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局部应用于眼部的噻吗洛尔的全身吸收。

Systemic absorption of topically applied ocular timolol.

作者信息

Kaila T, Salminen L, Huupponen R

机构信息

Department of Pharmacology, University of Turku, Finland.

出版信息

J Ocul Pharmacol. 1985 Spring;1(1):79-83. doi: 10.1089/jop.1985.1.79.

DOI:10.1089/jop.1985.1.79
PMID:3880069
Abstract

Symptoms and findings arising from the systemic beta blockade caused by topical ocularly applied timolol appear shortly after drug application. We studied the systemic absorption of 20 microliters of 0.5% timolol instilled unilaterally in the lower conjunctival cul-de-sac in 6 volunteers. At 3 min one subject, at 5 min three and at 8 min all but one showed measurable (greater than or equal to 215 pg/ml) timolol concentrations in the plasma. The rapid systemic absorption of topically applied ocular timolol observed in our study is consistent with the rapid appearance of the cardiovascular and pulmonary side effects reported in connection with timolol eye drop therapy.

摘要

局部眼部应用噻吗洛尔引起的全身β受体阻滞症状和体征在用药后不久就会出现。我们研究了6名志愿者单侧下结膜穹窿部滴入20微升0.5%噻吗洛尔后的全身吸收情况。3分钟时1名受试者、5分钟时3名受试者以及8分钟时除1名受试者外的所有受试者血浆中噻吗洛尔浓度均可测(大于或等于215皮克/毫升)。我们研究中观察到的局部应用眼部噻吗洛尔的快速全身吸收与噻吗洛尔滴眼液治疗相关报道的心血管和肺部副作用的快速出现一致。

相似文献

1
Systemic absorption of topically applied ocular timolol.局部应用于眼部的噻吗洛尔的全身吸收。
J Ocul Pharmacol. 1985 Spring;1(1):79-83. doi: 10.1089/jop.1985.1.79.
2
Effects of epinephrine pretreatment and solution pH on ocular and systemic absorption of ocularly applied timolol in rabbits.肾上腺素预处理和溶液pH值对兔眼局部应用噻吗洛尔的眼部及全身吸收的影响。
J Pharm Sci. 1990 Aug;79(8):688-91. doi: 10.1002/jps.2600790808.
3
Relative effectiveness of prodrug and viscous solution approaches in maximizing the ratio of ocular to systemic absorption of topically applied timolol.前药和粘性溶液方法在最大化局部应用噻吗洛尔的眼内吸收与全身吸收比率方面的相对有效性。
Exp Eye Res. 1988 Jan;46(1):59-69. doi: 10.1016/s0014-4835(88)80093-9.
4
Light-dark variations in ocular timolol concentrations following topical solution instillation in the pigmented rabbit.色素兔局部滴注溶液后眼内噻吗洛尔浓度的明暗变化
Life Sci. 1992;51(26):2025-31. doi: 10.1016/0024-3205(92)90152-f.
5
Ocular drug interactions involving topically applied timolol in the pigmented rabbit.涉及色素沉着兔局部应用噻吗洛尔的眼部药物相互作用。
Curr Eye Res. 1991 Mar;10(3):231-40. doi: 10.3109/02713689109003445.
6
Improving the ocular to systemic ratio of topical timolol by varying the dosing time.通过改变给药时间提高局部用噻吗洛尔的眼内与全身药物浓度比。
Invest Ophthalmol Vis Sci. 1991 Sep;32(10):2790-8.
7
Improved ocular: systemic absorption ratio of timolol by viscous vehicle and phenylephrine.通过粘性赋形剂和去氧肾上腺素提高噻吗洛尔的眼部:全身吸收比率。
Invest Ophthalmol Vis Sci. 1990 Sep;31(9):1827-33.
8
Nasal and conjunctival contributions to the systemic absorption of topical timolol in the pigmented rabbit: implications in the design of strategies to maximize the ratio of ocular to systemic absorption.色素兔中鼻和结膜对局部应用噻吗洛尔全身吸收的影响:对优化眼内与全身吸收比例策略设计的启示
J Ocul Pharmacol. 1987 Summer;3(2):159-69. doi: 10.1089/jop.1987.3.159.
9
Systemic absorption pathways of topically applied beta adrenergic antagonists in the pigmented rabbit.局部应用的β肾上腺素能拮抗剂在有色家兔体内的全身吸收途径
Exp Eye Res. 1993 Sep;57(3):341-9. doi: 10.1006/exer.1993.1133.
10
Plasma kinetics and antagonist activity of topical ocular timolol in elderly patients.
Graefes Arch Clin Exp Ophthalmol. 1995 Mar;233(3):131-4. doi: 10.1007/BF00166604.

引用本文的文献

1
Repurposing Ophthalmologic Timolol for Dermatologic Use: Caveats and Historical Review of Adverse Events.将眼科噻吗洛尔重新用于皮肤科:不良反应的注意事项和历史回顾。
Am J Clin Dermatol. 2021 Jan;22(1):89-99. doi: 10.1007/s40257-020-00567-3. Epub 2020 Nov 25.
2
Neuropsychiatric Adverse Events from Topical Ophthalmic Timolol.局部用噻吗洛尔引起的神经精神不良事件。
Clin Med Res. 2019 Dec;17(3-4):90-96. doi: 10.3121/cmr.2019.1486. Epub 2019 Aug 28.
3
Plasma kinetics and antagonist activity of topical ocular timolol in elderly patients.
Graefes Arch Clin Exp Ophthalmol. 1995 Mar;233(3):131-4. doi: 10.1007/BF00166604.
4
Systemic reactions to ophthalmic drug preparations.眼科药物制剂的全身反应。
Med Toxicol Adverse Drug Exp. 1987 Jul-Aug;2(4):287-93. doi: 10.1007/BF03259870.
5
Prevalence of debrisoquine oxidation phenotypes in glaucoma patients.青光眼患者中异喹胍氧化表型的患病率。
Int Ophthalmol. 1989 Jan;13(1-2):91-3. doi: 10.1007/BF02028645.