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2.
Rev. bras. ginecol. obstet ; 42(11): 705-711, Nov. 2020. tab
Article in English | LILACS | ID: biblio-1144171

ABSTRACT

Abstract Objective: To determine pregnancy outcomes in women with systemic lupus erythematosus (SLE) who were treated with hydroxychloroquine in a tertiary center. Methods: A retrospective study involving pregnant women with SLE who had antenatal follow-up and delivery in between 1 January 2007 and 1 January 2017. All participants were retrospectively enrolled and categorized into two groups based on hydroxychloroquine treatment during pregnancy. Results: There were 82 pregnancies included with 47 (57.3%) in the hydroxychloroquine group and 35 (42.7%) in the non-hydroxychloroquine group. Amongst hydroxychloroquine users, there were significantly more pregnancies with musculoskeletal involvement (p = 0.03), heavier mean neonatal birthweight (p = 0.02), and prolonged duration of pregnancy (p = 0.001). In non-hydroxychloroquine patients, there were significantly more recurrent miscarriages (p = 0.003), incidence of hypertension (p = 0.01) and gestational diabetes mellitus (p = 0.01) and concurrent medical illness (p = 0.005). Hydroxychloroquine use during pregnancy was protective against hypertension (p = 0.001), and the gestational age at delivery had significant effect on the neonatal birthweight (p = 0.001). However, duration of the disease had a significant negative effect on the neonatal birthweight (p = 0.016). Conclusion: Hydroxychloroquine enhanced better neonatal outcomes and reduced adverse pregnancy outcomes and antenatal complications such as hypertension and diabetes.


Subject(s)
Humans , Female , Pregnancy , Adult , Pregnancy Complications/drug therapy , Prenatal Care , Hydroxychloroquine/therapeutic use , Lupus Erythematosus, Systemic/drug therapy , Pregnancy Outcome , Retrospective Studies , Cohort Studies , Treatment Outcome , Tertiary Care Centers , Hydroxychloroquine/administration & dosage , Malaysia
3.
Rev. peru. med. exp. salud publica ; 37(2): 302-311, abr.-jun. 2020. graf
Article in Spanish | LILACS | ID: biblio-1127147

ABSTRACT

RESUMEN Durante las primeras semanas de 2020 se comenzaron a informar casos de personas con SARS-CoV-2 fuera de China, con un rápido aumento de casos y muertes en todo el mundo. El SARS-CoV-2 es un virus ARN monocatenario positivo, envuelto en una bicapa lipídica derivada de la membrana celular del huésped y constituido por cuatro proteínas estructurales (S, M, E y N), además de una hemaglutinina-esterasa. La unión de la proteína S con el receptor de enzima convertidora de angiotensina 2 (ECA2) permite la entrada del virus a la célula huésped y es una potencial diana terapéutica. El 81% de los enfermos hace cuadro leve; el 14%, grave; y el 5% requiere cuidados intensivos. La fiebre es el síntoma más frecuente, seguido de tos y disnea. La mayoría de los pacientes no presentan leucocitosis pero sí linfopenia, con cultivos de esputo que no muestran otros patógenos. En las biopsias de pulmón de pacientes graves el hallazgo más llamativo es el daño alveolar difuso. Radiológicamente se aprecian patrones de vidrio esmerilado y alveolar, siendo las lesiones de predominio basal, subpleural y posterior, con una distribución periférica multifocal, afectando más el lóbulo inferior derecho. Hay una marcada respuesta inflamatoria, que llega hasta la tormenta de citoquinas, en la que el tratamiento antiinflamatorio con terapia de pulso con metilprednisolona estaría indicado. Aunque no existan estudios en gran escala respecto al uso de cloroquina/hidroxicloroquina, debido a la situación mundial se ha autorizado su uso por su efecto anti SARS-CoV-2 y anti-inflamatorio, el cual puede ser potenciado con el uso de azitromicina.


