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1.
Vestn Oftalmol ; 140(2. Vyp. 2): 73-79, 2024.
Artigo em Russo | MEDLINE | ID: mdl-38739134

RESUMO

The management protocol for patients with neovascular age-related macular degeneration (nAMD) involves multiple intravitreal injections (IVI) of anti-VEGF drugs. The ability to reduce the peak intraocular pressure (IOP) rise is greatly important in clinical practice. PURPOSE: This study evaluates the effect of topical hypotensive drugs on the short-term IOP rise after IVI of anti-VEGF drugs in patients with nAMD. MATERIAL AND METHODS: The prospective study included 80 patients with newly diagnosed nAMD. Before the start of treatment, the patients were divided into 4 groups of 20 people each: 1st - controls, who received no prophylactic drugs, in the 2nd, 3rd and 4th groups local instillations of one drop of hypotensive drugs brinzolamide 1%, brinzolamide-timolol, brimonidine-timolol were performed in the conjunctival sac twice: 1 day before the injection (at 20:00) and on the day of the injection 2 hours before the manipulation (at 08:00), respectively. IOP was measured in each patient using ICare Pro non-contact tonometer before injection, as well as 1 min, 30 and 60 min after injection. RESULTS: Prophylactic use of hypotensive drugs was associated with a significant decrease in IOP immediately after IVI compared to the same parameter in the 1st group (p<0.001), the maximum decrease in IOP values was observed when using a fixed combination of brimonidine-timolol by 12.1 mm Hg compared to the controls (p<0.001), the combination of brinzolamide-timolol reduced IOP by 8.5 mm Hg (p<0.001), brinzolamide 1% led to the smallest decrease in IOP - by 5.1 mm Hg (p<0.001). CONCLUSION: Study patients that received instillations of brimonidine-timolol combination of one drop into the conjunctival sac 1 day before the injection and on the day of the injection showed the maximum decrease in IOP compared to patients of the other groups.


Assuntos
Inibidores da Angiogênese , Pressão Intraocular , Injeções Intravítreas , Hipertensão Ocular , Sulfonamidas , Humanos , Masculino , Feminino , Idoso , Pressão Intraocular/efeitos dos fármacos , Hipertensão Ocular/prevenção & controle , Hipertensão Ocular/tratamento farmacológico , Hipertensão Ocular/fisiopatologia , Inibidores da Angiogênese/administração & dosagem , Estudos Prospectivos , Sulfonamidas/administração & dosagem , Resultado do Tratamento , Anti-Hipertensivos/administração & dosagem , Fator A de Crescimento do Endotélio Vascular/antagonistas & inibidores , Tonometria Ocular/métodos , Pessoa de Meia-Idade , Timolol/administração & dosagem , Tartarato de Brimonidina/administração & dosagem , Soluções Oftálmicas/administração & dosagem , Tiazinas/administração & dosagem , Degeneração Macular/tratamento farmacológico , Degeneração Macular/diagnóstico
2.
Drug Des Devel Ther ; 18: 71-80, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38229917

RESUMO

Introduction: Nicotine is a major component of cigarette smoke with various detrimental cardiovascular effects, including increased oxidative stress in the heart. Agonism of α2-adrenergic receptors (ARs), such as with dexmedetomidine, has been documented to exert cardioprotective effects against oxidative stress and related apoptosis and necroptosis. α2-ARs are membrane-residing G protein-coupled receptors (GPCRs) that primarily activate Gi/o proteins. They are also subjected to GPCR-kinase (GRK)-2-dependent desensitization, which entails phosphorylation of the agonist-activated receptor by GRK2 to induce its decoupling from G proteins, thus terminating α2AR-mediated G protein signaling. Objective: In the present study, we sought to examine the effects of nicotine on α2AR signaling and effects in H9c2 cardiomyocytes exposed to H2O2 to induce oxidative cellular damage. Methods and Results: As expected, treatment of H9c2 cardiomyocytes with H2O2 significantly decreased cell viability and increased oxidative stress, as assessed by reactive oxygen species (ROS)-associated fluorescence levels (DCF assay) and superoxide dismutase activity. Both H2O2 effects were partly rescued by α2AR activation with brimonidine in control cardiomyocytes but not in cells pretreated with nicotine for 24 hours, in which brimonidine was unable to reduce H2O2-induced cell death and oxidative stress. This was due to severe α2AR desensitization, manifested as very low Gi protein activation by brimonidine, and accompanied by GRK2 upregulation in nicotine-treated cardiomyocytes. Finally, pharmacological inhibition of adenylyl cyclase (AC) blocked H2O2-dependent oxidative damage in nicotine-pretreated H9c2 cardiomyocytes, indicating that α2AR activation protects against oxidative injury via its classic coupling to Gai-mediated AC inhibition. Discussion/Conclusions: Nicotine can negate the cardioprotective effects of α2AR agonists against oxidative injury, which may have important implications for patients treated with this class of drugs that are chronic tobacco smokers.


