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Braz. J. Pharm. Sci. (Online) ; 56: e18092, 2020. tab, graf
Article in English | LILACS | ID: biblio-1142491


We synthesized a series of compounds bearing pharmacologically important 1,3,4-oxadiazole and piperidine moieties. Spectral data analysis by 1H-NMR, 13C-NMR, IR and EI-MS was used to elucidate the structures of the synthesized molecules. Docking studies explained the different types of interaction of the compounds with amino acids, while bovine serum albumin (BSA) binding interactions showed their pharmacological effectiveness. Antibacterial screening of these compounds demonstrated moderate to strong activity against Salmonella typhi and Bacillus subtilis but only weak to moderate activity against the other three bacterial strains tested. Seven compounds were the most active members as acetyl cholinesterase inhibitors. All the compounds presented displayed strong inhibitory activity against urease. Compounds 7l, 7m, 7n, 7o, 7p, 7r, 7u, 7v, 7x and 7v were highly active, with respective IC50 values of 2.14±0.003, 0.63±0.001, 2.17±0.006, 1.13±0.003, 1.21±0.005, 6.28±0.003, 2.39±0.005, 2.15±0.002, 2.26±0.003 and 2.14±0.002 µM, compared to thiourea, used as the reference standard (IC50 = 21.25±0.15 µM). These new urease inhibitors could replace existing drugs after their evaluation in comprehensive in vivo studies.

Computer Simulation/classification , Salmonella typhi/classification , Sulfonamides/adverse effects , Thiourea , Bacillus subtilis/classification , Urease , Serum Albumin, Bovine , Pharmaceutical Preparations/administration & dosage , Cholinesterase Inhibitors/pharmacology , Inhibitory Concentration 50 , Proton Magnetic Resonance Spectroscopy/methods , Data Analysis , Amino Acids/antagonists & inhibitors
Arq. gastroenterol ; 56(4): 390-393, Oct.-Dec. 2019. tab
Article in English | LILACS | ID: biblio-1055169


ABSTRACT BACKGROUND: Drug-induced liver injury is still misunderstood in Brazil due to diagnostic difficulties or lack of reporting incidents. OBJECTIVE: To assess the frequency of adverse events related to the use of medicines in a primary healthcare unit, in a city locate southwestern of the state of Bahia, Brazil. METHODS: Prospective study conducted at the Primary Center for Specialized Health (CEMEA), February at August of 2013 in Vitoria da Conquista, Bahia, Brazil. Interviews were conducted with patients over 18 years old, and their clinical and laboratorial data were collected. The CIOMS scale was used to validate the cases. RESULTS: A total of 149 patients, mainly Afro-Brazilian women, received follow-up. Among these patients, three cases of hepatotoxicity were identified, and the medicines associated to drug-induced liver injuries were: nimesulide, budesonide and valacyclovir. CONCLUSION: Drug-induced liver injury is rare in primary healthcare units. It also allowed estimating the incidence of hepatotoxicity induced by allopathic medicines which are standardized by public healthcare authorities.

RESUMO CONTEXTO: As lesões hepáticas induzidas por drogas (DILI), ainda são mal compreendidas no Brasil devido a dificuldades diagnósticas ou à falta de relatos. OBJETIVO: Avaliar a frequência de eventos adversos relacionados ao uso de medicamentos em uma unidade básica de saúde, em uma cidade do sudoeste baiano. MÉTODOS: Estudo prospectivo realizado no período de fevereiro a agosto de 2013 em Vitória da Conquista, Bahia, Brasil. Entrevistas foram realizadas com pacientes maiores de 18 anos; os dados clínicos e laboratoriais foram coletados. A escala do CIOMS foi usada para avaliar causalidade dos casos. RESULTADOS: Um total de 149 pacientes, principalmente mulheres afro-brasileiras, receberam acompanhamento. Entre esses pacientes, três casos de hepatotoxicidade foram identificados e os medicamentos associados à DILI foram: nimesulida, budesonida e valaciclovir. CONCLUSÃO: DILI é raro em unidades básicas de saúde. Os três casos foram todos reversíveis, sem necessidade de internação hospitalar. Políticas de saúde que fomentam a prática da farmacovigilância são extremamente importantes para a prevenção e detecção de DILI.

