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Research Article

Pharmacokinetics and Toxicity Testing

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Pages 343-385 | Published online: 26 Sep 2008

References

  • Zbinden G. Comparative and pharmacokinetic toxicity. Progress in Toxicology, Special Topics. Springer-Verlag, Berlin 1976; Vol. 2: 44
  • Zbinden G. Application of basic concepts to research in toxicology. Pharmacol. Rev. 1979; 30: 605
  • Zbinden G., Flury-Roversi M. Significance of the LD50test for the toxicological evaluation of chemical substances. Arch. Toxicol. 1981; 47: 77
  • Malmfors T. Toxicology as science. Trends Pharmacol. Sci. 1981; 2(1)I
  • Dayan A. D. The troubled toxicologist. Trends Pharmacol. Sci. 1981; 2(11)I
  • Aldridge W. N. Mechanisms of toxicity; new concepts are required in toxicology. Trends Pharmacol. Sci. 1981; 2(9)228
  • Graham-Smith D. Reported in Scrip May 13, 1981, No. 590: 4
  • Graham-Smith D. Problems facing a regulatory authority. Risk-Benefit Analysis in Drug Research, J. F. Cavalla. MTP Press, LancasterU.K. 1981; 51
  • Brimblecombe R. W. The impact of regulation on the discovery of new medicines. Trends Pharmacol. Sci. 1981; 2(2)I
  • Dayan A. D. The relative worth of animal testing. Risk-Benefit Analysis in Drug Research, J. F. Cavalla. MTP Press, LancasterU.K. 1981; 97
  • O'Reilly W. J. Pharmacokinetics in drug metabolism and toxicology. Can. J. Pharm. Sci. 1972; 7: 66
  • Withey J. R. Pharmacokinetic principles. Proc. Ist Int. Congr. Toxicology, G. L. Plaa, W. A. M. Duncan. Academic Press, New York 1978; 97
  • Garrett E. R. The pharmacokinetic bases of biological response quantification in toxicology, pharmacology and pharmacodynamics. Prog. Drug Res. 1977; 21: 105
  • Andersen M. E. Saturable metabolism and its relationship to toxicity. Crit. Rev. Toxicol. 1981; 9: 105
  • Hayes W. J., Jr. Tests for detecting and measuring long-term toxicity. Essays in Toxicology. Academic Press, New York 1972; Vol. 3: 65
  • Smith C. G., Poutsiaka J. W., Schreiber E. C. Problems in predicting drug effects across species lines. J. Int. Med. Res. 1973; 1: 489
  • Albert A. Selective Toxicity, 2nd ed. John Wiley & Sons, New York 1960, chap. 1
  • Mellett L. B. Comparative drug metabolism. Prog. Drug. Res. 1969; 13: 136
  • Dedrick R. L. Animal scale up. J. Pharmacokinet. Biopharm. 1973; 1: 435
  • Dedrick R. L., Bischoff K. B. Species similarities in pharmacokinetics. Fed. Proc. 1980; 39: 54
  • Rentsch G. Pharmacokinetic systems for interpreting long-term experiments. Proc. Eur. Soc. Toxicol. 1974; 15: 323
  • Cohen Y. Radionuclide-labelled compounds in the approach of pharmacokinetics. Proc. Eur. Soc. Toxicol. 1973; 14: 20
  • Hottendorf G. H., Van Harken D. R., Madissoo H., Cabana B. E. Pharmacokinetic considerations in toxicology. Proc. Eur. Soc. Toxicol. 1976; 17: 255
  • Monro A. M. Pharmacokinetics. Symp. Proc. Ser. No. 7. Institute of Mathematics and its Applications, London 1975; 46
  • Smyth R. D., Hottendorf G. H. Applications of pharmacokinetics and biopharmaceutics in the design of toxicological studies. Toxicol. Appl. Pharmacol. 1980; 53: 179
  • Gehring P. J., Watanabe P. G., Blau G. E. Pharmacokinetic studies in evaluation of the toxicological and environmental hazard of chemicals. Advances in Modern Toxicology, M. A. Mehlman, R. E. Shapiro, H. Blumenthal. John Wiley & Sons, New York 1976; Vol. 1: 195, (Part 1)
  • Tuey D. B. Toxicokinetics. Introduction to Biochemical Toxicology, E. Hodgson, F. E. Guthrie. Blackwell Scientific, Oxford 1980; 40
  • Karlog O., Neilsen P., Rasmussen F. Toxicokinetics. Arch. Toxicol. 1978; 55, Suppl. 1
  • Health and Safety Commission, Consultative document. Notification of New Substances, Draft Regulations and Approved Codes of Practice. Her Majesty's Stationery Office, London 1981
  • Jusko W. J. Pharmacokinetic principles in chemical teratology. Proc. Eur. Soc. Toxicol. 1973; 14: 9
  • Gillette J. R. A perspective on the role of chemically reactive metabolites of foreign compounds in toxicity. I. Biochem. Pharmacol. 1974; 23: 2785
  • Gillette J. R. A perspective on the role of chemically reactive metabolites of foreign compounds in toxicity. II. Biochem. Pharmacol. 1974; 23: 2927
  • Von Hammer R., Jauch R., Koss F. W. Pharmacokinetische untersuchungen als hilfsmittel zur interpretation des verlaufs von toxizitatsprufungen. Arzneim-Forsch./Drug Res. 1981; 28: 1978
  • Filser J. G., Bolt H. M. Inhalation pharmacokinetics based on gas uptake studies. Arch. Toxicol. 1981; 47: 279
  • Goldenthal E. I. (1968) FDA Papers. May 3, 1968. U.S. Food and Drug Administration, Washington, D.C.
