防己生物碱的毒性及降压作用
TOXICITY AND HYPOTENSIVE EFFECT OF THE ALKALOIDS OF SINOMENIUM ACUTUM
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摘要: 正常狗2只,以防己生物碱連日給药,最高一次灌胃量达160毫克/公斤,为降压有效量16倍,无急性不良反应发生,服药过程中体重、食量及外表皆无明显改变。实驗治疗的3只高血压皮桥狗,无論心电图、血清磺溴酞鈉存留率及全血非蛋白氮含量皆属正常;但个別狗首次給药曾发生特异反应,大剂量长期給药可使全血非蛋白氮含量稍高,临床試用尚宜适当注意。总碱对麻醉或不麻醉实驗动物无論靜脉注射或灌胃都有肯定的急性降压效果,其作用特点为降压迅速、显著,持續时間約2—4小时,連續多次給药有快速耐受現象。对慢性实驗治疗狗的疗效不著,可能与其作用特点有关,可考虑与作用緩慢而持久的降压药合并应用。总碱的降压与其抗腎上腺素作用及神經反射机制有关。总碱无阻断神經节作用,其降压与M-胆碱反应系統无关,也非組織胺释放所致。在本实驗条件下未見总碱有直接扩张血管的作用。靜脉注射1—2毫克/公斤,对麻醉狗的心輸出量有抑制性影响,总外周阻力的降低不明显。Abstract: The total alkaloids of Sinomenium acutum, fed by stomach tube or injected intravenously, produced a definite hypotensive effect in both anaesthetized and unanaesthetized animals. The onset was fast; the hypotension was marked and lasted 2—4 hours. Tachyphylaxis developed on repeated medications. This hypotension was mediated via the adrenolytic action and the nervous reflex mechanism, but not the histamine liberation. The alkaloids did not block ganglions, and exerted no influence on the M-cholinergic reactive system. Direct vasodilation was not observed. In anaesthetized dogs, intravenous injections of the alkaloids 1—2 mg/kg decreased the cardiac output, yet not the total peripheral resistance. Three renal hypertensive dogs were fed 10—40mg/kg/day for 15 days. The hypotensive effect was insignificant, owing probably to tachyphylaxis. The EKG, serum BSP retention, and blood NPN level revealed nothing abnormal. One of the three dogs collapsed immediately after the first medication, but tolerated well after the succeeding doses. Two normal dogs were fed 20—160 mg/kg/day for 16 days. Untoward reactions were not noticed, except a slight elevation of blood NPN in 1 dog.
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