部份中文霉酚酸酯处方资料（仅供参考）
商品名：CELLCEPT Oral Suspension
英文名：Mycophenolate Mofetil
中文名：霉酚酸酯口服混悬液
生产商：中外制药
セルセプトカプセル250/セルセプト懸濁用散31.8%
药用分类名称
免疫抑制剂
批准日期：2015年 12月
商標名
CELLCEPT Capsules
CELLCEPT Powder for Oral Suspension
一般的名称
ミコフェノール酸モフェチル（Mycophenolate Mofetil）（JAN）
化学名
2-morpholinyl（E）-6-（1,3-dihydro-4-hydroxy-6-methoxy-
7-methyl-3-oxoisobenzofuran-5-yl）-4-methyl-4-hexenoate
分子式
C23H31NO7
分子量
433.49
性状
它是白色结晶粉末。N，容易溶于N-二甲基甲酰胺，容易溶于醋酸盐，不易溶于甲醇，不易溶于乙醇（95）和二乙醚，几乎不溶于水。
化学構造式
熔融范围
94~98°C（熔融起始点和熔融端之间的差值在2.5°C以内）
处理注意事项
胶囊，避免潮湿和保存。
批准条件
制定并适当实施药品风险管理计划。
药效药理
作用机制
米科酚酸莫菲耶尔在体内迅速水解到MPA中。MPA，在denovo系统，在两个纯生物合成通路中，通过抑制肌酰胺单磷酸脱氢酶，这是denovo通路的调节酶，通过抑制不竞争、可逆和特异性，GTP，脱氧GTP，抑制DNA合成。 T、B淋巴细胞主要依赖于核酸合成，而免疫系统以外的细胞则依赖于de novo和salvage系统。由于MPA对salvage酶没有影响，因此选择性地抑制淋巴细胞的生长，诱导器官移植后出现排斥的发育不良。
免疫药理作用
体外测试
人类淋巴细胞系的生长，人类外周血淋巴细胞和脾血B淋巴细胞的生长和抗体生产，以及人类淋巴细胞的混合淋巴细胞反应被强烈抑制。 另一方面，人类成纤维细胞，脐带内皮细胞的生长抑制是温和的。
在vivo試験中
诱导抑制小鼠细胞毒性T淋巴细胞的诱导，抑制敏化小鼠和大鼠脾脏的抗体生产抑制，脾切除术大鼠的血液自然抗体产生能力降低，敏化小鼠淋巴结，显示脾脏DNA合成的特定抑制。
移植免疫抑制作用
在动物同种器官移植中，观察到渐进性急性排斥的改善（犬肾、大鼠心脏和小肠）。此外，抑制急性排斥，延长移植器官片的出生和存活时间，通过与其他剂联合施用来增强免疫抑制作用（狗肾、肝脏、大鼠心脏、小肠、小鼠胰腺）。此外，在大鼠血管炎模型中的冠状动脉炎，抑制了内膜生长和增厚。
适应症
肾移植后难治性排斥的治疗
（由于无效或副作用等原因，现有治疗剂无法施用，如果被诊断为难治性排斥）
抑制以下器官移植中的排斥
肾脏移植、心脏移植、肝移植、肺移植、胰腺移植
狼疮肾炎
用法与用量
肾移植
肾移植后难治性排斥的治疗
通常，成人每餐后口服1500mg，每天两次，每次12小时。
此外，年龄，适当增加或减少症状。
肾移植中排斥的抑制
成人：通常，每餐后口服1000mg作为每天2次，每次12小时。
另外，年龄，但适当增加或减少的症状，每天3，000mg上限。
儿童：通常，每餐后口服300~600mg/m2，每天2次，每次12小时。
另外，年龄，但适当增加或减少的症状，每天2，000mg上限。
心脏移植、肝移植、肺移植和胰腺移植的排斥抑制
通常，成人每天每餐后口服500至1，500mg，每天两次。
然而，由于该剂的耐药量和有效量因患者而异，因此需要仔细增加或减少剂量，以获得最佳的治疗效果。
狼疮肾炎
成人：通常，每餐后口服250~1，000mg，每天2次，每次12小时。
另外，年龄，但适当增加或减少的症状，每天3000mg上限。
儿童：通常，每餐后口服150~600mg/m2，每天2次，每次12小时。
另外，年龄，但适当增加或减少的症状，每天2，000mg上限。
包装
胶囊250
100粒（PTP10胶囊x10）
100粒（瓶装）
口服混悬液 31.8%
110克（瓶）
制造供应商
中外制药有限公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：http://www.info.pmda.go.jp/go/pack/3999017B1025_1_11/
CELLCEPT Powder for Oral Suspension 31.8%（セルセプト懸濁用散31.8％）
Brand name : CELLCEPT Powder for Oral Suspension 31.8%
　Active ingredient: Mycophenolate mofetil
　Dosage form: white powder
　Print on wrapping:
Effects of this medicine
This medicine controls immune function by suppressing lymphocyte growth.