Assuntos
Miócitos Cardíacos , Nicotina , Humanos , Nicotina/farmacologia , Nicotina/metabolismo , Peróxido de Hidrogênio/farmacologia , Peróxido de Hidrogênio/metabolismo , Receptores Adrenérgicos alfa 2/metabolismo , Estresse Oxidativo , Apoptose , Tartarato de Brimonidina/metabolismo , Tartarato de Brimonidina/farmacologia
3.
Rev. bras. oftalmol ; 83: e0009, 2024. tab, graf
Artigo em Português | LILACS | ID: biblio-1535599

RESUMO

RESUMO Objetivo: Avaliar o efeito do colírio de brimonidina 0,2% na redução da hiperemia e do sangramento ocular durante as cirurgias de estrabismo, em comparação com o colírio de nafazolina 0,025% + feniramina 0,3%. Métodos: Foram avaliados 14 pacientes com estrabismo e indicação de correção cirúrgica bilateral. Foi instilado antes do procedimento, de forma aleatória, um colírio em cada olho dos pacientes avaliados. A análise subjetiva da hiperemia conjuntival e do sangramento perioperatório foi realizada de forma duplo-cega, por dois cirurgiões. A avaliação objetiva do nível de hiperemia conjuntival foi realizada por análise das imagens obtidas por meio do software ImageJ®. Resultados: A análise de modelos multivariados de efeito misto indicou diferenças estatisticamente significantes entre os grupos em relação à hiperemia (avaliador 2) e ao sangramento intraoperatório (avaliadores 1 e 2), com maiores escores nos casos tratados com colírio de nafazolina + feniramina. Entretanto, não houve diferença estatística na análise objetiva realizada por meio da saturação de cores obtidas pelo programa ImageJ®. Conclusão: O colírio de brimonidina pode ser superior ao colírio de nafazolina + feniramina na redução do sangramento, levando-se em conta apenas a análise subjetiva.


ABSTRACT Objective: To evaluate the effect of 0.2% brimonidine eye drops in reducing hyperemia and ocular bleeding during strabismus surgeries, in comparison with 0.025% naphazoline + 0.3% pheniramine eye drops. Methods: Fourteen patients with strabismus and indication for bilateral surgical correction were evaluated. Before the procedure, the eye drops were instilled randomly in each eye of the evaluated patients. The subjective analysis of conjunctival hyperemia and perioperative bleeding was performed in a double-blind manner, by 02 surgeons. The objective assessment of the level of conjunctival hyperemia was performed by analyzing the images obtained using the ImageJ® software. Results: The analysis of multivariate mixed effect models indicated statistically significant differences between the groups in relation to hyperemia (rater 2) and intraoperative bleeding (raters 1 and 2) with higher scores in cases treated with naphazoline + pheniramine eye drops. However, there were no statistically significant differences in the objective analysis of color saturation obtained by the ImageJ® program. Conclusion: Brimonidine eye drops may be superior to naphazoline + pheniramine eye drops in reducing bleeding, taking into account the subjective analysis only.


Assuntos
Humanos , Masculino , Feminino , Criança , Adolescente , Adulto , Feniramina/administração & dosagem , Hemorragia Ocular/prevenção & controle , Estrabismo/cirurgia , Tartarato de Brimonidina/administração & dosagem , Hiperemia/prevenção & controle , Complicações Intraoperatórias/prevenção & controle , Nafazolina/administração & dosagem , Soluções Oftálmicas/administração & dosagem , Pré-Medicação , Procedimentos Cirúrgicos Oftalmológicos/métodos , Vasoconstrição/efeitos dos fármacos , Fotografação , Método Duplo-Cego , Administração Tópica , Agonistas de Receptores Adrenérgicos alfa 2/administração & dosagem , Hemostasia Cirúrgica/métodos
4.
J Drugs Dermatol ; 22(6): 566-575, 2023 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-37276164

