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At least 793 records · Page 44Linked to original sources
PubMed2000

The effect of the NK1 receptor antagonist CP-99,994 on emesis and c-fos protein induction by loperamide in the ferret.

The site of the anti-emetic action of the neurokinin1 receptor antagonist CP-99,994 was studied in the ferret using the centrally acting opiate receptor agonist loperamide at a dose (0.5 mg/kg s.c.) which induced emesis in all animals tested. CP-99,994 (1 mg/kg, s.c.x2) abolished the emetic response (retching and vomiting) and the behaviours (licking, wet dog shakes, mouth scratching and gagging) induced by loperamide over a 2-h observation period. The enantiomer of this compound CP-100,263 (1 mg/kg, s.c.x2) did not have any significant effect on emesis or related behaviours. Loperamide (0.5 mg/kg s.c.) administration (but not its vehicle) resulted in dense fos-like immunoreactivity (FLI) mainly throughout the rostro-caudal extent of the nucleus tractus solitarius but not the area postrema. Although CP-99,994 (1 mg/kgx2) abolished the loperamide-induced emesis, it did not have any statistically significant effect on FLI in the brainstem. In loperamide and CP-100,263 (1 mg/kg, s.c.x2) treated animals FLI was comparable to that in animals treated with loperamide and CP-99,994. The results from this study taken together with those from previous studies indicate that loperamide exerts its emetic effect via nucleus tractus solitarius dendrites projecting into the area postrema. The lack of significant effect of CP-99,994 on the FLI induced by loperamide in this nucleus suggests that it is acting at a site "deep" in the nucleus tractus solitarius or elsewhere. The marked reduction in behaviours associated with loperamide administration by CP-99,994 provides a preliminary indication that NK1 receptor antagonist (as represented by CP-99,994) may in the clinic have effects on behaviours induced by emetic agents in addition to their previously described effects on retching and vomiting.

Animals↗
PubMed2001

Symptoms of ovarian cancer.

OBJECTIVE: To examine the symptoms of ovarian cancer in patients compared with symptoms experienced by healthy women using a case-control design. METHODS: Cases (n = 168) were women with ovarian cancer diagnosed at two hospitals in New York between 1994 and 1997 who were interviewed shortly after diagnosis. They were compared with healthy women (n = 251 controls) from the community. Women were asked about the prevalence, duration, and constancy of eight symptoms and about use of three types of medications in the 6 to 12 months before diagnosis (cases) or interview (controls). RESULTS: Nearly all the cases (93%) reported at least one symptom, compared with 42% of controls. The most common symptoms among cases were: unusual bloating, fullness, and pressure in the abdomen (71%); unusual abdominal pain or lower back pain (52%); and lack of energy (43%). The proportions of controls reporting these symptoms were 9, 15, and 16%, respectively, resulting in odds ratios and 95% confidence intervals of 25.3 (15.6, 40.9), 6.2 (4.0, 9.6), and 3.9 (2.5, 6.1), respectively, for these symptoms. Bloating, fullness, and pressure was of more recent onset among cases than controls (4.9 months compared with 7.6 months, P =.01). There were only minor differences in reported symptoms between cases with early and later stage disease. CONCLUSION: Unusual bloating, fullness, and pressure, abdominal or back pain, and lack of energy are prominent symptoms in women with ovarian cancer and distinguish them from controls. Information on symptoms may make women and physicians more aware of changes associated with ovarian cancer.

Adult↗
PubMed1996

Infectious gastroenterocolitides in children: an update on emerging pathogens.

