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Profiles of Drug Substances,... 2021Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing... (Review)
Review
Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing (local anesthetic) activity. Betaxolol selectively and competitively binds to and blocks beta-1 (β1) adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. When applied topically in the eye, this agent reduces aqueous humor secretion and lowers the intraocular pressure (IOP). In addition, betaxolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels. Betaxolol (S)-(-)-enantiomer shows higher pharmacological activity. This chapter provides a complete review of nomenclature, physiochemical properties, methods of preparation, identification techniques and various qualitative and quantitative analytical techniques as well as pharmacology of betaxolol. In addition, the chapter also includes review of several methods for enantiomeric separation betaxolol using chromatographic techniques.
Topics: Adrenergic beta-Antagonists; Betaxolol; Blood Pressure; Eye Diseases; Heart; Humans; Intraocular Pressure; Kidney; Renin
PubMed: 33461701
DOI: 10.1016/bs.podrm.2020.07.002 -
Australian and New Zealand Journal of... Feb 1989Drugs classified as beta-blockers have proved to be valuable in the treatment of patients with glaucoma. Timolol has become the most widely used ocular hypotensive... (Review)
Review
Drugs classified as beta-blockers have proved to be valuable in the treatment of patients with glaucoma. Timolol has become the most widely used ocular hypotensive agent. Actual and potential side effects associated with its non-selective beta-blockade have prevented its use in patients with reactive airways disease, and to a lesser extent, with various cardiovascular conditions. Betaxolol is a relatively selective beta-1 blocker which in most patients is almost as effective as timolol in lowering intraocular pressure, and may be partly additive with dipivefrin. It is probably safer in patients unable to tolerate non-selective beta-blockers. However, it needs to be used with caution in these patients, who are unpredictably susceptible to systemic side effects.
Topics: Adrenergic beta-Antagonists; Betaxolol; Glaucoma; Humans; Intraocular Pressure; Propanolamines; Time Factors; Timolol
PubMed: 2569884
DOI: 10.1111/j.1442-9071.1989.tb00483.x -
Archives of Ophthalmology (Chicago,... Oct 1984
Clinical Trial Comparative Study Randomized Controlled Trial
Topics: Adrenergic beta-Antagonists; Betaxolol; Clinical Trials as Topic; Glaucoma; Humans; Intraocular Pressure; Propanolamines; Timolol
PubMed: 6148923
DOI: 10.1001/archopht.1984.01040031154003 -
Ceska a Slovenska Oftalmologie :... 2020The 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...
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 didnt 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.
Topics: Betaxolol; Carteolol; Evoked Potentials, Visual; Glaucoma; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Middle Aged
PubMed: 33126804
DOI: 10.31348/2020/17 -
Drugs Jul 1990Betaxolol is a lipophilic beta-adrenoceptor antagonist relatively selective for beta 1-adrenoceptors with only weak beta 2-blocking activity. Used topically in glaucoma... (Review)
Review
Betaxolol is a lipophilic beta-adrenoceptor antagonist relatively selective for beta 1-adrenoceptors with only weak beta 2-blocking activity. Used topically in glaucoma and ocular hypertension, betaxolol 0.5% solution produces a reduction in intraocular pressure of between 13 and 30%, an effect comparable with that of ocular timolol. It may usefully be combined with other types of anti-glaucoma agents. The most notable feature of its adverse effect profile is transient local stinging or irritation, occurring in 25 to 40% of patients. Following ocular administration, betaxolol appears to be largely devoid of adverse bronchopulmonary or cardiac effects, in comparison with nonselective ocular beta-adrenoceptor antagonists, which may be more likely to exert systemic effects. Betaxolol has negligible local anaesthetic activity, so that corneal desensitisation does not occur with its use. Thus, betaxolol is an alternative therapeutic option available to the physician for the management of chronic open-angle glaucoma and ocular hypertension. Its apparently lower propensity to affect the cardiopulmonary system represents a significant advantage over other ocular beta-adrenoceptor antagonists.
Topics: Betaxolol; Eye Diseases; Glaucoma; Humans; Intraocular Pressure; Ophthalmic Solutions
PubMed: 2202584
DOI: 10.2165/00003495-199040010-00005 -
International Journal of Pharmaceutics Apr 2021Blindness and impaired vision are considered as the most troublesome health conditions leading to significant socioeconomic strains. The current study focuses on...