ABSTRACT During the first weeks of 2020, cases of SARS-CoV-2 began to be reported outside of China, with a rapid increase in cases and deaths worldwide. SARS-CoV-2 is a positive single-stranded RNA virus, encased in a lipid bilayer derived from the host cell membrane and consists of four structural proteins (S, M, E and N), plus a haemagglutinin-sterase. The binding of the S protein to the ECA2 receptor allows the entry of the virus into the host cell and is a potential therapeutic target. 81% of patients develop mild symptoms, 14% have severe symptoms and 5% require intensive care management. Fever is the most frequent symptom, followed by cough and dyspnea. Most patients do not present leukocytosis, but they do present lymphopenia with sputum cultures that do not show other pathogens. In lung biopsies of severe patients, the most noticeable finding is diffuse alveolar damage. Radiologically, ground glass and alveolar patterns are observed; the lesions being predominantly basal, subpleural, and posterior, with a multifocal peripheral distribution, more affecting the right lower lobe. There is a marked inflammatory response, up to the cytokine storm, in which anti-inflammatory treatment with pulse therapy with methylprednisolone would be indicated. Although there are no large-scale studies regarding the use of chloroquine / hydroxychloroquine, due to the global situation, its use has been authorized for its anti-SARS-CoV-2 and anti-inflammatory effect, which can be potentiated with the use of azithromycin.


Subject(s)
Humans , Pneumonia, Viral/epidemiology , Coronavirus Infections/epidemiology , Inflammation/virology , Antiviral Agents/administration & dosage , Pneumonia, Viral/physiopathology , Pneumonia, Viral/drug therapy , Chloroquine/administration & dosage , Coronavirus Infections/physiopathology , Coronavirus Infections/drug therapy , Pandemics , COVID-19 , Hydroxychloroquine/administration & dosage , Inflammation/drug therapy , Anti-Inflammatory Agents/administration & dosage
4.
An. bras. dermatol ; 95(3): 340-342, May-June 2020. graf
Article in English | LILACS, ColecionaSUS | ID: biblio-1130888

ABSTRACT

Abstract Sarcoidosis is a multisystem granulomatous disorder of unknown aetiology. Cutaneous involvement occurs in up to 30% of patients and skin findings are often the initial presenting symptom. The facial atrophic form of sarcoidosis without associated ulceration in adolescents has rarely been described in the literature. We report a case of 13-year-old male patient with a facial atrophic sarcoidosis who was successfully treated with the combination of prednisone and hydroxychloroquine.


Subject(s)
Humans , Male , Adolescent , Sarcoidosis/drug therapy , Prednisone/administration & dosage , Facial Dermatoses/drug therapy , Hydroxychloroquine/administration & dosage , Anti-Inflammatory Agents/administration & dosage , Sarcoidosis/pathology , Biopsy , Treatment Outcome , Drug Therapy, Combination , Facial Dermatoses/pathology , Granuloma/pathology , Granuloma/drug therapy
7.
Brasilia; s.n; 16 abr. , 2020. 17 p.
Non-conventional in Portuguese | BRISA, LILACS, PIE | ID: biblio-1095205

ABSTRACT

Autores descrevem evidências do efeito benéfico da coadministração de hidroxicloroquina com azitromicina no tratamento de COVID-19 e sua potencial eficácia na redução precoce da contagiosidade. Trata-se de uma coorte com 80 pacientes infectados (sintomas moderados), internados e tratados com hidroxicloroquina (200 mg 3x/dia ­ total de 600 mg ­ durante 10 dias) + azitromicina (500 mg no 1º dia, seguido de 250 mg/dia por mais 4 dias). Um total de 80 pacientes recebeu tratamento diariamente durante dez dias. Os três desfechos principais do estudo foram: evolução clínica, contagiosidade (avaliada por PCR e cultura) e tempo de permanência na Unidade de Doenças Infecciosas (UDI). Resultados: Evolução clínica: A maioria (65/80, 81,3%) dos pacientes apresentou resultado favorável e recebeu alta. Apenas 15% necessitaram de oxigenoterapia durante a permanência na UDI. Um paciente de 86 anos morreu e outro de 74 anos se encontrava em terapia intensiva no momento da redação do artigo. Contagiosidade: Observou-se uma queda rápida da carga viral nasofaríngea, com 83% de negativos no 7º dia e 93% no 8º dia. As culturas de vírus das amostras respiratórias dos pacientes foram negativas em 97,5% dos pacientes no 5º dia. Tempo de permanência na UDI: dos 65 pacientes que receberam alta da UDI, o tempo médio de permanência foi de cinco dias.1


