Carteolol Research Articles

Clinical Observation of Carteolol Hydrochloride Eye Drops Combined with Travoprost Eye Drops in the Treatment of Open-Angle Glaucoma

Clinical Observation of Carteolol Hydrochloride Eye Drops Combined with Travoprost Eye Drops in the Treatment of Open-Angle Glaucoma

Timing and Efficacy Evaluation of 755-nm Long Pulse Alexandrite Laser and 2% Carteolol Hydrochloride Eye Drops Co-Treatment for Thicker Superficial Infantile Hemangioma.

Superficial Infantile hemangioma (SIH) is the most common type of IH. Some studies have shown the efficacy of 755-nm long pulse alexandrite laser (LPAL) and topical 2% carteolol hydrochloride (C-HCL) eye drops for the treatment of SIH. This article retrospectively analyzes the safety and efficacy of 755-nm LPAL combined with 2% C-HCL eye drops for treating thicker SIH, and explores the optimal treatment time for SIH. This study included 2-5 mm thick SIH patients who received co-treatment of 755-nm LPAL and 2% C-HCL eye drops. The SIH patients were divided into 3 groups based on their age and IH growth curve: ≤ 1 month (≤ 1M), 1-3 months (excluding 1 month; 1-3M), and 3-12 months (excluding 3 months; 3-12M). There was no difference in efficacy between the ≤ 1M and the 1-3M group, and were both better than the 3-12M group. Furthermore, there was no difference in the average number of treatments between the ≤ 1M and 1-3M groups and were both less than the 3-12M group. There was no significant difference in the incidence of adverse reactions between the groups. Compared with the ≤ 1M and 1-3M groups, the 3-12M group indicated more permanent skin lesions after the treatment. It was revealed that co-treatment with 755-nm LPAL and 2% C-HCL eye drops is safe and effective against thicker SIH. Compared with the 3-12M group, ≤ 3 months can achieve better efficacy, requires a shorter treatment time, less likely to leave permanent skin lesions such as scars. Moreover, patients with no proliferation can be observed to 1 month.

A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride

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.

Therapeutic potential of pupilloplasty combined with phacomulsification and intraocular lens implantation against uveitis-induced cataract.

To evaluate the therapeutic effect of pupilloplasty combined with phacomulsification and intraocular lens implantation (PPI) in uveitis-induced cataract. Total 28 patients with uveitis-induced cataract were enrolled. Within 3mo before the PPI, 7 cases accompanied with glaucoma maintained carteolol hydrochloride for lowering intraocular pressure, and 1 case maintained glucocorticoid for anti-inflammation. The baseline characteristics, treatment processes, and outcomes of enrolled cases were retrospectively analyzed. Hematoxylin and eosin (HE) staining was performed to reveal the histopathological changes of iris tissues. Iris hemorrhage was the only intraoperative complication observed in 2 cases. After the surgery, normal intraocular pressure, right position of intraocular lens, and improved visual gain [best corrected visual acuity (BCVA)>0.5] were achieved. Postoperative keratic precipitates was observed in 2 cases, which was recovered within 1wk. During the follow-up of 5-10y, no recurrence of uveitis was found in 27 cases (96.43%). Uveitis only recurred in one case with the onset of ankylosing spondylitis. HE staining showed iris stroma (all samples), pigment cell hyperplasia in pigment epithelium (n=9) and stroma (n=19), inflammatory cell infiltration in iris (n=7), and neovascularization in iris surface (n=2). PPI improves the visual gain and prevents the long-term recurrence of uveitis in patients with uveitis-induced cataract, including those with preoperative intraocular pressure abnormality (glaucoma) and inflammation (active uveitis). Uveitis presents stroma atrophy, pigment cell hyperplasia, and inflammatory cell infiltration, even in a quiet state.

Severe hypoglycemic attack exacerbated by carteolol hydrochloride ophthalmic solution in Langerhans cell histiocytosis

Severe hypoglycemic attack exacerbated by carteolol hydrochloride ophthalmic solution in Langerhans cell histiocytosis

A Comparative Study between a Transscleral Sustained-Release Device and Eyedrops on Intraocular Distribution of Carteolol Hydrochloride

A Comparative Study between a Transscleral Sustained-Release Device and Eyedrops on Intraocular Distribution of Carteolol Hydrochloride

Formulation of carteolol chitosomes for ocular delivery: formulation optimization, ex-vivo permeation, and ocular toxicity examination

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.

Research and correlation analysis on the dripper contamination of carteolol hydrochloride eye drops.

