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1.
BMC Ophthalmol ; 20(1): 489, 2020 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-33334316

RESUMO

BACKGROUND: Anterior uveitis secondary to topical brimonidine administration is rare and not well-defined. In glaucoma patients using brimonidine, one must consider this phenomenon to avoid mis-diagnosis and over-treatment with topical steroids which in turn may increase intraocular pressure (IOP). This is the largest case series including the longest patient follow-up in the current literature. METHODS: Sixteen patients (26 eyes) with consultant diagnosed brimonidine-associated anterior uveitis in a tertiary referral glaucoma clinic presenting between 2015 and 2019 were included in this retrospective case series. Clinical records were taken for descriptive analysis. Main outcome measures were the key clinical features, and disease course (therapy, IOP control, patient outcome). RESULTS: Key features were conjunctival ciliary injection and mutton fat keratic precipitation in all eyes. The findings were bilateral in 10 patients. Time between initiation of brimonidine treatment and presentation was 1 week to 49 months. Glaucoma sub-types were mostly pseudo-exfoliative and primary open angle glaucoma. Brimonidine treatment was stopped immediately. Additionally, topical corticosteroids were prescribed in 18 eyes and tapered down during the following 4 weeks. Thirteen eyes did not need surgical or laser treatment (median follow-up time 15 months). No patient showed recurrence of inflammation after cessation of brimonidine. CONCLUSIONS: This type of anterior uveitis is an uncommon but important manifestation which should always be considered in glaucoma patients on brimonidine treatment. Although treatable at its root cause, problems may persist, especially with respect to IOP control. The latter may necessitate glaucoma surgery after the resolved episode of the uveitis.


Assuntos
Agonistas de Receptores Adrenérgicos alfa 2/efeitos adversos , Anti-Hipertensivos/efeitos adversos , Tartarato de Brimonidina/efeitos adversos , Uveíte Anterior/induzido quimicamente , Administração Oftálmica , Idoso , Idoso de 80 Anos ou mais , Feminino , Seguimentos , Glaucoma de Ângulo Aberto/tratamento farmacológico , Humanos , Pressão Intraocular/efeitos dos fármacos , Masculino , Pessoa de Meia-Idade , Hipertensão Ocular/tratamento farmacológico , Soluções Oftálmicas , Estudos Retrospectivos , Uveíte Anterior/diagnóstico
2.
N Z Med J ; 133(1527): 83-94, 2020 12 18.
Artigo em Inglês | MEDLINE | ID: mdl-33332330

RESUMO

AIM: Drug-induced ocular inflammation is rare and may be overlooked as a cause of uveitis. The main objective was to describe the causes of drug-induced ocular inflammation. Secondary objectives included uveitis complications and drug rechallenge reactions. METHODS: A retrospective chart review at Auckland District Health Board's tertiary uveitis clinic (Auckland, New Zealand) was performed. Participants were identified using the uveitis database, which consists of 2,750 subjects. Fifty eyes of 35 subjects had drug-induced inflammation. RESULTS: Drug-induced inflammation occurred in 1.3% of subjects with uveitis. Mean age was 66.8±15.6 years, and 25 subjects (71.4%) were female. Drugs responsible were bisphosphonates (24 subjects, 68.6%), brimonidine (one subject, 2.9%), etanercept (three subjects, 8.6%), immune checkpoint inhibitors (two subjects, 5.7%), BRAF inhibitors (three subjects, 8.6%), EGFR inhibitors (one subject, 2.9%) and allopurinol/perindopril (one subject, 2.9%). In subjects with bisphosphonate inflammation, anterior uveitis occurred in 22 (91.7%) and scleritis in two (8.3%). A positive rechallenge reaction occurred in two subjects with zoledronate and one with alendronate. Uveitis occurred in six subjects (17.1%) treated with cancer drugs including immune checkpoint inhibitors, BRAF inhibitors and EGFR protein kinase inhibitors. Subjects with cancer-drug-induced uveitis were managed with corticosteroids and five subjects were able to continue therapy; in one subject uveitis was uncontrollable and required drug cessation. CONCLUSIONS: Ocular inflammation caused by bisphosphonates is usually mild and resolves on medication withdrawal. Uveitis seen in association with newer cancer medications can be more severe, but in most cases it can be managed without medication cessation.