RESUMO

Rosacea is a chronic skin disorder involving central facial erythema secondary to vascular instability and cutaneous inflammation. Rosacea is divided into different subtypes based on the morphology of the rash — erythematotelangiectatic, papulopustular, phymatous, and ocular rosacea. A less-known subtype called neurogenic rosacea has been proposed to categorize patients suffering from rosacea with erythematous flushing and burning sensation that is refractory to traditional treatment. There is minimal data on this subgroup of rosacea patients and its potential treatment options. This review aims to explore current medical literature to define characteristics of neurogenic rosacea and its management. We performed a systematic search of PubMed database and identified 6 articles meeting inclusion criteria with a total of 37 patients with suspected neurogenic rosacea. Combination treatments with topicals (eg, metronidazole, brimonidine), as well as oral medications including vascular (eg, beta blockers), psychiatric (eg, diazepam, duloxetine), neurologic (eg, pregabalin, sumatriptan), and antibiotic agents (eg, rifaximin), were often cited to have better outcomes, but this finding was highly variable between patients. There were isolated reports of effective management with onabotulinumtoxinA intradermal injections and endoscopic thoracic sympathectomy treatment. Current literature supports selecting agents aimed at treating the major symptom pattern (eg, erythema, telangiectasias, burning sensation). Neurogenic rosacea treatment: a literature review. Ivanic MG, Oulee A, Norden A, et al. J Drugs Dermatol. 2023;22(6):566-571. doi:10.36849/JDD.7181  .


Assuntos
Rosácea , Humanos , Rosácea/diagnóstico , Rosácea/tratamento farmacológico , Eritema/tratamento farmacológico , Metronidazol/uso terapêutico , Antibacterianos/uso terapêutico , Tartarato de Brimonidina
5.
Nat Commun ; 14(1): 2509, 2023 05 02.
Artigo em Inglês | MEDLINE | ID: mdl-37130851

RESUMO

Sustained drug delivery strategies have many potential benefits for treating a range of diseases, particularly chronic diseases that require treatment for years. For many chronic ocular diseases, patient adherence to eye drop dosing regimens and the need for frequent intraocular injections are significant barriers to effective disease management. Here, we utilize peptide engineering to impart melanin binding properties to peptide-drug conjugates to act as a sustained-release depot in the eye. We develop a super learning-based methodology to engineer multifunctional peptides that efficiently enter cells, bind to melanin, and have low cytotoxicity. When the lead multifunctional peptide (HR97) is conjugated to brimonidine, an intraocular pressure lowering drug that is prescribed for three times per day topical dosing, intraocular pressure reduction is observed for up to 18 days after a single intracameral injection in rabbits. Further, the cumulative intraocular pressure lowering effect increases ~17-fold compared to free brimonidine injection. Engineered multifunctional peptide-drug conjugates are a promising approach for providing sustained therapeutic delivery in the eye and beyond.


Assuntos
Sistemas de Liberação de Medicamentos , Melaninas , Animais , Coelhos , Tartarato de Brimonidina , Peptídeos , Aprendizado de Máquina
6.
Int J Dermatol ; 62(7): 888-894, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37212604

RESUMO

BACKGROUND: Facial erythema in rosacea is a troublesome embarrassing presentation with limited options of treatment. Daily brimonidine gel was shown to be an effective modality of treatment. Being unavailable in Egypt and the scarcity of objective evaluation of its therapeutic effect motivated the search for other alternatives. OBJECTIVE: To evaluate the use and effectiveness of topical brimonidine eye drops for the management of facial erythema in rosacea with the aid of objective assessment. METHODS: The study was conducted on 10 rosacea patients presented with facial erythema. Brimonidine tartrate eye drops 0.2% were applied twice daily for 3 months on areas of red facial skin. Punch biopsies were obtained before and after 3 months of treatment. Routine hematoxylin and eosin (H&E) staining as well as CD34 immunohistochemical staining were performed for all biopsies. Sections were examined to detect the changes in the count and the surface area of blood vessels. RESULTS: Evaluation of clinical results showed good improvement of facial redness at the end of treatment (55-75%). Only 10% of subjects expressed rebound erythema. H&E and CD34 stained sections showed an increased count of dilated dermal blood vessels, which decreased significantly after treatment in count and surface area (P = 0.005, and P = 0.004, respectively). CONCLUSION: Topical brimonidine eye drops proved to be effective in managing facial erythema in rosacea, providing an available and cheaper alternative to brimonidine gel. The study improved the subjective evaluation in the context of objective assessment of treatment efficacy.


Assuntos
Eritema , Rosácea , Humanos , Tartarato de Brimonidina/uso terapêutico , Administração Cutânea , Eritema/tratamento farmacológico , Rosácea/tratamento farmacológico , Resultado do Tratamento , Soluções Oftálmicas
8.
J Ocul Pharmacol Ther ; 38(8): 576-583, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-36178959