Subject(s)
Humans , Pneumonia, Viral/drug therapy , Communicable Diseases/drug therapy , Coronavirus Infections/drug therapy , Azithromycin/administration & dosage , Azithromycin/therapeutic use , Betacoronavirus/drug effects , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/therapeutic use , Disease Progression , Therapies, Investigational/instrumentation
8.
Brasilia; s.n; 15 abr. , 2020. 23 p.
Non-conventional in Portuguese | LILACS, BRISA, PIE | ID: biblio-1095207

ABSTRACT

Estudo multicêntrico, paralelo, randomizado, open-label, com 150 pacientes adultos com COVID-19. Dessa forma, 75 pacientes receberam hidroxicloroquina com tratamento padrão e outros 75 receberam somente o tratamento padrão. O desfecho primário foi a conversão negativa de SARS-CoV-2 em 28 dias. No geral, a taxa de conversão negativa de SARS-CoV-2 entre os pacientes designados para receber tratamento padrão mais HCQ foi de 85,4% (IC 95%: 73,8% ­ 93,8%), semelhante à do grupo tratamento padrão 81,3% (IC 95%: 71,2% ­ 89,6%) em 28 dias. O tempo de conversão negativo não diferiu entre o grupo tratamento padrão mais HCQ e o grupo tratamento padrão (mediana 8 dias vs. 7 dias; HR = 0,846; IC95%: 0,580 ­ 1,234; P = 0,341). A taxa de alívio dos sintomas e o tempo para alívio dos sintomas foram similares entre os grupos. Os autores relataram que "a eficácia da HCQ no alívio dos sintomas (RR = 8,83, IC 95%: 1,09 ­ 71,3) ficou mais evidente quando os efeitos de confusão de outros agentes antivirais foram removidos na análise posterior". No entanto, não foi observada diferença significativa na melhora dos sintomas em outras análises de subgrupos. No total, 21 pacientes (30%) que receberam HCQ relataram eventos adversos, proporção significativamente (P = 0,001) maior do que aqueles (7 pacientes, 8,8%) relatados no grupo tratamento padrão.1


Subject(s)
Humans , Adult , Pneumonia, Viral/drug therapy , Coronavirus Infections/drug therapy , Betacoronavirus/drug effects , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/therapeutic use , Technology Assessment, Biomedical , Disease Progression , Therapies, Investigational/instrumentation
10.
Evid. actual. práct. ambul ; 23(2): e002057, 2020.
Article in Spanish | LILACS | ID: biblio-1103663

ABSTRACT

La pandemia de COVID-19 está generando información epidemiológica y clínica en una escala sin precedentes para una enfermedad de reciente aparición. Aunque ya se han iniciado numerosos ensayos clínicos de fármacos antiguos y nuevos como potenciales antivirales específicos, la mayor parte de la información publicada hasta ahora carece de los controles básicos para la evaluación de la eficacia de un medicamento. Los medios de comunicación amplifican estos resultados preliminares y suman presión a los médicos asistenciales y a los decisores de políticas públicas. Este artículo revisa las pruebas disponibles sobre los cuatro tratamientos antivirales específicos más prometedores: hidroxicloroquina, lopinavir/ritonavir, remdesvir e interferones alfa y beta. Se comprueba en todos ellos que no hay demostración suficiente de eficacia como para recomendar su uso fuera de una investigación experimental adecuadamente controlada. En el uso individual de un medicamento no hay forma de saber si está beneficiando o perjudicando al paciente. Es erróneo asumir que la eventual curación se debe al fármaco y un mal desenlace debe atribuirse a la enfermedad. Sólo la comparación entre grupos de pacientes asignados al tratamiento experimental o a un control adecuado permite conocer la eficacia y seguridad de las intervenciones. El desafío es conciliar la urgencia de actuar con la generación de nuevos conocimientos.Aunque no resulta sencillo organizar ensayos clínicos en este contexto, las instituciones pueden sumarse a los proyectos en marcha a nivel nacional e internacional. El uso de estos fármacos debe considerarse experimental, por lo que es necesario obtener el consentimiento informado del paciente. (AU)