  • EEC Commission. Proposal for a Council Recommendation Concerning Tests Relating to the Placing on the Market of Proprietary Medicinal Products. Off. J. Eur. Communities December, 1980, No. C 355/6–29
  • Wallach D. P., Thomas R. C. Psicofuramine. VIII. Some pharmacological observations. Antibiot. Chemother. 1959; 9: 722
  • Handschumacher R. E., Creasey W. A., Fink M. E., Calabresi P., Welch A. D. Pharmacological and clinical studies with triacetyl-6-azauridine. Cancer Chemother. Rep. 1962; 16: 267
  • Dreyfuss J., Shaw J. M., Ross J. J. Absorption of Nadolol by mice, rats, hamsters, rabbits, dogs, monkeys and man. Xenobiotica 1978; 8: 503
  • Reeves P. R., Barnfield D. J., Longshaw S., McIntosh D. A. D., Winrow M. J. Disposition and metabolism of atenolol in animals. Xenobiotica 1978; 8: 305
  • Steiner K., Garbe A., Diekmann H. W., Nowak H. The fate of praziquantel in the organism. Eur. J. Drug Metab. Pharmacokinet. 1976; 1: 85
  • Hawkins D. R., Weston K. T., Chasseaud L. F., Darragh A., O'Kelly A. The absorption and excretion of14C-mecinarone in rat, dog and man. Eur. J. Drug Metab. Pharmacokinet. 1980; 5: 135
  • Chausseaud L. F., Hawkins D. R., Fry B. J., Lewis J. D., Saggers V. H., Sword I. P. Metabolism of a cinnamoylpiperazine. Xenobiotica 1974; 4: 393
  • Lesser J. M., Israili Z. H., Davis D. C., Dayton P. G. Hydrazaline-14C metabolism and disposition. Drug Metab. Disp. 1974; 2: 351
  • Cameron B. D., Chasseaud L. F., Hawkins D. R., Taylor T. Metabolism of a cinnamoylpiperazine. Xenobiotica 1976; 6: 441
  • Tocco D. J., Duncan A. E. W., Deluna F. A., Hucker H. B., Gruber V. F., Vandenheuvel W. J. A. Metabolism of timolol. Drug Metab. Disp. 1975; 3: 361
  • Wood B. A., Stopher D. A., Monro A. M. Metabolism of tolamolol in the mouse, rat, guinea pig, rabbit and dog. Xenobiotica 1975; 5: 183
  • Tocco D. J., Breault G. O., Zacchei A. G., Steelman S. L., Perrier C. V. Metabolism of MK-647. Drug Metab. Disp. 1975; 3: 453
  • Grindel J. M., O'Neill P. J., Yorgey K. A., Schwartz M. H., McKown L. A., Migdalof B. H., Wu W. Disposition and pharmacokinetics of zomepirac. Drug Metab. Disp. 1980; 8: 343
  • Warrander A., Metcalf R., Fromson J. M. Metabolism of fendosal. Drug Metab. Disp. 1981; 9: 161
  • Zacchei A. G., Weidner L. L., Besselaar G. H., Raftery E. B. Physiological disposition and metabolic fate of a new antiarrythmic agent a,a-dimethyl-4(a,a,β,β-tetrafluorophenetyl) benzylamine in the rat, dog, monkey, baboon and man. Drug Metab. Disp. 1976; 4: 387
  • Benziger D. P., Balfour K., Clemans S., Edelson J. Metabolism of cyclindole. Drug Metab. Disp. 1977; 5: 239
  • Case D. E., Illston H., Reeves P. R., Shuker B., Simons P. Metabolism of viloxazine in animals. Xenobiotica 1975; 5: 83
  • Forshell G. P. Lofepramine kinetics in rat, dog and man. Xenobiotica 1977; 7: 153
  • Sisenwine S. F., Tio C. O., Ruelius H. W. Iprindole disposition in several species. Xenobiotica 1979; 9: 237
  • Mayo B. C., Hawkins D. R., Humpel M., Chasseaud L. F., Girkin R. Lormetazepan biotransformation in animals. Xenobiotica 1980; 10: 413
  • Delong A. F., Smyth R. D., Polk A., Nayak R. K., Martin G., Douglas G. H., Cantwell N. H. R. Comparative metabolism of fenclorac. Drug Metab. Disp. 1977; 5: 122
  • Illing H. P. A., Fromson J. M. Isoxepac disposition and metabolism. Drug Metab. Disp. 1978; 6: 510
  • Janssen F. W., Kirkman S. K., Knowles J. A., Ruelius H. W. Disposition of oxaprozin. Drug Metab. Disp. 1978; 6: 465
  • Mroszczak E. J., Lee F. W. Tiopinac disposition. Drug Metab. Disp. 1980; 8: 415
  • Risdall P. C., Adams S. S., Crampton E. L., Marchant B. Metabolism of flurbiprofen. Xenobiotica 1978; 8: 691
  • Taylor J. A., Jr. Benzylthio-5-trifluoromethyl benzoic acid. Xenobiotica 1973; 3: 151
  • Hucker H. B., Stauffer S. C., Balletto A. J., White S. D., Zacchei A. G., Arison B. H. Disposition and metabolism of cyclobenzaprine. Drug Metab. Disp. 1978; 6: 659
  • Turnbull L. B., Teng L., Newman J., Bruce R. B., Maynard W. R. Disposition and metabolism of 3-(3-chlorophenoxy)-N-methyl pyrrolidine [14C]-carboxamide in the rat, dog and man. Drug Metab. Disp. 1976; 4: 379
  • Greenslade D., Havler M. E., Humphrey M. J., Jordan B. J., Lewis C. J., Rance M. J. Metabolism of tolmesoxide. Xenobiotica 1981; 11: 89
  • Taylor D. C., Cresswell P. R., Bartlett D. C. Cimetidine metabolism. Drug Metab. Disp. 1978; 6: 21
  • Taylor D. C., Cresswell P. R., Pepper E. S. Metiamide metabolism. Drug Metab. Disp. 1979; 7: 393
  • Tocco D. J., DeLuna F. A., Duncan A. E. W., Walker R. W., Arison B. H., Vandenheuval W. J. A. Physiological disposition and metabolism of 2-aminomethyl-4-(1,1 -dimethyl ethyl)-6-iodophenol hydrochloride. Drug Metab. Disp. 1979; 7: 330
  • Chu N. I., Amos B. A., Tokes L., Maddox M. L., Matin S. B., Hama K. M., Patterson J. W., Wagner P. J., Bell J. P., Chaplin M. D. Disposition of flunisolide. Drug Metab. Disp. 1979; 7: 81
  • Fromson J. M., Pearson S., Bramah S. Metabolism of tamoxifen by animals. Xenobiotica 1973; 3: 693
  • Daniel J. W., James G. W. L., Rowlands D. A., Taylor J. B. Comparative metabolism of azipranone. Xenobiotica 1978; 8: 321