RESUMO

Purpose: This study aims to compare the cytotoxic, apoptotic, and oxidative effects of preserved and preservative-free forms of brimonidine 0.15% on the human corneal epithelial cell (HCEC) line. Methods: Time-dependent cytotoxicity studies were performed with the Alamar Blue method. For apoptotic studies, PE Annexin V and 7-amino-actinomycin (7-AAD) staining and flow cytometry were performed. Messenger RNA (mRNA) expressions of Bax, Bcl-2, and caspase-3, -9, -12, and protein expressions of Bax and Bcl-2 were evaluated by quantitative real-time polymerase chain reaction and Western blot method, respectively. Results: Cell viability was 76.4% with the preserved solution and 36.05% with the preservative-free solution at the fifth minute. No significant difference was observed with either solution at the 15-min mark, whereas cell viability did not change significantly after 1 h. In the apoptosis evaluation, it was observed that the preservative-free solution increased the early apoptotic activity to a greater degree (P < 0.05). Preservative-free solution also induced gene expression of proapoptotic Bax, caspase-9 and -12, and protein expression of Bax while reducing the protein expression of anti-apoptotic Bcl-2 (P < 0.0001). Preserved solution induced only the gene expression of caspase-12, and reduced the protein expression of Bcl-2 (P < 0.0001). No significant difference was observed in the reactive oxygen species (ROS) levels of either solution compared with the control group (P > 0.05). Conclusion: It was demonstrated that the preserved solution is less cytotoxic to the HCEC line in the early period, has less early apoptotic activity, and does not significantly increase ROS levels.


Assuntos
Apoptose , Proteínas Proto-Oncogênicas c-bcl-2 , Humanos , Caspase 3/metabolismo , Caspase 3/farmacologia , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismo , Proteína X Associada a bcl-2/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Caspase 9/metabolismo , Caspase 9/farmacologia , Tartarato de Brimonidina/farmacologia , Anexina A5/metabolismo , Caspase 12/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/farmacologia , Células Epiteliais , Conservantes Farmacêuticos/farmacologia , Estresse Oxidativo , RNA Mensageiro/metabolismo
9.
Dermatol Ther ; 35(11): e15819, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36097378

RESUMO

Brimonidine is a vasoconstrictive agent used to treat several dermatologic disorders. Here, we review the uses of brimonidine in different aspects of dermatology. We searched keywords including rosacea, erythema, topical brimonidine, dermatology, and skin disease in PubMed, Cochrane, and Google Scholar to collect the related published articles. In a review of 15 articles, we found topical brimonidine improved the facial erythema of rosacea. In addition, it reduced the erythema associated with alcohol flushing syndrome, intense pulsed light therapy, and photodynamic therapy. Furthermore, topical brimonidine was used as a hemostatic agent in dermatosurgery procedures such as Mohs surgery and nail surgery to reduce intra-operative and postoperative bleeding. Some side effects such as erythema, flushing, and burning were reported in a few patients. Based on our findings, brimonidine is a beneficial drug that can be used in various dermatologic disorders with negligible side effects.


Assuntos
Dermatologia , Rosácea , Humanos , Tartarato de Brimonidina/efeitos adversos , Resultado do Tratamento , Rosácea/tratamento farmacológico , Eritema/tratamento farmacológico
10.
J Dtsch Dermatol Ges ; 20(8): 1147-1165, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35929658

RESUMO

This updated and upgraded S2k guideline deals with the diagnosis and treatment of rosacea, which is a common, chronic inflammatory skin disease mostly affecting the face. Initially, rosacea is characterized by recurrent erythema, telangiectasia and flushing. Later, the inflammatory component predominates, with persistent erythema with follicular papules, papulopustules and pustules. The development of phyma, which usually occurs on the acral localizations, is the most severe manifestation. For the treatment of rosacea, the interdisciplinary guideline committee, with representatives of the German Dermatological Society (DDG), the Professional Association of German Dermatologists (BVDD), the German Opthalmological Society (DOG), the Society for Dermopharmacy (GD), the Swiss Society for Dermatology and Venereology (SGDV) and the German Rosacea Aid e. V., recommends the avoidance of trigger factors and topical applications of metronidazole, azelaic acid or ivermectin. For symptomatic treatment of persistent centrofacial erythema, the topical vasoconstrictors brimonidine or oxymetazoline can also be used. Systemic therapy is recommended for therapy-resistant and severe forms of rosacea papulopustulosa. The drug of choice is low-dose doxycycline. Alternatively, low-dose isotretinoin can be recommended. Ocular rosacea should be treated with lid margin hygiene. For topical treatment, ciclosporin eye drops, azithromycin, ivermectin or metronidazole are suggested.


Assuntos
Fármacos Dermatológicos , Rosácea , Tartarato de Brimonidina , Fármacos Dermatológicos/uso terapêutico , Eritema/tratamento farmacológico , Humanos , Ivermectina/uso terapêutico , Metronidazol/uso terapêutico , Rosácea/diagnóstico , Rosácea/tratamento farmacológico
11.
J Dermatol ; 49(11): 1139-1147, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35904063

