CAIO DE ASSIS MOURA TAVARES

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Instituto do Coração, Hospital das Clínicas, Faculdade de Medicina - Médico
LIM/65, Hospital das Clínicas, Faculdade de Medicina

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  • article 13 Citação(ões) na Scopus
    Ranolazine Injection Into Coronary or Femoral Arteries Exerts Marked, Transient Regional Vasodilation Without Systemic Hypotension in an Intact Porcine Model
    (2011) NIEMINEN, Tuomo; TAVARES, Caio A. M.; PEGLER, Jose R. M.; BELARDINELLI, Luiz; VERRIER, Richard L.
    Background-We examined whether intracoronary or intrafemoral administration of ranolazine produces local vasodilation. Methods and Results-Effects of intra-arterial ranolazine on coronary and femoral artery vasodilation and systemic hemodynamic function were studied in anesthetized pigs (n=27). Ranolazine, nitroglycerin, or saline (control) was injected into the left anterior descending (LAD) coronary artery or femoral artery (2-mL bolus in 10 seconds). Pretreatment with prazosin (300 mu g/kg IV) allowed determination of alpha(1)-adrenergic receptor involvement (n=8). Rapid intracoronary administration of ranolazine (0.048 mg/kg) to achieve high local concentrations resulted in 91 +/- 11% increase in LAD coronary artery flow and 39 +/- 7% reduction in coronary vascular resistance (both, P<0.0001). This effect lasted 2-3 minutes without change in heart rate or rate-pressure product. Mean arterial pressure decreased marginally (by 2 +/- 1 mm Hg, P=0.01). Maximum systemic plasma concentration (0.93 +/- 0.29 mu mol/L) remained in subtherapeutic range. Pretreatment with prazosin abolished these effects. Intracoronary nitroglycerin (100 mu g) increased LAD coronary artery flow by 112 +/- 25% (P=0.02), but the effect lasted <2 minutes; mean arterial pressure decreased by 4 +/- 1 mmHg (P=0.01). Intrafemoral injection of ranolazine (0.24 mg/kg, ie, one-tenth of the systemic bolus) resulted in a 70 +/- 19% increase in femoral artery flow (P=0.05) and 26 +/- 5% reduction in femoral artery resistance (P=0.004). At 2 minutes after the injection, the femoral flow remained 16 +/- 9% above the baseline and dilatory effects occurred without tolerance to repeated injections. Conclusions-Intracoronary or intrafemoral ranolazine bolus exerts a marked, 2- to 3-minute dilatory effect that is comparable to nitroglycerin in magnitude but more persistent, attributable primarily to alpha(1)-adrenergic blockade. (Circ Cardiovasc Interv. 2011;4:481-487.)