Humans , Male , Female , Adult , Sulfonamides/adverse effects , Drug Monitoring/methods , Budesonide/adverse effects , Chemical and Drug Induced Liver Injury/epidemiology , Valacyclovir/adverse effects , Primary Health Care , Brazil/epidemiology , Prospective Studies , Middle Aged
Ann. hepatol ; 16(1): 71-76, Jan.-Feb. 2017. graf
Article in English | LILACS | ID: biblio-838088


Abstract: Background. Daclatasvir and asunaprevir dual therapy is approved for the treatment of HCV genotype 1b infection in several countries. Aim. To evaluate the efficacy and safety of daclatasvir and asunaprevir dual therapy in Turkish patients. Material and methods. Sixty-one patients with HCV genotype 1b were enrolled in the Turkish early access program. Most of the patients were in difficult-to-treat category. Patients were visited at each 4 week throughout the follow-up period. Laboratory findings and adverse events were recorded at each visit. Results. Fifty-seven of 61 enrolled patients completed 24 weeks of treatment. Two patients died as a result of underlying diseases at 12-14th weeks of treatment. Two patients stopped the treatment early as a consequence of virological breakthrough, and 2 patients had viral relapse at the post-treatment follow-up. Overall SVR12 rates were 90% (55/61) and 93.2% (55/59) according to intention-to-treat (ITT) and per protocol (PP) analysis respectively. In ITT analysis, SVR12 was achieved by 93% (13/14) in relapsers, 80% (12/15) in interferon-ineligible patients and 91% (20/22) in previous nonresponder patients. SVR12 rates were 86.5% and 91.4% in patients with cirrhosis according to ITT and PP analysis respectively. SVR12 was 95.8% in non-cirrhosis group in both analysis. Patients with previous protease inhibitor experience had an SVR12 of 87.5%. Common adverse events developed in 28.8% of patients. There were no treatment related severe adverse event or grade-4 laboratory abnormality. Conclusions. Daclatasvir and asunaprevir dual therapy is found to be effective and safe in difficult-to-treat Turkish patients with HCV genotype 1b infection.

Humans , Male , Female , Middle Aged , Aged , Antiviral Agents/therapeutic use , Sulfonamides/therapeutic use , Hepacivirus/drug effects , Hepatitis C, Chronic/drug therapy , Health Services Accessibility , Imidazoles/therapeutic use , Isoquinolines/therapeutic use , Antiviral Agents/economics , Antiviral Agents/adverse effects , Sulfonamides/economics , Sulfonamides/adverse effects , Time Factors , Turkey , RNA, Viral/genetics , Program Evaluation , Treatment Outcome , Drug Costs , Cost-Benefit Analysis , Hepacivirus/genetics , Viral Load , Hepatitis C, Chronic/diagnosis , Hepatitis C, Chronic/economics , Hepatitis C, Chronic/virology , Drug Therapy, Combination , Genotype , Health Services Accessibility/economics , Imidazoles/economics , Imidazoles/adverse effects , Isoquinolines/economics , Isoquinolines/adverse effects
Säo Paulo med. j ; 133(4): 371-376, July-Aug. 2015. tab, graf
Article in English | LILACS | ID: lil-763366


CONTEXT:Nimesulide is a selective inhibitor of the enzyme cyclooxygenase 2. Although considered to be a safe drug, cases of acute hepatitis and fulminant liver failure have been reported in Europe, the United States and South America, especially among elderly female patients. Until now, there had not been any reports in the literature relating to Brazilian subjects.CASE REPORT:An 81-year old female who had been using nimesulide therapy for six days presented hematemesis and epistaxis two days before hospitalization. Clinical examination showed an extensive coagulation disorder, diffuse hematomas, hypotension and tachypnea. Laboratory tests revealed abnormalities in coagulation tests; leukocytosis; reduced platelet, hemoglobin and red blood cell counts; and elevated direct bilirubin, serum aspartate transaminase (AST), gamma-glutamyl transpeptidase (GGT), alkaline phosphatase and renal function biomarkers. Hepatitis B and C tests were not reactive. Carcinoembryonic antigen (CEA), CA-19-9 and CA-125 levels were increased by, respectively, 1,000, 10,000 and 13 fold, whereas the alpha-fetoprotein level was normal, thus indicating a malignant tumor in the bile duct that did not originate from the liver. Thirty-six hours after hospitalization, the patient's condition worsened, leading to death. The necropsy findings included acute hepatitis with hepatocellular collapse, as well as metastasis of a carcinoma, probably from the bile duct.CONCLUSION:Despite the carcinoma presented by the patient, nimesulide use may have contributed towards the fatal acute liver failure. Until this issue has been clarified, caution is required in prescribing nimesulide for liver disease patients.

