部份中文美罗华处方资料（仅供参考）
药品英文名
Rituximab
药品别名
美罗华、利妥昔单抗、科妥昔单抗、MabThera、Rituxan
药物剂型
注射剂：500mg(50ml)，100mg(10ml)。
药理作用
本品与纵贯细胞膜的CD20抗原特异性结合。该抗原位于前B细胞和成熟B淋巴细胞，但在造血干细胞、后B细胞、正常血浆细胞，或其他正常组织中不存在。该抗原表达于95%以上的B淋巴细胞型的非霍奇金淋巴瘤。在与抗体结合后，CD20不被内在化或从细胞膜上脱落。CD20不以游离抗原形式在血流中循环，因此，也就不会与抗原竞争性结合。本品与B淋巴细胞上的CD20结合，并引发B细胞溶解的免疫反应。细胞溶解的可能机制包括补体依赖性细胞毒性(CDC)和抗体依赖性细胞的细胞毒性(ADCC)。此外，体外研究表明，本品可使药物抵抗性的人体淋巴细胞对一些化疗药物的细胞毒敏感。
药动学
给予125mg/m2，250mg/m2或375mg/m2的本品，静脉输注，每周1次，共4次。接受本品者的血清抗体浓度随剂量的增加而上升。在给予375mg/m2的患者中，在第一次输注后，本品的血浆t1/2为68.1h，血药峰值为238.7μg/ml，平均血浆清除率为每小时0.0459L。在第4次输注后，平均血清半衰期最高浓度和血浆清除率分别为每小时189.9，480.7和0.0145L。
此外，本品的血药浓度在缓解患者中的增高具有统计学意义，其典型意义是在3～6个月后仍可测到本品。在第1次给药后，中位外周B淋巴细胞数明显降低至正常水平以下，6个月后开始恢复，在治疗完成的9～12个月后恢复正常。
适应证
主要适用于中低度非霍奇金淋巴瘤，使用前需要对淋巴瘤病理切片进行CD20表达的检测，以求治疗的准确性和保证疗效。适用于复发或化疗抵抗性B淋巴细胞型的非霍奇金淋巴瘤患者。
禁忌证
1.对本品或鼠蛋白过敏者、孕妇、哺乳者禁用。
2.儿童禁用。
注意事项
1.有明显心脏病如心绞痛、心衰、哮喘、低血压等患者慎用。
2.输注速度不可过快，也不可进行静脉注射。
3.用药期间如发生变态反应或其他严重反应，应考虑减量或停药。
4.考虑本品可能引起低血压，因此，在开始使用本品时，应暂停使用抗高血压药或减量。
5.应准备好抢救过敏性休克的措施。
6.血细胞和血小板计数明显下降时，应停药。
7.用药期间，应定期检查血常规和血小板计数。
8.本品不可静脉推注。
9.避光，在2～8℃冰箱中保存。
不良反应
由于接受治疗的患者大多数都曾接受过多种抗癌治疗，其预后均较差，以下列出的不良反应不一定都是使用本品引起的，临床应进行细致分析。
1.与输注直接相关的不良反应有发热、寒战，主要发生在第1次输注中，通常在给药后2h内发生。继而发生荨麻疹、皮疹、疲劳、头痛、瘙痒、支气管痉挛、呼吸困难、舌或喉头水肿(血管神经性水肿)、鼻炎、呕吐、一过性低血压、潮红、心律失常和肿瘤部位疼痛。
2.原有心脏病的发作，如心绞痛和充血性心衰加重。不良反应有可能随继续用药而减轻。
3.少数患者有出血倾向，常较轻且可逆。严重的血小板减少和中性粒细胞减少的发生率为1.8%。严重贫血的发生率为1.4%。
4.全身不良反应还有腹胀、腹痛、背痛、胸痛、颈痛、盗汗、汗多、皮肤干燥和输注部位疼痛。
5.心血管系统的不良反应有高血压、直立性低血压、心动过缓、心动过速、血管扩张。
6.胃肠道可见腹泻、厌食和消化不良。
7.白细胞减少、淋巴结病、高血糖、周围水肿、LDH增高、体重减轻、低血钙和血尿酸升高。
8.关节痛、肌痛、骨痛、张力过高。
9.神经系统的不良反应可见眩晕、焦虑、抑郁、感觉异常、躁动、失眠、精神紧张、嗜睡和神经炎。
10.泪腺分泌紊乱、耳痛、味觉障碍、排尿困难和血尿可能发生。
用法用量
1.作为成年患者的单一治疗药，推荐剂量为375mg/m2，静脉输注前1h先给予止痛药(对乙酰氨基酚)和抗过敏药(苯海拉明)。首剂输注速度为每小时50mg，以后每30分钟增加每小时50mg，最高可达每小时400mg。每周1次，连用4次。
2.如患者耐受，可将输入速度提高为每小时100mg，以后每30分钟增加每小时100mg，最高可达每小时400mg。
药物相应作用
美罗华不可与其他药物混用。
关于美罗华（MabThera/Rituxan）：
美罗华（MabThera/Rituxan）是一种治疗性单克隆抗体，靶向结合正常和恶性B细胞表面的CD20抗原，随后调动人体天然防御，攻击和杀死标记的B细胞。骨髓内的干细胞（B细胞祖细胞）缺乏CD20抗原，从而使健康的B细胞能够在治疗后再生，并在几个月内恢复至正常水平。
MabThera® SC subcutaneous injection
For the treatment of Non-Hodgkin's Lymphoma
pronounced (mab-thir-ra)
contains the active ingredient rituximab (rch)
Consumer Medicine Information
What is in this leaflet
This leaflet answers some common questions about MabThera SC for subcutaneous (under the skin) injection. It does not contain all the available information.
It does not take the place of talking to your doctor or pharmacist.
All medicines have risks and benefits. Your doctor has weighed the risks of you being given MabThera SC against the benefits they expect it will have for you.
If you have any concerns about being given this medicine, ask your doctor or pharmacist.
Keep this leaflet. You may need to read it again.
What MabThera SC is used for
MabThera SC contains the active ingredient rituximab.
