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  • Title: Population pharmacokinetics of 2% topical dorzolamide in the aqueous humor of humans.
    Author: Schmitz K, Banditt P, Motschmann M, Meyer FP, Behrens-Baumann W.
    Journal: Invest Ophthalmol Vis Sci; 1999 Jun; 40(7):1621-4. PubMed ID: 10359348.
    Abstract:
    PURPOSE: To evaluate the concentration and kinetics of dorzolamide in the aqueous humor after its topical application. METHODS: Samples of aqueous humor were collected at the beginning of routine cataract surgery at defined intervals after topical application of a 2% solution of dorzolamide. After deep-frozen storage of the samples, drug extraction was achieved with a mixture of solvents. Quantification was carried out by high-performance liquid chromatography on a reversed-phase column. RESULTS: Peak concentrations of dorzolamide in aqueous humor were reached approximately 2 hours after application with 1000 ng/ml. Average values were approximately 1000 to 700 ng/ml after 4 to 6 hours and approximately 200 ng/ml after 12 hours. Mean half-life of absorption was 1.2 hours and for elimination 3.0 hours. CONCLUSIONS: Pharmacokinetics of dorzolamide in the aqueous humor of humans are in comparable dimensions as previously reported in experimental trials in pigmented rabbits. There is a clear linear absorption and elimination kinetic, which is demonstrated using the Bateman function. A better knowledge of the distribution and kinetics of dorzolamide will help to explain its reported effects on intraocular hemodynamics, distinct from its intraocular pressure lowering effect.
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