Thrombosis formation on disrupted atherosclerotic plaque is the most common acuse of cardiovascular diseases, in the pathophysiology, increased platelet reactivity is a descriptor of the risk of cardiovascular events ...Thrombosis formation on disrupted atherosclerotic plaque is the most common acuse of cardiovascular diseases, in the pathophysiology, increased platelet reactivity is a descriptor of the risk of cardiovascular events in healthy persons and in patients with overt coronary artery disease. Regardless of the stimulus for activation platelet-platelet interation and thrombus formation is ultimately regulated through the GP Ⅱ b/Ⅲ a receptor展开更多
Batifiban, a synthetic cyclic peptide, is a potent platelet glycoprotein GPⅡb/Ⅲa antagonist which may be useful in the treatment and prevention of acute coronary syndromes. The pharmacokinetics and pharmacodymanic ...Batifiban, a synthetic cyclic peptide, is a potent platelet glycoprotein GPⅡb/Ⅲa antagonist which may be useful in the treatment and prevention of acute coronary syndromes. The pharmacokinetics and pharmacodymanic （inhibition of platelet aggregation） effects, and tolerability of batifiban were investigated in healthy subjects following single bolus injection with doses of 55, 110, or 220 μg/kg, or multiple doses of an bolus followed intravenous infusion for 24 h （180 μg/kg plus 2.0 μg/minokg, and 220 μg/kg plus 2.5μg/minokg） in this phase I clinical trial. Plasma levels of batifiban and areas under the curve were found to be proportional to doses. Batifiban was rapidly eliminated with a half-life of approximately 2.5 h. Significant differences were noted for plasma levels of batifiban and areas under the curve between males and females. No significant differences in the terminal half-life were found between males and females. Batifiban reversibly inhibited ex vivo platelet aggregation in a dose- and concentration-dependent manner, consistent with its mechanism as a GPⅡ b/Ⅲa antagonist. Single and multiple intravenous doses of batifiban were found to be safe and well tolerated in healthy subjects. These results support a bolus injection plus intravenous infusion regimen of batifiban for the treatment and prevention of acute coronary syndromes.展开更多
Platelet activation plays an important role in thrombosis. Platelet glycoprotein Ⅱ b/Ⅲ a （ GPⅡ b/Ⅲ a ） is the receptor of fibrinogen. Platelet cross-linking with fibrinogen through GP Ⅱ b/Ⅲ a is the process of...Platelet activation plays an important role in thrombosis. Platelet glycoprotein Ⅱ b/Ⅲ a （ GPⅡ b/Ⅲ a ） is the receptor of fibrinogen. Platelet cross-linking with fibrinogen through GP Ⅱ b/Ⅲ a is the process of thrombosis. Ca^2＋ is an important intracellular second messenger in platelet activation. It has been reported that GP Ⅱ b/Ⅲ a receptors were involved in the calcium influx of activated platelet, and GP Ⅱ b/Ⅲ a receptor had characteristics of calcium channel or an adjacent calcium channel.展开更多
To compare clinical outcomes and safety of eptifibatide or tirofiban in patients with acute coronary syndrome（ACS） undergoing percutaneous coronary intervention（PCI）. Methods：Thirty-six patients with ACS（unstabl...To compare clinical outcomes and safety of eptifibatide or tirofiban in patients with acute coronary syndrome（ACS） undergoing percutaneous coronary intervention（PCI）. Methods：Thirty-six patients with ACS（unstable angina/non-ST-segment elevation myocardial infarction, UA/NSTEMI） who underwent PCI were randomly divided into two groups to receive eptifibatide or tirofiban treatment. Eptifibatide or tirofiban was predominantly initiated in the catheter laboratory before the intervention. In-hospital and 30-day MACE outcomes; bleeding as well as platelet counting were investigated in those two groups. Results：No in-hospital and 30-day MACE event occurred in the two groups. The number of ischemia leads after treatment reduced compared to that before PCI in the two groups. There was improvement in the number of ischemia leads for 24 h after administration in the tirofiban group than those in eptifibatide group（4.21 ± 2.46 vs. 3.89 ± 3.31, P =0.03）. The two groups showed no incidence of massive bleeding. Minor bleeding rates were 16.7% and 22.2% in the two groups respectively. Conclusion：Eptifibatide as an adjunct to PCI may further decrease the incidence of ischemia event in patients with ACS and improve the safety, but its long-term efficacy and side effects need further observation.展开更多
Objective:To evaluate the efficacy and safety of tirofiban hydrochloride in the treatment of ischemic stroke with thrombolytic therapy.Method:Two hundred patients with acute ischemic stroke thrombolysis were randomly ...Objective:To evaluate the efficacy and safety of tirofiban hydrochloride in the treatment of ischemic stroke with thrombolytic therapy.Method:Two hundred patients with acute ischemic stroke thrombolysis were randomly divided into the experimental group and the control group.The experimental group was given tirofiban with the addition of rtpa in the control group and the therapeutic effects of the two groups were compared.Results:In comparison with the control group,the NIHSS improvement rate was 98%in the experimental group within 14 days.The platelet aggregation rate and efficacy in the experimental group were significantly reduced than the control group(P<0.01).The major adverse reaction in the two groups was hemorrhage with an incidence rate of 3%.Conclusion:Tirofiban hydrochloride is a highly effective and selective platelet glycoprotein Ⅱb/Ⅲa receptor inhibitor,which is safe and effective in combination with heparin and aspirin.展开更多