MabThera SC belongs to a group of medicines known as anti-cancer agents. There are many different classes of anti-cancer agents. MabThera SC belongs to a class called monoclonal antibodies.
Monoclonal antibodies are proteins which specifically recognise and bind to other unique proteins in the body.
MabThera SC is used to treat non-Hodgkin's lymphoma.
MabThera SC works by binding to a protein on the surface of certain white blood cells known as B lymphocytes. During the process of binding to the protein, the abnormal growth of the B lymphocytes is stopped.
It is the abnormally growing B lymphocytes that are responsible for certain types of non-Hodgkin's lymphoma.
MabThera SC may be used on its own or together with chemotherapy.
If your doctor thinks it is appropriate for your circumstances you may continue to receive MabThera SC after the initial course of treatment.
Your doctor may have prescribed MabThera SC for another reason.
Ask your doctor if you have any questions why MabThera SC has been prescribed for you.
This medicine is available only with a doctor's prescription.
Before you are given MabThera SC
When you must not be given MabThera SC
Do not use MabThera SC:
if you have had an allergic reaction to rituximab or any of the ingredients listed at the end of this leaflet
if you have had an allergic reaction to any other proteins that are of mouse origin
Some of the symptoms of an allergic reaction may include severe skin rash, itching, hives, swelling of the face, lips, mouth or throat which may cause difficulty in swallowing or breathing, swelling of the hands, feet or ankles.
If you are not sure if you should start receiving MabThera SC, talk to your doctor.
Before you are given MabThera SC
Your doctor must know about all the following before you are given MabThera SC.
Tell your doctor if:
1.you have an infection, or a history of a recurring or long-term infection such as hepatitis B
2.you are taking or have previously taken medicines which may affect your immune system, such as chemotherapy or immunosuppressive medicines
If you are taking or have taken medicines which affect your immune system, you may have an increased risk of infections. There have been reports of a rare, serious brain infection called PML (progressive multifocal leuko-encephalopathy) usually affecting people with a weakened immune system. Your chance of getting PML may be higher if you are treated with MabThera SC and/or other medicines that weaken the immune system. PML can cause severe disability or even death.
3.you have a history of heart disease with:
- angina
- cardiac arrhythmias (abnormal beating of the heart)
- congestive heart failure
Your doctor will supervise you closely during treatment with MabThera SC.
