1887

Chapter 52 : Systemic 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

Systemic Antifungal Agents, Page 1 of 2

| /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap52-1.gif /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap52-2.gif

Abstract:

Schematically, the current systemic antifungal agents can be divided into two categories: that of the antifungal antibiotics, which include griseofulvin and amphotericin B (AMB), and that of the chemical agents, which comprise all of the other molecules, flucytosine (5FC), the extremely rich series of azoles and, more recently, the allylamines and echinocandins. Given their value in the treatment of systemic mycoses, the authors discuss the three systemic azoles currently commercially available in parallel with voriconazole, which is currently available under an authorization for compassionate use, and conclude with the most recent triazoles under development. The azole compounds possess a relatively broad spectrum against numerous pathogenic or opportunistic fungal species, a spectrum that is exceeded only by that of AMB. Although all of these derivatives share good activity against some of these fungi (such as , , and dimorphic fungi), major differences have been found in vitro and subsequently confirmed in animals and in clinical trials. Despite the considerable advances in antifungal therapy over the last few years, we are still far from possessing the ideal antifungal and progress is still necessary. Fungal infections remain a matter of concern, particularly in severe neutropenia (frequent inefficacy in disseminated mycoses) and AIDS (frequency of relapses and/or resistance in oroesophageal candidosis and cryptococcosis).

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52

Key Concept Ranking

Fungal Cell Structure
1.3798164
Fungal Proteins
1.1235555
Fungal Infections
1.0588616
Antifungal Agents
1.0300543
Ergosterol Inhibitors
0.73030794
1.3798164
Highlighted Text: Show | Hide
Loading full text...

Full text loading...

Figures

Image of Figure 1
Figure 1

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 2
Figure 2

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 3
Figure 3

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 4
Figure 4

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 5
Figure 5

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 6
Figure 6

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 7
Figure 7

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 8
Figure 8

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 9
Figure 9

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint
Image of Figure 10
Figure 10

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Permissions and Reprints Request Permissions
Download as Powerpoint