RESUMO

The treatment of persistent erythema and rosacea flushing is extremely challenging, especially for patients with anxiety. The aim of this study was to verify the efficacy of carvedilol in rosacea patients with persistent erythema and flushing. A total of 156 patients were randomized to use oral carvedilol 5 mg bid (twice per day) (n = 105) or topical brimonidine (n = 51) for a 10-week period with 6 weeks of follow-up. Both the efficacy of carvedilol and the status of anxiety/depression were analyzed by patient self-assessment (PSA), clinician erythema assessment (CEA), generalized anxiety disorder (GAD-7), and patient health questionnaire-9 (PHQ-9). Our study found that carvedilol exerted a dramatic reduction in CEA/PSA scores and sting/burning sensation scores in comparison to topical brimonidine. Additionally, carvedilol treatment dramatically improved telangiectasia, erythema, and pigmentation with no obvious side effects. Patients with carvedilol treatment showed an improvement of depression/anxiety, as reflected by lower GAD-7 and PHQ-9 scores than patients with topical brimonidine. Notably, we found carvedilol treatment had better outcomes among patients under 30 years of age with rosacea younger than 30 years old. Conclusively, our findings reveal that carvedilol could quickly and effectively improve facial erythema, which might stem from the improved the status of anxiety/depression.


Assuntos
Depressão , Rosácea , Humanos , Adulto , Carvedilol/uso terapêutico , Rosácea/tratamento farmacológico , Eritema/tratamento farmacológico , Tartarato de Brimonidina/efeitos adversos , Ansiedade
12.
Lasers Surg Med ; 54(10): 1288-1297, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-35593006

RESUMO

INTRODUCTION: The ability of ablative fractional lasers (AFL) to enhance topical drug uptake is well established. After AFL delivery, however, drug clearance by local vasculature is poorly understood. Modifications in vascular clearance may enhance AFL-assisted drug concentrations and prolong drug dwell time in the skin. Aiming to assess the role and modifiability of vascular clearance after AFL-assisted delivery, this study examined the impact of vasoregulative interventions on AFL-assisted 5-fluorouracil (5-FU) concentrations in in vivo skin. METHODS: 5-FU uptake was assessed in intact and AFL-exposed skin in a live pig model. After fractional CO2 laser exposure (15 mJ/microbeam, 5% density), vasoregulative intervention using topical brimonidine cream, epinephrine solution, or pulsed dye laser (PDL) was performed in designated treatment areas, followed by a single 5% 5-FU cream application. At 0, 1, 4, 48, and 72 h, 5-FU concentrations were measured in 500 and 1500 µm skin layers by mass spectrometry (n = 6). A supplemental assessment of blood flow following AFL ± vasoregulation was performed using optical coherence tomography (OCT) in a human volunteer. RESULTS: Compared to intact skin, AFL facilitated a prompt peak in 5-FU delivery that remained elevated up to 4 hours (1500 µm: 1.5 vs. 31.8 ng/ml [1 hour, p = 0.002]; 5.3 vs. 14.5 ng/ml [4 hours, p = 0.039]). However, AFL's impact was transient, with 5-FU concentrations comparable to intact skin at later time points. Overall, vasoregulative intervention with brimonidine or PDL led to significantly higher peak 5-FU concentrations, prolonging the drug's dwell time in the skin versus AFL delivery alone. As such, brimonidine and PDL led to twofold higher 5-FU concentrations than AFL alone in both skin layers by 1 hour (e.g., 500 µm: 107 ng/ml [brimonidine]; 96.9 ng/ml [PDL], 46.6 ng/ml [AFL alone], p ≤ 0.024), and remained significantly elevated at 4 hours (p ≤ 0.024). A similar pattern was observed for epinephrine, although trends remained nonsignificant (p ≥ 0.09). Prolonged 5-FU delivery was provided by PDL, resulting in sustained drug deposition compared to AFL alone at both 48 and 72 hours in the superficial skin layer (p ≤ 0.024). Supporting drug delivery findings, OCT revealed that increases in local blood flow after AFL were mitigated in test areas also exposed to PDL, brimonidine, or epinephrine, with PDL providing the greatest, sustained reduction in flow over 48 hours. CONCLUSION: Vasoregulative intervention in conjunction with AFL-assisted delivery enhances and prolongs 5-FU deposition in in vivo skin.


Assuntos
Lasers de Gás , Pele , Suínos , Humanos , Animais , Fluoruracila , Tartarato de Brimonidina/uso terapêutico , Epinefrina
14.
Photochem Photobiol ; 98(6): 1390-1394, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-35338500

