Antifungal Drugs (antifungal + drug)

Distribution by Scientific Domains

Terms modified by Antifungal Drugs

  • antifungal drug resistance

  • Selected Abstracts


    ChemInform Abstract: 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: Synthesis and Biological Activity of a Novel Group of Potential Antifungal Drugs.

    CHEMINFORM, Issue 49 2001
    Milan Pour
    Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]


    Pharmacological properties and clinical efficacy of a recently licensed systemic antifungal, caspofungin

    MYCOSES, Issue 4 2005
    Georg Maschmeyer
    Summary Caspofungin, a semisynthetic derivative of the pneumocandin B0, is the first licensed compound of a new class of antifungal agents, the echinocandins. It attacks the fungal cell by selective inhibition of the beta-(1,3)- d -glucan synthase, which is not present in mammalian cells. In vitro studies have indicated a potent fungicidal effect on Candida species, and in vivo studies in immunocompromised animals with invasive candidiasis demonstrated a favourable outcome. In randomized clinical trials in patients with oropharyngeal/oesophageal and invasive candidiasis, caspofungin was at least as effective as amphotericin B deoxycholate, yet showed a significantly superior safety profile. Of patients with invasive aspergillosis refractory to or intolerant of other antifungal agents, 45% showed a partial or complete response to caspofungin given as a salvage treatment. Also, it demonstrated comparable clinical efficacy but superior tolerability in the empirical antifungal therapy in neutropenic patients compared with liposomal amphothericin B. Caspofungin has an excellent tolerability and a low potential for drug interactions. Thus, caspofungin represents an interesting and clinically valuable new antifungal drug that broadens the available therapeutic armamentarium for the treatment of invasive fungal infections. [source]


    Optimal prophylactic dosage and disposition of micafungin in living donor liver recipients

    CLINICAL TRANSPLANTATION, Issue 6 2004
    Satoshi Kishino
    Abstract:, Micafungin, a new candin antifungal drug, has a good safety profile and a significant therapeutic effect against Candida and Aspergillus. Little is known, however, about the optimal prophylactic dosage and the disposition of micafungin in liver transplant recipients, or about the effect of continuous venovenous hemodialysis (CVVH) on the pharmacokinetics of micafungin. Six living donor liver transplant patients were enrolled in this study. The mean Cmax and Cmin (trough) values of micafungin in plasma were 6.31 ± 1.08 and 1.65 ± 0.54 ,g/mL, respectively. The mean elimination half-life (t1/2) and mean area under the curve up to 12 h post-dosing (AUC 0,12 h) were 13.63 ± 2.77 h and 50.04 ± 6.48 ,g·h/mL, respectively. The concentrations of micafungin at the inlet and outlet of the dialyzer were very similar. The mean (±SD) ratio of micafungin concentrations at the inlet and outlet of the dialyzer (coutlet/cinlet) and the clearance of micafungin were 0.96 ± 0.04 and 0.054 ± 0.04 mL/min/kg, respectively. The amount in the ultrafiltrate was 1.0 mg. Micafungin effectively prevents systemic fungal infection in patients who have undergone liver transplantation. No significant differences were observed in the disposition of micafungin in recipients, and the therapeutic drug level can be achieved by administration of micafungin at a dosage of 40,50 mg/d. The CVVH had little effect on micafungin kinetics, and no dose adjustment or modification of dosing interval was needed during CVVH. [source]


    Exploring the Phospholipid Biosynthetic Pathways of Aspergillus fumigatus by Computational Genome Analysis

    ENGINEERING IN LIFE SCIENCES (ELECTRONIC), Issue 6 2005
    H. Do
    Abstract Aspergillus fumigatus causes a wide range of diseases that include mycotoxicosis, allergic reactions and systematic diseases (invasive aspergillosis) with high mortality rates. In recent years, considerable progress in the genome sequencing of this fungus has been made by an international consortium, which includes the Wellcome Trust Sanger Institute (UK) and the Institute for Genome Research (USA). A tenfold whole genome shotgun sequence assembly of A. fumigatus has been made publicly available. In this study, it was attempted to identify the genes related to the phospholipid biosynthesis from the A. fumigatus genome by a gene prediction program (GlimmerM) and to reconstruct the metabolic pathway for phospholipids of A. fumigatus. Fifteen genes related to phospholipid pathway were identified in the A. fumigatus genomic sequence. The open reading frames predicted by GlimmerM showed a high amino acid sequence similarity with the other fungal phospholipid biosynthetic genes and well-conserved functional domains. The obtained results also demonstrated that the reconstructed pathway of A. fumigatus in phospholipid biosynthesis was very similar to that of other fungi such as Saccharomyces cerevisiae, Schizosaccharomyces pombe, Candida albicans, and Neurospora crassa. Therefore it is postulated that the antifungal drugs targeted for the biosynthesis of phospholipids could also be effective against A. fumigatus. [source]


