Oral bioavailability and intestinal secretion of amitriptyline: Role of P-glycoprotein?

International Journal of Pharmaceutics

Volumn 330, Issue 1-2, 2007, Pages 121-128

  Abaut, Anne Yvonne ^a   Chevanne, Francois ^a   Le Corre, Pascal ^a  

^a UNIVERSITÉ DE RENNES 1   (France)

Author keywords

Amitriptyline; Intestinal secretion; Oral bioavailability; P glycoprotein; Quinidine

Indexed keywords

AMITRIPTYLINE; GLYCOPROTEIN P; GLYCOPROTEIN P INHIBITOR; NORTRIPTYLINE; QUINIDINE; TRICYCLIC ANTIDEPRESSANT AGENT;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTINUOUS INFUSION; CONTROLLED STUDY; DIFFUSION CHAMBER; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG PENETRATION; DRUG UPTAKE; FEMALE; INTESTINE ABSORPTION; INTESTINE PERFUSION; INTESTINE SECRETION; JEJUNUM; NONHUMAN; PRIORITY JOURNAL; RABBIT;

ADMINISTRATION, ORAL; AMITRIPTYLINE; ANIMALS; ANTIDEPRESSIVE AGENTS, TRICYCLIC; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; ENZYME INHIBITORS; FEMALE; HALF-LIFE; INJECTIONS, INTRAVENOUS; INTESTINAL ABSORPTION; JEJUNUM; MALE; P-GLYCOPROTEIN; QUINIDINE; RABBITS; RATS; RATS, SPRAGUE-DAWLEY;

EID: 33846333128     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2006.09.026     Document Type: Article

References (27)

