Picotamide is an antiplatelet drug with a dual inhibitory action. Thus, picotamide inhibits both thromboxane A2 (TxA2) receptors and TxA2 synthase and, at variance with aspirin, does not interfere with endothelial prostacyclin (PGI2) production. Two large randomized trials have been performed to assess the clinical efficacy of picotamide in patients at risk of atherothrombosis. The ADEP study compared peripheral artery disease (PAD) patients randomized to picotamide or placebo. This study did not show a significant reduction of cardiovascular events by picotamide but a subgroup analysis showed its potential usefulness in patients with diabetes. To investigate this issue further, the DAVID study recently enrolled diabetic patients with PAD randomized to picotamide versus aspirin; the results showed a significant reduction of overall mortality in the picotamide group. Moreover long-term picotamide treatment in diabetes promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques. These data suggest that picotamide may represent an interesting drug to be further investigated in future trials in the atherothrombotic setting.
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Eur J Pharmacol
March 2024
Jagiellonian University, Jagiellonian Centre for Experimental Therapeutics (JCET), Bobrzynskiego 14, Krakow, Poland; Department of Pharmacology, Jagiellonian University Medical College, Grzegorzecka 16, 31-531, Kraków, Poland. Electronic address:
The angiotensin (Ang)-(1-12)/Ang II pathway contributes to cardiac pathology. However, its involvement in the development of peripheral endothelial dysfunction associated with heart failure (HF) remains unknown. Therefore, this study aimed to characterise the effect of exogenous Ang-(1-12) and its conversion to Ang II on endothelial function using the murine model of HF (Tgαq*44 mice), focusing on the role of chymase and vascular-derived thromboxane A (TXA).
View Article and Find Full Text PDFBioorg Med Chem
September 2021
School of Pharmacy, Nanjing Medical University, Nanjing 211166, China. Electronic address:
In order to discover antiplatelet drug with novel structure and expand our research scope, total twenty 1,3-benzenedisulfonyl piperazines, were designed and synthesized. These target compounds were divided into two series, namely 4-methoxy-1,3-benzenedisulfonyl piperazines of series 1 and 4-ethoxy-1,3-benzenedisulfonyl piperazines of series 2. With adenosine diphosphate (ADP), arachidonic acid (AA) and collagen as inducers, respectively, the Born turbidimetric method was used to screen the antiplatelet activity in vitro of all target compounds at a concentration of 1.
View Article and Find Full Text PDFPharmacol Res Perspect
May 2021
Department of Urology, University Hospital, LMU Munich, Munich, Germany.
Picotamide is a thromboxane A (TXA ) receptor antagonist and TXA synthase inhibitor. In clinical studies, it has been considered as a platelet aggregation inhibitor and improved renal function. In vitro studies suggested inhibition of smooth muscle contraction by picotamide, which is poorly understood.
View Article and Find Full Text PDFCurr Vasc Pharmacol
January 2022
Research and Study Center of the Italian Society of Angiology and Vascular Pathology (Societa Italiana di Angiologia e Patologia Vascolare, SIAPAV), Milan, Italy.
Background: Clopidogrel monotherapy is guideline-recommended in symptomatic peripheral artery disease (PAD). The advent of new antithrombotic strategies prompts an updated analysis of available evidence on antiplatelet therapy for PAD.
Methods: We searched MEDLINE, Embase and CENTRAL through January 2019 for randomised controlled trials and observational studies comparing antiplatelet therapies as monotherapy, dual therapy, or combination with anticoagulants.
Iran J Pharm Res
January 2019
School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
In our present investigation, a series of novel 4-methoxy-1,3-benzenediolyl-hydrazones were designed and synthesized, and their ability to inhibit platelet aggregation was evaluated by adenosine diphosphate (ADP) and arachidonic acid (AA). The structures of the synthesized compounds were confirmed by spectral data. Results demonstrated that the activities of all compounds excelled the positive drug Picotamide (25.
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