ABSTRACT
This study evaluated the in vivo potential antihypertensive effect of hydroalcoholic extract of Syzygium cumini leaves (HESC) in normotensive Wistar rats and in spontaneously hypertensive rats (SHR), as well as its in vitro effect on the vascular reactivity of resistance arteries. The hypotensive effect caused by intravenous infusion of HESC (0.01-4.0 mg/kg) in anesthetized Wistar rats was dose-dependent and was partially inhibited by pretreatment with atropine sulfate. SHR received HESC (0.5 g/kg/day), orally, for 8 weeks and mean arterial pressure, heart rate, and vascular reactivity were evaluated. Daily oral administration of HESC resulted in a time-dependent blood pressure reduction in SHR, with a maximum reduction of 62%. In the endothelium-deprived superior mesenteric arteries rings the treatment with HESC reduced by 40% the maximum effect (E maxâ¡) of contraction induced by NE. The contractile response to calcium and NE of endothelium-deprived mesenteric rings isolated from untreated SHR was reduced in a concentration-dependent manner by HESC (0.1, 0.25, and 0.5 mg/mL). This study demonstrated that Syzygium cumini reduces the blood pressure and heart rate of SHR and that this antihypertensive effect is probably due to the inhibition of arterial tone and extracellular calcium influx.
ABSTRACT
JUSTIFICATIVA E OBJETIVOS: Além da ação anestésica local, a ropivacaína apresenta efeito vasoconstritor, clinicamente significativo, que pode ser observado quando da anestesia infiltrativa, o que a torna um anestésico importante no bloqueio de campo. Este trabalho teve por objetivo caracterizar o mecanismo de ação constritora da ropivacaína em músculo liso. MÉTODO: Em preparações isoladas de ducto deferente de ratos foram construídas curvas concentração-efeito de noradrenalina na ausência ou na presença da ropivacaína. Em outra série de experimentos os ratos foram tratados com reserpina (10 mg.kg-1, por via intraperitoneal) para avaliar a reatividade dos ductos deferentes à tiramina ou noradrenalina, na ausência ou presença da ropivacaína. RESULTADOS: A ropivacaína nas concentrações de 5 ou 10 æg.mL-1 potencializou o efeito máximo (Emax) da noradrenalina em 47 por cento e 35 por cento, respectivamente, enquanto que nas concentrações de 50 ou 100 æg.mL-1 inibiu o efeito máximo produzido por este agonista. Em ductos deferentes isolados de ratos reserpinizados, a ropivacaína (10 ou 20 æg.mL-1) potencializou (150 por cento e 25 por cento, respectivamente) as contrações induzidas pela noradrenalina, enquanto que as concentrações de 50 ou 100 æg.mL-1 não alteraram as respostas à noradrenalina. CONCLUSÕES: Os resultados obtidos permitem concluir que a ropivacaína bloqueia a recaptação neuronal de noradrenalina pelos terminais nervosos simpáticos.
Subject(s)
Animals , Rats , Anesthetics, Local/administration & dosage , Anesthetics, Local/pharmacokinetics , Anesthetics, Local/pharmacology , Nerve Block/methods , Muscle, Smooth , Norepinephrine/therapeutic use , Rats, WistarABSTRACT
BACKGROUND AND OBJECTIVES: In addition to local anesthetic action, ropivacaine has clinically significant vasoconstrictor effects, which may be observed at infiltrative anesthesia, making it an important anesthetic for field blockade. This study aimed at characterizing the constrictor mechanism of ropivacaine on smooth muscles. METHODS: Norepinephrine concentration-effect curves in the absence or presence of ropivacaine were plotted on isolated preparations of vas deferens of rats. In another series of experiments rats were treated with reserpine (10 mg.kg-1, i.p.) to evaluate vas deferens reactivity to tyramine or norepinephrine, in the absence or presence of ropivacaine. RESULTS: Ropivacaine 5 or 10 microg.mL-1 potentiated maximum norepinephrine effect (Emax) in 47% and 35%, respectively, while higher concentrations (50 or 100 microg.mL-1) inhibited its maximum effect. In isolated vas deferens of rats treated with reserpine, ropivacaine (10 or 20 microg.mL-1) potentiated (150% and 25%, respectively) norepinephrine-induced contractions, while higher concentrations (50 or 100 microg.mL-1) have not changed responses to norepinephrine. CONCLUSIONS: Ropivacaine blocks neuronal norepinephrine reuptake by sympathetic nerve terminals.