RESUMO

We investigated whether topical brimonidine delayed or enhanced the development of squamous cell carcinoma (SCC) when ultraviolet radiation (UVR) was applied to a well-established murine model. Hairless female mice (n = 125) were randomized into five groups and treated as follows: 1% brimonidine cream before UVR (Group 1), 0.33% brimonidine gel before UVR (Group 2), 1% brimonidine cream after UVR (Group 3), UVR only (control; Group 4) and 1% brimonidine cream only (control; Group 5). For each animal, the first four tumors were recorded and followed until three tumors reached 4 mm or one tumor reached 12 mm in diameter. All animal experiments continued for up to 365 days or until death. Application of 1% brimonidine cream before UVR delayed tumor development relative to control mice treated with UVR alone (P = 0.000006). However, when 0.33% brimonidine gel was applied before UVR (P = 0.313) or 1% brimonidine cream was applied after UVR (P = 0.252), there was no significant delay in tumor development relative to control mice treated with UVR alone. The development of the second and third tumors followed a similar pattern. Topical 1% brimonidine cream applied before UVR exposure delayed SCC development in hairless mice. In contrast, when brimonidine was applied after UVR there was no significant delay in tumor development. These results suggest that the 1% brimonidine cream probably absorbed the UVR, and therefore, a delay in tumor formation was only seen when brimonidine was applied before irradiation. However, there can be multiple reasons for this delay in photocarcinogenesis.


Assuntos
Carcinoma de Células Escamosas , Neoplasias Induzidas por Radiação , Neoplasias Cutâneas , Feminino , Camundongos , Animais , Camundongos Pelados , Raios Ultravioleta/efeitos adversos , Tartarato de Brimonidina/farmacologia , Tartarato de Brimonidina/uso terapêutico , Neoplasias Cutâneas/etiologia , Neoplasias Cutâneas/prevenção & controle , Neoplasias Cutâneas/patologia , Carcinoma de Células Escamosas/etiologia , Carcinoma de Células Escamosas/patologia
15.
Eur J Ophthalmol ; 32(6): 3476-3481, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35164600

RESUMO

PURPOSE: To evaluate the efficacy of preoperative topical brimonidine use to maintain visibility during trabeculectomy and control intraoperative bleeding and postoperative subconjunctival hemorrhage. METHODS: The first group comprised 35 eyes of 34 patients administered brimonidine tartrate 0.15% (Brimogut, Bilim Ilac, Turkey) eye drops 6 and 3 min before surgery, and 33 eyes of 31 patients who received no medication for vasoconstriction formed the second group. Preoperative and postoperative photographs and operation video images were taken and vision analysis software used. Black-and-white images were obtained to identify the blood vessel and surface hemorrhage areas. The surface area of the hemorrhage was calculated by counting the black pixels with Image J software. RESULTS: There was no significant difference between two groups in terms of baseline (preoperative) eye redness (p > 0.05). In the first group, the eye redness values were 344.7 ± 19.5 pixels preoperatively and 244.1 ± 23.3 pixels at the beginning of the surgery, respectively (p < 0.001). However, no significant change was observed in the second group in eye redness (348.2 ± 17.5 pixels preoperatively and 360.7 ± 26.8 pixels at the beginning of the surgery, p > 0.05). Cautery was used for an average of 11.91 ± 1.96 s in the first group and 25.57 ± 4.66 s in the second to control intraoperative bleeding (P < 0.001). CONCLUSION: Preoperative topical brimonidine use in trabeculectomy surgery significantly decreased intraoperative bleeding and postoperative subconjunctival hemorrhage and facilitated bleeding control.


Assuntos
Doenças da Túnica Conjuntiva , Hemorragia Ocular , Trabeculectomia , Tartarato de Brimonidina , Doenças da Túnica Conjuntiva/tratamento farmacológico , Doenças da Túnica Conjuntiva/etiologia , Doenças da Túnica Conjuntiva/prevenção & controle , Hemorragia Ocular/tratamento farmacológico , Hemorragia Ocular/etiologia , Hemorragia Ocular/prevenção & controle , Humanos , Pressão Intraocular , Soluções Oftálmicas , Quinoxalinas/uso terapêutico
16.
Dermatol Ther ; 35(4): e15327, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35060229

RESUMO

Persistent post acne erythema (PAE) is common cosmetically unacceptable and challenging sequelae of acne lesions. Tranexamic acid (TXA) is an antifibrinolytic agent that shows a positive effect on wound healing in several studies, and it showed benefits in treating skin diseases like melasma, rosacea erythema and ultraviolet induced pigmentations. Oxymetazoline (OXZ) is a synthetic, highly selective agonist for alpha 1A-adrenoceptor. It is a potent vasoconstrictor. OXZ hydrochloride 1% cream was approved by the FDA in January 2017 as a topical treatment for persistent facial erythema in rosacea patients. Brimonidine tartrate (BMT) is highly selective α2 adrenergic receptor agonist, results in direct, potent vasoconstriction of small arterioles and veins. In 2013, brimonidine 0.33% gel was the first topical therapy to be FDA approved for the treatment of persistent facial erythema from rosacea. To evaluate the efficacy and safety of topical triple combination (TXA 5% + OXZ 1.5% + BMT 0.33%) in the treatment of PAE planned as split face comparative study. This study was conducted on 40 patients diagnosed with persistent PAE for at least 3 months, the right side of the face was treated with topical triple combination in liposomal base and was compared to the left side to which topical lipocream (placebo) was applied as a control. Our treatment plan lasted for 3 months. According to the investigator's global assessment of photographs and computerized analysis of erythema using image analysis software, topical triple combination applied on the right side of face was significantly effective in diminishing PAE when compared to topical placebo left side. Topical triple combination is a safe and cost-effective treatment for PAE.