The COVID-19 pandemic is generating epidemiological and clinical information on an unprecedented scale for a newly emerging disease. Although numerous clinical trials of old and new drugs as potential specific antivirals have already been started, most of the information published so far lacks basic controls for evaluating drug efficacy. The media amplify these preliminary results and add pressure to doctors and policymakers. This article reviews the available evidence for the four most promising specific antiviral treatments: hydroxychloroquine, lopinavir / ritonavir, remdesvir, and alpha and beta interferons. The findings show that none of them has sufficient demonstration of efficacy to recommend its use outside ofthe adequately controlled experimental study. In the individual use of a drug there is no way of knowing if it is benefiting orharming the patient. It is wrong to assume that the eventual cure is due to the drug and a poor outcome must be attributed to the disease. Only the comparison between groups of patients assigned to the experimental treatment or to an adequate control can establish the efficacy and safety of the interventions. The challenge is to reconcile the urgency to act with the generation of new knowledge. Although it is not easy to organize clinical trials in this context, the institutions can join theongoing projects at the national and international levels. The use of these drugs should be considered experimental, so it is necessary to obtain the informed consent of the patient. (AU)


Subject(s)
Humans , Antiviral Agents/pharmacology , Pneumonia, Viral/drug therapy , Interferons/pharmacology , Coronavirus Infections/drug therapy , Ritonavir/pharmacology , Lopinavir/pharmacology , Hydroxychloroquine/pharmacology , Antiviral Agents/adverse effects , Treatment Outcome , Azithromycin/pharmacology , Risk Assessment , Ritonavir/administration & dosage , Ritonavir/adverse effects , Evidence-Based Medicine/trends , Information Dissemination , Off-Label Use , Health Communication , Pandemics , Lopinavir/administration & dosage , Lopinavir/adverse effects , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/adverse effects , Informed Consent
12.
J. bras. nefrol ; 42(2,supl.1): 49-50, 2020.
Article in English | LILACS | ID: biblio-1134830

ABSTRACT

ABSTRACT Chloroquine and hydroxychloroquine have shown promising preliminary results and have been discussed as therapeutic options for patients with Covid-19. Despite the lack of robust evidence demonstrating the benefits and justifying the use of one of these drugs, the final decision is the responsibility of the attending physician and should be individualized and shared, whenever possible. This position statement recommends dosage adjustment for these drugs in the context of renal impairment.


RESUMO Em razão de resultados preliminares promissores, a hidroxicloroquina e a cloroquina têm sido discutidas como opção terapêutica para pacientes com Covid-19. Apesar da ausência de estudos robustos que evidenciem o benefício e justifiquem o uso de uma dessas drogas, a decisão final compete ao médico assistente, devendo ser individualizada e, sempre que possível, compartilhada. A presente nota pretende orientar o ajuste posológico dessas drogas no contexto da disfunção renal.


Subject(s)
Humans , Pneumonia, Viral/drug therapy , Chloroquine/administration & dosage , Coronavirus Infections/drug therapy , Renal Insufficiency , Hydroxychloroquine/administration & dosage , Antimalarials/administration & dosage , Societies, Medical , Brazil , Pandemics , COVID-19 , Nephrology
13.
Rev. ciênc. farm. básica apl ; 40: [3], 01/01/2019.
Article in English | LILACS | ID: biblio-1100191

