- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Preclinical, Journal: Experimental Evidence of Liver Injury by BSEP-Inhibiting Drugs With a Bile Salt Supplementation in Rats. (Pubmed Central) - Jul 29, 2020
Plasma transaminase levels significantly increased in rats receiving CDCA+KTZ, whereas neither treatment with CDCA alone, KTZ alone nor a combination of CDCA and miconazole, a safe analog to KTZ, induced liver injury...In conclusion, we found that oral CDCA supplementation predisposed rats to KTZ-induced liver injury due to the hepatic accumulation of bile acids. This method may be useful for assessing the potential of BSEP-inhibiting drugs inducing liver injury in vivo.
- |||||||||| fluconazole / Generic mfg.
Journal: Challenges in the Polyene- and Azole-Based Pharmacotherapy of Ocular Fungal Infections. (Pubmed Central) - Jul 7, 2020
Despite potent antifungal activity, the clinical utility of these agents in ophthalmic infections has been challenged by their physicochemical properties, the unique ocular anatomy and physiology, selective antifungal activity, ocular and systemic toxicity, emergence of resistance and cross-resistance, and absence of reliable techniques for developing a robust in vitro-in vivo correlation. This review discusses the aforementioned challenges and the common approaches undertaken to circumnavigate the difficulties associated with the polyene- and azole-based pharmacotherapy of ophthalmic fungal infections.
- |||||||||| clotrimazole / Generic mfg.
Journal: Automated in vivo screen in zebrafish identifies clotrimazole as targeting a metabolic vulnerability in a melanoma model. (Pubmed Central) - Jul 7, 2020
Furthermore, we show that the effects of clotrimazole are mediated by the inhibition of hexokinase activity, which is lethal to the abnormal metabolic profile of melanoma cells in vitro and in vivo. Thus, our study shows that the zebrafish can provide a phenotype-rich assay for fully automated screening approaches to identify drugs for synthetic lethal treatment in melanoma and suggest further testing of clotrimazole in combinatorial treatments.
- |||||||||| Journal: In vitro activity of chlorhexidine compared with seven antifungal agents against 98 Fusarium isolates recovered from fungal keratitis patients. (Pubmed Central) - Jun 10, 2020
Amphotericin B showed the most favorable in vitro inhibition of Fusarium species followed by natamycin, voriconazole and chlorhexidine, while 5-fluorocytosine, posaconazole, miconazole and caspofungin showed no relevant inhibiting effect. However, chlorhexidine showed fungicidal activity against 90% of F. oxysporum strains and 100% of the F. solani strains.Our study supports the clinical efficacy of chlorhexidine, and therefore warrants its further clinical evaluation for primary therapy of fungal keratitis, particularly in low and middle income countries where fungal keratitis is much more frequent and currently antifungal eye drops are often unavailable.
- |||||||||| triamcinolone acetonide topical / Generic mfg., Loramyc (SO-1105) / Onxeo, Sosei
It’s Not Yeast: Re-classification of Candida Diagnoses in the Lactating Breast () - May 29, 2020 - Abstract #ASBrS2020ASBrS_179;
Common diagnoses include subacute mastitis, blebs, dermatitis, and vasospasm. Accurate, timely diagnosis is crucial as pain is a risk factor for premature cessation of breastfeeding, and prompt symptomatic resolution occurs on appropriate therapy.
- |||||||||| fluconazole / Generic mfg., clotrimazole / Generic mfg.
Preclinical, Journal: The classic azole antifungal drugs are highly potent endocrine disruptors in vitro inhibiting steroidogenic CYP enzymes at concentrations lower than therapeutic Cmax. (Pubmed Central) - May 27, 2020
The aim of this study was to mechanistically investigate the endocrine disrupting potential of four commonly used azole antifungal drugs; clotrimazole, miconazole, ketoconazole and fluconazole in vitro using the H295R cell assay and two recombinant, CYP17A1 and CYP19A1 (aromatase), assays...The results indicate that these four azole drugs are highly potent in vitro and, based on plasma Cmax values, may exert endocrine disrupting effects at therapeutically relevant concentrations. This raises concern for endocrine related diseases in patients using azole antifungal drugs, particularly when taken during sensitive periods like pregnancy.
- |||||||||| clotrimazole / Generic mfg., Loramyc (SO-1105) / Onxeo, Sosei
Journal: Direct stimulation of adenylyl cyclase 9 by the fungicide imidazole miconazole. (Pubmed Central) - Apr 27, 2020
Differential modulation of mammalian tmAC paralogs appears to be achievable by an imidazole with phenylated side chains. Optimization of the lead compound and exploration of the underlying mechanism(s) of action in more detail could exploit this further.
