Effects of the rate and composition of fluid replacement on the pharmacokinetics and pharmacodynamics of intravenous furosemide
Tóm tắt
Effects of differences in the rate and composition of intravenous fluid replacement for urine loss on the pharmacokinetics and pharmacodynamics of furosemide were evaluated using the dog as a model animal. Each of six dogs received 8-hr constant intravenous infusion of 20 mg (15 mg used in one dog) of furosemide with 0% replacement (treatment I), 50% replacement (treatment II), and 100% replacement (treatment III) with lactated Ringer's solution, as well as with 100% replacement with 5% dextrose in water (treatment IV). Most pharmacokinetic parameters, such as plasma clearance, steady-state volume of distribution, mean residence time, and terminal half-life, were essentially the same in all four treatments. Renal clearances and urinary excretion rates of the drug in treatments II–IVwere essentially the same, but about 20% higher than those in treatment I.In spite of the similarities in kinetic properties, diuretic and/or natriuretic effects from furosemide were markedly different among the four treatments. For example, mean 10-hr urine outputs were 646, 1046, 3156, and 1976 ml and mean 10-hr sodium excretions were 87.0, 142, 383, and 97.2 mmole for treatments I–IV,respectively. Except for treatment III,diuresis and/or natriuresis were found to be time-dependent, generally decreasing with time until reaching a low plateau during later hours of infusion. The present findings also showed that (1)no fluid replacement and 100% replacement with 5% dextrose solution both produced the same degree of severe acute tolerance in natriuresis, indicating the insignificance of water compensation in tolerance development; (2)in treatment II,where neutral sodium balance was achieved, the development of acute tolerance in diuresis and natriuresis can mainly be attributed to negative water balance under this special condition; (3)at steady state the hourly diuresis and natriuresis could differ up to about ten times between treatments. Some implications for the kinetic/dynamic relationship or modeling, in the clinical use, and in the bioequivalence evaluation of dosage forms are discussed.
Tài liệu tham khảo
L. E. Earley and J. A. Martino. Influence of sodium balance on the ability of diuretics to inhibit tubular reabsorption.Circulation 42:323–334 (1970).
R. A. Branch, C. J. C. Roberts, M. Homeida, and D. Levine. Determinants of response to furosemide in normal subjects.Br. J. Clin. Pharmacol. 4:121–127 (1977).
M. Homeida, C. Roberts, and R. A. Branch. Influence of probenecid and spironolactone on furosemide kinetics and dynamics in man.Clin. Pharmacol. Ther. 22:402–409 (1979).
C. S. Wilcox, W. E. Mitch, R. A. Kelly, K. Skorecki, T. W. Meyer, P. A. Friedman, and P. F. Souney. Response of the kidney to furosemide. I. Effect of salt intake and renal compensation.J. Lab. Clin. Med. 102:450–458 (1983).
T. Kahn, A. M. Kaufman, and F. L. Mac-Moune. Response to repeated furosemide administration on low chloride and low sodium intake in the rat.Clin. Sci. 64:565–572 (1983).
M. M. Hammarlund, B. Odlind, and L. K. Paalzow. Acute tolerance to furosemide in humans. Pharmacokinetic-pharmacodynamic modeling.J. Pharmacol. Exp. Ther. 233:447–453 (1985).
E. S. Waller, S. F. Hamilton, J. W. Massareth, M. A. Sharanevych, R. V. Smith, G. J. Yakatan, and J. T. Doluisio. Disposition and absolute bioavailability of furosemide in healthy males.J. Pharm. Sci. 71:1105–1108 (1982).
J. G. Copeland, D. W. Campbell, J. R. Plachetka, N. W. Salomon, and D. F. Larson. Diuresis with continuous infusion of furosemide after cardiac surgery.Am. J. Surg. 146:796–799 (1983).
A. Ebihara, K. Tawara, and T. Oka. Pharmacodynamic and pharmacokinetic study after slow release formulations of furosemide in man.Arzneim. Forsch./Drug Res. 33:163–166 (1983).
J. J. McNeil, F. J. E. Vajda, V. Vuayasekaren, and W. J. Louis. Bioavailability comparison of two proprietary preparations of furosemide.Med. J. Austr. 2:505–507 (1977).
D. M. Paton. Bioavailability of two preparations of furosemide.N. Z. Med. J. 91:208–210 (1980).
K. Uchino, S. Isozaki, J. Amano, N. Tanaka, Y. Saitoh, F. Nakagawa, Z. Tamura, and H. Oka. Clinical pharmacokinetics and diuretic effect of furosemide in plain tablet and retard capsule with normal subjects and cirrhotic patients.J. Pharmacobiodyn. 6:684–691 (1983).
S. Kaojaren, B. Day, and D. C. Brater. The time course of furosemide into urine: An independent determinant of overall response.Kidney Int. 22:69–74 (1982).
