Characteristics of Tirofiban Hydrochloride

Tirofiban hydrochloride is a reversible non-peptide platelet GP IIb/IIIa receptor antagonist, developed by Merck in the United States. And it was marketed in the United Statesfor the first timein May 1998, and has beenmarketed in Switzerland, China, Germany, the United Kingdom, the Netherlands and other countries. The dosage form marketed in the United States is an injection for the treatment of acute coronary syndrome (ACS), including non-Q-wave myocardial infarction (MI) and unstable angina.

The main advantages ofTirofiban hydrochloride

a. Antithrombotic through inhibition of adenosine diphosphate (ADP) with strong selectivity.

b. The half-life is more longer about 2 hours, the platelets return to normal after 2 to 3 hours, and there is no significant increase in cerebral hemorrhage during use, and 65% is excreted through the kidneys.

c. Significantly reduce the incidence of acute and subacute ischemic complications.

d. The use of this drug after percutaneous transluminal coronary angioplasty (PTCA) can prevent the occurrence of bleeding and has fewer adverse reactions.

e. It can be used in combination with heparin and aspirin, which can significantly reduce adverse events such as cardiovascular complications, and reduce the incidence and mortality of myocardial infarction.

Theadvantages compared to similar drugs

For the treatment of ACS, the clinical use of aspirin and clopidogrel antiplatelet therapy combined with low molecular weight heparin anti-coagulation and anti-ischemia drugs has significantly improved the prognosis and significantly reduced the mortality rate. Aspirin is a cyclooxygenase inhibitor that blocks the derivatization of arachidonic acid into thromboxane A2(TXA2), and has an irreversible inhibition on TXA2-induced platelet aggregation. Clopidogrel is a drug that specifically inhibits the pathway of platelet activation by adenosine diphosphate (ADP), and has a specific and strong inhibitory effect on ADP-induced platelet aggregation, which is an irreversible reaction. Studies have shown that aspirin can reduce the risk of cardiac ischemic events by about 35%. The CAPRIE trial also demonstrated that clopidogrel (75mg/d) reduced ischemic events by 8.7% compared with aspirin (325mg/d). However, aspirin and clopidogrel can only block one of the platelet activation pathways to inhibit platelet aggregation, and platelet activation and aggregation can also be carried out through other pathways. Therefore, even in the case of using the above two drugs to treat ACS, Platelet thrombotic events may still occur.

Tirofiban is a highly specific non-peptide platelet membrane glycoprotein IIb/IIIa receptor antagonist. which acts on the last common pathway of platelet aggregation, occupying the cross-linking site of GP IIb/IIIa through the arginine-glycine-aspartic acid (RGD) sequence, and competitively inhibits fibrinogen or von Willebrand factor (vWF)-mediated platelet aggregation. Therefore, the addition of tirofiban to the standard treatment of ACS can more completely inhibit platelet aggregation and prevent the formation of platelet thrombi, thereby reducing the incidence of cardiac ischemia endpointevent.