呋喃西林的体内过程和一些药理作用

人和兔口服呋喃西林后,易从胃腸道內吸收,吸收的主要部位是小腸。給药后4小时血浆浓度到达最高峯,以后迅速下降。总胆管結扎后呋喃西林由胃腸道吸收显著減少。呋喃西林被吸收后,能分布至主要脏器內,其中以脑及脾脏中含量最高,极少量以原形由尿排出。体外試驗,呋喃西林与多种組織一起培养,即被分解。以四氯化碳損伤兔的肝脏功能后,不能提高呋喃西林在血浆中的浓度。呋喃西林对血压、呼吸、环己巴比妥鈉麻醉吋间无甚影响椅尥巳茸饔谩

OBSERVATION ON THE FATE AND CERTAIN PHARMA-COLOGICAL ACTION OF FUNACILLIN

1. After oral administration to rabbits and man, Funacillin was absorbed mainly in the small intestine and very slightly in the stomach and colon, reaching its peak concentration in the plasma in 4 hours, and then declining rapidly; a single dose (200 mg/kg body weight) given to a rabbit orally yielded in 4 hours a level of about 14 μg/ml and then a trace only at the end of 12 hours. 2.After absorption, Funacillin was distributed throughout different organs, as liver, brain (cortex, midbrain and brainstem), spleen, lung and kidney with varying degree of concentration which was highest in brain and spleen, the time of reaching its peak concentration in organs coincides with that in plasma. In the rabbits, whose liver function was damaged by carbon tetrachloride, the peak concentration in plasma was no higher than that in the normal rabbit. Ligation of the common bile duct caused a decrease in its concentration in plasma. 3. When incubated with slices of liver, brain, intestine and kidney, for 1 hour, Funacillin was not quantitatively recovered, because a certain amount had been decomposed by the tissue slices, particularly the liver. 4.Funacillin was excreted through the urine only in small amount (1—5% of the original dose). 5. Artificial pyrexia produced by subcutaneous injection of E. Coli vaccine to cats, was not abolished by Funacillin. 6. No demonstrable effect was observed on the blood pressure and respiration, when Funacillin was given intravenously to rabbits. 7. Funacillin did not prolong the anesthetic time of Evipan.