CONTEXTO:A nimesulida é um inibidor seletivo da enzima ciclo-oxigenase 2. Apesar de ela ser considerada fármaco seguro, casos de hepatite aguda e falência hepática fulminante foram descritos na Europa, Estados Unidos e América do Sul, principalmente em idosos do sexo feminino. Até o momento não há relatos na literatura em indivíduos brasileiros.RELATO DE CASO:Mulher de 81 anos, em uso terapêutico de nimesulida por seis dias, apresentou hematêmese e epistaxe dois dias antes da hospitalização. O exame clínico mostrou importante distúrbio de coagulação, hematomas difusos, hipotensão e taquipneia. Os exames laboratoriais mostravam alteração das provas de coagulação, leucocitose, redução do número de plaquetas, hemoglobina e hemácias, aumento de bilirrubina direta, elevação dos valores de aspartato aminotransferase (AST), gama glutamil transpeptidase (GGT), fosfatase alcalina e marcadores de função renal. Exames para hepatite B e C apresentaram-se não reagentes. Elevados níveis dos marcadores antígeno carcinoembriônico (CEA), CA-19-9 e CA-125 foram encontrados (1.000, 10.000 e 13 vezes, respectivamente), enquanto a alfa-fetoproteína estava normal, indicando um tumor maligno no ducto biliar, não oriundo do fígado. Trinta e seis horas após a hospitalização, a paciente evoluiu a óbito. Os achados necroscópicos incluíram hepatite aguda com colapso hepatocelular, bem como metástase de carcinoma, provavelmente do ducto biliar.CONCLUSÃO:Apesar do carcinoma apresentado pela paciente, o uso de nimesulida pode ter contribuído para o dano hepático. Até que esta questão seja esclarecida, a prescrição de nimesulida deve ser cuidadosa para pacientes com doenças hepáticas.

Aged, 80 and over , Female , Humans , Adenocarcinoma/secondary , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Liver Failure, Acute/chemically induced , Liver Neoplasms/pathology , Sulfonamides/adverse effects , Chemical and Drug Induced Liver Injury/pathology , Fatal Outcome , Liver Failure, Acute/pathology
An. bras. dermatol ; 90(3,supl.1): 242-246, May-June 2015. ilus
Article in English | LILACS | ID: lil-755771



Vemurafenib is a selective inhibitor of V600E-mutant BRAF protein used to treat metastatic and unresectable melanoma. Clinical trials have shown increased overall survival and progression-free survival in patients treated with Vemurafenib. However, cutaneous adverse events are common during treatment. We report fi ve cases of metastatic melanoma with BRAF V600E positivity, treated with Vemurafenib and its cutaneous adverse events. Dermatologists and oncologists need to be aware of possible skin changes caused by this medication, which is increasingly employed in melanoma treatment. Monitoring of patients during therapy is important for early treatment of adverse cutaneous cutaneous adverse events, improvement in quality of life and adherence to treatment.


Adult , Aged , Female , Humans , Male , Middle Aged , Antineoplastic Agents/adverse effects , Indoles/adverse effects , Melanoma/drug therapy , Proto-Oncogene Proteins B-raf/antagonists & inhibitors , Skin Diseases/chemically induced , Skin Neoplasms/drug therapy , Sulfonamides/adverse effects , Biopsy , Fatal Outcome , Melanoma/secondary , Neoplasm Metastasis/drug therapy , Skin Diseases/pathology , Skin Neoplasms/pathology , Time Factors , Treatment Outcome
Article in English | WPRIM | ID: wpr-157977


