164 results on '"Carteolol"'
Search Results
2. A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride
- Author
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Yoshiko Hashikawa, Yuki Kato, Hirokazu Kaji, Toshiaki Abe, and Nobuhiro Nagai
- Subjects
Controlled release ,poly(ethyleneglycol) dimethacrylate ,Intraocular drug distribution ,Carteolol ,Transscleral administration ,Science (General) ,Q1-390 ,Social sciences (General) ,H1-99 - Abstract
The objectives of this study were to develop a sustained-release device for carteolol hydrochloride (CH) and investigate any potential difference in the intraocular distribution of this agent between the transscleral administration of the device and treatment with eyedrops. The device was formulated with photocurable resin, poly (ethyleneglycol) dimethacrylate, to fit within the curve of the rabbit eyeball. In vitro study showed that CH was released in a sustained-release manner for 2 weeks. The concentration of CH in the retina, choroid/retinal pigment epithelium, sclera, iris, and aqueous humor was determined by high-performance liquid chromatography. Transscleral administration was able to deliver CH to the posterior segment (i.e., retina and choroid/retinal pigment epithelium) rather than the anterior segment (i.e., aqueous humor), while eyedrops delivered CH only to the anterior segment. Transscleral administration could deliver CH to aqueous humor at half the concentration versus treatment with eyedrops and reduced intraocular pressure (IOP) at 1 day after implantation; however, the IOP-lowering effect was not sustained thereafter. In conclusion, transscleral drug delivery may be a useful method for the reduction of IOP. Notably, the aqueous concentration must be equal to that delivered by the eyedrops, and this approach might be preferable for drug delivery to the posterior segment of the eye.
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- 2023
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3. Update on Treatment of Infantile Hemangiomas: What’s New in the Last Five Years?
- Author
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Laura Macca, Domenica Altavilla, Luca Di Bartolomeo, Natasha Irrera, Francesco Borgia, Federica Li Pomi, Federico Vaccaro, Violetta Squadrito, Francesco Squadrito, and Mario Vaccaro
- Subjects
infantile hemangioma ,steroids ,propranolol ,timolol ,carteolol ,itraconazole ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Among benign vascular tumors of infancy, hemangiomas are the commonest, affecting approximately 5–10% of one-year-old children. They are derived from a benign proliferation of vascular endothelial cells (VECs) in the mesoderm and may arise anywhere on the body around 1–2 weeks after birth. Infantile hemangiomas (IHs) are characterized by an early proliferative phase in the first year followed by a spontaneous progressive regression within the following 5 years or longer. IH prevalence is estimated to be 5%–10% in one-year-old children and commonly affects female, Caucasian and low-birth weight infants. Although most of them spontaneously regress, approximately 10% requires treatment to prevent complications due to the site of occurrence such as bleeding, ulceration, cosmetically disfigurement, functional impairment, or life-threatening complications. For over 30 years, steroids have represented the first-line treatment for IHs, but recently topical or systemic β-blockers are increasingly being used and recognized as effective and safe. A search for “Cutaneous infantile hemangioma” [All Fields] AND “Treatment” [All Fields] was performed by using PubMed and EMBASE databases. Treatment of IHs with labeled drugs, such as oral propranolol, but also with off-label drugs, such as topical β-blockers, including topical timolol and carteolol, steroids, itraconazole or sirolimus, with a focus on formulations types and adverse events were described in our review. We also discussed the benefits of pulsed dye laser and the treatment of IHs with involvement of central nervous system, namely the PHACE and LUMBAR syndrome.
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- 2022
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4. Retinal Vessel Density Changes on Optical Coherence Tomography Angiography and Predictive Factors in Normal-Tension Glaucoma Treated with Topical Beta-Blocker.
- Author
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Yun-Hsuan Lin, Shih-Ming Huang, Lan-Hsin Chuang, and Lung-Chien Chen
- Subjects
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OPTICAL coherence tomography , *OPACITY (Optics) , *RETINAL blood vessels , *ANGIOGRAPHY , *GLAUCOMA - Abstract
(1) Background: Topical antiglaucoma medications may alter the microcirculation in the optic nerve head. We aimed to evaluate the changes in retinal vessel density (VD) on optical coherence tomography angiography (OCTA) in patients with newly diagnosed normal-tension glaucoma (NTG) treated with a topical beta-blocker. (2) Methods: This study included 80 patients diagnosed with NTG not using systemic medication, who received topical carteolol treatment between December 2019 and November 2020. We studied the changes in the OCTA VD/signal strength index (SSI) after the 6-month treatment period and determined the predictive factors affecting the changes in VD/SSI. (3) Results: After the 6-month treatment period, the peripapillary VD increased in 40 patients but decreased in the other 40 patients. The univariate and multivariate analyses revealed that old age and hypertension were significant factors associated with a VD/SSI decrease after carteolol treatment. Moreover, high baseline peripapillary, superficial, and deep macular VDs were significantly associated with the VD decrease after carteolol treatment. (4) Conclusions: Carteolol treatment could increase or decrease the VD in patients with NTG. The baseline VD, age, and hypertension could affect these VD changes. Patients with NTG and higher baseline peripapillary or macular VD, older age, and hypertension are more likely to have a decreased VD after carteolol treatment. [ABSTRACT FROM AUTHOR]
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- 2021
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5. Efficacy and Safety Study of OPC-1085EL Ophthalmic Solution in Subjects With Glaucoma or Ocular Hypertension
- Published
- 2015
6. Efficacy and Safety Study of OPC-1085EL Ophthalmic Solution in Subjects With Glaucoma or Ocular Hypertension
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- 2015
7. Pharmacokinetic Study of OPC-1085EL Ophthalmic Solution in Healthy Male Adult Volunteers
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- 2015
8. Dose- and Time-Dependent Cytotoxicity of Carteolol in Corneal Endothelial Cells and the Underlying Mechanisms
- Author
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Wen Su, Jun Zhao, and Ting-Jun Fan
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carteolol ,cytotoxicity ,necroptosis ,apoptosis ,human corneal endothelial cells ,feline corneal endothelial cells ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Carteolol is a non-selective β-adrenoceptor antagonist used for the treatment of glaucoma, and its abuse might be cytotoxic to the cornea. However, its cytotoxicity and underlying mechanisms need to be elucidated. Herein, we used an in vivo model of feline corneas and an in vitro model of human corneal endothelial cells (HCECs), respectively. In vivo results displayed that 2% carteolol (clinical dosage) could induce monolayer density decline and breaking away of feline corneal endothelial (FCE) cells. An in vitro model of HCECs that were treated dose-dependently (0.015625–2%) with carteolol for 2–28 h, resulted in morphological abnormalities, declining in cell viability and elevating plasma membrane (PM) permeability in a dose- and time- dependent manner. High-dose (0.5–2%) carteolol treatment induced necrotic characteristics with uneven distribution of chromatin, marginalization and dispersed DNA degradation, inactivated caspase-2/-8, and increased RIPK1, RIPK3, MLKL, and pMLKL expression. The results suggested that high-dose carteolol could induce necroptosis via the RIPK/MLKL pathway. While low-dose (0.015625–0.25%) carteolol induced apoptotic characteristics with chromatin condensation, typical intranucleosomal DNA laddering patterns, G1 cell-cycle arrest, phosphatidylserine (PS) externalization, and apoptotic body formation in HCECs. Meanwhile, 0.25% carteolol treatment resulted in activated caspase-2, -3, -8, and -9, downregulation of Bcl-2 and Bcl-xL, upregulation of Bax and Bad, ΔΨm disruption, and release of cytoplasmic cytochrome c (Cyt.c) and AIF into the cytoplasm. These observations suggested that low-dose carteolol could induce apoptosis via a caspase activated and mitochondrial-dependent pathway. These results suggested that carteolol should be used carefully, as low as 0.015625% cartelol caused apoptotic cell death in HCECs in vitro.
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- 2020
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9. Dose- and Time-Dependent Cytotoxicity of Carteolol in Corneal Endothelial Cells and the Underlying Mechanisms.
- Author
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Su, Wen, Zhao, Jun, and Fan, Ting-Jun
- Subjects
ENDOTHELIAL cells ,CELL death ,APOPTOTIC bodies ,CELL survival ,CELL membranes ,CELL cycle ,CYTOCHROME c - Abstract
Carteolol is a non-selective β-adrenoceptor antagonist used for the treatment of glaucoma, and its abuse might be cytotoxic to the cornea. However, its cytotoxicity and underlying mechanisms need to be elucidated. Herein, we used an in vivo model of feline corneas and an in vitro model of human corneal endothelial cells (HCECs), respectively. In vivo results displayed that 2% carteolol (clinical dosage) could induce monolayer density decline and breaking away of feline corneal endothelial (FCE) cells. An in vitro model of HCECs that were treated dose-dependently (0.015625–2%) with carteolol for 2–28 h, resulted in morphological abnormalities, declining in cell viability and elevating plasma membrane (PM) permeability in a dose- and time- dependent manner. High-dose (0.5–2%) carteolol treatment induced necrotic characteristics with uneven distribution of chromatin, marginalization and dispersed DNA degradation, inactivated caspase-2/-8, and increased RIPK1, RIPK3, MLKL, and pMLKL expression. The results suggested that high-dose carteolol could induce necroptosis via the RIPK/MLKL pathway. While low-dose (0.015625–0.25%) carteolol induced apoptotic characteristics with chromatin condensation, typical intranucleosomal DNA laddering patterns, G
1 cell-cycle arrest, phosphatidylserine (PS) externalization, and apoptotic body formation in HCECs. Meanwhile, 0.25% carteolol treatment resulted in activated caspase-2, -3, -8, and -9, downregulation of Bcl-2 and Bcl-xL, upregulation of Bax and Bad, ΔΨm disruption, and release of cytoplasmic cytochrome c (Cyt.c) and AIF into the cytoplasm. These observations suggested that low-dose carteolol could induce apoptosis via a caspase activated and mitochondrial-dependent pathway. These results suggested that carteolol should be used carefully, as low as 0.015625% cartelol caused apoptotic cell death in HCECs in vitro. [ABSTRACT FROM AUTHOR]- Published
- 2020
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10. A Study to Evaluate Efficacy and Safety Effects Using Mikelan® LA Ophthalmic Solution (OS) 2% Versus Timoptol® XE Ophthalmic Solution (OS) 0.5% in Ocular Hypertension Patients
- Published
- 2011
11. Enhancement in Corneal Permeability of Dissolved Carteolol by Its Combination with Magnesium Hydroxide Nanoparticles.
