Summary
The plasma levels and urinary excretion of carteolol and its main metabolites 8-hydroxycarteolol and carteolol glucuronide were investigated in 6 healthy subjects and 9 patients with varying degrees of renal impairment following a single oral dose of 30 mg carteolol hydrochloride. In healthy subjects the half-life of carteolol was 7.1 h. 63% of the administered dose was recovered unchanged in urine, and in all 84% was excreted by the kidneys. The renal clearance of carteolol was 255 ml/min. In chronic renal failure (CRF) the terminal half-life was increased to a maximum of 41 h. Both the elimination rate constant and renal clearance were closely related to the creatinine clearance. In CRF the recovery of carteolol and its metabolites from urine was considerably reduced, suggesting that another pathway of drug elimination becomes relevant in renal disease. To avoid an increase in side-effects due to drug accumulation, the dosage of carteolol should be adjusted in relation to the reduction in creatinine clearance. The maintenance dose should be reduced to a half in patients with a creatinine clearance below 40 ml/min and above 10 ml/min. In those with a creatinine clearance of 10 ml/min or less, the dose should be reduced to 1/4.
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Hashimoto K, Kimura T, Yabuuchi Y (1976) Comparison of newly synthesized beta-adrenergic blockers OPC-1085 and SQ 111725 with pindolol and propranolol in the blood-perfused canine SA node and papillary muscle preparations. Jpn J Pharmacol 25: 504–506
Odenthal K-P (1983) Zur Pharmakodynamik von Carteolol. Arzneimittelforsch 33: 281–285
Berglund G, Descamps R, Thomis JA (1980) Pharmacokinetics of sotalol after chronic administration to patients with renal insufficiency. Eur J Clin Pharmacol 18: 321–326
Dreyfuss J, Brannick LJ, Vukovich RA, Shaw JM, Willard DA (1977) Metabolic studies in patients with nadolol: Oral and intravenous administration. J Clin Pharmacol 17: 300–307
Frishman W (1980) Clinical pharmacology of the new beta-adrenergic blocking drugs, part 9. Nadolol: A new long-acting beta-adrenoceptor blocking drug. Am Heart J 99: 124–128
Fitzgerald JD, Ruffin R, Smedstad KG, Roberts R, McAinsh J (1978) Studies on the pharmacokinetics and pharmacodynamics of atenolol in man. Eur J Clin Pharmacol 13: 81–89
Kirch W, Köhler H, Mutschler E, Schäfer M (1981) Pharmacokinetics of atenolol in relation to renal function. Eur J Clin Pharmacol 19: 65–71
Ishizaki T, Ohnishi A, Sasaki T, Kushida K, Horai Y, Chiba K, Suganuma T (1983) Pharmacokinetics and absolute bioavailability of carteolol, a new β-adrenergic receptor blocking agent. Eur J Clin Pharmacol 25: 95–101
Dettli L (1977) Elimination kinetics and dosage adjustment of drugs in patients with kidney disease. Prog Pharmacol Vol 1; No 4. Fischer, Stuttgart New York
S-Y Chu (1978) High pressure liquid chromatographic determination of 8-hydroxycarteolol in plasma and urine using electrochemical detection. J Pharm Sci 67: 1623–1625
Wellstein A, Palm D, Wiemer G, Schäfer-Korting M, Mutschler E (1984) A simple and reliable radioreceptor assay for β-adrenoceptor antagonists and active metabolites in native human plasma. Eur J Clin Pharmacol 27: 545–553
Knauf H, Schäfer-Korting M, Mutschler E (1981) Pharmakokinetik und biologische Wirkdauer von β-Rezeptorenblockern bei Niereninsuffizienz. Internist 22: 616–621
Lang W (1983) Tierexperimentelle Untersuchungen zur Pharmakokinetik von Carteolol. Arzneimittelforsch 33: 286–290
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Hasenfuß, G., Schäfer-Korting, M., Knauf, H. et al. Pharmacokinetics of carteolol in relation to renal function. Eur J Clin Pharmacol 29, 461–465 (1985). https://doi.org/10.1007/BF00613462
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DOI: https://doi.org/10.1007/BF00613462