BACKGROUND/AIMS: We assessed the efficacy and safety of bosentan in patients with pulmonary arterial hypertension (PAH). METHODS: We surveyed randomized controlled trials (RCTs) of the efficacy and safety of bosentan in patients with PAH using MEDLINE, EMBASE, the Cochrane Controlled Trials Register, and manual searches. Meta-analysis of RCTs was performed to determine treatment efficacy and safety outcomes. Results are presented as odds ratios (ORs) or weighted mean differences (WMDs). RESULTS: Meta-analysis of seven RCTs including a total of 410 patients and 296 controls revealed that the 6-minute work distance was significantly higher in the bosentan group than in the placebo group (WMD, 46.19; 95% confidence interval [CI], 21.20 to 71.19; p = 2.9 x 10(-5)). Compared with the placebo, bosentan significantly reduced the mean pulmonary arterial pressure in patients with PAH (WMD, -6.026; 95% CI, -8.785 to -3.268, p = 1.8 x 10(-6)). The bosentan therapy group worsened less clinically than the placebo group (OR, 0.252; 95% CI, 0.140 to 0.454; p = 4.6 x 10(-7)). The incidence of serious adverse events did not differ between the bosentan and placebo groups (OR, 0.948; 95% CI, 0.556 to 1.614; p = 0.843). However, the results of the abnormal liver function test (LFT) were significantly higher in the bosentan group than in the placebo group (OR, 2.312; 95% CI, 1.020 to 5.241; p = 0.045). CONCLUSIONS: This meta-analysis shows that bosentan can treat PAH effectively. However, bosentan increased the incidence of abnormal LFT results compared with the placebo.

Antihypertensive Agents/adverse effects , Arterial Pressure/drug effects , Humans , Hypertension, Pulmonary/diagnosis , Liver/drug effects , Liver Function Tests , Odds Ratio , Pulmonary Artery/drug effects , Risk Factors , Sulfonamides/adverse effects , Time Factors , Treatment Outcome
Article in English | WPRIM | ID: wpr-173135


Some patients with chronic obstructive pulmonary disease (COPD) have pulmonary hypertension (PH) that adversely affects survival. We performed a systematic review and meta-analysis to assess whether PH-specific therapies have an effect for stable COPD. Data sources were Medline, EMBASE, Cochrane Central Register of Controlled Trials, Korea med and references from relevant publications. Randomized prospective trials that compared PH specific therapy in COPD for more than 6 weeks with placebo were included. The outcomes were the exercise capacity and adverse events. Four randomized controlled trials involving 109 subjects were included in the analysis. Two trials involved bosentan, one sildenafil and one beraprost. The studies varied in duration of treatment from 3 to 18 months. In a pooled analysis of four trials, exercise-capacity was not significantly improved with PH-specific treatment for COPD (risk ratio, -5.1; 95% CI, -13.0 to 2.8). COPD with overt PH significantly improved the exercise capacity (mean difference, 111.6; 95% CI, 63.3 to 159.9) but COPD with PH unknown did not (mean difference, 26.6; 95% CI, -24.3 to 77.5). There was no significant difference in hypoxemia (mean difference, 2.6; 95% CI, -3.7 to 8.8). PH specific treatments have a significant effect in improving exercise capacity in COPD with overt PH.

Hypoxia , Antihypertensive Agents/adverse effects , Clinical Trials as Topic , Databases, Factual , Epoprostenol/adverse effects , Humans , Hypertension, Pulmonary/complications , Piperazines/adverse effects , Pulmonary Disease, Chronic Obstructive/etiology , Purines/adverse effects , Surveys and Questionnaires , Risk Factors , Sulfonamides/adverse effects , Sulfones/adverse effects
West Indian med. j ; 61(9): 932-936, Dec. 2012. ilus
Article in English | LILACS | ID: lil-694370


The use of new antiretroviral drugs in HIV infection is particularly important in patients with intolerance or resistance to other antiretroviral agents. Raltegravir and maraviroc represent new, important resources in salvage regimens. A reduced grade of liver fibro-steatosis after a combination of raltegravir and maraviroc (second-line) has not been studied and the mechanism by which these new drug classes induced a marked reduction of grade of liver diseases is currently unknown. In the present case report, nested in an ongoing multicentre observational study on the use of new antiretroviral inhibitors in heavy treatment-experienced HIV patients, we evaluated the correlation between a "short therapeutic regimen" raltegravir, maraviroc and fosamprenavir and liver diseases. The aim of this report is to describe the use of a three-drug regimen based on two novel-class antiretroviral agents (raltegravir and maraviroc) plus the protease inhibitor fosamprenavir, in an experienced HIV-infected patient with chronic progressive hepatitis C complicated by liver fibrosis; an overwhelming increased serum creatine kinase level occurred during treatment, and is probably related to integrase inhibitor administration. At present no information is available regarding this correlation.