  • Jeffery D. J., Jones K. H., Langley P. F. The metabolism of talampicillin in rat, dog and man. Xenobiotica 1978; 8: 419
  • Smith D. A., Neale M. G. Suitability of species selected for the chronic toxicity testing of proxicromil. Toxicol. Lett. 1980; 47, Spec. 1
  • Schwartz D. E., Jordan J. C., Vetter W., Oesterhelt G. Metabolism of ornidazole in animals and man. Xenobiotica 1979; 9: 571
  • Zacchei A. G., Wishousky T. I., Watson L. S. The physiological disposition of (2-cyclopentyl-6,7-dichloro-2-methyl-1 oxo-5-indananyloxy) acitic acid in the rat, dog, rhesus monkey and baboon. Drug Metab. Disp. 1978; 6: 313
  • Houston J. B., Wood S. G. Gastrointestinal absorption of drugs and other xenobiotics. Progress in Drug Metabolism, J. W. Bridges, L. F. Chasseaud. John Wiley & Sons, New York 1980; 57
  • Barry R. E. Length and absorptive surface area apportionment of segments of the hind gut for eight species of small mammals. J. Mammol. 1977; 58: 419
  • Orwig B. A., Dugger H. A., Bhuta S. I., Talbot K. C., Schwarz H. J. Biotransformation of fluproquazone in man and several animal species. Arzneim-Forsch./Drug Res. 1981; 31: 904
  • Watanabe J., Okabe H., Ichihashi T., Mizojiri K., Yamada H., Yamamoto R. Gastric emptying rate constants after oral administration of drug solution to mice, rats and rabbits. Chem. Pharm. Bull. 1977; 25: 2147
  • Theodorakis M. C. External scintigraphy for gastric emptying in Beagles. Am. J. Physiol. 1980; 239: G39
  • Chiou W. L., Riegelman S., Amberg J. R. Complications in using rabbits for the study of oral absorption. Chem. Pharm. Bull. 1969; 17: 2170
  • Yamato C., Takahashi T., Fujita T. Intestinal absorption of trazodone. Xenobiotica 1976; 6: 521
  • Bungay P. M., Dedrick R. L., Matthews H. B. Enteric transport of chlordecone in the rat. J. Pharmacokinet. Biopharm. 1981; 9: 309
  • Bridges J. W., Dent J. G., Johnson P. Drug effects on rat gastric emptying. Life Sci. 1976; 18: 97
  • Melamed S., Carlson G. R., Moss J. N., Belair E. J., Tansy M. F. GI pharmacology of polyethyleneimine 1: effect on gastric emptying in rats. J. Pharm. Sci. 1977; 66: 899
  • Yanai Y., Nakai Y., Nakajima N., Tanayama S. Metabolism of ethyltetrazolylchromone. Xenobiotica 1979; 9: 33
  • Tattersall M. L. Personal communication 1981
  • Franklin R. A. Gastric emptying and plasma meptazinol. Br. J. Pharmacol. 1977; 59: 565
  • Levy G., Gibaldi M., Procknal J. A. Effect of an anticholinergic agent on riboflavin absorption in man. J. Pharm. Sci. 1972; 61: 798
  • Harris P. A., Riegelman S. Influence of the route of administration on the area under the plasma concentration time curve. J. Pharm. Sci. 1969; 58: 71
  • Routledge P. A., Shand D. G. Presystemic drug elimination. Ann. Rev. Pharmacol. Toxicol. 1979; 19: 447
  • Higuchi S., Shiobara Y. Pharmacokinetics of nicardipine. Xenobiotica 1980; 10: 447
  • Boyd E. M. Route of drug administration. Predictive Toxicometrics. Bristol Scientechnica, BristolU.K. 1972; 137
  • Worden A. N., Harper K. H. Oral toxicity as influenced by method of administration. Proc. Eur. Soc. Toxicol. 1964; 4: 107
  • Mead B., Patterson L. H., Smith D. A. The disposition of FPL 55712 acid in rat and dog. J. Pharm. Pharmacol. 1981; 33: 682
  • Tam Y. K., Axelson J. E., McErlane B., Ongley R., Price J. D. E. Non-linear metoclopramide kinetics. J. Pharm. Exp. Ther. 1981; 217: 764
  • Nies A. S., Evans G. H., Shand D. G. Regional hemodynamic effects of propranolol in the unanaesthetised primate. Am. Heart J. 1973; 85: 97
  • Colombo T., Broggini M., Garattini S., Donelli M. G. Differential adriamycin distribution to blood components. Eur. J. Drug. Metab. Pharmacokinet. 1981; 6: 115
  • Fremstad D., Jacobsen S., Lunde K. M. Influence of serum protein binding on the pharmacokinetics of quinidine in normal and anuric rats. Acta Pharmacol. Toxicol. 1977; 41: 161
  • Klotz U., Golbs E. The pharmacokinetics and tissue distribution of the new antiarrhythmic agent, lorcainide in rats. Arzneim- Forsch/Drug Res. 1980; 30: 619
  • Kaplan S. A., Alexander K., Jack M. L., Puglisi C. V., De Silva J. A. F., Lee T. L., Weinfeld R. E. Pharmacokinetic profiles of clonazepam in dog and humans and of flunitrazepam in dog. J. Pharm. Sci. 1974; 63: 527
  • Bekersky I., Maggio A. C., Mattaliano V., Boxenbaum H. G., Maynard D. E., Cohn P. D., Kaplan S. A. Influence of phenobarbitone on the disposition of clonazepam and antipyrine in the dog. J. Pharmacokinet. Biopharm. 1977; 5: 507
  • Griffiths R., Lee R. M., Taylor D. C. Kinetics of cimetidine in man and experimental animals. Cimetidine, W. L. Borland, F. Simkins. Excerpta Medica, Amsterdam 1977; 38
  • Pedersen P. V., Miller R. Pharmacokinetics and bioavailability of cimetidine in humans. J. Pharm. Sci. 1980; 69: 394
  • Halkin H., Meffin P., Melmon K. L., Rowland M. Lidocaine and metabolite levels. Clin. Pharm. Ther. 1975; 17: 669
  • Tucker G. T., Wiklund L., Berlin-Wahlen A., Mather L. E. Hepatic clearance of local anaesthetics in man. J. Pharmacokinet. Biopharm. 1977; 5: 111
