564 results on '"Carteolol"'
Search Results
2. Beta-blocker carteolol and oxprenolol produce cutaneous analgesia in response to needle pinpricks in the rat.
- Author
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Chou, An-Kuo and Chen, Yu-Wen
- Subjects
ANALGESIA ,LOCAL anesthetics ,BUPIVACAINE ,RATS ,ADRENERGIC beta blockers - Abstract
This present study was undertaken to determine whether beta-blockers produce the cutaneous analgesic effect, comparing them with the long-acting local anesthetic bupivacaine. Using a rat model of infiltrative cutaneous analgesia, the effect of 5 beta-blockers (oxprenolol, carteolol, butaxamine, metoprolol, and acebutolol) and bupivacaine was compared and eventually combined with epinephrine. Among 5 beta-blockers, oxprenolol exhibited the most potent and the longest duration of cutaneous analgesia. In dose-response studies, the rank order of efficacy (ED
50 [50% effective dose]) was bupivacaine (0.40 [0.35–0.47] μmol) > oxprenolol (2.33 [2.06–2.64] μmol) > carteolol (4.86 [4.27–5.53] μmol) (p< 0.01). Carteolol provoked a longer duration of analgesia (p< 0.01) than oxprenolol or bupivacaine on an equipotent basis (ED25 , ED50 , and ED75 ). Adding epinephrine 1:200,000 to drug preparations (carteolol, oxprenolol, and bupivacaine) at ED95 had a peripheral action in prolonging the duration of action. Oxprenolol and carteolol had greater potencies and longer durations of cutaneous analgesia than butaxamine, metoprolol, and acebutolol. Oxprenolol produced a similar duration of action when compared to bupivacaine, while carteolol had a greater duration of action than bupivacaine. Cutaneous analgesia of oxprenolol (or carteolol) plus adrenaline was greater than that of bupivacaine plus adrenaline. [ABSTRACT FROM AUTHOR]- Published
- 2023
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- View/download PDF
3. 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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4. 脉冲染料激光、曲安奈德注射和外用卡替洛尔治疗 婴幼儿浅表性血管瘤的疗效分析.
- Author
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汪城河, 余淑萍, 苏振民, 林文雄, 江秋霞, 吴雅莹, 刘长江, 林东福, and 蔡加滨
- Subjects
- *
DYE lasers , *TRIAMCINOLONE acetonide , *PULSED lasers , *TREATMENT effectiveness , *HEMANGIOMAS - Abstract
Objective To explore the effectiveness and safety of pulsed dye laser, triamcinolone acetonide injection and external use of 2% carteolol in the treatment of superficial infantile hemangioma. Methods From April 2020 to June 2021, 90 infants (less than 6 months) with superficial hemangioma were randomly divided into pulsed dye laser group (laser group), triamcinolone acetonide injection group (injection group) and external use of carteolol group (external group), 30 infants in each group. The clinical efficacy at 3 and 6 months after treatment was observed. Results A total of 65 infants were contained in the final statistics, including 18 cases in the external group, 24 cases in the laser group and 23 cases in the injection group. At 6 months after treatment, there was no statistically significant difference in excellent and good rate among 3 groups (P>0.05). There was statistically significant difference in effective rate between the laser group and the external group (P<0.05). There was no statistically significant difference in thickness of lesions among 3 groups (P>0.05). There was statistically significant difference in thickness of lesions between 3 months after treatment and before treatment within the laser group and the injection group (P<0.05), While there was no statistically significant difference in the external group (P<0.05). Conclusion The pulsed dye laser, triamcinolone acetonide injection and external use of carteolol alone can obtain satisfactory efficacy in the treatment of superficial infantile hemangioma. The pulsed dye laser treatment hasrelatively certain advantages. [ABSTRACT FROM AUTHOR]
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- 2022
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5. 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
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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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6. Formulation of carteolol chitosomes for ocular delivery: formulation optimization, ex-vivo permeation, and ocular toxicity examination.