Multi-dose eye drops are easily contaminated by microorganisms, and reportedly, the highest contamination rate can reach 96.46%. The use of contaminated eye drops can cause serious eye infections. Carteolol hydrochloride eye drops provided by glaucoma patients who visited the ophthalmic clinic of the First Affiliated Hospital of Soochow University from May 2018 to December 2019 were collected. Microbial culture was carried out on the eye drops, and the microbial species were identified by standard procedures. At the same time, the unsealing time, storage method, hand cleaning before dripping, and contact with the eyelid or the surrounding environment during infusion were recorded. Univariate and multivariate logistic regression analyses were used to analyze the risk factors associated with the contamination of carteolol hydrochloride eye drops. A total of 244 bottles of carteolol hydrochloride eye drops were collected, and the positive rate of flora culture was 6.6%. A total of 18 strains of bacteria were isolated. The most common bacteria were Staphylococcus epidermidis and Corynebacterium. Univariate analysis showed that the risk factors associated with contamination were the unsealing time, the frequency of daily use, contact with the eyelid or the surrounding environment during the infusion process, and the use of more than 2 kinds of eye drops at the same time. Multivariate analysis showed that the unsealing time, the frequency of daily use, and contact with the eyelid or the surrounding environment were independent risk factors associated with contamination. A long unsealing time, frequent use, and non-standard operation can increase the risk of eye drop contamination, which cannot be ignored.

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.

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.

Efficacy of the combination of carteolol hydrochloride + latanoprost in the treatment of glaucoma and ocular hypertension

ABSTRACTIntroduction: The only evidence-based mechanism for prevention and treatment of glaucomatous optic neuropathy is decreasing the intraocular pressure (IOP). Prescribing multiple ocular hypotensive agents, such as the combination of carteolol and latanoprost, may synergistically improve IOP; however, doing so may increase the complexity of a medication regimen, in turn, impairing patient adherence. Fixed-combination glaucoma medications offer convenience and effectiveness. New to this class of glaucoma medication is fixed combination carteolol-latanoprost (FCCL).Area covered: This review intends to give the reader a better understanding of the efficacy of the combination of carteolol and latanoprost separately, and where FCCL fits into the vast medical arsenal of IOP drops. Furthermore, it outlines the particular pharmacologic mechanisms targeted, the pharmacokinetics, effectiveness, the advantages of fixed-combination administration, and tolerability.Expert opinion: The combination of carteolol and latanoprost, separately or in a fixed-combination, is more effective than either drug alone. Given the early stage in development of FCCL, it has yet to be determined how FCCL compares to other fixed-combination medications. However, pending further approval, fixed-combination carteolol-latanoprost may represent a reasonable alternative for a patient whose IOP is inadequately controlled on a prostaglandin analog alone and for whom a simplified combination is preferred.

Effect of long-term topical latanoprost medication on conjunctival thickness in patients with glaucoma.

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. 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. 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<0.001) in the latanoprost group. At 2-year follow-up, no statistically difference was found in CET (62.24±5.27 µm; t=1.086, P=0.282) or CT (201.23±12.45 µm; t=1.44, P=0.154) compared to it at baseline (CET: 61.23±5.42 µm; CT: 198.76±13.68 µm, respectively) in the carteolol group. A significant decrease in conjunctival thickness is found in glaucoma patients treated with long-term topical latanoprost; its potential effect on the outcome of filtration surgery should be considered.

A prospective study of topical carteolol therapy in Chinese infants with superficial infantile hemangioma.

To report our observations from a trial of the short-term effectiveness and safety of topical carteolol hydrochloride drops to treat infantile hemangiomas (IHs). From October 2012 to September 2015, the study recruited 349 children with superficial IHs. Participants were randomized to two groups: treatment (n=224 who received 2% carteolol hydrochloride drops administered to the lesion surface twice daily) and observation (n=125 who did not receive treatment). Therapy duration was 6months. The mean age at the beginning of treatment was 3.2months. Treatment responses were categorized as class 1 (total regression), class 2 (partial regression or controlled growth), or class 3 (no response). Of infants receiving carteolol treatment, 10.7% (24 patients) were categorized as class 1, 72.3% (162 patients) as class 2, and 17.0% (38 patients) as class 3. Of infants in the observation group, 5.6% (7 patients) were categorized as class 1, 25.6% (32 patients) as class 2, and 68.8% (86 patients) as class 3. No adverse effects were noted during treatment. Carteolol is an effective, safe topical treatment for superficial IHs. Carteolol may be used to treat proliferative superficial IHs, particularly in infants younger than 6months.