- Author
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Nagai, Noriaki, Yamaoka, Sakie, Fukuoka, Yuya, Ishii, Miyu, Otake, Hiroko, Kanai, Kazutaka, Okamoto, Norio, and Shimomura, Yoshikazu
- Subjects
- *
MAGNESIUM hydroxide , *NANOPARTICLES , *INTRAOCULAR pressure , *LABORATORY rabbits , *CORNEA - Abstract
We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol. The carteolol was solved in saline containing additives (0.5% methylcellulose, 0.001% benzalkonium chloride, 0.5% mannitol; CRT-solution). MH nanoparticles were prepared by a bead mill method with additives. Then carteolol/MH microparticle and carteolol/MH nanoparticle fixed combinations (mCMFC and nCMFC) were prepared by mixing the CRT-solution and MH particles. The transcorneal penetration and IOP-reducing effect of carteolol was evaluated in rabbits. The mean particle size of mCMFC was 7.2 μm, and the particle size was reduced to 73.5-113.5 nm by the bead mill treatment. The MH particles in nCMFC remained in the nano size range for 8 days after preparation, and the amounts of lacrimal fluid and corneal damage were unchanged by repetitive instillation of nCMFC (twice a day for 4 weeks). The transcorneal penetration of carteolol was enhanced by the combination with MH nanoparticles, and the IOP-reducing effect of nCMFC was significantly higher than that of CRT-solution or mCMFC. In conclusion, we designed nCMFC, and showed that the high levels of dissolved carteolol can be delivered into the aqueous humor by the instillation of nCMFC. Combination with MH nanoparticles may achieve an enhancement of corneal penetration for water-soluble drugs. These findings provide significant information that can be used to design further studies aimed at developing anti-glaucoma eye drugs. [ABSTRACT FROM AUTHOR]
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- 2018
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12. Latanoprost eye drops induce conjunctival lymphatic vessel development
- Author
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Cheng-Juan Yin, Kai Ma, Zhen-Yong Zhang, and Qing-Song Li
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medicine.medical_specialty ,genetic structures ,Mrna expression ,Immunofluorescence ,conjunctival lymphatic vessels ,chemistry.chemical_compound ,Western blot ,Ophthalmology ,medicine ,Lymphatic vessel ,Carteolol ,Latanoprost ,medicine.diagnostic_test ,business.industry ,RE1-994 ,eye diseases ,Lymphangiogenesis ,lymphangiogenesis ,Basic Research ,Lymphatic system ,medicine.anatomical_structure ,chemistry ,latanoprost ,sense organs ,business ,medicine.drug - Abstract
AIM: To investigate the effect of latanoprost eye drops on the conjunctival lymphatics. METHODS: Twenty-four healthy New Zealand White rabbits weighing 1.5 to 2.0 kg were randomly divided into three groups: latanoprost group (n=8) administered with latanoprost eye drops once a day for 2mo, carteolol group (n=8) administered with carteolol eye drops once a day for 2mo, and control group (n=8) without any treatment. The conjunctival tissues in the three groups were extracted to investigate the expression levels of 5’-nucleotidase (5’-Nase) by Western blot, reverse transcription-polymerase chain reaction (RT-PCR), and immunofluorescence staining, respectively. RESULTS: The protein expression level of 5’-Nase was significantly higher in latanoprost group than carteolol group (F=231.175, P0.05). The mRNA expression level of 5’-Nase in the latanoprost group was also significantly higher than carteolol group (F=71.169 P
- Published
- 2021
13. Carteolol triggers senescence via activation of β-arrestin–ERK–NOX4–ROS pathway in human corneal endothelial cells in vitro.
- Author
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Jiang, Guo-Jian, You, Xin-Guo, and Fan, Ting-Jun
- Subjects
- *
POLY ADP ribose , *ADP-ribosylation , *DNA repair , *ENDOTHELIAL cells , *AGING , *DNA ligases , *CORNEA - Abstract
Carteolol is a commonly-used topical medication for primary open-angle glaucoma. However, long-term and frequent ocular application of carteolol entails its residuals at low concentration in the aqueous humor for a long duration and may exert latent toxicity in the human corneal endothelial cells (HCEnCs). Here, we treated the HCEnCs in vitro with 0.0117% carteolol for 10 days. Thereafter, we removed the cartelolol and normally cultured the cells for 25 days to investigate the chronical toxicity of carteolol and the underlying mechanism. The results exhibited that 0.0117% carteolol induces senescent features in the HCEnCs, such as increased senescence-associated β-galactosidase positive rates, enlarged relative cell area and upregulated p16INK4A and senescence-associated secretory phenotypes, including IL-1α, TGF-β1, IL-10, TNF-α, CCL-27, IL-6 and IL-8, as well as decreased Lamin B1 expression and cell viability and proliferation. Thereby, further exploration demonstrated that the carteolol activates β-arrestin–ERK–NOX4 pathway to increase reactive oxygen species (ROS) production that imposes oxidative stress on energetic metabolism causing a vicious cycle between declining ATP and increasing ROS production and downregulation of NAD+ resulting in metabolic disturbance-mediated senescence of the HCEnCs. The excess ROS also impair DNA to activate the DNA damage response (DDR) pathway of ATM–p53–p21WAF1/CIP1 with diminished poly(ADP-Ribose) polymerase (PARP) 1, a NAD+-dependent enzyme for DNA damage repair, resulting in cell cycle arrest and subsequent DDR-mediated senescence. Taken together, carteolol induces excess ROS to trigger HCEnC senescence via metabolic disturbance and DDR pathway. [Display omitted] • 0.0117% carteolol induces senescence of human corneal endothelial cells (HCEnCs). • The carteolol activates β-arrestin–ERK–NOX4 axis to elevate ROS production. • The elevated ROS impair DNA and impose oxidative stress (OS) on energy metabolism. • The DNA damage elicits senescence of the HCEnCs via DNA damage response pathway. • The OS provokes metabolic disturbance resulting in senescence of the HCEnCs. [ABSTRACT FROM AUTHOR]
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- 2023
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14. Development and validation of UPLC/ESI-Q-TOF-MS for carteolol in aqueous humour: Stability, stress degradation and application in pharmacokinetics of nanoformulation
- Author
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Ameeduzzafar, Javed Ali, and Asgar Ali
- Subjects
Glaucoma ,Carteolol ,UPLC/ESI-Q-TOF-MS ,Chitosan nanoparticles ,Stress degradation ,Pharmacokinetics ,Chemistry ,QD1-999 - Abstract
Carteolol (CRT) is currently under development as a potential therapeutic agent for the treatment of open angle glaucoma. The purpose of the present work is to develop and validate a stability indicating assay method and its application to estimate CRT in aqueous humour and study the pharmacokinetic parameters. An ultra performance liquid chromatographic tandem mass spectroscopy (UPLC–MS/MS) method was developed and validated for the quantitative determination of CRT in rabbit aqueous humour, using propranolol as the internal standard (I.S.). Aqueous humour samples were prepared by a simple liquid–liquid extraction technique (LLE). The analyte and internal standard were separated by an Acquity UPLC BEH C18 (100.0 × 2.1 mm; 1.7 μm) column with a mobile phase of acetonitrile – 2 mM (milli mole) ammonium acetate (90/10, v/v) over 3 min of retention time. Detection was based on the multiple reactions monitoring with the precursor-to-product ion transitions m/z 293.2 → 237.12 for CRT and m/z 260.09 → 183.04 for I.S. The method was validated according to FDA guidelines on the bio-analytical method validation. The method developed was linear (r2 = 0.999) over the concentration range of 1–1000 ng/mL. The selectivity, sensitivity, linearity, accuracy, precision, extraction recovery, and stability were within the acceptable ranges. Forced degradation studies were performed on bulk sample of CRT as per ICH prescribed stress conditions, such as acid, base, oxidative and photolytic to show the forced of the method. Significant degradation was observed during basic stress condition. The pharmacokinetic study of CRT solution and nanoparticles in aqueous humour of rabbit eye was performed and results showed that CRT nanoparticles enhance the ocular bioavailability by 5.61-fold as compared to CRT-solution.
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- 2017
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15. Short-term efficacy of latanoprostene bunod for the treatment of open-angle glaucoma and ocular hypertension: a systematic literature review and a network meta-analysis
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Martin Barbeau, Paul Harasymowycz, Catherine Royer, Katherine Jobin-Gervais, Jean Lachaine, Amy Xianying Cui, Catherine Beauchemin, and K. Mathurin
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medicine.medical_specialty ,Network Meta-Analysis ,Brinzolamide ,Timolol ,03 medical and health sciences ,Cellular and Molecular Neuroscience ,chemistry.chemical_compound ,Travoprost ,0302 clinical medicine ,Dorzolamide ,Ophthalmology ,medicine ,Humans ,030212 general & internal medicine ,Latanoprost ,Carteolol ,Antihypertensive Agents ,Intraocular Pressure ,Prostaglandins A ,Bimatoprost ,business.industry ,Tafluprost ,Bayes Theorem ,Amides ,Sensory Systems ,Betaxolol ,Unoprostone ,chemistry ,Brimonidine Tartrate ,Prostaglandins F, Synthetic ,030221 ophthalmology & optometry ,Ocular Hypertension ,business ,Glaucoma, Open-Angle ,medicine.drug - Abstract
Background/aimsTo assess the comparative efficacy of latanoprostene bunod (LBN), a novel prostaglandin analogue (PGA), to other medications for open-angle glaucoma and ocular hypertension on lowering intraocular pressure (IOP).MethodsA systematic literature review adapted from the Li et al (Ophthalmology, 2016) study was conducted. Medline, Embase and PubMed were searched for randomised controlled trials published between 1 January 2014 and 19 March 2020. Studies had to report IOP reduction after 3 months for at least two different treatments among placebo, PGAs (bimatoprost 0.01%, bimatoprost 0.03%, latanoprost, LBN, tafluprost, unoprostone) or apraclonidine, betaxolol, brimonidine, brinzolamide, carteolol, dorzolamide, levobunolol, timolol, travoprost. A Bayesian network meta-analysis was performed to provide the relative effect in terms of mean difference (95% credible interval) of IOP reduction and ranking probabilities. Surface under the cumulative ranking curve (SUCRA) was generated.ResultsA total of 106 trials were included with data for 18 523 participants. LBN was significantly more effective than unoprostone (−3.45 (−4.77 to −2.12)). Although relative effect was not significative, compared with other PGAs, LBN numerically outperformed latanoprost (−0.70 (−1.83 to 0.43)) and tafluoprost (−0.41 (−1.87 to 1.07)), was similar to bimatoprost 0.01% (-0.02(−1.59 to 1.55)) and was slightly disadvantaged by bimatoprost 0.03% (−0.17 (−1.42 to 1.07)). LBN was significantly more efficient than the beta-blockers apraclonidine, betaxolol, brimonidine, brinzolamide, carteolol, dorzolamide and timolol. According to SUCRA, LBN was ranked second after bimatoprost 0.03%, followed by bimatoprost 0.01%.ConclusionLBN was significantly more effective than the PGA unoprostone and most of the beta-blockers. Compared with the most widely used PGAs, LBN numerically outperformed latanoprost and travoprost and was similar to bimatoprost 0.01%.