- Author
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Zafar, Ameeduzzafar, Alruwaili, Nabil K., Imam, Syed Sarim, Alsaidan, Omar Awad, Alharbi, Khalid Saad, Yasir, Mohd, Elmowafy, Mohammed, Ansari, Mohammad Javed, Salahuddin, Mohammed, and Alshehri, Sultan
- Subjects
OCULAR toxicology ,SKIN permeability ,CORNEA ,EXPERIMENTAL design ,THERAPEUTICS ,HEMORRHAGE - Abstract
Background:Conventional delivery systems like solution and suspension are commonly used for the treatment of ocular diseases but have low corneal residence time and hence the duration of effect is limited. These drawbacks of conventional systems can be reduced by preparing bioadhesive chitosan (CH) coated noisome. Methods: Niosomes (NIM) of carteolol (CT) were developed by the thin-film hydration method and optimised by the Box-Behnken statistical design. Further, the optimised CT-NIM was coated with CH to enhance the ocular residence time. The optimised formulation was evaluated for vesicle size, entrapment efficiency, and in-vitro drug release and transcorneal permeation, histopathology, etc. Results: CT-NIM-opt showed the vesicle size and entrapment efficiency of 235 ± 3.54 nm, and 70.45 ± 0.87%, respectively. DSC spectra exhibited that CT was completely encapsulated into the CH-CT-NIM matrix. Drug release from CH-CT-NIM-opt was more sustained (68.28 ± 4.2%) than CT-NIM (75.69 ± 4.5% in 12 h) and CT solution (99.89 ± 2.8% in 4 h). The CH-CT-NIM-opt represented a strong bio-adhesion (89.76 ± 3.6%) than CT-NIM-opt (15.65 ± 3.4%). The permeation flux exhibited 1.13-fold higher permeation than CT-NIM and 3.23 fold than CT solution. The corneal hydration was found to be within the limit value. The histopathology study exhibited no structural damage to the cornea. HET-CAM results showed zero scores indicating no bleeding or haemorrhage. CH-CT-NIM-opt was found to be isotonic and exhibited good stability when stored at 4 °C for the stated duration of time. Conclusion: The above findings suggested that NIM can be a potential carrier for the delivery of CT with better ocular residence time. [ABSTRACT FROM AUTHOR]
- Published
- 2021
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7. Research Conducted at Ocean University of China Has Updated Our Knowledge about Eye Proteins (Carteolol Triggers Senescence Via Activation of B-arrestin-erk-nox4-ros Pathway In Human Corneal Endothelial Cells In Vitro).
- Published
- 2024
8. 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
- *
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]
- Published
- 2021
- Full Text
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9. Efficacy and Safety Study of OPC-1085EL Ophthalmic Solution in Subjects With Glaucoma or Ocular Hypertension
- Published
- 2015
10. Efficacy and Safety Study of OPC-1085EL Ophthalmic Solution in Subjects With Glaucoma or Ocular Hypertension
- Published
- 2015
11. Pharmacokinetic Study of OPC-1085EL Ophthalmic Solution in Healthy Male Adult Volunteers
- Published
- 2015
12. 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
- Subjects
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.
- Published
- 2020
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13. 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
- Full Text
- View/download PDF
14. 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
15. Further exploration of the collision-induced dissociation of select beta blockers: Acebutolol, atenolol, bisoprolol, carteolol, and labetalol.
- Author
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Carlo MJ and Patrick AL
- Subjects
- Tandem Mass Spectrometry methods, Bisoprolol, Chromatography, Liquid methods, Acebutolol, Atenolol, Carteolol, Labetalol
- Abstract
Beta blockers are a class of drugs commonly used to treat heart-related diseases; they are also regulated under the World Anti-Doping Agency. Tandem mass spectrometry is often used in the pharmaceutical industry, clinical analysis laboratory, and antidoping laboratory for detection and characterization of drugs and their metabolites. A deeper chemical understanding of dissociation pathways may eventually lead to an improved ability to predict tandem mass spectra of compounds based strictly on their chemical structure (or vice versa), which is especially important for characterization of unknowns such as emerging designer drugs or novel metabolites. In addition to providing insights into dissociation pathways, the use of energy-resolved breakdown curves can produce improved selectivity and lend insights into optimal fragmentation conditions for liquid chromatography-tandem mass spectrometry LC-MS/MS workflows. Here, we perform energy-resolved collision cell and multistage ion trap collision-induced dissociation-mass spectrometry (CID-MS) experiments, along with complementary density functional theory calculations, on five beta blockers (acebutolol, atenolol, bisoprolol, carteolol, and labetalol), to better understand the details of the pathways giving rise to the observed MS/MS patterns. Results from this work are contextualized within previously reported literature on these compounds. New insights into the formation of the characteristic product ion m/z 116 and the pathway leading to characteristic loss of 77 u are highlighted. We also present comparisons of breakdown curves obtained via qToF, quadrupole ion trap, and in-source CID, allowing for differences between the data to be noted and providing a step toward allowing for improved selectivity of breakdown curves to be realized on simple instruments such as single quadrupoles or ion traps., (© 2023 John Wiley & Sons, Ltd.)