  • Heykants J., Knaeps A., Meuldermans W., Michiels M. On the pharmacokinetics of domperidone in animals and man. Eur. J. Drug Metab. Pharmacokinet. 1981; 6: 27
  • Johannessen W., Gadeholt G., Aarbakke J. Ether anaesthesia and drug kinetics. J. Pharm. Pharmacol. 1981; 33: 365
  • Dean M., O'Donnell L., Penglis S., Stock B. Antipyrine pharmacokinetics in the pregnant rat. Drug Metab. Disp. 1980; 8: 265
  • Ossenberg F. W., Peignoux M., Bourdiau D., Benhamou J. P. Pentobarbital pharmacokinetics in the normal and in the hepatectomized rat. J. Pharm. Exp. Ther. 1975; 194: 111
  • Buice R. G. Effect of hyperbilirubinemia on the pharmacokinetics of pentobarbital in the rat. Res. Commun. Chem. Pathol. Pharmacol. 1978; 21: 237
  • Lukas G., Kunjbala H. V., Brindle S. D., LeSher A. R., Wagner W. E. Biological disposition of sodium dichloroacetate in animals and humans. J. Pharm. Sci. 1980; 69: 419
  • Parke D. V. The metabolism and chemobiokinetics of environmental chemicals. The Principles and Methods in Modern Toxicology, C. L. Galli, S. D. Murphy, R. Paolletti. Elsevier, Amsterdam 1980; 85
  • Jansen A. B. A. Total radioactivity half lives. Drug Metab. Disp. 1979; 7: 350
  • Evans G. H., Nies A. S., Shand D. G. Plasma binding of propranolol. J. Pharm. Exp. Ther. 1973; 186: 114
  • Singhvi S. M., Kripalani K. J., Dean A. V., Reim G. R., Kulesza J. S., Meeker F. S., Ross J. J., Shaw J. M., Migdalof B. H. Absorption and bioavability of captopril in mice and rats after administration by gavage and in the diet. J. Pharm. Sci. 1981; 70: 885
  • Welling P. G. Drug kinetics. Foreign Compound Metabolism in Mammals. Chemical Society, London 1972; Vol. 2: 412
  • Perrier D., Gibaldi M. Influence of first pass effect on the systemic availability of propoxyphene. J. Clin. Pharmacol. 1972; 12: 449
  • Giacomini K. M., Nakeeb S. M., Levy G. Pharmacokinetic studies of propoxyphene. J. Pharm. Sci. 1980; 69: 786
  • Clark B., Neale M. G. Hepatic and renal clearance of sodium cromoglycate. J. Pharm. Pharmacol. 1981; 33: 744
  • Data J. L., Rane A., Gerkens J., Wilkinson G. R., Nies A. S., Branch R. A. Indomethacin and frusemide. J. Pharm. Exp. Ther. 1978; 206: 431
  • Branch R. A., Shand D. G., Wilkinson G. R., Nies A. S. The reduction of lidocaine clearance by dl-propranolol. J. Pharm. Exp. Ther. 1973; 184: 515
  • Deboer A. G., Breimer D. D., Pronk J., Gubbens-Stibbe J. M. Rectal bioavailability of lidocaine in rats. J. Pharm. Sci. 1980; 69: 804
  • Schuppan V. D., Schmidt I., Heller M. Untersuchungen zur pharmacokinetik von metroclopramid am menshen. Arzneim-Forsch. /Drug Res. 1979; 29: 151
  • Bakke O. M., Segura J. The absorption and elimination of metoclopramide in three animal species. J. Pharm. Pharmacol. 1976; 28: 32
  • Dedrick R. L. Animal scale up. Pharmacology and Pharmacokinetics, T. Teorell, R. L. Dedrick, P. G. Condliffe. Plenum Press, New York 1974; 117
  • Yakatan G. J., Maness D. D., Scholler J., Johnston J. T., Novick W. J., Doluisio J. T. Plasma and tissue levels of furosemide in dogs and monkeys following single and multiple oral doses. Res. Commun. Chem. Pathol. Pharmacol. 1979; 24: 465
  • Ehrnebo M. Pharmacokinetics and distribution properties of pentobarbital in humans following oral and intravenous administration. J. Pharm. Sci. 1974; 63: 1114
  • Davis L. E., Baggot J. D., Davis C. A. N., Powers T. E. Elimination kinetics of pentobarbital in nephrectomised dogs. Am. J. Vet. Res. 1973; 34: 231
  • El-Sayed M. G. A., Atef M., El-Gendi A. Y. I., Youssef S. A. H. Disposition kinetics of furosemide in dogs. Arch. Int. Pharmacodyn. 1981; 253: 4
  • Duggan D. E., Kwan K. C. Enterohepatic recirculation of drugs as a determinant of therapeutic ratio. Drug Metab. Rev. 1979; 9: 21
  • Domenech J., Lauroba J., Moreno J., Pla-Delfina J. M. A relationship between biological half-life and effective half-life according to pharmacological responses in non-steroid anti-inflammatory drugs. Arzneim-Forsch. /Drug Res. 1981; 31: 445
  • Andreasen F., Mikkelsen E. Distribution, elimination and effect of furosemide in normal subjects and in patients with heart failure. Eur. J. Clin. Pharmacol. 1977; 12: 15
  • Wallin J. D., Ryals P., Kaplowitz N. Metabolic clearance of furosemide in the rat. J. Pharm. Exp. Ther. 1977; 200: 52
  • Roberts S. M., Levy G. Pharmacokinetic studies on propoxyphene. IV. Effect of renal failure on systemic clearance in rats. J. Pharm. Sci. 1980; 69: 363
  • Smith D. A., Neale M. G. Metabolism and clearance of proxicromil, studies in rat, hamster, rabbit, dog, squirrel monkey, cynomolgus monkey, baboon and man. Eur. J. Drug Metab. Pharmacokinet 1983, to be published
  • Smith D. A. Unpublished observations 1980
  • Nation R. L. Drug kinetics in childbirth. Clin. Pharmacokinet. 1980; 5: 340
  • Dahlstrom B. E., Paalzow L. K., Lindberg C., Bogentoft C. Pharmacokinetics and analgesic effect of pethidine (meperidine) and its metabolites in the rat. Drug Metab. Disp. 1979; 7: 108
  • Smith D. A. Differences in toxicity due to species variation in the metabolism of an oral anti-allergy agent. Br. J. Pharmacol. 1979; 66: 422P
