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Biliary Drug Excretion

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The ADME Encyclopedia

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Synonyms

Biliary drug elimination; Biliary excretion

Definition

Biliary excretion refers to the elimination of endogenous and exogenous compounds (and their metabolites) predominantly by secretion through the canalicular membrane into the canaliculus, a space formed between the apical membranes of neighboring hepatocytes. The excretion process is completed when the bile transports its contents to the gut and they are ultimately eliminated in feces (some compounds secreted into the bile, however, may be subject to reabsorption from the intestine, entering into enterohepatic cycling).

Bile Formation

Bile is a complex greenish yellow fluid containing water, electrolytes, heavy metals, and several organic molecules including bile acids, cholesterol, bilirubin, and phospholipids. It is produced in the liver and then passed to the gallbladder for concentration and storage until it is secreted into the small intestine via the sphincter of Oddi. Due to its tensioactive properties, bile is...

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References

  1. Roberts MS, Magnusson BM, Burczynski FJ, Weiss M. Enterohepatic circulation: physiological, pharmacokinetic and clinical implications. Clin Pharmacokinet. 2002;41:751–90.

    Article  CAS  PubMed  Google Scholar 

  2. Klaassen CD, Watkins JB 3rd. Mechanisms of bile formation, hepatic uptake, and biliary excretion. Pharmacol Rev. 1984;36:1–67.

    CAS  PubMed  Google Scholar 

  3. Boyer JL. Bile formation and secretion. Compr Physiol. 2013;3:1035–78.

    Article  PubMed  PubMed Central  Google Scholar 

  4. Hundt M, Basit H, John S. Physiology, bile secretion. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2020. Available from. https://www.ncbi.nlm.nih.gov/books/NBK470209/

  5. Wang L, Boyer JL. The maintenance and generation of membrane polarity in hepatocytes. Hepatology. 2004;39:892–9.

    Article  PubMed  Google Scholar 

  6. Eipel C, Abshagen K, Vollmar B. Regulation of hepatic blood flow: the hepatic arterial buffer response revisited. World J Gastroenterol. 2010;16:6046–57.

    Article  PubMed  PubMed Central  Google Scholar 

  7. Lautt WW. Chapter 2, Overview. In: Hepatic circulation: physiology and pathophysiology. San Rafael: Morgan & Claypool Life Sciences; 2009. https://www.ncbi.nlm.nih.gov/books/NBK53069/

  8. Yáñez JA, Wang SW, Knemeyer IW, Wirth MA, Alton KB. Intestinal lymphatic transport for drug delivery. Adv Drug Deliv Rev. 2011;63:923–42.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  9. Roberts MS, Anissimov YG, Weiss M. Commentary: using the convection-dispersion model and transit time density functions in the analysis of organ distribution kinetics. J Pharm Sci. 2000;89:1579–86.

    Article  CAS  PubMed  Google Scholar 

  10. Mao Q, Unadkat JD. Role of the breast cancer resistance protein (BCRP/ABCG2) in drug transport--an update. AAPS J. 2015;17:65–82.

    Article  CAS  PubMed  Google Scholar 

  11. Nies AT, Keppler D. The apical conjugate efflux pump ABCC2 (MRP2). Pflugers Arch Eur J Physiol. 2007;453:643–59.

    Article  CAS  Google Scholar 

  12. Crawford JM. Role of vesicle-mediated transport pathways in hepatocellular bile secretion. Semin Liver Dis. 1996;16:169–89.

    Article  CAS  PubMed  Google Scholar 

  13. Zucker SD, Goessling W, Gollan JL. Intracellular transport of small hydrophobic compounds by the hepatocyte. Semin Liver Dis. 1996;16:159–67.

    Article  CAS  PubMed  Google Scholar 

  14. Döring B, Petzinger E. Phase 0 and phase III transport in various organs: combined concept of phases in xenobiotic transport and metabolism. Drug Metab Rev. 2014;46:261–82.

    Article  PubMed  Google Scholar 

  15. Boyer JL. Nuclear receptor ligands: rational and effective therapy for chronic cholestatic liver disease? Gastroenterology. 2005;129:735–40.

