部份中文氯吡格雷处方资料(仅供参考) 药品英文名 Clopidogrel Clopidogrel Denk 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。 包装规格 75mg*100片
厂家:德国 Denk clopidogrel BRAND NAME(S): Plavix GENERIC NAME(S): CLOPIDOGREL BISULFATE Uses Clopidogrel is used to prevent heart attacks and strokes in persons with heart disease (recent heart attack), recent stroke, or blood circulation disease (peripheral vascular disease). It is also used with aspirin to treat new/worsening chest pain (new heart attack, unstable angina) and to keep blood vessels open and prevent blood clots after certain procedures (such as cardiac stent). Clopidogrel works by blocking platelets from sticking together and prevents them from forming harmful clots. It is an antiplatelet drug. It helps keep blood flowing smoothly in your body. OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional. This medication may also be used to prevent heart attacks and strokes in persons with irregular heartbeat (atrial fibrillation). How to use clopidogrel Read the Medication Guide provided by your pharmacist before you start taking clopidogrel and each time you get a refill. If you have any questions, ask your doctor or pharmacist. Take this medication by mouth with or without food as directed by your doctor, usually once daily. Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. The dosage and length of treatment are based on your medical condition and response to treatment. If you are taking this medication to prevent clots after a stent implant or other procedure, take this medication with aspirin for many months to years after the procedure (depending on the procedure/type of stent) as directed by your doctor. Consult your doctor for more details and about the risks of stopping early. It is important to continue taking this medication even if you feel well. Do not stop taking this medication without consulting your doctor. Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details. Get medical help right away if you have any signs that this medication is not working, such as symptoms of a new heart attack or stroke (such as chest/jaw/left arm pain, shortness of breath, unusual sweating, weakness on one side of the body, slurred speech, sudden vision changes, confusion). What conditions does clopidogrel treat?Side Effects Easy bleeding/bruising, stomach upset/pain, diarrhea, and constipation may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects. Although unlikely, serious bleeding in the stomach, gut, eyes, or brain may occur. Also, clopidogrel can rarely cause a very serious blood disorder (thrombotic thrombocytopenic purpura-TTP). Symptoms may appear any time after starting this medication. Get medical help right away if any of these symptoms occur: severe stomach/abdominal pain, uncontrolled bleeding from gums or nose, bloody/black stools, confusion, fever, extreme skin paleness, purple skin patches, fainting, fast heartbeat, sudden severe headache, unusual weakness/tiredness, vomit with blood or that looks like coffee grounds, slurred speech, vision changes, seizures, yellowing eyes/skin, bloody/red/pink/dark urine, change in amount of urine. A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing. This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist. In the US - Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. List clopidogrel side effects by likelihood and severity.Precautions Before taking clopidogrel, tell your doctor or pharmacist if you are allergic to it; or to similar antiplatelet drugs (thienopyridines such as prasugrel); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details. Before using this medication, tell your doctor or pharmacist your medical history, especially of: bleeding conditions (such as stomach ulcers, bleeding in the brain/eye), recent surgery, serious injury/trauma, liver disease, bleeding disease (such as hemophilia). To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports. Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Your doctor may instruct you to stop clopidogrel for 5 to 7 days before surgery. Do not stop taking clopidogrel without talking with your heart doctor (cardiologist) first. This medicine may cause stomach bleeding. Daily use of alcohol while using this medicine may increase your risk for stomach bleeding. Limit alcoholic beverages. Ask your doctor or pharmacist about how much alcohol you may safely drink. During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding. What should I know regarding pregnancy, nursing and administering clopidogrel to children or the elderly?Interactions See also How to Use section. Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval. A product that may interact with this drug is: tipranavir. If you are currently taking aspirin, consult your doctor promptly and ask whether to continue or stop taking it with this medication for your specific condition (aspirin and clopidogrel may be used in combination after a coronary stent procedure, or for some heart conditions). If you are not currently taking aspirin, consult your doctor before starting it for any medical condition. Other medications can affect the removal of clopidogrel from your body, which may affect how clopidogrel works. Examples include certain acid reducers (proton pump inhibitors/PPIs such as omeprazole, esomeprazole), fluvoxamine, fluoxetine, cimetidine, fluconazole, ketoconazole, voriconazole, etravirine, felbamate, and ticlopidine, among others. Promptly ask your doctor or pharmacist for more details. Do not use non-prescription medications that contain PPIs (such as omeprazole, esomeprazole) or cimetidine for relief of upset stomach or heartburn. These medications can prevent clopidogrel from working well. Ask your doctor or pharmacist about safer alternatives such as liquid antacids, ranitidine, or famotidine. Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (NSAIDs such as ibuprofen, naproxen, or aspirin). These drugs may increase the risk of bleeding/antiplatelet effect when used with clopidogrel. Ask your pharmacist about using these products safely. Does clopidogrel interact with other medications? Should I avoid certain foods while taking clopidogrel?Overdose If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
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