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Itraconazole

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https://www.readbyqxmd.com/read/29346584/in-vitro-interactions-between-iap-antagonist-at406-and-azoles-against-planktonic-cells-and-biofilms-of-pathogenic-fungi-candida-albicans-and-exophiala-dermatitidis
#1
Yi Sun, Lujuan Gao, Chengyan He, Ming Li, Tongxiang Zeng
In vitro interactions of AT406, a novel IAP antagonist, and azoles including itraconazole, voriconazole, and fluconazole against planktonic cells and biofilms of Candida albicans and Exophiala dermatitidis were assessed via broth microdilution checkerboard technique. AT406 alone exhibited limited antifungal activity. However, synergistic effect between AT406 and fluconazole was observed against both planktonic cells and biofilms of C. albicans, including one fluconazole-resistant strain. Moreover, synergism was also demonstrated between AT406 and itraconazole against both planktonic cells and biofilms of E...
January 13, 2018: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/29346384/histoplasmosis-in-africa-an-emerging-or-a-neglected-disease
#2
REVIEW
Rita O Oladele, Olusola O Ayanlowo, Malcolm D Richardson, David W Denning
Histoplasmosis in Africa has markedly increased since the advent of the HIV/AIDS epidemic but is under-recognised. Pulmonary histoplasmosis may be misdiagnosed as tuberculosis (TB). In the last six decades (1952-2017), 470 cases of histoplasmosis have been reported. HIV-infected patients accounted for 38% (178) of the cases. West Africa had the highest number of recorded cases with 179; the majority (162 cases) were caused by Histoplasma capsulatum var. dubuosii (Hcd). From the Southern African region, 150 cases have been reported, and the majority (119) were caused by H...
January 2018: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29345955/investigation-of-polymer-surfactant-interactions-and-their-impact-on-itraconazole-solubility-and-precipitation-kinetics-for-developing-spray-dried-amorphous-solid-dispersions
#3
Tanvi Mahesh Deshpande, Helen Shi, John Pietryka, Stephen W Hoag, Ales Medek
Methods were developed to systematically screen different polymer-surfactant combinations for the purpose of enhancing amorphous active pharmaceutical ingredient (API) solubility while maintaining its physical stability. Itraconazole (ITZ) was chosen as the model API mostly due to its low aqueous solubility. Special attention was paid to determine the effect of a reduction in the critical micelle concentration (CMC) by specific polymer/surfactant combinations on the ITZ solubility and physical stability. However, only a slight correlation was actually found...
January 18, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29341245/pharmacokinetic-pharmacodynamic-drug-drug-interactions-of-avatrombopag-when-co-administered-with-dual-or-selective-cyp2c9-and-cyp3a-interacting-drugs
#4
Maiko Nomoto, Cynthia A Zamora, Edgar Schuck, Peter Boyd, Min-Kun Chang, Jagadeesh Aluri, Y Amy Siu, W George Lai, Sanae Yasuda, Jim Ferry, Bhaskar Rege
AIMS: Avatrombopag, a thrombopoietin receptor agonist, is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A. We assessed three drug-drug interactions of avatrombopag as a victim with dual or selective CYP2C9/3A inhibitors and inducers. METHODS: This was a 3-part, open-label study. Forty-eight healthy subjects received single 20 mg doses of avatrombopag alone or with one of 3 CYP2C9/3A inhibitors or inducers: fluconazole 400 mg once daily for 16 days, itraconazole 200 mg twice daily on Day 1 and 200 mg once daily on Days 2-16, or rifampin 600 mg once daily for 16 days...
January 16, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29340465/variability-in-the-clinical-distributions-of-candida-species-and-the-emergence-of-azole-resistant-non-candida-albicans-species-in-public-hospitals-in-the-midwest-region-of-brazil
#5
Karine Mattos, Luana Carbonera Rodrigues, Kelly Mari Pires de Oliveira, Pedro Fernando Diniz, Luiza Inahê Marques, Adriana Almeida Araujo, Marilene Rodrigues Chang
INTRODUCTION: Incidence and antifungal susceptibility of Candida spp. from two teaching public hospitals are described. METHODS: The minimum inhibitory concentrations of fluconazole, voriconazole, itraconazole, and amphotericin B were determined using Clinical Laboratory Standard Institute broth microdilution and genomic differentiation using PCR. RESULTS: Of 221 Candida isolates, 50.2% were obtained from intensive care unit patients; 71.5% were recovered from urine and 9...
