The Experts below are selected from a list of 273 Experts worldwide ranked by ideXlab platform
Haruo Nakamura - One of the best experts on this subject based on the ideXlab platform.
-
effect of Carteolol on silent myocardial ischemia variability in heart rate and the pain modulating system
American Heart Journal, 1997Co-Authors: Bonpei Takase, Hiroyuki Hikita, Akimi Uehata, Kimio Satomura, Akira Kurita, Haruo NakamuraAbstract:To investigate the effects of Carteolol, which is a nonselective β-adrenergic agent with intrinsic sympathomimetic activity, on silent myocardial ischemia, exercise-induced myocardial ischemia, indexes of heart rate variability, and pain-modulating system, 20 patients (mean 60±9 years) with chronic stable angina underwent exercise treadmill testing and 24-hour ambulatory electrocardiographic monitoring during 2 weeks of Carteolol administration (15 mg/day) in a double-blind, placebo-controlled design. Plasma levels of β-endorphin and bradykinin and electrical pain stimulation to the skin were measured at rest and peak exercise. Indexes of heart rate variability of both time-domain and frequency-domain analysis were derived from 24-hour ambulatory electrocardiographic monitoring. Carteolol decreased maximal heart rate responses to daily activities during ambulatory monitoring and significantly reduced the median frequency and duration of silent myocardial ischemic episodes (from 1.0 to 0.0 events/24 hr and from 16 to 0 min/24 hr, respectively). Carteolol significantly decreased the rate-pressure product at rest and during exercise with improving maximal ST segment depression, suggesting amelioration of exercise-induced myocardial ischemia. Carteolol did not significantly affect plasma levels of β-endorphin and bradykinin or pain threshold. It significantly decreased some indexes (standard deviation of all normal sinus R-R intervals in the entire 24-hour recording and standard deviation of the mean of all 5-minute segments of normal R-R intervals of a 24-hour recording) of heart rate variability. These results suggest that Carteolol may reduce total myocardial ischemic burden by the reduction of cardiac oxygen demand during daily activities and exercise stress, while not affecting plasma levels of β-endorphin, bradykinin, and pain threshold. Because Carteolol tended to decrease indexes of heart rate variability, significant caution might be necessary in prescribing the β-blocking agents with intrinsic sympathomimetic activity like Carteolol to patients with potential serious arrhythmia.
-
Effect of Carteolol on silent myocardial ischemia, variability in heart rate, and the pain-modulating system.
American heart journal, 1997Co-Authors: Bonpei Takase, Hiroyuki Hikita, Akimi Uehata, Kimio Satomura, Akira Kurita, Haruo NakamuraAbstract:To investigate the effects of Carteolol, which is a nonselective beta-adrenergic agent with intrinsic sympathomimetic activity, on silent myocardial ischemia, exercise-induced myocardial ischemia, indexes of heart rate variability, and pain-modulating system, 20 patients (mean 60 +/- 9 years) with chronic stable angina underwent exercise treadmill testing and 24-hour ambulatory electrocardiographic monitoring during 2 weeks of Carteolol administration (15 mg/day) in a double-blind, placebo-controlled design. Plasma levels of beta-endorphin and bradykinin and electrical pain stimulation to the skin were measured at rest and peak exercise. Indexes of heart rate variability of both time-domain and frequency-domain analysis were derived from 24-hour ambulatory electrocardiographic monitoring. Carteolol decreased maximal heart rate responses to daily activities during ambulatory monitoring and significantly reduced the median frequency and duration of silent myocardial ischemic episodes (from 1.0 to 0.0 events/24 hr and from 16 to 0 min/24 hr, respectively). Carteolol significantly decreased the rate-pressure product at rest and during exercise with improving maximal ST segment depression, suggesting amelioration of exercise-induced myocardial ischemia. Carteolol did not significantly affect plasma levels of beta-endorphin and bradykinin or pain threshold. It significantly decreased some indexes (standard deviation of all normal sinus R-R intervals in the entire 24-hour recording and standard deviation of the mean of all 5-minute segments of normal R-R intervals of a 24-hour recording) of heart rate variability. These results suggest that Carteolol may reduce total myocardial ischemic burden by the reduction of cardiac oxygen demand during daily activities and exercise stress, while not affecting plasma levels of beta-endorphin, bradykinin, and pain threshold. Because Carteolol tended to decrease indexes of heart rate variability, significant caution might be necessary in prescribing the beta-blocking agents with intrinsic sympathomimetic activity like Carteolol to patients with potential serious arrhythmia.