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- 2021
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16. Bradycardia Shock Caused by the Combined Use of Carteolol Eye Drops and Verapamil in an Elderly Patient with Atrial Fibrillation and Chronic Kidney Disease
- Author
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Naotaka Akutsu, Nobuhiro Murata, Masaki Monden, Yasuo Okumura, Riku Arai, and Daisuke Fukamachi
- Subjects
Bradycardia ,verapamil ,medicine.medical_specialty ,genetic structures ,Hyperkalemia ,eye drops ,Glaucoma ,Case Report ,030204 cardiovascular system & hematology ,03 medical and health sciences ,0302 clinical medicine ,Japan ,Internal medicine ,Atrial Fibrillation ,Internal Medicine ,Humans ,Medicine ,Carteolol ,Renal Insufficiency, Chronic ,Aged ,Polypharmacy ,business.industry ,Atrial fibrillation ,General Medicine ,hyperkalemia ,medicine.disease ,carteolol ,humanities ,Shock (circulatory) ,Cardiology ,030211 gastroenterology & hepatology ,Ophthalmic Solutions ,medicine.symptom ,business ,chronic kidney disease ,Kidney disease ,medicine.drug - Abstract
Ophthalmic carteolol is often used to treat glaucoma. Elderly patients with atrial fibrillation (AF) and chronic kidney disease (CKD) are common among the super-elderly in Japan. Because these patients are exposed to polypharmacy, they are at a high-risk of adverse drug interactions. We herein report an elderly patient with CKD who suffered bradycardia shock after the combined use of carteolol eye drops and verapamil for glaucoma and paroxysmal AF. This case highlights the fact that eye drops have a similar systemic effect to oral drugs, and especially in elderly patients with polypharmacy, drug interactions can unwittingly lead to serious events.
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- 2021
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17. Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops.
- Author
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Eto R, Kawano H, Suzuki A, Akashi R, Ikeda S, and Maemura K
- Subjects
- Humans, Ophthalmic Solutions adverse effects, Adrenergic beta-Antagonists adverse effects, Carteolol adverse effects, Coronary Vasospasm chemically induced, Coronary Vasospasm drug therapy, Glaucoma, Ocular Hypertension chemically induced, Ocular Hypertension drug therapy, Angina Pectoris, Variant
- Abstract
Vasospastic angina (VSA) can be worsened by oral nonselective beta-blockers. Ophthalmic carteolol eye drops are nonselective beta-blockers and effective against glaucoma and ocular hypertension. Systemic effects of ophthalmic beta-blockers on VSA have not yet been reported. We herein report a case of VSA that developed after a patient started carteolol eye drops for ocular hypertension. Even though benidipine, a calcium channel blocker, was started, a VSA attack with incessant non-sustained ventricular tachycardia occurred. Once the carteolol eyedrops were discontinued, the VSA resolved. This case demonstrates that carteolol eye drops can induce life-threatening VSA.
- Published
- 2023
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18. Short-Term Efficacy and Safety of Switching from a Latanoprost/Timolol Fixed Combination to a Latanoprost/Carteolol Fixed Combination
- Author
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Mayumi Iwasa, Kenji Inoue, Hua Piao, Goji Tomita, and Kyoko Ishida
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medicine.medical_specialty ,Intraocular pressure ,genetic structures ,business.industry ,Glaucoma ,Timolol ,Ocular hypertension ,medicine.disease ,eye diseases ,03 medical and health sciences ,Ophthalmology ,chemistry.chemical_compound ,0302 clinical medicine ,Blood pressure ,chemistry ,030221 ophthalmology & optometry ,medicine ,Carteolol ,sense organs ,Latanoprost ,Latanoprost/timolol ,business ,030217 neurology & neurosurgery ,medicine.drug - Abstract
Purpose To investigate the short-term intraocular pressure-lowering efficacy and safety of switching from a fixed combination of latanoprost/timolol to a fixed combination of latanoprost/carteolol. Patients and Methods The subjects were 30 eyes of 30 adult patients with primary open-angle glaucoma, normal-tension glaucoma, or ocular hypertension who were using a latanoprost-/timolol-fixed combination with insufficient intraocular pressure-lowering efficacy or adverse reactions. The subjects were switched from once-daily latanoprost/timolol to once-daily latanoprost/carteolol with no washout interval. Intraocular pressure, tear film break-up time, corneal epithelial defects, conjunctival hyperemia, blood pressure, and pulse rate were measured and compared before and 1 and 3 months after switching. Patients were monitored for adverse reactions at each visit, and dropouts were recorded. Results The mean intraocular pressure at 1 month (15.9±3.1 mmHg) and 3 months (16.3±3.8 mmHg) was not significantly different from that at baseline (16.1±3.1 mmHg). The tear film break-up time and corneal epithelial defects were significantly improved after switching (p
- Published
- 2020
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19. Cystoid Macular Edema Associated with Omidenepag Isopropyl in Phakic Eyes after Laser Iridotomy: A Case Report
- Author
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Kenji, Nakamoto, Naka, Shiratori, Yusuke, Nishio, Shio, Sugimoto, Yasuko, Takano, Masashi, Yamazaki, Yutaro, Tobita, Tsutomu, Igarashi, Hiroshi, Takahashi, Nakamoto, Kenji, Shiratori, Naka, Nishio, Yusuke, Sugimoto, Shio, Takano, Yasuko, Yamazaki, Masashi, Tobita, Yutaro, Igarashi, Tsutomu, and Takahashi, Hiroshi
- Subjects
medicine.medical_specialty ,genetic structures ,Pyridines ,education ,Bromfenac sodium ,Glycine ,Visual Acuity ,Glaucoma ,Cataract Extraction ,Macular Edema ,Laser iridotomy ,Ophthalmology ,medicine ,Humans ,Carteolol ,Macular edema ,Intraocular Pressure ,business.industry ,Lasers ,General Medicine ,Middle Aged ,medicine.disease ,eye diseases ,Discontinuation ,Decreased vision ,Pyrazoles ,sense organs ,Ophthalmic Solutions ,business ,Isopropyl ,medicine.drug - Abstract
Decreased vision and cystoid macular edema (CME) developed in phakic eyes of a patient who underwent laser iridotomy after changing the glaucoma eye drops from carteolol 2% long-acting ophthalmic solution to omidenepag isopropyl 0.002%. CME completely disappeared at approximately 2 months after discontinuation of omidenepag isopropyl in conjunction with the use of bromfenac sodium 0.1%.
- Published
- 2021
20. Retinal Vessel Density Changes on Optical Coherence Tomography Angiography and Predictive Factors in Normal-Tension Glaucoma Treated with Topical Beta-Blocker
- Author
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Lan-Hsin Chuang, Shih-Ming Huang, Lung-Chien Chen, and Yun-Hsuan Lin
- Subjects
medicine.medical_specialty ,hypertension ,genetic structures ,medicine.drug_class ,Pharmaceutical Science ,Glaucoma ,optical coherence tomography angiography ,Microcirculation ,Pharmacy and materia medica ,Ophthalmology ,Normal tension glaucoma ,vessel density ,Medicine ,Carteolol ,Beta blocker ,business.industry ,normal-tension glaucoma ,Optical coherence tomography angiography ,medicine.disease ,eye diseases ,carteolol ,Retinal vessel ,RS1-441 ,age ,Optic nerve ,beta-blocker ,sense organs ,business ,medicine.drug - Abstract
(1) Background: Topical antiglaucoma medications may alter the microcirculation in the optic nerve head. We aimed to evaluate the changes in retinal vessel density (VD) on optical coherence tomography angiography (OCTA) in patients with newly diagnosed normal-tension glaucoma (NTG) treated with a topical beta-blocker. (2) Methods: This study included 80 patients diagnosed with NTG not using systemic medication, who received topical carteolol treatment between December 2019 and November 2020. We studied the changes in the OCTA VD/signal strength index (SSI) after the 6-month treatment period and determined the predictive factors affecting the changes in VD/SSI. (3) Results: After the 6-month treatment period, the peripapillary VD increased in 40 patients but decreased in the other 40 patients. The univariate and multivariate analyses revealed that old age and hypertension were significant factors associated with a VD/SSI decrease after carteolol treatment. Moreover, high baseline peripapillary, superficial, and deep macular VDs were significantly associated with the VD decrease after carteolol treatment. (4) Conclusions: Carteolol treatment could increase or decrease the VD in patients with NTG. The baseline VD, age, and hypertension could affect these VD changes. Patients with NTG and higher baseline peripapillary or macular VD, older age, and hypertension are more likely to have a decreased VD after carteolol treatment.
- Published
- 2021
21. Efficacy and safety of the fixed combinations of tafluprost/timolol and latanoprost/carteolol
- Author
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Atsushi Shimazaki, Takahiro Akaishi, Takazumi Taniguchi, Masatomo Kato, Naoko Yamashita, Masahiro Fuwa, and Masafumi Mieda
- Subjects
Male ,0301 basic medicine ,Intraocular pressure ,medicine.medical_specialty ,genetic structures ,medicine.drug_class ,Timolol ,lcsh:Medicine ,Article ,Cell Line ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Ophthalmology ,medicine ,Animals ,Humans ,Carteolol ,Latanoprost ,lcsh:Science ,Antihypertensive Agents ,Intraocular Pressure ,Multidisciplinary ,business.industry ,Prostaglandins F ,lcsh:R ,Epithelium, Corneal ,Antagonist ,Tafluprost ,Glaucoma ,eye diseases ,Drug Combinations ,Macaca fascicularis ,030104 developmental biology ,Pharmacodynamics ,chemistry ,Preclinical research ,Toxicity ,lcsh:Q ,sense organs ,Prostaglandin analogue ,business ,030217 neurology & neurosurgery ,medicine.drug - Abstract
In this study, we made a comparative efficacy and safety assessment of two different fixed combinations of drugs, viz., tafluprost/timolol (TAF/TIM) and latanoprost/carteolol (LAT/CAR), by determining their effects on intraocular pressure (IOP) in ocular normotensive monkeys and examining their toxic effects on ocular surface using human corneal epithelial cells. TAF/TIM was found to be more effective in lowering IOP for a longer duration compared to LAT/CAR. We found that the difference in the intensity of IOP-lowering effect was because of the differences in the strength of timolol compared with that of carteolol as a beta-adrenergic antagonist and strength of tafluprost compared with that of latanoprost as a prostaglandin analogue. In addition, TAF/TIM showed much less cytotoxic effects compared to LAT/CAR on the human corneal epithelial cells. Our findings showed that TAF/TIM is better than LAT/CAR with regard to the IOP-lowering effect in monkeys and toxicity on ocular surface.
