英文药名：Brilinta(ticagrelor tablets) 中文药名：替格瑞洛片 生产厂家：阿斯利康公司 药品介绍 7月20日，美国食品和药物管理局(FDA)批准了抗凝药替格瑞洛（ticagrelor ，商品名Brilinta)用于减少急性冠脉综合征（ACS）病人的心血管死亡和心脏病发作。 ACS包括一组心脏缺血症状，其原因包括不稳定型心绞痛或心脏病发作。Brilinta通过预防体内新的血栓形成来维持血流，有助于减少再次心血管事件的危险。 研究人员已对Brilinta联合阿司匹林治疗进行了研究。加框警告提示医务人员和病人，阿司匹林的剂量每日超过100 mg，会降低该药的有效性。 FDA药物评价与研究中心心血管和肾脏产品部主任诺曼（Norman Stockbridge）说：“在临床试验中，在预防心脏病发作和死亡方面，Brilinta比波立维（通用名：氯吡格雷）更有效，但这个优势见于联用每日1次维持剂量为75~100 mg的阿司匹林时。” 黑框警告还提示，与其他抗凝药一样，Brilinta增加出血发生率，并可引起显著的、有时是致命的出血。在临床试验中，服用Brilinta病人报告的最常见的不良反应是出血和呼吸困难。 Brilinta获准伴随着一项风险评估和减缓策略，后者是一项帮助确保该药的益处大于危险的计划。作为这个计划的一部分，公司必须对医师进行教育扩展，提醒他们有关使用较大剂量阿司匹林的危险。另外，在Brilinta配药时将配发用药指导，告知病人关于用药的最重要信息。该用药指导将在每次给每例病人调配处方时配发。 为口服使用BRILINTA™ (ticagrelor)片 美国初始批准：2011 适应证和用途 BRILINTA是一种 P2Y12血小板抑制剂适用于在有急性冠状动脉综合征(ACS)(不稳定心绞痛，无-ST升高心肌梗死，或ST升高心肌梗死)患者中减少血栓性心血管事件率。与氯吡格雷[clopidogrel]比较，BRILINTA曾显示减低的组合终点率心血管死亡, 心肌梗死，或中风。在中风中心血管死亡和MI治疗间驱动无差别。用PCI治疗患者中药物也减低支架内血栓形成率。 在ACS中BRILINTA曾研究与阿司匹林联用。阿司匹林维持剂量超过100 mg减低BRILINTA的有效性。避免阿司匹林每天维持剂量超过100mg。 剂量和给药方法 （1）初始治疗用180 mg(两90 mg片)口服负荷剂量。 （2）继续治疗用90 mg每天2次。 （3）初始负荷剂量阿司匹林后(通常325 mg), 用BRILINTA与阿司匹林每天维持剂量75-100mg。 剂型和规格 90mg片 禁忌证 （1）颅内出血史。 （2）活动性病理性出血。 （3）严重肝受损。 警告和注意事项 （1）像其它抗血小板药，BRILINTA增加出血的风险。 （2）在PLATO试验中，用BRILINTA与阿司匹林维持剂量超过100 mg减低BRILINTA的有效性。 （3）中度肝受损：考虑治疗的风险和获益,注意增加对ticagrelor暴露的可能性。 （4）呼吸困难：报道用BRILINTA比用氯吡格雷呼吸困难更频。来自BRILINTA呼吸困难是自限性。除外其它原因。 （5）BRILINTA的终止：过早终止增加心肌梗死，支架内血栓形成，和死亡的风险。 不良反应 最常见不良反应是出血12%和呼吸困难14%。 报告怀疑不良反应, 联系AstraZeneca电话1-800-236-9933或FDA电话1-800-FDA-1088或www.fda.gov/medwatch 药物相互作用 （1）避免与强CYP3A抑制剂或CYP3A诱导剂使用。 （2）患者每天接受超过40 mg辛伐他汀[simvastatin]或洛伐他汀[lovastatin]可能处于增加他汀类他汀类-相关不良作用风险。 （3）随开始BRILINTA或任何变化监视地高辛[digoxin]水平。 Brilinta Rx Manufacturer: AstraZeneca Pharmaceuticals Pharmacological Class: P2Y12 platelet inhibitor (cyclopentyltriazolopyrimidine). Active Ingredient(s): Ticagrelor 90mg; tablets. Indication(s): To reduce the rate of thrombotic cardiovascular (CV) events in patients with acute coronary syndrome (ACS) (unstable angina or non-ST-elevation myocardial infarction [MI] or ST-elevation MI). Pharmacology: Ticagrelor is a platelet activation and aggregation inhibitor mediated by the P2Y12 class of ADP receptors. Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. Both ticagrelor and its active metabolite are approximately equipotent. Clinical Trials: In a randomized, double-blind study, the use of ticagrelor was compared to a regimen of clopidogrel, both given in combination with aspirin and other standard therapy in patients with acute coronary syndromes. Patients were treated for at least 6 months and for up to 12 months. The primary endpoint was the composite of first occurrence of cardiovascular death, non-fatal MI (excluding silent MI), or non-fatal stroke. The components were assessed as secondary endpoints. At study completion, ticagrelor has been shown to significantly reduce the rate of a combined endpoint of