部份中文霉酚酸酯处方资料（仅供参考） 药理作用 霉酚酸酯(简称MMF)是霉酚酸(MPA)的2-乙基酯类衍生物。MPA是高效、选择性、非竞争性、可逆性的次黄嘌呤单核苷酸脱氢酶(IMPDH)抑制剂，可抑制鸟嘌呤核苷酸的经典合成途径。MPA对淋巴细胞具有高度选择作用。 药代动力学 口服后迅速大量吸收，并代谢为活性成份MPA。口服平均生物利用度为静脉注射的94%(根据MPA曲线下面积)，口服后在循环中测不出MMF。 肾移植病人口服MMF，其吸收不受食物影响，但进食后血MPA峰值将降低40%。由于肠肝循环作用，服药后6-12小时将出现第二个血浆 MPA高峰，与消胆胺同时服用将使MPA曲线下面积减少约40%，表明MPA通过肠肝循环的量很多。在临床有效浓度下，97%的MPA与血浆蛋白结合。 MPA主要通过葡萄糖醛酸转移酶，代谢成MPA的的酚化葡萄糖苷糖(MPAG)，MPAG无药理活性。MMF代谢成的MPA有极少量(<1%)从尿液排出，多数(87%)以MPAG的形式从尿液排出。 移植后近期内(<40日)，平均曲线下面积(AUG)和血峰值(Cmax)比正常志愿者和移植肾功能稳定的病人约低50%。单剂研究显示，严重的慢性肾功能损害(肾小球滤过率<25 mL/分/1.73 m2)。MPA曲线下面积比正常志愿者和轻度肾功能损害病人高25-75%。同样情况下，MPAG曲线下面积高3-6倍，与MPAG主要由肾脏排出一致。尚未进行严重慢性肾功能损害病人的MMF多次剂量药物动力学研究。 移植手术后，肾功能延迟恢复的MPA 0-12小时曲线下面积与无肾功能延迟恢复的者无显著差异。但无活性成分的MPAG，其0-12小时曲线下面积比肾功能正常恢复病人高2-3倍。在酒精性肝硬化志愿者，肝脏实质疾病对MPA的糖苷酸化过程相对无影响，严重的胆道损害，如原发性胆性肝硬化，可能对这一过程产生影响。 适应症 预防同种肾移植病人的排斥反应及治疗难治性排斥反应，可与环孢素和肾上腺皮质激素同时应用。 用法用量 预防排斥剂量: 应于移植72小时内开始服用。肾移植病人服用推荐剂量为1g，1日2次。口服2g/日比口服3g/日安全性更高。 治疗难治性排斥反应: 在临床试验中，治疗难治性排斥的推荐剂量为1.5g/次，2次/日。如果发生中性粒细胞减少(中性粒细胞计数绝对值小于1.3 x103/mL)，应停药或减量。对有严重慢性肾功能损害的病人(肾小球滤过率小于25mL/分/1.73 m2)，应避免超过1g/次，每日2次的剂量(移植后即刻使用除外)。对这些病人应仔细观察。对移植后肾功能延期恢复的病人不需要作剂量调整。 任何疑问,请遵医嘱! 不良反应 服用本药后，主要的不良反应包括：呕吐、腹泻等胃肠道症状，白细胞减少症，败血症，尿频以及某些类型的感染的发生率增加。偶见血尿酸升高、高血钾、肌痛或嗜睡。 禁忌症 对MMF或MPA发生过敏反应的病人不能使用本药。 注意事项 服用本药的病人在第一个月每周1次进行全血细胞计数，第二和第三个月每月2次，余下的一年中每月1次，如果发生中性粒细胞减少(中性粒细胞绝对计数小于1.3x103/uL)时，应停止或减量使用本药，并对这些病人密切观察。 严重慢性肾功能损害(肾小球滤过率小于25mL/分/1.73 m2)的病人服用单剂量后，血浆MPA和MPAG的曲线下面积比轻度肾功能损害的病人及健康人高。应避免使用超过1g/次，每日2次的剂量，并且应对这些病人密切观察。肾移植后肾功能恢复的病人，平均0-12小时 MPA曲线下面积与正常恢复病人相仿。但MPAG的0-12小时曲线下面积前者比后者高2-3倍。对这些肾功能延迟恢复的病人无须作剂量调整，但应密切观察。 接受免疫抑制疗法的病人常使用联合用药方式。本药作为联合应用免疫抑制药物时，有增加淋巴瘤和其它恶性肿瘤(特别是皮肤瘤)发生的危险。这一危险性和免疫抑制的强度和持续时间有关，孕妇及哺乳期妇妇用药中应为是否可从人乳中分泌尚不清楚。免疫系统的过度抑制也可能导致对感染的易感性增加。 临床试验中，本药已与以下药物联合应用：抗淋巴细胞球抗体、环孢素和皮质激素类药物，以预防排斥反应和治疗难治性排斥反应。 孕妇及哺乳期妇女用药 动物实验中发现本药有致胎儿畸形的可能。尽管还未对孕妇作充分和良好的对照研究，只有在本药的潜在优点超过对胎儿的潜在危险时方予应用。应在妊娠试验阴性后，才开始服用本药。服用本药期间，应采取有效避孕措施。对大鼠的研究发现MMF可通过乳汁分泌，是否可从人乳中分泌骁尚不清楚，并且，MMF能对哺乳期婴儿可能有潜在的严重副作用，应根据MMF对于母亲的重要性作出用药决定。 儿童用药 儿童使用该药的安全性和有效性尚未确证。 药物相互作用 不能与硫唑嘌呤同时使用，对这两种药物的同时使用尚未进行试验。 已注意到消胆胺能显著减少MPA线曲下面积。 本药不应与能干扰肠肝再循环的药物同时使用，因这些药物可能会降低本药的药效。和阿昔洛韦同时服用时，MPAG和阿昔洛韦 的血浆浓度较两种药物单独服用时为高。当肾功损害时，MPAG和阿昔洛韦的血浆浓度都升高。这两种药物竞争性地通过肾小管排出，可能会进一步增加两种药物的浓度。 制酸药物和氢氧化镁以及氢氧化铝：同时服用制酸剂时，MMF的吸收减少。 消胆胺： 健康人先期服用消胆胺4g/次，每日3次，4日后给予单剂量MMF 1.5g，MPA的曲线下面积减少40%。 环孢素A的药物动力学不受MMF的影响。 更昔洛韦： 未观察到MMF和静脉注射更昔洛韦之间有药物动力学的交叉作用。 口服避孕药： 目前尚未发现MMF和口服避孕药1 mg炔诺酮/35 ug炔雌醇之间有相互影响。但这只是单次剂量研究所得出的结论，并不能排除长期服用本药后改变口服避孕药的药物动力学的可能性。这可能导致口服避孕药的药效降低。 磺胺甲基异唑：对MPA的生物利用度无影响。 其它药物： 给猴子同时服用丙磺舒和MMF，可使血浆MPAG曲线下面积增加3倍。为此，其它经肾小管排出的药物可与MPAG竞争，从而使血浆MPAG或这些药物的浓度升高。 药物过量 在人类尚无MMF剂量过大的报道。血透不能清除MPA，而当MPA 血浆浓度极高时(>100 ug/mL)，能清除小部分MPAG。MPA可通过药物排出增加(如给予消胆胺)而得到清除。 ------------------------------------------------------ 注：以下产品美国上市包装，不同剂型（规格），采购以咨询为准 ------------------------------------------------------ CellCept(mycophenolate mofetil)capsules, tablets, oral suspension and injection CELLCEPT 500MG SDV PWD 4/PAC  MYCOPHENOLATE MOFETIL     00004-0298-09 CELLCEPT CAP 250MG 100  MYCOPHENOLATE MOFETIL     00004-0259-01  CELLCEPT CAP 250MG 500=  MYCOPHENOLATE MOFETIL     00004-0259-43  CELLCEPT IV 500MG 20ML 4  MYCOPHENOLATE MOFETIL HCL     00004-0298-09 CELLCEPT O/S 200MG/ML 160ML  MYCOPHENOLATE MOFETIL     00004-0261-29   CELLCEPT TAB 500MG 100  MYCOPHENOLATE MOFETIL     00004-0260-01  CELLCEPT TAB 500MG 500=  MYCOPHENOLATE MOFETIL     00004-0260-43  CellCept(mycophenolate mofetil) Indication CellCept® (mycophenolate mofetil) is indicated for the prophylaxis of organ rejection in patients receiving allogeneic renal, cardiac, or hepatic transplants. CellCept should be used concomitantly with cyclosporine and corticosteroids. CellCept Intravenous is an alternative dosage form to CellCept capsules, tablets, and oral suspension. CellCept Intravenous should be administered within 24 hours following transplantation. CellCept Intravenous can be administered for up to 14 days; patients should be switched to oral CellCept as soon as they can tolerate oral medication. Important Safety Information Including BOXED WARNINGS WARNING: EMBROYOFETAL TOXICITY, MALIGNANCIES, AND SERIOUS INFECTIONS Use during pregnancy is associated with increased risks of first trimester pregnancy loss and congenital malformations. Females of reproductive potential (FRP) must be counseled regarding pregnancy prevention and planning. Immunosuppression may lead to increased susceptibility to infection and possible development of lymphoma. Only physicians experienced in immunosuppressive therapy and management of renal, cardiac, or hepatic transplant patients should prescribe Cellcept. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient. CONTRAINDICATIONS CellCept is contraindicated in patients with a hypersensitivity to mycophenolate mofetil, mycophenolic acid or any component of the drug product. CellCept Intravenous is contraindicated in patients who are allergic to Polysorbate 80 (TWEEN). WARNINGS •Pregnancy category D: Mycophenolate mofetil (MMF) can cause fetal harm when administered to a pregnant female. Use of MMF during pregnancy is associated with an increased risk of first trimester pregnancy loss and an increased risk of congenital malformations, especially external ear and other facial abnormalities including cleft lip and palate, and anomalies of the distal limbs, heart, esophagus, kidney, and nervous system. Females of reproductive potential must be made aware of the increased risk of first trimester pregnancy loss and congenital malformations and must be counseled regarding pregnancy prevention and planning •Patients receiving immunosuppressive regimens involving combinations of drugs, including CellCept, as part of an immunosuppressive regimen are at increased risk of developing lymphomas and other malignancies, particularly of the skin •CellCept has been administered in combination with the following agents in clinical trials: antithymocyte globulin, OKT3, cyclosporine, and