Histological evaluation of the effects of borax obtained from various sources in different rat organs / Evaluación histológica de los efectos del borax obtenido de diversas fuentes en diferentes órganos de rata

Boron is an essential element for life and intake via different sources into the body. Because effects of boron and compounds on the body has not been studied enough especially in tissue level, we planned this study to evaluate the effects of borax the most intaken form of boron compound on different intraabdominal organs histologically and also clinically. 42 male rats divided into equal 7 groups and different toxicological doses consistent with its LD50 dose (5000 mg/kg/d) were administered by gavage except control and sham groups. In the study, 2 different kinds of borax one of which was produced for research and the other for agriculture but the same formulation, were used and their effects were also compared. As a result it was found that borax did not cause any histological changes in kidney, large intestine, liver and stomach in lower doses. But if doses were increased, a slightly inflammatory cell migration was detected without clinical signs in liver and large intestine. However, when a single very high dose of borax was administered, very high edema, inflammatory cell migration and neovascularization was observed and clinically 2 out of 6 rats died within 5 hours. We suggested that very high dose intake of borax may cause sudden death and also during long periods and higher dose intake may pave the way of inflammatory bowel diseases. At the same time, in boron related studies we advice that the kind of boron and also their source should be evaluated carefully and the most suitable compound should be chosen in case of faulty results.

El boro es un elemento esencial para la vida e ingresa a través de diferentes fuentes al cuerpo. Dado que los efectos del boro y sus compuestos en el cuerpo no se han estudiado lo suficiente, especialmente a nivel tisular, se planificó este estudio para evaluar sus efectos y la forma de consumo más común del compuesto de boro sobre diferentes órganos intraabdominales a nivel histológico y clínico. Cuarenta y dos ratas macho divididas en 7 grupos, con diferentes dosis toxicológicas de acuerdo con su dosis DL50 (5000 mg/kg/d) administradas por sonda, excepto en los grupos control y simulado. En el estudio fueron usados 2 tipos diferentes de boro, uno producido para la investigación y el otro para la agricultura, pero de la misma formulación, y sus efectos fueron comparados. Se encontró que el boro no causó cambios histológicos en el riñón, intestino grueso, hígado y estómago en dosis bajas. Sin embargo, al aumentar la dosis, se detectó una leve migración de células inflamatorias, sin signos clínicos, en el hígado e intestino grueso. Por otra parte, cuando se administró una sola dosis muy alta de boro, se observó un amplio edema, migración de células inflamatorias y neovascularización; clínicamente 2 de 6 ratas murieron dentro de 5 horas. Sugerimos que la ingesta de dosis muy altas de bórax pueden causar la muerte súbita, además la ingesta de dosis altas y durante periodos de tiempo prolongado puede causar enfermedades inflamatorias del intestino. Es recomendable que en los estudios relacionados con el boro, el tipo de boro así como su fuente sean evaluados cuidadosamente, eligiendo el compuesto más adecuado en caso de resultados erróneos.

Gastrointestinal and cardiovascular risk of nonsteroidal anti-inflammatory drugs

Nonsteroidal anti-inflammatory drugs [NSAIDs] confer a gastrointestinal [GI] side effect profile and concerns regarding adverse cardiovascular effects have emerged associated with considerable morbidity and mortality. NSAIDs are highly effective in treating pain and inflammation, but it is well recognized that these agents are associated with substantial gastrointestinal toxicity. Cyclo-oxygenase-2 inhibitors may also reduce the risk for gastrointestinal events, although they may increase cardiovascular adverse events. The selection of an appropriate analgesic or antiinflammatory agent with or without gastroprotective therapy should be individualized

Histoenzymological study on the toxicity of copper sulphate in the digestive glands of Lymnaea luteola.

During 24 and 48 hr of exposure, the digestive glands of Lymnaea treated with a lethal concentration of 0.038 mgl(-1) CuSO4 revealed intense activity of acid phosphatase in perilobular margin. On the other hand, same area of the gland showed moderate activity of ATPase during 24 and 48 hr of exposure. However, alkaline phosphatase showed average activity in perialveolar region and perilobular margin during 24 and 48, and 72 hr of exposure respectively The changes in the activity of these enzymes were nonsignificant in alveolar margin and perialveolar region of the gland. It is interesting to note moderate activity of acid phosphatase in perialveolar region during 24 hr of exposure.

Effect of aqueous extract of Ocimum sanctum Linn. [Labiateae] on gastrointestinal tract

The effect of O. sanctum L. on gastrointestinal [GI] motility by BaSO4 revealed that O. sanctum L. aqueous extract significantly increased the peristaltic movement of GI tract compared to control. But the in vitro result on isolated guinea pig ileum differs from the in vivo gastrointestinal motility result. The in vitro result of hot water extract showed a dose dependent increase in relaxation on isolated guinea pig ileum similar to previous findings and it showed no interaction with acetylcholine

COX-2 inhibitors: What's the message for practising physician?