  • McManus M. E., Ilett K. F. Comparison of rate of hepatic metabolismin vitro and half-life for antipyrinein vivo in three species. Xenobiotica 1979; 9: 107
  • Gladigau V. V., Voltman K. O. Description of the pharmacokinetic behaviour of etozolin and its main metabolite. Arzneim-Forsch/Drug Res. 1977; 27: 1786
  • Aungst B. J., Veseel E. S., Shapiro I. R. Unusual characteristics of the dose dependent uptake of propylthiouracil by thyroid gland. in vivo, Biochem. Pharmacol. 1979; 28: 1479
  • Swanson B. N., Frolik C. A., Zaharevitz D. W., Roller P. P., Sporn M. B. Dose dependent kinetics of all-trans-retinoic acid in rats. Biochem. Pharmacol. 1981; 30: 107
  • Sweatman T. W., Renwick A. G. The tissue distribution and pharmacokinetics of saccharin in the rat. Toxicol. Appl. Pharmacol. 1980; 55: 18
  • Venkataramanan R., Axelson J. E. Dose dependent pharmacokinetics of tocainide in the rat. J. Pharm. Exp. Ther. 1980; 215: 231
  • Marre R., Freiesleben H. Antimicrobial agents in rats, serum levels of parenteral cephalosporins. Arzneim-Forsch./Drug Res. 1979; 29: 932
  • Smyth R. D., Hottendorf G. H. Application of pharmacokinetics and biopharmaceutics in the design of toxicological studies. Toxicol. Appl. Pharmacol. 1980; 53: 179
  • Latini R., Bonati M., Castelli D., Garattini S. Dose dependent kinetics of caffeine in rats. Toxicol. Lett. 1978; 2: 267
  • Miller R. P., Rotenberg K. S., Adir J. Effect of dose on the pharmacokinetics of intravenous nicotine in the rat. Drug Metab. Disp. 1977; 5: 436
  • Constantin M., Pognat J. F. Pharmacokinetics of amitrexine in the dog. Arzneim-Forsch./Drug Res. 1978; 28: 646
  • Konishi M., Agoh T., Sato T., Konaka R., Mori Y. Metabolism and disposition of peptidoaminobenzophenone (2-O-chlorobenzoyl-4-chloro-n-methyl-N′-glycylglycinanilide) and its major benzodiazepine metabolites in dogs. Drug Metab. Disp. 1979; 8: 253
  • Eason C. T., Clark B., Smith D. A., Parke D. V. The mechanism of hepatotoxicity of a chromone carboxylic acid in the dog. Xenobiotica 1982; 12: 155
  • Sasahara K., Nitanai T., Habara T., Morioka T., Nakajima E. Dosage form design for improvement of bioavailability of levodopa. II. Bioavailability of marketed levodopa preparations in dogs and Parkinsonian patients. J. Pharm. Sci. 1980; 69: 261
  • Ishigami M., Sabouromaru K., Niino K., Kido M., Morita S., Miyamoto G., Kohri H. Pharmacokinetics of procaterol in the rat, rabbit and beagle dog. Arzneim-Forsch./Drug Res. 1979; 25: 266
  • Gibson T. P., Nelson H. A. Digoxin alters quinidine and quinidine alters digoxin pharmacokinetics in dogs. J. Lab. Clin. Med. 1980; 95: 417
  • Jaillon P., Kates R. E. Phenytoin-induced changes in quinidine and 3-hydroxyquinidine pharmacokinetics in conscious dogs. J. Pharmacol. Exp. Ther. 1980; 213: 33
  • Loscher W., Esenwein H. Pharmacokinetics of sodium valproate in dog and mouse. Arzneim-Forsch./Drug Res. 1978; 28: 782
  • Laufen V. H., Juhran W., Fleissig W., Gotz R., Scharpf F., Bartsch G. On the pharmacokinetics of vincamine after i.v. and oral application to the dog. Arzneim-Forsch/Drug Res. 1977; 27: 1255
  • Kienel V. G. Comparison between the pharmacokinetics of epicillin and ampicillin. Arzneim-Forsch/Drug Res. 1976; 26: 781
  • Ladefoget O. The effect of carbon tetrachloride (CCL4) induced liver damage on the volume of distribution, the elimination half-life and body clearance of antipyrine and warfarin in rabbits. Acta Vet. Scand. 1979; 20: 429
  • Ahmad R. A., Rogers H. J. Non-linear pharmacokinetic behaviour of dapsone in the rabbit. J. Pharm. Pharmacol. 1981; 33: 547
  • Fukuchi S., Katayama K., Kakemi M., Ueda M., Koizumi T. Biological effects of furosemide in relation to its disposition in rabbits. Chem. Pharm. Bull. 1977; 25: 2217
  • Bloedow D. C., Ralston D. H., Hargrove J. C. Lidocaine pharmacokinetics in pregnant and nonpregnant sheep. J. Pharm. Sci. 1980; 69: 32
  • Madsen S. M., Ribel U. Pharmacokinetics of theophylline and 3-methylxanthine in guinea pigs. Acta Pharmacol. Toxicol. 1981; 48: 1
  • McAllister W. A. C., Winfield C. R., Collier J. V. Pharmacokinetics of prednisolone in normal and asthmatic subjects in relation to dose. Eur. J. Clin. Pharmacol. 1981; 20: 141
  • Doluisio J. T., Lapiana J. C., Dittert L. W. Pharmacokinetics of ampicillin trihydrate, sodium ampicillin and sodium dicloxacillin following intramuscular injection. J. Pharm. Sci. 1971; 60: 715
  • Jusko W. J., Rose J. Q. Monitoring prednisone and prednisolone. Ther. Drug Monitoring 1980; 2: 169
  • Clark B., Smith D. A. An Introduction to Pharmacokinetics. Blackwell Scientific, Oxford 1981
  • Ramzan M. I., Triggs E. J., Shanks C. A. Pharmacokinetic studies in man with gallamine triethiodide. Eur. J. Clin. Pharmacol. 1980; 17: 135
  • Casarelt L. J., Doull J. Toxicology, the Basic Science of Poisons. Macmillan, New York 1975, chap. 5
  • Sioufi A., Colussi D., Caudal F., Schoeller J. P., Massias P. Pharmacokinetics of phenylbutazone in healthy subjects after oral administration of single and multiple doses. J. Pharm. Sci. 1980; 69: 1413