- Published
- 2023
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16. 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]
- Published
- 2018
- Full Text
- View/download PDF
17. 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
- Subjects
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
18. Formulation of carteolol chitosomes for ocular delivery: formulation optimization, ex-vivo permeation, and ocular toxicity examination
- Author
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Syed Sarim Imam, Mohammad Javed Ansari, Omar Awad Alsaidan, Mohammed Salahuddin, Sultan Alshehri, Nabil K. Alruwaili, Khalid Saad Alharbi, Ameeduzzafar Zafar, Mohammed Elmowafy, and Mohd Yasir
- Subjects
genetic structures ,General Medicine ,Permeation ,Toxicology ,Residence time (fluid dynamics) ,eye diseases ,Ocular toxicity ,Chitosan ,chemistry.chemical_compound ,chemistry ,medicine ,Carteolol ,sense organs ,Duration of effect ,Suspension (vehicle) ,Ex vivo ,Biomedical engineering ,medicine.drug - Abstract
Background:Conventional delivery systems like solution and suspension are commonly used for the treatment of ocular diseases but have low corneal residence time and hence the duration of effect is ...
- Published
- 2021
- Full Text
- View/download PDF
19. Comparison of the 24-h efficacy and safety of fixed combination carteolol/latanoprost and timolol/latanoprost in patients with primary open-angle glaucoma and ocular hypertension: a prospective crossover study
- Author
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Yuta Saito, Yoshiyuki Shibasaki, Makoto Aihara, Nobuharu Kishimoto, Yoshihiro Wada, and Junichiro Kizaki
- Subjects
medicine.medical_specialty ,Intraocular pressure ,genetic structures ,Timolol ,Ocular hypertension ,chemistry.chemical_compound ,Ophthalmology ,medicine ,Humans ,Carteolol ,Prospective Studies ,Latanoprost ,Antihypertensive Agents ,Intraocular Pressure ,Cross-Over Studies ,business.industry ,General Medicine ,medicine.disease ,Crossover study ,eye diseases ,Drug Combinations ,Treatment Outcome ,Prostaglandin analog ,Blood pressure ,chemistry ,Prostaglandins F, Synthetic ,Ocular Hypertension ,sense organs ,business ,Glaucoma, Open-Angle ,medicine.drug - Abstract
To evaluate the 24-h efficacy and safety of fixed combination carteolol/latanoprost (LCFC) and timolol/latanoprost (LTFC) in patients with primary open-angle glaucoma and ocular hypertension.Prospective, randomized, crossover study METHODS: Twenty-two patients pretreated with a prostaglandin analog at baseline were randomly assigned at a 1:1 ratio to either LCFC or LTFC treatment. The patients received the assigned study drug in both eyes daily in the evening (20:00). Each treatment group crossed over after a 2-month treatment period. The 24-h curves of intraocular pressure (IOP), pulse rate, and blood pressure were evaluated. Safety was also assessed.The changes in mean daytime IOP from baseline at the end of the 2-month treatment period in the LCFC and LTFC groups were - 0.93 and - 1.15 mmHg, respectively. The changes in peak IOP in the 2 groups were - 0.91 and - 0.68 mmHg, respectively. The nighttime pulse rate in the LCFC group increased; that in the LTFC group was lower at all time points. The changes in pulse rate from baseline at 22:00, 2:00, 4:00, and 6:00 differed statistically between the 2 groups. No differences in changes from baseline in systolic and diastolic blood pressures were found between the groups.The 24-h IOP curve of patients in the LCFC group was similar to that of the LTFC group, but on the basis of the pulse rate findings, the effect of LCFC on the cardiovascular system over 24 h was less than that of LTFC.