    Successful treatment of disseminated aspergillosis with the combination of voriconazole, caspofungin, granulocyte transfusions, and surgery followed by allogeneic blood stem cell transplantation in a patient with primary failure of an autologous stem cell graft

    EUROPEAN JOURNAL OF HAEMATOLOGY, Issue 5 2005
    Robert Dinser
    Abstract:, The treatment of disseminated aspergillus infections in neutropenic patients remains a major challenge in spite of several new antifungal drugs. We report the case of a patient with multiple myeloma in prolonged neutropenia after primary failure of an autologous stem cell graft who developed invasive aspergillosis despite voriconazole monotherapy. He responded to a combination of voriconazole and caspofungin, supported by granulocyte transfusions and surgery. A subsequent allogeneic peripheral blood stem cell transplantation did not lead to recurring aspergillus infection. The patient is well and free of clinical disease with respect to the fungal infection and myeloma more than 18 months after the allogeneic transplantation. [source]


    Predicting the emergence of resistance to antifungal drugs

    FEMS MICROBIOLOGY LETTERS, Issue 1 2001
    Leah E Cowen
    Abstract The emergence of antifungal drug resistance is inevitable. Here I discuss antibiotic resistance in the context of the adaptive potential of fungi and I propose an approach to predicting the evolution of antifungal resistance using experimental evolution of DNA sequences and microbial populations. Prediction is based on determination of evolutionary potential at two levels, the gene and the genome. At the level of the gene, evolutionary potential depends on the sequence space of candidate resistance genes defined by the fitness effects of all possible mutations in all possible combinations. At the level of the genome, evolutionary potential depends on the adaptive landscape defined by the fitness effects of all possible interactions among alleles constituting the genotype. [source]


    Topical antifungal drugs for the treatment of onychomycosis: an overview of current strategies for monotherapy and combination therapy

    JOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY & VENEREOLOGY, Issue 1 2005
    R Baran
    ABSTRACT Background, Onychomycosis is a relatively common disease accounting for up to 50% of all nail disorders and its prevalence rises with age. As onychomycosis is an important medical disorder affecting both patient's health and quality of life, it requires prompt and effective treatment. Objective, Topical antifungal nail lacquers have been formulated to provide efficient delivery to the nail unit. As both amorolfine and ciclopirox have proved useful as monotherapy for onychomycosis that does not involve the nail matrix area, the purpose of this article is to check if, when combined with oral agents, the effectiveness and scope of treatment can be improved further. Methods, Combining data for mycological cure with clinical success (nail morphology) provides a more exacting efficacy measure. Results, Clinical investigations have shown that the combination of oral therapies with antifungal nail lacquer can confer considerable advantage over monotherapy with either drug type. Conclusion, The improved effectiveness and economic advantages of combined topical/oral therapies benefit both patients and health providers; these treatment regimens therefore have an important role to play in the modern management of onychomycosis. [source]


    Non-invasive monitoring of commonly used intraocular drugs against endophthalmitis by raman spectroscopy

    LASERS IN SURGERY AND MEDICINE, Issue 4 2003
    K. Hosseini MD
    Abstract Purpose To develop a non-contact and non-invasive method for quantification of the local concentration of certain antibiotic and antifungal drugs in the eye. Study Design/Materials and Methods An integrated CCD-based Raman spectroscopic system designed specifically for ophthalmic applications was used to non-invasively detect the presence of ceftazidime and amphotericin B in ocular media. Specific Raman signatures of the above named drugs were determined for various concentrations that were injected through a needle in the aqueous humor of rabbit eyes in vivo. Raman spectra were subsequently acquired by focusing an argon laser beam within the anterior chamber of the eye. Results Compared to ocular tissue, unique spectral features of ceftazidime appeared near 1,028, 1,506, 1,586, and 1,641 cm,1. Amphotericin B exhibited its characteristic peaks at 1,156.5 and 1,556 cm,1. The amplitude of the spectral peak corresponding to these drugs (acquired by 1 second exposure time and 25 mW of laser power) were determined to be linearly dependent on their local concentration in the anterior chamber of the eye. Conclusions Raman spectroscopy may offer an effective tool to non-invasively assess the local concentration of the delivered drugs within the ocular media. This technique potentially could be used to investigate the pharmacokinetics of intraocular drugs in vivo either from a releasing implant or a direct injection. Lasers Surg. Med. 32:265,270, 2003. © 2003 Wiley-Liss, Inc. [source]