4.you are taking medicine to control blood pressure
MabThera SC may cause a reduction in blood pressure at the beginning of treatment. Because MabThera SC may cause a temporary drop in your blood pressure, your doctor may advise you to temporarily stop taking your blood pressure medicine before you are given MabThera SC.
5.you have pre-existing lung disease
You may have a greater chance of breathing difficulties during treatment with MabThera SC.
6.you intend to have or have had immunisation with any vaccine (e.g. measles, rubella, flu, vaccines for travel purposes)
Some vaccines should not be given at the same time as MabThera SC or in the months after you receive MabThera SC. Your doctor will check if you should have any vaccines before you receive MabThera SC.
7.you are allergic to any other medicines or any other substances such as foods, preservatives or dyes
8.you are pregnant or intend to become pregnant
It is not known whether MabThera SC is harmful to an unborn baby. It is not recommended that you are given MabThera SC while you are pregnant.
If you are a woman of child bearing potential, you must use effective contraceptive methods to prevent pregnancy during treatment and for 12 months after completing treatment with MabThera SC.
9.you are breast feeding or plan to breast feed
It is not known if MabThera SC passes into breast milk. It is recommended that you discontinue breast feeding while you are treated with MabThera SC.
If you have not told your doctor about any of the above, tell them before you are given MabThera SC.
Use in children
The safety and effectiveness of MabThera SC have not been established in children.
Taking other medicines
Tell your doctor if you are taking any other medicines including any that you have bought without a prescription from a pharmacy, supermarket or health food shop.
As MabThera SC may cause a temporary drop in your blood pressure at the beginning of treatment, your doctor may advise you to temporarily stop taking your blood pressure medicine before you are given MabThera SC.
It is not known if MabThera SC will affect your normal response to a vaccine.
It is possible that after treatment with MabThera SC you may experience allergic reactions if you are treated with other medications containing monoclonal antibodies.
Your doctor and pharmacist will have more information on medicines to be careful with or to avoid while undergoing treatment with MabThera SC.
How MabThera SC is given
Your treatment with MabThera SC will always begin with an infusion of MabThera intravenous formulation into a vein. If the infusion is tolerated, then further treatment with MabThera SC can be given by subcutaneous injection. This means it is injected with a short needle into the fatty tissue just under the skin.
MabThera SC is given as a fixed dose of 1400 mg per injection. The injection occurs over approximately 5 minutes.
Your doctor will decide on the frequency of injections.
MabThera SC may be given with or without chemotherapy. When given in combination with chemotherapy, the standard treatment with MabThera SC consists of 1 subcutaneous injection on day 1 of each chemotherapy cycle.
MabThera SC must always be administered by a healthcare professional.
Depending on the circumstances of your disease or response to the drug your doctor may decide to change your treatment.
Maintenance treatment
If you respond to initial treatment your doctor may decide to continue your treatment with MabThera SC. You may receive MabThera SC once every 3 months for 2 years.
Overdose
As MabThera SC is given to you under the supervision of your doctor, it is very unlikely that you will receive too much. However, if you experience any side effects after being given MabThera SC, tell your doctor immediately.
While you are receiving MabThera
Things you must do
If you are a woman of child bearing potential, you must use effective contraceptive methods to prevent pregnancy during treatment with MabThera SC and for 12 months after completing treatment.
Tell your doctor if you become pregnant while receiving MabThera SC.
Tell all doctors, dentists and pharmacists who are treating you that you are receiving MabThera SC.
Tell your partner or caregiver you are receiving MabThera SC and ask them to tell you if they notice any changes in your movement or behaviour. If they notice any changes you should tell your doctor about them immediately. Your doctor may need to perform some tests and alter your treatment.
Be sure to keep all your appointments with your doctor so that your progress can be checked. Your doctor will perform regular blood tests.
Thngs you must not do
Do not breast feed your infant during treatment with MabThera SC. It is not known whether MabThera SC crosses into human milk.
Do not take any other medicines whether they require a prescription or not without first telling your doctor or consulting with a pharmacist.
Things to be careful of
Be careful driving or operating machinery until you know how MabThera SC affects you.
