• Title/Summary/Keyword: betaxolol

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Prophylactic effect of topical betaxolol and dorzolamide on the fellow eye in unilateral canine primary angle closure glaucoma: 60 cases (2016.1-2021.5)

  • Ahn, Junyeong;Kang, Seonmi;Shim, Jaeho;Jeong, Youngseok;Lee, Songhui;Lee, Eunji;Seo, Kangmoon
    • Korean Journal of Veterinary Research
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    • v.62 no.3
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    • pp.26.1-26.7
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    • 2022
  • This study was aimed to evaluate the prophylactic anti-glaucoma effect of topical 5% betaxolol (BTX) and 2% dorzolamide (DRZ) on the second eye in dogs with unilateral primary angle closure glaucoma (PACG). Medical records of 60 dogs with unilateral PACG who received prophylactic anti-glaucoma eyedrops in the second eye, from 2016 to 2021, were reviewed. The prophylactic effects of BTX were maintained on 28/60 (46.7%) eyes until last visit and BTX failure was observed on median 510 (range, 53-1,927) days in 32/60 (53.3%) eyes. After DRZ instillation in BTX failure eyes, the prophylactic effects were extended at median 610 (range, 157-2,270) days in 21/32 (65.6%) eyes. DRZ failure eyes (17/21, 81.0%) eyes required chemical ablation or surgical intervention due to uncontrolled intraocular pressure. The duration of prophylactic effects was decreased with aging (R2 = 0.334, p = 0.006). The predominant breeds were Shih-Tzu (41.9%) and American Cocker Spaniel (30.6%) with no significant differences in survival curves (p = 0.210). The average prophylactic effects of BTX persisted more than 1.5 year and could be selected the first prophylactic eye drop in unilateral PACG. Also, early surgical intervention should be considered in prophylactic medications failure cases.

Chiral Separation of $\beta$-Blockers after Derivatization with (-)-$\alpa$- Methoxy-$\alpa$-(trifuoromethyl)phenylacetyl Chloride by Gas Chromatography

  • Kim, Kyeong-Ho;Lee, Joo-Hyun;Ko, Mi-Young;Hong, Seon-Pyo;Youm, Jeong-Rok
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.402-406
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    • 2001
  • Gas chromatographic method was investigated for the chiral separation of several $\beta$-blockeros(atenolol, betaxolol, bisoprolol, metoprolol and pindolol) using (-)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride as a chiral derivatizing agent for amino group. Prior to N-acylation, hydroxyl group was converted into O-silyl ethers by react with N-methyl-H-(taimethylsilyl)trifluoroacetamide. The reaction was selective and rapid and the diasteromeric derivatives were well separated by capillary gas chromatography. (R)-isomers were eluted faster than (S)-isomers when (-)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride was used as the chiral derivatizing agent. But in the opposite sequence when (+)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride was used. No racemization was found during the reaction.

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Chiral Separation of $\beta$-Blockers after Derivatization with (-)-Menthyl chloroformate by Reversed-Phase High Performance Liquid Chromatography

  • Kim, Kyeong-Ho;Choi, Pok-Wha;Hong, Seon-Pyo;Kim, Hyun-Ju
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.608-613
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    • 1999
  • Optimum conditions of chiral derivatization reaction of $\beta$-blockers (acebutolol, arotinolol, betaxolol, bisoprolol, celiprolol, metoprolol and pindolol) with (-)-menthyl chloroformate were investigated for the resolution by HPLC. With more than 30 times molar excess of (-)-methyl chloroformate chiral derivatization reactions were completed within one hour at room temperature except arotinolol and celiprolol. Diastereomeric derivatives of $\beta$-blockers were well resolved on the ODS column using acetonitrile-methanol-water as a mobile phase.

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Studies on Drug Absorption Characteristics for Development of Ocular Dosage Forms: Ocular and Systemic Absorption of Topically Applied ${\beta}-Blockers$ in the Pigmented Rabbit

  • Lee, Yong-Hee
    • Journal of Pharmaceutical Investigation
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    • v.24 no.3
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    • pp.59-66
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    • 1994
  • The objective of this study was to determine the influence of drug lipophilicity on the extent of ocular and systemic absorption following topical solution instillation in the pigmented rabbit. ${\beta}-Blockers$ of various lipophilicity were chosen as model drugs, $25\;{\mu}l$ of a 15 mM drug solution in isotonic pH 7.4 buffer was instilled, and ocular tissue and plasma drug concentrations were monitored. Ocular absorption was apparently increased in all eye tissues, but non-corneal absorption ratio was decreased by increasing of drug lipophilicity. Systemic bioavailability was ranged from 61% for atenolol to 100% for timolol, and at least 50% of the systemically absorbed drug reached the blood stream from the nasal mucosa. Occluding the nasolacrimal duct for 5 min reduced the extent of systemic absorption of timolol and levobunolol, but did not do so for atenolol and betaxolol. Taken together, the ocular absorption of topically applied ophthalmic drugs would be modest for lipophilic drugs. By contrast, the systemic bioavailability would be modest for drugs at the extremes of lipophilicity, and the nasal contribution to systemically absorbed drug diminished with increasing of drug lipophilicity.

