Czarnik T R, Vernikos J
WSU Aerospace Medicine, Dayton, OH.
J Gravit Physiol. 1999 Jul;6(1):P161-4.
Despite nearly 40 years of spaceflight, the paucity of time spent in microgravity and somewhat scattered approach to the study to pharmacology in microgravity have resulted in little solid information. Moreover, they have generally only been studied in the first few days of spaceflight or its simulation by bedrest, when physiological changes are most dynamic. Nevertheless, early physiological responses to microgravity have been well documented and provide good support for the hypothesis that both pharmacokinetics and pharmacodynamics should be altered, with more significant changes occurring as stays in space increase in duration. Whether given orally, by intravenous (IV) or intramuscular (IM) injection, intranasally (IN) or rectally, a drug must distribute through the body, usually crossing certain membranes and becoming bound to other molecules, reach its receptor and bind to it in order to exert its action. This paper, then, will follow a drug's passage through the body in terms of pharmacokinetic parameters known to be affected by microgravity, and mention other factors.
尽管已有近40年的太空飞行历史,但由于在微重力环境下停留的时间有限,且对微重力药理学的研究方法较为分散,因此几乎没有可靠的信息。此外,这些研究通常仅在太空飞行的最初几天或通过卧床休息进行模拟时开展,而此时生理变化最为活跃。然而,对微重力的早期生理反应已有充分记录,并为药代动力学和药效学均应改变这一假说提供了有力支持,随着在太空停留时间的延长,变化会更加显著。无论药物是口服、静脉注射、肌肉注射、鼻内给药还是直肠给药,都必须在体内分布,通常要穿过某些膜并与其他分子结合,到达其受体并与之结合才能发挥作用。因此,本文将根据已知受微重力影响的药代动力学参数来跟踪药物在体内的传递过程,并提及其他因素。