部份中文氯吡格雷资料（仅供参考）
药品英文名
Clopidogrel
药品别名
硫酸氯吡格雷、波立维、氯匹多瑞、泰嘉、ClopidogrelBisulfate、Plavix
药物剂型
片剂：25mg，75mg。
药理作用
本品是ADP诱导的血小板聚集的抑制剂，它是通过直接抑制二磷酸腺苷与其结合以及继发ADP介导的糖尿病GPⅡb/Ⅲa复合物活化而起作用的。硫酸氢氯吡格雷的分子量为419.9。氯吡格雷必须经生物转化才能抑制血小板的聚集，但是还没有分离出产生这种作用的活性代谢产物，除了ADP外，氯吡格雷还能通过阻断由释放的ADP引起的血小板活化的扩增，抑制其他的激动剂诱导的血小板聚集，氯吡格雷不能抑制碳酸二酯酶的活性。氯吡格雷还通过不可逆的修饰血小板ADP起作用，暴露于氯吡格雷的血小板的寿命受到影响。
药动学
本品的血小板抑制是剂量依赖性的。从第一天起，每天重复给本品75mg，抑制ADP诱导血小板聚集，抑制作用在3～5天达到稳态。在稳态，每天服用本品75mg平均抑制水平维持在40%～60%，在治疗终止后一般在5天内血小板聚集和出血时间逐渐回到基线。在多次口服本品75mg以后，没有血小板抑制活性的母体化合物的血浆浓度很低。主要由肝脏代谢，血中代谢产物主要是羧酸盐衍生物，其对血小板聚集也无影响，占血浆中药物相关化合物的85%。在人体口服14C标记的氯吡格雷以后，在5天内约有50%由尿液排除，约46%由粪便排出，一次和重复给药后，血浆中主要的代谢产物的消除半衰期为8h，与血小板共价结合的占放射性标记的2%，其半衰期为11天。
适应证
预防和治疗因血小板高聚集状态引起的心、脑及其他动脉的循环障碍疾病，如近期发作的脑卒中、心肌梗死和确诊的外周动脉疾病。可减少动脉粥样硬化性疾病发生(心肌梗死、卒中和血管疾病所致死亡)。
禁忌证
1.对本药成分过敏者。
2.严重的肝功能损害。
3.近期活动性病理性出血，如消化性溃疡或颅内出血。
4.急性心肌梗死最初几天。
5.肾功能不全或有尿结石患者禁用。
6.活动性消化溃疡患者禁用。
注意事项
1.慎用：
(1)不稳定型心绞痛、经皮穿刺冠状动脉内支架安置术、冠状动脉旁路移植术等；
(2)急性缺血性脑卒中(发病时间少于7天)；
(3)由于创伤、手术或其他病理原因而可能引起出血增多以及有伤口(特别是在胃肠道和眼内)易出血的患者；
(4)服用易出现胃肠道损伤药物(如非甾体解热镇痛药)的患者；
(5)肾功能损害者；
(6)孕妇及哺乳期妇女。
2.择期手术患者可在术前1周停止使用本药。
3.本药无专用的解毒药。如果需要迅速恢复正常的出血时间，可进行血小板输注以拮抗本药的药理作用。
4.药物对老人的影响：老年人在血浆中主要代谢物浓度明显高于年轻健康志愿者，但较高的血浆浓度与血小板聚集及出血时间的差异无关，故没有必要对老年人调整剂量。
5.用药前后及用药时应当检查或监测白细胞和血小板计数。
不良反应
1.血液系统：常见出血，包括胃肠道出血、紫癜、血肿、鼻出血、血尿和眼部出血(主要是结膜出血)。偶见颅内出血，严重血小板减少。罕见严重中性粒细胞减少，血栓性血小板减少性紫癜。有引起再生障碍性贫血的报道。
2.胃肠道：常见腹痛、消化不良、恶心、胃炎、腹泻和便秘等，偶见胃及十二指肠溃疡。
3.皮肤：常见皮疹、斑丘疹、红斑疹、荨麻疹及皮肤瘙痒。
4.中枢和周围神经系统：常见头痛、眩晕和感觉异常等。
5.其他：偶见支气管痉挛、血管性水肿或类过敏性反应。
用法用量
口服给药：每次50mg或75mg，每天1次，可与食物同服也可单独服用。
药物相应作用
1.与华法林同用可增加出血的危险，服用本药时不推荐同时使用华法林。
2.与萘普生、阿司匹林同用可能增加胃肠道出血的潜在危险性。
3.与月见草油、姜黄素、辣椒辣素、黑叶母菊、银杏属、大蒜、丹参等合用，可增加出血的危险性。
4.本品与肝素并用应慎用。
5.本品高浓度可抑制CyP2C9，使苯妥英钠，甲苯磺丁脲，氟伐他丁及甾体抗炎药的代谢降低，从而使后者的毒性增强，应予注意。
6.可增强其他口服抗凝剂的抗凝血酶原作用。
临床研究
国外报道，有一双盲、对照、多中心的临床研究中，19 185例血栓栓塞患者分成两组，分别应用本品或阿司匹林，每次75mg，每天1次，或阿司匹林每次0.325g，每天1次，随访3年，结果两组在降低脑缺血性卒中，心肌梗死及血管病变的致死亡率方面，本品为5.32%，后者为5.83%，本品优于阿司匹林。
本品的药理作用与噻氯匹啶相类似，优点为起效快、不良反应相对轻微，特别是对骨髓抑制作用轻微，较少引起粒细胞减少症。氯吡格雷疗效略高于阿司匹林，不良反应轻微，但价格十分昂贵，主要适应证为不能耐受阿司匹林的心脑血管疾病患者。
Grepid 75 mg film-coated tablets
What is it and how is it used?