November 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/29331473/a-randomized-trial-of-itraconazole-versus-prednisolone-in-acute-stage-abpa-complicating-asthma
#6
Ritesh Agarwal, Sahajal Dhooria, Inderpaul Singh Sehgal, Ashutosh N Aggarwal, Mandeep Garg, Biman Saikia, Digambar Behera, Arunaloke Chakrabarti
BACKGROUND AND AIMS: Whether itraconazole monotherapy is effective in the acute-stage of allergic bronchopulmonary aspergillosis (ABPA) remains unknown. Herein, we compare the efficacy and safety of itraconazole and prednisolone monotherapy in ABPA. METHODS: We randomized treatment-naïve subjects with ABPA complicating asthma (January 2012 to December 2013) to receive either oral itraconazole or prednisolone for four months. The study was not blinded. The primary outcomes were proportion of subjects showing composite response after six weeks, percentage decline in IgE after treatment, and numbers of subjects experiencing exacerbation...
January 10, 2018: Chest
https://www.readbyqxmd.com/read/29330782/characterization-of-the-pharmacokinetics-of-vilaprisan-bioavailability-excretion-biotransformation-and-drug-drug-interaction-potential
#7
Marcus-Hillert Schultze-Mosgau, Joachim Höchel, Olaf Prien, Torsten Zimmermann, Ashley Brooks, Jim Bush, Antje Rottmann
BACKGROUND AND OBJECTIVES: In-vitro data suggest that clearance of vilaprisan is mediated by cytochrome P450 3A4 (oxidation) and aldoketoreductases (reduction). To fully understand the elimination and biotransformation pathways of vilaprisan, a selective progesterone receptor modulator, and to quantify the impact of cytochrome P450 3A4 inhibition on the pharmacokinetics of vilaprisan, two clinical studies in healthy postmenopausal women were conducted. METHODS: In study 1, pharmacokinetics, mass balance, and metabolite patterns were determined after single oral administration of 5 mg of [14C]-labeled vilaprisan in six subjects...
January 12, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29330133/the-evaluation-of-drug-induced-changes-in-left-ventricular-function-in-pentobarbital-anesthetized-dogs
#8
Yevgeniya E Koshman, Brett R Herzberg, Terese R Seifert, James S Polakowski, Scott W Mittelstadt
INTRODUCTION: The goal of this study was to determine whether assessment of myocardial contractility and hemodynamics in an anesthetized dog model, could consistently detect drug-induced changes in the inotropic state of the heart using drugs known to have clinically relevant positive and negative effects on myocardial contractility. METHODS: Derived parameters included: diastolic, systolic and mean arterial BP, peak systolic LVP, HR, end-diastolic LVP, and LVdP/dtmax as the primary contractility index...
January 9, 2018: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/29327700/disseminated-cutaneous-fusariosis-in-human-immunodeficiency-virus-infected-patient-and-dramatic-response-with-oral-itraconazole
#9
Indu Kumari, Satyendra Kumar Singh, Rishabh Kumar Chauhan, Satyendra Kumar Kaushal
Fusarium species are known to cause disseminated cutaneous lesions in immunocompromised patients. Some cases of fusariosis are reported in patients infected with the human immunodeficiency virus. There are two reports in such patients with systemic comorbidities like lymphoma, neutropenia and infective port-a-catheter. Another reported patient had systemic fusariosis, without skin involvement. Diagnosis and treatment of cutaneous fusariosis is difficult and resistance to antifungals is a problem. Our patient was at an advanced human immunodeficiency virus infection stage with disseminated cutaneous fusariosis, without any systemic involvement, who responded completely to oral itraconazole...
January 9, 2018: Indian Journal of Dermatology, Venereology and Leprology
https://www.readbyqxmd.com/read/29325818/simultaneous-determination-of-voriconazole-posaconazole-itraconazole-and-hydroxy-itraconazole-in-human-plasma-using-lcms-ms
#10
Nicole Jenkins, Marion Black, Hans G Schneider
INTRODUCTION: Invasive fungal infections are an increasing cause of mortality and morbidity in high risk patient populations such as those on immunosuppressive therapy. Triazole antifungals are recommended for the prevention and treatment of such infections. The aim of this study was to develop and validate a simple, sensitive and robust LCMS/MS method for the simultaneous analysis in human plasma of three frequently used antifungal drugs: voriconazole, posaconazole, and itraconazole...
