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Lee HA, Kim KS, Kim EJ. General Pharmacology of Artesunate, a Commonly used Antimalarial Drug:Effects on Central Nervous, Cardiovascular, and Respiratory System. Toxicol Res. 2010;26(3):223-32doi: 10.5487/TR.2010.26.3.223.
Lee, H. A., Kim, K. S., & Kim, E. J. (2010). General Pharmacology of Artesunate, a Commonly used Antimalarial Drug:Effects on Central Nervous, Cardiovascular, and Respiratory System. Toxicological research, 26(3), 223-32. https://doi.org/10.5487/TR.2010.26.3.223
Lee, Hyang-Ae, et al. "General Pharmacology of Artesunate, a Commonly used Antimalarial Drug:Effects on Central Nervous, Cardiovascular, and Respiratory System." Toxicological research vol. 26,3 (2010): 223-32. doi: https://doi.org/10.5487/TR.2010.26.3.223
Lee HA, Kim KS, Kim EJ. General Pharmacology of Artesunate, a Commonly used Antimalarial Drug:Effects on Central Nervous, Cardiovascular, and Respiratory System. Toxicol Res. 2010 Sep;26(3):223-32. doi: 10.5487/TR.2010.26.3.223. PMID: 24278528; PMCID: PMC3834478.
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Toxicol Res. 2010 Sep;26(3):223-32. doi: 10.5487/TR.2010.26.3.223.

General Pharmacology of Artesunate, a Commonly used Antimalarial Drug:Effects on Central Nervous, Cardiovascular, and Respiratory System.

Toxicological research

Hyang-Ae Lee, Ki-Suk Kim, Eun-Joo Kim

Affiliations

  1. Department of Pharmacological Research, Korea Institute of Toxicology, Korea Research Institute of Chemical Technology, Daejeon 305-343, Korea.

PMID: 24278528 PMCID: PMC3834478 DOI: 10.5487/TR.2010.26.3.223

Abstract

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 mg/kg and to rats and guinea pigs at 100, 200, and 400 mg/kg. In dogs, test drugs were administered orally in gelatin capsules at doses of 50, 100, and 150 mg/kg. 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 mg/kg. However, all of these changes were observed at doses much greater than clinical therapeutic doses (2.4 mg/kg in humans, when used as an anti-malarial) . Thus, it can be concluded that artesunate is safe at clinical therapeutic doses.

Keywords: Antimalarial drug; Artesunate; Cardiovascular system; Central nervous system; General pharmacology; Respiratory system

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