Grepid belongs to a group of medicines called antiplatelet medicinal products. Platelets are very small structures in the blood which clump together during blood clotting. By preventing this clumping, antiplatelet medicinal products reduce the chances of blood clots forming (a process called thrombosis).
Grepid is taken to prevent blood clots (thrombi) forming in hardened blood vessels (arteries), a process known as atherothrombosis, which can lead to atherothrombotic events (such as stroke, heart attack or death).
You have been prescribed Grepid to help prevent blood clots and reduce the risk of these severe events because:
you have a condition of hardening of arteries (also known as atherosclerosis), and
you have previously experienced a heart attack, stroke or have a condition known as peripheral arterial disease.
What do you have to consider before using it?
Do not take Grepid
if you are allergic (hypersensitive) to clopidogrel or any of the other ingredients of Grepid
if you have a medical condition that is currently causing bleeding such as a stomach ulcer or bleeding within the brain
if you suffer from severe liver disease.
If you think any of these apply to you, or if you are in any doubt at all, consult your doctor before taking Grepid.
Take special care with Grepid
If any of the situations mentioned below apply to you, you should tell your doctor before taking this Grepid:
if you have a risk of bleeding, such as
a medical condition that puts you at risk of internal bleeding (such as a stomach ulcer).
a blood disorder that makes you prone to internal bleeding (bleeding inside any tissues, organs or joints of your body)
a recent serious injury
a recent surgery (including dental).
a planned surgery (including dental) in the next seven days
if you have had a clot in an artery of your brain (ischaemic stroke) which occurred within the last seven days
if you have kidney or liver disease
While you are taking Grepid:
You should tell your doctor if a surgery (including dental) is planned.
You should also tell your doctor immediately if you develop a medical condition (also known as Thrombotic Thrombocytopenic Purpura or TTP) that includes fever and bruising under the skin that may appear as red pinpoint dots, with or without unexplained extreme tiredness, confusion, yellowing of the skin or eyes (jaundice) (see section 4 ‘POSSIBLE SIDE EFFECTS’).
If you cut or injure yourself, it may take longer than usual for bleeding to stop. This is linked to the way your medicine works as it prevents the ability of blood clots to form. For minor cuts and injuries e.g., cutting yourself, shaving, this is usually of no concern. However, if you are concerned by your bleeding, you should contact your doctor straightaway (see section 4 ‘POSSIBLE SIDE EFFECTS’).
Your doctor may order blood tests.
Clopidogrel is not intended for use in children or adolescents.
Taking other medicines
Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including medicines obtained without a prescription.
Some other medicines may influence the use of Grepid or vice versa.
You should specially tell your doctor if you take:
oral anticoagulants, medicines used to reduce blood clotting
a non-steroidal anti-inflammatory medicine, usually used to treat painful and/or inflammatory conditions of muscles or joints
heparin or any other injectable medicine used to reduce blood clotting
omeprazole, esomeprazole or cimetidine, medicines to treat upset stomach
fluconazole, voriconazole, ciprofloxacin, or chloramphenicol, medicines to treat bacterial and fungal infections
fluoxetine, fluvoxamine, or moclobemide, medicines to treat depression
carbamazepine or oxcarbazepine, medicines to treat some forms of epilepsy
ticlopidine, other antiplatelet agent.