corticosteroids. The efficacy and safety of the use of CellCept in combination with other immunosuppressive agents have not been determined •Because of the danger of oversuppression of the immune system which can increase susceptibility to infection, which may lead to serious, including fatal outcomes, combination immunosuppressant therapy should be used with caution •Polyomavirus associated nephropathy (PVAN), JC virus associated progressive multifocal leukoencephalopathy (PML), cytomegalovirus (CMV) infections, reactivation of hepatitis B (HBV) or hepatitis C (HCV) have been reported in patients treated with immunosuppressants, including CellCept. Reduction in immunosuppression should be considered for patients who develop evidence of new or reactivated viral infections. Physicians should also consider the risk that reduced immunosuppression represents to the functioning allograft •Monitor patients for neutropenia. If neutropenia develops [absolute neutrophil count (ANC) •Cases of pure red cell aplasia (PRCA) have been reported in patients treated with CellCept in combination with other immunosuppressive agents •CAUTION: CELLCEPT INTRAVENOUS SOLUTION MUST NOT BE ADMINISTERED BY RAPID OR BOLUS INTRAVENOUS INJECTION PRECAUTIONS •Females of reproductive potential must be made aware of the increased risk of first trimester pregnancy loss and congenital malformations and must be counseled regarding pregnancy prevention and planning ◦Pregnancy Testing: a serum or urine pregnancy test with a sensitivity of at least 25 mIU/mL must be administered immediately before starting CellCept. Another pregnancy test with the same sensitivity should be done 8 to 10 days later. Repeat pregnancy tests should be performed during routine follow-up visits. In the event of a positive pregnancy test, females should be counseled with regard to whether the maternal benefits of mycophenolate treatment may outweigh the risks to the fetus in certain situations, please report the pregnancy to Mycophenolate Pregnancy Registry (1-800-617-8191) ◦Contraception: Patients taking CellCept must receive contraceptive counseling and use acceptable contraception (see Table 8 of the full Prescribing Information for acceptable contraception methods). Patients must use acceptable birth control during entire CellCept therapy, and for 6 weeks after stopping CellCept, unless the patient chooses abstinence •CellCept may be used for cardiac or hepatic transplant patients with severe chronic renal impairment if the potential benefits outweigh the potential risks •A higher incidence of opportunistic infections was observed in cardiac transplant patients treated with CellCept than in those receiving azathioprine therapy •CellCept should not be administered concomitantly with azathioprine and used with caution when used in the concomitant administration with drugs that interfere with enterohepatic recirculation •CellCept should be avoided in patients with rare hereditary deficiency of hypoxanthine-guanine phosphoribosyl-transferase (HGPRT) such as Lesch-Nyhan or Kelley-Seegmiller syndrome •Gastrointestinal bleeding (requiring hospitalization) has been observed •During treatment with CellCept, avoid the use of live attenuated vaccines and advise patients that vaccinations may be less effective •Care should be taken if CellCept Oral Suspension is administered to patients with phenylketonuria ADVERSE REACTIONS •The principal adverse reactions associated with the administration of CellCept include diarrhea, leukopenia, sepsis, vomiting, and there is evidence of a higher frequency of certain types of infections, eg, opportunistic infections (see WARNINGS in full Prescribing Information). Phlebitis and thrombosis have been reported with intravenous administration. Please refer to the full Prescribing Information for additional ADVERSE REACTIONS. CellCept(mycophenolate mofetil)capsules, tablets, oral suspension and injection How is CellCept Supplied CellCept (mycophenolate mofetil capsules) 250 mg Blue-brown, two-piece hard gelatin capsules, printed in black with "CellCept 250" on the blue cap and "Roche" on the brown body. Supplied in the following presentations: NDC Number Size NDC 0004-0259-01 Bottle of 100 NDC 0004-0259-05 Package containing 12 bottles of 120 NDC 0004-0259-43 Bottle of 500 Storage Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). CellCept (mycophenolate mofetil tablets) 500 mg Lavender-colored, caplet-shaped, film-coated tablets printed in black with "CellCept 500" on one side and "Roche" on the other. Supplied in the following presentations: NDC Number Size NDC 0004-0260-01 Bottle of 100 NDC 0004-0260-43 Bottle of 500 Storage and Dispensing Information Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). Dispense in light-resistant containers, such as the manufacturer's original containers. CellCept Oral Suspension (mycophenolate mofetil for oral suspension) Supplied as a white to off-white powder blend for constitution to a white to off-white mixed-fruit flavor suspension. Supplied in the following presentation: NDC Number Size NDC 0004-0261-29 225 mL bottle with bottle adapter and 2 oral dispensers Storage Store dry powder at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). Store constituted suspension at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) for up to 60 days. Storage in a refrigerator at 2° to 8°C (36° to 46°F) is acceptable. Do not freeze. CellCept Intravenous (mycophenolate mofetil hydrochloride for injection) Supplied in a 20 mL, sterile vial containing the equivalent of 500 mg mycophenolate mofetil as the hydrochloride salt in cartons of 4 vials: NDC Number NDC 0004-0298-09 Storage Store powder and reconstituted/infusion solutions at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). https://www.drugs.com/pro/cellcept.html