The development of Cox-2 inhibitors as potentially gastro-safe NSAIDs is based on the notion that Cox-1 predominates in the stomach, yielding protective prostaglandins, while Cox-2 is induced in inflammation giving rise to pain, swelling and stiffness. The conventional NSAIDs are the most widely prescribed drugs. Despite excellent efficacy in rheumatic disorders their toxicity can lead to significant morbidity and mortality. With the introduction of Cox-2 specific inhibitors, there is a widespread belief that at last safe anti-inflammatory drugs are at hand and are being used extensively.This article reviews the available data regarding their safety on gastrointestinal and cardiorenal systems. It will help the physicians to make a decision while prescribing these drugs to their patients especially who have risk factors

General pharmacological profiles of bee venom and its water soluble fractions in rodent models

Recently, the antinociceptive and anti-inflammatory efficacy of bee venom (BV, Apis mellifera) has been confirmed in rodent models of inflammation and arthritis. Interestingly, the antinociceptive and anti-inflammatory effect of whole BV can be reproduced by two water-soluble fractions of BV (>20 kDa:BVAF1 and<10 kDa: BVAF3). Based on these scientific findings, BV and its effective water-soluble fractions have been proposed as potential anti-inflammatory and antinociceptive pharmaceuticals. While BV's anti-inflammatory and antinociceptive properties have been well documented, there have been no careful studies of potential, side effects of BV and its fractions when administered in the therapeutic range (BV, 5 microgram/kg; BVAF1, 0.2 microgram/kg: BVAF3, 3 microgram/kg; subcutaneous or intradermal). Such information is critical for future clinical use of BV in humans. Because of this paucity of information, the present study was designed to determine the general pharmacological/physiological effects of BV and its fractions administration on the rodent central nervous, cardiovascular, respiratory and gastrointestinal system. Subcutaneous BV and its fractions treatment did not produce any significant effects on general physiological functions at the highest dose tested (200-fold and 100-fold doses higher than that used clinically, respectively) except writhing test. These results demonstrate that doses of BV or BV subfractions in the therapeutic range or higher can be used as safe antinociceptive and anti-inflammatory agents.

Oral administration of calcium pectinate beads: study of resistance of digestive system at mouse

The controlled pharmaceutical forms, which include pharmaceutical vectors, have not been restricted to vascular, external or respiratory use, but they became useful for digestive system for the treatment of many diseases [1, 4, 15]. That due is to the great advantages of this via system. In this research, we studied the fate of pectin beads after their oral administration to a mouse. Design and Various forms of pectin were used to prepare beads in the presence of calcium ions to obtain egg- box model [2, 20]. This technique has enabled to get beads, which can carry the used active substances into the colon level, after they were coated with a protective material against gastrointestinal effects. 1- Pectin beads with dimensions 900- 1200 microm, were prepared using 6% of calcium ions [w/v]. They had a different swelling time and a good stability [80- 90%] in the gastrointestinal medium. Also they had an ability to release their contained active substance after three hours of their oral administration into studied mouse. 2- Time of active substance release from pectin beads was controlled into five different areas of digestive system of mouse. Also the fate of pectin beads was studied

Applications of inulin and oligofructose in health and nutrition.

Inulin and oligofructose belong to a class of carbohydrates known as fructans. The main sources of inulin and oligofructose that are used in the food industry are chicory and Jerusalem artichoke. Inulin and oligofructose are considered as functional food ingredients since they affect the physiological and biochemical processes in rats and human beings, resulting in better health and reduction in the risk of many diseases. Experimental studies have shown their use as bifidogenic agents, stimulating the immune system of the body, decreasing the pathogenic bacteria in the intestine, relieving constipation, decreasing the risk of osteoporosis by increasing mineral absorption, especially of calcium, reducing the risk of atherosclerosis by lowering the synthesis of triglycerides and fatty acids in the liver and decreasing their level in serum. These fructans modulate the hormonal level of insulin and glucagon, thereby regulating carbohydrate and lipid metabolism by lowering the blood glucose levels; they are also effective in lowering the blood urea and uric acid levels, thereby maintaining the nitrogen balance. Inulin and oligofructose also reduce the incidence of colon cancer. The biochemical basis of these beneficial effects of inulin and oligofructose have been discussed. Oligofructose are non cariogenic as they are not used by Streptococcus mutans to form acids and insoluble glucans that are the main culprits in dental caries. Because of the large number of health promoting functions of inulin and oligofructose, these have wide applications in various types of foods like confectionery, fruit preparations, milk desserts, yogurt and fresh cheese, baked goods, chocolate, ice cream and sauces. Inulin can also be used for the preparation of fructose syrups.