An occasional use of acetylsalicylic acid (not more than 1000 mg in 24 hour period) should generally not cause a problem, but prolonged use in other circumstances should be discussed with your doctor.
Taking Grepid with food and drink
Grepid may be taken with or without food.
Pregnancy and breast-feeding
It is preferable not to take this product during pregnancy.
If you are pregnant or suspect that you are pregnant, you should tell your doctor or pharmacist before taking Grepid. If you become pregnant while taking Grepid, consult your doctor immediately as it is recommended not to take clopidogrel while you are pregnant.
You should not breastfeed while taking this medicine.
If you are breastfeeding or planning to breastfeed, talk to your doctor before taking this medicine.
Ask your doctor or pharmacist for advice before taking any medicine.
Driving and using machines
Grepid is unlikely to affect your ability to drive or to use machines.
Important information about some of the ingredients of Grepid
Grepid contains lactose. If you have been told by your doctor that you have an intolerance to some sugars (e.g. lactose), contact you doctor before taking this medicine.
How is it used?
Always take Grepid exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.
The usual dose is one 75 mg tablet of Grepid per day to be taken orally with or without food and at the same time each day.
You should take Grepid for as long as your doctor continues to prescribe it.
If you take more Grepid than you should
Contact your doctor or the nearest hospital emergency department because of the increased risk of bleeding.
If you forget to take Grepid
If you forget to take a dose of Grepid, but remember within 12 hours of your usual time, take your tablet straightaway and then take your next tablet at the usual time.
If you forget for more than 12 hours, simply take the next single dose at the usual time. Do not take a double dose to make up for the forgotten individual doses.
If you stop taking Grepid
Do not stop the treatment unless your doctor tells you so. Contact your doctor or pharmacist before stopping.
If you have any further questions on the use of this product, ask your doctor or pharmacist.
What are possible side effects?
Like all medicines, Grepid can cause side effects, although not everybody gets them.
The frequency of possible side effects listed below is defined using the following convention:
very common (affects more than 1 user in 10)
common (affects 1 to 10 users in 100)
uncommon (affects 1 to 10 users in 1,000)
rare (affects 1 to 10 users in 10,000)
very rare (affects less than 1 user in 10,000)
not known (frequency cannot be estimated from the available data) Contact your doctor immediately if you experience:
fever, signs of infection or extreme tiredness. These may be due to rare decrease of some blood cells.
signs of liver problems such as yellowing of the skin and/or the eyes (jaundice), whether or not associated with bleeding which appears under the skin as red pinpoint dots and/or confusion (see section 2 ‘Take special care with Grepid’).
swelling in the mouth or skin disorders such as rashes and itching, blisters of the skin. These may be the signs of an allergic reaction.
The most common side effect reported with Grepid is bleeding. Bleeding may occur as bleeding in the stomach or bowels, bruising, haematoma (unusual bleeding or bruising under the skin), nose bleed, blood in the urine. In a small number of cases, bleeding in the eye, inside the head, the lung or the joints has also been reported.
If you experience prolonged bleeding when taking Grepid
If you cut or injure yourself, it may take longer than usual for bleeding to stop. This is linked to the way your medicine works as it prevents the ability of blood clots to form. For minor cuts and injuries e.g., cutting yourself, shaving, this is usually of no concern. However, if you are concerned by your bleeding, you should contact your doctor straightaway (see ‘Take special care with Grepid’).
Other side effects reported with Grepid are:
Common side effects: Diarrhoea, abdominal pain, indigestion or heartburn
Uncommon side effects:Headache, stomach ulcer, vomiting, nausea, constipation, excessive gas in stomach or intestines, rashes, itching, dizziness, sensation of tingling and numbness.
Rare side effects: Vertigo.
Very rare side effects: Jaundice; severe abdominal pain with or without back pain; fever, breathing difficulties sometimes associated with cough; generalised allergic reactions; swelling in the mouth; blisters of the skin; skin allergy; inflammation of the mouth (stomatitis); decrease in blood pressure; confusion; hallucinations; joint pain; muscular pain; changes in the way things taste.
In addition, your doctor may identify changes in your blood or urine test results.
If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.
How should it be stored?
Keep out of the reach and sight of children.
Do not use Grepid after the expiry date which is stated on the carton and on the blister, after EXP.
This medicinal product does not require any special storage conditions.
Do not use Grepid if you notice any visible sign of deterioration.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.