It is usually used to treat refractory rejection after renal transplant (when you do not respond to the existing medicines, or can not be treated due to side effects, and when the rejections are diagnosed as refractory), to suppress rejection in renal/heart/liver/lung/pancreas transplant and for Lupus nephritis.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you are a patient with digestive disease, chronic renal failure, phenylketonuria or hereditary fructose intolerance.
If your renal function is showing slow recovery after renal transplant.
•If you are pregnant, possibly pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is <<        to be written by a healthcare professional>>
•To treat refractory rejection after renal transplant: In general, for adults, take 1,500 mg of the active ingredient at a time, twice a day, every 12 hours after meals. It should be adjusted according to the age and symptoms.
To suppress rejection after renal transplant: In general, for adults, take 1,000mg of the active ingredient at a time, twice a day, every 12 hours after meals. It should be adjusted according to the age and symptoms. The maximum dosage is 3,000mg of the active ingredient a day. In general, for children, take 300 to 600mg/m2 of the active ingredient at a time, twice a day, every 12 hours after meals. It should be adjusted according to the age and symptoms. The maximum dosage is 2,000mg of the active ingredient a day.
To suppress rejection after heart/liver/lung/pancreas transplant: In general, for adults, take 500 to 1,500mg of the active ingredient at a time, twice a day, every 12 hours after meals. The tolerance dose and the effective dose vary according to each patient. The dosage should be carefully adjusted to obtain the optimum curative effect.
Lupus nephritis: In general, for adults, take 250 to 1,000mg of the active ingredient at a time, twice a day, every 12 hours after meals. It should be adjusted according to the age and symptoms. The maximum dosage is 3,000mg of the active ingredient a day. In general, for children, take 150 to 600mg/m2 of the active ingredient at a time, twice a day, every 12 hours after meals. It should be adjusted according to the age and symptoms. The maximum dosage is 2,000mg of the active ingredient a day.
This medicine is a made-up suspension by adding purified water to the powder at the pharmacy/healthcare facility. 1 mL of made-up suspension contain 200mg of the active ingredient.
Strictly follow the instructions in any case.
•The maximum dosage for severe chronic renal failure is 1,000mg of the active ingredient at a time, twice a day.
•If you miss a dose, take the missed dose as soon as possible. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist immediately.
•Do not stop taking this medicine unless your doctor instructs you to do so. (Your life can be endangered by discontinuing the medicine, or adjusting the dose on your own just because you feel better.)
Precautions while taking this medicine
•In using the medicine, you and your family need to be informed of these precautions as follows until everyone fully understands them.
-Teratogenic action (possibility to cause fetal malformation) has been reported in humans. If you have a possibility to become pregnant, pregnancy test will be performed before use of the medicine in order to confirm that you are not already pregnant. You must avoid pregnancy and confirm that you do not become pregnant before/during use of the medicine and for 6 weeks after discontinuing it. If you think you may be pregnant, tell your doctor immediately.
-Contact your doctor immediately when you notice that you are having infectious symptoms, oblivious bruise, internal bleeding, bleeding, anemia, and diarrhea.
-In order to avoid the risk of skin cancer caused by sunlight/ultraviolet rays, put on clothes such as a hat and effective sunscreen.