El uso de nuevos medicamentos antiretrovirales para la infección por VIH es particularmente importante en los pacientes con intolerancia o resistencia a otros agentes antiretrovirales. Raltegravir (RTV) y maraviroc (MRV) representan nuevos e importantes recursos en las terapias de salvamento. Un grado reducido de fibroesteatosis hepática después de una combinación de raltegravir y maraviroc (terapia de segunda línea) no ha sido estudiado, y el mecanismo por el cual estas nuevas clases de droga indujeron una marcada reducción de grado de las enfermedades hepáticas se desconoce hasta el momento. Como parte de la realización en curso de un estudio observacional multicentro acerca del uso de nuevos inhibidores antiretrovirales en pacientes de VIH altamente experimentados en el tratamiento, en el presente reporte de caso se evalúa la correlación entre un "régimen terapéutico corto" (raltegravir, maraviroc y fosamprenavir) y las enfermedades del hígado. El objetivo de este reporte es describir el uso de un régimen de tres medicamentos - basado en dos agentes antiretrovirales de nuevo tipo (raltegravir y maraviroc) además del fosamprenavir inhibidor de la proteasa - en un paciente de VIH experimentado. El paciente también sufre de hepatitis C evolutiva, progresiva, crónica, complicada por fibrosis hepática. Durante el tratamiento, se produjo un aumento extraordinario del nivel de creatina quinasa sérica, el cual probablemente esta relacionado con la administración del inhibidor de la integrasa. Actualmente no hay información disponible con respecto a esta correlación.

Adult , Humans , Male , Carbamates/adverse effects , Cardiomyopathies/drug therapy , Creatine Kinase/blood , Cyclohexanes/adverse effects , Chemical and Drug Induced Liver Injury/diagnosis , Fatty Liver/chemically induced , HIV Fusion Inhibitors/adverse effects , HIV Infections/drug therapy , HIV Integrase Inhibitors/adverse effects , HIV Protease Inhibitors/adverse effects , Hepatitis C, Chronic/drug therapy , Liver Cirrhosis/chemically induced , Organophosphates/adverse effects , Pyrrolidinones/adverse effects , Sulfonamides/adverse effects , Triazoles/adverse effects , Carbamates/therapeutic use , Cyclohexanes/therapeutic use , Drug Substitution , Drug Therapy, Combination , Fatty Liver/diagnosis , HIV Fusion Inhibitors/therapeutic use , HIV Integrase Inhibitors/therapeutic use , HIV Protease Inhibitors/therapeutic use , Liver Cirrhosis/diagnosis , Organophosphates/therapeutic use , Pyrrolidinones/therapeutic use , Sulfonamides/therapeutic use , Triazoles/therapeutic use
Rev. bras. oftalmol ; 71(3): 160-163, maio-jun. 2012. graf, tab
Article in Portuguese | LILACS | ID: lil-643913


OBJETIVO: Avaliar a eficácia e conforto dos pacientes portadores de glaucoma primário de ângulo aberto (GPAA) ou hipertensão ocular (HO) em uso da combinação fixa de timolol 0,5% e brinzolamida 1%. MÉTODOS: Foram acompanhados prospectivamente 26 pacientes portadores de GPAA ou HO, num total de 50 olhos que foram instituídos a utilizarem a combinação fixa de timolol 0,5% e brinzolamida 1%. As avaliações foram feitas por um único examinador por tonometria de aplanação (Goldman) em 7 e 30 dias. Os possíveis efeitos colaterais e intolerância foram descritos pelos próprios pacientes através da pergunta: "Você sentiu alguma alteração ao pingar a medicação prescrita?" Os dados foram coletados e analisados estatisticamente. RESULTADOS: Os valores de pressão intraocular (PIO) foram significativamente menores nas avaliações de 7 e 30 dias (p<0,001). A média da redução da PIO foi de 38%, variando de uma média inicial de 23,8 mmHg para 14,6 e 14,4 mmHg nos dias 7 e 30, respectivamente. Dos 26 pacientes incluídos apenas 4 relataram alguma queixa ao pingar o colírio, sendo que as queixas variaram de ardência, leve queimação e embaçamento. CONCLUSÃO: A combinação fixa de timolol 0,5% e brinzolamida 1% mostrou-se eficaz no tratamento de pacientes com GPAA e HO com eficácia semelhante a da literatura e apresentou um baixo índice de efeitos desconfortáveis relatados pelos usuários da medicação.

