OBJECTIVE Paclitaxel added to angiographic contrast medium (CM) has been shown to inhibit restenosis in the porcine coronary overstretch model. This study determined early local tissue concentrations after the administration of different paclitaxel doses and preparations. METHODS Fifteen pigs received 2 stents each in the left coronary artery. During and/or after the intervention, paclitaxel-containing CM or diluted Taxol was injected. Fifteen minutes after the last intracoronary injection, paclitaxel concentrations in the arterial wall and myocardium were measured by high-performance liquid chromatography. RESULTS Mean paclitaxel concentrations in the left coronary arteries reached 3-10 microM. Higher volumes and higher paclitaxel concentrations resulted in higher tissue concentrations. Paclitaxel in CM was better tolerated and led to higher local concentrations than diluted Taxol. Low paclitaxel concentrations in the uninjected right coronary artery and in plasma indicate selectivity. CONCLUSIONS When admixed to CM, paclitaxel results in local tissue concentrations proportional to the amount of the drug injected.