Assuntos
Difosfonatos/efeitos adversos , Uveíte Anterior/induzido quimicamente , Ácido Zoledrônico/efeitos adversos , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Alendronato/efeitos adversos , Alopurinol/efeitos adversos , Anti-Inflamatórios não Esteroides/efeitos adversos , Anticorpos Monoclonais Humanizados/efeitos adversos , Anti-Hipertensivos/efeitos adversos , Tartarato de Brimonidina/efeitos adversos , Receptores ErbB/antagonistas & inibidores , Cloridrato de Erlotinib/efeitos adversos , Etanercepte/efeitos adversos , Feminino , Humanos , Imidazóis/efeitos adversos , Masculino , Pessoa de Meia-Idade , Nivolumabe/efeitos adversos , Oximas/efeitos adversos , Inibidores de Proteínas Quinases/efeitos adversos , Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores , Estudos Retrospectivos , Esclerite/induzido quimicamente , Vemurafenib/efeitos adversos
3.
Clin Ther ; 42(2): 263-275, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-32089329

RESUMO

PURPOSE: Many patients with open-angle glaucoma eventually require >2 medications to lower their intraocular pressure (IOP). Fixed-combination ophthalmic solutions can be advantageous in patients who require multiple medications, but the number of fixed combinations combining 3 complementary IOP-lowering agents remains limited. This study assessed the efficacy and safety of a triple fixed combination (TFC) of bimatoprost 0.01%/brimonidine 0.15%/timolol 0.5% ophthalmic solution in patients with primary open-angle glaucoma (POAG) or ocular hypertension (OHT), compared with a dual fixed combination (DFC) of brimonidine 0.2%/timolol 0.5%. METHODS: Patients with a baseline IOP of 23-34 mm Hg in both eyes and no history of IOP-lowering procedures were eligible for participation in this multicenter, double-masked, randomized, Phase III study. After washout of previous treatment (if applicable), patients were randomized to receive TFC or DFC twice daily in each eye for 3 months. The primary efficacy variable was the change from baseline in mean IOP in the worse eye at week 12 in the modified intent-to-treat (mITT) population. TFC was superior to DFC if the treatment difference (TFC - DFC) favored TFC at week 12 (P ≤ 0.05; 2-sample t test). Secondary and sensitivity analyses were also performed. Safety, including adverse events, was assessed at all visits. FINDINGS: The mITT/safety population included 185 patients (TFC, n = 90; DFC, n = 95). TFC superiority was demonstrated at all postbaseline visits (all, P < 0.001) through week 12 (week 12 treatment difference: ─2.17 mm Hg; 95% CI, ─3.12 to ─1.22). While treatment-related conjunctival hyperemia was more frequent with TFC than with DFC (47.8% vs 23.2%; P < 0.001), consistent with the additional presence of bimatoprost in TFC, most cases were mild and the numbers of patient discontinuations at week 12 were similar between the TFC and DFC groups (11 [12.2%] vs 7 [7.4%] patients; P = 0.266). No unexpected adverse events were reported. IMPLICATIONS: Compared with DFC, TFC provided superior IOP lowering throughout the primary efficacy period. An acceptable tolerability profile was observed through 12 months of use of TFC, offering an effective therapeutic option in patients with POAG or OHT who require multiple medications to control their IOP. Additional studies are required for the assessment of the long-term effects of TFC. ClinicalTrials.gov identifier: NCT01217606.


Assuntos
Anti-Hipertensivos/administração & dosagem , Bimatoprost/administração & dosagem , Tartarato de Brimonidina/administração & dosagem , Hipertensão Ocular/tratamento farmacológico , Soluções Oftálmicas/administração & dosagem , Timolol/administração & dosagem , Idoso , Anti-Hipertensivos/efeitos adversos , Bimatoprost/efeitos adversos , Brasil , Tartarato de Brimonidina/efeitos adversos , Método Duplo-Cego , Combinação de Medicamentos , Feminino , Humanos , Pressão Intraocular/efeitos dos fármacos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/efeitos adversos , Timolol/efeitos adversos
4.
Cutan Ocul Toxicol ; 39(1): 21-24, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31615279

