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Absorption of ocular timolol

G Alvan, B Calissendorff, P Seideman

    Clinical Pharmacokinetics
    |January 1, 1980
    PubMed
    Summary
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    Topical timolol ophthalmic solution showed minimal systemic absorption in healthy volunteers and glaucoma patients. Detectable levels were not consistently found in plasma, but the drug was present in urine samples.

    Area of Science:

    • Ophthalmology
    • Pharmacokinetics
    • Drug Absorption

    Background:

    • Timolol is a beta-blocker commonly used to treat glaucoma.
    • Understanding systemic absorption is crucial for assessing potential side effects.

    Purpose of the Study:

    • To quantify the systemic absorption of timolol after topical ocular administration.
    • To evaluate timolol absorption in both healthy individuals and glaucoma patients.

    Main Methods:

    • Administered 0.5% timolol ophthalmic solution to healthy volunteers and glaucoma patients.
    • Collected overflow with paper tissue and analyzed plasma and urine for timolol levels.

    Main Results:

    • 12-88% of the topical dose was recovered from paper tissue.

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  • Plasma concentrations of timolol were very low (≤5 ng/ml) and often undetectable.
  • Timolol was detected in the urine of all participants, indicating systemic absorption.
  • Conclusions:

    • Topical ocular timolol exhibits limited systemic absorption.
    • Urine analysis confirms systemic absorption despite low plasma concentrations.
    • Further research may be needed to correlate absorption levels with clinical effects.