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- 2019
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22. Carteolol hydrochloride reduces visible light-induced retinal damage in vivo and BSO/glutamate-induced oxidative stress in vitro
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Yoshiki Kuse, Masamitsu Shimazawa, Akihiro Ohira, Keiichi Kuwahara, Kei Takahashi, Masaki Tanito, Hideaki Hara, Sachiko Kaidzu, and Masato Matsuo
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Male ,0301 basic medicine ,GPX1 ,Programmed cell death ,Light ,genetic structures ,Swine ,Adrenergic beta-Antagonists ,Radiation-Protective Agents ,Carteolol Hydrochloride ,Pharmacology ,medicine.disease_cause ,Retina ,Cell Line ,Mice ,03 medical and health sciences ,0302 clinical medicine ,medicine ,Animals ,Carteolol ,Outer nuclear layer ,Antihypertensive Agents ,chemistry.chemical_classification ,Reactive oxygen species ,lcsh:RM1-950 ,eye diseases ,Rats ,Oxidative Stress ,lcsh:Therapeutics. Pharmacology ,030104 developmental biology ,medicine.anatomical_structure ,chemistry ,Molecular Medicine ,sense organs ,Reactive Oxygen Species ,030217 neurology & neurosurgery ,Intracellular ,Oxidative stress ,medicine.drug - Abstract
The purpose of this study was to determine whether carteolol eye drops, a β-adrenoceptor antagonist used as an intraocular hypotensive agent, has protective effects against the light-induced oxidative stress in retina. Dark-adapted pigmented rats were pre-treated with topical carteolol ophthalmic solution or saline and then exposed to visible light. The effects on electroretinogram (ERG), morphology, oxidative stress, and expression of mRNAs in the retinas were determined. The l-buthionine-(S,R)-sulfoximine (BSO)/glutamate-induced oxidative stress in 661 W cells, a murine photoreceptor cell line, was evaluated by cell death assays, production of reactive oxygen species (ROS), and activation of caspase. In vivo studies showed that exposure to light caused a decrease in the amplitudes of ERGs and the outer nuclear layer (ONL) thickness and an increase of the 8-hydroxy-2′-deoxyguanosine (8-OHdG)-positive cells in the ONL. These changes were significantly reduced by pre-treatment with carteolol. Carteolol also significantly up-regulated the mRNA levels of thioredoxin 1 and glutathione peroxidase 1 compared to saline-treated group. Moreover, carteolol and timolol, another β-adrenoceptor antagonist, significantly inhibited BSO/glutamate-induced cell death and reduced caspase-3/7 activity and ROS production in vitro. Therefore, carteolol could protect retina from light-induced damage with multiple effects such as enhancing the antioxidative potential and decreasing the intracellular ROS production. Keywords: Carteolol hydrochloride, Light-induced retinal damage, Oxidative stress, Antioxidative potential, Reactive oxygen species
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- 2019
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23. A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride.
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Hashikawa Y, Kato Y, Kaji H, Abe T, and Nagai N
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The objectives of this study were to develop a sustained-release device for carteolol hydrochloride (CH) and investigate any potential difference in the intraocular distribution of this agent between the transscleral administration of the device and treatment with eyedrops. The device was formulated with photocurable resin, poly (ethyleneglycol) dimethacrylate, to fit within the curve of the rabbit eyeball. In vitro study showed that CH was released in a sustained-release manner for 2 weeks. The concentration of CH in the retina, choroid/retinal pigment epithelium, sclera, iris, and aqueous humor was determined by high-performance liquid chromatography. Transscleral administration was able to deliver CH to the posterior segment (i.e., retina and choroid/retinal pigment epithelium) rather than the anterior segment (i.e., aqueous humor), while eyedrops delivered CH only to the anterior segment. Transscleral administration could deliver CH to aqueous humor at half the concentration versus treatment with eyedrops and reduced intraocular pressure (IOP) at 1 day after implantation; however, the IOP-lowering effect was not sustained thereafter. In conclusion, transscleral drug delivery may be a useful method for the reduction of IOP. Notably, the aqueous concentration must be equal to that delivered by the eyedrops, and this approach might be preferable for drug delivery to the posterior segment of the eye., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2023 The Authors.)
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- 2023
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24. Carteolol hydrochloride reduces visible light-induced retinal damage invivo and BSO/glutamate-induced oxidative stress invitro.
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- 2020
25. [Type IV hypersensitivity to timolol]
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Silvio, Espínola and Dory, Mora
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Adult ,Male ,Adrenergic beta-Antagonists ,Timolol ,Humans ,Hypersensitivity, Delayed ,Carteolol ,Glaucoma, Open-Angle - Abstract
In recent years, there have been reports of contact dermatitis due to the beta-blockers that are used in the treatment of glaucoma, such as timolol, levubonolol, carteolol, or betaxolol.A 37-year-old male patient, who was diagnosed with bilateral primary open-angle glaucoma two years ago, was in therapy with dorzolamide and a topical β-adrenergic blocker (timolol) in drops twice a day. Months later, he reported conjunctival hyperemia, stinging, and inflammation of both eyelids, followed by erythematous dermatitis, which improved upon treatment discontinuation. The patch test came back negative, but the conjunctival provocation test came back positive 48 hours later.Sensitization to the ophthalmic drops that are used to control glaucoma proved to be the mechanism that was causing the clinical picture of the patient. Performing a tolerance test for active anti-glaucoma agents may be helpful in improving tolerance to the medical treatment of some patients, thus, avoiding laser procedures and/or precipitated antiglaucomatous surgeries.Antecedentes: En los últimos años se han comunicado casos de dermatitis de contacto debido a betabloqueadores utilizados en el tratamiento del glaucoma como el timolol, levubonol, carteolol o betaxolol. Caso clínico: Hombre de 37 años de edad con diagnóstico dos años atrás de glaucoma primario de ángulo abierto bilateral, en terapia con dorzolamida y un agente betabloqueador adrenérgico tópico (timolol) en gotas, dos veces al día. Meses después consultó por hiperemia conjuntival, escozor e inflamación de párpados de ambos ojos seguida de dermatitis eritematosa, que mejoraban al suspender el tratamiento. La prueba del parche resultó negativa, pero la prueba de provocación conjuntival resultó positiva a las 48 horas. Conclusión: La sensibilización a las gotas oftálmicas que se emplean para controlar el glaucoma resultó ser el mecanismo responsable del cuadro clínico de la paciente. La prueba de tolerancia a los principios activos antiglaucomatosos puede resultar de ayuda para mejorar la tolerancia al tratamiento médico de algunos pacientes, con lo que podría evitarse procedimientos con láser o cirugías antiglaucomatosas precipitadas.
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- 2021
26. Hipersensibilidad tipo IV por timolol
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Dory Mora and Silvio Espínola
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medicine.medical_specialty ,business.industry ,Patch test ,Timolol ,Glaucoma ,medicine.disease ,Dermatology ,Betaxolol ,Discontinuation ,030207 dermatology & venereal diseases ,03 medical and health sciences ,0302 clinical medicine ,Dorzolamide ,030221 ophthalmology & optometry ,medicine ,Immunology and Allergy ,Carteolol ,business ,Contact dermatitis ,medicine.drug - Abstract
Antecedentes: En los últimos años se han comunicado casos de dermatitis de contacto debido a betabloqueadores utilizados en el tratamiento del glaucoma como el timolol, levubonol, carteolol o betaxolol. Caso clínico: Hombre de 37 años de edad con diagnóstico dos años atrás de glaucoma primario de ángulo abierto bilateral, en terapia con dorzolamida y un agente betabloqueador adrenérgico tópico (timolol) en gotas, dos veces al día. Meses después consultó por hiperemia conjuntival, escozor e inflamación de párpados de ambos ojos seguida de dermatitis eritematosa, que mejoraban al suspender el tratamiento. La prueba del parche que resultó negativ, pero la prueba de provocación conjuntival resultó positiva a las 48 horas. Conclusión: La sensibilización a las gotas oftálmicas que se emplean para controlar el glaucoma resultó ser el mecanismo responsable del cuadro clínico de la paciente. La prueba de tolerancia a los principios activos antiglaucomatosos puede resultar de ayuda para mejorar la tolerancia al tratamiento médico de algunos pacientes, evitándose así procedimientos con láser o cirugías antiglaucomatosas precipitadas.
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- 2021
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27. Lipase Catalyzed Synthesis of Enantiopure Precursors and Derivatives for β-Blockers Practolol, Pindolol and Carteolol
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Elisabeth Egholm Jacobsen, Mari Rødseth, Guro Buaas Austli, Sigrid Sløgedal Løvland, Mari Bergan Hansen, and Morten Andre Gundersen
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Chlorohydrins ,paracetamol ,TP1-1185 ,010402 general chemistry ,01 natural sciences ,Medicinal chemistry ,Catalysis ,Kinetic resolution ,chemistry.chemical_compound ,medicine ,Candida antarctica Lipase B ,Carteolol ,(S)-practolol ,Physical and Theoretical Chemistry ,Enantiomeric excess ,QD1-999 ,(S)-carteolol ,dimer formation ,010405 organic chemistry ,Chemistry ,Chemical technology ,0104 chemical sciences ,absolute configuration ,Enantiopure drug ,Yield (chemistry) ,(S)-pindolol ,Enantiomer ,Acetamide ,chiral chromatography ,medicine.drug - Abstract
Sustainable methods for producing enantiopure drugs have been developed. Chlorohydrins as building blocks for several β-blockers have been synthesized in high enantiomeric purity by chemo-enzymatic methods. The yield of the chlorohydrins increased by the use of catalytic amount of base. The reason for this was found to be the reduced formation of the dimeric by-products compared to the use of higher concentration of the base. An overall reduction of reagents and reaction time was also obtained compared to our previously reported data of similar compounds. The enantiomers of the chlorohydrin building blocks were obtained by kinetic resolution of the racemate in transesterification reactions catalyzed by Candida antarctica Lipase B (CALB). Optical rotations confirmed the absolute configuration of the enantiopure drugs. The β-blocker (S)-practolol ((S)-N-(4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide) was synthesized with 96% enantiomeric excess (ee) from the chlorohydrin (R)-N-(4-(3-chloro-2 hydroxypropoxy)phenyl)acetamide, which was produced in 97% ee and with 27% yield. Racemic building block 1-((1H-indol-4-yl)oxy)-3-chloropropan-2-ol for the β-blocker pindolol was produced in 53% yield and (R)-1-((1H-indol-4-yl)oxy)-3-chloropropan-2-ol was produced in 92% ee. The chlorohydrin 7-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one, a building block for a derivative of carteolol was produced in 77% yield. (R)-7-(3-Chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one was obtained in 96% ee. The S-enantiomer of this carteolol derivative was produced in 97% ee in 87% yield. Racemic building block 5-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one, building block for the drug carteolol, was also produced in 53% yield, with 96% ee of the R-chlorohydrin (R)-5-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one. (S)-Carteolol was produced in 96% ee with low yield, which easily can be improved.