RESUMO

Purpose: To compare the efficacy, safety, and potential advantages of the preservative-free versus preserved brimonidine %0.15 preparations in patients with primer open-angle glaucoma (POAG) or ocular hypertension (OHT).Methods: Forty-two eyes of the 21 treatment-naive patients with POAG or OHT were enrolled in this study. Eyes were randomly assigned to receive brimonidine-purite 0.15% or preservative-free brimonidine 0.15% two times daily. Efficacy of the two eye drops was assessed by measuring the intraocular pressure (IOP) at 9-10 am at baseline and week 4. Safety and potential advantages of the drops were evaluated at weeks 4 in terms of ocular symptoms and tear parameters. Ocular symptom values of the patients were evaluated with a scale of 0-4 (0 = no discomfort and 4 = severe discomfort).Results: Both of the brimonidine tartrate formulations resulted in statistically similar IOP reduction (preserved formulation; -5.2 mmHg [22.9% reduction] preservative-free formulation; -5.7 mmHg [24.1% reduction], p = 0.37). It was found that brimonidine tartrate formulations with and without topical preservatives did not produce a statistically significant difference in pain, stinging, and blurred vision at the upon instillation (p > 0.05). However, the burning sensation was significantly higher in the preservative-free formulation at the first instillation compared to the preserved formulation (p = 0.01). Also, there was no statistically significant difference between the two formulations in terms of symptoms (itching, burning, tearing, stinging, and photophobia) and tear parameters during the day (p > 0.05).Conclusions: Although topical preservative-free brimonidine tartrate treated eyes had a more burning sensation at the first drop, the two formulations were similar in terms of ocular tolerability in the short term period. Also, both formulations were found to reduce IOP at a similar rate.


Assuntos
Tartarato de Brimonidina/uso terapêutico , Glaucoma de Ângulo Aberto/tratamento farmacológico , Hipertensão Ocular/tratamento farmacológico , Conservantes Farmacêuticos/administração & dosagem , Agonistas de Receptores Adrenérgicos alfa 2/química , Agonistas de Receptores Adrenérgicos alfa 2/uso terapêutico , Adulto , Tartarato de Brimonidina/administração & dosagem , Tartarato de Brimonidina/efeitos adversos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/química , Soluções Oftálmicas/uso terapêutico , Conservantes Farmacêuticos/química
5.
Eur J Ophthalmol ; 30(5): NP23-NP25, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31096781

RESUMO

PURPOSE: To report two cases with corneal sterile infiltration presumably due to topical ocular hypotensive agent. METHOD: Case report. RESULTS: Case 1: A 65-year-old man presented with corneal opacity and neovascularization in his left eye. A diagnosis of glaucoma was made 2 years previously, and anti-glaucoma agents were prescribed (brimonidine tartrate, ripasudil hydrochloride hydrate, and brinzolamide) for both eyes. Case 2: A 75-year-old woman noticed corneal opacity in the left eye. A diagnosis of glaucoma was made 35 years previously, and anti-glaucoma agents were prescribed (brimonidine tartrate, 1% dorzolamide, and bimatoprost) for both eyes. In both cases, ocular examination revealed follicular conjunctivitis and blepharitis in both eyes, and corneal sterile infiltration with neovascularization in the left eyes. The three topical drugs were discontinued and replaced with 0.1% fluorometholone. Both the blepharitis and corneal sterile infiltration improved thereafter, although corneal opacity remained across the stromal layer. CONCLUSION: We encountered two cases of corneal and conjunctival complications that were suspected as side effects after brimonidine eye drop use. Special care should be taken to observe the condition of ocular surface when topical brimonidine is administered.


Assuntos
Anti-Hipertensivos/efeitos adversos , Blefarite/induzido quimicamente , Conjuntivite/induzido quimicamente , Neovascularização da Córnea/induzido quimicamente , Opacidade da Córnea/induzido quimicamente , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/etiologia , Idoso , Bimatoprost/efeitos adversos , Blefarite/diagnóstico , Tartarato de Brimonidina/efeitos adversos , Conjuntivite/diagnóstico , Neovascularização da Córnea/diagnóstico , Opacidade da Córnea/diagnóstico , Feminino , Humanos , Glaucoma de Baixa Tensão/tratamento farmacológico , Masculino , Soluções Oftálmicas , Sulfonamidas/efeitos adversos , Tiazinas/efeitos adversos , Tiofenos/efeitos adversos
7.
Indian J Ophthalmol ; 67(8): 1297-1302, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31332113