D. E. Smith, W. L. Gee, D. C. Brater, E. T. Lin, and L. Z. Benet. Preliminary evaluation of furosemide-probenecid interactions in humans.J. Pharm. Sci. 69:571–575 (1980).
D. C. Brater, P. Chennavasin, and R. Seiwell. Furosemide in patients with heart failure: Shift in dose-response curves.Clin. Pharmacol. Ther. 28:182–186 (1980).
D. C. Brater, P. Chennavasin, B. Day, A. Burdetta, and S. Anderson. Bumetanide and furosemide.Clin. Pharmacol. Ther. 34:207–213 (1983).
M. R. Kelly, A. D. Blair, A. W. Forey, N. A. Smidt, and R. E. Cutler. A comparison of the diuretic response to oral and intravenous furosemide in “diuretic-resistant” patients.Curr. Ther. Res. 21:1–9 (1977).
D. E. Smith, E. T. Lin, and L. Z. Benet. Absorption and disposition of furosemide in healthy volunteers, measured with a metabolite-specific assay.Drug Metab. Dispos. 8:337–342 (1980).
F. Andreasen, C. K. Christensen, F. K. Jacobsen, J. Jansen, C. E. Mogensen, and O. L. Pedersen. The individual variation in pharmacokinetics and pharmacodynamics in young normal male subjects.Eur. J. Clin. Invest. 12:247–255 (1982).
M. G. Lee, M. L. Chen, and W. L. Chiou. Pharmacokinetics of blood II: Unusual distribution and storage effect of furosemide.Res. Commun. Chem. Pathol. Pharmacol. 34:17–28 (1981).
M. G. Lee and W. L. Chiou. Evaluation of potential causes for the incomplete bioavailability of furosemide: Gastric first-pass metabolism,J. Pharmacokin. Biopharm. 11:623–640 (1983).
C. Y. Lui, M. G. Lee, and W. L. Chiou. Concentration andpH dependent steady-state volume of distribution of methotrexate estimated by a simple physiologically based method.J. Pharmacokin. Biopharm. 12:597–610 (1984).
W. L. Chiou, G. Lam, M. L. Chen, and M. G. Lee. Effect of arterial-venous plasma concentration differences on the determination of mean residence time of drug in the body.Res. Commun. Chem. Pathol. Pharmacol. 35:17–26 (1982).
W. L. Chiou. Mean hepatic transit time in determinations of mean absorption time.J. Pharm. Sci. 72:1365–1368 (1983).
L. Z. Benet and R. L. Galeazzi. Noncompartmental determination of the steady state volume of distribution.J. Pharm. Sci. 68:1071–1074 (1979).
W. L. Chiou. New calculation method for mean apparent drug volume of distribution and application to rational dosage regimens.J. Pharm. Sci. 68:1067–1069 (1979).
J. T. Helwig and K. A. Council.SAS User's Guide, SAS Instruments, 1979.
W. L. Chiou. Compartment- and model-independent linear plateau principle of drugs during a constant rate absorption or intravenous infusion.J. Pharmacokin. Biopharm. 8:311–318 (1980).
M. G. Lee, T. Li, and W. L. Chiou. Effect of intravenous infusion time on the pharmacokinetics and pharmacodynamics of the same total dose of furosemide.Biopharm. Drug Dispos., in press.
D. C. Brater. Resistance to loop diuretics. Why it happens and what to do about it.Drugs 30:427–443 (1985).
W. D. Sansum and R. T. Woodyatt. Studies on the theory of diuresis. VII. Timed interval injection of glucose at lower rates.J. Biol. Chem. 30:155–173 (1917).
B. Beermann. Kinetics and dynamics of furosemide and slow-acting furosemide.Clin. Pharmacol. Ther. 32:584–591 (1982).
B. K. Martin, M. Uihlein, R. M. J. Ings, L. A. Steven, and J. M. McEwen. Comparative bioavailability of two furosemide formulations in humans.J. Pharm. Sci. 73:437–441 (1984).
E. Dalen and B. Lindstrom. Bioavailability of two furosemide preparations.Br. J. Clin. Pharmacol. 6:537–538 (1978).
L. Z. Benet. Pharmacokinetics/pharmacodynamics of furosemide in man: A review.J. Pharmacokin. Biopharm. 7:1–27 (1979).
D. C. Brater. Clinical use of loop diuretics.Hasp. Form. 1983(October):962–975.
D. E. Smith, D. C. Brater, E. T. Lin, and L. Z. Benet. Attenuation of furosemide's diuretic effect by indomethacin: Pharmacokinetic evaluation.J. Pharmacokin. Biopharm. 7:265–274 (1979).
P. Chennavasin, R. Seiwell, D. C. Brater, and W. M. Liang. Pharmacodynamic analysis of the furosemide-probenecid interaction in man.Kidney Int. 16:187–195 (1979).