Classical Michaelis-Menten and system theory approach to modeling metabolite formation kinetics
Tóm tắt
The two compartment open model with Michaelis-Menten elimination kinetics is theorethicaly basic when single doses of drug are administered. To simulate data or to fit real data using this model, one must resort to numerical integration. A biomathematical model for multiple dosage regimen calculations of nonlinear metabolic systems in steady-state and a working example with phenytoin are presented. High correlation between phenytoin steady-state serum levels calculated from individual Km and Vmax values in the 15 adult epileptic outpatients and the observed levels at the third adjustment of phenytoin daily dose (r=0.961, p<0.01) were found.
Tài liệu tham khảo
Dedík, L., Durišová, M. (1995): CXT — A programme for analysis of linear, dynamic systems in the frequency domain. Int. J. Bio-Med. Comput., 39, 231–41.
Dedík, L., Durišová, M. (1996): CXT-MAIN: A software package for determination of the analytical form of the pharmacokinetic system weighting function. Comput, Methods, Programs, Biomed., 51, 183–92.
Dedík, L., Durišová, M. (1999): System Approach in Technical, Environmental and Biomedical Studies. Publishing House of Slovak University of Technology, Bratislava.
Durišová, M., Dedík, L. (1994): Comparative study of human pentacaine pharmacokinetics in time and frequency domain. Methods. Find. Exp. Clin. Pharmacol., 16, 219–32.
Dedík, L., Durišová, M. (1994): Frequency response method in pharmacokinetics. J. Pharmacokin. Biopharm., 22, 293–307.
Durišová, M., Dedík, L., Balan, M. (1995): Building a structured model of a complex pharmacokinetic system with time delays. Bull. Math. Biol., 57, 787–808.
Durišová, M., Dedík, L. (1997): Modeling in frequency domain used for assessment ofin vivo dissolution profile. Pharm. Res., 14, 860–4.
Dedík, L., Durišová, M. (2001): Modeling drug absorption from enteric coated granules. Methods. Find. Exp. Clin. Pharmacol., 23, 213–7.
Dedík, L., Durišová, M. (2002): System-approach methods for modeling and testing similarity of in vitro dissolutions of drug dosage formulations. Comput. Methods. Programs. Biomed., 69, 49–55.
Dedík, L., Durišová, M. (2002): System-approach to modeling metabolite formation from parent drug: a working example with methotrexate. Methods Find. Exp. Clin. Pharmacol., 24, 481–486.
Popović J. (1999): Derivation of Laplace transform for the general disposition deconvolution equation in drug metabolism kinetics. Exp. Toxic. Pathol., 51, 409–411.
Bray, H.G., Thorpe, W.V. and White, K. (1951): Kinetic Studies of the Metabolism of Foreign Organic Compounds I. Benzyl Alcohol and Benzaldehyde and Its Conjugation with Glycine and Glucuronic Acid in the Rabbit, Biochem. J., 48, 88–96.
Krüger-Thiemer, E. (1968): Pharmacokinetics and Dose — Concentration Relationship, IIIrd. Intern. Pharmacol. Meeteng, Sao Paulo 1966, Proc. 7, 63–113.
Krüger-Thiemer, E. (1968): Nonlinear Dose — Concentration Relationship. Farmaco (Pavia) Ed. Sci., 23, 717–756.
Henri, V. (1901): Compt. Rendu Hebd. Séanc. Acad. Sci. (Paris), 133, 891.
Briggs, G.E., Haldone, J.B.S. (1925): Biochem. J., 19, 383.
Botts, J., Morales, M. (1953): Faraday Soc. Trans., 49, 696, and (1958): 54, 593.
Walter, C. (1974): Graphical Procedure for the Detection of Deviations from the Classical Model of Enzyme Kinetics. J. Biol. Chem., 249, 699–703.
Michaelis, L., Menten, M.L. (1913): Die Kinetik der Invertinwirkung. Biochem. Z., 49, 333–369.
Gibaldi M., Boyes N.R., Feldman S. (1971): Influence of first-pass effect on availability of drugs on oral administration. J. Pharm. Sci., 60: 1338–1340
Vaughan P.D. (1975): Estimation of biological availability after oral drug administration when the drug is eliminated by urinary excretion and metabolism. J. Pharm. Pharmac., 27: 458–461
Rubin M.G., Tozer N.T. (1984): Theoretical considerations in the calculation of bioavailability of drugs exhibiting Michaelis-Menten elimination kinetics. J. Pharmacokin. Biopharm., 12: 437–450
Popović J, Banić B., Popović V. (1982): Biomathematical model for individualization of dosages for drugs with non-linear pharmacokinetic behaviour. Period, biol., 84, 176–179.
Popović J. (1985): Kinetic model of a drug with parallel first-order and capacity-limited elimination and its application. Iugoslav. Physiol. Pharmacol. Acta, 21, Suppl. 3, 287–288.