RESUMO

Purpose: To compare the lipid layer thickness (LLT) using the LipiView® ocular surface interferometer (TearScience® Inc, Morrisville, NC) between the eye treated with glaucoma medication and untreated normal eye in the unilateral glaucoma patients, and evaluate the effect of topical glaucoma medication on the LLT parameters in glaucoma eyes. Methods: The participants in this cross-sectional comparative study were unilateral glaucoma patients treated with topical glaucoma medications for more than 12 months. Three LLT parameters (average, minimum, and maximum) obtained by the LipiView® were compared between the glaucomatous eye and normal eye. The factors associated with LLT parameters in the eyes treated with glaucoma medication were investigated with multiple regression analysis. Results: Thirty patients with unilateral normal tension glaucoma were enrolled in the present study. Lipid layer average, minimum, and maximum were 64.83 ± 16.50, 51.63 ± 16.73, and 82.53 ± 20.62 in glaucomatous eyes, 77.26 ± 17.81, 62.83 ± 20.99, and 86.13 ± 15.42 in normal eyes. Lipid layer average and minimum were significantly thinner than those in normal eyes (P < 0.001, P < 0.001, respectively). Longer duration of glaucoma eye drops and a greater number of glaucoma medications were associated with the lower LLT average (ß = -0.456, P < 0.001, ß = -8.517, P = 0.003, respectively), and increasing glaucoma medications have a significant correlation with lower LLT minimum in glaucoma eyes (ß = -8.814, P = 0.026). Conclusion: The present study highlights that patients with long-term glaucoma medications need to be assessed for LLT parameters objectively evaluate their ocular surface health.


Assuntos
Anti-Hipertensivos/efeitos adversos , Metabolismo dos Lipídeos/efeitos dos fármacos , Glaucoma de Baixa Tensão/tratamento farmacológico , Lágrimas/metabolismo , Administração Oftálmica , Adulto , Idoso , Tartarato de Brimonidina/efeitos adversos , Estudos Transversais , Combinação de Medicamentos , Síndromes do Olho Seco/diagnóstico , Feminino , Gonioscopia , Humanos , Interferometria , Pressão Intraocular/fisiologia , Glaucoma de Baixa Tensão/metabolismo , Masculino , Disfunção da Glândula Tarsal/diagnóstico , Pessoa de Meia-Idade , Soluções Oftálmicas , Sulfonamidas/efeitos adversos , Tiofenos/efeitos adversos , Timolol/efeitos adversos , Tonometria Ocular
8.
Arq. bras. oftalmol ; 82(3): 236-238, May-June 2019. graf
Artigo em Inglês | LILACS | ID: biblio-1001314

RESUMO

ABSTRACT This report was written to describe a case of unilateral brimonidine-induced conjunctival lichen planus. Because the ophthalmic examination indicated chronic conjunctivitis or drug-induced pseudopemphigoid, the patient underwent thorough ophthalmic and systemic examinations, as well as conjunctival biopsy and direct immunofluorescence studies. A 71-year-old woman with unilateral left eye findings of chronic conjunctivitis was referred to our Ophthalmology Department. The patient reported that chronic conjunctivitis began shortly after she initiated use of topical brimonidine. Ophthalmic examination revealed foreshortening of the inferior fornix and symblepharon. Conjunctival biopsy revealed submucous lymphocytes and shaggy distribution of fibrinogen on direct immunofluorescence; this was suggestive of ocular lichen planus. No other systemic lesions were found that were consistent with the presentation of lichen planus. A good response was observed to topical cyclosporine treatment. To our knowledge, this may be the first report of unilateral ocular lichen planus without systemic findings. The correlation with the initiation of topical brimonidine suggests that this might be the first case of biopsy-confirmed brimonidine-induced ocular lichen planus.