- Published
- 2021
28. Phosphorus dendrimers as powerful nanoplatforms for drug delivery, as fluorescent probes and for liposome interaction studies: A concise overview
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Dzmitry Shcharbin, Serge Mignani, Jean-Pierre Majoral, Maria Bryszewska, Xiangyang Shi, Institute of Biophysics and Cell Engineering, NASB, Minsk, National Academy of Sciences of Belarus (NASB), Department of General Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, University of Lódź, Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques (LCBPT - UMR 8601), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université de Paris (UP), Centro de Química da Madeira, Universidade da Madeira (UMA), State Key Laboratory for Fiber & Material Modification of Donghua University, Donghua University [Shanghai], Laboratoire de chimie de coordination (LCC), Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie de Toulouse (ICT-FR 2599), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Polish National Agency for Academic Exchange, grant EUROPARTNER, No. PPI/APM/2018/1/00007/U/001, Belarusian Republican Foundation for Fundamental Research and State Committee of Science and Technology of Belarus, grants B19ARMG-002 and B20SLKG-002, FCT-Fundaçao para a Ciencia e a Tecnologia (Base Fund UIDB/00674/2020 and Programmatic Fund UIDP/00674/2020, Portuguese Government Funds), ARDITI-Agencia Regional para o Desenvolvimento da Investigaçao Tecnologia e Inovaçao through the project M1420-01-0145-FEDER-000005-CQMþ (Madeira 14e20 Program), Transnational EuroNanoMed III (ERANET), CNRS, Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Paris Cité (UPCité), Institut de Chimie de Toulouse (ICT), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), and Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)
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Dendrimers ,siRNA delivery ,Endosome ,Nano-carriers ,Genetic enhancement ,In vitro and in vivo gene therapy ,01 natural sciences ,Cell Line ,Insertional mutagenesis ,03 medical and health sciences ,Organophosphorus Compounds ,Phosphorus dendrimers ,Dendrimer ,Drug Discovery ,Animals ,Humans ,Gene silencing ,[CHIM.COOR]Chemical Sciences/Coordination chemistry ,RNA, Small Interfering ,Carteolol ,Fluorescent Dyes ,030304 developmental biology ,Pharmacology ,Inflammation ,Drug Carriers ,0303 health sciences ,Liposome ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Gene Transfer Techniques ,General Medicine ,0104 chemical sciences ,Cytoplasm ,Liposomes ,Drug delivery ,Biophysics ,Cancers ,Polyplexes - Abstract
International audience; Gene therapy is a new and promising tool to treat many severe diseases and the silencing of proteins is the safest and the most efficient tool to treat diseases because it does not induce changes in human genome and avoids a huge problem encompassing insertional mutagenesis. Using small RNAs to switch on/off target proteins is limited due to existence of some barriers for them in the human body (blood RNAses, serum albumins, cell walls, etc). For therapeutic applications they need the efficient and non-toxic carrier which will deliver them into cell cytoplasm. Within the huge range of carriers available, dendrimers can be underlined as new promising efficient carriers. This review summarizes several findings in phosphorus dendrimers based on in vitro and in vivo studies. As a result, we can conclude that advantages of phosphorus dendrimers are strong interaction with siRNA/DNA and formation of small and compact positively charged complexes of high and fast penetration into cells; efficient release of siRNA/pDNA in endosomes due to “proton sponge” effect; possibility of their modification including addition of fluorescent probes - in this case fluorescent dendrimer can be used both as a gene carrier and a tracer of delivery into cells. Additional benefit of using fluorescent phosphorus dendrimers is their ability to monitor the macrophage physiological status in vitro and in vivo.
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- 2020
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29. Betaxolol, Brimonidin and Carteolol in the Therapy of Normal-Tension Glaucoma
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Jan Lestak, M Fůs, K Marešová, and I Weissová
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medicine.medical_specialty ,Intraocular pressure ,Visual acuity ,genetic structures ,Glaucoma ,Betaxolol ,03 medical and health sciences ,0302 clinical medicine ,Ophthalmology ,Normal tension glaucoma ,medicine ,Humans ,Carteolol ,Intraocular Pressure ,030304 developmental biology ,0303 health sciences ,business.industry ,Brimonidine ,Middle Aged ,medicine.disease ,eye diseases ,Visual field ,030221 ophthalmology & optometry ,Evoked Potentials, Visual ,sense organs ,medicine.symptom ,business ,Glaucoma, Open-Angle ,medicine.drug - Abstract
Purpose: The purpose of the study was to evaluate influence of betaxolol, brimonidine and carteolol in the progression of the visual field defects during time at patients with normotensive glaucoma (NTG). Materials and methods: This study included (60 eyes of) 30 patients with NTG. First group consisted of 20 eyes of 10 patients of the average age of 58.5 years, who were treated by betaxolol. Second group also consisted of 20 eyes of 10 patients of the average age of 62.6 years and they were treated by brimonidine. Third group had the same count of the eyes and patients, the average age was 61.1 years and these patients were treated by carteolol. Diagnose of NTG was based on the comprehensive ophthalmological examination including electroretinography and visual evoked potentials. Visual fields were examined by fast threshold glaucoma test using Medmont M700 device. We compared pattern defect (PD) in the visual field for 3 years. The including criteria were: similar visual field findings at the beginning of the study, stable eye therapy (treatment was not changed during the study), uncorrected or best corrected (up to +-3 D) visual acuity of 1,0 of ETDRS, intraocular pressure between 10-15 mm Hg, if present, then compensated cardiovascular disease, no other internal or neurological disorders. Results: We didn’t notice any statistically important difference of PD. The study revealed that brimonidin (p=0,99) and betaxolol (p = 0,81) had the best effect. Conclusion: Local therapy of betaxolol, brimonidine and carteolol has an essential clinical value in normotensive glaucoma. All the mentioned treatments had a protective effect on the visual field. However, local side-effects of brimonidinu are a question.
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- 2020
30. Seasonal fluctuation in intraocular pressure and its associated factors in primary open-angle glaucoma
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Takahiko Noro, Shumpei Ogawa, Akiko Sotozono, Masayuki Tatemichi, Ryo Terauchi, and Tadashi Nakano
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Intraocular pressure ,medicine.medical_specialty ,genetic structures ,Open angle glaucoma ,Timolol ,Glaucoma ,Spherical equivalent ,Article ,03 medical and health sciences ,Tonometry, Ocular ,0302 clinical medicine ,Ophthalmology ,Normal tension glaucoma ,medicine ,Humans ,Carteolol ,Low Tension Glaucoma ,Intraocular Pressure ,business.industry ,medicine.disease ,eye diseases ,030221 ophthalmology & optometry ,Multiple linear regression analysis ,sense organs ,Seasons ,Ophthalmic Solutions ,business ,030217 neurology & neurosurgery ,Glaucoma, Open-Angle ,medicine.drug - Abstract
BACKGROUND/OBJECTIVES: To evaluate seasonal fluctuations in intraocular pressure (IOP) in primary open-angle glaucoma (POAG) and its associated factors. SUBJECTS/METHODS: POAG patients treated only with glaucoma eye drops were enroled. Winter and summer IOPs were evaluated. The Seasonal fluctuation rate of IOP was defined as follows: (mean winter IOP—mean summer IOP)/mean IOP in all seasons. Multiple linear regression analysis was used to explore factors associated with the seasonal IOP fluctuation rate including: age, gender, family history of glaucoma, type of glaucoma, number of eye drops, type of eye drops, mean deviation (MD) value, MD slope, disc haemorrhage, central corneal thickness and spherical equivalent. RESULTS: Winter IOP was higher than summer IOP in 204 POAG eyes of 204 patients, including 162 eyes with normal tension glaucoma (NTG) (13.2 ± 2.7 vs. 12.0 ± 2.3 mmHg, P
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- 2020
31. Lens-induced myopization and intraocular pressure in young guinea pigs
- Author
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Hai Di Kou, Wen Bin Wei, Yi Fan Li, Hao-Tian Wu, Li Dong, Yin Jun Lan, Jost B. Jonas, and Ya Xing Wang
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Refractive error ,Intraocular pressure ,medicine.medical_specialty ,genetic structures ,medicine.drug_class ,medicine.medical_treatment ,Guinea Pigs ,Eye ,03 medical and health sciences ,Tonometry, Ocular ,Axial length ,0302 clinical medicine ,lcsh:Ophthalmology ,Ophthalmology ,Lens, Crystalline ,medicine ,Myopia ,Animals ,Carteolol ,Beta-blocker ,Beta blocker ,Dioptre ,business.industry ,General Medicine ,medicine.disease ,eye diseases ,Outcome parameter ,Artificial tears ,lcsh:RE1-994 ,030221 ophthalmology & optometry ,sense organs ,business ,030217 neurology & neurosurgery ,medicine.drug ,Research Article - Abstract
Background Intraocular pressure (IOP) is an important physiological measure of the eye and is associated with some ocular disorders. We aimed to assess the influence of topical beta blocker-induced IOP reduction on lens-induced axial elongation in young guinea pigs. Methods The experimental study included 20 pigmented guinea pigs (age: 2–3 weeks). Myopia was induced in the right eyes for 5 weeks with − 10 diopter lenses. The right eyes additionally received either one drop of carteolol 2% (study group, n = 10) or one drop of artificial tears daily (control group, n = 10), while the contralateral eyes of all animals remained untouched. The outcome parameter was axial elongation during the follow-up period. The mean of all IOP measurements taken during the study was referred to as mean IOP. Results Greater axial elongation was associated with a shorter axial length at baseline (P P P = 0.59), the mean IOP during the study period (P = 0.12), the mean of all IOP measurements (P = 0.17), the difference between the IOP at study end and baseline IOP (P = 0.38), the difference between the mean IOP during the study period and the baseline IOP (P = 0.11), or the application of carteolol eye drops versus artificial tears eye drops (P = 0.07). The univariate analysis of the relationships between axial elongation and the IOP parameters yielded similar results. The inter-eye difference between the right eye and the left eye in axial elongation was significantly associated with the inter-eye difference in baseline axial length (P = 0.001; beta:-0.67) but not significantly correlated with the inter-eye difference in any of the IOP-related parameters (all P > 0.25). Conclusions In young guinea pigs with or without lens-induced axial elongation, neither the physiological IOP nor the IOP reduced by carteolol, a topical beta-blocker, was associated with the magnitude of axial elongation. These results suggest that IOP, regardless of whether it is influenced by carteolol, does not play a major role in axial elongation in young guinea pigs.
