部份中文硫酸氢氯吡格雷处方资料（仅供参考） 英文名：Clopidogrel Sulfate 商标名：PLAVIX 中文名：硫酸氢氯吡格雷薄膜片 生产商：赛诺菲-安万特 药品简介： 硫酸氢氯吡格雷（Plavix，Clopidogrel）是一种抗凝血药物，适用于有过近期发作的中风、心肌梗塞和确诊外周动脉硬化的患者。 类别名称： 抗血小板剂 药物剂型 片剂：25mg，75mg。 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。 适应症 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)。 禁忌症 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。 包装规格[注：本品美国上市包装，采购以咨询为准] PLAVIX TAB 75MG 90  CLOPIDOGREL BISULFATE  ER SQUIBB & SONS LLC  63653-1171-01 PLAVIX TAB 300MG HUD 3X10  CLOPIDOGREL BISULFATE  ER SQUIBB & SONS LLC  63653-1332-02 PLAVIX TAB 75MG 30  CLOPIDOGREL BISULFATE  ER SQUIBB & SONS LLC  63653-1171-06  PLAVIX TAB 75MG UD 100  CLOPIDOGREL BISULFATE  ER SQUIBB & SONS LLC  63653-1171-03 PLAVIX TAB 75MG 500  CLOPIDOGREL BISULFATE  ER SQUIBB & SONS LLC  63653-1171-05 --------------------------------------------------------- PLAVIX(clopidogrel bisulfate) PLAVIX(clopidogrel bisulfate) is an inhibitor of ADP-induced platelet aggregation acting by direct inhibition of adenosine diphosphate (ADP) binding to its receptor and of the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Chemically it is methyl (+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetate sulfate (1:1). The empirical formula of clopidogrel bisulfate is C16H16ClNO2S•H2SO4 and its molecular weight is 419.9. Clopidogrel bisulfate is a white to off-white powder. It is practically insoluble in water at neutral pH but freely soluble at pH 1. It also dissolves freely in methanol, dissolves sparingly in methylene chloride, and is practically insoluble in ethyl ether. It has a specific optical rotation of about +56°. PLAVIX for oral administration is provided as either pink, round, biconvex, debossed, film-coated tablets containing 97.875 mg of clopidogrel bisulfate which is the molar equivalent of 75 mg of clopidogrel base or pink, oblong, debossed film-coated tablets containing 391.5 mg of clopidogrel bisulfate which is the molar equivalent of 300 mg of clopidogrel base. Each tablet contains hydrogenated castor oil, hydroxypropylcellulose, mannitol, microcrystalline cellulose and polyethylene glycol 6000 as inactive ingredients. The pink film coating contains ferric oxide, hypromellose 2910, lactose monohydrate, titanium dioxide and triacetin. The tablets are polished with Carnauba wax. CLINICAL PHARMACOLOGY Mechanism of Action and Pharmacodynamic Properties Clopidogrel is a prodrug, one of whose metabolites is an inhibitor of platelet aggregation. A variety of drugs that inhibit platelet function have been shown to decrease morbid events in people with established cardiovascular atherosclerotic disease as evidenced by stroke or transient ischemic attacks, myocardial infarction, unstable angina or the need for vascular bypass or angioplasty. This indicates that platelets participate in the initiation and/or evolution of these events and that inhibiting platelet function can reduce the event rate. Clopidogrel must be metabolized by CYP450 enzymes to produce the active metabolite that inhibits platelet aggregation. The active metabolite of clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation. This action is irreversible. Consequently, platelets exposed to clopidogrel's active metabolite are affected for the remainder of their lifespan (about 7 to 10 days). Platelet aggregation induced by agonists other than ADP is also inhibited by blocking the amplification of platelet activation by released ADP. Because the active metabolite is formed by CYP450 enzymes, some of which are polymorphic or subject to inhibition by other drugs, not all patients will have adequate platelet inhibition. Dose dependent inhibition of platelet aggregation can be seen 2 hours after single oral doses of PLAVIX. Repeated doses of 75 mg PLAVIX per day inhibit ADP-induced platelet aggregation on the first day, and inhibition reaches steady state between Day 3 and Day 7. At steady state, the average inhibition level observed with a dose of 75 mg PLAVIX per day was between 40% and 60%. Platelet aggregation and bleeding time gradually return to baseline values after treatment is discontinued, generally in about 5 days. Pharmacokinetics Absorption After single and repeated oral doses of 75 mg per day, clopidogrel is rapidly absorbed. Mean peak plasma levels of unchanged clopidogrel (approximately 2.2-2.5 ng/mL after a single 75-mg oral dose) occurred approximately 45 minutes after dosing. Absorption is at least 50%, based on urinary excretion of clopidogrel metabolites. Effect of Food The effect of food on the bioavailability of the parent compound or active metabolite is currently not known. Distribution Clopidogrel and the main circulating inactive metabolite bind reversibly in vitro to human plasma proteins (98% and 94%, respectively). The binding is nonsaturable in vitro up to a concentration of 100 mcg/mL. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=01b14603-8f29-4fa3-8d7e-9d523f802e0b https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=13815 https://www.medicines.org.uk/emc/medicine/11005