Do side-effects reduce compliance to iron supplementation? A study of daily- and weekly-dose regimens in pregnancy.

Side-effects of iron supplementation lead to poor compliance. A weekly-dose schedule of iron supplementation rather than a daily-dose regimen has been suggested to produce fewer side-effects, thereby achieving a higher compliance. This study compared side-effects of iron supplementation and their impact on compliance among pregnant women in Bangladesh. These women were assigned to receive either weekly doses of 2 x 60 mg iron (one tablet each Friday morning and evening) or a daily dose of 1 x 60 mg iron. Fifty antenatal care centres were randomly assigned to prescribe either a weekly- or a daily-supplementation regimen (86 women in each group). Side-effects were assessed by recall after one month of supplementation and used for predicting compliance in the second and third months of supplementation. Compliance was monitored using a pill bottle equipped with an electronic counting device that recorded date and time whenever the pill bottle was opened. Of five gastrointestinal side-effects (heartburn, nausea, vomiting, diarrhoea, or constipation) assessed, vomiting occurred more frequently in the weekly group (21%) than in the daily group (11%, p<0.05). Compliance (ratio between observed and recommended tablet intake) was significantly higher in the weekly-supplementation regimen (93%) than in the daily-supplementation regimen (61%, p<0.05). Overall, gastrointestinal side-effects were not significantly associated with compliance. However, the presence of nausea and/or vomiting reduced compliance in both the regimens-but only among women from the lower socioeconomic group. In conclusion, weekly supplementation of iron in pregnancy had a higher compliance compared to daily supplementation of iron despite a higher frequency of side-effects. The findings support the view that gastrointestinal side-effects generally have a limited influence on compliance, at least in the dose ranges studied. Efforts to further reduce side-effects of iron supplementation may not be a successful strategy for improving compliance and effectiveness of antenatal iron supplementation.

Inhibiteurus selectifs de la cyclo-oxygenase-2 et tube digestif

The use of non steroidal anti-inflammatory drugs [NSAIDS] is tempered by the development of side effects primarily in the gastro-intestinal tract. These effects result mainly from inhibition of the enzyme cyclo-oxygenase [COX]-1. Two NSAIDS [celecoxib and rofecoxib] COX-2 specific inhibitors had considerably lower ulcerogenic rates and lower serious gastro intestinal side effects when compared with other NSAIDs used in rhumatoid arthritis and osteoarthritis. However, the exact place of COX-2 specific inhibitors remain to be determined as compared with the association of other NSAIDs and proton pump inhibitors in the elderly. The efficacy of COX-2 specific inhibitors in digestive tumors is still unclear

Theophylline toxicity in Thai children.

Theophylline is a useful drug in the treatment of respiratory diseases with bronchospasm but it has very narrow safety margin. The study was carried out in 44 admitted Thai children with plasma theophylline levels > 20 microg/ml to determine the association between blood levels and symptoms of theophylline toxicity. The prevalence of theophylline toxicity (plasma theophylline level > 20 microg/ml) in Thai children is about 11%. Thirty-four percent of the patients who had theophylline levels less than 30 microg/ml and 78% of those who had levels more than 30 microg/ml had symptoms of theophylline toxicity. The symptoms were related to the gastrointestinal tract (34%), cardiovascular system (18.2%), neurological system (6.8%) and metabolism (54.5%). The possible causes of theophylline toxicity were respiratory tract infection, theophylline overdosage, interaction with other drugs, impairment of liver function, congenital heart disease and theophylline usage in neonates. Theophylline is still a useful drug but should be used with caution. Theophylline levels should be checked in every child who receives theophylline.

Evaluation of methanolic extract of Ficus platyphylla on gastrointestinal activity.

Methanolic extract of Ficus platyphylla was tested on isolated rabbit jejunum, rat duodenum and gastrointestinal motility in mice. The extract showed a biphasic effect on isolated smooth muscle. Lower concentration of extract caused contraction, while higher concentrations produced relaxation. The contractile phase was attenuated by atropine, while relaxant phase attenuated histamine induced contraction of guinea pig ileum. The extract also exhibited a dose-dependent inhibition of gastrointestinal motility. Acute toxicity test in mice established LD50 value (i.p.) of the extract to be 2000 mg/kg. Preliminary phytochemical screening of the extract gave positive test for flavonoids, tannins and saponins.