- Published
- 2021
- Full Text
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20. 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]
- Published
- 2023
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21. New Cardiovascular Research Study Results Reported from Nagasaki University (Life-threatening Vasospastic Angina Induced By Carteolol Eye Drops).
- Subjects
EYE drops ,OCULAR hypertension ,ANGINA pectoris ,MEDICAL personnel ,INFORMATION professionals ,AMINO alcohols - Abstract
A research study conducted at Nagasaki University in Japan has found that the use of carteolol eye drops, a nonselective beta-blocker commonly used for glaucoma and ocular hypertension, can induce life-threatening vasospastic angina (VSA). The study reported a case in which a patient developed VSA after starting carteolol eye drops, and the symptoms resolved once the eye drops were discontinued. This research highlights the potential systemic effects of ophthalmic beta-blockers on VSA and provides important information for healthcare professionals and patients. The study has been peer-reviewed and published in the journal Internal Medicine. [Extracted from the article]
- Published
- 2023
22. 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.
- Published
- 2017
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23. 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
- Subjects
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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24. Bradycardia Shock Caused by the Combined Use of Carteolol Eye Drops and Verapamil in an Elderly Patient with Atrial Fibrillation and Chronic Kidney Disease
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Naotaka Akutsu, Nobuhiro Murata, Masaki Monden, Yasuo Okumura, Riku Arai, and Daisuke Fukamachi
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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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25. 'The Use Of Substances For The Treatment Of Loss Of Eyesight In Humans With Glaucoma And Other Degenerative Eye Diseases' in Patent Application Approval Process (USPTO 20200085906)
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Emedastine -- Intellectual property ,Levocabastine ,Physical fitness ,Ophthalmic agents -- Intellectual property ,Trifluridine -- Intellectual property ,Oxytetracycline -- Intellectual property ,Povidone -- Intellectual property ,Amino acids -- Intellectual property ,Blindness ,Pindolol -- Intellectual property ,Alzheimer's disease ,Glaucoma ,Eye diseases ,Brinzolamide ,Diseases ,Obesity ,Bimatoprost ,Carteolol ,Editors ,Health - Abstract
2020 APR 11 (NewsRx) -- By a News Reporter-Staff News Editor at Obesity, Fitness & Wellness Week -- A patent application by the inventor RUSS, HERMANN (Altendorf, CH), filed on [...]
- Published
- 2020
26. Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops.
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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.
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- 2023
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27. Short-Term Efficacy and Safety of Switching from a Latanoprost/Timolol Fixed Combination to a Latanoprost/Carteolol Fixed Combination
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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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28. Toxicity profiles of fixed-combination eye drops for glaucoma therapy using cultivated human corneal epithelial sheets
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Makoto Aihara, Kohdai Kitamoto, Tomohiko Usui, and Yumi Hashimoto
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medicine.medical_specialty ,genetic structures ,Cell Survival ,Brinzolamide ,Timolol ,chemistry.chemical_compound ,Microscopy, Electron, Transmission ,Dorzolamide ,Ophthalmology ,Electric Impedance ,medicine ,Humans ,Carteolol ,Viability assay ,Latanoprost ,Antihypertensive Agents ,Cells, Cultured ,Epithelium, Corneal ,Tafluprost ,Glaucoma ,General Medicine ,eye diseases ,Drug Combinations ,chemistry ,sense organs ,Travoprost ,Ophthalmic Solutions ,medicine.drug - Abstract
We aimed to investigate the toxicity of 6 fixed-combination drugs for glaucoma therapy using human corneal epithelial sheets (HCES). Experimental. We used 6 kinds of commercially available fixed-combination drugs: latanoprost/carteolol (LAT/CAR), latanoprost/timolol (LAT/TIM), tafluprost/timolol (TAF/TIM), travoprost/timolol (TRA/TIM), brinzolamide/timolol (BRZ/TIM), and dorzolamide/timolol (DRZ/TIM) including different preservatives. The cell viability and barrier function of the HCES after exposure to the eye drops for 10 or 30 minutes were assessed using the WST-1 assay and transepithelial electrical resistance (TEER) measurements, respectively. The HCES were also evaluated using hematoxylin and eosin (HE) staining and transmission electron microscopy. The cell viability significantly decreased in the HCES treated with LAT/TIM or DRZ/TIM after 10 and 30 minutes and in those treated with BRZ/TIM after 30 minutes. The barrier function increased significantly in the HCES treated with LAT/CAR. Histologically, the HCES were damaged after treatment with LAT/TIM, BRZ/TIM, or DRZ/TIM for 30 minutes. Transmission electron microscopy indicated narrow intercellular spaces and multiple intercellular junctions in the HCES treated with LAT/CAR, TAF/TIM, or TRA/TIM. The HCES treated with DRZ/TIM, BRZ/TIM, or LAT/TIM contained cytoplasmic vacuoles and collapsed cellular structures. Glaucoma fixed-combination eye drops demonstrated a different toxic effect on the cell viability, barrier function, and morphologic changes of HCES.