    The Cryptococcus neoformans MAP kinase Mpk1 regulates cell integrity in response to antifungal drugs and loss of calcineurin function

    MOLECULAR MICROBIOLOGY, Issue 5 2003
    Peter R. Kraus
    Summary Cell wall integrity is crucial for fungal growth, development and stress survival. In the model yeast Saccharomyces cerevisiae, the cell integrity Mpk1/Slt2 MAP kinase and calcineurin pathways monitor cell wall integrity and promote cell wall remodelling under stress conditions. We have identified the Cryptococcus neoformans homologue of the S. cerevisiae Mpk1/Slt2 MAP kinase and have characterized its role in the maintenance of cell integrity in response to elevated growth temperature and in the presence of cell wall synthesis inhibitors. C. neoformans Mpk1 is required for growth at 37°C in vitro, and this growth defect is suppressed by osmotic stabilization. C. neoformans mutants lacking Mpk1 are attenuated for virulence in the mouse model of cryptococcosis. Phosphorylation of Mpk1 is induced in response to perturbations of cell wall biosynthesis by the antifungal drugs nikkomycin Z (a chitin synthase inhibitor), caspofungin (a ,-1,3-glucan synthase inhibitor), or FK506 (a calcineurin inhibitor), and mutants lacking Mpk1 display enhanced sensitivity to nikkomycin Z and caspofungin. Lastly, we show that calcineurin and Mpk1 play complementing roles in regulating cell integrity in C. neoformans. Our studies demonstrate that pharmacological inhibition of the cell integrity pathway would enhance the activity of antifungal drugs that target the cell wall. [source]


    Oral yeast carriage in patients with advanced cancer

    MOLECULAR ORAL MICROBIOLOGY, Issue 2 2002
    A. N. Davies
    The aim of this study was to investigate oral yeast carriage amongst patients with advanced cancer. Oral rinse samples were obtained from 120 subjects. Yeasts were isolated using Sabouraud's dextrose agar and CHROMagarÔ Candida, and were identified using a combination of the API 20 C AUX yeast identification system, species-specific PCR and 26S rDNA gene sequencing. Oral yeast carriage was present in 66% of subjects. The frequency of isolation of individual species was: Candida albicans, 46%; Candida glabrata, 18%; Candida dubliniensis, 5%; others, <,5%. The increasing isolation of non- Candida albicans species is clinically important, since these species are often more resistant to antifungal drugs. Oral yeast carriage was associated with denture wearing (P = 0.006), and low stimulated whole salivary flow rate (P = 0.009). Identification of these risk factors offers new strategies for the prevention of oral candidosis in this group of patients. [source]


    Increase in aspergillosis and severe mycotic infection in patients with leukemia and MDS: Comparison of the data from the Annual of the Pathological Autopsy Cases in Japan in 1989, 1993 and 1997

    PATHOLOGY INTERNATIONAL, Issue 11 2003
    Hikaru Kume
    To study the relationship between the changes in visceral mycoses rates and recently advanced medical care in hematological settings, data on visceral mycosis cases with leukemia and myelodysplastic syndrome (MDS) that had been reported in the Annual of the Pathological Autopsy Cases in Japan in 1989, 1993 and 1997 were analyzed. The frequency rate of visceral mycoses with leukemia and MDS was 27.9% (435/1557) in 1989, 23.0% (319/1388) in 1993 and 22.3% (246/1105) in 1997. In comparing the rate of mycoses in recipients of organ or bone marrow transplantation with that of non-recipients, that of recipients was approximately 10% higher. The predominant causative agents were Candida and Aspergillus, at approximately the same rate as in 1989. The rate of candidosis decreased to one-half that of aspergillosis by 1993. Furthermore, severe mycotic infections clearly increased from 58.9% in 1989 to 75.6% in 1997. Among a total of 1000 cases with mycotic infection in those 3 years, acute lymphatic leukemia and acute myeloid leukemia were the major diseases (40.6% and 34.8%, respectively), followed by MDS (26.1%). The reasons for increased rates of aspergillosis and of severe mycotic infection can be surmised to be: (i) candidosis had become controllable by prophylaxis and by empiric therapy for mycoses with effective antifungal drugs; (ii) the marketed antifungal drugs were not sufficiently effective against severe infections or Aspergillus infections; and (iii) the number of patients surviving in an immunocompromised state had increased due to developments in chemotherapy and progress in medical care. [source]


