广谱三唑类抗真菌药voriconazole（商标名：VFEND）获美国批准上市 伏立康唑(voriconazole，VRC，UK109，496)是美国辉瑞公司在氟康唑的结构基础上合成的一种新型三唑类广谱抗真菌药，于2002年5月在美国批准上市，商品名为Vfend ，中文商品名为威凡。 其口服和静脉给药均有很好的抗真菌活性。体内、外实验表明，伏立康唑对多种致病真菌均有较好的抗菌活性。伏立康唑临床主要用于抑制和杀死隐球菌属、曲霉菌属及念珠菌属，尤其是用于对氟康唑无效的念珠菌感染、对伊曲康唑和两性霉素B无效的曲霉菌感染和对两性霉素B耐药的土霉菌感染等。伏立康唑已成为临床治疗真菌病的一种新的有效药物。 Vfend（伏立康唑[Voriconazole]）片剂，口服混悬液，和IV 初步U. S.批准：2002年 适应症 本品是三唑类抗真菌的药物，在治疗中使用的表示： 侵袭性曲霉病 念珠菌（nonneutropenics）和皮肤念珠菌病的传播，腹部，肾脏，膀胱壁，和创伤。 食道念珠菌。 Scedosporium apiospermum和镰刀菌引起的严重感染。包括茄病镰刀菌，患者不能耐受的，或难治性外，其他治疗。 剂量和用法 推荐的给药方案 感染负荷剂量维持剂量*四*第四口腔 查看完整的处方信息用于静脉注射的指示。 增加剂量时，本品与苯妥英或依非韦伦共同管理;减少剂量与肝功能不全患者 口服和静脉注射维持剂量不产生相同的伏立康唑的风险。200毫克的剂量口服提供了一个接触类似3毫克/公斤IV剂量300毫克剂量口服提供了一个类似4毫克/公斤的四剂量的暴露。 体重不到40公斤的成人患者应接受口服维持剂量的一半。 在临床研究中，四，本品治疗的时间中位数为10天;口服本品治疗的中位数时间为76天。 与念珠菌的患者接受3毫克/公斤q12h;与其他深部组织的念珠菌感染的患者接受4毫克/公斤q12h。 侵袭性曲霉病 6毫克/公斤q12h第一个24小时4毫克/公斤q12h 200毫克q12h 念珠菌在第一个24小时3-4毫克/公斤q12h＃200毫克q12h nonneutropenics和其他深部组织的念珠菌感染6毫克/公斤q12h 食道念珠菌没有评估不评估200毫克q12h Scedosporiosis和Fusariosis 6毫克/公斤为第一个24小时q12h 4毫克/公斤200毫克q12h q12h 剂型和优势 粉末注射液：200毫克伏立康唑和3200毫克磺丁基醚β-环糊精钠（SBECD）。 薄膜衣片：50毫克，200毫克伏立康唑。 粉口服混悬液：40伏立康唑毫克/毫升。  禁忌 伏立康唑或辅料过敏。 为了减少严重不良事件的风险，不使用，本品与特非那定，阿司咪唑，西沙必利，匹莫齐特或奎尼丁，西罗莫司。 为了防止损失，本品疗效，不要使用与利福平，卡马西平，长效巴比妥类药物，利托那韦，利福布丁，麦角生物碱，和圣约翰草。  警告和注意事项 药物交互作用：审查病人的合并用药。几种药物可能会大大改变伏立康唑的浓度。伏立康唑可能会改变PK几种药物或PD。 肝毒性：严重肝反应的报道。评估期间，在启动和伏立康唑治疗过程中的肝功能检查 视力障碍：显示器的视觉功能，如果继续治疗超过28天 妊娠D类：不给孕妇管理 半乳糖不耐受：没有管理与半乳糖的不容忍现象，拉普乳糖酶缺乏或葡萄糖 - 半乳糖吸收不良的患者 心律失常，QT间期延长：管理与心律失常的条件患者慎用 输注相关反应：过敏性反应已有报道 皮肤病反应：剥脱性皮肤反应和光敏性已报告 不良反应 最常见的（所有的伤亡，发生率≥2％）：视觉障碍，发热，恶心，皮疹，呕吐，寒战，头痛，肝功能检测异常，心动过速，幻觉。  药物相互作用 CYP3A4，CYP2C9和CYP2C19的抑制剂和诱导剂，可能会改变本品的浓度。调整本品剂量的不良事件或缺乏有效性和显示器。 本品会增加浓度的药物，CYP3A4，CYP2C9和CYP2C19基板和活动。减少剂量，缺乏疗效或这些酶的底物与药物相关的不良事件的监控 在特殊人群中使用 怀孕或哺乳妇女：本品不应该在怀孕或哺乳妇女使用 儿科：<12岁患者的安全性/有效性尚未确定 肝功能损害：使用一半的患者有轻度至中度肝功能不全（Child - Pugh分级A和B）的维持剂量 肾损害：静脉给药避免在中度至严重肾功能不全患者（肌酐清除率<50毫升/分钟） 修订日期：06/2011 ----------------------------------------------------- 【原产地英文商品名】VFEND IV for injection 200mg/20ml/vial 【原产地英文药品名】VORICONAZOLE 【中文参考商品译名】威凡 IV注射剂 200毫克/20毫升/瓶 【中文参考药品译名】伏立康唑 【生产厂家中文参考译名】辉瑞 【生产厂家英文名】PFIZER 【产  地  国  家】美国 Voriconazole-Vfend®-Renal Dosing DOSAGE AND ADMINISTRATION: Administration VFEND Tablets or Oral Suspension should be taken at least one hour before, or one hour following, a meal. VFEND I.V. for Injection requires reconstitution to 10mg/mL and subsequent dilution to 5 mg/mL or less prior to administration as an infusion, at a maximum rate of 3mg/kg per hour over 1–2 hours (see Intravenous Administration). NOT FOR IV BOLUS INJECTION Use of VFEND I.V. with other Parenteral Drug Products Blood products and concentrated electrolytes VFEND I.V. must not be infused concomitantly with any blood product or short-term infusion of concentrated electrolytes, even if the two infusions are running in separate intravenous lines (or cannulas). Electrolyte disturbances such as hypokalemia, hypomagnesemia and hypocalcemia should be corrected prior to initiation of VFEND therapy (see package insert for PRECAUTIONS). Intravenous solutions containing (non-concentrated) electrolytes VFEND