- |||||||||| glibenclamide / Generic mfg., carbamazepine / Generic mfg.
Journal: Simultaneous Analysis of Multiclass Contaminants of Emerging Concern in Sediments by Liquid Chromatography with Tandem Quadrupole Mass Spectrometry. (Pubmed Central) - Apr 22, 2020
The method performance was also compared with a well-established US-EPA Method 1694 by analyzing sediment samples collected from Yundang Lagoon (Xiamen, China) with field-incurred CEC residues. The sediment samples were detected with residues of parabens, gemfibrozil, ketoprofen, naproxen, fenoprofen, diclofenac, miconazole, carbamazepine, benzophenon-3, glibenclamide, sildinafil citrate and some bisphenol analogues.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Journal: Preparation, and Assessment of Antidermatophyte Activity of Miconazole-Urea Water-Soluble Film. (Pubmed Central) - Apr 21, 2020
In vivo test showed that combination of 0.004 mg/L miconazole with 20% urea (M + U20) showed the highest efficacy percentage (95.83%), which was statistically superior to the infected untreated control (p < 0.001) in fungal burden reduction as well as improvement in clinical scores (p < 0.001). This work supports the hypothesis and suggests a new promising dosage form for the treatment of T. rubrum infections.
- |||||||||| fluconazole / Generic mfg., clotrimazole / Generic mfg.
Clinical, Journal: Analysis of homology and drug sensitivity of vaginal isolates of 10 patients with recurrent vulvovaginal candidiasis in recurrent episodes (Pubmed Central) - Apr 15, 2020
(2) After clinical medication, the sensitivity of vaginal isolates to azoles was generally decreased, but remained highly sensitive to nystatin, nystatin (first and second clinical isolates: 100% sensitivity and 100% sensitivity)>clotrimazole (100% sensitivity and 90% sensitivity)>fluconazole (80% sensitivity and 70% sensitivity)>itraconazole (60% sensitivity and 50% sensitivity)>miconazole (30% sensitivity and 20% sensitivity)...(2) Antifungal agents could selectively induce drug resistance to Candidas, and Candidas show cross-resistance to antifungal agents. Repeated fungal culture and drug sensitivity test in patients with RVVC are very necessary for correct selection of antifungals.
- |||||||||| tacrolimus / Generic mfg., fluconazole / Generic mfg., Sebifin (terbinafine HCL) / Generic mfg.
Journal: Molecular epidemiology, in vitro susceptibility and exoenzyme screening of Malassezia clinical isolates. (Pubmed Central) - Apr 14, 2020
The minimum inhibitory concentrations (MICs) of nine antifungals (posaconazole, voriconazole, itraconazole, fluconazole, ketoconazole, miconazole, bifonazole, terbinafine and caspofungin) and tacrolimus, the interactions between three antifungals (itraconazole, ketoconazole and terbinafine) and tacrolimus, and the extracellular enzyme profile were evaluated using broth and checkerboard microdilution and the Api-Zym system, respectively.Results...Synergistic effects between terbinafine and itraconazole or tacrolimas and antifungals may be irrelevant to clinical application. Overproduction of lipases could enhance the skin inhabitation of M. furfur.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Journal, IO Biomarker: Miconazole triggers various forms of cell death in human breast cancer MDA-MB-231 cells. (Pubmed Central) - Mar 29, 2020
The initial mechanism of MCZ-mediated cell death in human breast cancer MDA-MB-231 cells involves an increase in the Bax/Bcl-2 ratio, downregulation of apoptosis induced by Akt and p-Akt-473, a simultaneous upregulation of the receptor-interacting protein 3 (RIP3) and mixed lineage kinase domain-like (MLKL) protein expression, and ROS production to induce necroptosis. Our results suggest that MCZ may be a potential lead compound for the development of anti-breast cancer drugs.
- |||||||||| clotrimazole topical / Generic mfg.