    Influence of topical antifungal drugs on ciliary beat frequency of human nasal mucosa,

    THE LARYNGOSCOPE, Issue 7 2010
    An In Vitro Study
    Abstract Objectives/Hypothesis: Topical antifungal treatment is a subject of discussion in the treatment of chronic rhinosinusitis. The aim of this research was to study the effects of antifungal drugs on ciliary beat frequency (CBF) of human nasal mucosa under in vitro conditions. Study Design: Case series of in vitro experiments and in vitro study of cultured ciliated cells of human nasal mucosa. Methods: Human nasal mucosa was acquired during routine endoscopic sinus surgery. Cells were cultivated on object slides and exposed to different antifungal drugs in a newly developed test system. This system allowed continuous and reproducible exposure to different drugs at constant temperature, pH value, and osmolarity. The drugs were amphotericin B in two different concentrations and itraconazole. Results: Rinsing with higher concentrations of amphotericin B led to an immediate decrease of CBF, with a total stop after 15 minutes. A different result was seen in the group with lower concentrations; CBF decreased again quickly after rinsing with the test drug, but all of them recovered after rinsing with neutral solution. When using itraconazole a decline in CBF was observed again; one half of the samples returned to activity. Conclusions: Our in vitro results demonstrate a dose-dependent effect of the antifungal drugs amphotericin B and itraconazole on ciliary beat frequency of human nose epithelium. Laryngoscope, 2010 [source]


    Pharmacokinetic interaction of ketoconazole and itraconazole with ciprofloxacin

    BIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 1 2008
    Hisham S. Abou-Auda
    Abstract The effect of the concomitant administration of the antifungal drugs ketoconazole (KTC) and itraconazole (ITC) on the pharmacokinetics of ciprofloxacin (CIP) following short- and long-term administration in mice was investigated. Animals received either a dose of CIP (20,mg/kg, i.p.), CIP (20,mg/kg, i.p.) together with KTC (50,mg/kg, p.o.) or CIP (20,mg/kg, i.p.) and ITC (30,mg/kg, p.o.). The same treatments were repeated for 7 days. Blood samples were collected up to 4,h following drug administration and two urine samples were collected at 2,h and 4,h after drug administration. CIP plasma concentrations were significantly higher in KTC- and ITC-treated groups compared with the corresponding control groups. The concomitant administration of KTC or ITC with CIP also significantly (p<0.05) increased Cmax, t1/2, MRT and AUC0,, with no change in Tmax. CIP clearance was significantly reduced by both agents. KTC and ITC reduced CIP urinary excretion. This study suggests that an important pharmacokinetic interaction between CIP and KTC or ITC is likely to occur when either of the two antifungal drugs is administered concomitantly with CIP. The results may suggest possible reductions in total clearance of CIP, owing to inhibition of its renal tubular excretion by KTC and ITC. Copyright © 2007 John Wiley & Sons, Ltd. [source]


    The first case of cutaneous mucormycosis caused by Rhizopus azygosporus

    BRITISH JOURNAL OF DERMATOLOGY, Issue 2 2005
    A. Fujimoto
    Summary A rapidly enlarging leg ulcer appeared in a 54-year-old woman with systemic lupus erythematosus receiving aggressive immunosuppressive therapy. Skin biopsy revealed proliferation of hyphae in the midst of a neutrophilic abscess. Culture yielded Rhizopus azygosporus. As no organ involvement was detected by thorough examination, the patient was diagnosed as having primary cutaneous mucormycosis. Although intravenous amphotericin B therapy seemed to be very effective, it had to be discontinued due to nephrotoxicity. She unfortunately died of subsequent disseminated fungal infection and cerebral infarction in which the primary cause could not be determined. Minimum inhibitory concentrations of several antifungal drugs to the isolate were examined and amphotericin B proved to be the only agent that may potentially reach the effective plasma concentration. This is the first case report of cutaneous mucormycosis caused by R. azygosporus. [source]


