PRAZIQUANTEL, A NEW BROAD-SPECTRUM ANTISCHISTOSOMAL AGENT
PRAZIQUANTEL, A NEW BROAD-SPECTRUM ANTISCHISTOSOMAL AGENT
复制标题
DOI：
10.1007/bf00389899
复制
发表时间：
1977-01-01
期刊：
影响因子：
--
通讯作者：
ANDREWS, P
中科院分区：
文献类型：
--
作者：
GONNERT, R;ANDREWS, P
吡喹酮，（2-环己基羰基）-1,2,3,6,7,11b-六氢- 2h吡嗪[2,1a]异喹啉-4 -1，是一类新的抗血吸虫化合物。描述了吡喹酮对小鼠、Mastomys和叙利亚仓鼠的曼氏血吸虫疗效的详细研究结果。吡喹酮经口服和所有非肠外给药途径试验后有效。使寄生虫减少至少95%所需的吡喹酮用量取决于宿主物种以及给药途径和时间表。小鼠的总剂量为200- 1000mg /kg， Mastomys和仓鼠的总剂量为100- 500mg /kg。在所有3种药物中，将总剂量分成3个或更多的小剂量，在1天内给药，其疗效约为单次口服相同总剂量后的两倍。单次s.c剂量仅稍微有效一点，而单次滴注橄榄油的效果大约是单次口服的两倍。吡喹酮对侵染阶段非常有效，对7日龄以内的血吸虫则效果稍差。它对2至4周龄的幼虫效果较差，但对5周龄及以上的血吸虫再次有效。吡喹酮对两种性别的曼氏血吸虫均有相同效果。它对未配对的幼雌虫效果较差，但对单雄虫完全有效。吡喹酮对小鼠曼氏梭菌的治疗效果不受宿主的品系或性别、蠕虫负荷或感染年龄的影响。考虑到现有的所有数据，吡喹酮有望成为一种非常有效的抗血吸虫药物。
Praziquantel, (2-cyclohexylcarbonyl)-1,2,3,6,7,11b-hexa-hydro-2H pyrazino[2,1a]isoquinolin-4-one, belongs to a new series of antischistosomal compounds. The results of a detailed study of the efficacy of praziquantel on Schistosoma mansoni in mice, Mastomys and Syrian hamsters are described. Praziquantel is effective after oral and all parenteral routes of administration tested. The amount of praziquantel required to achieve parasite reductions of at least 95% depends on the host species and on the routes and schedules of administration. Total doses range from 200-1000 mg/kg in mice and from 100-500 mg/kg for Mastomys and hamsters. In all 3 species, splitting of the total dose into 3 or more fractional doses given within 1 day approximately doubles the efficacy over that achieved after a single oral administration of the same total dose. A single s.c. dose is only slightly more effective, while a single i.m. injection in olive oil is about twice as effective as a single oral administration. Praziquantel is very effective against the invading stages and slightly less against schistosomules up to an age of 7 days. It is less effective against 2 to 4 wk old juveniles, but is effective again against 5 wk old and older schistosomes. Praziquantel is equally effective against both sexes of S. mansoni. It is less effective against unpaired and therefore juvenile female worms, but fully effective against single male worms. The efficacy of praziquantel on S. mansoni in mice is not influenced by the strain or sex of the host, the worm burden or age of the infection. Considering all data available, praziquantel promises to be a very potent antischistosomal drug.