药代动力学

维基百科,自由的百科全书
跳转至: 导航搜索

药代动力学英语Pharmacokinetics;又称药物代谢动力学药动学)是研究药物在动物体内的含量随时间变化规律的科学,是药理学的一种。主要研究机体对药物的处置的动态变化,包括药物在机体内的吸收、分布、代谢及排泄的过程。

药物动力学应用在药物治疗、临床药理、分子药理、生物化、生物药剂、分析化学、药剂、药理毒理等多种科学领域中。药物动力学渗透到药物开发的各个领域:如药物评价、设计、剂型改进和临床指导合理用药,以及优化给药方案等具有重大的实用价值。药物动力学对指导新药设计,优化给药方案,改进剂型,提供高效、速效(或缓释)、低毒(或低副作用)的药物制剂,已经发挥了重大作用。

基本概念:

  1. 隔室模型:单隔室模型、二隔室模型、多隔室模型。
  2. 消除速度常数:K = Kb + Ke + Kbi + Klu + ...
  3. 生物半衰期:即体内药量或血药浓度下降一半所需要的时间。
  4. 清除率:Cl = (-dX-dt)/C = KV 。

參考文獻[编辑]

  1. Alberts et al., Introducción a la Biología Celular, pág. 375-376, 2ª edición, Ed. Médica Panamericana
  2. Alberts et al., Biología Molecular de la célula, pág. 595, 4ª edición, Ed. Omega
  3. Armijo JA. 2003. Farmacocinética: Absorción, Distribución y Eliminación de los Fármacos. En: Flórez J, Armijo JA, Mediavilla A, Farmacología Humana, 4ta edición. Masson. Barcelona. pp: 51-79.
  4. Balani SK, Miwa GT, Gan LS, Wu JT, Lee FW., Strategy of utilizing in vitro and in vivo ADME tools for lead optimization and drug candidate selection, Curr Top Med Chem. 2005;5(11):1033-8.
  5. Beal, S.; Sheiner L.B. "The NONMEM System". The American Statistician 34: 118–9. (1980). doi:10.2307/2684123.
  6. Cooper, La célula, pág 470-471, 2ª edición, Ed. Marbán
  7. Covey TR, Lee ED, Henion JD "High-speed liquid chromatography/tandem mass spectrometry for the determination of drugs in biological samples". Anal. Chem. 58: 2453–60. (October 1986). doi:10.1021/ac00125a022. PMID 3789400.
  8. Covey TR, JB Crowther, EA Dewey, JD Henion "Thermospray liquid chromatography/mass spectrometry determination of drugs and their metabolites in biological fluids". Anal. Chem. 57 (2): 474–81. (February 1985). doi:10.1021/ac50001a036. PMID 3977076.
  9. Danielson P (2002). "The cytochrome P450 superfamily: biochemistry, evolution and drug metabolism in humans". Curr Drug Metab 3 (6): 561-97. PMID 12369887.
  10. Davies K (1995). "Oxidative stress: the paradox of aerobic life". Biochem Soc Symp 61: 1-31. PMID 8660387.
  11. Devlin, T. M. 2004. Bioquímica, 4ª edición. Reverté, Barcelona. ISBN 84-291-7208-4
  12. Galvão T, Mohn W, de Lorenzo V (2005). "Exploring the microbial biodegradation and biotransformation gene pool". Trends Biotechnol 23 (10): 497-506. PMID 16125262.
  13. Hsieh Y, Korfmacher WA "Increasing speed and throughput when using HPLC-MS/MS systems for drug metabolism and pharmacokinetic screening". Current Drug Metabolism 7 (5): 479–89.(June 2006). PMID 16787157. Disponible en [1]
  14. Janssen D, Dinkla I, Poelarends G, Terpstra P (2005). "Bacterial degradation of xenobiotic compounds: evolution and distribution of novel enzyme activities". Environ Microbiol 7 (12): 1868-82. PMID 16309386.
  15. Kathleen Knights; Bronwen Bryant (2002). Pharmacology for Health Professionals. Amsterdam: Elsevier. ISBN 0-7295-3664-5.
  16. King C, Rios G, Green M, Tephly T (2000). "UDP-glucuronosyltransferases". Curr Drug Metab 1 (2): 143-61. PMID 11465080.
  17. Malcolm Rowland, Thomas N. Tozer. "Farmacocinética clínica: Conceptos y Aplicaciones"
  18. Pharmacokinetics. (2006). En Mosby's Dictionary of Medicine, Nursing, & Health Professions. Philadelphia, PA: Elsevier Health Sciences. Disponible en [2] Última visita 11, diciembre de 2008,
  19. Sheehan D, Meade G, Foley V, Dowd C (2001). "Structure, function and evolution of glutathione transferases: implications for classification of non-mammalian members of an ancient enzyme superfamily". Biochem J 360 (Pt 1): 1-16. PMID 11695986.
  20. Sheiner, L.B.; Beal, S.L., Rosenberg, B. Marathe, V.V. "Forecasting Individual Pharmacokinetics". Clin. Pharmacol. Ther. 26: 294–305. (1979). PMID 466923.
  21. Sheiner, L.B.; Rosenberg, B., Marathe, V.V. "Estimation of Population Characteristics of Pharmacokinetic Parameters from Routine Clinical Data". J. Pharmacokin. Biopharm. 5: 445–79. 1.997 doi:10.1007/BF01061728.
  22. Sies H (1997). "Oxidative stress: oxidants and antioxidants". Exp Physiol 82 (2): 291-5. PMID 9129943.
  23. Singh SS., Preclinical pharmacokinetics: an approach towards safer and efficacious drugs, Curr Drug Metab. 2006 Feb;7(2):165-82.
  24. Testa B, Krämer S (2006). "The biochemistry of drug metabolism--an introduction: part 1. Principles and overview". Chem Biodivers 3 (10): 1053-101. PMID 17193224.
  25. Tetko IV, Bruneau P, Mewes HW, Rohrer DC, Poda GI., Can we estimate the accuracy of ADME-Tox predictions?, Drug Discov Today. 2006 Aug;11(15-16):700-7, pre-print.
  26. Tu B, Weissman J (2004). "Oxidative protein folding in eukaryotes: mechanisms and consequences". J Cell Biol 164 (3): 341-6. PMID 14757749.
  27. Vertuani S, Angusti A, Manfredini S (2004). "The antioxidants and pro-antioxidants network: an overview". Curr Pharm Des 10 (14): 1677-94. PMID 15134565.

外部鏈接[编辑]