Reacciones adversas causadas por quimioprofilaxis con doxiciclina / Adverse reactions caused by chemoprophylaxis with doxicicline

Se realizó un estudio descriptivo y prospectivo de 86 trabajadores del Puerto Guillermón Moncada de Santiago de Cuba, quienes recibieron tratamiento quimioprofiláctico con doxiciclina y presentaron reacciones adversas asociadas a dicho tratamiento, en noviembre del 2015, con vistas a caracterizarles y determinar la relación de causalidad existente entre la administración del medicamento, la aparición de efectos indeseables y las posibles interacciones farmacológicas. En esta serie, las reacciones adversas resultaron leves y no graves; las relaciones de causalidad, definitivas en la mayoría de los afectados (65,1 por ciento), aunque se determinaron algunas como probables y posibles, en tanto, las reacciones más frecuentes se presentaron en la esfera gastrointestinal

A descriptive and prospective study of 86 workers from Guillermón Moncada Port was carried out in Santiago de Cuba. They received chemoprophylactic treatment with doxicicline and presented adverse reactions associated with this treatment, in November, 2015, aimed at characterizing them and determining the relationship of causation existing between the administration of medication, emergence of undesirable effects and possible pharmacological interactions. In this series, the adverse reactions were light and no severe; the causation relationships, were definitive in most of the affected patients (65.1 percent), although some were determined as probable and possible, while, the most frequent reactions were presented in the gastrointestinal sphere

Enantioselective metabolism of hydroxychloroquine employing rats and mice hepatic microsomes / Metabolismo enantiosseletiva da hidroxicloroquina empregando microssomas hepáticos de ratos e camundongos

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.