Masato Matsuo - One of the best experts on this subject based on the ideXlab platform.
-
Carteolol hydrochloride reduces visible light induced retinal damage in vivo and bso glutamate induced oxidative stress in vitro
Journal of Pharmacological Sciences, 2019Co-Authors: Masato Matsuo, Yoshiki Kuse, Kei Takahashi, Keiichi Kuwahara, Masaki Tanito, Sachiko Kaidzu, Masamitsu Shimazawa, Hideaki Hara, Akihiro OhiraAbstract: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.
-
Carteolol hydrochloride reduces visible light-induced retinal damage in vivo and BSO/glutamate-induced oxidative stress in vitro.
Journal of Pharmacological Sciences, 2018Co-Authors: Masato Matsuo, Yoshiki Kuse, Kei Takahashi, Keiichi Kuwahara, Masaki Tanito, Sachiko Kaidzu, Masamitsu Shimazawa, Hideaki Hara, Akihiro OhiraAbstract: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.
Lawrence L Nussbaum - One of the best experts on this subject based on the ideXlab platform.
-
efficacy of Carteolol hydrochloride 1 vs timolol maleate 0 5 in patients with increased intraocular pressure
American Journal of Ophthalmology, 1997Co-Authors: W C Stewart, John S Cohen, Peter A Netland, Howard Weiss, Lawrence L NussbaumAbstract:Purpose To evaluate the ocular hypotensive effect and safety of Carteolol hydrochloride 1% vs timolol maleate 0.5%. Methods One hundred seventy-six patients with ocular hypertension or primary open-angle glaucoma were randomly assigned to receive either Carteolol 1% twice a day or timolol maleate 0.5% solution twice a day in a randomized, double-masked, multicenter, parallel-group, active-control comparison trial during a 3-month period. Results After 12 weeks, Carteolol 1% reduced the mean ± SE intraocular pressure from 25.0 ± 0.3 to 19.5 ± 0.3 mm Hg; timolol maleate 0.5% reduced the mean intraocular pressure from 25.2 ± 0.3 to 19.6 ± 0.3 mm Hg. The mean difference in trough intraocular pressure between Carteolol and timolol maleate of –0.14 mm Hg was not significantly ( P = .745) different (95% confidence limits, –0.97 to 0.70 mm Hg). Trough pulse and blood pressure also showed no consistent statistically significant differences between groups. The 2-hour postdose pulse, however, demonstrated a greater decrease in the timolol maleate than in the Carteolol group ( P P = .039), and the Carteolol group reported fewer ocular symptoms than the timolol maleate group did ( P Conclusions Both Carteolol 1% and timolol maleate 0.5% are highly effective in lowering intraocular pressure when measured at the end of the dosing interval. Carteolol 1% demonstrates an ocular hypotensive effect and safety profile similar to those of timolol maleate 0.5% solution.
-
cardiovascular effects of topical Carteolol hydrochloride and timolol maleate in patients with ocular hypertension and primary open angle glaucoma
American Journal of Ophthalmology, 1997Co-Authors: Peter A Netland, W C Stewart, John S Cohen, Howard Weiss, Lawrence L NussbaumAbstract:Purpose To compare the effects of topical timolol maleate 0.5% and Carteolol hydrochloride 1% on pulse rate and blood pressure. Methods In a randomized, double-masked, parallel-design, multicenter clinical trial, we compared the effects of timolol and Carteolol on pulse rate and blood pressure measured by 24-hour ambulatory blood pressure monitoring in 169 adult patients with either ocular hypertension or primary open-angle glaucoma. Results From noon to 8 PM, baseline mean pulse rate of 82 to 83 beats per minute (bpm) had decreased by 4 to 6 bpm in both groups after 4 weeks of therapy with timolol or Carteolol. From midnight to 4 AM, the pulse rate in the Carteolol group was significantly above baseline ( P = .005), while the timolol group was significantly below baseline ( P P = .002). Conclusions Timolol causes significantly lower mean heart rate during the nighttime and more nocturnal bradycardia than Carteolol does in patients with ocular hypertension and primary open-angle glaucoma. These differences may be because of the intrinsic sympathomimetic activity of Carteolol.
