ABSTRACT
Objective:To investigate the effects of preoperative ticagrelor application on postoperative NF-κB signa-ling pathway,platelet aggregation and myocardial microcirculatory perfusion in patients with acute myocardial in-farction(AMI)and multivessel lesions undergoing percutaneous coronary intervention(PCI).Methods:A total of 120 AMI patients with multivessel lesions treated in our hospital were selected,randomly and equally divided into clopidogrel group and ticagrelor group.Corresponding drugs were given in each group before and after PCI.NF-κB signaling pathway related indexes,platelet aggregation rate,myocardial microcirculatory indexes before and af-ter medication,and incidence of major adverse cardio-and cerebrovascular events(MACCE)were observed and compared between two groups.Results:On 7d after PCI,compared with clopidogrel group,there were significant reductions in corrected TIMI frame count(CTFC)of left anterior descending(LAD)[(23.83±2.69)vs.(20.48± 3.05)],left circumflex(LCX)[(20.93±2.82)vs.(18.35±2.37)]and right coronary artery(RCA)[(23.68± 3.15)vs.(21.13±2.79)]in ticagrelor group,P=0.001 all;compared with clopidogrel group after 30d treatment,there were significant reductions in platelet maximum aggregation rate,maximum depression amplitude of ST seg-ment,ST segment depression time,24h ischemia onset times,levels of Toll-like receptor 4(TLR4)protein,NF-κB protein,tumor necrosis factor(TNF)-a and interleukin(IL)-6 in ticagrelor group,P=0.001 all.There was no significant difference in incidence rate of MACE between two group within six months,P=0.186.Conclu-sion:Ticagrelor can improve myocardial microcirculation,inhibit platelet aggregation,and reduce inflammatory re-sponse in AMI patients with multivessel lesions,and the mechanism may be related to the inhibition of NF-κB sig-naling pathway activity by ticagrelor.
ABSTRACT
Se demostró la intercambiabilidad terapéutica mediante un estudio de bioequivalencia en 25 voluntarios sanos de una formulación cubana de carbamazepina de 200 mg con respecto al producto innovador (Tegretol®), en condiciones de administración a dosis única; el diseño experimental fue cruzado a doble ciegas y aleatorizado; el periodo de lavado fue de 15 días. Las extracciones para la obtención del plasma, se realizaron a las 0; 0,5; 1; 1,5; 2; 3; 4; 6; 8; 10; 12; 16; 20; 24; 48; 72; 96 y 120 h. Para el análisis se empleó un método analítico por cromatografía líquida de alta eficiencia, isocrático en fase reversa con detección ultravioleta. Se estimaron mediante técnicas no compartimentales los parámetros farmacocinéticos (AUC0-t, AUCt-¥, Cmax, Tmax y T1/2) representativos de la biodisponibilidad en magnitud y velocidad. Sobre la base de los resultados estadísticos, ambas formulaciones resultaron bioequivalentes.
It was possible to demonstrate the therapeutic interchange level by means of a bioequivalence study in 25 healthy volunteers of a Cuban formula of Carbamazepine(200 mg) according to the innovative product (Tegretol®) for a administration of unique dose; the experimental design was of crossed, double-blind and random type; washing period was of 15 days. Extractions for plasma obtaining were performed at 0, 0,5, 1, 1,5, 2, 3, 4, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96 and 120 hours. In analysis we used an analytical method by high performance liquid chromatography, isocratic type in reverse phase with UV detection. By means of non-compartment techniques pharmacokinetic parameters (AUC0-t, AUC t-¥, Cmax, Tmax, and T½) were estimated, which are representative of bioavailability in magnitude and speed. On the base of statistical results, both formulae were bioequivalent.