  • Tanner A., Bocher F., Caffin J., Halliday J., Powell L. Dose dependent prednisolone kinetics. Clin. Pharm. Ther. 1979; 25: 571
  • Galinsky R. E., Levy G. Dose- and time-dependent elimination of acetominophen in rats: pharmacokinetic implications of cosubstrate depletion. J. Pharm. Exp. Ther. 1981; 219: 14
  • Price Evans D. A. Human pharmacogenetics. Drug Metabolism from Microbe to Man, D. V. Parke, R. L. Smith. Taylor & Francis, London 1977; 369
  • Caldwell J., Davies S., Smith R. L. Inter-individual differences in the conjugation of paracetamol with glucuronic acid and sulphate. Br. J. Pharmacol. 1980; 70: 112P
  • Eichelbaum M., Spannbrucker N., Steineke B., Dengler H. J. Defective N-oxidation of sparteine in man: a new pharmacogenetic effect. Eur. J. Clin. Pharmacol. 1979; 16: 183
  • Singlas E., Goujet M. A., Simon P. Pharmacokinetics of perhexiline maleate in anginal patients with and without peripheral neuropathy. Eur. J. Clin. Pharmacol. 1978; 14: 195
  • Blaschke T. F. Protein binding and kinetics of drugs in liver diseases. Clin. Pharmacokinet. 1977; 2: 32
  • Belpaire F. M., Bogaert M. G., Mussche M. M. Influence of acute renal failure on the protein binding of drugs in animals and in man. Eur. J. Clin. Pharmacol. 1977; 11: 27
  • Guentert T. W., Oie S. Effect of plasma protein binding on quinidine kinetics in the rabbit. J. Pharm. Exp. Ther. 1980; 215: 165
  • Yu H. Y., Sawada Y., Sugiyama Y., Iga T., Hanano M. Effect of sulfadimethoxine on thiopental distribution and elimination in rats. J. Pharm. Sci. 1981; 70: 323
  • Richey D. P., Bender A. D. Pharmacokinetic consequences of ageing. Ann. Rev. Pharmacol. Toxicol. 1977; 17: 49
  • Hulse M., Feldman S., Bruckner J. V. Effect of blood sampling schedules on protein drug binding in the rat. J. Pharm. Exp. Ther. 1981; 218: 416
  • Walker C. H. Species differences in microsomal monooxygenase activity and their relationship to biological half-lives. Drug Metab. Rev. 1978; 7: 295
  • Brodie B. B., Reid W. D. Some pharmacological consequences of species variation in rates of metabolism. Fed. Proc. 1967; 6: 1062
  • Loftsson T., Kaminski J. J., Bodor N. Improved delivery through biological membranes. VIII. Design, synthesis andin vivo testing of prodrugs of aspirin. J. Pharm. Sci. 1981; 70: 743
  • Rowland M., Riegelman S. Pharmacokinetics of acetylsalicylic acid and salicylic acid after intravenous administration in man. J. Pharm. Sci. 1968; 57: 1313
  • Kaneniwa N., Hiura M., Nakagawa S. Effect of lipid solubility and dose on the elimination of barbiturates in rabbits. Chem. Pharm. Bull. 1979; 27: 1501
  • Ohnhaus E. E., Thorgeirsson S. S., Davies D. S., Breckenridge A. Changes in liver blood flow during enzyme induction. Biochem. Pharmacol. 1971; 20: 2561
  • Denis P., Ossenberg F. W., Benhamou J. P. Hepatic blood flow and enzyme induction in the rat. Biochem. Pharmacol. 1975; 24: 249
  • Nies A. S., Wilkinson G. R., Rush B. D., Strother J. R., McDevitt D. G. Effects of alteration of hepatic microsomal enzyme activity on liver blood flow in the rat. Biochem. Pharmacol. 1991; 25, 1976
  • Rappoport A. M. Physioanatomical basis of toxic liver injury. Toxic Injury of the Liver, E. Farber, M. M. Fisher. Marcel Dekker, New York 1979; 1, Part A
  • Heywood R. Target organ toxicity. Toxicol. Lett. 1981; 8: 349
  • Peto R., Pike M. C., Day N. E., Gray R. G., Lee P. N., Parish S., Peto J., Richards S., Wahrendorf J. IARC Monogr. Long-Term and Short-Term Screening Assays for Carcinogens: a Critical Appraisal. IARC, Lyon 1980; 311, Suppl. 2
  • Sladek N. E., Domeyer B. E., Merriman R. L., Brophy G. T. Differential effects of Walker 256 carcinosarcoma cells growing subcutaneously, intramuscularly, or intraperitoneally on hepatic microsomal mixed function oxygenase activity. Drug Metab. Disp. 1978; 6: 412
  • Balant L. P., McAinsh J. Use of metabolite data in the evaluation of pharmacokinetics and drug action. Concepts in Drug Metabolism, P. Jenner, B. Testa. Marcel Dekker, New York 1980; 311
  • Migdalof B. H., Yorgey K. A., Popkave C. G. The time course of tolmetin and its metabolites in the plasma of individual rats and mice. Drug Metab. Disp. 1976; 4: 468
  • Chanoine F., Benedetti M. S., Ancher J. F., Dostert P. Absorption, distribution, elimination and metabolism of14C-heptaminol hydrochloride in rat. Arzneim-Forsch./Drug Res. 1981; 31: 1430
  • Smyth R. D., Van Harken D. R., Pfeffer M., Nardella P. A., Vasiljev M., Pinto J. S., Hottendorf G. H. Biological disposition of 8-methoxsalen in rat and man. Arzneim. Forsch./Drug Res. 1980; 30: 1725
  • Hucker H. B., Stauffer S. C., White S. D., Rhodes R. E., Arison B. H., Umbenhauer E. R., Bower R. J., McMahon F. G. Physiologic disposition and metabolic fate of a new anti inflammatory agentcis-5-fluoro-2-methyl-1-[p-(methylsulfinyl)-benzlidenyl]-indene-3-acetic acid in the rat, dog, rhesus monkey and man. Drug Metab. Disp. 1973; 1: 721
  • Dain J. G., Bhuta S. I., Coombs R. A., Talbot K. C., Duggar H. A. Metabolism of butalbital, 5-allyl-5-isobutyl barbituric acid in the dog. Drug Metab. Disp. 1980; 8: 247
