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    ​《ISPN学习》总第540期
    日期:2019-09-26 19:08:06    




    《ISPN学习》2019年09月25日总第540期
     
     
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    ISPN  Review        
    Synthetic triazoles
    合成三氮唑

     
    The synthetic triazoles include:
    • fluconazole
    • itraconazole
    • voriconazole.
     
    合成三唑类药包括:氟康唑、伊曲康唑、伏立康唑。
     
    Fluconazole belongs to a class of synthetic, broad-spectrum triazoles and is also referred to as a bistriazole antimycotic drug.
    Itraconazole and voriconazole also belong to the synthetic triazole class of drugs. They inhibit the synthesis of ergosterol, a vital component of fungal cell membranes.
     
    氟康唑属于合成、广谱三唑类药,也称为双三唑抗真菌药。
    伊曲康唑和伏立康唑也属于合成三唑类药,可以抑制麦角固醇的合成,后者为真菌细胞粘膜的重要成分。

     
    Pharmacokinetics
    After oral administration, fluconazole is about 90% absorbed. It’s distributed into all body fluids, and more than 80% of the drug is excreted unchanged in urine.
    Oral bioavailability is greatest when itraconazole is taken with food; voriconazole is more effective if taken 1 hour before or after a meal.
    Itraconazole and voriconazole are bound to plasma proteins and extensively metabolized in the liver into a large number of metabolites. They’re minimally excreted in stool.
     
    药动学
    口服后,氟康唑吸收率约90%左右,并分布于全身体液中。80%的药物经尿原型排出。
    伊曲康唑与食物一起服用时,生物利用度最高;伏立康唑则在餐前或餐后1小时服用效果更佳。
    伊曲康唑和伏立康唑与血浆蛋白结合,广泛性代谢与肝,产生代谢物。少量经粪便排出。
     

    Pharmacodynamics
    Fluconazole inhibits fungal cytochrome P-450, an enzyme responsible for fungal sterol synthesis, causing fungal cell walls to weaken. Itraconazole and voriconazole interfere with fungal cell-wall synthesis by inhibiting the formation of ergosterol and increasing cell-wall permeability, making the fungus susceptible to osmotic instability.
     
    氟康唑抑制真菌细胞色素P-450(该酶负责真菌甾醇合成),引起真菌细胞壁衰弱。伊曲康唑和伏立康唑通过抑制麦角固醇形成和增加细胞壁渗透性,干扰真菌细胞壁合成,使真菌易受渗透不稳定性影响。
     
    Pharmacotherapeutics
    Fluconazole is used to treat mouth, throat, and esophageal candidiasis and serious systemic candidal infections, including UTIs, peritonitis, and pneumonia. It’s also used to treat cryptococcal meningitis.
     
    药物治疗学
    氟康唑用于治疗口腔、咽喉和食道念珠菌病和严重的系统性念珠菌感染,包括UTI、腹膜炎和肺炎。也用于治疗隐球菌性脑膜炎。


    Itraconazole is used to treat blastomycosis, nonmeningeal histoplasmosis, candidiasis, aspergillosis, and fungal nail disease. Voriconazole is used to treat invasive aspergillosis and serious fungal infections caused by Scedosporium apiospermum and Fusarium species.

    伊曲康唑用于治疗芽生菌病、非脑膜组织胞浆菌病、念珠菌病、曲霉菌病和真菌指甲疾病。伏立康唑用于治疗侵入性曲霉菌病和由端赛多孢子菌和镰刀菌引起的严重真菌感染。
     
    Drug interactions
    Fluconazole may have interactions with other drugs:
    • Using fluconazole with warfarin may increase the risk of bleeding.
    • It may increase levels of phenytoin and cyclosporine.
    • It may increase the plasma levels of oral antidiabetic drugs, such as glyburide, tolbutamide, and glipizide, increasing the risk of hypoglycemia.
    • Rifampin and cimetidine enhance the metabolism of fluconazole, reducing its plasma level.
    • Fluconazole may increase the activity of zidovudine.
    Itraconazole and voriconazole may have these interactions:
    • Both may increase the risk of bleeding when combined with oral anticoagulants.
    • Antacids, H2-receptor antagonists, phenytoin, and rifampin lower plasma itraconazole levels.
    • Voriconazole may inhibit the metabolism of phenytoin, benzodiazepines, calcium channel blockers, sulfonylureas, and tacrolimus.
    • Voriconazole is contraindicated with sirolimus and ergot alkaloids because voriconazole may increase plasma levels of sirolimus and ergots.
    • Voriconazole is contraindicated with quinidine and pimozide because of the risk of prolonged QT interval and, rarely, torsades de pointes.
     