cardiovascular death, MI or stroke compared to clopidogrel (9.8% vs. 11.7%, respectively, hazard ratio [HR] 0.84). The difference between treatments on the composite resulted from effects on CV death (HR 0.79) and MI (HR 0.84); each was statistically significant when considered as a secondary endpoint and there was no difference on strokes. There was also a decrease in all-cause mortality. Among 11,298 patients with PCI receiving any stent during this study, there was a lower risk of stent thrombosis (1.3% for adjudicated “definite”) than with clopidogrel (1.9%). Legal Classification: Rx Adults: Initiate loading dose: 180mg once, then continue with 90mg twice daily. After the initial loading dose of aspirin (usually 325mg), take ticagrelor with maintenance dose of aspirin 75–100mg daily. ACS patients: may start ticagrelor after receiving a loading dose of clopidogrel. Children: Not established. Contraindication(s): History of intracranial hemorrhage. Active pathological bleeding (eg, peptic ulcer, intracranial hemorrhage). Severe hepatic impairment. Warnings/Precautions: Do not start in patients planned to undergo urgent CABG. When possible, discontinue at least 5 days before any surgery. Suspect bleeding in hypotensive patients who have recently undergone coronary angiography, PCI, CABG, or other surgery. Older age, history of bleeding disorders, undergoing percutaneous invasive procedures, concomitant anticoagulants, fibrinolytics, higher doses of aspirin, and chronic NSAID use: increased risk of bleeding. Avoid interruption of treatment; if temporarily discontinued, restart as soon as possible. Premature discontinuation increases risk for CV events (eg, MI, stent thrombosis, death). Effectiveness reduced with aspirin maintenance dose >100mg; avoid. Moderate hepatic impairment. Pregnancy (Cat. C). Nursing mothers: not recommended. Interaction(s): Concomitant strong CYP3A inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, telithromycin,) or potent CYP3A inducers (eg, rifampin, dexamethasone, phenytoin, carbamazepine, phenobarbital): not recommended. Potentiates simvastatin, lovastatin; avoid >40mg/day doses. Monitor digoxin during ticagrelor initiation and dose adjustments. Adverse Reaction(s): Bleeding (may be fatal), dyspnea, headache, cough, dizziness, GI upset, atrial fibrillation, hyper- or hypotension, back pain, fatigue, chest pain. How Supplied: Tabs—60, 180 Last Updated: 8/25/2011 ------------------------------------------------------ 产地国家: 美国 原产地英文商品名: Brilinta tabs 90mg/tab 60tabs/box 原产地英文药品名: TICAGRELOR 中文参考商品译名: Brilinta片 90毫克/片 60片/瓶 中文参考药品译名: 替卡格雷 生产厂家中文参考译名: 美国阿斯利康 生产厂家英文名: AstraZeneca ------------------------------------------------------ 产地国家: 美国 原产地英文商品名: Brilinta tabs 90mg/tab 180tabs/box 原产地英文药品名: TICAGRELOR 中文参考商品译名: Brilinta片 90毫克/片 180片/瓶 中文参考药品译名: 替卡格雷 生产厂家中文参考译名: 美国阿斯利康 生产厂家英文名: AstraZeneca