I.V. can be infused at the same time as other intravenous solutions containing (non-concentrated) electrolytes, but must be infused through a separate line. Total parenteral nutrition (TPN) VFEND I.V. can be infused at the same time as total parenteral nutrition, but must be infused in a separate line. If infused through a multiple-lumen catheter, TPN needs to be administered using a different port from the one used for VFEND I.V. Use in Adults =============================== Invasive aspergillosis and serious fungal infections due to Fusarium spp. and Scedosporium apiospermum For the treatment of adults with invasive aspergillosis and infections due to Fusarium spp. and Scedosporium apiospermum, therapy must be initiated with the specified loading dose regimen of intravenous VFEND to achieve plasma concentrations on Day 1 that are close to steady state. On the basis of high oral bioavailability, switching between intravenous and oral administration is appropriate when clinically indicated (see package insert for CLINICAL PHARMACOLOGY). Once the patient can tolerate medication given by mouth, the oral tablet form or oral suspension form of VFEND may be utilized. (See Table below.) Candidemia in nonneutropenic patients and other deep tissue Candida infections See Table below. Patients should be treated for at least 14 days following resolution of symptoms or following last positive culture, whichever is longer. Esophageal Candidiasis See Table below. Patients should be treated for a minimum of 14 days and for at least 7 days following resolution of symptoms. Dosage Adjustment ======================================= If patient response is inadequate, the oral maintenance dose may be increased from 200 mg every 12 hours to 300 mg every 12 hours. For adult patients weighing less than 40 kg, the oral maintenance dose may be increased from 100 mg every 12 hours to 150 mg every 12 hours. If patients are unable to tolerate 300 mg orally every 12 hours, reduce the oral maintenance dose by 50 mg steps to a minimum of 200 mg every 12 hours (or to 100 mg every 12 hours for adult patients weighing less than 40 kg). If patients are unable to tolerate 4 mg/kg IV, reduce the intravenous maintenance dose to 3 mg/kg every 12 hours. Phenytoin may be coadministered with VFEND if the intravenous maintenance dose of VFEND is increased to 5 mg/kg every 12 hours, or the oral maintenance dose is increased from 200 mg to 400 mg every 12 hours (100 mg to 200 mg every 12 hours in adult patients weighing less than 40 kg) (see package insert: CLINICAL PHARMACOLOGY, PRECAUTIONS - Drug Interactions). When voriconazole is coadministered with efavirenz, the voriconazole maintenance dose should be increased to 400 mg Q12h and the efavirenz dose should be decreased to 300 mg Q24h. When treatment with voriconazole is stopped, the initial dosage of efavirenz should be restored (see package insert: CLINICAL PHARMACOLOGY and PRECAUTIONS – Drug Interactions). Duration of therapy should be based on the severity of