Mechanism for increased bioavailability of tacrine in fasted rats

Journal of Pharmacy and Pharmacology

Volumn 58, Issue 5, 2006, Pages 643-649

  Sung, Jong Hyuk ^a,b   Hong, Soon Sun ^a   Ahn, Sung Hoon ^a   Li, Hong ^a   Seo, Seung Yong ^a   Park, Chul Hong ^b   Park, Byung Soon ^b   Chung, Suk Jae ^a  

^a Seoul National University   (South Korea)

^b Taehwa Bldg   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

TACRINE; VELNACRINE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; DIET RESTRICTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG METABOLISM; DRUG PENETRATION; DRUG STRUCTURE; DRUG UPTAKE; FEEDING; FIRST PASS EFFECT; INTESTINE; MALE; NONHUMAN; RAT; SYSTEMIC CIRCULATION; URINARY EXCRETION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CHOLINESTERASE INHIBITORS; FASTING; INJECTIONS, INTRAVENOUS; INTESTINAL ABSORPTION; MALE; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY; TACRINE;

EID: 33646456460     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.58.5.0009     Document Type: Article

References (25)

1. Ahlin, A., Hassan, M., Junthe, T., Nyback, H. (1994) Tacrine in Alzheimer's disease: pharmacokinetic and clinical comparison of oral and rectal administration. Int. Clin. Psychopharmacol. 9: 263-270
2. Brown, B. L., Allis, J. W., Simmons, J. E., House, D. E. (1995) Fasting for less than 24 h induces cytochrome P450 2E1 and 2B1/2 activities in rats. Toxicol. Lett. 81: 39-44
3. Carey, H. V., Hayden, U. L. (2000) Neural control of intestinal ion transport and paracellular permeability is altered by nutritional status. Am. J. Physiol. Regul. Integr. Comp. Physiol. 278: R1589-R1594
4. Carey, H. V., Hayden, U. L., Tucker, K. E. (1994) Fasting alters basal and stimulated ion transport in piglet jejunum. Am. J. Physiol. 267: R156-R163
5. Crismon, M. L. (1994) Tacrine: first drug approved for Alzheimer's disease. Ann. Pharmacother. 28: 744-751
6. Gibaldi, M., Perrier, D. (1982) Pharmacokinetics. 2nd edn, Marcel Dekker Inc., New York
7. Gong, T., Huang, Y., Zhang, Z. R., Li, L. L. (2004) Synthesis and characterization of 9-[p-(N,N-dipropyl sulfamide)]benzoylamino-1,2,3,4,-4H- acridine - a potential prodrug for the CNS delivery of tacrine. J. Drug Target. 12: 177-182
8. Hartvig, P., Askmark, H., Aquilonius, S. M., Wiklund, L., Lindstrom, B. (1990) Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4- tetrahydroacridine, tacrine. Eur. J. Clin. Pharmacol. 38: 259-263
9. Jann, M. W., Shirley, K. L., Small, G. W. (2002) Clinical pharmacokinetics and pharmacodynamics of choline esterase inhibitors. Clin. Pharmacokinet. 41: 719-739
10. Kim, J., Cho, Y., Choi, H. (2000) Effect of vehicles and pressure sensitive adhesives on the permeation of tacrine across hairless mouse skin. Int. J. Pharm. 196: 105-113
11. Lee, H. T., Lee, Y. J., Chung, S. J., Shim, C. K. (2000) Effect of prokinetic agents, cisapride and metoclopramide, on the bioavailability in humans and intestinal permeability in rats of ranitidine, and intestinal charcoal transit in rats. Res. Commun. Mol. Pathol. Pharmacol. 108: 311-323
12. Lou, G., Montgomery, P. R., Sitar, D. S. (1996) Bioavailability and pharmacokinetic disposition of tacrine in elderly patients with Alzheimer's disease. J. Psychiatry Neurosci. 21: 334-339
13. Madden, S., Spaldin, V., Park, B. K. (1995a) Clinical pharmacokinetics of tacrine. Clin. Pharmacokinet. 28: 449-457
14. Madden, S., Spaldin, V., Hayes, R. N., Woolf, T. F., Pool, W. F., Park, B. K. (1995b) Species variation in the bioactivation of tacrine by hepatic microsomes. Xenobiotica 25: 103-116
15. McNally, W., Roth, M., Young, R., Bockbrader, H., Chang, T. (1989) Quantitative whole-body autoradiographic determination of tacrine tissue distribution in rats following intravenous or oral dose. Pharm. Res. 6: 924-930
16. Monteith, D. K., Emmerling, M. R., Garvin, J., Theiss, J. C. (1996) Cytotoxicity study of tacrine, structurally and pharmacologically related compounds using rat hepatocytes. Drug Chem. Toxicol. 19: 71-84
17. Ogura, H., Kosasa, T., Kuriya, Y., Yamanish, Y. (2000) Donepezil, a centrally acting acetylcholinesterase inhibitor, alleviates learning deficits in hypocholinergic model in rats. Methods Find. Exp. Clin. Pharmacol. 22: 89-95
18. Pool, W. F., Reily, M. D., Bjorge, S. M., Woolf, T. F. (1997) Metabolic disposition of the cognition activator tacrine in rats, dogs, and humans. Species comparisons. Drug Metab. Dispos. 25: 590-597
19. Puri, S. K., Hsu, R. S., Ho, I., Lassman, H. B. (1989a) Single dose safety, tolerance, and pharmacokinetics of HP 029 in healthy young men: a potential Alzheimer agent. J. Clin. Pharmacol. 29: 278-284
20. Puri, S. K., Hsu, R. S., Ho, I., Lassman, H. B. (1989b) The effect of food on the bioavailability of velnacrine (HP 029) in healthy elderly men: a potential Alzheimer agent. J. Clin. Pharmacol. 29: 956-960
21. Shutske, G. M., Pierrat, F. A., Kapples, K. J., Cornfeldt, M. L., Szewczak, M. R., Huger, F. P., Bores, G. M., Haroutunian, V., Davis, K. L. (1989) 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. J. Med. Chem. 32: 1805-1813
22. Siegfried, K. R. (1993) Pharmacodynamic and early clinical studies with velnacrine. Acta Neurol. Scand. Suppl. 149: 26-28
23. Sung, J. H., Yu, K. H., Park, J. S., Tsuruo, T., Kim, D. D., Shim, C. K., Chung, S. J. (2005) Saturable distribution of tacrine into the striatal extracellular fluid of the rat: evidence of involvement of multiple organic cation transporters in the transport. Drug Metab. Dispos. 33: 440-448
24. Truman, C. A., Ford, J. M., Roberts, C. J. (1991) Comparison of the chromatographic characteristics of metabolites of tacrine hydrochloride in human serum and urine with those of in vitro metabolic products from hepatic microsomes. Biochem. Pharmacol. 42: 956-959
25. Welty, D. F., Siedlik, P. H., Posvar, E. L., Selen, A., Sedman, A. J. (1994) The temporal effect of food on tacrine bioavailability. J. Clin. Pharmacol. 34: 985-988