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Arquivos Brasileiros de Oftalmologia Sep 2022We report a case of bilateral acute depigmentation of the iris in which satisfactory intraocular pressure control was obtained after resolution of the acute disease with...
We report a case of bilateral acute depigmentation of the iris in which satisfactory intraocular pressure control was obtained after resolution of the acute disease with a trabecular implant (iStent®). A 62-year-old woman presented with bilateral simultaneous acute eye pain, photophobia, increased intraocular pressure (34 mmHg), circulating pigment in the anterior chamber, areas of depigmentation in the iris, and posterior synechiae. She had received oral amoxicillin-clavulanate and moxifloxacin for pneumonia 2 months previously. Bilateral acute depigmentation of the iris was suspected as well as a viral etiology. She received oral acetazolamide, aciclovir, and prednisone, besides topical prednisolone, betaxolol, brimonidine, dorzolamide, and atropine. The disease gradually resolved in 4 months but, after 1 year, she developed bilateral cataracts, and still needed three drugs for intraocular pressure control (16/18 mmHg). Cataract-iStent® combined surgery was performed in both eyes. One year after surgery, intraocular pressure was 11/12 mmHg, without medication. iStent® was safe and effective on this secondary glaucoma.
PubMed: 36169432
DOI: 10.5935/0004-2749.2021-0239 -
British Journal of Clinical Pharmacology Feb 19811 Observations were made in five subjects who exercised before and at 2, 3, 6, 8, 24, 33 and 48 h after the oral administration of placebo and 5, 10, 20 and 40 mg... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
1 Observations were made in five subjects who exercised before and at 2, 3, 6, 8, 24, 33 and 48 h after the oral administration of placebo and 5, 10, 20 and 40 mg betaxolol. 2 The exercise heart rate remained constant at all times after the placebo. All doses of betaxolol significantly reduced the exercise tachycardia at all times. The maximum effect (34.4 +/- 2.2%) occurred after 40 mg. 3 There was a small decline in effect from the peak to 24 h when 40 mg produced a 23.3 +/- 2.7% reduction and a further decline to 48 h when there was a 14.6 +/- 1.8% reduction. 4 Plasma levels of betaxolol were measured in these studies. The peak plasma concentration occurred between 3 and 8 h with different doses. The plasma elimination half-lives after 10, 20 and 40 mg were 11.4 +/- 2.5, 15.9 +/- 4.9 and 15.1 +/- 3.1 h. 5 The effects of 40 mg betaxolol, 200 mg atenolol, 160 mg propranolol, 160 mg oxprenolol, 400 mg sotalol and placebo on an exercise tachycardia were compared in five subjects who received all treatments in random order. 6 There was no significant difference in the maximum reduction produced in an exercise tachycardia by the different drugs. 7 The effect of all drugs decreased with time. The effect of oxprenolol had worn off at 24 h but at 48 h only atenolol and betaxolol produced significant reductions in the exercise tachycardia. 8 Plasma concentrations of the different drugs were measured and plasma elimination half-lives determined. The half-life for betaxolol was 24.5 h which was longer than that for any of the other drugs. 9 These observations show that betaxolol is a potent beta-adrenoceptor antagonist with a long duration of effect on an exercise tachycardia and a long plasma elimination half-life.
Topics: Adrenergic beta-Antagonists; Adult; Betaxolol; Female; Heart Rate; Hemodynamics; Humans; Kinetics; Male; Physical Exertion; Propanolamines
PubMed: 6111331
DOI: 10.1111/j.1365-2125.1981.tb01121.x -
Critical Care (London, England) Jun 2021β-adrenergic antagonists (BAAs) are used to treat cardiovascular disease such as ischemic heart disease, congestive heart failure, dysrhythmias, and hypertension....
