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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Considerations on pharmacodynamics and pharmacokinetics: can everything be explained by the extent of drug binding to its receptor?
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Considerations on pharmacodynamics and pharmacokinetics: can everything be explained by the extent of drug binding to its receptor?

机译：关于药效学和药代动力学的考虑：能否通过药物与其受体结合的程度来解释一切？

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摘要

It is frequently assumed that pharmacological responses depend solely on the extent of drug binding to its receptor according to the occupational theory. It is therefore presumed that the intensity of the effect is determined by drug concentration at its receptor site, yielding a unique concentration-effect relationship. However, when dependence, abstinence, and tolerance phenomena occur, as well as for pharmacological responses in vivo that are modulated by homeostatic mechanisms, the rate of drug input shifts the concentration-effect relationship. Hence, such responses cannot be explained on the sole basis of the extent of drug binding to its receptor. Information on the cellular and molecular processes involved in the generation of abstinence, dependence, and tolerance will undoubtedly result in the development of pharmacodynamic models allowing a satisfactory explanation of drug effects modulated by these phenomena. Notwithstanding, integrative physiology concepts are required to develop pharmacokinetic-pharmacodynamic models allowing the description of drug effects in an intact organism. It is therefore important to emphasize that integrative physiology cannot be neglected in pharmacology teaching and research, but should be considered as an equally valuable tool as molecular biology and other biomedical disciplines for the understanding of pharmacological effects.
机译：通常根据职业理论，药理学反应仅取决于药物与其受体结合的程度。因此，推测作用的强度取决于其受体部位的药物浓度，从而产生独特的浓度-作用关系。但是，当出现依赖性，节制和耐受现象，以及体内受稳态机制调节的药理反应时，药物输入的速率会改变浓度-效应关系。因此，不能仅凭药物与其受体结合的程度来解释这种反应。禁欲，依赖性和耐受性产生所涉及的细胞和分子过程的信息无疑将导致药效学模型的发展，从而可以令人满意地解释由这些现象调节的药物作用。尽管如此，需要综合的生理学概念来发展药代动力学-药效学模型，以描述完整生物体中的药物作用。因此，重要的是要强调，综合生理学在药理学教学和研究中不可忽略，而应被视为与分子生物学和其他生物医学学科同等有价值的工具，以了解药理作用。

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