ABSTRACT

The use of chloroquine and hydroxychloroquine as off-label treatments for covid-19 disease is a resort for critical care patients under enteral nutrition (EN). However, the use of solid pharmaceutical forms of these drugs through feeding tubes can pose a challenge to the health care team. Therefore, we performed a review of literature regarding administration of chloroquine and hydroxychloroquine through feeding tubes. For this end, a search was performed on PubMed and Lilacs database using key-words and free terms referring to drug administration via feeding tubes, and, specifically chloroquine and hydroxychloroquine. Also, a search on Micromedex® database and on the Handbook of Drug Administration via Enteral Feeding Tubes were performed. A total of 1.784 articles were retrieved. However, 4 articles fitted in the inclusion criteria. Two articles exploring the administration of chloroquine via feeding tubes on children with malaria found no difference on clinical results or tolerability when comparing it with oral or intramuscular administration. Other article showed full dispersion of hydroxychloroquine on water after crushing with mortar and pestle. A review found no information regarding the administration of hydroxychloroquine via postpyloric feeding tubes. No information was found on Micromedex® or the consulted Handbook; however, they pointed out the interaction between chloroquine and multivalent ions if coadministered.(AU)


Subject(s)
Humans , Chloroquine/administration & dosage , Enteral Nutrition/instrumentation , Coronavirus , Hydroxychloroquine/administration & dosage , Coronavirus Infections/therapy
15.
Med. interna (Caracas) ; 34(1): 36-42, 2018. tab
Article in Spanish | LILACS, LIVECS | ID: biblio-1008252

ABSTRACT

: relacionar el uso de hidroxicloroquina con la presencia de retinopatía en pacientes reumatológicos. Métodos: se realizó un estudio retrospectivo y descriptivo, de revisión de historias clínicas de pacientes reumatológicos en tratamiento con hidroxicloroquina. Se seleccionaron aquellos con evaluación oftalmológica previa al inicio del tratamiento y estudios como la OCT-SD. Se recolectaron variables clínico epidemiológicas, cálculo de dosis diaria y acumulada del fármaco, y duración del tratamiento. Resultados: se revisaron 150 historias, de las cuales 47 cumplieron con los criterios de inclusión; 44 (93,6%) eran del género femenino y 3 (6,4%) del género masculino. La edad promedio fue de 47 ± 14 años. La hipertensión arterial fue la comorbilidad más frecuente. La patología reumatológica más frecuente fue el Lupus (53,2%). La dosis diaria de hidroxicloroquina fue ≤ 6,5 mg/kg/día en los 47 pacientes; el tiempo promedio de consumo fue de 5 años; y la dosis acumulada promedio fue de 498,5 ± 503,68 gramos. Se detectó toxicidad retiniana en 18 pacientes (38,3%), de los cuales: 17(36,2%) tuvo daño precoz y 1 (2,1%) daño moderado. Se observó relación estadística significativa entre toxicidad retiniana y dosis acumulada menores a 1.000 gramos (p= 0,032) y un tiempo de consumo mayor o igual a 5 años (p = 0,045) Conclusiones: las alteraciones iniciales en las capas externas de la retina ayudan a la detección precoz de toxicidad retiniana por hidroxicloroquina, siendo la OCT-SD un método sensible y fácil de realizar en la práctica clínica(AU)


To establish the relationship between the use of hydroxychloroquine and retinopathies in rheumatologic patients. Methods: This is a retrospective, descriptive study of the medical charts of rheumatologic patients' who were receiving hydroxychloroquine. We selected patients previously seen in ophthalmologic services, and ophthalmologic coherence tomography (SD OCT) had been realized. We collected clinical and epidemiologic variables such as daily doses, accumulated doses and prescription duration. Results: we selected 47 medical charts; the female gender is 44 and three gender male. Mean age was 47 +14 years.Hypertension was the most frequent comorbidity.Lupus was the most frequent rheumatologic illness.Hydroxychloroquine daily dose was < 6.5 mg/Kg/day and treatment`s mean duration was 5 years; average accumulated dosage was 498.5 + 503.68 grs. We established retinal toxicity in 18 patients (38.3%), in which 17 (36.2%) had early damage, and 1(2.1%) had moderated damage. There was a statistical correlation between retinal toxicity and accumulated doses of less than 1.000 grs. (p: 0.032) as well as with time of use > 5 years (p:0.045) Conclusions: Early alterations of retinal superficial layers help in the detection of early retinal toxicity due to hydroxychloroquine use. OCTSD is a feasible and sensible study in daily medical practice(AU)