MabThera SC generally does not cause any problems with your ability to drive or operate machinery. However, as with many other medicines, MabThera SC may cause dizziness in some people.
Side effects
Tell your doctor or pharmacist as soon as possible if you do not feel well while you are receiving MabThera SC.
Do not be alarmed by this list of possible side effects. You may not experience any of them.
MabThera SC helps many people who have non-Hodgkin's lymphoma but it may have unwanted side effects.
All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.
Your doctor may recommend that you take medication to prevent pain or allergy before you receive your MabThera SC injection.
Ask your doctor or pharmacist to answer any questions you may have.
The following is a list of the more common side effects.
Tell your doctor if you notice any of the following and they worry you:
side effects at the injection site including pain, swelling, bruising, bleeding, skin redness, itching and rash
wheezing or coughing
dizziness or lightheadedness, especially on standing up
nausea (feeling sick) or vomiting
headache
fatigue (feeling tired) and/or feeling weak
fast heart beat
chest pain which may spread to the neck and shoulders
pain where the cancer is located
muscle and joint pain
stomach pain or discomfort
throat irritation
sore mouth or mouth ulcers
bleeding or bruising more easily than normal
shingles (herpes zoster infection)
diarrhoea
increased blood pressure
indigestion
loss of appetite
muscle stiffness
nervousness, feeling anxious or agitated
increased cough
inability to sleep
pins and needles, or decreased feeling in the skin
stuffy nose or chest
sweating or night sweats
watery, itchy or crusty eyes
changes to sense of taste
weight loss
ear pain and/or buzzing, hissing, whistling, ringing or other persistent noise in the ears
constipation
a general feeling of being unwell
unusual hair loss or thinning
Tell your doctor immediately or go to Accident and Emergency at your nearest hospital if you notice any of the following:
severe skin rash, itching, hives
swelling of the face, lips, mouth or throat which may cause difficulty in swallowing or breathing, swelling of the hands, feet or ankles
one or a combination of the following: severe shortness of breath, severe difficulty breathing, severe wheezing, severe coughing
vision loss associated with headaches, confusion and seizures
one or a combination of the following: confusion, disorientation or memory loss, changes in the way you move, walk or talk, decreased strength or progressive weakness in your body, blurred or loss of vision
yellowing of skin and eyes, light coloured bowel motions, dark coloured urine
These are serious side effects. You may need urgent medical attention. Serious side effects are rare.
In combination with chemotherapy
If you have been given MabThera SC in combination with chemotherapy, as well as the side effects listed above, the following additional side effect may also occur:
bronchitis (inflammation in the lungs)
If you are 65 years of age or over and have been given MabThera SC in combination with chemotherapy, the following side effects may occur more commonly:
frequent infections with symptoms such as fever, severe chills, sore throat or mouth ulcers
These events may be related to MabThera SC, but you may get other side effects from your chemotherapy.
Please consult your doctor for possible side effects that may be caused by your chemotherapy.
This is not a complete list of all possible side effects. Your doctor or pharmacist has a more complete list. Others may occur in some people and there may be some side effects not yet known.
Tell your doctor if you notice anything else that is making you feel unwell.
Ask your doctor or pharmacist if you don't understand anything in this list.
Do not be alarmed by this list of possible side effects. You may not experience any of them.
After receiving MabThera SC
Storage
MabThera SC should be stored in the pharmacy or on the hospital ward.
MabThera SC should be kept in a refrigerator at 2-8°C. It should not be frozen.
MabThera SC should be stored away from light.
Product Description
Availability
MabThera SC is available as a 1400 mg/11.7 mL solution for subcutaneous injection in a single dose vial. It is supplied as one vial per carton.
MabThera is also available as a concentrate for intravenous infusion in 100 mg/10 mL and 500 mg/50 mL single dose vials.
What MabThera SC looks like
MabThera SC is available as a clear to opalescent, colourless to yellowish solution.
Ingredients
MabThera SC contains the active ingredient rituximab (rch). Each vial of MabThera SC also contains the following inactive ingredients:
vorhyaluronidase alfa
histidine
histidine hydrochloride
trehalose dihydrate
methionine
polysorbate 80
water for injection
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Distributor
MabThera SC is distributed by:
Roche Products Pty Limited