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Plasma levobunolol levels following topical administration with reference to systemic side effects
Summary
Topical levobunolol eye drops showed detectable plasma levels within 1 hour in normal volunteers. Systemic absorption was minimal, with slight cardiovascular changes noted only at the 1% concentration.
Area of Science:
- Ophthalmology
- Pharmacokinetics
- Cardiovascular Pharmacology
Background:
- Levobunolol is a beta-adrenergic receptor antagonist used topically for glaucoma treatment.
- Understanding systemic absorption and potential cardiovascular effects is crucial for patient safety.
Purpose of the Study:
- To determine plasma concentrations of levobunolol following topical ocular administration.
- To assess cardiovascular effects associated with different concentrations of topical levobunolol.
Main Methods:
- Normal volunteers received single topical ocular instillations of 0.5% or 1% levobunolol.
- Plasma levobunolol levels were measured at various time points post-instillation.
- Twice-daily instillations for one week were also studied, alongside cardiovascular monitoring.
Main Results:
- Plasma levobunolol was detected within 1 hour of topical application.
- Mean plasma levels ranged from 0.1-0.3 ng/ml (0.5% group) and 0.3-0.6 ng/ml (1% group).
- Minimal cardiovascular changes occurred with 0.5% levobunolol, while 1% caused decreased heart rate and blood pressure.
Conclusions:
- Topical levobunolol exhibits systemic absorption, with levels similar after acute and one-week twice-daily use.
- The 1% concentration of levobunolol may lead to clinically relevant cardiovascular effects.
- Careful monitoring is advised, especially with higher concentrations of topical levobunolol.