Avaliação do efeito da partição de comprimidos de furosemida sobre a uniformidade da dose / Influence of tablet splitting on dose uniformity

Buscando avaliar a uniformidade da dose unitária de comprimidos submetidos ao procedimento de partição, este trabalho avaliou a dureza, friabilidade, variação de peso e uniformidade de conteúdo em quatro amostras de comprimidos de furosemida de 40 mg, obtidas de diferentes fornecedores. Todas as amostras estudadas atendiam às especificações oficiais antes de serem submetidas ao procedimento de partição; porém, após serem partidas, o teor de fármaco nas metades apresentou excessiva variação, mostrando que esse procedimento pode ser terapeuticamente desaconselhável.

In order to assess the uniformity of the dose of active ingredient in the halves of tablets subjected to splitting, the hardness, friability, weight variability and uniformity of content were studied in four samples of 40 mg tablets of furosemide obtained on the Brazilian market, both whole and split into two parts. All the tablets complied with the official specifications before splitting, but, after this procedure, the drug content in the halves showed excessive variation, indicating that this procedure is inadvisable.

Evaluation of blockbuster drugs under the rule-of-five.

The current drug research techniques, combinatorial synthesis and high throughput screening, enabled the obtaining and pre-evaluation of thousands of compounds in short time. In order to chose the best hits to become leads, observation of drug-likeness tries to optimize this selection. Probably, the most widely used filter is Lipinski's Rule-of-five, which proposes that molecules with poor permeation and oral absorption have molecular weight > 500, Clog P > 5, hydrogen-bond donor > 5 and hydrogen-bond acceptor > 10. In order to evaluate the Rule-of-five, the top pharmaceutical products in 2007 were analyzed. Among 60 drugs, 7 (atorvastatin, montelukast, docetaxel, telmisartan, tacrolimus, leuprolide and olmesartan) did not fit the rule, and 5 failed only one of the threshold values. It was possible to conclude that the rule is very useful to select better compounds in chemolibraries, but it must be used carefully and with criteria, to avoid a possible exclusion of promising compounds.

Possíveis interações medicamentosas com psicotrópicos encontradas em pacientes da Zona Leste de São Paulo / Possible drug interactions with psychotropics found in patients in East São Paulo

Interação medicamentosa é o resultado de uma interferência no efeito de um medicamento por outros agentes. Dentre os fatores que resultam nas interações medicamentosas destacam-se a automedicação e a prática da polifarmácia. O objetivo deste trabalho foi realizar um levantamento de interações medicamentosas que ocorrem com fármacos que atuam no sistema nervoso central, suas possíveis consequências, bem como os motivos que propiciam tal situação. Foi realizado um estudo observacional transversal de 60 indivíduos da zona leste de São Paulo que utilizam medicamentos psicotrópicos, maiores de 21 anos e de ambos os sexos, por meio de um questionário entre junho e agosto de 2008. Os principais psicotrópicos utilizados pelos indivíduos foram benzodiazepínicos e antidepressivos (54 indivíduos), sendo que estes fármacos apresentam alto índice de interações medicamentosas. Cerca de 77% utilizam outros medicamentos em paralelo ao tratamento com psicotrópicos, sendo que destes apenas 35% o fazem com supervisão médica e 27% dos indivíduos utilizaram bebidas alcoólicas concomitantemente. As principais interações encontradas envolveram antidepressivos com benzodiazepínicos, antiulcerogênicos, anticonvulsivantes e álcool. Conclui-se que a automedicação e o uso inadequado de medicamentos são fatores que podem propiciar a ocorrência das interações medicamentosas encontradas, algumas com consequências graves.

A drug interaction is the interference in the effect of a drug by another substance. Outstanding among the factors that result in drug interactions are selfmedication and the practice of polypharmacy. The aim of this work was to conduct a survey of drug interactions that occur with drugs that act on the central nervous system, their possible consequences and the reasons for their occurrence. An observational cross-sectional study was performed on 60 subjects from East Sao Paulo who take psychotropic drugs (over 21 years old and of both genders), by means of a questionnaire applied from June to August 2008. The main drugs taken by those interviewed were benzodiazepines and antidepressants (54 subjects), which are drugs that have high rates of drug interactions. About 77% took other drugs, in parallel with the psychotropic drug treatment, of which only 35% were under medical supervision, and 27% of subjects drank alcohol while taking psychotropic drugs. The main interactions found involved antidepressants with benzodiazepines, antiulcerogenics, anticonvulsants and alcohol. We concluded that self-medication and inadequate drug usage are factors that favor the occurrence of the drug interactions found, some of them with dangerous consequences.

Theoretical evaluation of the susceptometric measurement of iron in human liver by four different susceptometers.

This paper is an evaluation of liver iron quantification using a simulated magnetic susceptibility measurement in the hepatic region. Susceptometers having homogeneous and non-homogeneous magnetizing fields coupled with axial second-order and planar first-order gradiometric magnetic detectors were considered. The intensity of magnetic flux threading the detector coils was evaluated considering samples with volume and susceptibility equivalent to liver iron, tissue and lung air individually. These volumes were represented by cylindrical and spherical geometries. The main sources of error in quantifying iron overload in susceptometric measurement of hepatic tissue were evaluated for four configurations of the susceptometer.

Reliability of serological methods for detection of leishmaniasis in Portuguese domestic and wild reservoirs

A direst agglutination test (DAT) and an immunofluorescence (IFAT) were compared for detection of Leishmania infantum infection in 43 dogs and five foxes from Alto-Douro and Arrabida, two known endemic areas in Portugal. In four dogs with proved canine leishmaniasis, both DAT and IFAT showed positive readings (titres ò1:320 and ò1:128). Of 34 samples collected form apparently healthly dogs, ten were positive by both serological tests and eight were serologically positive by one test or the other. Three foxes out of five captured in this area, scored titres indicative of leishmaniasis in both DAT and IFAT. The concordance between DAT and IFAT in all collected samples (48) was 81.25 per cent. Considering these and previous studies in the adjancent Mediterranean areas, the seroprevalence of L. infantum infection in the canine and vulpine populations appear to be high magnitude.

Reliability of serological methods for detection of leishmaniasis in Portuguese domestic and wild reservoirs.

A direct agglutination test (DAT) and an immunofluorescence technique (IFAT) were compared for detection of Leishmania infantum infection in 43 dogs and five foxes from Alto-Douro and Arrábida, two known endemic areas in Portugal. In four dogs with proved canine leishmaniasis, both DAT and IFAT showed positive readings (titres > or = 1:320 and > or = 1:128). Of 34 samples collected from apparently healthy dogs, ten were positive by both serological tests and eight were serologically positive by one test or the other. Three foxes out of five captured in this area, scored titres indicative of leishmaniasis in both DAT and IFAT. The concordance between DAT and IFAT in all collected samples (48) was 81.25%. Considering these and previous studies in the adjacent Mediterranean areas, the seroprevalence of L. infantum infection in the canine and vulpine populations appear to be of high magnitude.

Endoscopy in the upper G.I. bleedings.

From 388 patients with upper G.I. bleeding investigated by endoscopy, radiology or emergent surgery, one third bled from duodenal ulcer, one third oesophageal varices, and from the remain the most frequent were gastric ulcer (14%) and gastric cancer (9%). From a sample of 53 patients with liver cirrhosis, 66% bled from varices and 34% from other lesions. The proportion of patients who bled from oesophageal varices is higher under 60 yrs. The mortality was higher after 60 yrs, except when there was associated chronic liver disease or renal or cardio-respiratory failure. In this group of patients, near half in our series, the mortality is the same under and above 60 years.