References

/content/book/10.1128/9781555815929.ch52
1. Albengres E,, Le, Louet H,, Tillement JP, 1998, Systemic antifungal agents, drug interactions of clinical significance, Drug Saf, 18, 8397.
2. Anaissie E,, Paetznick V,, Proffitt R,, Adler-Moore J,, Bodey GP, 1991, Comparison of the in vitro antifungal activity of free and liposome-encapsulated amphotericin B, Eur J Clin Microbiol Infect Dis, 10, 665668.
3. Andrès E,, Tiphine M,, Letscher-Bru V,, Herbrecht R, 2001, Nouvelles formes lipidiques de l’amphotéricine B, revue de la littérature, Rev Méd Interne, 22, 141150.
4. Bodey GP, 1992, Azole antifungal agents, Clin Infect Dis, 14, Suppl 1, S161S169.
5. Bolard J, 1986, How do the polyene macrolide antibiotics affect the cellular membrane properties? Biochim Biophys Acta, 864, 257304.
6. Bolard J, 1991, Mechanism of action of an anti-Candida drug, amphotericin B and its derivatives, p214238, in Prasad R, ed, Candida albicans, Cellular and Molecular Biology, Springer Verlag.
7. Bonaly R, 1977, La griséofulvine, mode d’action et cinétique, CR Entretiens de Mycologie Fondamentale et Appliquée, CHR Hôpital Jeanne d’Arc, Dommartin les Toul, 17 November 1977.
8. Brajtburg J,, Powderly WG,, Kobayashi GS,, Medoff G, 1990, Amphotericin B, current understanding of mechanisms of action, Antimicrob Agents Chemother, 34, 183188.
9. Chandrasekar PH,, Manavathu E, 2001, Voriconazole, a second-generation triazole, Drugs of Today, 37, 135148.
10. Chiller T,, Stevens DA, 2000, Treatment strategies for Aspergillus infections, Drug Resistance Updates, 3, 8997.
11. Dellamonica P, 1989, Réflexions sur la 5-fluorocytosine, La Lettre de l’Infectiologue, 4, 598599.
12. Denning DW,, Stevens DA, 1990, Antifungal and surgical treatment of invasive aspergillosis, review of 2,121 published cases, Rev Infect Dis, 12, 11471201.
13. Dodds ES,, Drew RH,, Perfect JR, 2000, Antifungal pharmacodynamics, review of literature and clinical applications, pharmacotherapy, 20, 13351355.
14. Drouhet E,, Dupont B, 1988, Antifongiques, p 17381760, in Giroud JP,, Mathe G,, Meyniel G, ed, Pharmacologie clinique, bases de la thérapeutique, 2nd ed, Expansion Scientifique Française, Paris.
15. Dupont B,, Drouhet E, 1990, Antifongiques, Editions Techniques Encycl Méd Chir, Maladies infectieuses, 8004 M10, p915.
16. Dykewicz C, 2001, Summary of the Guidelines for Preventing Opportunistic Infections among Hematopoietic Stem Cell Transplant Recipients, Clin Infect Dis, 33, 139144.
17. Gallis HA,, Drew RH,, Pickard WW, 1990, Amphotericin B, 30 years of clinical experience, Rev Infect Dis, 12, 308329.
18. Goa KL,, Barradell LB, 1995, Fluconazole, an update of its pharmacodynamic and pharmacokinetic properties and therapeutic use in major superficial and systemic mycoses in immunocompromised patients, Drugs, 50, 658690.
19. Goldman RC,, Frost DJ,, Capobianco JO,, Kadam S,, Rasmussen RR,, Abad-Zapatero C, 1995, Antifungal drug targets: Candida secreted aspartyl protease and fungal wall β-glucan synthesis, Inf Agents Dis, 4, 228247.
20. Grant SM,, Clissold SP, 1990, Fluconazole, a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in superficial and systemic mycoses, Drugs, 39, 877916.
21. Graybill JR, 1989, New antifungal agents, Eur J Clin Microbiol Infect Dis, 8, 402412.
22. Graybill JR, 1992, Future directions of antifungal chemotherapy, Clin Infect Dis, 14 (Suppl 1), S170S181.
23. Hoang A, 2001, Caspofungin acetate, an antifungal agent, Am J Health-Sys Pharm, 58, 12061214.
24. Hood S,, Denning DW, 1997, Treatment of fungal infection in AIDS, J Antimicrob Chemother, 37, suppl B, 7185.
25. Hughes WT,, Armstrong D,, Bodey GP,, Brown AE,, Edwards JE,, Feld R,, Pizzo P,, Rolston VI,, Shenep JL,, Young LS, 1997, Guidelines from the Infectious Diseases Society of America, Clin Infect Dis, 25, 551573.
26. Iwata K,, Vanden, Bossche H, 1986, In vitro and in vivo evaluation of antifungal agents, Elsevier Science Publishers BV, Amsterdam.
27. Jensen GM, 1998, 38th Intersci Conf Antimicrob Agents Chemother.
28. Joly V,, Saint-Julien L,, Carbon C,, Yeni P, 1990, Interactions of free and liposomal amphotericin B with renal tubular cells in primary culture, J Pharmacol Exp Ther, 255, 1722.
29. Klepser ME, 2001, Antifungal resistance among Candida species, Pharmacotherapy, 21, 124S132S.
30. Kobayashi GS,, Odds FC, 1989, Current perspectives on antifungal susceptibility testing, focus on fluconazole, p 26, Pfizer Monograph, Scientific Therapeutic Information, Inc., New Jersey.
31. Kontoyiannis DP, 2001, A clinical perspective for the management of invasive fungal infections, Focus on IDSA guidelines, Pharmacotherapy, 21, 175S187S.
32. Lortholary O,, Dupont B, 1997, Apport des antifongiques azolés dans la prophylaxie des infections fongiques, Ann Med Interne, 3, 258267.
33. Meyer RD, 1992, Current role of therapy with amphotericin B, Clin Infect Dis, 14 (Suppl 1), S154S160.