January 8, 2018: Clinical Biochemistry
https://www.readbyqxmd.com/read/29324336/new-1-5-and-2-5-disubstituted-tetrazoles-dependent-activity-towards-surface-barrier-of-candida-albicans
#11
Monika Staniszewska, Małgorzata Gizińska, Ewa Mikulak, Klaudia Adamus, Mirosława Koronkiewicz, Edyta Łukowska-Chojnacka
A series of novel tetrazole derivatives was synthetized using N-alkylation or Michael-type addition reactions, and screened for their fungistatic potential against Candida albicans (the lack of endpoint = 100%). Among them, the selected compounds 2d, 4b, and 6a differing in substituents at the tetrazole ring were non-toxic to Galleria mellonella larvae in vivo and exerted slight toxicity against Caco-2 in vitro (CC50 at 256 μg/mL). An antagonistic effect of tetrazole derivatives 2d, 4b, and 6a respectively in combination with Fluconazole was shown using the checker board and colorimetric methods (fractional inhibitory concentration indexes FICIs >1)...
December 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29320899/in-vitro-analysis-of-itraconazole-cis-diastereoisomers-inhibition-of-nine-cytochrome-p450-enzymes-stereoselective-inhibition-of-cyp3a
#12
Kristyna Krasulova, Zdenek Dvorak, Pavel Anzenbacher
Itraconazole (ITZ), an antifungal azole derivate is a chiral drug that consists of four cis-diastereoisomers ((+)-2R,4S,2'R-ITZ-A; (+)-2R,4S,2'S-ITZ-B; (-)2S,4R,2'S-ITZ-C and (-) 2S,4R,2'R-ITZ-D) which may differ in their pharmacokinetics and pharmacodynamics. As itraconazole is known as a CYP3A4 inhibitor causing severe drug-drug interaction, the inhibitory potencies of its individual optical isomers towards nine drug-metabolising cytochrome P450 (including CYP3A, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP2E1), were investigated...
January 10, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29319446/comparison-of-absorption-characteristics-of-oral-reference-and-compounded-itraconazole-formulations-in-healthy-cats
#13
Dianne I Mawby, Jacqueline C Whittemore, Leanne E Fowler, Mark G Papich
OBJECTIVE To compare absorption characteristics of orally administered compounded itraconazole capsules and suspension with those of reference (brand-name) formulations in healthy cats. DESIGN Randomized crossover study. ANIMALS 8 healthy adult cats. PROCEDURES After 12 hours of food withholding, cats received 50 mg of itraconazole (reference capsule, reference solution, compounded capsule, and compounded suspension) in a randomized crossover design, with a 21-day washout period. Capsules were administered with a small meal...
January 15, 2018: Journal of the American Veterinary Medical Association
https://www.readbyqxmd.com/read/29319442/clinical-signs-treatment-and-prognostic-factors-for-dogs-with-histoplasmosis
#14
Allison G Wilson, Kate S KuKanich, Andrew S Hanzlicek, Mark E Payton
OBJECTIVE To determine the clinical manifestations of histoplasmosis in a large sample of dogs, compare outcomes achieved with fluconazole versus itraconazole, and identify variables available at the time of diagnosis with prognostic value. DESIGN Retrospective case series with nested cohort study. ANIMALS 79 dogs with confirmed histoplasmosis evaluated at 2 veterinary teaching hospitals from 1999 through 2015. PROCEDURES Medical records were reviewed and data extracted regarding clinical signs at evaluation, physical examination findings, clinical laboratory values, other diagnostic test results, treatments, and outcomes...
January 15, 2018: Journal of the American Veterinary Medical Association
https://www.readbyqxmd.com/read/29311090/investigation-of-multiple-resistance-mechanisms-in-voriconazole-resistant-aspergillus-flavus-clinical-isolates-from-a-chest-hospital-surveillance-in-delhi-india
#15
Cheshta Sharma, Rakesh Kumar, Nitin Kumar, Aradhana Masih, Dinesh Gupta, Anuradha Chowdhary
Invasive and allergic infections by Aspergillus flavus are more common in tropical and subtropical countries. The emergence of voriconazole (VRC) resistance in A. flavus impacts the management of aspergillosis as azoles are used as the first line and empiric therapy. We screened molecularly confirmed 120 A. flavus isolates obtained from respiratory and sino-nasal specimens in a chest hospital in Delhi for azole resistance using CLSI BMD method. Overall, 2.5% (n=3/120) of A. flavus isolates had VRC MICs above epidemiological cutoff values (>1μg/ml)...
