Department of Pharmacology, Postgraduate Institute of Medical Education and Research, Chandigarh 160012, India. drbikashus @ yahoo.com
Pharmacology. 2009;84(6):323-32. doi: 10.1159/000252658. Epub 2009 Oct 23.
Artemisinin has been used effectively in malaria treatment. With the emerging resistance to malaria, the optimum and judicial use of the drug has become important. The drug metabolism and toxicology can have an impact on the therapeutic profile and clinical use of this antimalarial agent. In this review, we discuss the pharmacokinetics and toxicological aspects of artemisinin and its therapeutic implications. Artemisinins have several dosing routes including oral, intramuscular, intravenous and rectal. With repeated dosing, artemisinin has propensity for autoinduction, leading to decreased plasma levels on repeated dosing. Combination with other antimalarials in most cases did not influence the pharmacokinetics of artemisinins. Interactions with cytochrome P(450) inhibitors are known but these neither affect the efficacy nor the toxicity of the respective derivative. Artemisinins are generally regarded to be of low toxicity. Two major problems associated with them are neurotoxicity and reproductive toxicity. But the extent of this neurotoxicity is dependent on the nature of the compound, on the route of administration, and on the nature of the formulation. Moreover, it occurs in humans at very high doses. However, as a matter of precaution, the use of artemisinins in the first trimester of pregnancy has been contraindicated.
青蒿素在疟疾治疗中已被有效应用。随着抗疟药性的出现，该药物的最佳和合理使用变得尤为重要。药物代谢和毒理学可能会影响这种抗疟药物的治疗特性和临床应用。在这篇综述中，我们讨论了青蒿素的药代动力学和毒理学方面及其治疗意义。青蒿素具有多种给药途径，包括口服、肌肉内、静脉内和直肠内。重复给药后，青蒿素有自动诱导的倾向，导致重复给药时血浆水平下降。与其他抗疟药物联合使用在大多数情况下不会影响青蒿素的药代动力学。与细胞色素 P450 抑制剂的相互作用是已知的，但这些既不影响各自衍生物的疗效也不影响其毒性。青蒿素通常被认为毒性较低。与它们相关的两个主要问题是神经毒性和生殖毒性。但这种神经毒性的程度取决于化合物的性质、给药途径和制剂的性质。此外，它只在人类中出现于非常高的剂量下。然而，作为预防措施，青蒿素在妊娠早期的使用已被禁止。