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- 2020
32. Changes in optic nerve head blood flow induced by the combined therapy of latanoprost and beta blockers.
- Author
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Sugiyama, Tetsuya, Kojima, Shota, Ishida, Osamu, and Ikeda, Tsunehiko
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- *
OPTIC nerve , *ADRENERGIC beta blockers , *BLOOD flow , *GLAUCOMA treatment , *VASODILATORS - Abstract
Purpose To assess the effects of combined therapy with latanoprost and beta blockers on optic nerve head (ONH) blood flow in normal-tension glaucoma (NTG) patients. Methods Intraocular pressure (IOP), ONH blood flow (laser speckle flowgraphy) and blood pressure were measured in 15 eyes of 15 NTG patients (41–76 years old) before treatment or after a 1-month washout period. Similar measurements were performed at 2 months after the commencement of treatment with latanoprost and at 3 months after the start of combined therapy of latanoprost with 0.5% timolol or 2% carteolol in a crossover study using the envelope method. Measurement was carried out 2–3 hr after the morning application of eyedrops. Results Latanoprost decreased IOP with no significant change in ONH blood flow. Concomitant use of timolol or carteolol further decreased IOP with no significant difference between these two drugs. Only the combined therapy of latanoprost with carteolol significantly (p < 0.01) increased ONH blood flow by approximately 10%, compared to initial levels. There was no significant change in mean blood pressure, ocular perfusion pressure or pulse rate as a result of these therapies. Conclusion: Topical latanoprost–carteolol combined therapy increased ONH blood flow in NTG patients, unlike latanoprost–timolol therapy. Because ocular perfusion pressure was unchanged, direct vasodilative effects were suspected as the mechanism. [ABSTRACT FROM AUTHOR]
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- 2009
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33. Update on Treatment of Infantile Hemangiomas: What's New in the Last Five Years?
- Author
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Macca L, Altavilla D, Di Bartolomeo L, Irrera N, Borgia F, Li Pomi F, Vaccaro F, Squadrito V, Squadrito F, and Vaccaro M
- Abstract
Among benign vascular tumors of infancy, hemangiomas are the commonest, affecting approximately 5-10% of one-year-old children. They are derived from a benign proliferation of vascular endothelial cells (VECs) in the mesoderm and may arise anywhere on the body around 1-2 weeks after birth. Infantile hemangiomas (IHs) are characterized by an early proliferative phase in the first year followed by a spontaneous progressive regression within the following 5 years or longer. IH prevalence is estimated to be 5%-10% in one-year-old children and commonly affects female, Caucasian and low-birth weight infants. Although most of them spontaneously regress, approximately 10% requires treatment to prevent complications due to the site of occurrence such as bleeding, ulceration, cosmetically disfigurement, functional impairment, or life-threatening complications. For over 30 years, steroids have represented the first-line treatment for IHs, but recently topical or systemic β-blockers are increasingly being used and recognized as effective and safe. A search for "Cutaneous infantile hemangioma" [All Fields] AND "Treatment" [All Fields] was performed by using PubMed and EMBASE databases. Treatment of IHs with labeled drugs, such as oral propranolol, but also with off-label drugs, such as topical β-blockers, including topical timolol and carteolol, steroids, itraconazole or sirolimus, with a focus on formulations types and adverse events were described in our review. We also discussed the benefits of pulsed dye laser and the treatment of IHs with involvement of central nervous system, namely the PHACE and LUMBAR syndrome., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. The handling editor FS is currently organizing a Research Topic with the author DA., (Copyright © 2022 Macca, Altavilla, Di Bartolomeo, Irrera, Borgia, Li Pomi, Vaccaro, Squadrito, Squadrito and Vaccaro.)
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- 2022
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34. Enantioseparation of chiral β-blockers using polynorepinephrine-coated nanoparticles and chiral capillary electrophoresis
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Zhenqun Li, Jia Wu, Li Jia, and Xue Xiao
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Adrenergic beta-Antagonists ,Nanoparticle ,02 engineering and technology ,01 natural sciences ,Biochemistry ,Analytical Chemistry ,chemistry.chemical_compound ,Magnetics ,Norepinephrine ,Capillary electrophoresis ,Limit of Detection ,Humans ,Carteolol ,Magnetite Nanoparticles ,Solid Phase Microextraction ,Detection limit ,Catechol ,Chromatography ,Chemistry ,010401 analytical chemistry ,Extraction (chemistry) ,Electrophoresis, Capillary ,Stereoisomerism ,Equipment Design ,021001 nanoscience & nanotechnology ,0104 chemical sciences ,Betaxolol ,Magnetic nanoparticles ,Amine gas treating ,Enantiomer ,0210 nano-technology ,Metoprolol - Abstract
A method of combining magnetic solid-phase separation (MSPE) and chiral capillary electrophoresis (CE) is developed for enantioseparation of trace amounts of β-blockers. Polynorepinephrine-functionalized magnetic nanoparticles (polyNE-MNPs) are synthesized and applied to simultaneously extract three β-blockers (carteolol, metoprolol, and betaxolol). The prepared polyNE-MNPs are spherical with a diameter of 198 ± 17 nm and the thickness of the polyNE coating is about 14 nm. PolyNE possesses abundant catechol hydroxyl and secondary amine groups, endowing the MNPs with excellent hydrophilicity. Under the optimum conditions, the extraction efficiencies of polyNE-MNPs for β-blockers are in the range of 89.6 to 100%, with relative standard deviations (RSDs) below 3.5%. The extraction process can be finished in 4 min. Field-enhanced sample injection (FESI) in chiral CE is constructed to further enhance the sensitivities of β-blocker enantiomers. The limits of detection for β-blocker enantiomers by the FESI-CE with polyNE-MNPs are in the range of 0.401 to 1.59 ng mL−1. The practicability of this method in real samples is evaluated by analysis of human urine samples. The recoveries for each enantiomer of β-blockers in the real samples range from 89.5 to 92.8%, with RSDs ranging from 0.37 to 5.9%. The whole detection process can be finished in less than 0.5 h. The method demonstrates its great potential in the pharmacokinetic and pharmacodynamic studies of chiral drugs in humans.
- Published
- 2018
35. Effect of long-term topical latanoprost medication on conjunctival thickness in patients with glaucoma
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Kai Ma, Qing-Song Li, Fang-Fang Bao, and Zhen-Yong Zhang
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0301 basic medicine ,medicine.medical_specialty ,genetic structures ,medicine.medical_treatment ,Glaucoma ,Carteolol Hydrochloride ,Conjunctival Epithelium ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,lcsh:Ophthalmology ,Clinical Research ,Ophthalmology ,Glaucoma surgery ,Medicine ,In patient ,Carteolol ,conjunctival thickness ,Latanoprost ,optical coherence tomography ,business.industry ,Significant difference ,medicine.disease ,eye diseases ,glaucoma ,030104 developmental biology ,latanoprost ,chemistry ,lcsh:RE1-994 ,glaucoma surgery ,030221 ophthalmology & optometry ,sense organs ,business ,medicine.drug - Abstract
AIM: To investigate the effect of long-term use of topically administered latanoprost on conjunctival thickness (CT) and conjunctival epithelium thickness (CET) in the patients with glaucoma. METHODS: A series of 106 glaucomatous patients were included. Of the 106 eyes, 55 eyes were treated with latanoprost eye drops once a day (latanoprost group), while 51 eyes were treated with carteolol hydrochloride eye drops (carteolol group). All the included patients completed a 2-year follow-up. CT and CET were measured with optical coherence tomography (OCT) in all patients at presentation and at 2-year visit, respectively. Statistical analysis was then performed to compare the change in CT and CET. RESULTS: At presentation, there was no difference in CET (t=0.400, P=0.689) or CT (t=1.14, P=0.259) between the two groups. No significant difference was found in CET (61.65±5.35 μm at baseline, 60.36±6.36 μm at 2-year follow-up, respectively; t=1.977, P=0.0531), while there was a significant decrease in CT from 201.45±14.99 μm at baseline to 167.81±14.57 μm at 2-year visit (t=14.1407, P
- Published
- 2018
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36. A facile and efficient single-step approach for the fabrication of vancomycin functionalized polymer-based monolith as chiral stationary phase for nano-liquid chromatography
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Dongsheng Xu, Zhengjin Jiang, Elena Sánchez-López, Salvatore Fanali, Qiqin Wang, María Luisa Marina, Huikai Shao, Rongying Luo, and Universidad de Alcalá. Departamento de Química Analítica, Química Física e Ingeniería Química
- Subjects
Fabrication ,Capillary action ,Polymers ,02 engineering and technology ,Methacrylate ,01 natural sciences ,Biochemistry ,Analytical Chemistry ,Polymerization ,Enantioseparation ,Organic polymeric monolith ,chemistry.chemical_compound ,Vancomycin ,Nanotechnology ,Nano-LC ,Monolith ,Carteolol ,Chromatography, High Pressure Liquid ,geography ,Functionalized polymer ,Chromatography, Reverse-Phase ,geography.geographical_feature_category ,Chromatography ,Dimethyl sulfoxide ,010401 analytical chemistry ,Organic Chemistry ,Reproducibility of Results ,Stereoisomerism ,General Medicine ,Química ,021001 nanoscience & nanotechnology ,Silicon Dioxide ,0104 chemical sciences ,Thalidomide ,Chemistry ,chemistry ,Chemical engineering ,Pharmaceutical Preparations ,Methacrylates ,Methanol ,0210 nano-technology ,Colchicine ,Derivative (chemistry) ,Isocyanates - Abstract
A facile single-step preparation strategy for fabricating vancomycin functionalized organic polymer based monolith within 100 mu m fused-silica capillary was developed. The synthetic chiral functional monomer, i.e 2-isocyanatoethyl methacrylate (ICNEML) derivative of vancomycin, was co-polymerized with the cross-linker ethylene dimethacrylate (EDMA) in the presence of methanol and dimethyl sulfoxide as the selected porogens. The co-polymerization conditions were systematically optimized in order to obtain satisfactory column performance. Adequate permeability, stability and column morphology were observed for the optimized poly(ICNEML-vancomycin-co-EDMA) monolith. A series of chiral drugs were evaluated on the monolith in either several other beta-blockers. The proposed single-step approach not only resulted in a vancomycin functionalized organer polar organic-phase or reversed-phase modes. After the optimization of separation conditions, baseline or partial enantioseparation were obtained for series of drugs including thalidomide, colchicine, carteolol, salbutamol, clenbuterol andic polymer-based monolith with acceptable performance, but also significantly simplified the preparation procedure by reducing time and labor.
- Published
- 2018
37. 'Tesofensine And Beta Blocker Combination Formulations' in Patent Application Approval Process (USPTO 20200129478)
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Eating disorders ,Antihypertensive agents ,Adrenergic beta-antagonists ,Type 2 diabetes ,Povidone -- Intellectual property ,Antiangina agents ,Aliphatic amines -- Intellectual property ,Antiarrhythmia agents -- Intellectual property ,Obesity ,Nebivolol ,Bucindolol ,Carteolol ,Pindolol ,Oxprenolol ,Penbutolol ,Esmolol ,Editors ,Health - Abstract
2020 MAY 18 (NewsRx) -- By a News Reporter-Staff News Editor at Obesity & Diabetes Week -- A patent application by the inventors NIELSEN, Peter G. (Vaerlose, DK); THOMSEN, Mikael [...]
