Contragestational effects of dihydroartemisinin and artesunate
Xu, J.H.; Zhang, Y.P.
Yao Xue Xue Bao 31(9): 657-661
1996
ISSN/ISBN: 0513-4870 PMID: 9863230 Document Number: 464195
In experiments carried out in mice, hamsters, guinea pigs and rabbits both dihydroartemisinin and artesunate showed contragestational effect. In mice and rabbits they caused embryo absorption whereas in hamsters and guinea pigs they induced abortion. The contragestational ED-50 of dihydroartemisinin given sc on d 7 of pregnancy in mice and d 5 of pregnancy in hamsters were 32.8 (27.7 apprx 38.9) mg cntdot kg-1 and 6.1 (5.6 apprx 6.7) mg cntdot kg-1 respectively. The ED-50 of this drug given im on d 18 of pregnancy in guinea pigs was 18.3 (13.9 apprx 24.2) mg cntdot kg-1. Dihydroartemisinin also showed mid-pregnancy terminating effect in hamsters. The contragestational ED-50 of artesunate given sc on d 5 of pregnancy in hamsters and the ED-50 of sodium artesunate given sc on d 5 apprx 8 of pregnancy in hamsters were 12.2 (10.3 apprx 14. 4) mg cntdot kg-1 and 1.0 (0.9-1.2) mg cntdot kg-1 daily respectively. Results of light microscopic examination revealed that dihydroartemisinin was selectively toxic to embryo sac. At dose levels sufficient to induce embryo sac necrosis, dihydroartemisinin did not injure the uterus and ovary of the maternal animals. On the ground of the foregoing observations we consider that dihydroartemisinin, artesunate and their analogous drugs should not be used to treat malaria in pregnant women and there is the possibility to exploit intentional abortion agents from artemisinin derivatives.