普乐可复-Prograf
【别名】他克莫司,大环哌南,普乐可复

【外文名】Tacrolimus, Prograf, FK506

【药理作用】在分子水平，他克莫司的作用显然是利用与细胞性蛋白质（FK 12）相结合，而在细胞内蓄积产生效用。FK 12-他克莫司复合物会专一性地结合以及抑制calcinurin，其会抑制T细胞中所产生钙离子依赖型讯息传导路径作用，因此防止不连续性淋巴因子基因的转录。本药是具有高度免疫抑制的药物，其活性在体外及体内实验中都已被证实。本药抑制形成主要移值排斥作用之细胞毒性淋巴球的生成。本药是具有高度免疫抑制的药物，其活性在体外及体内实验中都已被证实。本药抑制形成主要移植排斥作用之细胞毒性淋巴球的生成。本药抑制T细胞的活化作用以及T辅助细胞依赖B细胞的增生作用。也会抑制如白介素-2、白介素-3及γ-干扰素等淋巴因子的生成与白介素-2受体的表达。在分子水平，本药的效应似乎是由结合到细胞性蛋白质（FK ）所产生，此蛋白质也会造成该化合物累积在细胞间。在体内试验中发现，本药显示出对肝脏及肾脏移植有效。

【适应症】肝脏及肾脏移植患者的首选免疫抑制药物，肝脏及肾脏移植后排斥反应对传统免疫抑制方案耐药者，也可选用该药物。
【用法用量】下列口服及静脉注射给药之建议剂量只是概略指标，本药的实际剂量应依据个别病人的需要而加以调整，建议剂量只有起始剂量，因此治疗过程中应藉由临床判断并辅以他克莫司血中浓度的监测以调整剂量。口服给药每日剂量分两次投予。最好是在空腹或至少进食前1hr或进食后2-3hr服用胶囊，以达到最大吸收量。口服胶囊时，通常须连续服用以抑制移植排斥作用。并没有治疗期间的限制。静脉注射给药输注用浓缩液必须在聚乙烯或玻璃瓶中用5%葡萄糖注射或者生理食盐水稀释。所形成的最终输注用溶液的浓度必须在0.004-0.1mg/ml范围间。24hr内输注20-250ml。此溶液不可以一次全量快速注释给药。当患者的状况允许时，应尽快将静脉注射疗法改为口服疗法。静脉注射疗法不应该连续超过7天。首次免疫抑制剂量 - 成人肝脏移植者为0.1-0.2mg/kg/天，肾脏移植患者为0.15-0.3mg/kg/天，分2次口服。应该在肝脏移植手术后约6hr以及肾脏移植手术24hr内开始给药。如果病患的临床状况不适于口服给药。如果病患的临床状况不适于口服给药，则应该给予连续24hr的静脉输注他克莫司治疗。起始静脉注射剂量对肝脏移植患者为0.01-0.05mg/kg/天，而对肾脏移植患者为0.05-0.1mg/kg/天。首次免疫抑制剂量 - 儿童儿童病患通常需要成人建议剂量的1.5-2倍，才能达到相同的治疗血浓度。肝脏及肾脏移植：0.3mg/kg/天，分2次口服。如果不能口服给药时，应该给予连续24hr的静脉输注，对肝脏移植的儿童为0.05mg/kg/天，而对肾脏移植的儿童为0.1mg/kg/天。维持治疗需要口服本药来达到连续免疫抑制作用以维持移植物的生存。在维持治疗中常可减低剂量。主要是根据各病患个体对于排斥及耐受性的临床评估而调整。在病患手术后的恢复期，本药的药物动力学可能会改变，因此需要调整本药的剂量。如果疾病发生变化（例如产生排斥现象），必须考虑更换免疫抑制疗法。增加激素、使用短期的单株/多株抗体以及增加本药的剂量都曾被用来控制排斥发作。如果有中毒征兆（例如明显的不良反应）出现，必须降低本药的剂量。当本药的激素合用时，激素用量通常可以减低，且在少数病例中可以持续地进行单一治疗法。对传统免疫抑制治疗无效如果病患以传本药的治疗应该以该特定移植中首次免疫抑制所建议的初始剂量来开始给药。同时给予环孢素及本药可能会延长环孢素的半衰期，并且产生毒性作用。应该在考虑环孢素的血浓度以及病患的临床状况后，方可开始使用本药治疗。实际上，通常是在停止给予环孢素后12-24hr才开始使用本药。由于环孢素后的清除率可能会受影响，所以在换药后应该监测环孢素的血药浓度。特殊病人肝功能不全之病患；对于手术前或手术后功能不全，如最初移植功能不良的病患可能需要减低剂量。肾功能不全之病患：由于他克莫司的肾清除率很低，所以依据药物动力学的原则是不需要调整剂量。但是由于其潜在肾毒性，所以建议小心监测包括血肌酐、肌酐清除率的计算及排尿量等肾功能。本药的血中浓度不因透析而降低。老年病患有限的经验显示其剂量应同成年患者。

