Fluconazole metabolism

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    Fluconazole metabolism


    There are currently a number of licensed azole antifungal drugs; however; only 4 (namely, fluconazole, itraconazole, posaconazole, and voriconazole) are used frequently in a clinical setting for prophylaxis or treatment of systemic fungal infections. In this article, we review the pharmacokinetic interactions of these azole antifungal drugs with other coadministered agents. We describe these (2-way) interactions and the extent to which metabolic pathways and/or other supposed mechanisms are involved in these interactions. This article provides an overview of all published drug-drug interactions in humans (either healthy volunteers or patients), and on the basis of these findings, we have developed recommendations for managing the specific interactions. Azole antifungal drugs exhibit a wide range and variety of drug-drug interactions. They are a substrate for and inhibitors of cytochrome P450 (CYP450) enzymes, as well as inhibitors of membrane transporters such as P-glycoprotein (P-g P). The inhibition or induction of CYP450 enzymes may alter the pharmacokinetic profile of the drugs involved and can thus affect both interacting agents. A 61-year-old female presented with weight gain, abdominal striae and worsening depression. Hb A1c increased to 76 mmol/mol despite increasing insulin. Investigations confirmed cortisol excess; afternoon serum cortisol was 552 nmol/l with an inappropriate ACTH of 9.3 pmol/l. In total, 24-h urinary free cortisol (UFC):creatinine ratio was 150 nmol/mmol with failure to suppress after 48 h of low-dose dexamethasone. Inferior petrosal sinus sampling confirmed Cushing's disease. Transsphenoidal resection was performed and symptoms improved. However, disease recurred 6 months later with elevated 24-h UFC 2200 nmol/day. Ketoconazole was later added at 400 mg daily, with dose reduction in metyrapone. When ketoconazole became unavailable, fluconazole 200 mg daily was substituted.

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    In Endocrinology, Diabetes & Metabolism Case Reports. Fluconazole, another azole antifungal, is an alternative, although its in vivo efficacy is unclear. Introduction Fluconazole is a triazole fungistatic agent used in the treatment of systemic and superficial fungal infections. Fluconazole therapy can cause transient. Fluconazole. Fluconazole. The drug's metabolism and its low lipophilicity and small molecular size may allow increased drug concentrations and efficacy in the.

    Печеночная и/или почечная недостаточность, появление сыпи на фоне применения флуконазола у пациентов с поверхностной грибковой инфекцией и инвазивными/системными грибковыми инфекциями, одновременный прием терфенадина и флуконазола в дозе менее 400 мг/сут, одновременный прием потенциально гепатотоксичных ЛС, алкоголизм, потенциально проаритмогенные состояния у пациентов с множественными факторами риска (органические заболевания сердца, нарушения электролитного баланса, одновременный прием ЛС, вызывающих аритмии), беременность. Применение при беременности и кормлении грудью: Применение препарата у беременных нецелесообразно, за исключением тяжелых или угрожающих жизни форм грибковых инфекций, когда потенциальная польза от применения флуконазола для матери значительно превышает риск для плода. Поскольку концентрация флуконазола в грудном молоке и в плазме одинакова, применять препарат в период лактации противопоказано. кожная сыпь, редко — мультиформная экссудативная эритема (в т.ч. ангионевротический отек, отек лица, крапивница, зуд кожи). Взрослым и детям старше 15 лет (массой тела более 50 кг) при криптококковом менингите и криптококковых инфекциях других локализаций в первый день обычно назначают 400 мг (8 капс. Продолжительность лечения при криптококковых инфекциях зависит от клинической эффективности, подтвержденной микологическим исследованием; при криптококковом менингите курс лечения должен быть не менее 6–8 нед. по 50 мг), а затем продолжают лечение в дозе 200 мг (4 капс. Для профилактики рецидива криптококкового менингита у больных СПИДом, после завершения полного курса первичной терапии, флуконазол назначают в дозе 200 мг (4 капс. по 50 мг) в сутки в течение длительного периода времени. При недостаточной клинической эффективности доза препарата может быть увеличена до 400 мг (8 капс. Длительность терапии зависит от клинической эффективности. При орофарингеальном кандидозе препарат обычно назначают по 150 мг 1 раз/сут, продолжительность лечения — 7–14 дней. The effects of rifampin on the pharmacokinetics of fluconazole were analyzed in an open-label, placebo-controlled, parallel study. Sixteen healthy male volunteers, randomized into two groups, received 200 mg of oral fluconazole on days 1 and 22. On days 8 through 27, group I received oral rifampin, 600 mg/d, and group II received placebo. On days 1 and 22, respectively, the AUC (micrograms.hr/m L) (mean /- SD) was 160.5 /- 19.5 and 124 /- 22.2 in group I, 152 /- 25 and 152.8 /- 33.9 in group II; the Kel (hr-1) was .0211 /- .0030 and .0264 /- .0040 in group I, .0219 /- .0036 and .0216 /- .0053 in group II. Cmax and Tmax did not change significantly in either group. Urinary 6 beta-hydroxycortisol/cortisol increased from 3.47 /- 1.04 to 15.2 /- 5.07 in group I, but was unchanged (3.54 /- 1.33-4.26 /- 2.36) in group II on days 1 and 22, respectively. The findings in this study indicate that rifampin induces the metabolism of fluconazole.23745159 - Alternate dosing of cetuximab for patients with metastatic colorectal cancer.2031819 - Heart rate response to an i.v. test dose of adrenaline and lignocaine with and without ...1645989 - The effect of incomplete bile duct obstruction on diisopropanolnitrosamine-induced chol...23150149 - Nat2 genotype guided regimen reduces isoniazid-induced liver injury and early treatment...24281379 - Effect of co-administration of rivaroxaban and clopidogrel on bleeding time, pharmacody...24856989 - Glucocorticoid treatment in rheumatoid arthritis.894509 - Factors affecting serum oxytetracycline levels in beef calves.20087759 - Interaction of vitamin k antagonists with heparin affect monitoring by activated clotti...14968949 - Extracranial stereotactic radioablation: physical principles.

    Fluconazole metabolism

    PDF Fluconazole and phenytoin A predictable, Fluconazole - National Institutes of Health

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    METABOLISM SITES. Fluconazole is primarily excreted by the kidneys, with approximately 80% of the administered dose appearing in the urine as unmetabolised drug. Fluconazole is an antifungal drug used for the treatment of systemic and superficial fungalFluconazole has many advantages over the other antifungal drugs including the option of oral. DIFLUCAN 50 mg & 150 mg capsules* are also indicated for the treatment of. Losartan Fluconazole inhibits the metabolism of losartan to its active metabolite.

     
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    FLUCONAZOLE TABLETS - DailyMed Pharmacokinetics and Metabolism. The pharmacokinetic properties of fluconazole are similar following administration by the intravenous or oral routes.

    The disposition and metabolism of 14Cfluconazole in humans.
     
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