    The future of onychomycosis therapy may involve a combination of approaches

    BRITISH JOURNAL OF DERMATOLOGY, Issue S60 2001
    R.J. Hay
    Onychomycosis is a fungal infection of the nail unit, most commonly caused by the anthropophilic dermatophyte fungi. It is generally accepted that this disease is increasing in prevalence despite the introduction of new and efficacious antifungal drugs. Several studies have documented health-related quality-of-life issues associated with onychomycosis and it is clear that patient treatment is both necessary and desirable. The aetiology and pathogenesis of onychomycosis is coming under increasing scrutiny and work in this field has grown substantially in recent years. This is reflected by the increased assurance with which clinicians can now prescribe treatment and be confident of improvement in a majority of their patients. However, a significant proportion of patients, perhaps as many as 25,40% of those encountered in clinical practice, are classified as treatment failures. Clinical indicators for poor prognosis include the development of residual foci of subungual fungal growth, onycholysis and severe disease. These observations have led to a resurgence of interest in combination treatments for use in patients at risk of failure/relapse. Several types of combination can be considered, including the use of oral or topical drugs and the concomitant use of surgical techniques, all of which have a place in the treatment of onychomycosis. [source]


    Neonatal liver abscesses due to Candida infection effectively treated with caspofungin

    ACTA PAEDIATRICA, Issue 5 2009
    Luca Filippi
    Abstract Candidiasis is relatively frequent in neonatal and pediatric intensive care units (ICUs), particularly in preterm infants less than 28 weeks of gestational age. Neonatal candidiasis shows high mortality and is often associated to poor neurodevelopmental prognosis in survivor patients. Amphotericin B and fluconazole are the first choice drugs for the treatment of neonatal candidiasis. Caspofungin is an alternative antifungal agent, which is recommended for invasive candidiasis in adults, but has been poorly experienced in neonates and infants as far as now. We report the first two infants with Candida liver abscesses treated with caspofungin. In the first infant bloodstream and liver lesions were cleared by combination therapy with fluconazole, liposomal amphotericin and caspofungin, while in the second one by caspofungin alone. Conclusion: Our observations confirm the efficacy and tolerability of caspofungin in the treatment of neonatal candidiasis refractory to conventional antifungal drugs. More extensive data are recommended in order to asses a specific neonatal schedule. [source]


    Determination of the absolute configuration and solution conformation of the antifungal agents ketoconazole, itraconazole, and miconazole with vibrational circular dichroism

    CHIRALITY, Issue S1 2005
    David Dunmire
    Abstract The absolute configuration assignments of three antifungal agents, (+)-(2R,4S)-ketoconazole, (+)-(2R,4S)-itraconazole (with (S)-configuration at the sec -butyl group) and (+)-(S)-miconazole nitrate have been confirmed by using vibrational circular dichroism (VCD). For these three antifungal drugs, this study also provides evidence for the most abundant conformations of miconazole and for the relative conformations of the azole, dichlorophenyl, and methoxyphenyl groups in ketoconazole and itraconazole, in chloroform solution. Chirality 17:S101,S108, 2005. © 2005 Wiley-Liss, Inc. [source]


    Drug interactions in dermatological practice

    CLINICAL & EXPERIMENTAL DERMATOLOGY, Issue 5 2008
    H. L. Tey
    Summary Systemic drugs are increasingly used in the treatment of dermatological diseases. Due to the high prevalence of polypharmacy, dermatologists are increasingly faced with the complex problem of drug interaction. Unlike adverse drug reactions, which are often unpredictable, drug interactions can be avoided. This article presents the significant drug interactions that are encountered in clinical practice, with the interactions categorized into those involving antimicrobials, immunosuppressants, antimalarials and colchicine, retinoids and psychiatric medications. There are few commonly used drugs that often cause drug interactions. These include ciclosporin, azole antifungal drugs, erythromycin, sulfonamides and rifampicin, and dermatologists should be alert whenever encountering them. A section on interactions of drugs with health supplements, herbs and food is also included, in view of the increasing use of alternative and complementary therapies in many parts of the world. [source]