Clinical, Review, Journal: Cutaneous candidiasis - An evidence-based review of topical and systemic treatments to inform clinical practice. (Pubmed Central) - Mar 13, 2020
In conclusions, clotrimazole, nystatin and miconazole were the most studied topical drugs and demonstrated equal good efficacy and mild adverse effects similar to combinations of anti-fungal, anti-bacterial, and topical corticosteroids. Oral fluconazole was as effective as topical clotrimazole and is the only commercially available evidence-based option for systemic treatment of cutaneous candidiasis.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Journal: Effects of epoxygenases on the nonadrenergic noncholinergic relaxant responses induced by electrical field stimulation in rabbit corpus cavernosum. (Pubmed Central) - Feb 16, 2020
Miconazole (10 -10 M), 17-octadecynoic acid (ODYA) (10 -10 M), 14,15-epoxyeicosatrienoic acid (EET) (10 -10 M), 11,12-EET (10 -3 × 10 M) and 20-hydroxyeicosatetraenoic acid (HETE) (10 -3 × 10 M) were added cumulatively (n = 5-7 for each set of experiments)...No drug caused a significant relaxation response on tissues contracted with phenylephrine. Epoxygenases contribute to EFS-mediated NO-dependent and NO-independent NANC relaxations by presynaptic mechanisms, offering a new treatment alternative for erectile dysfunction which needs to be explored in further in vivo, molecular and clinical studies.
- |||||||||| clotrimazole / Generic mfg.
Journal: LAM Genes Contribute to Environmental Stress Tolerance but Sensibilize Yeast Cells to Azoles. (Pubmed Central) - Feb 13, 2020
Alternatively, LAM deletions might alleviate the toxic effect of sterols as Lam proteins can transport toxic sterol biosynthesis intermediates into membrane compartments that are sensitive to these compounds. Our findings reveal novel biological roles of LAM genes in stress tolerance and suggest that mutations in these genes may confer upregulation of a mechanism that provides resistance to azole antifungals in pathogenic fungi.
- |||||||||| fluconazole / Generic mfg., clotrimazole / Generic mfg.
Journal: Occurrence and risk assessment of azole antifungal drugs in water and wastewater. (Pubmed Central) - Feb 1, 2020
Clotrimazole, econazole, fluconazole, itraconazole, ketoconazole and miconazole were detected at least once in the water samples, while posaconazole and voriconazole were not detected in any of the samples for all seasons at which the samples were collected...Furthermore, risk estimates showed a potential for the detected concentrations of fluconazole and itraconazole in water samples to pose moderate to high risk for development of antifungal drug resistance. Some of the azole antifungal drugs are ubiquitous in the wastewater and future monitoring and validation studies should be conducted for those drugs that seem to pose human health and ecological risks.
- |||||||||| ceftriaxone / Generic mfg.
Journal: Periorbital necrotising fasciitis secondary to scratching. (Pubmed Central) - Dec 20, 2019
The patient was admitted to hospital with the diagnosis of periorbital necrotising fasciitis, in order to receive treatment with intravenous ceftriaxone, linezolid, and immediate surgical debridement...Daily wound management consisted of debridement of necrotic remains, disinfection with chlorhexidine, and wound dressing with mupirocin, sulfadiazine, and miconazole ointments...Palpebral reconstruction was performed on day 15, consisting of a preauricular total thickness skin graft for the superior eyelid, and lateral malar advancement to cover the lower eyelid. Adequate cosmetic and functional results were obtained.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei, warfarin / Generic mfg.
Journal: Topical miconazole and warfarin. (Pubmed Central) - Dec 20, 2019
Adequate cosmetic and functional results were obtained. No abstract available
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Journal: Preparation, Optimization, and Evaluation of Hyaluronic Acid-Based Hydrogel Loaded with Miconazole Self-Nanoemulsion for the Treatment of Oral Thrush. (Pubmed Central) - Dec 6, 2019
The optimized formulation exhibited higher ex vivo skin permeability and enhanced antifungal activity by 1.85 and 2.179, respectively, compared to MZ-SNEDDS, and by 1.52 and 1.72 folds, respectively, compared to marketed gel. Optimized MZ-NE hyaluronic acid-based oral gel demonstrated better antifungal activity, indicating its potential in oral thrush pharmacotherapy.
- |||||||||| fluconazole / Generic Mfg.
Review, Journal: Treatment of Madura foot: a systematic review. (Pubmed Central) - Nov 14, 2019
Therapy for Madura foot is informed by case series and case reports which provide low level evidence for practice. Antimicrobials in conjunction with surgery lead to resolution of disease.
- |||||||||| citalopram / Generic Mfg., sertraline / Generic Mfg., carbamazepine / Generic Mfg.
