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5.15 Local drugs in interventional cardiology pharmacology
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Published:July 2018
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Abstract
Percutaneous coronary intervention causes vascular injury potentially leading to restenosis via a cascade of inflammation, vascular smooth muscle proliferation, and extracellular matrix deposition. A number of approaches to local drug delivery to effectively reduce restenosis have been explored but local delivery on drug-eluting stents and drug-coated balloons have been the most successful strategies. A wide range of anti-inflammatory and antiproliferative agents has been investigated, with mTOR inhibitors and paclitaxel proving most successful in outcome studies. The clinical efficacy of locally delivered drugs depends on the release kinetics from the delivery device, the degree of uptake into the vascular wall, and the pharmacodynamic profile of the active drug. Drug-eluting stent efficacy is dependent on the platform macro- and microstructure in addition to the properties of polymer coatings; sirolimus and its analogues are the agents of choice. Most efficient drug transfer and uptake from drug-coated balloons is achieved using a matrix consisting of paclitaxel and a hydrophilic spacer or excipient.
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