Akihiro Ohira - One of the best experts on this subject based on the ideXlab platform.
-
Carteolol hydrochloride reduces visible light induced retinal damage in vivo and bso glutamate induced oxidative stress in vitro
Journal of Pharmacological Sciences, 2019Co-Authors: Masato Matsuo, Yoshiki Kuse, Kei Takahashi, Keiichi Kuwahara, Masaki Tanito, Sachiko Kaidzu, Masamitsu Shimazawa, Hideaki Hara, Akihiro OhiraAbstract: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.
-
Carteolol hydrochloride reduces visible light-induced retinal damage in vivo and BSO/glutamate-induced oxidative stress in vitro.
Journal of Pharmacological Sciences, 2018Co-Authors: Masato Matsuo, Yoshiki Kuse, Kei Takahashi, Keiichi Kuwahara, Masaki Tanito, Sachiko Kaidzu, Masamitsu Shimazawa, Hideaki Hara, Akihiro OhiraAbstract: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.
Gillian M. Keating - One of the best experts on this subject based on the ideXlab platform.
-
Ocular Carteolol
Drugs & Aging, 2007Co-Authors: Sheridan Henness, Tracy Swainston Harrison, Gillian M. KeatingAbstract:Ocular Carteolol (Mikelan®, Teoptic®, Ocupress®) is a nonselective β-adrenoceptor antagonist with intrinsic sympathomimetic activity (ISA). Ocular Carteolol effectively reduces intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) or ocular hypertension (OH). Twice-daily administration of standard Carteolol has generally similar IOP-lowering efficacy to other ocular β-adrenoceptor antagonists such as timolol, betaxolol and metipranolol in patients with OAG or OH. In addition, long-term treatment with Carteolol has similar efficacy to timolol and betaxolol in terms of reducing IOP and maintaining visual fields in patients with newly diagnosed primary OAG (POAG). The new long-acting formulation of once-daily Carteolol has equivalent efficacy to the standard formulation of Carteolol administered twice daily in patients with OAG or OH. Both the standard and long-acting formulations of ocular Carteolol are generally well tolerated in terms of topical adverse effects involving the eyes or systemic adverse effects involving the cardiovascular system. Thus, twice-daily Carteolol is a well established option in the treatment of glaucoma and OH, and the new once-daily formulation of long-acting Carteolol offers similar efficacy and tolerability with a potential for improved patient adherence. Pharmacological Properties Carteolol is a nonselective β-adrenoceptor antagonist with properties unlike those of other β-adrenoceptor antagonists (i.e. ISA and minimal local anaesthetic activity). Ocular Carteolol significantly reduced IOP in healthy volunteers. In addition, significant reductions in aqueous humour production were seen with Carteolol in patients with POAG; it did not alter corneal sensitivity, tear secretion or pupil diameter. Unlike timolol or betaxolol, Carteolol also appeared to improve perfusion of the optic nerve head. Ocular Carteolol did not affect respiratory function in healthy volunteers, although bronchoconstriction was seen in patients with asthma. Although Carteolol had similar cardiovascular effects to other ocular β-adrenoceptor antagonists in healthy volunteers and patients with asthma, unlike timolol, it did not have a deleterious effect on the lipid profile in patients with POAG or OH. Plasma Carteolol concentrations were significantly lower with the long-acting formulation of ocular Carteolol than with the standard formulation. In animal models, the precorneal residence time of Carteolol was increased with the long-acting versus the standard formulation, allowing for prolonged ocular delivery. Moreover, compared with standard Carteolol, a single dose of long-acting Carteolol resulted in significantly higher Carteolol concentrations at certain timepoints in the iris and ciliary body, indicating enhanced ocular penetration. Therapeutic Efficacy The results of numerous trials showed that the ocular hypotensive efficacy of standard Carteolol 1% or 2% twice daily was similar to that