Journal: Soil influences on uptake and transfer of pharmaceuticals from sewage sludge amended soils to spinach. (Pubmed Central) - Nov 10, 2019
However, in the case of some other compounds (i.e. sertraline, amitriptyline, mirtazapine, metoprolol), uptake and the subsequent translocation and transformation from 3 soils of a higher pH and base cation saturation (Stagnic Chernozem Siltic, Haplic Chernozem and Greyic Phaeozem) significantly differed from 4 soils with a lower pH and base cation saturation (Haplic Luvisol, Haplic Cambisol, Dystric Cambisol and Arenosol Epieutric). Such observations proved strong compound dependent influences of soil conditions on various compounds bioaccumulations in plants and necessity of studying these processes always in diverse soils.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Journal: Imidazole Compounds for Protecting Choroidal Endothelial Cells from Complement Injury. (Pubmed Central) - Oct 31, 2019
Two closely related molecules identified in the screen, econazole nitrate and miconazole nitrate, were followed in validation and mechanistic studies...Both exosome release and cell surface roughness (assessed using a Holomonitor system) were reduced by drug pretreatment in RF/6A cells, whereas endosome formation increased with both drugs, consistent with imidazole-mediated alterations of cell surface dynamics. The results in the current study provide further proof of principle that small molecules can protect choroidal ECs from MAC-induced cell death and suggest that FDA approved compounds may be beneficial in reducing vascular loss and progression of AMD.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Clinical, Journal: Oral lichen planus. Case report and literature review (Pubmed Central) - Oct 25, 2019
Treatment with mometasone was started thrice daily for 20 days and intermittently with miconazole gel to prevent iatrogenic mycosis by the corticosteroid...In autoimmune diseases, clinical-histopathological correlation is important for a definitive diagnosis to be established. Clinical follow-up of these patients should be carried out in the long term, in order to achieve remission of the lesions, control of the disease and avoid future complications.
- |||||||||| clotrimazole / Generic Mfg.
FDA event, Journal: Identification of FDA-approved drugs as antivirulence agents targeting the pqs quorum sensing system of Pseudomonas aeruginosa. (Pubmed Central) - Oct 10, 2019
Moreover, clofoctol protected Galleria mellonella larvae from P. aeruginosa infection and inhibited the pqs QS system in P. aeruginosa isolates from cystic fibrosis patients. Notably, clofoctol is already approved for clinical treatment of pulmonary infections caused by Gram-positive bacterial pathogens, hence this drug has considerable clinical potential as an antivirulence agent for the treatment of P. aeruginosa lung infections.
- |||||||||| clotrimazole / Generic Mfg.
Journal: Therapeutic tools for oral candidiasis: Current and new antifungal drugs. (Pubmed Central) - Oct 2, 2019
Nystatin, miconazole, and fluconazole are very effective for treating oral candidiasis. There are systemic alternatives for treating recalcitrant infections, such as the new triazoles, echinocandins, or lipidic presentations of amphotericin B.
- |||||||||| Spherazole (itraconazole) / RA Chem, JW Pharma, Spherics, Loramyc (SO-1105) / Onxeo, Sosei
Journal: Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres. (Pubmed Central) - Sep 30, 2019
Differential scanning calorimetry measurements suggested complete amorphization of MCZ in MCZ-PLGA MS, whereas crystalline ITCZ was detected in the ITCZ-PLGA MS. This complete amorphization of MCZ is considered to be one of the reasons for the initial burst release.
- |||||||||| Flagyl (metronidazole) / SLA
Clinical, Journal: Mycoplasma genitalium infection in Kenyan and US women. (Pubmed Central) - Sep 28, 2019
genitalium infection is common among sexually active women in Kenya and the Southern US. Given associations between MG and adverse reproductive health outcomes, this high burden of M. genitalium in reproductive-aged women could contribute to substantial morbidity.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei
Preclinical, Journal: Effects of using Antifungal Gel on Retentive Bond Strength of Two Forms of Denture Adhesives: An in vitro Study. (Pubmed Central) - Sep 22, 2019
Given associations between MG and adverse reproductive health outcomes, this high burden of M. genitalium in reproductive-aged women could contribute to substantial morbidity. The incorporation of an antifungal agent into denture adhesives is required in many denture patients to suppress fugal growth and eliminate the undesirable health effects associated with such infections.
- |||||||||| Loramyc (SO-1105) / Onxeo, Sosei, warfarin / Generic Mfg.
Journal: Morbidity and mortality associated with the interaction of miconazole oral gel and warfarin. (Pubmed Central) - Sep 20, 2019
This paper reports on recent developments concerning this interaction, and the important patient safety issues involved. In situations where topical treatment for oral candidiasis is indicated, nystatin should be prescribed instead of miconazole oral gel in patients taking warfarin, unless close monitoring and titration of the anticoagulant effect is undertaken.
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