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Pharmacokinetics of carteolol in patients with impaired renal function
Abstract:
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 degrees 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.
Insights
Carteolol dosage requires adjustment in renal dysfunction. This study found carteolol levels correlate with kidney function markers, indicating dose individualization is crucial for patient safety.
Area of Science:
- Pharmacology
- Nephrology
- Clinical Pharmacy
Background:
- Renal impairment can significantly alter drug pharmacokinetics.
- Carteolol is a beta-blocker used for various conditions, but its renal excretion profile requires clarification.
Purpose of the Study:
- To investigate the pharmacokinetics of carteolol in patients with varying degrees of renal impairment.
- To establish guidelines for appropriate carteolol dosing in renal dysfunction.
Main Methods:
- Studied 15 patients with renal impairment receiving carteolol hydrochloride (5-20 mg/day) for 2-45 months.
- Measured plasma concentrations and urinary excretion of carteolol.
- Correlated drug levels and excretion with serum creatinine and creatinine clearance.
Main Results:
- Plasma carteolol levels showed strong linear correlation with serum creatinine (r=0.87) and inverse correlation with creatinine clearance (r=0.82).
- Urinary carteolol excretion correlated with creatinine clearance (r=0.79), indicating active tubular secretion.
- Fractional renal excretion exceeded 100%, confirming active secretion even in renal failure.
Conclusions:
- Carteolol pharmacokinetics are significantly influenced by renal function.
- Dosing of carteolol should be individualized based on the degree of renal impairment.
- Active tubular secretion of carteolol necessitates careful dose adjustment in patients with kidney disease.