Summary
In order to determine the appropriate dosage of carteolol in renal dysfunction, the pharmacokinetics of carteolol has been examined in appropriate patients. The plasma concentrations and urinary excretion of carteolol were investigated in 15 patients with varying degrees of renal impairment during the administration of 5–20 mg carteolol hydrochloride (5 mg/tablet) for 2–45 months.
Plasma carteolol levels were linearly correlated with the serum creatinine concentration (r = 0.87) and reciprocally with the creatinine clearance (r = 0.82). The urinary carteolol concentration was correlated with the urinary creatinine concentration (r = 0.69) and the urinary carteolol excretion was also correlated with the creatinine clearance (r = 0.79). These relationships become even closer when the plasma carteolol concentrations and urinary excretion rate of carteolol were factored by the administered tablets. The fractional renal excretion of carteolol was virtually constant at various degress of renal function, and it always exceeded 100%, which indicates that carteolol was actively secreted, even in patients with renal failure. The estimated tubular secretion rate of carteolol was logarithmically correlated with the fractional renal excretion of carteolol (r = 0.93).
The results indicate that the dose of carteolol should be determined according to the degree of renal impairment.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Chiba S (1977) Differential inotropic-chronotropic action of carteolol. Jpn J Pharmacol 27: 585–587
Nakagawa K, Murakami N, Yoshizaki S, Tominaga M, Mori H, Yabuuchi Y, Shintani S (1974) Derivatives of 3,4-dihydrocartostyril as β-adrenergic blocking agent. J Med Chem 17: 529–533
Hasimoto K, Kimura T, Yabuuchi Y (1976) Comparison of newly synthetized beta-adrenergic blockers, OPC-1085 and SQI11725, with pindolol and propranolol in the blood-perfused canine SA node and papillary muscle preparations. Jpn J Pharmacol 25: 504–506
Fitzgerald JD (1969) Perspectives in adrenergic beta-receptor blockade. Clin Pharmacol Ther 10: 292–306
Tarkiainen A, Saraste K, Seppala T, Gordin A, Auvinen J (1981) A controlled study of the antihypertensive effect of carteolol, a new β-adrenergic receptor blocking drug, in combination with hydrochlorthiazide and amiloride. Eur J Clin Pharmacol 19: 239–244
Alcocer L, Aspe J, Arce-Gourez E (1980) The antianginal activity of the beta-blocker carteolol. Clin Res 28: 153A
Tabei K, Furuya H, Asano Y, Hosoda S (1989) Effect of carteolol on renal function in healthy subjects and patients with hypertension. Eur J Clin Pharmacol 36: 83–86
Ishizaki T, Sasaki T, Kushida K, Horai Y, Chiba K, Suganuma R (1983) Pharmacokinetics and absolute bioavailability of carteolol, a new adrenergic blocking agent. Eur J Clin Pharmacol 25: 95–101
Odomi M, Akiyama H, Matsuura K, Shimizu T (1985) The determination of carteolol in human plasma and urine by high-performance liquid chromatography. Yakugaku Zasshi 105: 459–463
Lang W (1983) Tierexperimentelle Untersuchungen zur Pharmakokinetik von Carteolol. Arzneimforsch 33: 283–290
Hasenfuß G, Schafer-Korting M, Knauf H, Mutschler E, Just H (1985) Pharmacokinetics of carteolol in relation to renal function. Eur J Clin Pharmacol 29: 461–465
Sennello LT, Finley RA, Luther RR (1987) The effect of impaired renal function on the multiple dose clinical pharmacokinetics of carteolol. Adv Ther 4: pp. 298
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Amemiya, M., Tabei, K., Furuya, H. et al. Pharmacokinetics of carteolol in patients with impaired renal function. Eur J Clin Pharmacol 43, 417–421 (1992). https://doi.org/10.1007/BF02220619
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF02220619