伯氨喹和三氟乙酰伯氨喹对家兔溶血毒性的比较

COMPARATIVE STUDY ON HEMOLYTIC TOXICITY OF TRIFLUOROACETOPRIMAQUINE AND PRIMAQUINE IN RABBITS 

健康家兔分别灌胃伯氨喹（ＰＱ）和三氟乙酰伯氨喹（Ｍ８５０６）４０ｍｇ／ｋｇ·ｄ×４ｄ，给药前（ｄｏ）和给药后ｄ３、ｄ５、ｄ７、ｄ１０、ｄ１４和ｄ２１分别经兔耳静脉取血测定高铁血红蛋白（ｍｅｔＨｂ）、网织红细胞（ｒｅｔ）和亨氏小体（Ｈｂｄ）。ＰＱ组ｍｅｔＨｂ、ｒｅｔ和Ｈｂｄ于给药后ｄ３－ｄ５均开始升高，ｄ７－ｄ１０达高峰，ｄ１０以后逐渐下降。Ｍ８５０６组仅Ｈｂｄ升高较为显著，ｍｅｔＨｂ和ｒｅｔ的变化与对照组相仿，未见显著增高，提示在等剂量条件下Ｍ８５０６的溶血毒性并不高于ＰＱ。

trifluoroacetoprimaquine (M8506) exhibited high effect on tissue schizont of P.cynomolgi and low toxicity in mice,rats and dogs as compared with primaquine (PQ) accor ding to our previous studies.In order to determine their hemolytic toxicity,we dosed rabbits with M8506 and PQ at a dose of 40 mg/kg per day for 4 days,respectively.Blood samples were drawn from the ear vien of the rabbits for determining of the following parameters,ie.methemoglobin (metHb),reticulocyte (ret)and Heizbody (Hbd) on d o before treatment and on d 3,d 5,d 7,d 10 ,d 14 and d 21 after treatment.The results showed that after drug administration the levels of metHb,ret and Hbd in PQ group increased on d 3-d 5,and reached their peak le vels on d 7-d 10 ,and then declined gradually from d 10 -d 14 .The mean percentage concentration of metHb,mean count of ret and Hbd in PQ group on d 7 after medication were 22.1 ± 21.8% , 92.0 ± 88.0/ 1 000 RBCand 203.8 ± 126.7/ 1 000 RBC,which were significantly higher than those of the control (8.2 ± 5.3% , 37.5 ± 16.2/ 1 000 RBC and 57.4 ± 45.1/ 1 000 RBC) .In M8506 group,the mean Hbd count (196.3 ± 123.1/ 1 000 RBC,on d 7 after treatment was also higher than that of the controls,but its mean metHb percentage concentration (10.8 ± 8.9%) and mean ret count (42.2 ± 20.3/ 1 000 RBC) were similar to those of the controls ( P > 0.05) .The results suggested that the hemolytic toxicity induced by M8506 in rabbits might be similar to or even lower than that induced by PQ.