RESUMO Este relato é para descrever um caso de líquen plano conjuntival unilateral induzido por brimonidina. Como o exame oftalmológico indicava conjuntivite crônica ou pseudopenfigóide induzido por medicamento, o paciente foi submetido a exames oftalmológicos e sistémicos completos, além de biópsia conjuntival e estudos de imunofluorescência direta. Uma mulher de 71 anos de idade com achados unilaterais do olho esquerdo de conjuntivite crônica foi encaminhada ao nosso departamento de Oftalmologia. A paciente relatou que a conjuntivite crônica começou logo após o início do uso da brimonidina tópica. O exame oftalmológico revelou encurtamento do fórnice inferior e do symblepharon. A biópsia conjuntival revelou linfócitos submucosos e distribuição felpuda de fibrinogênio na imunofluorescência direta; isso era sugestivo de líquen plano ocular. Não foram encontradas outras lesões sistêmicas compatíveis com a apresentação do líquen plano. Uma boa resposta foi observada no tratamento tópico com ciclosporina. Pelo nosso conhecimento, este pode ser o primeiro relato de líquen plano ocular unilateral sem achados sistêmicos. A correlação com o início da brimonidina tópica sugere que este pode ser o primeiro caso de líquen plano ocular induzido por brimonidina confirmado por biópsia.


Assuntos
Humanos , Feminino , Idoso , Doenças da Túnica Conjuntiva/induzido quimicamente , Tartarato de Brimonidina/efeitos adversos , Líquen Plano/induzido quimicamente , Anti-Hipertensivos/efeitos adversos , Biópsia , Ciclosporina/uso terapêutico , Túnica Conjuntiva/patologia , Doenças da Túnica Conjuntiva/patologia , Doenças da Túnica Conjuntiva/tratamento farmacológico , Imunossupressores/uso terapêutico , Líquen Plano/patologia , Líquen Plano/tratamento farmacológico
9.
Microsc Microanal ; 25(6): 1352-1366, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31018876

RESUMO

Brimonidine, an anti-glaucoma medicine, acts as an adrenergic agonist which decreases the synthesis of aqueous humour and increases the amount of drainage through Schlemm's canal and trabecular meshwork, but shows dose-dependent (0.2% solution thrice daily) toxicity. To reduce the side effects and improve the efficacy, brimonidine was nanoencapsulated on ultra-small-sized chitosan nanoparticles (nanobrimonidine) (28 ± 4 nm) with 39% encapsulation efficiency, monodispersity, freeze-thawing capability, storage stability, and 2% drug loading capacity. This nanocomplex showed burst, half, and complete release at 0.5, 45, and 100 h, respectively. Nanobrimonidine did not show any in vitro toxicity and was taken up by caveolae-mediated endocytosis. The nanobrimonidine-treated trabeculectomy tissue of glaucoma patients showed better dilation of the trabecular meshwork under the electron microscope. This is direct evidence for better bioavailability of nanobrimonidine after topical administration. Thus, the developed nanobrimonidine has the potential to improve the efficacy, reduce dosage and frequency, and improve delivery to the anterior chamber of the eye.


Assuntos
Agonistas de Receptores Adrenérgicos alfa 2/administração & dosagem , Tartarato de Brimonidina/administração & dosagem , Glaucoma/tratamento farmacológico , Nanocompostos/administração & dosagem , Malha Trabecular/efeitos dos fármacos , Agonistas de Receptores Adrenérgicos alfa 2/efeitos adversos , Agonistas de Receptores Adrenérgicos alfa 2/farmacocinética , Tartarato de Brimonidina/efeitos adversos , Tartarato de Brimonidina/farmacocinética , Quitosana/administração & dosagem , Portadores de Fármacos/administração & dosagem , Humanos , Modelos Teóricos , Resultado do Tratamento
10.
Arq Bras Oftalmol ; 82(3): 236-238, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30916215

RESUMO

This report was written to describe a case of unilateral brimonidine-induced conjunctival lichen planus. Because the ophthalmic examination indicated chronic conjunctivitis or drug-induced pseudopemphigoid, the patient underwent thorough ophthalmic and systemic examinations, as well as conjunctival biopsy and direct immunofluorescence studies. A 71-year-old woman with unilateral left eye findings of chronic conjunctivitis was referred to our Ophthalmology Department. The patient reported that chronic conjunctivitis began shortly after she initiated use of topical brimonidine. Ophthalmic examination revealed foreshortening of the inferior fornix and symblepharon. Conjunctival biopsy revealed submucous lymphocytes and shaggy distribution of fibrinogen on direct immunofluorescence; this was suggestive of ocular lichen planus. No other systemic lesions were found that were consistent with the presentation of lichen planus. A good response was observed to topical cyclosporine treatment. To our knowledge, this may be the first report of unilateral ocular lichen planus without systemic findings. The correlation with the initiation of topical brimonidine suggests that this might be the first case of biopsy-confirmed brimonidine-induced ocular lichen planus.