A new modification method of a Cetyl Trimethyl Ammonium Bromide/Nano-ZnO and Multi-walled Carbon Nanotubes Electrode for Determination of Anti Doping in Urine

The preparation and application of Cetyl Trimethyl Ammonium Bromide/Nano-ZnO and Multi-walled Carbon Nanotubes (CTAB/ZnO-MWNTs) Modified Electrodes was studied, establishing a new electrochemical method for determination of carteolol hydrochloride in urine. After its pre-enrichment by adsorption and extraction on modified electrodes, electrochemical behaviors of carteolol hydrochloride on the modified electrodes were studied by CV and DPV. The response is linear at the range of 1×10-3 ∼ 2×10-1 g/L, with a detection limit of 2×10-4 g/L. Under appropriate conditions, the content of carteolol hydrochloride in urine can be determined directly by the method, which had strong anti-interference ability and the recovery is 96.5% - 110.5%. In addition, extraction and adsorption behaviors of the modified electrodes for carteolol hydrochloride were studied by chronocoulumetry, and the results showed that extraction during the enrichment process played a major role at low concentrations, and contribution of surface adsorption became greater with the increase of concentrations.

Determination of Carteolol in Pure and Pharmaceutical Formulation by Spectrophotometric Method

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.

Development and validation of UPLC/ESI-Q-TOF-MS for carteolol in aqueous humour: Stability, stress degradation and application in pharmacokinetics of nanoformulation

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 (100.0×2.1mm; 1.7μm) column with a mobile phase of acetonitrile – 2mM (milli mole) ammonium acetate (90/10, v/v) over 3min 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 1–1000ng/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.

Spectroscopic studies on the interaction of carteolol hydrochloride and urea-induced bovine serum albumin

The interaction of carteolol hydrochloride, to 0.2molL−1 urea-induced bovine serum albumin in aqueous solution has been first investigated by fluorescence spectra and ultraviolet–visible (UV–vis) spectra at pH 7.40. The quenching mechanism, binding parameter and sites (n), the binding mode (ΔG, ΔH, and ΔS) as well as the binding distance (r) have been obtained according to the experimental results. We also use the synchronous fluorescence method to study the effect of CTL on the conformation change of urea-induced BSA.

Preparation of carteolol hydrochloride matrix sustained-release pellets and evaluation in vitro/in vivo

The aim of this study was to prepare carteolol hydrochloride matrix sustained-release pellets, and to compare its performance in vivo with carteolol common tablets. The formula was optimized according to the roundness and the release of pellets with single-factor, and orthogonal test. The carteolol hydrochloride matrix sustained-release pellets were got by extrusion-spheronisaion, while the release rate in vitro was determined by rotate basket method with UV detection. The carteolol hydrochloride sustained release property was studied in New Zealand white rabbits after oral administration. The optimized prescription is composed of carteolol hydrochloride 5.5 g, MCC 6.0 g, SA 26.3 g, EC 21.0 g, CMC-Na 1.2 g. Drug release property in vitro were as follows: the release time is over 12 h, the drug release behaviors follow the first order equation and the process of drug releasing is drug diffusion with frame erosion. The Cmax, Tmax and AUC(0→24) of the pellets were 2.58 ± 0.43 (mg/ml), 4.20 ± 0.87 (h) and 22.19 ± 4.23 (mg/ml h), respectively. The Cmax, Tmax and AUC(0→24) of the tablets were 3.75 ± 0.59 (mg/ml), 1.00 ± 0.72 (h) and 18.70 ± 3.75 (mg/ml h). The carteolol hydrochloride sustained-release pellets have reasonable formulation and simple preparation technology; the pellets acquired perfect sustained-release properties in vitro/in vivo. Key words: Carteolol hydrochloride, sustained-release, pellets, in vitro, in vivo, evaluation

Clinical effect of St.John's Wort Extract on intraocular pressure in perioperative period of narrowangle glaucoma