•While taking the medicine, you may have to take a blood test frequently.
•Avoid breastfeeding.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include diarrhea, cytomegalus virus infection, pneumonia, herpes zoster and anemia. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•cold-like symptoms, general dullness, fever, vomiting [infection]
•absent-mindedness, impaired mind, memory loss, loss of consciousness, paralysis of the limbs, difficulty speaking, convulsion [progressive multifocal leukoencephalopathy]
•general dullness, headache, fever, swelling, lower abdominal pain, frequent urination, feeling of residual urine, bloody urine, decreased urinary volume [BK virus associated nephropathy]
•general dullness, dizziness, palpitation, shortness of breath, headache, fever, sore throat, ear ringing, nose/gum/subcutaneous bleeding, bleeding tendency, blue spot, continuous bleeding [pancytopenia, neutropenia, agranulocytosis, leukopenia, thrombocytopenia, anemia, pure red cell aplasia]
•swollen lymph node, night sweat, fever, weight loss, loss of appetite, bleeding tendency, anemia [malignant lymphoma, lymphoproliferative disease]
•itchy/painful/bleeding/growing mole, red-brown scab, mole turning into ulcer [malignancy (especially on the skin)]
•bloody/black stool, feeling sick at the stomach, nausea, vomiting, vomiting of blood, stomachache, severe abdominal pain, failure of passing stool/gas [gastrointestinal ulcer, gastrointestinal bleeding, perforation of the digestive tract, ileus]
•sweat, muddy stool, watery stool, severe abdominal pain, nausea [severe diarrhea]
•impaired mind/judgment, decreased consciousness, dull headache, hyperventilation, breathing difficulty, brief cessation of breathing, dizziness, shaky hands and legs, feeling of weariness, general dullness, decreased urinary volume, thirst [acidosis, hypoxia, dehydration]
•excess intake of water, increased urinary volume, general dullness, weight loss, thirst [diabetes]
•nausea, vomiting of blood, enlarged feeling of abdomen, vomiting, chest pain, chest constrictive/oppressive feeling, severe abdominal/leg pain, bleeding, sensory numbness [thrombosis]
•fever, decreased urinary volume, headache, loss of appetite, dry mouth, swollen hands and legs/face [serious renal disorder]
•easy breathing in upright position, breathing difficulty, shortness of breath, swollen body, general dullness, easy fatigability, loss of appetite, palpitation, chest pressured/constrictive feeling, cold sweat, chest pain, loss of consciousness, cessation of breathing [cardiac failure, angina, pulmonary hypertension, pericardial effusion collection, cardiac arrest]
•disturbed pulse, chest disorder feeling, chest uncomfortable feeling, chest pain, palpitation, decreased consciousness, dizziness, faint, shortness of breath [arrhythmia (extrasystole, atrial fibrillation, atrial flutter, supraventricular/ventricular tachycardia, etc.)]
•yellowness in the skin and/or the white of the eye, dark urine, vomiting, nausea, loss of appetite, itch, general dullness [hepatic function disorder, jaundice]
•shortness of breath, breathing difficulty, nausea, vomiting, easy breathing in upright position, cessation of breathing for more than 10 seconds, chest pain [pulmonary edema, apnea, pneumothorax]
•convulsion, confused/disturbed consciousness, impaired mind, seeing or hearing something that is not really there, inability to get along with others, bad temper, good mood, inability to control emotion [convulsion, confusion, hallucination,psychosis]
•asthma, hives, stuffy/runny nose, itchy eye, sneeze [allergic reaction]
•inability to hear voices/sounds, difficulty hearing, ear ringing [hearing loss]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep out of the reach of children. Store at room temperature (1 to 30℃), away from direct sunlight. It can be stored in the refrigerator. Avoid freezing.
•Use the made-up suspension within 60 days. The expiration date will be written on the bottle label.
•Discard the remainder. Do not store them. Ask the pharmacist or healthcare facility how to discard them.
Chugai Pharmaceutical Co., Ltd.Internal
Published: 8/2016
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.