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Vitreous and aqueous concentrations of brimonidine following topical application of brimonidine tartrate 0.1% ophthalmic solution in humans.
J Ocul Pharmacol Ther. 2015 Jun; 31(5):282-5.JO

Abstract

PURPOSE

To determine the vitreous and aqueous concentrations of brimonidine after topical application of the ophthalmic solution 0.1%.

METHODS

The prospective observational case series included patients with an idiopathic epiretinal membrane or macular hole who were scheduled for a pars plana vitrectomy. Brimonidine tartrate ophthalmic solution 0.1% was topically administered twice daily for 1 week preoperatively. Vitreous and aqueous humor was collected before vitrectomy, and then, the brimonidine concentration was measured with liquid chromatography tandem spectrometry (LC/MS/MS).

RESULTS

Twenty-four patients (19 phakic eyes and 5 pseudophakic eyes) were enrolled. The mean concentrations in the aqueous humor and vitreous were 336.0 ± 276.2 and 4.8 ± 3.2 nM, respectively. A significant relationship was observed between the vitreous and aqueous samples (P = 0.034, R(2) = 0.22). Nineteen (79%) of the 24 eyes showed more than 2 nM of brimonidine tartrate concentration in the vitreous. In the phakic eyes, the mean concentration of brimonidine in the vitreous was 4.9 ± 3.3 nM, while the mean concentration in the pseudophakic eyes was 4.1 ± 2.4 nM, demonstrating no significant difference between pseudophakic and phakic eyes (P = 0.59).

CONCLUSIONS

After 1 week of dosing, in most of the patients who topically received brimonidine tartrate 0.1%, the concentration in the vitreous of the molecule was above 2 nM, which is known to activate neuroprotective α-2 receptors in animal retina. The drug penetration into the vitreous seems to be independent of lens status.

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Authors+Show Affiliations

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

No affiliation info available

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan. 3Department of Ophthalmology and Visual Sciences, Kyoto University Graduate School of Medicine, Kyoto, Japan.

1Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui-ken, Japan.

Pub Type(s)

Clinical Trial

Journal Article

Observational Study

Language

eng

PubMed ID

25918904

Citation

Takamura, Yoshihiro, et al. "Vitreous and Aqueous Concentrations of Brimonidine Following Topical Application of Brimonidine Tartrate 0.1% Ophthalmic Solution in Humans." Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics, vol. 31, no. 5, 2015, pp. 282-5.

Takamura Y, Tomomatsu T, Matsumura T, et al. Vitreous and aqueous concentrations of brimonidine following topical application of brimonidine tartrate 0.1% ophthalmic solution in humans. J Ocul Pharmacol Ther. 2015;31(5):282-5.

Takamura, Y., Tomomatsu, T., Matsumura, T., Takihara, Y., Kozai, S., Arimura, S., Yokota, S., & Inatani, M. (2015). Vitreous and aqueous concentrations of brimonidine following topical application of brimonidine tartrate 0.1% ophthalmic solution in humans. Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics, 31(5), 282-5. https://doi.org/10.1089/jop.2015.0003

Takamura Y, et al. Vitreous and Aqueous Concentrations of Brimonidine Following Topical Application of Brimonidine Tartrate 0.1% Ophthalmic Solution in Humans. J Ocul Pharmacol Ther. 2015;31(5):282-5. PubMed PMID: 25918904.

* Article titles in AMA citation format should be in sentence-case

TY - JOUR T1 - Vitreous and aqueous concentrations of brimonidine following topical application of brimonidine tartrate 0.1% ophthalmic solution in humans. AU - Takamura,Yoshihiro, AU - Tomomatsu,Takeshi, AU - Matsumura,Takehiro, AU - Takihara,Yuji, AU - Kozai,Seiko, AU - Arimura,Shogo, AU - Yokota,Satoshi, AU - Inatani,Masaru, Y1 - 2015/04/28/ PY - 2015/4/29/entrez PY - 2015/4/29/pubmed PY - 2016/2/26/medline SP - 282 EP - 5 JF - Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics JO - J Ocul Pharmacol Ther VL - 31 IS - 5 N2 - PURPOSE: To determine the vitreous and aqueous concentrations of brimonidine after topical application of the ophthalmic solution 0.1%. METHODS: The prospective observational case series included patients with an idiopathic epiretinal membrane or macular hole who were scheduled for a pars plana vitrectomy. Brimonidine tartrate ophthalmic solution 0.1% was topically administered twice daily for 1 week preoperatively. Vitreous and aqueous humor was collected before vitrectomy, and then, the brimonidine concentration was measured with liquid chromatography tandem spectrometry (LC/MS/MS). RESULTS: Twenty-four patients (19 phakic eyes and 5 pseudophakic eyes) were enrolled. The mean concentrations in the aqueous humor and vitreous were 336.0 ± 276.2 and 4.8 ± 3.2 nM, respectively. A significant relationship was observed between the vitreous and aqueous samples (P = 0.034, R(2) = 0.22). Nineteen (79%) of the 24 eyes showed more than 2 nM of brimonidine tartrate concentration in the vitreous. In the phakic eyes, the mean concentration of brimonidine in the vitreous was 4.9 ± 3.3 nM, while the mean concentration in the pseudophakic eyes was 4.1 ± 2.4 nM, demonstrating no significant difference between pseudophakic and phakic eyes (P = 0.59). CONCLUSIONS: After 1 week of dosing, in most of the patients who topically received brimonidine tartrate 0.1%, the concentration in the vitreous of the molecule was above 2 nM, which is known to activate neuroprotective α-2 receptors in animal retina. The drug penetration into the vitreous seems to be independent of lens status. SN - 1557-7732 UR - https://www.unboundmedicine.com/medline/citation/25918904/Vitreous_and_aqueous_concentrations_of_brimonidine_following_topical_application_of_brimonidine_tartrate_0_1_ophthalmic_solution_in_humans_ DB - PRIME DP - Unbound Medicine ER -