【原产地英文商品名】PROGRAF 5mg/cap 100caps/box
【原产地英文药品名】TACROLIMUS ANHYDROUS
【中文参考商品译名】
提示：以下产品是不同的规格和不同的价格，购买时请以电话咨询为准
·普乐可复 5毫克/胶囊 100胶囊/盒（生产厂家：安斯泰来）
·无水他克莫司(普乐可复仿制药) 5毫克/胶囊 100胶囊/盒
·无水他克莫司(普乐可复仿制药) 0.5毫克/胶囊 100胶囊/盒
·无水他克莫司(普乐可复仿制药) 1毫克/胶囊 100胶囊/盒
·普乐可复 1毫克/胶囊 100胶囊/盒（生产厂家：安斯泰来）
·普乐可复 0.5毫克/胶囊 100胶囊/盒（生产厂家：安斯泰来）
【中文参考药品译名】无水他克莫司
【生产厂家中文参考译名】安斯泰来
【生产厂家英文名】ASTELLAS

Generic Name: tacrolimus

Brand Names: Prograf

What is Prograf?
Prograf lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats it as an invader.

Prograf is used together with other medicines to prevent your body from rejecting a heart, liver, or kidney transplant.

Prograf may also be used for other purposes not listed here.

Important information about Prograf
Taking Prograf may increase your risk of developing certain types of cancer, especially skin cancer. The risk may be higher in people who are treated over long periods of time with drugs that weaken the immune system. Talk with your doctor about your individual risk.

While taking Prograf avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.

There are many other medicines that can interact with Prograf. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.

Do not consume grapefruit or grapefruit juice during treatment with Prograf unless your doctor has told you do. Prograf can have a dangerous interaction with grapefruit or grapefruit juice.

Prograf can lower the blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need to be tested on a regular basis. Your kidney or liver function may also need to be tested. Do not miss any scheduled appointments.

Some people receiving Prograf after a kidney transplant have developed diabetes, most often in people who are Hispanic or African-American. Talk with your doctor about your individual risk of diabetes.

Before taking Prograf
You should not take Prograf if you are allergic to tacrolimus or hydrogenated castor oil.

If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before taking Prograf, tell your doctor if you have:
kidney disease; liver disease; high blood pressure; or
if you have used cyclosporine (Neoral, Sandimmune, Gengraf) within the past 24 hours.

Some people receiving Prograf after a kidney transplant have developed diabetes. This effect has been seen most often in people who are Hispanic or African-American. Talk with your doctor about your individual risk of diabetes if you have concerns.

Taking Prograf may increase your risk of developing certain types of cancer, especially skin cancer. The risk may be higher in people who are treated over long periods of time with drugs that weaken the immune system. Talk with your doctor about your individual risk.
FDA pregnancy category C. It is not known whether Prograf is harmful to an unborn baby. Before taking Prograf, tell your doctor if you are pregnant or plan to become pregnant during treatment. Tacrolimus can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.