Assuntos
Acne Vulgar , Eritema , Acne Vulgar/complicações , Acne Vulgar/tratamento farmacológico , Administração Tópica , Tartarato de Brimonidina/administração & dosagem , Quimioterapia Combinada/efeitos adversos , Eritema/tratamento farmacológico , Eritema/etiologia , Humanos , Oximetazolina/administração & dosagem , Rosácea/tratamento farmacológico , Resultado do Tratamento
17.
Biotechnol Appl Biochem ; 69(1): 281-288, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33438819

RESUMO

Oxidative stress is to upregulate the pentose phosphate pathway (PPP). The PPP consists of two functional branches, glucose-6-phosphate dehydrogenase (G6PD) and 6-phosphogluconaste dehydrogenase (6PGD). Glutathione reductase (GR) has a significant role in catalyzing an oxidized glutathione form into a reduced form. The purpose of this study is to investigate the effects of brimonidine and proparacaine on the activity of 6PGD, G6PD, and GR enzymes purified from human erythrocytes. Brimonidine displayed considerable inhibition profile against G6PD with IC50 value and KI constant of 29.93 ± 3.56 and 48.46 ± 0.66 µM, respectively. On the other hand, proparacaine had no inhibitory effect against G6PD. KI values were found to be 66.06 ± 0.78 and 811.50 ± 11.13 µM for brimonidine and proparacaine, respectively, for 6PGD. KI values were found to be 144.10 ± 2.01 and 1,654.00 ± 26.29 µM for brimonidine and proparacaine, respectively, for GR. Herein, also in silico molecular docking studies were performed between drugs and enzymes.


Assuntos
Glucosefosfato Desidrogenase , Fosfogluconato Desidrogenase , Tartarato de Brimonidina/farmacologia , Glucose-6-Fosfato , Glucosefosfato Desidrogenase/metabolismo , Glutationa , Glutationa Redutase/metabolismo , Humanos , Simulação de Acoplamento Molecular , Via de Pentose Fosfato , Fosfogluconato Desidrogenase/metabolismo , Propoxicaína
18.
Clin Exp Optom ; 105(8): 813-816, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-34753412

RESUMO

CLINICAL RELEVANCE: Posterior capsule opacification is a common late complication of cataract surgery. Posterior capsule opening with Nd:YAG laser, which is the standard treatment, may cause transient elevation of intraocular pressure (IOP). BACKGROUND: To evaluate the efficacy of betaxolol 0.|5% compared to brimonidine 0.2%, in prevention of intraocular pressure increase after Nd:YAG Laser posterior capsulotomy. METHODS: In a double masked randomised clinical trial, 38 eyes from 38 pseudophakic patients over 21 years of age who had significant posterior capsule opacification after phacoemulsification were randomly assigned to receive either betaxolol 0.|5% (18 eyes) or brimonidine 0.|2% (20 eyes) one hour before Nd:YAG Laser posterior capsulotomy.| Exclusion criteria were: glaucoma or history of glaucoma surgery, active uveitis, active ocular infection, pregnancy, unstable cardiovascular condition and severe asthma and lung diseases. Intraocular pressure was measured by Goldmann applanation tonometry, 1 hour before applying the laser and 4 hours after the laser application. RESULTS: There was no statistically significant difference between the two groups regarding the baseline mean IOP and the 4-hour post-laser mean IOP. There was a statistically significant decrease in the 4-hour post-laser mean IOP as compared to the baseline mean IOP in each group. The mean IOP change in the betaxolol group, was -2.39 ± 1.79 mm Hg and in the brimonidine group was -4.25 ± 2.20 mm Hg. The difference was statistically significant (P = 0.007). None of the patients experienced clinically significant IOP increase (≥5 mm Hg) in either group. CONCLUSION: Use of a single topical dose of betaxolol 0.5% and brimonidine 0.2%, 1 hour before laser treatment, can prevent significant acute IOP increase after Nd:YAG laser posterior capsulotomy, and betaxolol may provide a new alternative for prophylactic use.