OBJETICVE: To evaluate the efficacy and side effects of timolol 0,5% and brinzolamide 1% fixed combination in patients with primary open angle glaucoma (POAG) and ocular hypertension (OH). METHODS: 50 eyes of 26 patients with POAG or OH were evaluated with topical therapy with fixed combination of timolol 0.5% and brinzolamide 1%.The measurements with Goldmann tonometry were applied by only one ophthalmologist after 7 and 30 days on medication. The side effects were described by the patient based on the following question: "Did you feel any alteration with the prescribed drops?" The data were collected and analized statistically. RESULTS: The intraocular pressure (IOP) was lower in 7 and 30 days (p<0.001).The mean reduction in IOP was 38% with a variation from 23,8 mmhg to 14.6 and 14.4 mmhg in 7 and 30 days. Four patients had side effects: burning and blurring vision were related. CONCLUSION: the fixed combination of timolol 0.5% and brinzolamide 1% had good results with lower IOP in the treatment of patients with POAG and OH just like in the literature and had few side effects.

Humans , Middle Aged , Aged , Aged, 80 and over , Sulfonamides/therapeutic use , Thiazines/therapeutic use , Timolol/therapeutic use , Glaucoma, Open-Angle/drug therapy , Ocular Hypertension/drug therapy , Antihypertensive Agents/therapeutic use , Ophthalmic Solutions , Sulfonamides/adverse effects , Sulfonamides/pharmacology , Thiazines/adverse effects , Thiazines/pharmacology , Timolol/adverse effects , Timolol/pharmacology , Instillation, Drug , Prospective Studies , Drug Combinations , Intraocular Pressure/drug effects , Antihypertensive Agents/adverse effects , Antihypertensive Agents/pharmacology
Article in English | WPRIM | ID: wpr-25811


This paper presents a case of reversible dysphasia occurring in a patient prescribed atorvastatin in combination with indapamide. A milder dysphasia recurred with the prescription of rosuvastatin and was documented on clinical examination. This resolved following cessation of rosuvastatin. The case highlights both a need for a wider understanding of potential drug interactions through the CYP 450 system and for an increased awareness, questioning and reporting of drug side-effects.

Anticholesteremic Agents/adverse effects , Antihypertensive Agents/therapeutic use , Anxiety/diagnosis , Aphasia/diagnosis , Cytochrome P-450 Enzyme System/metabolism , Depression/diagnosis , Drug Interactions , Female , Fluorobenzenes/adverse effects , Heptanoic Acids/adverse effects , Humans , Hypercholesterolemia/drug therapy , Indapamide/therapeutic use , Middle Aged , Pyrimidines/adverse effects , Pyrroles/adverse effects , Sulfonamides/adverse effects
Article in English | WPRIM | ID: wpr-171214


We report a case of anterior ischemic optic neuropathy associated with udenafil. A 54-year-old male presented with an acute onset visual field defect of the right eye after udenafil use. Examination revealed a relative afferent pupillary defect and a swollen disc. Automated visual fields revealed an enlarged blind spot and a narrowed visual field. Fluorescein angiography revealed both an inferior choroidal filling delay and an inferior sector filling delay of the optic disc in the arteriovenous phase as well as diffuse leakage of the optic disc in the late phase. Optical coherent tomography revealed increased thickness of the retinal nerve fiber layer, especially in the area of the inferior disc. The patient was counseled to discontinue the use of udenafil and to monitor his blood pressure regularly. The disc swelling was resolved with residual optic atrophy one month after discontinuing the use of udenafil.

