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Prasugrel, although good, is a difficult substitute for clopidogrel in elderly patients with coronary artery disease

5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]- 5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2 (4h)-one is used as the intermediate of Prasugrel .
  Prasugrel is a thiophenopyridine antiplatelet developed by Eli Lilly and daiichisankyo, a Japanese pharmaceutical manufacturer. It is a precursor drug. It forms an active molecule after metabolism through cytochrome P450 in the liver and combines with platelet P2Y12 receptor to exert an active against platelet aggregation. Clinical studies have proved that 60 mg dose has better anticoagulant effect than 300 mg standard dose and 600 mg increased dose of clopidogrel, which can reduce the comprehensive risk of heart attack, stroke and death due to heart disease by 20%, and has fast effect, good curative effect, good drug resistance and bioavailability, and low toxicity.

  For the cardiovascular disease treatment drug thiophene arsenicals, the emergence of prasugrel was once seen as a replacement for clopidogrel, but new dosing guidelines have emerged in the clinic, so can prasugrel really replace clopidogrel mom? How do you think about clopidogrel and prasugrel?
  Prasugrel is a new generation of thiophene arsenicals, a competitive inhibitor of P2Y12 receptor, which can effectively control inflammation in vivo, reduce the risk of arterial thrombosis, and significantly reduce the incidence of ischemic events. Moreover, compared with clopidogrel, the conversion of prasugrel into an active metabolite requires only one reaction, which means that it has a stronger antiplatelet effect and a shorter onset of action.
  However, in subsequent studies, it was found that more than 75 pairs of patients had difficulty benefiting from prasugrel, both because of the increased risk of bleeding associated with prasugrel administration and because many patients with advanced coronary artery disease have a history of stroke, and patients with a history of stroke are more likely to have a recurrent stroke when taking prasugrel.
  Therefore, in the dosing guidelines: 60 mg/d maintenance dose of Pragrel is not recommended for patients over 75 years of age, but because of its high efficiency, 5 mg/d Pragrel is recommended as a maintenance dose for patients over 75 years of age in Europe and the United States.
  Clopidogrel has been the most commonly used drug in the thiophene arsenical class and its medication status is difficult to be shaken.
  On the one hand, clopidogrel can be used as an alternative treatment for aspirin resistance or intolerance; on the other hand, after acute coronary syndrome or percutaneous coronary intervention, combined treatment with aspirin for 12 months is the standard regimen for antiplatelet therapy.
  Many people will wonder, so is it better to take aspirin and clopidogrel double combination antiplatelet therapy for a longer period of time?
  Here I can tell you very clearly: No. Although 12 months of dual antiplatelet therapy with aspirin and clopidogrel has a significant effect on reducing events such as myocardial infarction, cardiac death, and stroke, in a recent study, it was noted that in an observational study of patients receiving 12 months or 30 months of dual antiplatelet therapy, there was a decrease in ischemic events but an increase in minor bleeding events in patients over the age of 75.
  So, are there any criteria for patients with coronary artery disease in advanced age? I will tell you this.
  1. 6 months of combined aspirin and clopidogrel for patients over 75 years of age with drug-eluting stents placed in patients with stable coronary artery disease and 1 month of combined aspirin and clopidogrel for patients with bare metal stents placed in patients with stable coronary artery disease.
  2, acute coronary syndromes over 75 years of age after receiving interventional therapy, aspirin and clopidogrel in combination with antiplatelet therapy for at least 12 months, if the risk of bleeding is relatively high recommended to apply clopidogrel instead of prasugrel or tigretol.
  3. Clopidogrel is not recommended for load in patients over 75 years of age who are receiving thrombolytic therapy.
  4. The application of clopidogrel in Asian population needs to pay attention to the effect of genetic polymorphism, and genetic polymorphism testing may be considered in elderly patients with high thrombotic risk or recurrent thrombotic events.



PRODUCT TAGS

-2-oxoethyl);5-(2-Cyclopropyl-1-(2-fluorophenyl);-5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H);5-(2-Cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl)-5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H)-;3,5-[cyclopropylcarbonyl-2-flurobenzyl)-2-oxo-2,4,Chemicalbook5,6,7,7a-hexahydrothieno[3,2-c]-pyridine;PrasugrelThiolactone(MixtureofDiastereomers);5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-5,6,7,7a-tetrah;5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4H,5H,6H,7H-thieno[3,2-c]pyridin-2-ylacetate


  • date

    2022-10-09

  • location

    Shanghai, China