The recognition that bacterial infections induce signal transduction responses in infected epithelial cells also provides new avenues to consider as novel forms of therapy. For example, the chemokine interleukin-8, which attracts neutrophils to sites of mucosal infection, is produced by epithelial cells of gastric and intestinal origin in response to bacterial infection. Inhibitors of chemokine production or inhibition of the biologic effects of neutrophil chemoattractants have the potential to reduce both mucosal inflammatory responses and the attendant clinical sequelae. Eukaryotic cells also respond to infection with elevations in cytosolic second messengers, including inositol triphosphate (IP3) and calcium ([Ca2+]i). In intestinal epithelium, these second messengers can mediate the diarrheal response to infection. Calcium/calmodulin inhibitors may have a beneficial effect in treating those gastrointestinal infections mediated through changes in the level of cytosolic free calcium. DuPont and colleagues showed, for example, that oral therapy with zaldaride maleate relieves symptoms of disease and shortens the duration of diarrhea in travelers with ETEC-induced diarrhea. Evaluation of additional signal transduction responses to microbial infections should provide both new insights into the pathogenesis of gastrointestinal infectious diseases and novel approaches to consider for the prevention and therapy for these human illnesses.

Antidiarrheals↗
PubMed1997

In vitro adsorption of mebeverine hydrochloride onto kaolin and its relationship to pharmacological effects of the drug in vivo.

The in vitro uptake of mebeverine hydrochloride from an initial drug concentration of 0.25-4.25 or 0.2-3.6 g% w/v onto kaolin 5.0 g% w/v at pH 1.8 or 7.5, respectively, at 37 degrees C was represented by a double- layered adsorption isotherm. The calculated data were in accordance with a Langmuir adsorption isotherm for an initial drug concentration up to 2.1 or 2.0 g% w/v when a monolayer was formed at pH 1.8 or 7.5, respectively. The adsorption process is pH dependent, and is affected by the electrolyte concentration and valency. The amount of the drug desorbed (mg% w/v) by washing with different elution media at 37 degrees C followed the sequence 0.1 M hydrochloric acid > 0.1 M magnesium chloride > 0.1 M sodium chloride > simulated intestinal fluid. The results obtained from this study indicate that two mechanisms, ion exchange and physical adsorption, were involved in the uptake of mebeverine hydrochloride by kaolin. The presence of different concentrations of kaolin with the tablets or capsules of the drug, adversely affected the release rate. The in vivo and in vitro studies on guinea pig ileum showed that the presence of kaolin in a mixture with mebeverine hydrochloride did not affect to any significant level the inhibiting effect of the musculotropic drug on carbachol-induced contractions in the isolated guinea pig ileum. In vivo studies showed similar results for barium chloride as well.

Adsorption↗
PubMed1989

Pharmacy dispensing practices for Sudanese children with diarrhoea.

In order to study the dispensing practices of Khartoum and Khartoum North pharmacies with respect to the management of infantile diarrhoea, a Sudanese woman presented pharmacists with a brief description of an infant with acute diarrhoea. Sixty-three pharmacies were visited; only 3 (5%) recommended oral rehydration salts (ORS) alone. An additional 4 pharmacies (6%) recommended ORS plus either an antimicrobial agent or a physician visit. 39 pharmacies (62%) recommended antimicrobial therapy alone, 9 (14%) recommended a physician visit alone and 7 pharmacies (11%) had no available treatment. On average, antimicrobials cost four times more than two packets of ORS. In order to increase pharmacists' recommendation of ORS, health professional training may be required, perhaps in association with dispensing subsidies. Increased public awareness of ORS should also be encouraged.

Adult↗
PubMed2003

Potential roles of P-gp and calcium channels in loperamide and diphenoxylate transport.

This study examined the accumulation and transport of two related systemic opioids used as antidiarrhoeal drugs and compared their rates of transport with known P-glycoprotein (P-gp) substrates used in our in vitro environment. Cellular uptake and efflux and transcellular transport were all determined using Caco-2 cells after exposure to loperamide or diphenoxylate, with or without a range of efflux inhibitors. Bidirectional transport studies of 5 microM loperamide showed efflux to be fivefold higher than influx (42 x 10(-6) compared to 8 x 10(-6) cm/s); however, this decreased to twofold at 10 microM and was abolished using 100 microM loperamide. An uptake pathway was also discovered when P-gp was inhibited which, in the presence of Ca(2+) channel blockers, was amplified, providing a potential mechanism for central nervous system effects to be increased upon blockage of L-type calcium channels, quite separate from any P-gp inhibition. Diphenoxylate transport, however, showed little sign of P-gp-mediated efflux. Diphenoxylate accumulated readily within cells, yet transport through cells was very low. Additionally, efflux inhibitors had little impact on transport or accumulation, suggesting that diphenoxylate was not a substrate for an efflux mechanism.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed2001

Influence of heavy organic pollutants of anthropic origin on PAH retention by kaolinite.