    药物相互作用
    氟康唑与其他药物的相互作用:
    氟康唑与华法林使用可能增加出血风险
    可能增加苯妥英和环孢菌素浓度
    可能增加口服降糖药的血浆浓度,如格列本、甲苯磺丁脲和格列吡嗪,增加低血糖风险
    利福平和西米替丁强化氟康唑代谢,降低血浆浓度
    氟康唑可能增加刘齐多夫定活性。
    伊曲康唑和伏立康唑可能有这些相互作用:
    与口服抗凝药一起使用时,两药均可增加出血风险
    制酸剂、H2受体拮抗药、苯妥英和利福平降低血浆伊曲康唑浓度
    伏立康唑可能抑制苯妥英、苯二氮卓类药、钙通道阻滞剂、磺脲类药和他克莫司的代谢
    伏立康唑禁忌与西罗莫司和麦角生物碱一起使用,因为伏立康唑可能增加西罗莫司和麦角的血浆浓度
    伏立康唑禁忌与奎尼丁和匹莫齐特一起使用,因为有延长QT间期和罕见的扭转性室速风险。

     
    Adverse reactions to fluconazole include:
    • abdominal pain
    • diarrhea
    • dizziness
    • headache
    • elevated liver enzyme levels
    • nausea and vomiting
    • rash.
     
    氟康唑不良反应包括:
    腹痛、腹泻、头晕、头痛、肝酶水平升高、恶心呕吐及皮疹。

     
    Adverse reactions to itraconazole include:
    • dizziness
    • headache
    • hypertension
    • impaired liver function
    • nausea.
     
    伊曲康唑不良反应包括:
    头晕、头痛、高血压、肝功能受损及恶心。

     
    Adverse reactions to voriconazole include:
    • vision disturbances
    • fever
    • chills
    • headache
    • tachycardia
    • nausea and vomiting
    • rash
    • elevated liver enzyme.

    伏立康唑不良反应包括:
    视觉障碍、发烧、寒战、头痛、心动过速、恶心呕吐、皮疹及肝酶水平升高。

     


    Vocabulary for Today    
    triazole – n. 三唑类药
    fluconazole – n. 氟康唑
    itraconazole – n. 伊曲康唑
    voriconazole – n. 伏立康唑
    bistriazole antimycotic drug – 双三唑抗真菌药
    ergosterol – n. 麦角固醇
    blastomycosis – n. 芽生菌病
    nonmeningeal – a. 非脑膜(炎)的
    histoplasmosis – n. 组织胞浆菌病
    aspergillosis – n. 曲霉菌病
    Scedosporium apiospermum – 尖端赛多孢子菌
    Fusarium – n. 镰刀菌
    glyburide – n. 格列本
    tolbutamide – n. 甲苯磺丁脲
    glipizide – n. 格列吡嗪
    sulfonylureas – n. 磺脲类
    tacrolimus – n. 他克莫司
    sirolimus – n. 西罗莫司
    torsades de pointes – n. 扭转性室速
     
     
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    Video            

     Imidazole
     
    Test                 
    1. Silver sulfadiazine is prescribed for a client with a burn injury. Which laboratory finding requires the need for follow-up by the nurse?
    A. Glucose level of 99 mg/dL (5.65 mmol/L)
    B. Magnesium level of 1.5 mEq/L (0.75 mmol/L)
    C. Platelet level of 300,000 mm3 (300 × 109/L)
    D. White blood cell count of 3000 mm3 (3.0 × 109/L)
    2. Sirolimus (Rapamune) is prescribed to a post-renal transplantation client. Upon the review of the chart, the nurse expects which of the following laboratory results?
    A. Elevated serum potassium.
    B. Decreased cholesterol level.
    C. Elevated platelet count.
    D. Elevated triglyceride level.
     
    (本期答案见页底)
     
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    本期ISPN Review答案

    1. D. White blood cell count of 3000 mm3 (3.0 × 109/L)
    Silver sulfadiazine is used for the treatment of burn injuries. Adverse effects of this medication include rash and itching, blue-green or gray skin discoloration, leukopenia, and interstitial nephritis. The nurse should monitor a complete blood count, particularly the white blood cells, frequently for the client taking this medication. If leukopenia develops, the health care provider is notified and the medication is usually discontinued. The white blood cell count noted in option 4 is indicative of leukopenia. The other laboratory values are not specific to this medication, and are also within normal limits.
    2. D. Elevated triglyceride level.
    Sirolimus (Rapamune) raises cholesterol and triglyceride levels. This medication also causes a decrease in potassium and platelet count.
     





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