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$\beta$-차단제의 약효검색범

  • 안형수
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.47-47
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    • 1992
  • $\beta$수용체에 대한 차단약으로 propranolol이 1964년에 도입된 후, 현재까지 수십여종의 $\beta$-차단약이 개발되었다. 그중 특이 $\beta$1 수용체에 대해 선택적인 억제효과를 지닌 atenolol, metoprolol, betaxolol, celiprolol 및 최근에 bisoprolol 등이 개발되어 임상적으로 부정맥, 협심증, 고혈압의 치료에 사용되고 있다. 그 작용기전으로는 심박출량의 감소, renin 유리억제, 중추억제효과 등이 제시되고 있으나, 이들의 약효검색은 주로 $\beta$1수용체가 많이 존재하는 심장에 대한 억제효과를 중심으로 실시한다. 즉, SHR 및 개를 사용한 생체실험과 심장, 심방 ($\beta$1) 및 기완지, 혈관($\beta$2)을 이용한 적출장기실험을 통하여 isoproterenol에 대한 억제효과를 용량반응 곡선으로 그리고, Van rossum 법에 의해 pA$_2$ 치를 구하여 $\beta$-차단제의 효력을 평가한다. 특히, pA$_2$ 치가 클수록 $\beta$-차단제의 효력이 큰 약물이다. 또한 수용체 결합실험으로 소의 심실 세포막을 분리하여 $^3$H-DHA 와의 결합실험을 통해 해리항수(Kd) 를 측정하고, 이어서 $^3$H-DHA의 일정농도와 함께 미지의 $\beta$-차단제를 여러 농도로 변화시켜 가하여 치환곡선을 작성한다. 여기에서 얻은 치환약의 $IC_{50}$/ 치로부터 치환약의 해리항수(Ki)를 산출한다. 이때 약물과 수용체의 친화력은 해리항수의 역수이므로 해리항수가 적을수록 $\beta$ 수용체에 대한 친화력이 큰 약물이다. 시사되었으며, 이 조직에서 또한 5-$HT_2$와 5-$HT_3$ 수용체의 존재를 확인하고 각각의 기능을 분명히 했다.가 수월하게 하였고 메모리를 동적으로 관리할 수 있게 하였다. 또한 기존의 smpl에 디버깅용 함수 및 설비(facility) 제어용 함수를 추가하여 시뮬레이션 프로그램 작성을 용이하게 하였다. 예를 들면 who_server(), who_queue(), pop_Q(), push_Q(), pop_server(), push_server(), we(), wf(), printfct() 같은 함수들이다. 또한 동시에 발생되는 사건들의 순서를 조종하기 위해, 동시에 발생할 수 있는 각각의 사건에 우선순위를 두어 이 우선 순위에 의하여 사건 리스트(event list)에서 자동적으로 사건들의 순서가 결정되도록 확장하였으며, 설비 제어방식에 있어서도 FIFO, LIFO, 우선 순위 방식등을 선택할 수 있도록 확장하였다. SIMPLE는 자료구조 및 프로그램이 공개되어 있으므로 프로그래머가 원하는 기능을 쉽게 추가할 수 있는 장점도 있다. 아울러 SMPLE에서 새로이 추가된 자료구조와 함수 및 설비제어 방식등을 활용하여 실제 중형급 시스템에 대한 시뮬레이션 구현과 시스템 분석의 예를 보인다._3$", chain segment, with the activation energy of carriers from the shallow trap with 0.4[eV], in he amorphous regions.의 증발산율은 우기의 기상자료를 이용하여 구한 결과 0.05 - 0.10 mm/hr 의 범위로서 이로 인한 강우손실량은 큰 의미가 없음을 알았다.재발이 나타난 3례의 환자를 제외한 9례 (75%)에서는 현재까지 재발소견을 보이지 않고 있다. 이러한 결과는 다른 보고자들과 유사한 결과를 보이고 있지만 아직까지 증례가 많지 않기 때문에 생존율을 얻기에는 미흡한 점이

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