The adsorption of heavy fuel oil No. 2 (F2) on a reference kaolinite (Arvor kaolin, France), and the influence of this anthropic organic matter on the phenanthrene (PHEN) retention capacity of a kaolinite were investigated in the laboratory. The heaviest and most polar compounds of F2 are adsorbed on kaolinite preferentially to the other compounds and also partly irreversibly. The precoating of kaolinite by F2 significantly increases the sorption of PHEN in the range of concentrations studied (10-500 microg l(-1)). The partition coefficients normalized to organic carbon content (Koc) of kaolin precoated with fuel oil (5.2 < log Koc < 5.5) are one order of magnitude higher than those of the original kaolin (4.2 < logKoc < 4.5), and show very good agreement with the literature for polluted industrial soils. The Koc measured on the uncoated kaolin are in close agreement with the values determined for natural soils in which humic substances represent the organic component. This demonstrates that the composition of organic matter is the primary factor in PHEN retention by the soils. Therefore, in predicting the transport of PHEN, and other Polycyclic aromatic hydrocarbons (PAHs) in general, in soils of industrial sites containing heavy hydrocarbons or tars requires that the specific nature of the organic matter contained in these soils be taken into consideration.

Adsorption↗
PubMed1999

Possible mechanisms through which dietary pectin influences fibrin network architecture in hypercholesterolaemic subjects.

It is suspected that not only fibrinogen concentration but also the quality of fibrin networks may contribute to cardiovascular risk. Evidence is accumulating that a "prudent" diet may protect against diseases associated with raised clotting factors. The effect of diet on fibrinogen is, however, still controversial. In a previous study performed in our laboratory, it was shown that dietary pectin influences fibrin network architecture in hypercholesterolaemic men without causing any changes in fibrinogen concentration. To elucidate the possible mechanisms, it was necessary to study the possibility that pectin may itself have indirect effects on fibrin network architecture. Pectin is fermented in the gastrointestinal tract to acetate, propionate, and butyrate. In humans, only acetate reaches the circulation beyond the liver. This investigation primarily examined the possibility that pectin may, through acetate, influence fibrin network architecture in vivo. The effects of pectin and acetate supplementation in hypercholesterolaemic subjects were compared. Furthermore, this study also aimed at describing the possible in vitro effects of acetate on fibrin network architecture. Two groups of 10 male hyperlipidaemic volunteers each received a pectin (15 g/day) or acetate (6.8 g/day) supplement for 4 weeks. Acetate supplementation did not cause a significant change in plasma fibrinogen levels. As in the pectin group, significant differences were found in the characteristics of fibrin networks developed in plasma after 4 weeks of acetate supplementation. Fibrin networks were more permeable (from 213+/-76 to 307+/-81 x 10(11) cm2), had lower tensile strength (from 23+/-3 to 32+/-9% compaction), and were more lyseable (from 252+/-11 to 130+/-15 minutes). These results strongly suggest that the effect of pectin on network architecture could partially be mediated by acetate. Progressive amounts of acetate were used in vitro to investigate the possibility that acetate may be directly responsible for changes that occurred in fibrin network architecture in the plasma medium. Results indicated that acetate influenced fibrin network architecture directly. From the results, it seems highly possible that acetate may be responsible in part for the beneficial effects of pectin supplementation in vivo. It is evident that pectin or acetate supplementation can be useful during the treatment or prevention of some clinical manifestations, especially those associated with raised total cholesterol and possibly also plasma fibrinogen.

Adult↗
PubMed2001

The antisecretory factor: synthesis, anatomical and cellular distribution, and biological action in experimental and clinical studies.