- Published
- 2020
38. Patent Issued for Tesofensine And Beta Blocker Combination Formulations (USPTO 10,537,551)
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Eating disorders ,Antihypertensive agents ,Adrenergic beta-antagonists ,Type 2 diabetes ,Povidone -- Intellectual property ,Antiangina agents ,Aliphatic amines -- Intellectual property ,Antiarrhythmia agents -- Intellectual property ,Obesity ,Nebivolol ,Bucindolol ,Carteolol ,Pindolol ,Oxprenolol ,Penbutolol ,Esmolol ,Editors ,Health - Abstract
2020 FEB 3 (NewsRx) -- By a News Reporter-Staff News Editor at Obesity & Diabetes Week -- According to news reporting originating from Alexandria, Virginia, by NewsRx journalists, a patent [...]
- Published
- 2020
39. Patent Issued for Crystalline Form Of Benzylbenzene SGLT2 Inhibitor (USPTO 10,533,032)
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Antihypertensive agents ,Tezosentan -- Intellectual property ,Angiotensin II receptor blockers ,Oxcarbazepine ,Hypoglycemic agents ,Perindopril ,Clopidogrel -- Intellectual property ,Midostaurin -- Intellectual property ,Cilostazol -- Intellectual property ,Lofexidine -- Intellectual property ,Torsemide -- Intellectual property ,Adrenergic beta-antagonists ,Type 2 diabetes ,Thiazides -- Intellectual property ,Calcium channel blockers -- Intellectual property ,Antiarrhythmia agents -- Intellectual property ,Anopheles ,Ambrisentan ,Olmesartan medoxomil ,Liraglutide ,Methyclothiazide ,Obesity ,Alogliptin ,Nebivolol ,Exenatide ,Eprosartan ,Lercanidipine ,Penbutolol ,Esmolol ,Editors ,Hydrochlorothiazide ,Indapamide ,Saxagliptin ,Valsartan ,Trichlormethiazide ,Sitagliptin ,Sitaxsentan ,Pindolol ,Hydroflumethiazide ,Omapatrilat ,Telmisartan ,Fosinopril ,Carteolol ,Miglitol ,Nisoldipine ,Bosentan ,Bepridil ,Health - Abstract
2020 JAN 27 (NewsRx) -- By a News Reporter-Staff News Editor at Obesity & Diabetes Week -- Theracos Sub LLC (Marlborough, Massachusetts, United States) has been issued patent number 10,533,032, [...]
- Published
- 2020
40. Intraocular pressure with rebound tonometry and effects of topical intraocular pressure reducing medications in guinea pigs
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Lu Na, Xiu-Mei Luo, Yue Di, and Tong Qiao
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Intraocular pressure ,medicine.medical_specialty ,genetic structures ,040301 veterinary sciences ,Brinzolamide ,0403 veterinary science ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Ophthalmology ,medicine ,Carteolol ,Latanoprost ,Maximum level ,business.industry ,Brimonidine ,Significant difference ,04 agricultural and veterinary sciences ,REBOUND TONOMETRY ,eye diseases ,Basic Research ,chemistry ,030221 ophthalmology & optometry ,sense organs ,business ,medicine.drug - Abstract
AIM To investigate the intraocular pressure (IOP) of adult guinea pig eyes with rebound tonometry (RBT), and assess the effects of four distinctive topical IOP reducing medications including Carteolol, Brimonidine, Brinzolamide and Latanoprost. METHODS The IOPs of twenty-four 12-week-old guinea pigs (48 eyes) were measured every two hours in one day with RBT as baselines. All the animals were then divided into four groups (Carteolol, Brimonidine, Brinzolamide and Latanaprost groups, n=6). The IOPs were measured and compared to the baseline 1, 2, 3, 5, 7, 9, 15 and 24h after treatment. RESULTS The mean baseline IOP of 24 guinea pigs (48 eyes) was 10.3±0.36 mm Hg (6-13 mm Hg) and no binocular significant differences of IOPs were observed (t=1.76, P>0.05). No significant difference of IOP in Carteolol group at each time point was observed before and after treatment (t=1.48, P>0.05). In Brimonidine group, IOP was 2.2±1.9 mm Hg lower than the baseline after one hour (t=3.856, P=0.003) and lasted for one hour. In Brinzolamide group, IOP was 1.4±1.1 mm Hg lower than the baseline after one hour (t=4.53, P=0.001) and lasted for 7h and the IOP declined most at 3h. In Latanaprost group, IOP was 2.1±1.3 mm Hg lower than the baseline after one hour (t=6.11, P=0.001) and lasted for one hour. CONCLUSION The IOP of guinea pig eyes is relatively stable compared to human eyes. In four reducing IOP medications, no significant effect of Carteolol is observed. Brinzolamide has the longest duration, while the Brimonidine has the shortest duration and the maximum level of treatment.
- Published
- 2017
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41. Efficacy and safety of carteolol long-acting solution 2% compared with timolol gel-forming solution 0.5% in patients with primary open-angle glaucoma and ocular hypertension: A randomized, parallel-group, open-label phase IV study in Taiwan
- Author
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Hsin-Yu Yao, Yi-Hao Chen, Ming-Cheng Tai, and Da-Wen Lu
- Subjects
Intraocular pressure ,primary open-angle glaucoma ,Open angle glaucoma ,genetic structures ,Ocular hypertension ,Timolol ,Glaucoma ,lcsh:Medicine ,chemistry.chemical_compound ,Medicine ,Carteolol ,Latanoprost ,Adverse effect ,business.industry ,lcsh:R ,lcsh:Medical emergencies. Critical care. Intensive care. First aid ,General Medicine ,lcsh:RC86-88.9 ,medicine.disease ,Carteolol long-acting solution ,eye diseases ,chemistry ,latanoprost ,Anesthesia ,ocular hypertension ,timolol gel-forming solution ,sense organs ,business ,medicine.drug - Abstract
Purpose: The purpose of this study is to compare the efficacy and safety of 2% long-acting carteolol solution with 0.5% timolol gel-forming solution added to primary treatment of 0.005% latanoprost solution in patients with primary open-angle glaucoma and ocular hypertension. Materials and Methods: After at least 4 weeks primary treatment with latanoprost, all patients received the combination therapy with either 2% long-acting carteolol or 0.5% timolol gel in addition to latanoprost for 8 weeks. We measured intraocular pressure (IOP) and evaluated systemic and local adverse events between Day 1 and Day 56. Results: Carteolol significantly reduced the IOP from baseline (latanoprost monotherapy) by 11.0% at Day 28 and 11.2% at Day 56. Timolol also reduced IOP by 11.5% at Day 28 and 11.0% at Day 56. There was no statistically significant difference in the IOP reduction between the two groups. There was no adverse event related to the administration of these anti-glaucoma medications during the study period. Conclusions: Both once daily carteolol and timolol medications are safe and effective treatments combined with latanoprost single therapy.
- Published
- 2014
42. Insidious-onset, non-wheezing carteolol-induced asthma in an atopic patient without asthma history
- Author
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Jih-Shuin Jerng, Jo-Hsuan Wu, and Chien-Chia Su
- Subjects
0301 basic medicine ,medicine.medical_specialty ,Bronchoconstriction ,Adrenergic beta-Antagonists ,Provocation test ,Glaucoma ,Ocular hypertension ,Administration, Ophthalmic ,Pulmonary function testing ,Atopy ,Young Adult ,03 medical and health sciences ,0302 clinical medicine ,Internal medicine ,medicine ,Humans ,Carteolol ,Asthma ,Unexpected Outcome (Positive or Negative) Including Adverse Drug Reactions ,business.industry ,General Medicine ,medicine.disease ,Discontinuation ,030104 developmental biology ,030221 ophthalmology & optometry ,Ocular Hypertension ,business ,Tomography, Optical Coherence ,medicine.drug - Abstract
Carteolol, a non-selective beta-antagonist with a potential risk of severe bronchial constriction in patients with asthma, is one of the most commonly prescribed medication for managing ocular pressure in glaucoma. We present a case of a 24-year-old woman with a history of atopy but no known asthma who presented an insidious onset of clinical manifestations compatible with drug-induced asthma after the initiation of carteolol for ocular hypertension control. The patient developed progressive chest tightness and dyspnoea for 2 months before the pulmonary function test revealed a positive bronchoprovocation response. She reported significant improvement of respiratory symptoms within 2 weeks after the discontinuation of carteolol, and a negative provocation response was later confirmed by repeat pulmonary function test. In conclusion, eye drops with non-selective beta-antagonising effect can induce asthmatic symptoms in patients without a previous diagnosis of asthma and should be administered with caution in patients with associated risk factors.
- Published
- 2019
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43. Bradycardia Shock Caused by the Combined Use of Carteolol Eye Drops and Verapamil in an Elderly Patient with Atrial Fibrillation and Chronic Kidney Disease.
- Author
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Arai R, Fukamachi D, Monden M, Akutsu N, Murata N, and Okumura Y
- Subjects
- Aged, Bradycardia chemically induced, Humans, Japan, Ophthalmic Solutions adverse effects, Verapamil adverse effects, Atrial Fibrillation complications, Atrial Fibrillation drug therapy, Carteolol, Renal Insufficiency, Chronic complications
- Abstract
Ophthalmic carteolol is often used to treat glaucoma. Elderly patients with atrial fibrillation (AF) and chronic kidney disease (CKD) are common among the super-elderly in Japan. Because these patients are exposed to polypharmacy, they are at a high-risk of adverse drug interactions. We herein report an elderly patient with CKD who suffered bradycardia shock after the combined use of carteolol eye drops and verapamil for glaucoma and paroxysmal AF. This case highlights the fact that eye drops have a similar systemic effect to oral drugs, and especially in elderly patients with polypharmacy, drug interactions can unwittingly lead to serious events.
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- 2021
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44. Determination of Carteolol in Pure and Pharmaceutical Formulation by Spectrophotometric Method
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Mohammad Shraitah, Malek Okdeh, and Chahid Moustpha
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Chromatography ,medicine.diagnostic_test ,Chemistry ,010401 analytical chemistry ,Complex formation ,Molar absorptivity ,Pharmaceutical formulation ,Pharmacology ,030226 pharmacology & pharmacy ,01 natural sciences ,Red Color ,0104 chemical sciences ,03 medical and health sciences ,0302 clinical medicine ,Spectrophotometry ,medicine ,Carteolol ,Alizarin yellow R sodium salt ,medicine.drug - Abstract
An accurate, simple, fast, and good sensitive Spectrophotometric method have been developed for the determination of Carteolol based on the formation of complex (ion-pair complexes) between the Carteolol (CRT) and Alizarin yellow R Sodium salt (AR) at pH=11.20. This reaction produces a complex red color which is absorbed maximally at 500 nm. Beer’s law was obeyed in the range of 1.80-197.30 ug/mL with molar absorptivity of 1.7663×103 L mole-1cm-1. The effects of analytical parameters on the reported system were investigated. The results were validated statistically. The proposed method was applied to commercially available tablets. Interferences of the other ingredients and excipients were not observed.