This paper designed a detailed procedure for monogenic hypertension diagnosis by Whole Exome Sequencing(WES)and provided reliable precise medication guidance.Identification of mutated points provides the clinician val...This paper designed a detailed procedure for monogenic hypertension diagnosis by Whole Exome Sequencing(WES)and provided reliable precise medication guidance.Identification of mutated points provides the clinician valuable information for effective individualized therapeutic option.Therapeutic options that specifically restore the pathway disturbed by these point mutations can be selected to give a precise medicinal guidance.展开更多
文摘Thrombosis formation on disrupted atherosclerotic plaque is the most common acuse of cardiovascular diseases, in the pathophysiology, increased platelet reactivity is a descriptor of the risk of cardiovascular events in healthy persons and in patients with overt coronary artery disease. Regardless of the stimulus for activation platelet-platelet interation and thrombus formation is ultimately regulated through the GP Ⅱ b/Ⅲ a receptor
文摘Batifiban, a synthetic cyclic peptide, is a potent platelet glycoprotein GPⅡb/Ⅲa antagonist which may be useful in the treatment and prevention of acute coronary syndromes. The pharmacokinetics and pharmacodymanic （inhibition of platelet aggregation） effects, and tolerability of batifiban were investigated in healthy subjects following single bolus injection with doses of 55, 110, or 220 μg/kg, or multiple doses of an bolus followed intravenous infusion for 24 h （180 μg/kg plus 2.0 μg/minokg, and 220 μg/kg plus 2.5μg/minokg） in this phase I clinical trial. Plasma levels of batifiban and areas under the curve were found to be proportional to doses. Batifiban was rapidly eliminated with a half-life of approximately 2.5 h. Significant differences were noted for plasma levels of batifiban and areas under the curve between males and females. No significant differences in the terminal half-life were found between males and females. Batifiban reversibly inhibited ex vivo platelet aggregation in a dose- and concentration-dependent manner, consistent with its mechanism as a GPⅡ b/Ⅲa antagonist. Single and multiple intravenous doses of batifiban were found to be safe and well tolerated in healthy subjects. These results support a bolus injection plus intravenous infusion regimen of batifiban for the treatment and prevention of acute coronary syndromes.
文摘Platelet activation plays an important role in thrombosis. Platelet glycoprotein Ⅱ b/Ⅲ a （ GPⅡ b/Ⅲ a ） is the receptor of fibrinogen. Platelet cross-linking with fibrinogen through GP Ⅱ b/Ⅲ a is the process of thrombosis. Ca^2＋ is an important intracellular second messenger in platelet activation. It has been reported that GP Ⅱ b/Ⅲ a receptors were involved in the calcium influx of activated platelet, and GP Ⅱ b/Ⅲ a receptor had characteristics of calcium channel or an adjacent calcium channel.
基金supported by a grant from ShenZhen Hybio Engineering Co.,Ltd.
文摘To compare clinical outcomes and safety of eptifibatide or tirofiban in patients with acute coronary syndrome（ACS） undergoing percutaneous coronary intervention（PCI）. Methods：Thirty-six patients with ACS（unstable angina/non-ST-segment elevation myocardial infarction, UA/NSTEMI） who underwent PCI were randomly divided into two groups to receive eptifibatide or tirofiban treatment. Eptifibatide or tirofiban was predominantly initiated in the catheter laboratory before the intervention. In-hospital and 30-day MACE outcomes; bleeding as well as platelet counting were investigated in those two groups. Results：No in-hospital and 30-day MACE event occurred in the two groups. The number of ischemia leads after treatment reduced compared to that before PCI in the two groups. There was improvement in the number of ischemia leads for 24 h after administration in the tirofiban group than those in eptifibatide group（4.21 ± 2.46 vs. 3.89 ± 3.31, P =0.03）. The two groups showed no incidence of massive bleeding. Minor bleeding rates were 16.7% and 22.2% in the two groups respectively. Conclusion：Eptifibatide as an adjunct to PCI may further decrease the incidence of ischemia event in patients with ACS and improve the safety, but its long-term efficacy and side effects need further observation.
文摘Objective:To evaluate the efficacy and safety of tirofiban hydrochloride in the treatment of ischemic stroke with thrombolytic therapy.Method:Two hundred patients with acute ischemic stroke thrombolysis were randomly divided into the experimental group and the control group.The experimental group was given tirofiban with the addition of rtpa in the control group and the therapeutic effects of the two groups were compared.Results:In comparison with the control group,the NIHSS improvement rate was 98%in the experimental group within 14 days.The platelet aggregation rate and efficacy in the experimental group were significantly reduced than the control group(P<0.01).The major adverse reaction in the two groups was hemorrhage with an incidence rate of 3%.Conclusion:Tirofiban hydrochloride is a highly effective and selective platelet glycoprotein Ⅱb/Ⅲa receptor inhibitor,which is safe and effective in combination with heparin and aspirin.
文摘This paper designed a detailed procedure for monogenic hypertension diagnosis by Whole Exome Sequencing(WES)and provided reliable precise medication guidance.Identification of mutated points provides the clinician valuable information for effective individualized therapeutic option.Therapeutic options that specifically restore the pathway disturbed by these point mutations can be selected to give a precise medicinal guidance.