Assuntos
Anti-Hipertensivos/efeitos adversos , Tartarato de Brimonidina/efeitos adversos , Doenças da Túnica Conjuntiva/induzido quimicamente , Líquen Plano/induzido quimicamente , Idoso , Biópsia , Túnica Conjuntiva/patologia , Doenças da Túnica Conjuntiva/tratamento farmacológico , Doenças da Túnica Conjuntiva/patologia , Ciclosporina/uso terapêutico , Feminino , Humanos , Imunossupressores/uso terapêutico , Líquen Plano/tratamento farmacológico , Líquen Plano/patologia
15.
Arch Soc Esp Oftalmol ; 93(10): 511-514, 2018 Oct.
Artigo em Inglês, Espanhol | MEDLINE | ID: mdl-29910082

RESUMO

CLINICAL CASE: The case concerns an 81-year-old woman on treatment with a topical fixed combination of timolol and brimonidine who was diagnosed in the Emergency Department with acute anterior granulomatous hypertensive uveitis. The patient responded favourably to the withdrawal of the eye drops without showing any subsequent relapse. DISCUSSION: Uveitis due to brimonidine is a rare adverse effect, but it must be known. Once the diagnosis is suspected, the effective treatment is the withdrawal of brimonidine, with or without the addition of topical corticosteroids to control inflammation depending on the severity of the condition. It is a process with an excellent prognosis.


Assuntos
Agonistas de Receptores Adrenérgicos alfa 2/efeitos adversos , Tartarato de Brimonidina/efeitos adversos , Soluções Oftálmicas/efeitos adversos , Uveíte Anterior/induzido quimicamente , Doença Aguda , Agonistas de Receptores Adrenérgicos alfa 2/uso terapêutico , Idoso de 80 Anos ou mais , Tartarato de Brimonidina/uso terapêutico , Conjuntivite Alérgica/induzido quimicamente , Ciclopentolato/uso terapêutico , Quimioterapia Combinada , Epitélio Anterior/patologia , Feminino , Glaucoma de Ângulo Aberto/tratamento farmacológico , Granuloma/induzido quimicamente , Humanos , Latanoprosta/uso terapêutico , Lubrificantes Oftálmicos , Hipertensão Ocular/induzido quimicamente , Prednisolona/análogos & derivados , Prednisolona/uso terapêutico , Sulfonamidas/uso terapêutico , Tiofenos/uso terapêutico , Timolol/uso terapêutico , Uveíte Anterior/diagnóstico , Uveíte Anterior/tratamento farmacológico
16.
Dermatol Clin ; 36(2): 151-159, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29499798

RESUMO

Persistent centrofacial erythema is a predominant component of rosacea. The authors review the topical and systemic treatments for rosacea-related erythema and flushing to aid in treatment decision making in clinical practice. Databases were searched for literature pertaining to treatment options for erythema related to rosacea. The paucity of large-scale clinical trials in patients with the erythematotelangiectatic rosacea subtype makes it difficult to draw firm conclusions regarding treatment. Although certain topical and oral treatments appear to have modest benefit in reducing erythema, there is a need for high-quality, well-designed, and rigorously reported studies for the treatments for rosacea.


Assuntos
Agonistas alfa-Adrenérgicos/uso terapêutico , Anti-Hipertensivos/uso terapêutico , Tartarato de Brimonidina/uso terapêutico , Eritema/tratamento farmacológico , Eritema/etiologia , Oximetazolina/uso terapêutico , Rosácea/complicações , Administração Cutânea , Anti-Hipertensivos/administração & dosagem , Tartarato de Brimonidina/efeitos adversos , Inibidores de Calcineurina/uso terapêutico , Face , Humanos , Uso Off-Label , Retinoides/administração & dosagem , Tetraciclinas/uso terapêutico
17.
Drugs R D ; 18(1): 87-90, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29374829