34. Neely MN,, Ghannoum MA, 2000, The exciting future of antifungal therapy, Eur J Clin Microbiol Infect Dis, 19, 897914.
35. Odds FC, 1988, Antifungal agents and their use in Candida infections, p 279313, in Candida and Candidosis, a Review and Bibliography, 2nd ed, Baillière Tindall, London.
36. Patterson BE,, Coates PE, 1995, UK 109496, a novel wide-spectrum triazole derivative for the treatment of fungal infection, pharmacokinetics in man, 35th Intersci Conf Antimicrob Agents Chemother, abstract F-78.
37. Patterson TF, 1999, Role of newer azoles in surgical patients, J Chemother, 11, 504512.
38. Polak A, 1998, The past, present and future of antimycotic combination therapy, Mycoses, 42, 355370.
39. Polak A,, Scholer HJ, 1980, Mode of action of 5-fluorocytosine, Rev Institut Pasteur Lyon, 13, 233244.
40. Powderly WG,, Kobayashi GS,, Herzig GP,, Medoff G, 1988, Amphotericin B-resistant yeast infection in severely immunocom-promised patients, Am J Med, 84, 826832.
41. Prentice HG,, Hann IM,, Herbrecht R,, Aoun M,, Kvaloy S,, Catovsky D,, Pinkerton CR,, Schey SA,, Jacobs F,, Oakhill A,, Stevens RF,, Darbyshire PJ,, Gibson BE, 1997, A randomized comparison of liposomal versus conventional amphotericin B for treatment of pyrexia of unknown origin in neutropenic patients, Br J Haematol, 98, 711718.
42. Rex JH,, Walsh TJ,, Sobel JD,, Filler SG,, Pappas PG,, Dismukes WE,, Edwards JE, 2000, Practice guidelines for the treatment of candidiasis, Clin Infect Dis, 30, 662678.
43. Rosa FW,, Hernandez C,, Carlo WA, 1987, Griseofulvin teratology, including two thoracopagus conjoined twins, Lancet, i, 171.
44. Saag MS,, Graybill RJ,, Larsen RA,, Pappas PG,, Perfect JR,, Powderly WG,, Sobel JD, Dismukes WE for the Mycoses Study Group Cryptococcal Subproject, 2000, Practice guidelines for the management of cryptococcal disease, Clin Infect Dis, 30, 710718.
45. Smith KJ,, Warnock DW,, Kennedy CTC,, Johnson EM,, Hopwood V,, Van Cutsem J,, Vanden Bossche H, 1986, Azole resistance in Candida albicans, J Med Vet Mycol, 24, 133144.
46. Stevens DA,, Kan VL,, Judson MA,, Morrison VA,, Dummer S,, Denning DW,, Bennett JE,, Walsh TJ,, Patterson TF,, Pankey GA, 2000, Practice guidelines for diseases caused by Aspergillus, Clin Infect Dis, 30, 696709.
47. Storm G,, van, Etten E, 1997, Biopharmaceutical aspects of lipid formulations of amphotericin B, Eur J Clin Microbiol Dis, 16, 6473.
48. Vanden Bossche H, 1991, Ergosterol biosynthesis inhibitors, in Prasad R, ed, Candida albicans, Springer-Verlag, Berlin.
49. Vanden Bossche H,, Mackenzie DW,, Cauwenbergh G,, Van Cutsem J,, Drouhet E,, Dupont B, 1990, Mycoses in AIDS patients, Plenum Press, New York.
50. Van Tyle HJ, 1984, Ketoconazole, mechanism of action, spectrum of activity, pharmacokinetics, drug interactions, adverse reactions and therapeutic use, Pharmacotherapy, 4, 343373.
51. Walsh TJ,, Finberg RW,, Arndt C,, Hiezmez J,, Schwartz C,, Bodensteiner D,, et al, 1999, Liposomal amphotericin B for empirical therapy in patients with persistent fever and neutropenia, National Institute of Allergy and Infectious Diseases Mycoses Study Group, N Engl J Med, 340, 764771.
52. Walsh TJ,, Pizzo A, 1988, Treatment of systemic fungal infections, recent progress and current problems, Eur J Clin Microbiol Infect Dis, 7, 460475.
53. Warnock DW, 1998, Fungal infections in neutropenia, current problems and chemotherapeutic control, J Antimicrob Chemother, 41, suppl D, 95105.
54. White TC,, Marr KA,, Bowden RA, 1998, Clinical, cellular and molecular factors that contribute to antifungal drug resistance, Clin Microbiol Rev, 11, 382402.

Tables

Generic image for table
Table 1

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 2

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 3

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 4

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 5

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 6

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 7

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 8

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 9

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 10

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 11

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 12

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 13

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 14

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 15

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 16

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 17

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52
Generic image for table
Table 18

Citation: Grillot R, Lebeau B. 2005. Systemic Antifungal Agents, p 1260-1287. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch52

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