plavix
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plavix
ClopidogrelSystematic (IUPAC) name(+)-(S)-methyl 2-(2-chlorophenyl)-2-(6,7-dihydrothienopyridin-5(4H)-yl)acetateIdentifiersCAS number113665-84-2ATC codeB01AC04PubChem60606DrugBankAPRD00444ChemSpider54632Chemical dataFormulaC16H16ClNO2S Mol. mass321.82 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability>50%Protein binding94–98%MetabolismHepaticHalf life7–8 hours (inactive metabolite)Excretion50% renal46% biliaryTherapeutic considerationsPregnancy cat.B1(AU) B(US)Legal statusPrescription Only (S4)(AU) POM(UK) ℞-only(US)RoutesOralClopidogrel is a potent oral antiplatelet agent often used in the treatment of coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi-Aventis under the trade names Iscover and Plavix respectively, by Sun Pharmaceuticals under the trade name Clopilet and by Ranbaxy Laboratories under the trade name Ceruvin. It works by blocking a receptor called P2Y12. Adverse effects include hemorrhage.// PharmacologyThe mechanism of action of clopidogrel is an irreversible blockade of the adenosine diphosphate (ADP) receptor on platelet cell membranes. This part of this receptor that it binds to is named P2Y12 and is important in platelet aggregation, the cross-linking of platelets by fibrin. The blockade of this receptor inhibits platelet aggregation by blocking activation of the glycoprotein IIb/IIIa pathway. The IIb/IIIa complex functions as a receptor mainly for fibrinogen and vitronectin but also for fibronectin and von Willebrand factor. Activation of this receptor complex is the "final common pathway" for platelet aggregation. and is important in platelet aggregation, the cross-linking of platelets by fibrin.Platelet inhibition can be demonstrated two hours after a single dose of oral clopidogrel, but the onset of action is slow, so that a loading-dose of 300-600 mg is usually administered. Clinical use IndicationsClopidogrel is indicated for:Prevention of vascular ischaemic events in patients with symptomatic atherosclerosisAcute coronary syndrome without ST-segment elevation (NSTEMI), along with aspirinST elevation MI (STEMI)It is also used, along with aspirin, for the prevention of thrombosis after placement of intracoronary stent. International guidelines granted the highest grade of recommendation for NSTE-ACS, PCI and stent, for Clopidogrel in addition to Aspirin. Consensus-based therapeutic guidelines recommend also the use of clopidogrel, instead of aspirin, in patients requiring antiplatelet therapy but with a history of gastric ulceration, as inhibition of the synthesis of prostaglandins by aspirin (acetylsalicylic acid) can exacerbate this condition. A recent study has shown that in patients with healed aspirin-induced ulcers, however, patients receiving aspirin plus the proton pump inhibitor esomeprazole had a lower incidence of recurrent ulcer bleeding than patients receiving clopidogrel. Dosage formsClopidogrel is marketed as clopidogrel bisulfate (clopidogrel hydrogen sulfate), most commonly under the trade names Plavix, as 75 mg oral tablets. Pharmacokinetics and metabolismAfter repeated 75-mg oral doses of clopidogrel (base), plasma concentrations of the parent compound, which has no platelet inhibiting effect, are very low and are generally below the quantification limit (0.000258 mg/L) beyond 2 hours after dosing.Clopidogrel is a pro-drug which requires metabolism by the liver for its activation.The active metabolite has an elimination half-life of about 8 hours and acts by forming a disulfide bridge with the platelet ADP receptor.Following an oral dose of 14C-labeled clopidogrel in humans, approximately 50% was excreted in the urine and approximately 46% in the feces in the 5 days after dosing.Effect of Food: Administration of CLAVIX (clopidogrel bisulfate) with meals did not significantly modify the bioavailability of clopidogrel as assessed by the pharmacokinetics of the main circulating metabolite.Absorption and Distribution: Clopidogrel is rapidly absorbed after oral administration of repeated doses of 75 mg clopidogrel (base), with peak plasma levels (appx. 3 mg/L) of the main circulating metabolite occurring approximately 1 hour after dosing. The pharmacokinetics of the main circulating metabolite are linear (plasma concentrations increased in proportion to does) in the dose range of 50 to 150 mg of clopidogrel. Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites. Clopidogrel and the main circulating metabolite bind reversibly in vitro to human plasma proteins (98% and 94%, respectively). The binding is nonsaturable in vitro up to a concentration of 110 μg/mL.Metabolism and Elimination: In vitro and in vivo, clopidogrel undergoes rapid hydrolysis into its carboxylic acid derivative. In plasma and urine, the glucuronide of the carboxylic acid derivative is also observed. Adverse effectsSerious adverse drug reactions associated with clopidogrel therapy include:Severe neutropenia (Incidence: 1/2,000)Thrombotic thrombocytopenic purpura (TTP) (Incidence: 4/1,000,000 patients treated)Hemorrhage - The incidence of hemorrhage may be increased by the co-administration of aspirin.Gastrointestinal Hemorrhage (Incidence: 2.0%)Cerebral Hemorrhage (Incidence: 0.1 to 0.4%)Use of non-steroidal anti-inflammatory drugs is discouraged in those taking clopidogrel due to increased risk of digestive tract hemorrhage MarketingPlavix has been the 2nd top selling drug in the world over the past years and was still growing by over 20% in 2007.Plavix is marketed worldwide in nearly 110 countries.In 2006, generic clopidogrel was briefly marketed by Apotex, a Canadian generic pharmaceutical company before a court order halted further production until resolution of a patent infringement case brought by Bristol-Myers Squibb. The court ruled that Bristol-Myers Squibb's patent was valid and has patent protection until November 2011. In 2007, the production was halted to many retail pharmacies and will be changing back to Plavix. In 2005 it was reported that Plavix was the world's second highest selling pharmaceutical with sales of US$5.9 billion. Generic clopidogrel is also produced by several pharmaceutical companies in India at significantly lower retail prices, up to 1/30th of the price.
.By Peter Loftus Of DOW JONES NEWSWIRES Bristol-Myers Squibb Co. It can also be employed for other conditions as determined by your doctor., Prilosec, Nexium) according to an Aetna analysis published in the September 16th issue of the Journal of the American College of Cardiology. With Plavix not losing patent until 2012 and 2019, Sanofi and analysts are trying to understand the move.htmlJim Duggan was prescribed Plavix after he had three coronary stents implanted.Generic Plavix is employed for: The reduction of the risk of race or heart attack in the patients who already had a heart attack or a race, or have other circulatory problems which had with the contracting and the hardening of the arteries.The FDA has approved the use of Plavix (clopidogrel) for people who have had a type of heart attack called acute ST-segment elevation myocardial infarction (STEMI), and who are not going to have coronary artery repair (angioplasty). It is being smuggled into the country as parallel imports, like the fake batches of Eli Lilly's antipsychotic Zyprexa. Under federal law, such anti-competitive agreements need to be submitted to the FTC.S.g. partner Bristol-Myers Squibb Co. Plavix is known at times by its generic name of Clopidogrel bisulfate.UK's health regulator
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