Blindness and impaired vision are considered as the most troublesome health conditions leading to significant socioeconomic strains. The current study focuses on development of nanoparticulate systems (i.e., niosomes) as drug vehicles to enhance the ocular availability of betaxolol hydrochloride for management of glaucoma. Betaxolol-loaded niosomes were further laden into pH-responsive in situ forming gels to further extend precorneal retention of the drug. The niosomes were evaluated in terms of vesicle size, morphology, size distribution, surface charge and encapsulation efficiency. The optimized niosomes, comprised of Span® 40 and cholesterol at a molar ratio of 4:1, displayed particle size of 332 ± 7 nm, zeta potential of -46 ± 1 mV, and encapsulation efficiency of 69 ± 5%. The optimal nanodispersion was then incorporated into a pH-triggered in situ forming gel comprised of Carbopol® 934P and hydroxyethyl cellulose. The formed gels were translucent, pseudoplastic, mucoadhesive, and displayed a sustained in vitro drug release pattern. Upon instillation of the betaxolol-loaded niosomal gel into rabbits' eyes, a prolonged intraocular pressure reduction and significant enhancement in the relative bioavailability of betaxolol (280 and 254.7%) in normal and glaucomatous rabbits, were attained compared to the marketed eye drops, respectively. Hence, the developed pH-triggered nanoparticulate gelling system might provide a promising carrier for ophthalmic drug delivery and for improved augmentation of glaucoma.
Topics: Animals; Betaxolol; Drug Carriers; Drug Delivery Systems; Gels; Glaucoma; Hydrogen-Ion Concentration; Liposomes; Particle Size; Rabbits
PubMed: 33609725
DOI: 10.1016/j.ijpharm.2021.120380 -
Lancet (London, England) Jan 1990
Topics: Betaxolol; Humans; Male; Middle Aged; Stuttering
PubMed: 1967682
DOI: 10.1016/0140-6736(90)90311-r -
Eye (London, England) 1994
Topics: Aged; Betaxolol; Female; Humans; Ocular Hypertension; Uveitis, Anterior
PubMed: 7867841
DOI: 10.1038/eye.1994.181 -
Pediatrics International : Official... Jan 2022Beta-blockers have gradually become an attractive option for the treatment of infantile hemangiomas. Topical application is preferred to oral administration because of...
BACKGROUND
Beta-blockers have gradually become an attractive option for the treatment of infantile hemangiomas. Topical application is preferred to oral administration because of their potential systemic adverse effects. The aim of this study is to investigate the effect of betaxolol in treating superficial infantile hemangioma.
METHODS
Seventy-four infants admitted to the First Affiliated Hospital of Xinjiang Medical University from 2018 to 2019 were observed and recorded. Variables such as color, size, tension, and thickness were recorded monthly and evaluated using visual analog scales. Multi-factor analysis of variance with repeated measurements and the non-parametric Kruskal-Wallis H test were used to compare clinical effectiveness across the different groups.
RESULTS
After 6 months of treatment, 33.78% (25/74) showed excellent results, 55.41% (41/74) had good responses, 8.11% (6/74) had moderate responses, and 2.70% (2/74) had poor responses. Local discomfort and systemic complications were not found. There was no significant difference in gender and location of occurrence among groups (p > 0.05), and the effect of topical application of betaxolol was optimum in the children aged 0-3 months (p = 0.002). None of three age groups had statistically significant difference in heart rate and blood pressure after accepting treatment (1 month, p = 0.618; 4 months, p = 0.138; 6 months, p = 0.757).
CONCLUSIONS
Our study showed that topical administration of betaxolol was effective and well tolerated for superficial infantile hemangiomas, particularly in the early proliferative stage. However, its safety and efficacy need further research.
Topics: Infant; Child; Humans; Timolol; Hemangioma; Pilot Projects; Betaxolol; Hemangioma, Capillary; Adrenergic beta-Antagonists; Treatment Outcome; Skin Neoplasms
PubMed: 36222187
DOI: 10.1111/ped.15384 -
Annals of Clinical Psychiatry :... Mar 1998Betaxolol, a long-acting beta-adrenergic blocker that enters the central nervous system, was examined for therapeutic effects on the persistent anxiety of anxiety... (Clinical Trial)
Clinical Trial
Betaxolol, a long-acting beta-adrenergic blocker that enters the central nervous system, was examined for therapeutic effects on the persistent anxiety of anxiety disorders. Prior studies of beta-blockers examined only agents that were short-acting or did not enter the brain. Betaxolol was administered to 31 patients in open trials. Of 13 outpatients, 11 had generalized anxiety disorder (GAD) and 2 had adjustment disorder with anxiety. Five with GAD had concurrent panic disorder. Of 18 inpatients, 16 had GAD and 2 had adjustment disorder with anxiety. Betaxolol doses were increased until the patient responded or declined further dosage. Severity was rated on a 4-point global scale. Before betaxolol, all were moderately or severely ill. In all patients with panic disorder panic attacks stopped within 2 days (p<0.001). Anxiety decreased to no more than marginally ill in 85% of outpatients (p<0.0001) and all inpatients (p<0.0001). Betaxolol doses were usually 5 mg once or twice daily; four inpatients took 10 to 20 mg twice daily. In sum, betaxolol administration was rapidly followed by improvements that were easily noticed by the doctor, even in patients with longstanding anxiety and obsessive-compulsive personality disorder. Preliminary observations in posttraumatic stress disorder are similar.
Topics: Adrenergic beta-Antagonists; Adult; Aged; Anti-Anxiety Agents; Anxiety Disorders; Betaxolol; Female; Humans; Male; Middle Aged; Severity of Illness Index; Treatment Outcome
PubMed: 9622045
DOI: 10.1023/a:1026146528290