BACKGROUND
β-adrenergic antagonists (BAAs) are used to treat cardiovascular disease such as ischemic heart disease, congestive heart failure, dysrhythmias, and hypertension. Poisoning from BAAs can lead to severe morbidity and mortality. We aimed to determine the utility of extracorporeal treatments (ECTRs) in BAAs poisoning.
METHODS
We conducted systematic reviews of the literature, screened studies, extracted data, and summarized findings following published EXTRIP methods.
RESULTS
A total of 76 studies (4 in vitro and 2 animal experiments, 1 pharmacokinetic simulation study, 37 pharmacokinetic studies on patients with end-stage kidney disease, and 32 case reports or case series) met inclusion criteria. Toxicokinetic or pharmacokinetic data were available on 334 patients (including 73 for atenolol, 54 for propranolol, and 17 for sotalol). For intermittent hemodialysis, atenolol, nadolol, practolol, and sotalol were assessed as dialyzable; acebutolol, bisoprolol, and metipranolol were assessed as moderately dialyzable; metoprolol and talinolol were considered slightly dialyzable; and betaxolol, carvedilol, labetalol, mepindolol, propranolol, and timolol were considered not dialyzable. Data were available for clinical analysis on 37 BAA poisoned patients (including 9 patients for atenolol, 9 for propranolol, and 9 for sotalol), and no reliable comparison between the ECTR cohort and historical controls treated with standard care alone could be performed. The EXTRIP workgroup recommends against using ECTR for patients severely poisoned with propranolol (strong recommendation, very low quality evidence). The workgroup offered no recommendation for ECTR in patients severely poisoned with atenolol or sotalol because of apparent balance of risks and benefits, except for impaired kidney function in which ECTR is suggested (weak recommendation, very low quality of evidence). Indications for ECTR in patients with impaired kidney function include refractory bradycardia and hypotension for atenolol or sotalol poisoning, and recurrent torsade de pointes for sotalol. Although other BAAs were considered dialyzable, clinical data were too limited to develop recommendations.
CONCLUSIONS
BAAs have different properties affecting their removal by ECTR. The EXTRIP workgroup assessed propranolol as non-dialyzable. Atenolol and sotalol were assessed as dialyzable in patients with kidney impairment, and the workgroup suggests ECTR in patients severely poisoned with these drugs when aforementioned indications are present.
Topics: Adrenergic beta-Antagonists; Consensus; Drug Overdose; Extracorporeal Membrane Oxygenation; Humans
PubMed: 34112223
DOI: 10.1186/s13054-021-03585-7 -
Hypertension Research : Official... Mar 2002We evaluated the protective effects of long-term treatment with betaxolol, a specific beta-antagonist, on platelet-derived growth factor (PDGF) A-chain and transforming...
Betaxolol inhibits extracellular signal-regulated kinase and P70S6 kinase activities and gene expressions of platelet-derived growth factor A-chain and transforming growth factor-beta1 in Dahl salt-sensitive hypertensive rats.
We evaluated the protective effects of long-term treatment with betaxolol, a specific beta-antagonist, on platelet-derived growth factor (PDGF) A-chain and transforming growth factor (TGF)-beta1 gene expression in the left ventricle of Dahl salt-sensitive hypertensive rats fed a high-salt diet. In addition, we evaluated the relations between these effects and coronary microvascular remodeling, expression of extracellular signal-regulated kinases (ERK) belonging to one subfamily of mitogen-activated protein kinases, and expression of p70S6 kinase belonging to one subfamily of ribosomal S6 kinases. Betaxolol (0.9 mg/kg/day, subdepressor dose) was administered for 5 weeks, from 6 weeks of age to the left ventricular hypertrophy stage at 11 weeks of age. Increased PDGF A-chain and TGF-beta1 mRNA and protein expression were suppressed by betaxolol. Upregulated activities of ERK1/2 and p70S6 kinase phosphorylations were decreased by betaxolol. Betaxolol administration resulted in significant improvements in the wall-to-lumen ratio, perivascular fibrosis and myocardial fibrosis. Thus, we conclude that ERK1/2 and p70S6 kinase activities may play a key role in coronary microvascular remodeling of Dahl salt-sensitive hypertensive rats, and that beneficial effects of betaxolol on cardiovascular remodeling may be at least partially mediated by decreased PDGF A-chain and TGF-beta1 expression in the left ventricle.
