制造商：
阿斯利康制药
类药物：
P2Y12血小板抑制剂（cyclopentyltriazolopyrimidine）。
活性成分（S）：
替卡格雷90mg;片。
指示（S）：
为了降低率在急性冠脉综合征（ACS）（不稳定型心绞痛，非ST段抬高心肌梗死[MI]或ST段抬高心肌梗死）患者血栓性心血管（CV）事件。
药理学：
替卡格雷是血小板活化和聚集抑制剂介导的ADP受体P2Y12类。替卡格雷和其主要代谢产物与血小板P2Y12 ADP受体，以防止信号转导与血小板活化可逆的互动。替卡格雷及其活性代谢物约equipotent。
临床试验：
在一项随机，双盲对照研究，使用替卡格雷的氯吡格雷方案相比，两者结合阿司匹林和其他标准治疗急性冠脉综合征患者中。患者接受治疗至少6个月至12个月。
主要终点为心血管死亡，非致命性心肌梗死（不包括无声心肌梗死），非致命性中风或第一次出现的复合。作为次要终点的组件进行了评估。
在研究完成后，替卡格雷已经显示出显着降低了心血管死亡复合终点率，心肌梗死或中风的比较氯吡格雷（分别为9.8％和11.7％，风险比[HR] 0.84）。综合治疗之间的差异，导致心血管死亡（HR 0.79）和MI（HR 0.84）的影响;统计学意义视为次要终点时，有没有笔画的区别。也有各种原因的死亡率减少。
其中11298例与PCI接收任何支架，在这项研究中，有一个风险较低的支架内血栓形成与氯吡格雷（1.9％）比（1.3％）裁决“明确的”。
法律分类：
接收
成人：
启动负荷剂量：180mg一次，然后继续用90mg，每日两次。初始负荷剂量的阿司匹林（325mg通常）后，替卡格雷维持剂量阿司匹林75每日100mg。 ACS患者：可能会开始后收到氯吡格雷负荷剂量替卡格雷。
儿童：
不成立的。
禁忌（S）：
颅内出血的历史。主动病理出血（如消化性溃疡，颅内出血）。严重肝功能损害。
警告/注意事项：
不要在计划接受紧急冠状动脉搭桥术的患者开始。在可能的情况下，停止任何手术前至少5天。犯罪嫌疑人在最近发生的PCI，冠状动脉造影，冠状动脉搭桥术，或其他手术低血压患者的出血。年龄大，出血性疾病史，接受经皮侵入性手术，随之而来的抗凝血剂，纤维蛋白溶解，较高剂量的阿司匹林，长期使用NSAID：增加出血的风险。避免中断治疗;如果暂时停产，尽快重新启动。过早停药会增加心血管事件（如心肌梗死，支架血栓，死亡）的风险。有效性降低阿司匹林的维持剂量> 100毫克;避免。中度肝功能损害。怀孕（部件C）。哺乳母亲：不推荐。
相互作用（S）：
伴随强烈的CYP3A的抑制剂（如酮康唑，伊曲康唑，伏立康唑，克拉霉素，奈法唑酮，利托那韦，沙奎那韦，奈非那韦，茚地那韦，阿扎那韦，泰利霉素，）或有力CYP3A的诱导剂（如利福平，地塞米松，苯妥英，卡马西平，苯巴比妥）：不推荐。 Potentiates辛伐他汀，洛伐他汀，避免> 40mg/day剂量。监视器在替卡格雷启动和调整剂量地高辛。
不良反应（S）：
出血（可能是致命的），呼吸困难，头痛，咳嗽，头晕，胃肠不适，房颤，超或低血压，腰背酸痛，乏力，胸痛。
如何提供：
标签- 60，180
最后更新：
2011年8月25日
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