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- 2020
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29. Topical ophthalmic beta-blockers are associated with ocular pseudopemphigoid: A pharmacovigilance study of antiglaucoma medications utilising the FDA adverse event reporting system
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Patrick Michael Jedlowski and Mahdieh Fazel Jedlowski
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Pharmacovigilance ,Antiglaucoma Agents ,Adrenergic beta-Antagonists ,Preservatives, Pharmaceutical ,Irritants ,Humans ,Dermatology ,Ophthalmic Solutions ,Carteolol ,Betaxolol - Abstract
The association between antiglaucoma medications and the development of ocular pseudopemphigoid (OPP) has been described; however, the independent risk of each medication has not been quantified.Case/non-case analyses were performed in the FDA Adverse Events Reporting System (FAERS) using data from 2010-2020 to examine the reporting odds ratio (ROR) signal for OPP for all classes of antiglaucoma medications under multiple conditions: (i) comparison to all other drugs in FAERs, (ii) comparison to other antiglaucoma medications, (iii) comparison to vehicle/hydrating eye drops with cases of OPP and (iv) comparison to vehicle/hydrating eyedrops with and without cases of OPP to control for topical irritant and preservative effects.A statistically significant ROR for OPP was found for aggregate antiglaucoma medications under the first condition but not the third or fourth (i.96.97 (95% CI 52.54-178.98). The largest signal for OPP when compared to other glaucoma drugs and eye drops was seen with unoprostone (ii.68.96 (95% CI 8.35-569.50, iii.39.85 (95% CI 4.14-383.33), iv.581.67 (95% CI 49.38-6851.57) followed by carteolol (ii.32.51(95% CI 9.02-117.67), iii.10.67 (95% CI 1.77-64.13), iv.77.84 (95% CI 12.95-467.78) and betaxolol (ii.23.38 (95% CI 7.28-74.46), iii.6.94 (95% CI 1.27-38.01), iv.50.67 (95% CI 9.26-277.25). A statistically significant ROR was noted only for the beta-blockers class aggregate under conditions ii and iv.Our findings support an association between OPP and antiglaucoma medications; under the most stringent control for topical irritant/preservative effect by of comparison to topical eye drops, unoprostone, carteolol, betaxolol and timolol all had a significant ROR for OPP.
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- 2022
30. New Drug Research Study Findings Have Been Reported by Researchers at University of Yamanashi (Persistence of the Carteolol Hydrochloride/latanoprost Fixed-combination Ophthalmic Solution, Compared With the Other Beta-blocker/prostanoid Fp...).
- Abstract
Keywords: Yamanashi; Japan; Asia; Drug Research; Amino Alcohols; Carteolol; Health and Medicine; Medical Devices; Ophthalmic Solution; Organic Chemicals; Pharmaceutical Solutions; Phenoxypropanolamines; Propanolamines EN Yamanashi Japan Asia Drug Research Amino Alcohols Carteolol Health and Medicine Medical Devices Ophthalmic Solution Organic Chemicals Pharmaceutical Solutions Phenoxypropanolamines Propanolamines 1022 1022 1 09/19/23 20230924 NES 230924 2023 SEP 22 (NewsRx) -- By a News Reporter-Staff News Editor at Medical Devices & Surgical Technology Week -- Current study results on Drug Research have been published. According to the news editors, the research concluded: "The study results suggest that persistence rates vary depending on the BB/FP and CAR/LAT appears to be more persistent than other BB/FP.". [Extracted from the article]
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- 2023
31. New Eye Proteins Study Findings Recently Were Reported by Researchers at Ocean University of China (Carteolol Triggers Senescence Via Activation of Beta-arrestin-erk-nox4-ros Pathway In Human Corneal Endothelial Cells In Vitro).