Topics: Adrenergic beta-Antagonists; Animals; Betaxolol; Body Weight; Gene Expression; Hemodynamics; Hypertension; Male; Mitogen-Activated Protein Kinases; Myocardium; Organ Size; Phosphorylation; Platelet-Derived Growth Factor; RNA, Messenger; Rats; Rats, Inbred Dahl; Ribosomal Protein S6 Kinases, 70-kDa; Transforming Growth Factor beta; Transforming Growth Factor beta1
PubMed: 12047037
DOI: 10.1291/hypres.25.211 -
Ceska a Slovenska Oftalmologie :... 2021The aim of the study was to determine whether hypertensive glaucoma (HTG) with different types of treatment leads to significant damage in any of the evaluated...
AIM
The aim of the study was to determine whether hypertensive glaucoma (HTG) with different types of treatment leads to significant damage in any of the evaluated parameters.
SAMPLE AND METHODOLOGY
The sample, consisting of 36 HTG patients (72 eyes), was divided into three subgroups: In the first group, patients were treated with combination therapy (latanoprost + timolol, latanoprost + dorzolamide + timolol, dorzolamide + timolol). The group consisted of seven women and five men, with an average age of 64 years (49-81). In the second group, patients were treated with beta-blockers (carteolol, betaxolol, timolol). The group consisted of five women and five men, with an average age of 62 years (27-77). In the third group, patients were treated with prostaglandins (latanoprost, bimatoprost). The group consisted of eleven women and three men, with an average age of 61 years (61-78). Criteria for inclusion in the study were visual acuity of 1.0 with a possible correction of less than ±3 dioptres, approximately the same changes in the visual fields of all patients, an intraocular pressure (IOP) of less than 18 mmHg, and no other ocular or neurological disease. The retinal nerve fibre layer (RNFL) on the optic nerve target and vessel density (VD) was measured using an Avanti RTVue XR from Optovue. We determined the values of VD in whole image (WI) and VD of peripapillary (PP). In both cases, we then measured all vessels (VDa) and small vessels (VDs). The visual field was examined by means of a fast threshold glaucoma program with a Medmont M 700 instrument. In addition to the sum of sensitivities in apostilbs (asb) in the range of 0-22 degrees, the overall visual field defect (OD) was also evaluated. The statistical analysis was carried out using a multivariate regression model with adjustment for age and gender. The measured values of the third group were taken as baseline.
RESULTS
In the statistical analysis, we have found differences in visual field in the combination treatment group (p = 0.0006) and differences were recorded for RNFL in the beta-blocker group (p = 0.04).
Topics: Angiography; Female; Glaucoma; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Male; Middle Aged; Timolol; Tomography, Optical Coherence; Visual Fields
PubMed: 35081717
DOI: 10.31348/2021/33 -
International Journal of Molecular... Mar 2023Uveal melanoma (UM) is the most common primary cancer of the eye in adults. A new systemic therapy is needed to reduce the high metastasis and mortality rate. As...