RESUMO

BACKGROUND: Topical α-adrenergic agonist therapy has been developed to treat the persistent erythema of rosacea patients. Brimonidine and oxymetazoline are both topical α-adrenergic agonists. OBJECTIVES: The objective of this in vitro safety pharmacology study was to compare the potential safety profiles of brimonidine and oxymetazoline. METHODS: Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including α-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors. A valvular interstitial cell (VIC) proliferation assay was performed with oxymetazoline hydrochloride. RESULTS: Brimonidine was highly selective for the α2 adrenergic receptors, specifically α2A, whereas oxymetazoline was found to be much less selective and was highly active against a wide range of targets. Negligible activity was observed with brimonidine at the 5-HT2B receptor, whereas oxymetazoline had significant 5-HT2B receptor agonist activity and caused proliferation of mitral VICs in vitro. CONCLUSION: As the 5-HT2B receptor is potentially involved in drug-induced valvulopathy, the benefit/risk ratio should be carefully considered, especially in patients with cardiovascular disease or other comorbidities.


Assuntos
Bioensaio , Tartarato de Brimonidina/efeitos adversos , Proliferação de Células/efeitos dos fármacos , Oximetazolina/efeitos adversos , Administração Tópica , Agonistas alfa-Adrenérgicos/administração & dosagem , Agonistas alfa-Adrenérgicos/efeitos adversos , Agonistas alfa-Adrenérgicos/farmacologia , Tartarato de Brimonidina/administração & dosagem , Tartarato de Brimonidina/farmacologia , Células Cultivadas , Valvas Cardíacas/efeitos dos fármacos , Humanos , Oximetazolina/administração & dosagem , Oximetazolina/farmacologia
18.
J Ocul Pharmacol Ther ; 34(3): 274-279, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29297751

RESUMO

PURPOSE: To evaluate efficacy and safety of brinzolamide (1%)/brimonidine (0.2%) fixed combination (BBFC) in normal tension glaucoma (NTG). METHODS: This retrospective study included NTG patients treated with BBFC as their primary therapy, NTG patients who had changed their medication to BBFC from brinzolamide or brimonidine, and NTG patients who had changed their medication to BBFC from concomitantly using brinzolamide and brimonidine. The intraocular pressure (IOP), mean deviation value, and adverse drug reactions were evaluated. RESULTS: In the BBFC primary therapy group, the baseline IOP was 17.1 ± 1.4 mmHg, and the mean IOP at 18 months after using BBFC was 12.4 ± 1.8 mmHg. In the brinzolamide monotherapy group, the baseline IOP was 16.2 ± 1.4 mmHg, the mean IOP using brinzolamide was 13.4 ± 1.6 mmHg, and the mean IOP at 18 months after changing to BBFC was 12.3 ± 1.4 mmHg. In the brimonidine monotherapy group, the baseline IOP was 16.5 ± 1.5 mmHg, the mean IOP using brimonidine was 13.3 ± 1.6 mmHg, and the mean IOP at 18 months after changing to BBFC was 12.4 ± 1.4 mmHg. In the unfixed brinzolamide and brimonidine group, the baseline IOP was 17.5 ± 1.3 mmHg, the mean IOP when using unfixed brinzolamide and brimonidine was 12.4 ± 1.4 mmHg, and the mean IOP at 18 months after changing to BBFC was 12.6 ± 1.5 mmHg. There were no serious adverse drug reactions. CONCLUSIONS: BBFC provides a significant IOP reduction and is a safe antiglaucoma medication for NTG patients.


Assuntos
Anti-Hipertensivos/uso terapêutico , Tartarato de Brimonidina/uso terapêutico , Pressão Intraocular/efeitos dos fármacos , Glaucoma de Baixa Tensão/tratamento farmacológico , Soluções Oftálmicas/uso terapêutico , Sulfonamidas/uso terapêutico , Tiazinas/uso terapêutico , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/efeitos adversos , Tartarato de Brimonidina/administração & dosagem , Tartarato de Brimonidina/efeitos adversos , Combinação de Medicamentos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/efeitos adversos , Estudos Retrospectivos , Sulfonamidas/administração & dosagem , Sulfonamidas/efeitos adversos , Tiazinas/administração & dosagem , Tiazinas/efeitos adversos
19.
Cornea ; 36(12): 1567-1569, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28938378