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- 2016
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45. 'Compositions For The Treatment Of Hypertension' in Patent Application Approval Process (USPTO 20190314383)
- Subjects
Antihypertensive agents ,Angiotensin II receptor blockers ,Hypertension ,Adrenergic beta-antagonists ,Angiotensin II -- Intellectual property ,Antiangina agents ,Thiazides -- Intellectual property ,Calcium channel blockers -- Intellectual property ,Antiarrhythmia agents -- Intellectual property ,Mortality ,Levobetaxolol ,Methyclothiazide ,Nebivolol ,Eprosartan ,Lercanidipine ,Penbutolol ,Clevidipine ,Esmolol ,Editors ,Hydrochlorothiazide ,Indapamide ,Valsartan ,Trichlormethiazide ,Pindolol ,Oxprenolol ,Hydroflumethiazide ,Telmisartan ,Morbidity ,Carteolol ,Nisoldipine ,Polythiazide ,Bepridil ,Health - Abstract
2019 NOV 4 (NewsRx) -- By a News Reporter-Staff News Editor at Hematology Week -- A patent application by the inventors RODGERS, Anthony (Newtown NSW, AU); CHOW, Clara (Sydney NSW, [...]
- Published
- 2019
46. Simultaneous quantification of carteolol and dorzolamide in rabbit aqueous humor and ciliary body by liquid chromatography/atmospheric pressure chemical ionization mass spectrometry
- Author
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Rosaria Saletti, Alessio Zammataro, Salvatore Foti, Vera Muccilli, Vincenzo Cunsolo, and Claudine Civiale
- Subjects
Male ,Spectrometry, Mass, Electrospray Ionization ,Rabbit aqueous humor ,Clinical Biochemistry ,Ethyl acetate ,Atmospheric-pressure chemical ionization ,Thiophenes ,Mass spectrometry ,Biochemistry ,Analytical Chemistry ,Aqueous Humor ,chemistry.chemical_compound ,Dorzolamide ,medicine ,Animals ,Humans ,Protein precipitation ,Sample preparation ,Carteolol ,Antihypertensive Agents ,Chromatography, High Pressure Liquid ,RP-HPLC/APCI-MS/MS ,Sulfonamides ,Chromatography ,Ciliary Body ,Extraction (chemistry) ,Cell Biology ,General Medicine ,Quantitative determination ,Rabbit ciliary body ,Disease Models, Animal ,chemistry ,Ocular Hypertension ,Rabbits ,medicine.drug - Abstract
A rapid, sensitive and selective method for the simultaneous quantification of carteolol and dorzolamide in rabbit aqueous humor (AH) and ciliary body (CB) has been developed and validated using reversed phase-high performance liquid chromatography (RP-HPLC) with isocratic elution coupled with atmospheric pressure chemical ionization mass spectrometry/mass spectrometry (APCI-MS/MS). The analytes and nadolol (used as internal standard, IS) were purified from AH by protein precipitation. The sample preparation from CB was based on a two steps extraction procedure at different pH, utilizing a liquid–liquid extraction with a mixture of ethyl acetate, toluene and isopropanol 50:40:10 (v/v) at pH 8, followed by a second extraction with ethyl acetate at pH 11. The combined organic extracts were then back extracted into 0.1% aqueous trifluoroacetic acid (TFA). The accuracy and precision values, calculated from three different sets of quality control samples analyzed in sestuplicate on three different days, were within the generally accepted criteria for analytical methods (
- Published
- 2010
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47. Enhancement in Corneal Permeability of Dissolved Carteolol by Its Combination with Magnesium Hydroxide Nanoparticles
- Author
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Norio Okamoto, Noriaki Nagai, Hiroko Otake, Sakie Yamaoka, Yuya Fukuoka, Yoshikazu Shimomura, Miyu Ishii, and Kazutaka Kanai
- Subjects
0301 basic medicine ,genetic structures ,Adrenergic beta-Antagonists ,chemistry.chemical_element ,carteolol ,nanoparticle ,magnesium hydroxide ,glaucoma ,corneal penetration ,Permeability ,Article ,Catalysis ,Cornea ,lcsh:Chemistry ,Inorganic Chemistry ,03 medical and health sciences ,Benzalkonium chloride ,0302 clinical medicine ,medicine ,Animals ,Carteolol ,Particle Size ,Physical and Theoretical Chemistry ,Microparticle ,lcsh:QH301-705.5 ,Molecular Biology ,Spectroscopy ,Dose-Response Relationship, Drug ,Magnesium ,Organic Chemistry ,General Medicine ,Penetration (firestop) ,Computer Science Applications ,Bioavailability ,030104 developmental biology ,Solubility ,lcsh:Biology (General) ,lcsh:QD1-999 ,chemistry ,030221 ophthalmology & optometry ,Nanoparticles ,Rabbits ,Mannitol ,Particle size ,medicine.drug ,Nuclear chemistry - Abstract
We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol. The carteolol was solved in saline containing additives (0.5% methylcellulose, 0.001% benzalkonium chloride, 0.5% mannitol; CRT-solution). MH nanoparticles were prepared by a bead mill method with additives. Then carteolol/MH microparticle and carteolol/MH nanoparticle fixed combinations (mCMFC and nCMFC) were prepared by mixing the CRT-solution and MH particles. The transcorneal penetration and IOP-reducing effect of carteolol was evaluated in rabbits. The mean particle size of mCMFC was 7.2 μm, and the particle size was reduced to 73.5–113.5 nm by the bead mill treatment. The MH particles in nCMFC remained in the nano size range for 8 days after preparation, and the amounts of lacrimal fluid and corneal damage were unchanged by repetitive instillation of nCMFC (twice a day for 4 weeks). The transcorneal penetration of carteolol was enhanced by the combination with MH nanoparticles, and the IOP-reducing effect of nCMFC was significantly higher than that of CRT-solution or mCMFC. In conclusion, we designed nCMFC, and showed that the high levels of dissolved carteolol can be delivered into the aqueous humor by the instillation of nCMFC. Combination with MH nanoparticles may achieve an enhancement of corneal penetration for water-soluble drugs. These findings provide significant information that can be used to design further studies aimed at developing anti-glaucoma eye drugs.
- Published
- 2018
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48. [Type IV hypersensitivity to timolol].
- Author
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Espínola S and Mora D
- Subjects
- Adrenergic beta-Antagonists adverse effects, Adult, Humans, Male, Timolol adverse effects, Carteolol, Glaucoma, Open-Angle drug therapy, Hypersensitivity, Delayed
- Abstract
Background: In recent years, there have been reports of contact dermatitis due to the beta-blockers that are used in the treatment of glaucoma, such as timolol, levubonolol, carteolol, or betaxolol., Case Report: A 37-year-old male patient, who was diagnosed with bilateral primary open-angle glaucoma two years ago, was in therapy with dorzolamide and a topical β-adrenergic blocker (timolol) in drops twice a day. Months later, he reported conjunctival hyperemia, stinging, and inflammation of both eyelids, followed by erythematous dermatitis, which improved upon treatment discontinuation. The patch test came back negative, but the conjunctival provocation test came back positive 48 hours later., Conclusion: Sensitization to the ophthalmic drops that are used to control glaucoma proved to be the mechanism that was causing the clinical picture of the patient. Performing a tolerance test for active anti-glaucoma agents may be helpful in improving tolerance to the medical treatment of some patients, thus, avoiding laser procedures and/or precipitated antiglaucomatous surgeries.
- Published
- 2020
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49. Acute effect of topical carteolol on ocular pulsatile volume change
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Sei Yamazaki and Hiroyuki Baba
- Subjects
Adult ,Male ,Administration, Topical ,Pulsatile flow ,Acute effect ,Volume change ,Eye ,Tonometry, Ocular ,Heart Rate ,medicine ,Humans ,Carteolol ,Intraocular Pressure ,Chemistry ,Total flow ,Pulse (signal processing) ,General Medicine ,Blood flow ,Middle Aged ,Ophthalmology ,Pulsatile Flow ,Anesthesia ,Pressure amplitude ,Female ,sense organs ,Ophthalmic Solutions ,Blood Flow Velocity ,medicine.drug - Abstract
To determine whether topical carteolol affects ocular blood flow, we studied effects of carteolol 2% on the ocular pulse waves in 9 normal volunteers, and analyzed the results as variations in pulsatile volume changes (PVC) for one minute (PVCm) using the Friedenwald's pressure-volume relationship. PVC means a volume for the pressure amplitude in each pulse. The pulse waves were recorded with a pneumatonometer and analyzed by a computer. The PVCm change 15 min after the carteolol instillation was evaluated with the control performed with biological salt solution in the same manner. The data showed a net increase in the PVCm of the carteolol-instilled eyes (21.3 +/- 6.4 microliters/min: mean +/- standard error, p < 0.05, paired t-test). Considering a finding that PVCm takes 50% of the total ocular blood flow, the results suggest a possible alteration in the total flow by a carteolol instillation.
- Published
- 2009
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50. Cellular Cytotoxicity of Antiglaucoma Drugs in Cultured Corneal Endothelial Cells
- Author
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Kwou-Yeung Wu, Hwei-Zu Wang, and Show-Jen Hong
- Subjects
genetic structures ,Levobunolol ,cellular cytotoxicity ,Timolol ,Pharmacology ,Betaxolol ,Dorzolamide ,medicine ,antiglaucoma drugs ,Animals ,Carteolol ,Cells, Cultured ,Medicine(all) ,lcsh:R5-920 ,Dose-Response Relationship, Drug ,L-Lactate Dehydrogenase ,Dipivefrin ,business.industry ,Brimonidine ,Endothelium, Corneal ,Pilocarpine ,Endothelial Cells ,lactate dehydrogenase ,Glaucoma ,General Medicine ,eye diseases ,corneal endothelial cells ,Unoprostone ,Cattle ,sense organs ,lcsh:Medicine (General) ,business ,medicine.drug - Abstract
In this study, the various antiglaucoma drugs including betaxolol, timolol, levobunolol, carteolol, brimonidine, dipivefrin, dorzolamide, brinzolamide, latanoprost, unoprostone, and pilocarpine were used to investigate the effects of cellular cytotoxicity in cultured bovine corneal endothelial cells. After exposure to the drugs in three dilutions, 1/100, 1/1,000, and 1/10,000, for 100 minutes, cells were estimated based on the release assay of lactate dehydrogenase (LDH) enzyme. It was found that cellular LDH was significantly released in the medium only at 1/100 th dilution of betaxolol, brimonidine, dorzolamide, dipivefrin, latanoprost and unoprostone to 130%, 123%, 145%, 157%, 128% and 237%, respectively, compared with controls upon exposure to drugs for 100 minutes. Moreover, benzalkonium chloride preservative at the concentrations ranging from 0.001 to 0.00001mg/mL did not affect cellular LDH release in bovine corneal endothelial cells. These results indicate that high concentrations of antiglaucoma drugs may induce cytotoxicity in corneal endothelial cells.
- Published
- 2007
- Full Text
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