Objective To research the matching factor about intraocular pressure in perioperative period by studying the influence of St. John's Wort Extract to intraocular pressure during this time. Methods The 56 narrow - angle glaucoma patients were charged into St. John's Wort Extract group or control group randomly and all cases were treated with carteolol hydrochloride eyedrop by 2 times and Brinzolamide 3 times every day for lowering IOP in 3 days before operation, while the St. John S Wort Extract 300mg was given to the treatment group' s cases everyday before operation for 3 day. Control group was charged with placebo.The same score before St. John' S Wort Extract and before operation between groups was analysed by t test The IOP Of St. JohnS Wort Extract group and cintrol group 7 day. after operation was contrasted by t test and line that the cirrelation coefficient with SPSS 13.0. Results The difference of IOP between before and after the theory of St. JohnS Wort Extract were charged by t test (t =2.017 P =0.046)and the treatment group was significanly higher(8.91 ±2.73mmHg) than the control group(3.66 ± 1.93mmHg),meanwhile,1 week after operation, the IOP of treatment group(6. 37 ± 2.49mmHg)were significantly lower than control (9.25 ± 1.98),the differnece were significantly showed by t test (t = 2. 009 P =0. 041 ). In operation day, HAMA score of control gronp(13. 35 ±2.58)and treatment group(8.67 ±2.32) showed significant difference (t =2.013 P= 0.044) while HAMA score seems positive correlation to IOP in treatment group and control groups cases in operation day (r1 =0. 397 P1 =0. 046, r2 =415 P2 =0. 033). Conclusion St. John's Wort Extract seems the effect of lower IOP for glaucoma operation through modifing anxiety of narrow-angle glaucoma patients. Key words: St. John's Wort Extract; Perioperative period; Narrow-angle; Glaucoma; anxiety

Clinical observation on secondary glaucoma after silicone oil tamponade

Objective To investigate the risk factors and treatment of silicone oil glaucoma (SOG).Methods Ninety-five eyes of 93 patients who underwent pars plana vitrectomy and silicone oil tamponade were evaluated in this study. The lens was removed in 58 eyes in which intraocular lens (IOL) was implanted in 10 eyes, so 48 eyes were aphakic. Silicone oil tamponade time was ≤6 months in 32 eyes,and ＞6 months in 63 eyes. The follow-up time ranged from 2 to 25 months, with a mean of (9.5±5.1)months. The fundus and intraocular pressure (IOP) were evaluated at 1 week, 2 weeks and 1 month after surgery. The diagnosis of SOG was established if the one-month postoperative IOP ＞ 21 mm Hg (1 mm Hg=0.133 kPa), and primary and neovascular glaucoma were excluded. After the diagnosis of SOG, carteolol hydrochloride and brinzolamide solution were immediately applied to the eye, and intravenous mannitol infusion was performed. If the IOP still can not be controlled after 1 week of such treatment, silicone oil removal surgery will be performed. If removal of silicone oil can not control the IOP,trabeculectomy surgery will be performed. Results SOG occurred in 21 eyes (22.1%), including 5 phakic eyes (10.6% of 47 phakic eyes) and 16 aphakic eyes (33.3% of 48 aphakic eyes) , 3 eyes (9.4% of 32 eyes)with short tamponade time (≤6 months) and 18 eyes (28.6% of 63 eyes) with long tamponade time (＞6months). The average silicone oil tamponade time was (10.8±5.1) months. Emulsification of the silicone oil occurred in 17 eyes (81.0%). After silicone oil removed, IOP was controlled in 17 eyes (81.0%) within one week. Conclusions Aphakic eye and the duration of silicone oil tamponade are the risk factors of SOG.Emulsification of silicone oil is the main cause. Silicone oil removal is an effective way to treat SOG. Key words: Vitrectomy; Silicone oils/adverse effects; Glaucoma/secondary; Risk factors

Effect of topical carteolol on visual function in normal-tension glaucoma

The effects of carteolol hydrochloride on visual function in normal-tension glaucoma (NTG) were investigated. 22eyes of NTG patients were divided into two groups, i.e., (1) a group receiving topical application of 2% carteolol hydrochloride b.i.d. and 2 an unmedicated group. During a 18 month period, intraocular pressure and visual field (measured by Humphrey automated perimetry) were measured every 3 months, and the measurements obtained in the two groups were compared. Analysis of the results revealed a considerable reduction in intraocular pressure in the carteolol group as compared with the control group. The progression of mean deviation tended to be less in the carteolol group, but the intergroup difference in this respect was not statistically significant. However, increase in corrected pattern standard deviation was clearly less pronounced in the carteolol group than in the control group. These results supported the conclusion that carteolol is effective in inhibiting deterioration of the local visual field. This is attributed to increased ocular perfusion due to diminished intraocular pressure, as well as an inhibitory effect upon vasoconstriction in the optic nerve head due to intrinsic sympathomimetic activity, preventing decrease in papillary blood flow and adverse effects upon ocular circulation.