  • Cayen M. N., Kraml M., Robinson W. T., Dvornik D. Disposition of furobufen in mice, rats, dogs and man. Drug Metab. Disp. 1981; 9: 119
  • Dieterle W., Faigle J. W. Species differences in the disposition and metabolism of sulfinpyrazone. Xenobiotica 1981; 11: 559
  • Wilson A. G. E., Pickett R. D., Eling T. E., Anderson M. W. Studies on the persistence of basic amines in the rabbit lung. Drug Metab. Disp. 1979; 7: 420
  • Abernathy D. R., Greenblatt D. J., Divoll M., Harmatz J. S., Shader R. I. Alterations in drug distribution and clearance due to obesity. J. Pharm. Exp. Ther. 1981; 217: 681
  • Smith D. A., Fisher A. N. Age related changes in the clearance and oral absorption of sodium cromoglycate in the developing albino rat. J. Pharm. Pharmacol. 1980; 32: 823
  • Fisher A. N., Smith D. A. Interpretation of clearance data in experiments involving bodyweight changes. Abstr. Stowe School Symp. Drug Metabolism. 1982
  • Collins J. M., Blake D. A., Egner P. G. Phenytoin metabolism in the rat. Drug Metab. Disp. 1978; 6: 251
  • Smith D. A. Unpublished observations 1982
  • Smith R. L. Species differences in the biliary excretion of drugs. Proc. Eur. Soc. Study Drug Toxicol. 1970; 11: 19
  • Levine W. G. Biliary excretion of drugs and other xenobiotics. Ann. Rev. Pharmacol. Toxicol. 1978; 18: 81
  • O'Flaherty E. J. Toxicants and Drugs, Kinetics and Dynamics. John Wiley & Sons, New York 1981
  • Dixon B. A., Caldwell J., Smith R. L. Metabolism of arylacetic acids. II. The fate of [14C] hydratropic acid and its variation with species. Xenobiotica 1977; 7: 695
  • Mehta R., Hirom P. C., Milburn P. The influence of dose on the pattern of conjugation of phenol and 1-napthol in nonhuman primates. Xenobiotica 1978; 8: 445
  • Hall B. E., James S. P. Some pathways of xenobiotic metabolism in the adult and neonatal marmoset (. Callithrix jacchus), Xenobiotica 1980; 10: 421
  • Koster H., Halsema I., Scholtens E., Knippers M., Mulder G. J. Dose dependent shifts in the sulfation and glucuronidation of phenolic compounds in the ratin vivo and in isolated hepatocytes. The role of saturation of phenolsulfotransferases. Biochem. Pharmacol. 1981; 30: 2569
  • Spector W. S. Acute toxicities. Handbook of Toxicology. W. B. Saunders, Philadelphia 1956; Vol. 1
  • Klaassen C. D., Strom S. C. Comparison of biliary excretory function and bile composition in male, female and lactating female rats. Drug Metab. Disp. 1978; 6: 120
  • Eason C. T. The Mechanism of Hepatotoxicity of an Anti-Allergy Compound, Ph.D. thesis. University of Surrey, SurreyU.K. 1981
  • Wheldrake J. F., Hawke D., Baudinette R. V. Mixed function oxidase activity in a desert rodent. Notomys alexis, Xenobiotica 1979; 9: 565
  • Green T. P., Mirkin B. L. Furosemide disposition in normal and proteinuric rats: urinary drug-protein binding as a determinant of drug excretion. J. Pharm. Exp. Ther. 1981; 218: 122
  • Altman P. L., Dittmer D. S. Biological handbooks. Blood and Other Body Fluids. American Society for Experimental Biology, Newark, N.J. 1971; 363–409
  • Thornton P. C., Wright P. A., Sacra P. J., Goodier T. E. W. The ferretMustela putorius furo, as a new species in toxicology. Lab. Anim. 1979; 13: 119
  • Cornelius C. E. Rates of chloresis in various species. Am. J. Dig. Dis. 1976; 21: 426
  • Boyd E. M., Dolman M., Knight L. M., Sheppard E. P. The chronic oral toxicity of caffeine. Can. J. Physiol. Pharmacol. 1965; 43: 995
  • Boyd E. M., Jarzylo S. V. Daily oral doses of pilocarpine tolerated by albino rats. Arch. Int. Pharmacodyn. Ther. 1968; 175: 84
  • Boyd E. M. Analgesic abuse: maximal tolerated daily doses of acetylsalicyclic acid. Can. Med. Assoc. J. 1968; 99: 790
  • Chan P. K., Reddy C. S., Hayes A. W. Acute toxicity of penicillic acid and its interaction with pentobarbital and other compounds. Toxicol. Appl. Pharmacol. 1980; 52: 1
  • Tattersall M. L. Statistics and the LD50. Arch. Toxicol. 1982; 267, Suppl 5
  • Litchfield J. T., Wilcoxon F. A simplified method of evaluating dose-effect experiments. J. Pharmacol. Exp. Ther. 1949; 96: 99
  • Alder S., Janton C., Zbinden G. Preclinical Safety Requirements in 1980. Institute of Toxicology, Zurich 1981
  • Kimura E. T., Tekeli S., Lewkowski J. P., Majors K. R., Kestenson J. W. Acute and subacute toxicity studies with fortimicin A sulphate (Abbott - 44747), a new aminoglycoside antibiotic. Toxicol. Appl. Pharmacol. 1980; 53: 399
  • Chou B. J., Mir G. N., Brown W. R., Rapp W. R., Yelnosky J. Toxicity studies on lidomidine hydrochloride (WHR-1142A), a novel antidiarrheal agent. Arzneim-Forsch./Drug Res. 1978; 28: 1471
  • Herman V. M., Wiegleb J., Leuschner F. Toxicological studies on etozolin. Arzneim-Forsch./Drug Res. 1977; 27: 1758
  • Gerber N., Weller W. L., Lynn R., Rango R. E., Sweetman B. J., Bush M. J. Study of dose dependent metabolism of 5,5-diphenyl hydantoin in the rat using new methodology for isolation and quantitation of metabolitesin vivo and. in vitro, J. Pharmacol. Exp. Ther. 1971; 178: 567