Uveal melanoma (UM) is the most common primary cancer of the eye in adults. A new systemic therapy is needed to reduce the high metastasis and mortality rate. As β-blockers are known to have anti-tumor effects on various cancer entities, this study focuses on investigating the effect of β1-selective blockers atenolol, celiprolol, bisoprolol, metoprolol, esmolol, betaxolol, and in particular, nebivolol on UM. The study was performed on 3D tumor spheroids as well as 2D cell cultures, testing tumor viability, morphological changes, long-term survival, and apoptosis. Flow cytometry revealed the presence of all three β-adrenoceptors with a dominance of β2-receptors on cell surfaces. Among the blockers tested, solely nebivolol concentration-dependently decreased viability and altered 3D tumor spheroid structure. Nebivolol blocked the repopulation of cells spreading from 3D tumor spheroids, indicating a tumor control potential at a concentration of ≥20 µM. Mechanistically, nebivolol induced ATP depletion and caspase-3/7 activity, indicating that mitochondria-dependent signaling is involved. D-nebivolol or nebivolol combined with the β2-antagonist ICI 118.551 displayed the highest anti-tumor effects, suggesting a contribution of both β1- and β2-receptors. Thus, the present study reveals the tumor control potential of nebivolol in UM, which may offer a perspective for co-adjuvant therapy to reduce recurrence or metastasis.
Topics: Adult; Humans; Nebivolol; Ethanolamines; Benzopyrans; Adrenergic beta-Antagonists; Melanoma; Receptors, Adrenergic, beta
PubMed: 36982966
DOI: 10.3390/ijms24065894 -
Molecular Vision Jun 2007To investigate the effect of beta-adrenergic receptor antagonists against oxidative stress on purified rat retinal ganglion cells (RGCs), timolol, betaxolol, carteolol...
PURPOSE
To investigate the effect of beta-adrenergic receptor antagonists against oxidative stress on purified rat retinal ganglion cells (RGCs), timolol, betaxolol, carteolol and nipradilol were included in the present study.
METHODS
RGCs were purified using a 2 step panning procedure from postnatal days 6-8 using Wistar rats. After 72 h in culture under normal condition, RGCs were exposed to oxidative stress induced by B27 medium without anti-oxidant. To verify whether this stress is apoptotic or necrotic, Annexin V and propidium iodide were used to detect apoptotic and necrotic cells after 2 h stress. The presence of a proinhibitor for intracellular cathepsin B, and an inhibitor for thiol protease (cathepsin B/H/L, calpain), was also assessed to verify necrotic cell death event in oxidative conditions. Next, RGC cultures under oxidative stress were incubated with timolol, betaxolol, carteolol, and nipradilol added, respectively, for 24 h culture. The RGC viability in each condition normalized to that under normal condition was evaluated as live cell percentage based on total experiments of 8-15.
RESULTS
Two h after oxidative stress, Annexin V and propidium iodide positive cells increased. Increased cell death under oxidative stress was significantly reduced by inhibitors for cathepsin or calpain. These data suggest that increased cell death under the current oxidative stress was due to necrosis. Under oxidative stress for 24 h, RGC viability reduced to 52.5-60.2% as compared with normal. With 10 nM and 100 nM timolol, live cell significantly increased to 69.3% and 75.5%, respectively. Both betaxolol and nipradilol enhanced live RGCs significantly in concentration of 100 nM and 1 microM, with viability of 70.5%, 71.6%, and 70.4%, 74.7%, respectively. While with 10 nM, 100 nM and 1 microM addition of carteolol, there was no significant increase in live RGC percentage which ranged from 53.1-55.0%.
CONCLUSIONS
Timolol, betaxolol and nipradilol, but not carteolol, showed neuroprotective effects against oxidative stress induced by B27 without antioxidant on purified rat RGCs at concentrations of 10 nM or higher. Although the neuroprotective mechanism of beta-blockers for oxidative stress is still unknown, this additive effect may deserve future studies.
Topics: Adrenergic beta-Antagonists; Animals; Apoptosis; Cells, Cultured; Ganglia, Sensory; Necrosis; Oxidative Stress; Rats; Rats, Wistar; Retina
PubMed: 17615544
DOI: No ID Found -
The British Journal of Ophthalmology May 2022To assess the comparative efficacy of latanoprostene bunod (LBN), a novel prostaglandin analogue (PGA), to other medications for open-angle glaucoma and ocular... (Meta-Analysis)
Meta-Analysis
BACKGROUND/AIMS
To 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).
