Azoles

Andes, David R.; Dismukes, William E.

doi:10.1007/978-1-4419-6640-7_5

Cited by 3 publications

(2 citation statements)

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“…The oral solution should be given on an empty stomach; the capsules are given with food, and medications that decrease gastric acidity (antacids, histamine receptor blockers, proton pump inhibitors) must be avoided because gastric acid is needed for absorption. Therapeutic drug monitoring should be performed when giving itraconazole [ 42 ]. Serum levels should be obtained after steady state has been reached (usually about two weeks).…”

Section: Azole Treatment Of Endemic Mycoses In Transplant Recipienmentioning

confidence: 99%

“…The loading dose is 400 mg twice daily, and then 200 mg twice daily is recommended. However, the serum concentrations of voriconazole are highly variable and hard to predict [ 42 ]. Therefore, therapeutic drug monitoring is essential when using this agent, and should be done at steady state after about 5–7 days.…”

Section: Azole Treatment Of Endemic Mycoses In Transplant Recipienmentioning

confidence: 99%

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Histoplasmosis and Blastomycosis in Solid Organ Transplant Recipients

Kauffman

Miceli

2015

JoF

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Histoplasmosis and blastomycosis are geographically restricted dimorphic fungi that cause infection after the conidia produced in the mold phase are inhaled into the lungs. In the lungs, at 37 °C, these organisms undergo transformation into the yeast phase. In transplant recipients, infection can occur by exposure to the mold in the environment, by reactivation of infection that had occurred previously and had been controlled by the host until immunosuppressive medications were given post-transplantation, and finally by transmission from the donor organ in the case of histoplasmosis. In transplant recipients, disseminated infection is common, and pulmonary infection is more likely to be severe than in a non-immunosuppressed person. Diagnosis has been improved, allowing earlier treatment, with the use of rapid antigen tests performed on serum and urine. Initial treatment, for all but the mildest cases of acute pulmonary histoplasmosis, should be with a lipid formulation of amphotericin B. After clinical improvement has occurred, step-down therapy with itraconazole is recommended for a total of 12 months for most transplant recipients, but some patients will require long-term suppressive therapy to prevent relapse of disease.

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Section: Azole Treatment Of Endemic Mycoses In Transplant Recipienmentioning

confidence: 99%

Section: Azole Treatment Of Endemic Mycoses In Transplant Recipienmentioning

confidence: 99%

Histoplasmosis and Blastomycosis in Solid Organ Transplant Recipients

Kauffman

Miceli

2015

JoF

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Aspergillus fumigatus Cross-Resistance between Clinical and Demethylase Inhibitor Azole Drugs

Garcia-Rubio

González-Jiménez

Lúcio

et al. 2021

Appl Environ Microbiol

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Drug resistance poses a serious threat to human health and agricultural production. Azole drugs are the largest group of 14-α sterol demethylation inhibitor fungicides that are used both in agriculture and in clinical practice. As plant pathogenic molds share their natural environment with fungi that cause opportunistic infections in humans, both are exposed to a strong and persistent pressure of demethylase inhibitor (DMI) fungicides, including imidazole and triazole drugs. As a result, a loss of efficacy has occurred for this drug class in several species. In the clinical setting, Aspergillus fumigatus azole resistance is a growing public health problem and finding the source of this resistance has gained much attention. It is urgent to determine if there is a direct link between the agricultural use of azole compounds and the different A. fumigatus resistance mechanisms described for clinical triazoles. In this work we have performed A. fumigatus susceptibility testing to clinical triazoles and crop protection DMIs using a collection of azole susceptible and resistant strains which harbor most of the described azole resistance mechanisms. Various DMI susceptibility profiles have been found in the different A. fumigatus populations groups based on their azole resistance mechanism and previous WGS analysis, which suggests that the different resistance mechanisms have different origins and are specifically associated to the local use of a particular DMI.Importance Due to the worldwide emergence of A. fumigatus azole resistance, this opportunistic pathogen poses a serious health threat and, therefore, it has been included in the Watch List of the CDC 2019 Antimicrobial Resistance Threats Report. Azoles play a critical role in the control and management of fungal diseases, not only in the clinical setting but also in agriculture. Thus, azole resistance leads to a limited therapeutic arsenal which reduces the treatment options for aspergillosis patients, increasing their mortality risk. Evidence is needed to understand whether A. fumigatus azole resistance is emerging from an agricultural source due to the extended use of demethylase inhibitors as fungicides, or whether it is coming from somewhere else such as the clinical setting. If the environmental route is demonstrated, the current use and management of azole antifungal compounds might be forced to change in the forthcoming years.

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New Antifungal Agents with Azole Moieties

et al. 2022

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Fungal conditions affect a multitude of people worldwide, leading to increased hospitalization and mortality rates, and the need for novel antifungals is emerging with the rise of resistance and immunocompromised patients. Continuous use of azole drugs, which act by inhibiting the fungal CYP51, involved in the synthesis of ergosterol, essential to the fungal cell membrane, has enhanced the resistance and tolerance of some fungal strains to treatment, thereby limiting the arsenal of available drugs. The goal of this review is to gather literature information on new promising azole developments in clinical trials, with in vitro and in vivo results against fungal strains, and complementary assays, such as toxicity, susceptibility assays, docking studies, among others. Several molecules are reviewed as novel azole structures in clinical trials and with recent/imminent approvals, as well as other innovative molecules with promising antifungal activity. Structure–activity relationship (SAR) studies are displayed whenever possible. The azole moiety is brought over as a privileged structure, with multiple different compounds emerging with distinct pharmacophores and SAR. Particularly, 1,2,3-triazole natural product conjugates emerged in the last years, presenting promising antifungal activity and a broad spectrum against various fungi.

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Azoles

Cited by 3 publications

References 356 publications

Histoplasmosis and Blastomycosis in Solid Organ Transplant Recipients

Histoplasmosis and Blastomycosis in Solid Organ Transplant Recipients

Aspergillus fumigatus Cross-Resistance between Clinical and Demethylase Inhibitor Azole Drugs

New Antifungal Agents with Azole Moieties

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