Subject(s)
Humans , Male , Female , Lupus Erythematosus, Cutaneous/drug therapy , Rheumatic Diseases/drug therapy , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/adverse effects , Hypertension/physiopathology , Hypertensive Retinopathy , Internal Medicine
16.
Rev. chil. pediatr ; 86(1): 47-51, feb. 2015. ilus, graf
Article in Spanish | LILACS | ID: lil-745610

ABSTRACT

Introducción: El síndrome de Sjögren (SS) es una enfermedad crónica, autoinmune, que afecta principalmente a las glándulas exocrinas lagrimales y salivales. En niños es una enfermedad rara. Objetivo: Presentar el caso de un adolescente con síntomas inespecíficos, en que la sospecha clínica hizo llegar al diagnóstico de SS. Caso Clínico: Paciente de 12 años, de sexo masculino, con historia de artralgias de 3 años de evolución y xeroftalmia dudosa. El examen físico mostró leve congestión conjuntival, boca seca e hiperlaxitud de rodillas. Pruebas de laboratorio: hemograma y VHS normales, anticuerpos antinucleares (+) > 60, Ro (+) > 60 U, factor reumatoideo (+) 160 UI/ml. Se sospechó SS y se completó el estudio: test de Shirmer, que determinó ojo seco leve; gammagrafía de las glándulas salivales, que mostró disfunción de las glándulas submaxilares y parotídeas; biopsia de glándulas salivales, que mostró focos de infiltrado linfoide acinar y periductal. Se confirmó SS y se inició tratamiento con prednisona 7,5 mg/día e hidroxicloroquina 200 mg/día y tratamientos locales, con buena respuesta. Conclusiones: Los criterios diagnósticos del SS en adultos identifican solo al 39% de los pacientes pediátricos por la baja frecuencia de síntomas de sicca. Aún no existen criterios diagnósticos validados para niños. Un buen diagnóstico permitirá aliviar los síntomas, evitar complicaciones y detectar enfermedades asociadas.


Introduction: Sjögren’s syndrome (SS) is a chronic autoimmune disease that primarily affects the lacrimal and salivary exocrine glands. In children, it is a rare condition. Objective: To present the case of an adolescent with non-specific symptoms, but with a clinical suspicion of SS. Case report: A male 12-year old patient, with history of arthralgias for 3 years and suspicion of xerophthalmia. Physical examination showed mild conjunctival congestion, dry mouth and hypermobility of the knees. Laboratory work: blood count and ESR were normal, antinuclear antibodies (+) > 60, Ro (+) > 60 U, and rheumatoid factor concentration (+) 160 IU/ml. SS was suspected, and a study was carried out: Schirmer test determined mild dry eye, salivary gland scintigraphy showed parotid and submandibular gland dysfunction, and salivary gland biopsy reported focal lymphocytic acinar and periductal infiltration. SS was confirmed and treated with prednisone 7.5 mg/day and hydroxychloroquine 200 mg/day, and local treatment, with good response. Conclusions: The diagnostic criteria for SS in adults identified only 39% of pediatric patients, due to the low frequency of sicca symptoms. Still there are no validated diagnostic criteria for children. A good diagnosis will alleviate symptoms, prevent complications and detect associated diseases.


Subject(s)
Humans , Male , Child , Salivary Glands/pathology , Xerostomia/etiology , Sjogren's Syndrome/diagnosis , Xerophthalmia/etiology , Parotid Gland/pathology , Prednisone/administration & dosage , Prednisone/therapeutic use , Sjogren's Syndrome/drug therapy , Treatment Outcome , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/therapeutic use
17.
Rev. méd. Chile ; 141(8): 1019-1025, ago. 2013. tab
Article in Spanish | LILACS | ID: lil-698700