METHODS
A systematic literature review adapted from the Li (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.
RESULTS
A 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%.
CONCLUSION
LBN 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%.
Topics: Amides; Antihypertensive Agents; Bayes Theorem; Betaxolol; Bimatoprost; Brimonidine Tartrate; Carteolol; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Latanoprost; Network Meta-Analysis; Ocular Hypertension; Prostaglandins A; Prostaglandins F, Synthetic; Timolol; Travoprost
PubMed: 33397657
DOI: 10.1136/bjophthalmol-2020-317262 -
Behavioural Brain Research Jan 2016Drug seeking is maintained by encounters with drug-associated cues, and disrupting retrieval of these drug-cue associations would reduce the risk of relapse. Retrieval...
Drug seeking is maintained by encounters with drug-associated cues, and disrupting retrieval of these drug-cue associations would reduce the risk of relapse. Retrieval of cocaine-associated memories is dependent on β-adrenergic receptor (β-AR) activation, and blockade of these receptors induces a persistent retrieval deficit. Whether retrieval of cocaine-associated memory is mediated by a specific β-AR subtype, however, remains unclear. Using a cocaine conditioned place preference (CPP) procedure, we examined whether retrieval of a cocaine CPP memory is mediated collectively by β1- and β2-ARs, or by one of these β-AR subtypes alone. We show that co-blockade of β1- and β2-ARs abolished CPP expression on that and subsequent drug-free CPP tests, resulting in a long-lasting retrieval deficit that prevented subsequent cocaine-induced reinstatement. To dissociate the necessity of either β1- or β2-ARs alone, we administered subtype-specific antagonists prior to retrieval. Administration of a β1-AR antagonist before the initial CPP trial dose-dependently reduced expression of a CPP on that and subsequent drug-free trials as compared to vehicle administration. In contrast, administration of a β2-AR antagonist had no effect on initial CPP expression, although the highest dose reduced subsequent CPP expression. Importantly, either β1- or β2-AR blockade prior to an initial retrieval trial prevented subsequent cocaine-induced reinstatement. Our findings indicate that the β1-AR subtype mediates retrieval of a cocaine CPP, and that acutely blocking either β1- or β2-ARs can prevent subsequent cocaine-induced reinstatement. Thus, β-AR antagonists, particularly β1-ARs antagonists, could serve as adjuncts for addiction therapies to prevent retrieval of drug-associated memories and provide protection against relapse.
Topics: Adrenergic beta-1 Receptor Antagonists; Adrenergic beta-2 Receptor Antagonists; Animals; Behavior, Animal; Cocaine; Dopamine Uptake Inhibitors; Dose-Response Relationship, Drug; Drug-Seeking Behavior; Male; Mental Recall; Rats; Rats, Long-Evans; Receptors, Adrenergic, beta-1; Receptors, Adrenergic, beta-2
PubMed: 26318933
DOI: 10.1016/j.bbr.2015.08.030 -
Archives of Disease in Childhood Jul 1984Both betaxolol and propranolol, beta blockers with different pharmacological properties, increase the reliability of somatotropic testing with glucagon. The combination... (Clinical Trial)
Clinical Trial Comparative Study
Both betaxolol and propranolol, beta blockers with different pharmacological properties, increase the reliability of somatotropic testing with glucagon. The combination of glucagon and betaxolol, however, is much better tolerated than that of glucagon and propranolol. The use of a beta 1 cardioselective adrenoceptor block for growth hormone testing is recommended.
Topics: Adolescent; Adrenergic beta-Antagonists; Betaxolol; Child; Child, Preschool; Female; Glucagon; Growth Disorders; Growth Hormone; Humans; Infant; Male; Propanolamines; Propranolol; Stimulation, Chemical
PubMed: 6147121
DOI: 10.1136/adc.59.7.670