    Clinical and microbiological assessment of patients with a long-term diagnosis of human immunodeficiency virus infection and Candida oral colonization

    CLINICAL MICROBIOLOGY AND INFECTION, Issue 4 2009
    A. C. D. Delgado
    Abstract The objective of this study was to evaluate Candida oral colonization in human immunodeficiency virus (HIV)-infected patients undergoing long-term highly active antiretroviral therapy (ARV). The cross-sectional study included 331 HIV patients, diagnosed from 1983 to 2003. Oral swabs were performed, and Candida species were determined using ID 32C. Isolates were tested for antifungal susceptibility. Clinical and laboratory data were collected to identify the association with Candida colonization. In total, 161 Candida isolates were detected among 147 of the 331 patients (44%), independently of the time when HIV infection was diagnosed. Candida albicans strains represented 137 (85%) of the isolates, and were susceptible to all of the tested antifungal drugs. Among the non- C. albicans strains, six isolates were dose-dependently susceptible to fluconazole, nine to itraconazole, and seven to ketoconazole. The isolation of Candida was significantly higher in patients with virological failure (83/147; p 0.0002) and CD4+ T-lymphocyte counts <200 cells/mm3 (30/83; p 0.0003). Recovery of Candida in the oral cavity was independent of protease inhibitor (PI) usage (p 0.60). Colonized patients typically underwent salvage therapy (p 0.003), and had more episodes of opportunistic fungal infections (p 0.046) and malignancies (p 0.004). Oral Candida colonization in patients under ARV therapy was associated with the immunosupressed status of HIV-infected patients, i.e. low number of CD4+ T-cells per cubic millimetre, failure of ARV therapy (salvage therapy), and higher number of opportunistic infections and malignancies. Despite the fact that PIs have in vitro antifungal activity, the use of this class of antiretroviral agent did not influence the presence of Candida in the oral cavity of AIDS patients. [source]


    Alternaria infections: laboratory diagnosis and relevant clinical features

    CLINICAL MICROBIOLOGY AND INFECTION, Issue 8 2008
    F. J. Pastor
    Abstract The genus Alternaria contains several species of melanized hyphomycetes that cause opportunistic human infections. The published literature contains 210 reported cases of human alternarioses between 1933 and the present day. The most frequent clinical manifestations are cutaneous and subcutaneous infections (74.3%), followed by oculomycosis (9.5%), invasive and non-invasive rhinosinusitis (8.1%) and onychomycosis (8.1%). Immunosuppression is frequently associated with cutaneous and subcutaneous infections and rhinosinusitis. The most important risk factors for cutaneous and subcutaneous infections are solid organ transplantation and Cushing's syndrome, and those for rhinosinusitis are bone marrow transplants. Having been exposed to soil and garbage is common in all cases of oculomycosis, with corticotherapy being a risk factor in 50% of these cases. Previous contact with soil and/or trauma to the nails is associated with most cases of onychomycosis. In general, alternariosis shows a good response to conventional antifungal drugs. On some occasions, steroid suppression or reduction is sufficient to resolve an infection. Itraconazole is the antifungal drug used most frequently to successfully treat onychomycosis and cutaneous and subcutaneous infections. Posaconazole and voriconazole are promising therapeutic options, with the latter being especially so for oculomycosis. [source]


    Therapeutic drug monitoring of itraconazole and the relevance of pharmacokinetic interactions

    CLINICAL MICROBIOLOGY AND INFECTION, Issue 2006
    A. Domínguez-Gil Hurlé
    Abstract A review of the pharmacological aspects of greatest relevance in relation to the monitoring of itraconazole serum levels is presented in this article. The main causes of pharmacokinetic variability, e.g., poor aqueous solubility, the presystemic first-pass effect with the involvement of transporters such as P-glycoprotein, the high extent of metabolism mediated by the CYP450 system and a high probability of pharmacological interactions, are documented and discussed. The pharmacokinetic,pharmacodynamic criteria used to optimise antibiotic therapy, as well as their application to antifungal drugs, are also discussed. Data concerning the breakpoints established for the minimum serum concentrations of itraconazole are included, and the most relevant justifications for drug monitoring are cited. [source]