Acute Disease , Choroid/pathology , Humans , Male , Middle Aged , Optic Neuropathy, Ischemic/chemically induced , Phosphodiesterase 5 Inhibitors/adverse effects , Pyrimidines/adverse effects , Sulfonamides/adverse effects , Tomography, Optical Coherence , Visual Fields
Int. braz. j. urol ; 37(4): 566-576, July-Aug. 2011. ilus, tab
Article in English | LILACS | ID: lil-600811


AIMS: Tamsulosin, a superselective subtype alpha 1a and 1d blocker, is used for the treatment of male lower urinary tract symptoms (LUTS) commonly caused by benign prostatic hyperplasia (BPH). This prospective study evaluated the efficacy and safety of a new formulation, Tamsulosin OCAS® (Oral Controlled Absorption System), for LUTS associated with BPH in Thai patients. MATERIALS AND METHODS: Fifty one patients over 40 years old with complaints of LUTS associated with BPH were recruited. Patients received an 8 week course of once daily 0.4 mg tamsulosin OCAS®, and were followed up at 2 (visit 3), 4 (visit 4) and 8 (visit 5) weeks post-treatment. At each visit, patients were assessed using the International Prostate Symptom Score (IPSS), Nocturia Quality of Life (N-QoL) Questionnaire, QoL Assessment Index (IPSS-QoL), and International Index of Erectile Function (IIEF). The primary outcome was efficacy of Tamsulosin. The secondary outcomes included change in the mean number of nocturia episodes, hours of undisturbed sleep (HUS) and uroflowmetry measurements. RESULTS: Total IPSS significantly decreased at week 8 from baseline (from 19.52 to 6.08; p < 0.001). Similarly, the voiding and storage subscores of IPSS also continued to improve significantly starting from the second and third visits, respectively (p < 0.001 versus baseline). The IPSS-QoL and N-QoL scores significantly improved at visit 3 through end of study. In addition, we observed significant nocturia and HUS improvement in their last clinic visit. Uroflowmetry parameters, Qmax and Qave, improved significantly at 3rd clinic visit . Three patients experienced mild dizziness. CONCLUSION: Tamsulosin OCAS® treatment led to significant improvements in LUTS, HUS and QoL in Thai patients with bladder outlet obstruction from BPH with few side effects.

Aged , Aged, 80 and over , Humans , Male , Middle Aged , Adrenergic alpha-1 Receptor Antagonists/therapeutic use , Lower Urinary Tract Symptoms/drug therapy , Prostatic Hyperplasia/complications , Sulfonamides/therapeutic use , Urinary Bladder Neck Obstruction/complications , Administration, Oral , Analysis of Variance , Adrenergic alpha-1 Receptor Antagonists/adverse effects , Follow-Up Studies , Lower Urinary Tract Symptoms/etiology , Quality of Life , Sulfonamides/adverse effects , Time Factors , Treatment Outcome
Indian J Ophthalmol ; 2010 May; 58(3): 248-252
Article in English | IMSEAR | ID: sea-136068


The sulphonamide group of drugs is implicated in bilateral acute angle closure (AAC) due to an idiosyncratic response. We report a series of three cases with bilateral AAC caused by different sulphonamide derivatives, their presentation and management.

Acute Disease , Adult , Female , Glaucoma, Angle-Closure/chemically induced , Humans , Hypoglycemic Agents/adverse effects , Male , Middle Aged , Sulfonamides/adverse effects
West Indian med. j ; 59(1): 102-105, Jan. 2010. ilus, tab
Article in English | LILACS | ID: lil-672576


Antibiotic and non-antibiotic sulphonamides are often prescribed. Although chemical differences make cross-reactivity rare, reactions may be severe in patients allergic to sulphur. Adverse reactions are common with sulphonamides but low platelets and skin changes are rarely associated with eye-drops for glaucoma. A woman treated with dorzolamide and timolol presented with disseminated eruption. On admission, her physical examination was unremarkable except for the skin changes and severe thrombocytopaenia was detected. Skin biopsy showed hyperkeratosis, acanthosis, perivascular and periadnexal infiltrates with no vasculitis. After discontinuation of eye-drops, the eruption improved but low platelets persisted. Skin changes reappeared with use of dapsone which suggested sulphonamide cross-reactivity.

A menudo se prescriben sulfonamidas antibióticas y no-antibióticas. Aunque las diferencias químicas hacen que la reactividad cruzada sea algo raro, las reacciones pueden ser severas en los pacientes alérgicos al azufre. Las reacciones adversas son comunes con las sulfonamidas pero las plaquetas bajas y los cambios en la piel raramente se asocian con las gotas oculares para el glaucoma. A una mujer a quien se le hizo un tratamiento con dorzolamida y timolol, se le presentó una erupción diseminada. En el momento del ingreso, su examen físico fue común y corriente excepto por los cambios en la piel. Además se le detectó una trombocitopenia severa. La biopsia de la piel reveló hiperqueratosis, acanthosis, infiltrados perivasculares y periadnexales sin vasculitis. Tras descontinuar las gotas oculares, la erupción mejoró pero las plaquetas bajas persistieron. Los cambios de la piel reaparecieron con el uso de dapsona, lo que hizo pensar en una reactividad cruzada de la sulfonamida.