1. Arndt P., Volk C., Gorboulev V., Budiman T., Popp C., Ulzheimer-Teuber I., Akhoundova A., Koppatz S., Bamberg E., Nagel G., and Koepsell H. Interaction of cations, anions and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am. J. Physiol. Renal Physiol. 281 (2001) F454-F468
2. Barbui C., and Hotopf M. Amitriptyline vs. the rest: still the leading antidepressant after 40 years of randomized controlled trials. Br. J. Psychiatry 178 (2001) 129-144
3. Benet L.Z., Wu C.Y., Hebert M.F., and Wacher V.J. Intestinal drug metabolism and antitransport processes: a potential paradigm shift in oral drug delivery. J. Control. Release 39 (1996) 139-143
4. Benet L.Z., and Cummins C.L. The drug efflux-metabolism alliance: biochemical aspects. Adv. Drug Deliv. Rev. 50 (2001) S3-S11
5. Bryson H.M., and Wilde M.I. Amitriptyline: a review of its pharmacological properties and therapeutic use in chronic pain states. Drugs and aging 8 (1996) 459-476
6. Fardel O., Ratanasavanh D., Loyer P., Ketterer B., and Guillouzo A. Overexpression of the multidrug resistance gene product in adult rat hepatocytes during primary culture. Eur. J. Biochem. 205 (1992) 847-852
7. Ford J.M., and Hait W.N. Pharmacology of drugs that alter multidrug resistance in cancer. Pharmacol. Rev. 42 (1990) 155-199
8. Gottesman M.M., Hrycyna C.A., Schoenlein P.V., Germann U.A., and Pastan I. Genetic analysis of the multidrug transporter. Annu. Rev. Genet. 29 (1995) 607-649
9. Grauer T.M., and Uhr M. P-glycoprotein reduces the ability of amitriptyline metabolites to cross the blood-brain barrier in mice after a 10-day administration of amitriptyline. J. Psychopharmacol. 18 (2004) 66-74
10. Harris A.L., and Hochhauser D. Mechanisms of multidrug resistance in cancer treatment. Acta Oncol. 31 (1992) 205-213
11. Kharasch E.D., Hoffer C., Altuntas T.G., and Whittington D. Quinidine as a probe for the role of P-glycoprotein in the intestinal absorption and clinical effects of fentantyl. J. Clin. Pharmacol. 44 (2004) 224-233
12. Kiuchi Y., Suzuki H., Hirohashi T., Tyson C.A., and Sugiyama Y. cDNA cloning and inducible expression of human multidrug resistance associated protein 3 (MRP3). FEBS Lett. 433 (1998) 149-152
13. Marzolini C., Paus E., Buclin T., and Kim R.B. Polymorphisms in human MDR1 P-glycoprotein: recent advances and clinical relevance. Clin. Pharmacol. Ther. 75 (2004) 13-33
14. Peng K.C., Cluzeaud F., Bens M., Duong Van Huyen J.P., Wioland M.A., Lacave R., and Vandewalle A. Tissue and cell distribution of the multidrug resistance-associated protein (MRP) in mouse intestine and kidney. J. Histochem. Cytochem. 47 (1999) 757-768
15. Sadeque A.J.M., Wandel C., He H., Shah S., and Wood A.J.J. Increased drug delivery to the brain by P-glycoprotein inhibition. Clin. Pharmacol. Ther. 68 (2000) 231-237
16. Schultz P., Dick P., Blaschkle T.F., and Hollister L. Discrepancies between pharmacokinetic studies of amitriptyline. Clin. Pharmacokinet. 10 (1985) 257-268
17. Su S.F., and Huang J.D. Inhibition of the intestinal digoxin absorption and exsorption by quinidine. Drug Metabol. Dispos. 24 (1995) 142-147
18. Thiebaut F., Tsuruo T., Hamada H., Gottesman M.M., Pastan I., and Willingham M.C. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc. Natl. Acad. Sci. USA 84 (1987) 7735-7738
19. Uhr M., Steckler T., Yassouridis A., and Holsboer F. Penetration of amitriptyline, but not fluoxetine into brain is enhanced in mice with blood-brain barrier deficiency due to mdr1a P-glycoprotein gene disruption. Neuropsychopharmacology 22 (2000) 380-387
20. Uhr M., Grauer M.T., Yassouridis A., and Ebinger M. Blood-brain barrier penetration and pharmacokinetics of amitriptyline and its metabolites in P-glycoprotein (abcb 1 ab) knock-out mice and controls. J. Psychiatr. Res. (2005) 29
21. Van Montfoort J.E., Muller M., Groothuis G.M.M., Meijer D.K.F., Koepsell H., and Meier P.J. Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J. Pharmacol. Exp. Ther. 298 (2001) 110-115
22. Varga A., Nugel H., Baerh R., Marx U., Hever A., Nasca J., Ocsovsky I., and Molnar J. Reversal of multidrug resistance by amitriptyline in vitro. Anticancer res. 16 (1996) 209-211
23. Venkatakrishnan K., Greenblatt D.J., Von Molkte L.L., Schmider J., Harmatz J.S., and Shader R.I. Five distinct human cytochromes mediate amitriptyline N-demethylation in vitro: dominance of CYP2C19 and 3A4. J. Clin. Pharmacol. 38 (1998) 112-121
24. Venkatakrishnan K., Schmider J., Harmatz J.S., Ehrenberg B.L., Von Molkte L.L., Graf J.A., Mertazis P., Corbett K.E., Rodriguez M.C., Shader R.I., and Greenblatt D.J. Relative contribution of CYP3A to amitriptyline clearance in humans: in vitro and in vivo studies. J. Clin. Pharmacol. 41 (2001) 1043-1054
25. Wacher J.V., Salphati L., and Benet L.Z. Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv. Drug Deliv. Rev. 46 (2001) 89-102
26. Wu X., George R.L., Huang W., Wang H., Conway S.J., Leibach F.H., and Ganpathy V. Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim. Biophys. Acta 1466 (2000) 315-327
27. Wu C.Y., and Benet L.Z. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm. Res. 22 (2005) 11-23