- Abstract
Keywords: Shandong; People's Republic of China; Asia; Amino Alcohols; Arrestins; Carteolol; Endothelial Cells; Eye Proteins; Immunology; Membrane Proteins; Organic Chemicals; Phenoxypropanolamines; Propanolamines; Surface Antigens EN Shandong People's Republic of China Asia Amino Alcohols Arrestins Carteolol Endothelial Cells Eye Proteins Immunology Membrane Proteins Organic Chemicals Phenoxypropanolamines Propanolamines Surface Antigens 706 706 1 08/07/23 20230811 NES 230811 2023 AUG 11 (NewsRx) -- By a News Reporter-Staff News Editor at Genomics & Genetics Weekly -- New research on Proteins - Eye Proteins is the subject of a report. Shandong, People's Republic of China, Asia, Amino Alcohols, Carteolol, Arrestins, Endothelial Cells, Eye Proteins, Immunology, Membrane Proteins, Organic Chemicals, Phenoxypropanolamines, Surface Antigens, Propanolamines. [Extracted from the article]
- Published
- 2023
32. Cystoid Macular Edema Associated with Omidenepag Isopropyl in Phakic Eyes after Laser Iridotomy: A Case Report
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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
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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
33. Cytotoxicity of carteolol to human corneal epithelial cells by inducing apoptosis via triggering the Bcl-2 family protein-mediated mitochondrial pro-apoptotic pathway.
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Shan, Ming and Fan, Ting-Jun
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- *
THERAPEUTICS , *HYPERTENSION , *QUINOLINE , *EPITHELIAL cells , *CELL-mediated cytotoxicity , *DRUG toxicity , *APOPTOSIS , *BCL-2 proteins - Abstract
Carteolol is a frequently used nonselective β-adrenoceptor antagonist for glaucoma and ocular hypertension treatment, and its repeated/prolonged usage might be cytotoxic to the cornea, especially the outmost human corneal epithelium (HCEP). The aim of the present study was to characterize the cytotoxicity of carteolol to HCEP and its underlying cellular and molecular mechanisms using an in vitro model of HCEP cells. After HCEP cells were treated with carteolol at concentrations varying from 2% to 0.015625%, the cytotoxicity, apoptosis-inducing effect and pro-apoptotic pathway was investigated, respectively. Our results showed that carteolol at concentrations above 0.03125% induced time- and dose-dependent growth retardation, cytopathic morphological changes and viability decline of HCEP cells. Moreover, carteolol induced G 1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, and apoptotic body formation of HCEP cells. Furthermore, carteolol also induced activation of caspase-9 and − 3, disruption of mitochondrial transmembrane potential, up-regulation the cytoplasmic amount of cytochrome c and apoptosis-inducing factor, and up-regulation of pro-apoptotic Bax and Bad, down-regulation of anti-apoptotic Bcl-2 and Bcl-xL. In conclusion, carteolol above 1/64 of its clinical therapeutic dosage has a time- and dose-dependent cytotoxicity to HCEP cells, which is achieved by inducing apoptosis via triggering Bcl-2 family protein-mediated mitochondrial pro-apoptotic pathway. [ABSTRACT FROM AUTHOR]
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- 2016
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34. Formulation of carteolol chitosomes for ocular delivery: formulation optimization
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Ameeduzzafar, Zafar, Nabil K, Alruwaili, Syed Sarim, Imam, Omar Awad, Alsaidan, Khalid Saad, Alharbi, Mohd, Yasir, Mohammed, Elmowafy, Mohammad Javed, Ansari, Mohammed, Salahuddin, and Sultan, Alshehri
- Subjects
Cornea ,Chitosan ,Drug Liberation ,Time Factors ,Goats ,Adrenergic beta-Antagonists ,Liposomes ,Animals ,Humans ,Administration, Ophthalmic ,Carteolol ,Glaucoma, Open-Angle - Published
- 2021
35. Retinal Vessel Density Changes on Optical Coherence Tomography Angiography and Predictive Factors in Normal-Tension Glaucoma Treated with Topical Beta-Blocker
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Lan-Hsin Chuang, Shih-Ming Huang, Lung-Chien Chen, and Yun-Hsuan Lin
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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
36. 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
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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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37. 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
- Subjects
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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38. Carteolol hydrochloride reduces visible light-induced retinal damage invivo and BSO/glutamate-induced oxidative stress invitro
- Subjects
Male ,Light ,Swine ,Adrenergic beta-Antagonists ,Radiation-Protective Agents ,Retina ,Cell Line ,Rats ,Mice ,Oxidative Stress ,Animals ,Carteolol ,Reactive Oxygen Species ,Antihypertensive Agents - Published
