Bruggeman C A, Engels W, Endert J
Department of Medical Microbiology, University of Limburg, Maastricht, The Netherlands.
Arch Virol. 1987;97(1-2):27-35. doi: 10.1007/BF01310731.
Subcutaneous (s.c.) administration of Acyclovir (ACV) (100 mg/1 kg bodyweight) resulted in an ACV blood level of 80 microM at 2 h post infection. Thereafter the level declined rapidly reaching undetectable levels at 12 h post infection. Administration of pro-ACV (100 mg/kg body weight) by s.c. or intravenous (i.v.) route resulted in ACV levels of 75 microM and 160 microM respectively after 30 min. But here again the blood level of ACV declined rapidly and was completely disappeared after 12 h. Continuous administration of pro-ACV in daily doses of 100, 250 and 350 mg/kg body weight resulted in ACV blood levels of 15 microM, 19 microM and 39 microM, respectively. The effect of ACV and pro-ACV on the replication of CMV was measured in immunesuppressed rats. In rats inoculated with RCMV the daily administration of 25 to 50 mg ACV per kg body weight by s.c. injections twice daily, did not result in a reduction of virus titers in spleen and liver, but when the RCMV-infected rats were treated by 100 mg pro-ACV per kg body weight virus titers in the spleen and liver were significantly reduced as compared with those in sham-treated animals.
皮下注射阿昔洛韦(ACV)(100毫克/1千克体重)后,感染后2小时ACV血药浓度为80微摩尔/升。此后,该浓度迅速下降,在感染后12小时降至检测不到的水平。通过皮下或静脉注射途径给予前体阿昔洛韦(100毫克/千克体重),30分钟后ACV血药浓度分别为75微摩尔/升和160微摩尔/升。但同样,ACV血药浓度迅速下降,12小时后完全消失。以每日100、250和350毫克/千克体重的剂量持续给予前体阿昔洛韦,ACV血药浓度分别为15微摩尔/升、19微摩尔/升和39微摩尔/升。在免疫抑制大鼠中测量了ACV和前体阿昔洛韦对巨细胞病毒复制的影响。在接种了RCMV的大鼠中,每天两次皮下注射每千克体重25至50毫克ACV,脾脏和肝脏中的病毒滴度没有降低,但当用每千克体重100毫克前体阿昔洛韦治疗RCMV感染的大鼠时,与假处理动物相比,脾脏和肝脏中的病毒滴度显著降低。