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Plavix is marketed worldwide in nearly 110 countries, with sales of US$6.6 billion in 2009. [45] It was the second-top-selling drug in the world in 2007 [46] and was still growing by over 20% in 2007. US sales were US$3.8 billion in 2008. [47] Before the expiry of its patent, clopidogrel was the second best-selling drug in the world.
Overall mortality rates were similar for each drug. [4] Clopidogrel, unlike prasugrel, was issued a black box warning from the FDA on 12 March 2010, as the estimated 2–14% of the US population who have low levels of the CYP2C19 liver enzyme needed to activate clopidogrel may not get the full effect. Tests are available to predict if a patient ...
Metabolism of ticlopidine, clopidogrel and prasugrel to an active metabolite. Clopidogrel is a prodrug that is metabolized by two pathways. In one of the pathway most of the dose of clopidogrel (85%) is hydrolyzed by esterases to an inactive carboxylic acid derivate and rapidly cleared via glucoridination followed by renal excretion.
Clopidogrel has a common drug interaction with CYP2C19 inhibitors, particularly omeprazole and esomeprazole which are indicated for treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD). As the activation of clopidogrel requires an enzyme called CYP2C19, its inhibitors should be avoided. [38]
The drug is usually applied together with aspirin or clopidogrel and (low molecular weight or unfractionated) heparin. Additionally, the usual supportive treatment consisting of applications of nitrates, beta-blockers, opioid analgesics and/or benzodiazepines should be employed as indicated.
According to guidelines, taking aspirin or clopidogrel is recommended to reduce AMI ("heart attack"), stroke, and other causes of vascular death in people with symptomatic peripheral artery disease. [20] It is recommended that aspirin and clopidogrel be taken alone and not in conjunction with one another (i.e., not as dual antiplatelet therapy
Ticagrelor (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that is distinct from the mechanism of the thienopyridines in that it reversibly (rather than irreversibly) inhibits the P2Y 12 receptor.
Since bupropion is metabolized to hydroxybupropion by the enzyme CYP2B6, drug interactions with CYP2B6 inhibitors are possible: this includes such medications as paroxetine, sertraline, norfluoxetine (active metabolite of fluoxetine), diazepam, clopidogrel, and orphenadrine. The expected result is an increase of bupropion and a decrease in ...
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