Non-steroidal-anti-inflammatory-drugs indiced gastrotoxicity

Non-Steroidal-Anti-Inflammatory-Drugs [NSAIDs] toxicity in the upper gastrointestinal tract is amongst the most common serious drug-induced toxicity. Enormous progress has been made in the understanding of NSAIDs-induced peptic ulcer disease in the last decade. Inhibitors in at-risk patients would require further investigation. The introduction of Cox-II specific agents offers the opportunity for safe and effective treatment for patients who are at high risk for developing GI complications. However, large, long-term, randomized and controlled studies are needed in the future to assess the overall safety of Cox-II specific inhibitors, especially in organs outside the GI tract. Whilst several matters of detail about use of Cox-II specific inhibitors persist, there is sufficient data to be confident that Cox-II specific inhibitors represent a therapeutic revolution capable of reducing NSAIDs associated gastric complications substantially. Whether such complications will be at placebo levels will require further study. The available data is still limited, particularly in the at-risk groups i.e., elderly, patients with previous history of GI complications, and are on corticosteroids

Inhibidores selectivos de la COX-2 (ISC-2): evidencias actuales sobre su real eficacia y seguridad / COX-2 selective inhibitors (C2SI): update evidence of their efficacy and safety

A principios de la década pasada, fueron descubiertas dos isoformas de la enzima ciclooxigenasa, encargada de catalizar la producción de postaglandinas a partir del ácido araquidónico. La COX-1, expresada en forma constitutiva a nivel gastrointestinal, renal y plaquetario, y la COX-2, enzima principalmente inducible en proceso como la inflamación, el dolor y la fiebre. Numerosos estudios, han demostrado tanto la eficacia, como la seguridad gástrica y plaquetaria de los inhibidores selectivos de la COX-2, en estudios fase II y en estudios clínicos fase III. Basados en estos estudios, en 1999 fueron aprobados por la FDA, dos inhibidores selectivos, celecoxib y refecoxib, para su uso en pacientes con artrosis y artritis reumatoídea. Estos fármacos se encuentran también disponibles en nuestro país. Estudios recientes demuestran, sin embargo, que ambas isoformas de COX, participarían en el proceso inflamatorio, y por lo tanto, su eficacia analgésica y antiinflamatoria, serían menor a la obtenida con los antiinflamatorios no esteroidales tradicionales. Por otro lado, tanto a nivel gástrico como renal se ha visto participación de la COX-2 en procesos fisiológicos, como la resolución de la inflamación en mucosas dañadas y en la embriogénesis renal en ratas. Por último, existen varias evidencias que demuestran funciones fisiológicas de la COX-2, en sitios tan disímiles como el sistema nervioso central y el colon. En estas localizaciones ha sido implicada en la patogenia de la enfermedad de Alzheimer y del cáncer de colon, lo que abre la posibilidad de desarrollar nuevas líneas de investigación, destinadas a encontrar nuevos tratamientos para éstas y otras patologías

Celecoxib vs indometacina y lesiones gastricas agudas en ratas / Celecobix vs indomethacin and acute gastric lesions in rats

En diferentes grupos de ratas Wistar (n = 15 en c/grupo), se estudiaron las dosis ulcerogénicas AINES COX-1 como Indometacina vs Celecoxib (inhibidor selectivo COX-2), en la producción de úlceras antrales gástricas y necrosis de la mucosa del intestino delgado y colon. Se encontró que Celecoxib, dado en forma oral o subcutánea cada 12 hs durante 5 días, no provocó lesiones en mucosa gastrointestinal, en cambio, dado el Celecoxib después de la Indometacina, agravé las úlceras antrales gástricas y dio necrosis masiva tanto del intestino delgado y del colon y óbito de todas las ratas. Se concluyó que Celecoxib no provocó lesiones gastrointestinales en mucosa sana; en contraste, se amplificaron las lesiones preexistentes gastrointestinales inducidas por Indometacina.

Aspirina e distúrbios gastrointestinais / Aspirin and gastrointestinal symptoms

Os efeitos gastrointestinais da aspirina dor epigástrica, pirose, náuseas, perda gastrointestinal de sangue oculto e, ocasionalmente, hemorragia digestiva altaconstituem as principais reações adversas desse fármaco e o fato mais importante na limitaçäo de seu uso clínico.Essas reações säo dose dependentes.A causa completamente elucidada, mas admite-se como fator principal a inibiçäo da síntese de eicosanóides na mucosa gástrica.A toxidade gastrointestinal da aspirina, quw pode induzir erosões e úlceras, é dose dependente e diminui nitidamente com a utilizaçäo de doses baixas 75,100,160 ou 200mg/ dia, as quais se monsraram täo eficazes quanto as doses altas nas diversas condições cardiovasculares em que foram avaliadas.O uso de doses baixas de aspirina é a medida mais importate para previnir a ocorrência de efeitos colaterais gastrointestinais.Outras medidas incluem: utilizaçäo de soluções diluídas, de preparações tamponadas ou de liberaçäo entérica e, eventualmente, o uso concomitante de ranitidina, omeprazol ou similar.Os pacientes que näo toleram a aspirina, mesmo em doses baixas e com os cuidados acima, devem substituí-la por outro antiplaquetário.