of timolol 0.25% or 0.5% twice daily, betaxolol 0.5% twice daily or metipranolol 0.3% twice daily in patients with POAG, OAG or OH after 1–12 months of treatment. However, 3 months of treatment with levobunolol 0.5% twice daily resulted in a significantly greater reduction in IOP than Carteolol 2% twice daily in patients with OAG or OH. A significant reduction from baseline in IOP was seen with Carteolol in most studies. Long-term treatment (for up to 7 years) with Carteolol 1% twice daily had similar efficacy to timolol 0.25% twice daily and betaxolol 0.5% twice daily in terms of reducing IOP and maintaining visual fields in patients with newly diagnosed POAG. Combination therapy with Carteolol plus latanoprost reduced IOP to a significantly greater extent than monotherapy with latanoprost or combination therapy with nipradilol plus latanoprost in patients with POAG or normal-tension glaucoma. The ocular hypotensive efficacy of long-acting Carteolol administered once daily was equivalent to that of the standard formulation of Carteolol administered twice daily in two well designed trials in patients with OAG or OH. In addition, data from a third trial revealed significant reductions from baseline in IOP with both the long-acting and standard formulations of Carteolol in patients with PAOG or OH. Tolerability Ocular administration of standard or long-acting Carteolol was generally well tolerated in patients with POAG, OAG or OH. In general, there were no significant differences in the incidence of ocular symptoms (e.g. burning/stinging at instillation, tearing, ocular pain, blurred vision, itching, conjunctival hyperaemia) between patients receiving Carteolol and those receiving comparators such as timolol, metipranolol or levobunolol. However, several studies reported better ocular tolerability of Carteolol versus timolol for certain endpoints (e.g. fewer ocular symptoms overall and less burning and eye pain). The long-acting formulation of Carteolol was associated with a low incidence of blurred vision (≤2% of patients). Few differences emerged between Carteolol and other β-adrenoceptor antagonists in terms of cardiovascular effects (i.e. effects on heart rate and blood pressure) in patients with POAG, OAG or OH. However, one study found a significantly lower incidence of cardiovascular adverse events overall and a significantly lower incidence of bradycardia with Carteolol than with timolol; in particular, Carteolol seemed less likely to induce nocturnal bradycardia.
-
ocular Carteolol a review of its use in the management of glaucoma and ocular hypertension
Drugs & Aging, 2007Co-Authors: Sheridan Henness, Tracy Swainston Harrison, Gillian M. KeatingAbstract:Abstract Ocular Carteolol (Mikelan), Teoptic, Ocupress) is a nonselective beta-adrenoceptor antagonist with intrinsic sympathomimetic activity (ISA). Ocular Carteolol effectively reduces intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) or ocular hypertension (OH). Twice-daily administration of standard Carteolol has generally similar IOP-lowering efficacy to other ocular beta-adrenoceptor antagonists such as timolol, betaxolol and metipranolol in patients with OAG or OH. In addition, long-term treatment with Carteolol has similar efficacy to timolol and betaxolol in terms of reducing IOP and maintaining visual fields in patients with newly diagnosed primary OAG (POAG). The new long-acting formulation of once-daily Carteolol has equivalent efficacy to the standard formulation of Carteolol administered twice daily in patients with OAG or OH. Both the standard and long-acting formulations of ocular Carteolol are generally well tolerated in terms of topical adverse effects involving the eyes or systemic adverse effects involving the cardiovascular system. Thus, twice-daily Carteolol is a well established option in the treatment of glaucoma and OH, and the new once-daily formulation of long-acting Carteolol offers similar efficacy and tolerability with a potential for improved patient adherence.