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Clopidogrel : ウィキペディア英語版
Clopidogrel

Clopidogrel (INN) is an oral, thienopyridine-class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, cerebrovascular disease, and to prevent myocardial infarction (heart attack) and stroke. It is marketed by Bristol-Myers Squibb and Sanofi under the trade name Plavix. The drug works by irreversibly inhibiting a receptor called P2Y12, an adenosine diphosphate (ADP) chemoreceptor on platelet cell membranes. Adverse effects include bleeding, severe neutropenia, and thrombotic thrombocytopenic purpura.
Before the expiry of its patent, clopidogrel was the second best-selling drug in the world. In 2010, it grossed over US$9 billion in global sales.
== Medical use ==

Clopidogrel is used to prevent heart attack and stroke in people who are at high risk of these events, including those with a history of myocardial infarction and other forms of acute coronary syndrome, stroke, and those with peripheral artery disease.
Treatment with clopidogrel or a related drug is recommended by the American Heart Association and the American College of Cardiology for people who:
* Present for treatment with a myocardial infarction with ST-elevation including
:
* A loading dose given in advance of percutaneous coronary intervention (PCI), followed by a full year of treatment for those receiving a vascular stent
:
* A loading dose given in advance of fibrinolytic therapy, continued for at least 14 days
* Present for treatment of a non-ST elevation myocardial infarction or unstable angina
:
* Including a loading dose and maintenance therapy in those receiving PCI and unable to tolerate aspirin therapy
:
* Maintenance therapy for up to 12 months in those at medium to high risk for which a noninvasive treatment strategy is chosen
* In those with stable ischemic heart disease, treatment with clopidogrel is described as a "reasonable" option for monotherapy in those who cannot tolerate aspirin, as is treatment with clopidogrel in combination with aspirin in certain high risk patients.
It is also used, along with acetylsalicylic acid (ASA, aspirin), for the prevention of thrombosis after placement of an coronary stent〔Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3〕 or as an alternative antiplatelet drug for people intolerant to aspirin.〔Michael D Randall; Karen E Neil (2004). Disease management. 2nd ed. London: Pharmaceutical Press. 159.〕
Clopidogrel's benefit is primarily in those who smoke cigarettes, with only slight benefit in those who do not.
Consensus-based therapeutic guidelines also recommend the use of clopidogrel rather than ASA for antiplatelet therapy in people with a history of gastric ulceration, as inhibition of the synthesis of prostaglandins by ASA can exacerbate this condition. In people with healed ASA-induced ulcers, however, those receiving ASA plus the proton pump inhibitor esomeprazole had a lower incidence of recurrent ulcer bleeding than those receiving clopidogrel. However, prophylaxis with proton pump inhibitors along with clopidogrel following acute coronary syndrome may increase adverse cardiac outcomes, possibly due to inhibition of CYP2C19, which is required for the conversion of clopidogrel to its active form. The European Medicines Agency has issued a public statement on a possible interaction between clopidogrel and proton pump inhibitors. However, several cardiologists have voiced concern that the studies on which these warnings are based have many limitations and that it is not certain whether an interaction between clopidogrel and proton pump inhibitors is real.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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