China
Africa
Explore chapters and articles related to this topic
Intravenous anti-platelet therapy—GP IIb/IIIa blockers and cangrelor
Published in K Sarat Chandra, AJ Swamy, Acute Coronary Syndromes, 2020
Shraddha Ranjan, Gagandeep Singh Wander
It has been proven that shorter GP IIb/IIIa inhibitor infusions and the use of a radial approach may significantly improve the safety profile of GP IIb/IIIa inhibitors and restore interest in their use. If high-risk patients are targeted who have been not adequately preloaded with clopidogrel and have a low risk of bleeding, the net clinical benefit of these drugs increases a lot. These drugs are usually started at the time of PCI as bailout or before PCI if the patient has not been adequately preloaded with P2Y12 inhibitors. Eptifibatide and tirofiban have renal clearance and need dose modification in renal dysfunction. Intracoronary administration of abciximab has been shown to be safe and effective with favourable effects on TIMI flow.
Antiplatelet therapy in interventional cardiology
Published in John Edward Boland, David W. M. Muller, Interventional Cardiology and Cardiac Catheterisation, 2019
Tirofiban is a competitive inhibitor of the fibrinogen‐binding site. It is short acting (2–4 hours) with a half‐life of 2 hours. Tirofiban was trialled in 2139 patients with acute coronary syndromes undergoing percutaneous revascularisation.51 Over 90% were treated with angioplasty alone. Patients received either placebo or tirofiban (10 µg/kg bolus followed by a 36 hours infusion of 0.15 µg/kg/min). At 30 days, the combined endpoint of death, MI, revascularisation or need for non-elective stenting during the procedure was not significantly different in the tirofiban and placebo groups (10% vs. 12.2% p = 0.16), although there was a difference at 7 days (7.6% vs. 10.4% p = 0.022).
Percutaneous coronary intervention in the elderly
Published in Wilbert S. Aronow, Jerome L. Fleg, Michael W. Rich, Tresch and Aronow’s Cardiovascular Disease in the Elderly, 2019
The greatest concern with use of GP IIb/IIIa inhibitors in the elderly is the increased risk of bleeding, both at the access site (26% vs. 20%) and non-access site (5.2% vs. 2.5%), but without increased intracranial hemorrhage or increased need for blood transfusion (88). Most of this excess bleeding risk could be decreased with careful dosing since an evaluation of the CRUSADE registry showed a remarkable 64.5% overdoing of GP IIb/IIIa inhibitors in patients aged >75 years compared to only 8.5% in patients <65 years old. Overdosing GP IIb/IIIa inhibitors was associated with increased risk of bleeding (OR 1.38, 95% CI 1.12–1.70). Abciximab is given at a dose of 0.25 mg/kg IV bolus, then 0.125 mcg/kg/min IV (max 10 mcg/min), and no adjustment is needed for renal clearance. However, dose adjustment is required for eptifibatide and tirofiban. With normal renal function, eptifibatide is given as 180 mcg/kg IV bolus ×2, 10 min apart (max 22.6 mg each bolus) and then an infusion of 2 mcg/kg/min (max 15 mg/hr) after first bolus. For patients with a creatinine clearance of < 50 mL/min, the infusion should be decreased to 1 mcg/kg/min (max 7.5 mg/hr). It is contraindicated in dialysis patients.
Targeting protein-protein interactions with low molecular weight and short peptide modulators: insights on disease pathways and starting points for drug discovery
Published in Expert Opinion on Drug Discovery, 2023
Daniela Trisciuzzi, Bruno O. Villoutreix, Lydia Siragusa, Massimo Baroni, Gabriele Cruciani, Orazio Nicolotti
Interfering PPIs with LMW molecules or short peptides is difficult, but there are some successful stories. Tirofiban is a LMW compound that prevents blood clotting by acting as reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor (also known as integrin αIIbβ3) which impedes platelet aggregation [25]. Maraviroc is an allosteric inhibitor of the HIV gp120/CCR5 receptor interaction blocking HIV viral entry [26]. More recently, venetoclax has been approved and is considered as the first selective LMW BH3-mimetic inhibitors of the anti-apoptotic Bcl-2 protein family [27]. In recent years, some attempts to bias these ‘intractable’ targets focused on the development of allosteric modulators, acknowledged as valuable solutions to modulate PPIs [28]. Some examples are the LMW allosteric modulators of tubulin dimerization or new peptide modulators interfering with the PD-1/PD-L1 pathway or targeting lymphocyte function-associated antigen-1-intercellular adhesion molecule 1 (LFA-1/ICAM-1) [28,29]. Noteworthy, the SARS-CoV-2 spike protein-angiotensin-converting enzyme 2 (ACE2) system represents an interesting target for drug discovery and some allosteric modulators have been reported [30,31].
Analysis of risk factors for the efficacy of tirofiban in the treatment of acute ischemic stroke
Published in Neurological Research, 2023
Chong Liu, Lu Yin, Yinqin Hu, Zhizhen Shi, Qiaoyan Zhu, Qian Xiao, Guoyi Li, Jiwei Cheng, Yangbo Hou
The single factor analysis of the early efficacy of tirofiban included the comparison of the two groups of patients regarding gender, age, medical history, hypertension, diabetes, cerebral infarction, coronary atherosclerotic heart disease, atrial fibrillation, smoking history, elevated triglycerides, low density lipoprotein cholesterol, elevated HbA1c, elevated homocysteine, mRS score at admission, NIHSS score at admission, days of treatment, time from onset to treatment, TOAST and OCSP classification, use of antithrombotic agents, intravenous thrombolysis or interventional therapy. And there was no statistical significance between the two groups (P > 0.05); no symptomatic intracranial hemorrhage or other adverse reactions occurred in the 2 groups (P = 0). There were statistically significant differences between the two groups in heavy drinking, elevated total cholesterol, NIHSS score at initiation of treatment and time from onset to treatment (P < 0.05), as shown in Table 1.
Tirofiban potentiates agonist-induced platelet activation and degranulation, despite effectively inhibiting aggregation
Published in Platelets, 2022
Martina Aguiar Bucsai, Christian Idel, Barbara Wollenberg, Christine Mannhalter, Admar Verschoor
Tirofiban has also become a valuable laboratory tool due to its ability to effectively prevent the fibrin-mediated coalescing of individual activated platelets into an amorphous, insoluble clot in vitro. Such inhibition has become especially important and useful in settings where the formation of cell clumps would negatively influence, even preclude, assessment via important analytic laboratory methods, such as flow cytometry. The analysis of platelet surface activation markers through flow cytometry is one of the most frequently used methods to assess platelet responsiveness, as it can simultaneously provide information about platelet activation, degranulation, and interaction with each other (aggregation) and with other cells [22]. Moreover, it is appealing to use flow cytometry analysis due to its robustness, the ability to perform multi-parametric (depending on the number of fluorophores used and detectable by the machine) analysis in rapid fashion, and its widespread availability.