dis 32:223227.
124. Sterling TR,, Merz WG. 1998. Resistance to amphotericin B: emerging clinical and microbiological patterns. Drug Resist Updat 1:161165.
125. Atkinson BJ,, Lewis RE,, Kontoyiannis DP. 2008. Candida lusitaniae fungemia in cancer patients: risk factors for amphotericin B failure and outcome. Med Mycol 46:541546.
126. Bekersky I,, Fielding RN,, Dressler DE,, Lee JW,, Buell DN,, Walsh TJ. 2002. Pharmacokinetics, excretion, and mass balance of liposomal amphotericin B (AmBisome) and amphotericin B deoxycholate in humans. Antimicrob Agents Chemother 46:828833.
127. Janknegt R,, de Marie S,, Bakker-Woudenberg LA,, Crommelin DJ. 1992. Liposomal and lipid formulations of amphotericin B. Clinical pharmacokinetics. Clin Pharmacokinet 23:279291.
128. Vogelsinger H,, Weiler S,, Djanani A,, Kountchev J,, Bellmann-Weiler R,, Wiedermann CJ,, Bellmann R. 2006. Amphotericin B tissue distribution in autopsy material after treatment with liposomal amphotericin B and amphotericin B colloidal dispersion. J Antimicrob Chemother 57:11531160.
129. Goodwin SD,, Cleary JD,, Walawander CA,, Taylor JW,, Grasela TH,Jr. 1995. Pretreatment regimens for adverse events related to infusion of amphotericin B. Clin Infect Dis 20:755761.
130. Wong-Beringer A,, Jacobs RA,, Guglielmo BJ. 1998. Lipid formulations of amphotericin B: clinical efficacy and toxicities. Clin Infect Dis 27:603618.
131. Barrett JP,, Vardulaki KA,, Conlon C,, Cooke J,, Daza-Ramirez P,, Evans EG,, Hawkey PM,, Herbrecht R,, Marks DI,, Moraleda JM,, Park GR,, Senn SJ,, Viscoli C; Amphotericin B Systematic Review Study Group. 2003. A systematic review of the antifungal effectiveness and tolerability of amphotericin B formulations. Clin Ther 25:12951320.
132. Pfaller MA,, Messer SA,, Boyken L,, Huynh H,, Hollis RJ,, Diekema DJ. 2002. In vitro activities of 5-fluorocytosine against 8,803 clinical isolates of Candida spp.: global assessment of primary resistance using National Committee for Clinical Laboratory Standards susceptibility testing methods. Antimicrob Agents Chemother 46:35183521.
133. Hospenthal DR,, Bennett JE. 1998. Flucytosine monotherapy for cryptococcosis. Clin Infect Dis 27:260264.
134. Vermes A,, Guchelaar HJ,, Dankert J. 2000. Flucytosine: A review of its pharmacology, clinical indications, pharmacokinetics, toxicity and drug interactions. J Antimicrob Chemother 46:171179.
135. Knasmüller S,, Parzefall W,, Helma C,, Kassie F,, Ecker S,, Schulte-Hermann R. 1997. Toxic effects of griseofulvin: disease models, mechanisms, and risk assessment. Crit Rev Toxicol, 27:495537.
136. Pasqualotto AC,, Thiele KO,, Goldani LZ. 2010. Novel triazole antifungal drugs: focus on isavuconazole, ravuconazole and albaconazole. Curr Opin Investig Drugs 11:165174.
137. Thompson GR,III,, Wiederhold NP. 2010. Isavuconazole: A comprehensive review of spectrum of activity of a new triazole. Mycopathologia 170:291313.
138. Livermore J,, Hope W. 2012. Evaluation of the pharmacokinetics and clinical utility of isavuconazole for treatment of invasive fungal infections. Expert Opin Drug Metab Toxicol 8:759765.
139. Thompson GR,III,, Wiederhold NP,, Sutton DA,, Fothergill A,, Patterson TF. 2009. In vitro activity of isavuconazole against Trichosporon, Rhodotorula, Geotrichum, Saccharomyces and Pichia species. J Antimicrob Chemother 64:7983.
140. Seifert H,, Aurbach U,, Stefanik D,, Cornely O. 2007. In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates. Antimicrob Agents Chemother 51:18181821.
141. Perkhofer S,, Lechner V,, Lass-Flörl C; European Committee on Antimicrobial Susceptibility Testing. 2009. In vitro activity of isavuconazole against Aspergillus species and zygomycetes according to the methodology of the European Committee on Antimicrobial Susceptibility Testing. Antimicrob Agents Chemother 53:6451647.
142. Sigurgeirsson B,, van Rossem K,, Malahias S,, Raterink K. 2013. A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis. J Am Acad Dermatol 69:416425.

Tables

Generic image for table
TABLE 1

Spectrum and extent of activity of commonly used systemic antifungal agents

Citation: Lockhart S, Warnock D. 2015. Antifungal Agents*, p 2223-2235. In Jorgensen J, Pfaller M, Carroll K, Funke G, Landry M, Richter S, Warnock D (ed), Manual of Clinical Microbiology, Eleventh Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817381.ch129

This is a required field
Please enter a valid email address
Please check the format of the address you have entered.
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error