- 2019
39. A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride.
- Author
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Hashikawa Y, Kato Y, Kaji H, Abe T, and Nagai N
- 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., 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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40. Carteolol hydrochloride reduces visible light-induced retinal damage invivo and BSO/glutamate-induced oxidative stress invitro.
- Published
- 2020
41. [Type IV hypersensitivity to timolol]
- Author
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Silvio, Espínola and Dory, Mora
- Subjects
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.
- Published
- 2021
42. Optical Coherence Tomography Angiography Vessel Density Changes in Normal-tension Glaucoma Treated With Carteolol, Brimonidine, or Dorzolamide
- Author
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Shih-Ming Huang, Yun-Hsuan Lin, Wei-Wen Su, Lung-Chien Chen, and Lan-Hsin Chuang
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Male ,Retinal Ganglion Cells ,medicine.medical_specialty ,genetic structures ,Nerve fiber layer ,Glaucoma ,Thiophenes ,chemistry.chemical_compound ,Nerve Fibers ,Dorzolamide ,Normal tension glaucoma ,Ophthalmology ,medicine ,Humans ,Carteolol ,Fluorescein Angiography ,Intraocular Pressure ,Retrospective Studies ,Sulfonamides ,business.industry ,Brimonidine ,Angiography ,Retinal Vessels ,Retinal ,medicine.disease ,eye diseases ,medicine.anatomical_structure ,chemistry ,Brimonidine Tartrate ,Optic nerve ,Female ,sense organs ,Visual Fields ,business ,Glaucoma, Open-Angle ,Tomography, Optical Coherence ,medicine.drug - Abstract
Precis In patients with normal-tension glaucoma, topical dorzolamide might enhance the vessel density (VD), topical carteolol decreased the VD in the inferior-temporal peripapillary retina, whereas topical brimonidine did not change the VD. Purpose Topical anti-glaucoma medications may improve ocular perfusion pressure or micro-circulation in the optic nerve head. The study evaluated the responses of the retinal vessel density (VD) to topical carteolol, brimonidine, and dorzolamide in normal-tension glaucoma (NTG) using optical coherence tomography angiography (OCTA). Patents and methods This is a retrospective non-randomized, comparative study. The study included 131 individuals (77 men, 54 women) diagnosed with NTG, without systemic medication usage, who visited the glaucoma clinic of Chang Gung Memorial Hospital, Taiwan between January 2019 and May 2020. If both eyes were diagnosed with NTG, only the right eye was included. Of these, there were 80 carteolol-treated eyes, 27 brimonidine-treated eyes, and 24 dorzolamide-treated eyes. We studied the response of OCTA parameters and retinal nerve fiber layer (RNFL) thickness to drugs, six months after treatment. Results In dorzolamide-treated eyes, increases in the peripapillary superficial retinal VD, especially in the superior-nasal area, were significant; however, no RNFL thickness changes were observed. In contrast, the superficial retinal VD decreased at the inferior-temporal peripapillary area, and RNFL thickness decreased in the inferior-nasal paripapillary area of the carteolol-treated eyes. Finally, in brimonidine-treated eyes, changes in either VD parameters or RNFL thickness were not significant. Conclusions Topical dorzolamide possibly enhanced the VD of the peripapillary retina in NTG eyes. On the contrary, topical carteolol possibly decreased VD in the inferior-temporal peripapillary retina. Finally, in cases treated with topical brimonidine, the peripapillary microcirculation remained unchanged. The study shows preliminary results, future large-scaled studies are warranted to confirm the findings.