Popović J. (1985): Influence of first-pass effect on availability of drugs with simultaneous biotransformation in the liver and first-order elimination through the kidneys. Iugoslav. Physiol. Pharmacol. Acta, 21, Suppl. 3, 289–290.
Popović J. (1986): Dosage regimen calculations for drugs with first-order absorption, non-linear first-pass metabolism and parallel non-linear and first-order elimination. Period, biol., 88 (2), 183–184.
Popović J. (1987): Relationship between the steady-state serum level and the dose of drugs with first-pass and parallel michaelis-menten and first-order elimination. Acta pharmaceutica jugoslavica, Vol. 37, No. 4, 313–317.
Popović J. (author) (1992): Steady-state pharmacokinetics and dosing of Phenytoin and phenobarbital in patients, In: Sunchine I (ed): Recent developments in therapeutic drug monitoring. New York, Basel, Hong Kong, Marcel Dekker, Inc. Chapter 61, pages 409–414.
Popovic J. (1994): Toxicokinetic model of xenobiotic with parallel first order and capacity-limited elimination and its application on simulated data. Arch. Toxicol. Kinet. Xenobiot. Metab., 2(2), 417–418.
Richens A., Dunlop, A. (1975): Serum phenytoin levels in management of epilepsy. Lancet. 2, 247–24.
M. T. Ludden, W. D. Hawkins, P.J. Allen, and F. S. Hoffman. (1976): Optimum phenytoin dosage regimens. Lancet, 7, 307–308.
Ludden M.T., Allen P.J., Valutsky A.W., et al. (1977): Individualization of phenytoin dosage regimens. Clin. Pharmacol.Ther., 21, 287–293.
Mullen P. (1978): Optimal phenytoin therapy: A new technique for individualizing dosage. Clin. Pharmacol. Ther., 23, 228–232.
Wagner G.J. (1978): Time to reach steady-state and prediction of steady-state concentrations for drugs obeying Michaelis-Menten elimination kinetics. Pharmacokinet. Biopharm., 6, 209–225.
Mullen W.P., Foster W.P. (1979): Comparative evaluation of six techniques for determining the Michaelis-Menten parameters relating phenytoin dose and steady-state serum concentrations. J. Pharm. Pharmacol., 31, 100–104.
Ludden M.T. (1980): Individualization of phenytoin therapy. Pharm. Pharmacol., 32, 152.
Schumacher E.G. (1980):Using pharmacokinetics in drug therapy VI: Comparing methods tor dealing with nonlinear drugs like phenytoin. Am. I. Hosp. Pharm., 37, 128–132.
Vozeh S., Muir T.K., Sheiner B.L., Follath F. (1981): Predicting individual phenytoin dosage. J. Pharmacokinet. Biopharm., 9, 131–146.
Soldin J.S., Gilbert-Hill J. (1976): Rapid micromethod for measuring anticonvulsant drugs in serum by high-performance liquid chromatography. Clin. Chem., 22, 856–859.
Chiba K., Ishizaki T., Miura H., Minagawa K. (1980): Michaelis-Menten pharmacokinetics of diphenylhydantoin and application in the pediatric age patient. J. Pediatr., 96, 479–494.
Koren G., Brand N., MacLeod M.S. (1984): Influence of bioavailability on the calculated. Michaelis-Menten parameters of phenytoin in children. Ther. Drug Monitor., 6, 11–14.
Vazquez Rodriguez A., (1991): Comparison of methods for the prediction of phenytoin concentrations. J. Clin. Pharm. Ther., 16(1), 55–62
Cai W.M., (1991): A Bayesian qraphic method for predicting individual phenytoin dosage schedule. Zhongguo Vao Li Xue Bao, 12(2), 141–4.
Armijo J.A., (1991): Graphic estimation of phenytoin dose in adults and children. Ther. Drug. Monit., 13 (6), 507–10.
Burger D.M., (1994): Therapeutic drug monitoring of phenytoin in patients with the acquired immunodeficiccy syndrome. Ther. Drug. Monit., 16 (6), 616–20.
Wang X. (2003): A comparison of central (cerebrospinal and extracellular fluids) and peripheral blood kinetics of phenytoin after intravenous phenytoin andfosphenytoin. Seizure, 12 (6), 330–6.
Martineiii E.F. (2003): Rapidi.v. loading with phenytoin with subsequent dose adaptation using non-steady-state serum levels and a Bayesian forecasting computer program to predict maintenence doses. J. Clin. Pharm. Ther., 28 (5), 385–93
Purkins L. (2003) Coadministration of voriconazole and phenytoin: pharmacokinetic interaction, safety, and toleration. Br. J. Clin. Pharmacol., 56(1), 37–44.
Glick T.H. (2004): Preventing phenytoin intoxication: safer use of a familiar anticonvulsant. J. Farm. Pract., 53 (3), 197–202.