RESUMO

PURPOSE: The primary side effects associated with 0.1% brimonidine tartrate (BT) ophthalmic solution with sodium chlorite are allergic conjunctivitis, blepharitis, and conjunctival hyperemia. However, cornea-related side effects are rare. In this study, we report 2 similar cases in which corneal neovascularization, corneal infiltration, and corneal opacity developed after BT eye-drop use. METHODS: Retrospective report of 2 cases of corneal infiltration after BT eye-drop use. RESULTS: Case 1 involved a 78-year-old woman with follicular conjunctivitis, corneal neovascularization, and infiltration in her left eye after unilateral instillation of BT eye drops in that eye. Case 2 involved a 75-year-old woman with bilateral corneal neovascularization and infiltration after instillation of BT eye drops. In both cases, the corneal complications were deemed to be side effects of BT, so those eye drops were replaced with 0.1% fluorometholone eye drops. After replacement, blepharitis and corneal neovascularization successfully resolved; however, a layer of opacity remained across the transparent layer of the cornea in both cases. CONCLUSIONS: We encountered 2 cases of corneal and conjunctival complications that developed as side effects after BT eye-drop use, thus indicating that strict attention should be paid to the possibility of side effects after initiation of antiglaucoma eye-drop use.


Assuntos
Anti-Hipertensivos/efeitos adversos , Tartarato de Brimonidina/efeitos adversos , Conjuntivite/induzido quimicamente , Neovascularização da Córnea/induzido quimicamente , Soluções Oftálmicas/efeitos adversos , Idoso , Feminino , Glaucoma/tratamento farmacológico , Humanos
20.
J Drugs Dermatol ; 16(9): 909-916, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28915286

RESUMO

BACKGROUND: There is currently a lack of data on the simultaneous treatment of different features of rosacea. Individually, ivermectin 1% (IVM) cream and brimonidine 0.33% (BR) gel have demonstrated efficacy on inflammatory lesions and persistent erythema, respectively. OBJECTIVE: To evaluate the efficacy, safety, patient satisfaction, and optimal timing of administration of IVM associated with BR (IVM+BR) versus their vehicles in rosacea (investigator global assessment [IGA] ≥3). METHODS: Multicenter, randomized, double-blind study including subjects with rosacea characterized by moderate to severe persistent erythema and inflammatory lesions. The active treatment group included the IVM+BR/12 weeks subgroup (once-daily BR and once-daily IVM for 12 weeks), and the IVM+BR/8 weeks subgroup (once-daily BR vehicle for 4 weeks followed by once-daily BR for the remaining 8 weeks and once-daily IVM for 12 weeks). The vehicle group received once-daily BR vehicle and once-daily IVM vehicle for 12 weeks. RESULTS: The association showed superior efficacy (IGA success [clear/almost clear]) for erythema and inflammatory lesions in the total active group (combined active subgroups) compared to vehicle (55.8% vs. 36.8%, P=0.007) at week 12. The success rate increased from 32.7% to 61.2% at hour 0 and hour 3, respectively, in the IVM+BR/12 weeks subgroup, and from 28.3% to 50% in the IVM+BR/8 weeks subgroup. Reductions in erythema and inflammatory lesion counts confirmed the additive effect of BR to IVM treatment. Subjects reported greater improvement in the active subgroups than in the vehicle group, and similar rates for facial appearance satisfaction after the first 4 weeks of treatment in both active subgroups. All groups showed similar tolerability profiles. CONCLUSION: Concomitant administration of IVM cream with BR gel demonstrated good efficacy and safety, endorsing the comprehensive approach to this complex disease. Early introduction of BR, along with a complete daily skin care regimen may accelerate treatment success without impairing tolerability.

J Drugs Dermatol. 2017;16(9):909-916.

.


Assuntos
Tartarato de Brimonidina/administração & dosagem , Fármacos Dermatológicos/administração & dosagem , Ivermectina/administração & dosagem , Rosácea/tratamento farmacológico , Administração Cutânea , Adulto , Idoso , Idoso de 80 Anos ou mais , Tartarato de Brimonidina/efeitos adversos , Fármacos Dermatológicos/efeitos adversos , Método Duplo-Cego , Quimioterapia Combinada , Feminino , Géis , Humanos , Ivermectina/efeitos adversos , Masculino , Pessoa de Meia-Idade , Satisfação do Paciente , Creme para a Pele , Resultado do Tratamento , Adulto Jovem
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