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- 2021
43. 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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44. 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
45. Tohoku University Graduate School of Medicine Researchers Describe New Findings in Science and Technology (A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride).
- Abstract
Amino Alcohols, Biological Factors, Biological Pigments, Carteolol, Organic Chemicals, Phenoxypropanolamines, Propanolamines, Retinal Pigments, Science, Science and Technology Keywords: Amino Alcohols; Biological Factors; Biological Pigments; Carteolol; Organic Chemicals; Phenoxypropanolamines; Propanolamines; Retinal Pigments; Science; Science and Technology EN Amino Alcohols Biological Factors Biological Pigments Carteolol Organic Chemicals Phenoxypropanolamines Propanolamines Retinal Pigments Science Science and Technology 2738 2738 1 03/27/23 20230331 NES 230331 2023 MAR 31 (NewsRx) -- By a News Reporter-Staff News Editor at Drug Week -- Current study results on science and technology have been published. [Extracted from the article]
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- 2023
46. 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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47. 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
48. 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
49. Lens-induced myopization and intraocular pressure in young guinea pigs
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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
50. Short-term Efficacy and Safety of a Latanoprost/Carteolol Fixed Combination Switched From Concomitant Therapy to in Patients With Primary Open-angle Glaucoma or Ocular Hypertension
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Goji Tomita, Kyoko Ishida, Mayumi Iwasa, Minako Shiokawa, and Kenji Inoue
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Adult ,Male ,medicine.medical_specialty ,genetic structures ,Open angle glaucoma ,Glaucoma ,Ocular hypertension ,Carteolol Hydrochloride ,Tonometry, Ocular ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Surveys and Questionnaires ,Ophthalmology ,Concomitant Therapy ,medicine ,Humans ,Carteolol ,Prospective Studies ,Latanoprost ,Antihypertensive Agents ,Intraocular Pressure ,Aged ,Aged, 80 and over ,Drug Substitution ,business.industry ,Middle Aged ,medicine.disease ,eye diseases ,Drug Combinations ,Treatment Outcome ,chemistry ,Concomitant ,030221 ophthalmology & optometry ,Drug Therapy, Combination ,Female ,Ocular Hypertension ,sense organs ,business ,Glaucoma, Open-Angle ,030217 neurology & neurosurgery ,Follow-Up Studies ,medicine.drug - Abstract
We prospectively investigated the efficacy and safety of switching from concomitant latanoprost and carteolol hydrochloride (CH) to a latanoprost/carteolol fixed combination (LCFC) in patients with primary open-angle glaucoma or ocular hypertension.A total of 43 patients (43 eyes) who were using latanoprost (once daily in the evening) and CH (once daily in the morning) concomitantly were switched to LCFC (once daily in the morning) with no washout interval. The primary efficacy endpoint was change in intraocular pressure (IOP) between baseline (before switching) and 1 and 3 months after switching. Systemic blood pressure and pulse rate, corneal epithelial defects, and tear film break-up time (TBUT) were also compared before and 1 and 3 months after switching. A questionnaire was administered 1 month after switching to investigate ocular comfort and treatment preferences. Adverse reactions and dropouts were recorded.There was no significant difference in IOP after switching to LCFC (15.0±2.6, 15.1±2.4, and 15.0±2.4 mm Hg at baseline and at 1 and 3 months, respectively). There was a significant decrease in corneal epithelial defects and significant increase in TBUT, without significant changes in systemic blood pressure or pulse rate. Three patients (7.3%) preferred concomitant latanoprost and CH; 33 (80.5%) preferred the LCFC. One patient each (9.3%) discontinued treatment because of foreign body sensation, blepharitis, increased IOP, or loss to follow-up.Switching from concomitant latanoprost and CH to LCFC led to similar IOP control with good safety and patient acceptance, at least in the short term.
- Published
- 2018
- Full Text
- View/download PDF
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