the patient's underlying disease, recovery from immunosuppression, and clinical response. Use in Geriatric Patients ================================ No dose adjustment is necessary for geriatric patients. Use in Patients with Hepatic Insufficiency ================================ In the clinical program, patients were included who had baseline liver function tests (ALT, AST) up to 5 times the upper limit of normal. No dose adjustment is necessary in patients with this degree of abnormal liver function, but continued monitoring of liver function tests for further elevations is recommended. It is recommended that the standard loading dose regimens be used but that the maintenance dose be halved in patients with mild to moderate hepatic cirrhosis (Child-Pugh Class A and B). VFEND has not been studied in patients with severe hepatic cirrhosis (Child-Pugh Class C) or in patients with chronic hepatitis B or chronic hepatitis C disease. VFEND has been associated with elevations in liver function tests and clinical signs of liver damage, such as jaundice, and should only be used in patients with severe hepatic insufficiency if the benefit outweighs the potential risk. Patients with hepatic insufficiency must be carefully monitored for drug toxicity. Renal Dosing [CRCL <50ml/min]: INTRAVENOUS voriconazole should be avoided, unless the benefit justifies the risk. Accumulation of the intravenous vehicle (SBECD) may occur. After initial loading dose, oral voriconazole should be administered to these patients. Oral: no adjustments necessary. -------------------------------------------------------------------- Use in Patients with Renal Insufficiency The pharmacokinetics of orally administered VFEND are not significantly affected by renal insufficiency. Therefore, no adjustment is necessary for oral dosing in patients with mild to severe renal impairment (see package insert: CLINICAL PHARMACOLOGY - Special Populations). In patients with moderate or severe renal insufficiency (creatinine clearance <50 mL/min), accumulation of the intravenous vehicle, SBECD, occurs. Oral voriconazole should be administered to these patients, unless an assessment of the benefit/risk to the patient justifies the use of intravenous voriconazole. Serum creatinine levels should be closely monitored in these patients, and, if increases occur, consideration should be given to changing to oral voriconazole therapy (see DOSAGE and ADMINISTRATION). Voriconazole is hemodialyzed with clearance of 121 mL/min. The intravenous vehicle, SBECD, is hemodialyzed with clearance of 55 mL/min. A 4-hour hemodialysis session does not remove a sufficient amount of voriconazole to warrant dose adjustment. Hemodialysis  INTRAVENOUS voriconazole should be avoided. Reference(s) National Institutes of Health, U.S. National Library of Medicine, DailyMed Database. Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here. Disclaimer The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. 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