  • Stella V. J., Chu C. K. Effect of short term exposure to polychlorinated biphenyls on pharmacokinetics of intravenous pentobarbital in rats. J. Pharm. Sci. 1980; 69: 1274
  • Aldridge A., Niems A. H. The effects of phenobarbital and β-napthoflavone on the elimination kinetics and metabolite pattern of caffeine in the beagle dog. Drug Metab. Disp. 1979; 7: 378
  • Yacobi A., Slattery J. T., Levy G. Comparative pharmacokinetics of coumarin anticoagulants. J. Pharm. Sci. 1980; 69: 634
  • Gillette J. R. Kinetic aspects of metabolism and elimination of foreign compounds in animals. Enzymatic Basis of Detoxication, W. B. Jakoby. Academic Press, New York 1980; Vol. 1: 9
  • Vessel E. S. Genetic and environmental factors affecting drug disposition in man. Clin. Pharmacol. Ther. 1977; 22: 659
  • Levy G. Pharmacokinetics in renal disease. Am. J. Med. 1977; 62: 461
  • Klotz U. Influence of liver disease on the elimination of drugs. Eur. J. Drug Metab. Pharmacokinet. 1978; 3: 129
  • Williams R. L., Benet L. Z. Drug pharmacokinetics in cardiac and hepatic disease. Ann. Rev. Pharmacol. Toxicol. 1980; 20: 389
  • Gillette J. R., Pang K. S. Theoretic aspects of pharmacokinetic drug interactions. Clin. Pharmacol. Ther. 1977; 22: 623
  • Chatfield D. H., Green J. N. Disposition and metabolism of benoxaprofen in laboratory animals and man. Xenobiotica 1978; 8: 133
  • Kensler C. J. Experimental procedures in the evaluation of chemical carcinogens. Regulatory Aspects of Carcinogens and Food Additives—The Delaney Clause, F. Coulston. Academic Press, New York 1979; 239
  • Skone-James S. G. Carcinogenicity studies on di(2-ethylhexyl) adipate. Bibra Bull. 1981; 20(5)237
  • Kraybill H. F. By appropriate methods: the Delaney clause. Regulatory Aspects of Carcinogens and Food Additive—The Delaney Clause, F. Coulston. Academic Press, New York 1979; 61
  • Nies A. S., Shand D. G., Wilkinson G. R. Altered hepatic blood flow and drug disposition. Clin. Pharmacokinet. 1976; 1: 135
  • Welling P. G. Drug kinetics. Foreign Compound Metabolism in Mammals. The Chemical Society, London 1975; Vol. 3: 107
  • Brown S. S. Kinetics of absorption, distribution and excretion. Foreign Compound Metabolism in Mammals. The Chemical Society, London 1970; Vol. 1: 98
  • Katchem B., Buxbaum S., Meyer J., Ning J. Metabolism and pharmacokinetics of a new nonsteroid, anti-inflammatory agent, 2-(3-chloro-o-toluidino)nicotinic acid (lonixin) in rats, dogs and monkeys. J. Pharm. Exp. Ther. 1973; 184: 453
  • Stohs S. J., Al-Turk W. A., Angle C. R. Glutathione- S-transferase and glutathione reductase in hepatic and extrahepatic tissues of female mice as a function of age. Biochem. Pharmacol. 1982; 31: 2113
  • Kitani K., Kanai S., Miu R., Morita Y., Kashara M. The effect of ageing on the biliary excretion of ouabain in the rat. Exp. Geront. 1978; 13: 9
  • Kato R., Takanaka A. The effect of phenobartitone on electron transport system, oxidation and reduction of drugs in liver microsomes of rats of different ages. J. Biochem. 1968; 63: 406
  • Schmucker D. L., Wang R. K. Effect of ageing and phenobarbital on the rat liver microsomal drug-metabolising system. Mech. Ageing Dev. 1981; 15: 189
  • Kato R., Vassanelli P., Frontino G., Chiesara E. Variations in the activity of the liver microsomal drug metabolising enzymes in rats in relation to age. Biochem. Pharmacol. 1964; 13: 1037
  • Klotz U. Effect of age on levels of diazepam in plasma and brain of rats. Nauyn-Schmiedeberg's Arch. 1979; 307: 167
  • Latini R., Bonati M., Manzi E., Tacconi M. T., Sadurska B., Bizzi A. Caffeine disposition and effects in young and one-year old rats. J. Pharm. Pharmacol. 1980; 32: 596
  • Glantz S. A., Kernoff R., Goldman R. H. Age related changes in ouabain pharmacology. Circ., Res. 1976; 39: 409
  • Mahgoub A., Idle J. R., Dring L. G., Lancaster R., Smith R. L. Polymorphic hydroxylation of debrisoquine in man. Lancet 1977; ii: 584
  • Inaba T., Otton S. V., Kalow W. Deficient metabolism of debrisoquine and sparteine. Clin. Pharm. Therap. 1980; 27: 547
  • Sloan T. P., Mahgoub A., Lanaester R., Idle J. R., Smith R. L. Polymorphism of carbon oxidation of drugs and clinical implications. Br. Med. J. 1978; 2: 655
  • Tucker G. T., Silas J. H., Iyun A. O., Lennard M. S., Smith A. J. Polymorphic, hydroxylation of debrisoquine. Lancet 1977; ii: 718
  • Glocklin V. C. General considerations for studies of the metabolism of drugs and other chemicals. Drug Met. Rev. 1982; 13: 929
  • Gehring P. J., Watanabe P. G., Young J. D. The relevance of dose-dependent pharmacokinetics in the assessment of carcinogenic hazard of chemicals. The Origins of Human Cancer, Cold Spring Harbour Conference, H. H. Hiatt, J. D. Watson, J. A. Wouster. 1977; 187
  • Poynter D. Problems in assessing the toxicity of inhaled drugs. Evaluation of Bronchodilator Drugs, An Asthma Research Council Symposium, D. M. Burley, S. W. Clarke, M. F. Cuthbert, J. W. Paterson, J. H. Shelly. Trust for Education and Research in Therapeutics. 1974; 167

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