Female , Humans , Middle Aged , Anti-Infective Agents/adverse effects , Antihypertensive Agents/adverse effects , Drug Eruptions , Dapsone/adverse effects , Glaucoma/drug therapy , Ophthalmic Solutions/adverse effects , Sulfonamides/adverse effects , Thiophenes/adverse effects , Thrombocytopenia/chemically induced , Timolol/adverse effects , Anti-Infective Agents/administration & dosage , Antihypertensive Agents/administration & dosage , Biopsy , Dapsone/administration & dosage , Liver Function Tests , Platelet Count , Sulfonamides/administration & dosage , Thiophenes/administration & dosage , Timolol/administration & dosage
Clinics ; 65(10): 1009-1011, 2010. tab
Article in English | LILACS | ID: lil-565985


BACKGROUND: Drug hypersensitivity is responsible for substantial mortality and morbidity, and increased health costs. However, epidemiological data on drug hypersensitivity in general or specific populations are scarce. METHODS: We performed a cross-sectional survey of 1015 university students, using a self-reported questionnaire. RESULTS: The prevalence of self-reported drug hypersensitivity was 12,11 percent (123/1015). The most frequently implicated drugs were non-steroidal anti-inflammatory drugs (45,9 percent) and beta-lactam and sulfonamide antibiotics (25,40 percent). The majority of the patients reported dermatological manifestations (99), followed by respiratory (40), digestive (23) and other (19). Forty-five patients had an immediate type reaction, and 76,72 percent (89) had the drug by oral route. CONCLUSION: The results showed that drug hypersensitivity is highly prevalent in university students, and that nonsteroidal anti-inflammatory drug and antibiotics (beta-lactams and sulfonamide) are the most frequently concerned drugs.

Adolescent , Adult , Female , Humans , Male , Middle Aged , Young Adult , Drug Hypersensitivity/epidemiology , Students/statistics & numerical data , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Brazil/epidemiology , Cross-Sectional Studies , Drug Hypersensitivity/classification , Prevalence , Sulfonamides/adverse effects , beta-Lactams/adverse effects
Article in English | WPRIM | ID: wpr-64132


We evaluated the therapeutic effects of tamsulosin for women with non-neurogenic voiding dysfunction. Women who had voiding dysfunctions for at least 3 months were included. Inclusion criteria were age > or =18 yr, International Prostate Symptom Score (IPSS) of > or =15, and maximum flow rate (Q(max)) of > or =12 mL/sec and/or postvoid residuals (PVR) of > or =150 mL. Patients with neurogenic voiding dysfunction or anatomical bladder outlet obstruction were excluded. All patients were classified according to the Blaivas-Groutz nomogram as having no or mild obstruction (group A) or moderate or severe obstruction (group B). After 8 weeks of treatment, treatment outcomes and adverse effects were evaluated. One hundred and six patients were evaluable (70 in group A, 36 in group B). After treatments, mean IPSS, bother scores, Q(max), PVR, diurnal and nocturnal micturition frequencies and scored form of the Bristol Female Lower Urinary Tract Symptoms questionnaire (BFLUTS-SF) were changed significantly. Eighty-nine patients (84%) reported that the treatment was beneficial. The proportion of patients reported that their bladder symptoms caused "moderate to many severe problems" were significantly decreased. No significant difference were observed between the groups in terms of IPSS, bother score, Q(max), PVR, micturition frequency, and BFLUTS-SF changes. Adverse effects related to medication were dizziness (n=3), de novo stress urinary incontinence (SUI) (n=3), aggravation of underlying SUI (n=1), fatigue (n=1). Tamsulosin was found to be effective in female patients with voiding dysfunction regardless of obstruction grade.

Adrenergic alpha-Antagonists/adverse effects , Adult , Aged , Aged, 80 and over , Female , Humans , Middle Aged , Surveys and Questionnaires , Severity of Illness Index , Sulfonamides/adverse effects , Treatment Outcome , Urination Disorders/drug therapy