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Timolol kinetics in chronic renal insufficiency.

D T Lowenthal, J M Pitone, M B Affrime

    Clinical Pharmacology and Therapeutics
    |May 1, 1978
    PubMed
    Summary

    This study investigated oral timolol pharmacokinetics in individuals with normal, moderate, or end-stage renal insufficiency. Dosage adjustments are not indicated for moderate renal impairment, but caution is advised during dialysis due to potential hypotension and bradycardia.

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    Area of Science:

    • Pharmacology
    • Nephrology
    • Clinical Therapeutics

    Background:

    • Renal function significantly impacts drug pharmacokinetics.
    • Timolol is a beta-blocker used for various conditions.
    • Understanding timolol's behavior in renal impairment is crucial for safe dosing.

    Purpose of the Study:

    • To assess the pharmacokinetic profile of oral timolol (20 mg) in subjects with varying renal function.
    • To determine if dosage modification of timolol is necessary in patients with chronic renal insufficiency.
    • To evaluate the physiological response to timolol in different renal function groups.

    Main Methods:

    • A single-dose kinetic study of oral timolol (20 mg) was conducted.
    • Three volunteer groups were included: normal renal function, moderate chronic renal insufficiency (20-50 ml/min), and end-stage renal disease.

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  • Plasma concentrations, half-life, blood pressure, and pulse were monitored.

    • Main Results:

    • No statistically significant differences in timolol absorption or half-life were observed between normal and moderately impaired renal function groups.
    • Physiological responses (blood pressure, pulse) to timolol were similar between normal and MCRI groups, except between 12-24 hours.
    • Timolol administration during dialysis induced significant hypotension and bradycardia.

    Conclusions:

    • Dosage modification for oral timolol does not appear necessary for patients with moderate chronic renal insufficiency.
    • Caution is warranted when administering timolol to patients undergoing dialysis due to adverse cardiovascular effects.
    • Further research may be needed to fully elucidate timolol's behavior in end-stage renal disease.