ABSTRACT

Background: Rheumatoid arthritis (RA) is associated with a decrease in insulin sensitivity (IS), which has been identified as an independent risk factor for the development of early atherosclerosis. Hydroxychloroquine (HCQ) may have beneficial effects on glucose homeostasis and lipid profile. Aim: To assess the effect of HCQ on IS and lipid profile in patients with RA. Material and Methods: An open clinical trial was performed in 15 patients aged between 35 and 56 years. During three months, patients received 400 mg/day of HCQ orally. Before and after the pharmacological intervention, demographic and anthropometric variables, serum glucose, total cholesterol (TC), triglycerides (TG), HDL-cholesterol, LDL-cholesterol, VLDL-cholesterol, insulin and uric acid were measured. IS was estimated as the rate of glucose clearance per minute obtained with the insulin tolerance test (KITT). Results: Baseline and final KITT values were 4.3 ± 1.2 and 4.80 ± 1.1%/min, respectively (p = 0.03). Significant reductions in serum TC (p = 0.04) and TG (p = 0.01) were also observed. No other significant differences were observed. Conclusions: Oral administration of 400 mg/day of HCQ during three months in RA patients is associated with an improvement in IS, TC and TG.


Subject(s)
Adult , Female , Humans , Middle Aged , Antirheumatic Agents/therapeutic use , Arthritis, Rheumatoid/drug therapy , Hydroxychloroquine/therapeutic use , Insulin Resistance/physiology , Lipid Metabolism/drug effects , Antirheumatic Agents/administration & dosage , Blood Glucose/analysis , Body Mass Index , Cholesterol/blood , Hydroxychloroquine/administration & dosage , Lipids/blood , Triglycerides/blood
18.
Braz. j. pharm. sci ; 45(4): 658-667, Oct.-Dec. 2009. ilus, tab
Article in English | LILACS | ID: lil-543661

ABSTRACT

Hydroxychloroquine (HCQ) is an important chiral drug used, mainly, in the treatment of rheumatoid arthritis, systemic lupus erythematosus and malaria, and whose pharmacokinetic and pharmacodynamic properties look to be stereoselective. Respecting the pharmacokinetic properties, some previous studies indicate that the stereoselectivity could express itself in the processes of metabolism, distribution and excretion and that the stereoselective metabolism looks to be a function of the studied species. So, the in vitro metabolism of HCQ was investigated using hepatic microsomes of rats and mice. The microsomal fraction of livers of Wistar rats and Balb-C mice was separated by ultracentrifugation and 500 μL were incubated for 180 minutes with 10 μL of racemic HCQ 1000 μg mL-1. Two stereospecific analytical methods, high performance liquid chromatography (HPLC) and capillary electrophoresis (CE), were used to separate and quantify the formed metabolites. It was verified that the main formed metabolite is the (-)-(R)-desethyl hydroxychloroquine for both animal species.


A hidroxicloroquina (HCQ) é um importante fármaco quiral usado, principalmente, no tratamento de artrite reumatóide, lupus eritematoso sistêmico e malária e cujas propriedades farmacocinéticas e farmacodinâmicas parecem ser estereosseletivas. Em relação às propriedades farmacocinéticas, alguns estudos prévios indicam que a estereosseletividade pode se expressar nos processos de metabolismo, distribuição e excreção e que o metabolismo estereosseletivo parece ser função da espécie estudada. Sendo assim, o metabolismo in vitro da HCQ foi investigado usando microssomas de fígado de ratos e de camundongos. A fração microssômica de fígados de ratos Wistar e de camundongos Balb-C foi isolada por ultracentrifugação e 500 μL foram incubados por 180 minutos com 10 μL de HCQ racêmica 1000 μg mL-1. Dois métodos analíticos estereoespecíficos, por cromatografia líquida de alta eficiência (HPLC) e eletroforese capilar (CE), foram usados para separar e quantificar os metabólitos formados. Verificou-se que o principal metabólito formado é o (-)-(R)-desetilidroxicloroquina para ambas as espécies de animais.


