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KMID : 0379520100260030223
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한국독성학회지
2010 Volume.26 No. 3 p.223 ~ p.232
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General Pharmacology of Artesunate, a Commonly used Antimalarial Drug : Effects on Central Nervous, Cardiovascular, and Respiratory System
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Lee Hyang-Ae
Kim Ki-Suk
Kim Eun-Joo
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Abstract
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Artesunate, a semi-synthetic derivative of artemisinin, is used primarily as a treatment for malaria. Its effects on the central nervous system, general behavior, and cardiovascular, respiratory, and other organ systems were studied using mice, rats, guinea pigs, and dogs. Artesunate was administered orally to mice at doses of 125, 250, and 500 ㎎/㎏ and to rats and guinea pigs at 100, 200, and 400 ㎎/㎏. In dogs, test drugs were administered orally in gelatin capsules at doses of 50, 100, and 150 ㎎/㎏. Artesunate induced insignificant changes in general pharmacological studies, including general behavior, motor coordination, body temperature, analgesia, convulsion modulation, blood pressure, heart rate (HR), and electrocardiogram (ECG) in dogs in vivo; respiration in guinea pigs; and gut motility or direct effects on isolated guinea pig ileum, contractile responses, and renal function. On the other hand, artesunate decreased the HR and coronary flow rate (CFR) in the rat in vitro; however, the extent of the changes was small and they were not confirmed in in vivo studies in the dog. Artesunate increased hexobarbital-induced sleeping time in a dose-related manner. Artesunate induced dose-related decreases in the volume of gastric secretions and the total acidity of gastric contents, and induced increases in pH at a dose of 400 ㎎/㎏. However, all of these changes were observed at doses much greater than clinical therapeutic doses (2.4 ㎎/㎏ in humans, when used as an anti-malarial). Thus, it can be concluded that artesunate is safe at clinical therapeutic doses.
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KEYWORD
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Artesunate, General pharmacology, Antimalarial drug, Central nervous system, Cardiovascular system, Respiratory system
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