    Article  PubMed  Google Scholar 

  16. Sztul ES, Biemesderfer D, Caplan MJ, Kashgarian M, Boyer JL. Localization of Na+,K+-ATPase alpha-subunit to the sinusoidal and lateral but not canalicular membranes of rat hepatocytes. J Cell Biol. 1987;104:1239–48.

    Article  CAS  PubMed  Google Scholar 

  17. Shitara Y, Sato H, Sugiyama Y. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol. 2005;45:689–723.

    Article  CAS  PubMed  Google Scholar 

  18. Malik MY, Jaiswal S, Sharma A, Shukla M, Lal J. Role of enterohepatic recirculation in drug disposition: cooperation and complications. Drug Metab Rev. 2016;48:281–327.

    Article  CAS  PubMed  Google Scholar 

  19. Samodelov SL, Kullak-Ublick GA, Gai Z, Visentin M. Organic cation transporters in human physiology, pharmacology, and toxicology. Int J Mol Sci. 2020;21:7890.

    Article  CAS  PubMed Central  Google Scholar 

  20. Shen H, Lai Y, Rodrigues AD. Organic anion transporter 2: an enigmatic human solute carrier. Drug Metab Dispos. 2017;45:228–36.

    Article  CAS  PubMed  Google Scholar 

  21. Nicolaou M, Andress EJ, Zolnerciks JK, Dixon PH, Williamson C, Linton KJ. Canalicular ABC transporters and liver disease. J Pathol. 2012;226:300–15.

    Article  CAS  PubMed  Google Scholar 

  22. Patrick JE, Kosoglou T, Stauber KL, Alton KB, Maxwell SE, Zhu Y, et al. Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects. Drug Metab Dispos. 2002;30:430–7.

    Article  CAS  PubMed  Google Scholar 

  23. Shin SJ, Noh CK, Lim SG, Lee KM, Lee KJ. Non-steroidal anti-inflammatory drug-induced enteropathy. Intest Res. 2017;15:446–55.

    Article  PubMed  PubMed Central  Google Scholar 

  24. Zhong ZY, Sun BB, Shu N, Xie QS, Tang XG, Ling ZL, et al. Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity. Acta Pharmacol Sin. 2016;37:1002–12.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  25. Sharifi M, Ghafourian T. Estimation of biliary excretion of foreign compounds using properties of molecular structure. AAPS J. 2014;16:65–7.

    Article  CAS  PubMed  Google Scholar 

  26. Yang X, Gandhi YA, Duignan DB, Morris ME. Prediction of biliary excretion in rats and humans using molecular weight and quantitative structure–pharmacokinetic relationships. AAPS. 2009;11:511–25.

    Article  CAS  Google Scholar 

  27. Varma MV, Chang G, Lai Y, Feng B, El-Kattan AF, Litchfield J, et al. Physicochemical property space of hepatobiliary transport and computational models for predicting rat biliary excretion. Drug Metab Dispos. 2012;40:1527–37.

    Article  CAS  PubMed  Google Scholar 

  28. Hosey CM, Broccatelli F, Benet LZ. Predicting when biliary excretion of parent drug is a major route of elimination in humans. AAPS J. 2014;16:1085–96.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

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Authors and Affiliations

  1. Laboratory of Bioactive Research and Development (LIDeB), Department of Biological Sciences, University of La Plata (UNLP), La Plata, Buenos Aires, Argentina

    Alan Talevi & Carolina L. Bellera

  2. Argentinean National Council of Scientific and Technical Research (CONICET) – CCT, La Plata, Buenos Aires, Argentina

    Alan Talevi

  3. Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), La Plata, Buenos Aires, Argentina

    Carolina L. Bellera

Authors
  1. Alan Talevi
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  2. Carolina L. Bellera
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Corresponding author

Correspondence to Alan Talevi .

Editor information

Editors and Affiliations

  1. University of La Plata (UNLP), Argentinian National Council of Scientific and Technical Research (CONICET), La Plata, Argentina

    Alan Talevi

Section Editor information

  1. Medicinal Chemistry, Department of Biological Sciences, Faculty of Exact Sciences, National University of la Plata (UNLP) - Argentinean National Council of Scientific and Technical Research (CONICET), La Plata, Buenos Aires, Argentina

    Alan Talevi

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Talevi, A., Bellera, C.L. (2022). Biliary Drug Excretion. In: Talevi, A. (eds) The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-84860-6_71

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