Subject(s)
Animals , Adult , Mice , Rats , Animals, Laboratory , Disease Models, Animal , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/metabolism , Microsomes, Liver , Microsomes, Liver/metabolism , Pharmacokinetics , Drug-Related Side Effects and Adverse Reactions/metabolism , Arthritis, Rheumatoid , Chromatography, High Pressure Liquid/methods , Electrophoresis, Capillary/methods , Lupus Erythematosus, Systemic/drug therapy , Malaria
19.
Indian J Dermatol Venereol Leprol ; 2008 Jan-Feb; 74(1): 18-22
Article in English | IMSEAR | ID: sea-52057

ABSTRACT

BACKGROUND: Polymorphic light eruption is the most common photodermatosis characterized by nonscarring, pruritic, erythematous papules and plaques. AIM: To evaluate the efficacy and safety of hydroxychloroquine in comparison with chloroquine in patients suffering from polymorphic light eruption. METHODS: This was a randomized, double-blind, comparative, multicentric study conducted at two centers. This study enrolled 68 (58.1%) males, 49 (41.8%) females whose ages ranged from 18-73 years and average weight was 57.89 +/- 8.27 kg. A total of 117 patients were enrolled in the study. Out of 117 patients, 63 patients were randomized to receive hydroxychloroquine tablets 200 mg twice daily for the first month and 200 mg once daily for the next month. Similarly, 54 patients were randomized to receive chloroquine tablets 250 mg twice daily for the first month and 250 mg once daily for the next month. The total duration of therapy for both the study arms was two months. The severity and frequency of burning, itching, erythema and scaling were evaluated at predetermined intervals (at baseline, after four, eight and 12 weeks of therapy). RESULTS: A significant reduction in severity scores for burning, itching and erythema was observed in patients treated with hydroxychloroquine than with chloroquine (P P = 0.229). The good to excellent response was reported by 68.9% of the patients who received hydroxychloroquine and by 63% of the patients who received chloroquine. The adverse events reported were mild to moderate and none of the patients reported any serious adverse events or ocular toxicity in this study. CONCLUSION: Hydroxychloroquine was found to be significantly more effective than chloroquine in the treatment of polymorphic light eruption and can be used safely in the dosage studied in such patients with little risk of ocular toxicity.


Subject(s)
Adolescent , Adult , Aged , Antimalarials/administration & dosage , Chloroquine/administration & dosage , Female , Humans , Hydroxychloroquine/administration & dosage , Male , Middle Aged , Photosensitivity Disorders/drug therapy , Sunlight/adverse effects , Treatment Outcome
20.
Salud(i)ciencia (Impresa) ; 15(6): 1002-1005, nov. 2007.
Article in Spanish | BINACIS, LILACS | ID: biblio-1121027

ABSTRACT

The positive effects of hydroxychloroquine in treating systemic lupus erythematosus is well known. Hydroxychloroquine is a well tolerated and safe drug even during pregnancy and breast feeding, and it has a low cost. Retinopathy is the most serious side-effect associated with its use since irreversible blindness can occur; therefore, an appropriate monitoring of the eye by an ophthalmologist becomes essential. The remarkable effectiveness of hydroxychloroquine to control disease activity has been demonstrated; and there is also evidence suggesting that this drug contributes to prevent damage accrual and to improve survival in lupus patients. Besides the immunomodulating and immunosuppressant properties of hydroxychloroquine, it also has beneficial effects on lipid and glucose metabolism as well as antithrombotic effects that could contribute to prevent arteriosclerosis in these patients


La utilidad de la hidroxicloroquina en el tratamiento del lupus eritematoso sistémico está ampliamente demostrada. Es un fármaco seguro (incluso durante el embarazo y la lactancia), bien tolerado y económico. La retinopatía asociada a su uso es el único efecto adverso realmente peligroso por cuanto puede provocar ceguera irreversible, que puede evitarse mediante un adecuado control oftalmológico. Existen suficientes datos que respaldan el notable efecto que tiene la hidroxicloroquina sobre el control de la actividad de la enfermedad. También hay hallazgos que sugieren que disminuye el daño acumulado en los pacientes lúpicos y podría aumentar su supervivencia. Las propiedades de la hidroxicloroquina parecen ir más allá de su efecto inmumodulador e inmunosupresor. Así, tiene efectos beneficiosos sobre el metabolismo lipídico y glucémico y efectos antitrombóticos que podrían contribuir a prevenir la aterosclerosis


Subject(s)
Pharmacology , Hydroxychloroquine , Hydroxychloroquine/administration & dosage , Hydroxychloroquine/pharmacology , Lupus Erythematosus, Systemic , Antimalarials
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