Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study

Purpose: To evaluate the concentrations of brimonidine and brinzolamide in the vitreous and aqueous humor after instillation of a 0.1% brimonidine tartrate and 1% brinzolamide fixed-combination ophthalmic suspension. Methods: The present investigation involved patients with macular holes or idiopath...

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Main Authors: Yusuke Orii, Eriko Kunikane, Yutaka Yamada, Masakazu Morioka, Kentaro Iwasaki, Shogo Arimura, Akemi Mizuno, Masaru Inatani
Format: Article
Language:English
Published: MDPI AG 2023-06-01
Series:Journal of Clinical Medicine
Subjects:
Online Access:https://www.mdpi.com/2077-0383/12/13/4175
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author Yusuke Orii
Eriko Kunikane
Yutaka Yamada
Masakazu Morioka
Kentaro Iwasaki
Shogo Arimura
Akemi Mizuno
Masaru Inatani
author_facet Yusuke Orii
Eriko Kunikane
Yutaka Yamada
Masakazu Morioka
Kentaro Iwasaki
Shogo Arimura
Akemi Mizuno
Masaru Inatani
author_sort Yusuke Orii
collection DOAJ
description Purpose: To evaluate the concentrations of brimonidine and brinzolamide in the vitreous and aqueous humor after instillation of a 0.1% brimonidine tartrate and 1% brinzolamide fixed-combination ophthalmic suspension. Methods: The present investigation involved patients with macular holes or idiopathic epiretinal membranes who were planning to undergo vitrectomy. One week prior to surgery, the patients received twice-daily topical treatment with 0.1% brimonidine tartrate and 1% brinzolamide fixed-combination ophthalmic suspension. Before vitrectomy, vitreous and aqueous humor samples were collected, and the mean concentrations of brimonidine and brinzolamide were determined through liquid chromatography-tandem spectrometry. Results: Ten eyes (nine phakic and one pseudophakic eyes; 10 patients) were examined. The concentration of brimonidine in vitreous and aqueous humor samples was 5.02 ± 2.24 and 559 ± 670 nM, respectively. The concentration of brimonidine in the vitreous humor, which is needed to activate α2 receptors, was >2 nM in all patients. The concentration of brinzolamide was 8.96 ± 4.65 and 1100 ± 813 nM, respectively. However, there was no significant correlation between the concentrations of brimonidine in the vitreous and aqueous humor samples. Conclusions: Sufficient concentrations of brimonidine were detected in all vitreous samples. The dissociated correlation of the drug concentrations between aqueous and vitreous humors implies the possibility of another pathway to vitreous humor, different from the pathway to aqueous humor.
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spelling doaj.art-fd72971388034518a95deb04ec211fa22023-11-18T16:50:06ZengMDPI AGJournal of Clinical Medicine2077-03832023-06-011213417510.3390/jcm12134175Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional StudyYusuke Orii0Eriko Kunikane1Yutaka Yamada2Masakazu Morioka3Kentaro Iwasaki4Shogo Arimura5Akemi Mizuno6Masaru Inatani7Department of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanSenju Pharmaceutical Co., Ltd., Osaka 541-0048, JapanDepartment of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanDepartment of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanDepartment of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanDepartment of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanSenju Pharmaceutical Co., Ltd., Osaka 541-0048, JapanDepartment of Ophthalmology, Faculty of Medical Sciences, University of Fukui, Fukui 910-1193, JapanPurpose: To evaluate the concentrations of brimonidine and brinzolamide in the vitreous and aqueous humor after instillation of a 0.1% brimonidine tartrate and 1% brinzolamide fixed-combination ophthalmic suspension. Methods: The present investigation involved patients with macular holes or idiopathic epiretinal membranes who were planning to undergo vitrectomy. One week prior to surgery, the patients received twice-daily topical treatment with 0.1% brimonidine tartrate and 1% brinzolamide fixed-combination ophthalmic suspension. Before vitrectomy, vitreous and aqueous humor samples were collected, and the mean concentrations of brimonidine and brinzolamide were determined through liquid chromatography-tandem spectrometry. Results: Ten eyes (nine phakic and one pseudophakic eyes; 10 patients) were examined. The concentration of brimonidine in vitreous and aqueous humor samples was 5.02 ± 2.24 and 559 ± 670 nM, respectively. The concentration of brimonidine in the vitreous humor, which is needed to activate α2 receptors, was >2 nM in all patients. The concentration of brinzolamide was 8.96 ± 4.65 and 1100 ± 813 nM, respectively. However, there was no significant correlation between the concentrations of brimonidine in the vitreous and aqueous humor samples. Conclusions: Sufficient concentrations of brimonidine were detected in all vitreous samples. The dissociated correlation of the drug concentrations between aqueous and vitreous humors implies the possibility of another pathway to vitreous humor, different from the pathway to aqueous humor.https://www.mdpi.com/2077-0383/12/13/4175brimonidinebrinzolamidefixed-combination ophthalmic suspensionvitreous humorsaqueous humors
spellingShingle Yusuke Orii
Eriko Kunikane
Yutaka Yamada
Masakazu Morioka
Kentaro Iwasaki
Shogo Arimura
Akemi Mizuno
Masaru Inatani
Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
Journal of Clinical Medicine
brimonidine
brinzolamide
fixed-combination ophthalmic suspension
vitreous humors
aqueous humors
title Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
title_full Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
title_fullStr Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
title_full_unstemmed Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
title_short Ocular Distribution of Brimonidine and Brinzolamide after Topical Instillation of a 0.1% Brimonidine Tartrate and 1% Brinzolamide Fixed-Combination Ophthalmic Suspension: An Interventional Study
title_sort ocular distribution of brimonidine and brinzolamide after topical instillation of a 0 1 brimonidine tartrate and 1 brinzolamide fixed combination ophthalmic suspension an interventional study
topic brimonidine
brinzolamide
fixed-combination ophthalmic suspension
vitreous humors
aqueous humors
url https://www.mdpi.com/2077-0383/12/13/4175
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