Assuntos
Opacificação da Cápsula , Glaucoma , Cápsula do Cristalino , Hipertensão Ocular , Humanos , Pressão Intraocular , Tartarato de Brimonidina/uso terapêutico , Betaxolol/uso terapêutico , Opacificação da Cápsula/cirurgia , Hipertensão Ocular/etiologia , Hipertensão Ocular/prevenção & controle , Capsulotomia Posterior/efeitos adversos , Glaucoma/tratamento farmacológico , Complicações Pós-Operatórias/prevenção & controle
19.
J Nanobiotechnology ; 19(1): 436, 2021 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-34930292

RESUMO

BACKGROUND: Oxidative stress contributes to retina ganglion cells (RGCs) loss in variety of ocular diseases, including ocular trauma, ocular vein occlusion, and glaucoma. Scavenging the excessed reactive oxygen species (ROS) in retinal neurovascular unit could be beneficial to RGCs survival. In this study, a polydopamine (PDA)-based nanoplatform is developed to protect RGCs. RESULTS: The PDA nanoparticles efficiently eliminate multi-types of ROS, protect endothelia and neuronal cells from oxidative damage, and inhibit microglia activation in retinas. In an optic nerve crush (ONC) model, single intravitreal injection of PDA nanoparticles could significantly attenuate RGCs loss via eliminating ROS in retinas, reducing the inflammatory response and maintaining barrier function of retinal vascular endothelia. Comparative transcriptome analysis of the retina implied that PDA nanoparticles improve RGCs survival probably by altering the expression of genes involved in inflammation and ROS production. Importantly, as a versatile drug carrier, PDA nanoparticles could deliver brimonidine (a neuroprotection drug) to synergistically attenuate RGCs loss and promote axon regeneration, thus restore visual function. CONCLUSIONS: The PDA nanoparticle-based therapeutic nanoplatform displayed excellent performance in ROS elimination, providing a promising probability for treating retinal degeneration diseases.


Assuntos
Indóis/uso terapêutico , Nanopartículas/química , Traumatismos do Nervo Óptico/patologia , Polímeros/uso terapêutico , Degeneração Retiniana/tratamento farmacológico , Animais , Tartarato de Brimonidina/química , Tartarato de Brimonidina/farmacologia , Tartarato de Brimonidina/uso terapêutico , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Células Endoteliais da Veia Umbilical Humana , Humanos , Peróxido de Hidrogênio/farmacologia , Indóis/química , Indóis/farmacologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Polímeros/química , Polímeros/farmacologia , Espécies Reativas de Oxigênio/química , Retina/efeitos dos fármacos , Retina/fisiologia , Degeneração Retiniana/patologia , Células Ganglionares da Retina/citologia , Células Ganglionares da Retina/metabolismo , Transcriptoma/efeitos dos fármacos
20.
JNMA J Nepal Med Assoc ; 59(233): 15-18, 2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-34508462

RESUMO

INTRODUCTION: Posterior capsular opacification is a common complication after cataract surgery. Neodynium Yttrium Aluminium Garnet laser capsulotomy is still the preferred treatment for posterior capsular opacification. This study was done to determine the use of Brimonidine eye drop in preventing the rise of intraocular pressure post-Neodynium Yttrium Aluminium Garnet laser capsulotomy. METHODS: A descriptive cross-sectional study was conducted in Lumbini eye institute and research center, Bhairahawa, Nepal, in 200 eyes with posterior capsular opacification using Brimonidine from Feb 1, 2019, to July 30, 2019. The Institutional Review Committee approved the study with approval number 0237. A convenient sampling method was used. Pre-capsulotomy best-corrected visual acuity, slit-lamp examination of the anterior segment, and dilated fundus examination were done. Intraocular pressure was measured with Goldmann Applanation Tonometer. Post capsulotomy patients were evaluated after one hour, two hours, and two weeks for intraocular pressure and any complications. The statistical analysis was done using Statistical Package of Social Sciences version 20.0 statistical analysis software. The descriptive statistical analysis of the study was done after the collection of the data. RESULTS: Mean age of patients at presentation was 61.61±SD 1.09. The mean intraocular pressure following Neodynium Yttrium aluminum garnet laser capsulotomy using brimonidine at 1 hour was 12.73±3.3 mmHg.and two hours was 11.98±3.2 mmHg. The mean energy per pulse was 2.3±SD 0.3 mJ. The mean duration of posterior capsular opacification from cataract surgery was 22.28 weeks. CONCLUSIONS: Neodynium Yttrium Aluminium Garnet laser capsulotomy had lower intraocular pressure after the Brimonidine eye drop procedure. The maximum mean reduction in intraocular pressure was observed after two hours.


Assuntos
Opacificação da Cápsula , Lasers de Estado Sólido , Cápsula do Cristalino , Tartarato de Brimonidina/uso terapêutico , Opacificação da Cápsula/etiologia , Opacificação da Cápsula/cirurgia , Estudos Transversais , Humanos , Pressão Intraocular , Lasers de Estado Sólido/efeitos adversos , Complicações Pós-Operatórias , Ítrio
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