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29310381/primary-cutaneous-aspergillosis-caused-by-aspergillus-fumigatus-in-an-immunocompetent-patient-a-case-report
#16
Xiaoyan Liu, Jun Yang, Weiyuan Ma
RATIONALE: Primary cutaneous aspergillosis in immunocompromised patients has been well described in extensive investigations. However, in immunocompetent hosts, primary cutaneous infection of aspergillus occurs rarely, and remains poorly characterized. PATIENT CONCERNS: We present a case of primary cutaneous aspergillosis manifested by erythematous plague covered with flava eschar. DIAGNOSES: The patient was diagnosed with primary cutaneous aspergillosis...
December 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29305665/synergistic-effect-of-polyvinyl-alcohol-and-copovidone-in-itraconazole-amorphous-solid-dispersions
#17
Kamil Wlodarski, Feng Zhang, Tongzhou Liu, Wieslaw Sawicki, Thomas Kipping
PURPOSE: The first objective is to evaluate the feasibility of melt-extruding polyvinyl alcohol-based amorphous solid dispersions for oral drug delivery. The second objective is to investigate the miscibility between polyvinyl alcohol 4-88 and copovidone, and to characterize the properties of ternary itraconazole amorphous solid dispersions comprising both polymers. METHODS: Samples were prepared using a co-rotating, twin-screw extruder. A solution precipitation study was conducted to compare the precipitation inhibition of polyvinyl alcohol against other commonly used polymers for amorphous solid dispersions...
January 5, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29260114/ocular-sporotrichosis-a-frequently-misdiagnosed-cause-of-granulomatous-conjunctivitis-in-epidemic-areas
#18
João Paulo M Yamagata, Fabiana B Rudolph, Maria Clara L Nobre, Leninha V Nascimento, Felipe Maurício S Sampaio, Andrea Arinelli, Dayvison F Freitas
Purpose: Sporotrichosis is a subcutaneous mycosis caused by Sporothrix sp., a dimorphic fungus. Although the cutaneous form is the most frequent form, the ocular presentation has been increasingly diagnosed in epidemic areas. We describe three cases of ocular sporotrichosis with the involvement of the ocular adnexa due to autoinoculation without trauma with successful antifungal treatment. Observations: Patient 1: A 68-year-old woman presented with granulomatous conjunctivitis of the right eye with an ulcerated nodule on the right temporal region for 5 months...
December 2017: American Journal of Ophthalmology Case Reports
https://www.readbyqxmd.com/read/29245279/mitral-regurgitation-after-anthracycline-based-chemotherapy-in-an-adult-patient-with-breast-cancer-a-case-report
#19
Xiaoyan Liu, Yanlin Zhu, Xue Lin, Ligang Fang, Xiaowei Yan
RATIONALE: Anthracyclines cardiotoxicity characterized by dilated myocardiopathy has been well described in the literature. However, anthracyclines-induced valvular diseases have been seldom reported. PATIENT CONCERNS: In this study, we present the case of a 62-year-old Chinese female patient with breast cancer developing severe mitral regurgitation after anthracycline exposure. DIAGNOSES: The patient was diagnosed with mitral regurgitation with preserved left ventricular ejection fraction and normal cardiac chamber dimensions in the sixth month after the last course of anthracycline-containing chemotherapy...
December 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29241703/the-artificial-membrane-insert-system-as-predictive-tool-for-formulation-performance-evaluation
#20
Philippe Berben, Joachim Brouwers, Patrick Augustijns
In view of the increasing interest of pharmaceutical companies for cell- and tissue-free models to implement permeation into formulation testing, this study explored the capability of an artificial membrane insert system (AMI-system) as predictive tool to evaluate the performance of absorption-enabling formulations. Firstly, to explore the usefulness of the AMI-system in supersaturation assessment, permeation was monitored after induction of different degrees of loviride supersaturation. Secondly, to explore the usefulness of the AMI-system in formulation evaluation, a two-stage dissolution test was performed prior to permeation assessment...
December 12, 2017: International Journal of Pharmaceutics
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