Summary
The pharmacokinetics of the new lipidlowering drug bezafibrate has been investigated in patients with impaired renal function and hyperlipoproteinaemia. 12 patients received a single oral dose of bezafibrate 300 mg. Plasma and urine samples were collected and bezafibrate was analyzed by gas chromatography. Eight of the patients had moderately impaired renal function, with a creatinine clearance between 20 and 40 ml/min; the mean plasma half-life of bezafibrate in them was 7.8±3.9 h (SD) and the plasma clearance was 0.03±0.02 l/kg · h. Three of the patients had a creatinine clearance>40 ml/min; in them the plasma half-life was shorter, 4.6±1.2 h, and the plasma clearance was higher, 0.06±0.01 l/kg · h. The slowest elimination of bezafibrate was found in a patient with a creatinine clearance of only 13 ml/min. This patient had a plasma half-life of 20.1 h, which is ten times longer than has been reported in healthy volunteers. Thus, when treating hyperlipoproteinaemia in patients with impaired renal function, the dosage of bezafibrate must be individualized because of its reduced renal elimination.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Abshagen U, Bablok W, Koch K, Lang PD, Schmidt HAE, Senn M, Stork H (1979) Disposition pharmacokinetics of bezafibrate in man. Eur J Clin Pharmacol 16:31–38
Abshagen U, Spörl-Radun S, Marinow J (1980a) Steady-state kinetics of bezafibrate and clofibrate in healthy female volunteers. Eur J Clin Pharmacol 17:305–308
Abshagen U, Kösters W, Kaufmann B, Lang PD (1980b) Pharmacokinetics of bezafibrate after single and multiple doses in the presence of renal failure. Klin Wochenschr 58:889–896
Arntz H-R, Klemens UH, Lang PD, Vollmar J (1978) Vergleich von Clofibrat und Bezafibrat bei Hyperlipoproteinämie Typ IIa and Typ IIb. Med Klin 73:1731–1737
Bolzano K, Krempler F, Schellenberg B, Schlierf G (1979) Eine vergleichende Studie von Bezafibrat und Clofibrat bei Patienten mit Hyperlipoproteinämie von Typ IIB und IV. Acta Med Austraca 6:90–94
Endele R (1978) A gas chromatographic method for the determination of bezafibrate in serum and urine. J Chromatogr 154:261–263
Goldberg AP, Sherrard DJ, Haas LB, Brunzell JD (1977) Control of clofibrate toxicity in uremic hypertriglyceridemia. Clin Pharmacol Ther 21:317–325
Katsilambros N, Braaten J, Ferguson BD, Bradley RF (1972) Muscular syndrome after clofibrate. N Engl J Med 286:1110
Köster W, Abshagen U, Lang PD, Endele R (1979) Pharmakokinetik und Metabolismus von Bezafibrat bei Patienten mit eingeschränkter Nierenfunktion. In: Greten H, Lang PD und Schettler (eds) Lipoproteine und Herzinfarkt. Gerhard Witzstrock, Baden-Baden, pp 113–116
Lageder H, Irsigler K (1978) Double-blind comparison of bezafibrate and clofibrate in patients with primary hyperlipoproteinaemia. In: Carlson LA, Paoletti R, Weber G (eds) International Conference on Atherosclerosis. Raven Press, New York, p 726
Norbeck H-E, Anderson P (1981) Treatment of uremic hypertrigly-ceridaemia with bezafibrate. Atherosclerosis (in press)
Olsson AG, Rössner S, Walldius G, Carlsson LA, Lang PD (1977) Effect of BM 15.075 on lipoprotein concentrations in different types of hyperlipoproteinaemia. Atherosclerosis 27:279–287
Perides AM, Alvarez-Ude F, Kerr DNS, Skillen AW (1975) Clofibrate induced muscular damage in patients with chronic renal failure. Lancet 2:1279–1282
Wagner JG, Northam JL, Alway CD, Carpenter OS, (1965) Blood levels of drug at equilibrium state after multiple dosing. Nature 207:1391–1402
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Anderson, P., Norbeck, H.E. Clinical pharmacokinetics of bezafibrate in patients with impaired renal function. Eur J Clin Pharmacol 21, 209–214 (1981). https://doi.org/10.1007/BF00627922
Received:
Revised:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00627922