The antisecretory factor (AF) is a 41-kDa protein that provides protection against diarrheal diseases and intestinal inflammation. Its cDNA has been cloned and sequenced. AF is highly potent, with 10(-12) mol of recombinant AF being sufficient to counteract experimentally induced diarrhea in rat. The antisecretory activity is exerted by a peptide located between positions 35 and 50 of the AF sequence. Synthetic peptides based on this sequence are promising candidates for drugs to counteract intestinal hypersecretion, as well as imbalances of fluid transport in other body compartments. AF probably exerts its effects via nerves; AF immediately and potently inhibits ion transport across isolated nerve membranes from Deiters' cells. Immunocytochemistry has shown that AF is present in most tissues in the body, and in situ nucleic acid hybridization has shown that cells that store AF are also capable of AF synthesis. The endogenous plasma level of AF is increased by enterotoxins and by certain food constituents such as hydrothermally processed cereals. These cereals significantly improve clinical performance in patients suffering from inflammatory bowel diseases. AF-enhancing food also protects domestic animals against diarrheal diseases, and such feed has been used successfully in Swedish swine farming for the past 10 years. Increased understanding of AF action might result in expanded clinical applications and confirm that AF is an important regulator of homeostasis.

Animal Feed↗
PubMedDate not supplied

Pharmacological characterization of cyclosporine A-induced kaolin intake in rats.

Kaolin intake behavior of rats is known to be one of the useful animal models to evaluate the emetic and antiemetic actions of drugs. The present study was aimed at elucidating the pharmacological characterization of cyclosporine A (CsA)-induced kaolin intake in rats. Subchronic treatment (once a day for 3 days) with CsA produced a dose- and time-dependent increase in kaolin intake. Scopolamine (muscarinic antagonist), mepyramine (selective histamine H(1) antagonist) and diphenhydramine (H(1) and muscarinic antagonist) but neither domperidone (dopamine D(2) antagonist) nor ondansetron (serotonin 5-HT(3) antagonist) significantly inhibited CsA-induced kaolin intake. These findings suggest that an activation of central muscarinic and H(1) receptor is closely associated with CsA-induced kaolin intake in rats. Use of scopolamine and/or diphenhydramine may be possible regimens to alleviate and avoid nausea and vomiting in patients with CsA therapy.

Animals↗
PubMed2002

Prevention and self-treatment of travelers' diarrhea.

Of the 50 million people who travel from the industrialized world to developing countries every year, between 20% and 50% will develop at least one episode of diarrhea, making it the most common ailment of travel. Although usually a mild illness, travelers' diarrhea can result in significant morbidity and hardship while overseas. Precautions can be taken to minimize the risk of developing diarrhea. If diarrhea does develop despite precautions, effective treatment, usually a combination of an antibiotic and an antimotility agent, can be taken along and started by the traveler at the onset of symptoms.

Antibiotic Prophylaxis↗
PubMed2002

Evaluation of diarrhea in the returned traveler.

Diarrhea in the returned traveler is common, but it is generally self-limited. Although the concern is often directed at the presence of an ongoing infection, postinfectious and noninfectious etiologies must be considered [table: see text] also. Answers to the clinical questions posed in this article will guide the clinician toward an appropriate diagnostic and management strategy.

Antidiarrheals↗
PubMed2001

Irritable bowel syndrome.

Irritable bowel syndrome is a common gastrointestinal disorder characterized by abdominal pain and a change in bowel habits. It is estimated to occur in 9% to 22% of the US population, and is more often diagnosed in women than in men. There are no diagnostic markers for irritable bowel syndrome and no evidence of organic disease. Moreover, the pathophysiology is not completely understood; however, abnormal gastrointestinal motility, altered sensory activity, central neural dysfunction, psychological disturbances, and luminal factors have been proposed. Treatment requires a multifaceted approach. Education, dietary measures, fiber supplementation, and pharmacological and psychological interventions have been used in the management of this disorder.

Antidiarrheals↗
PubMed1996

Evaluation of the adult patient with diarrhea.

This article provides the primary care clinician with a general diagnostic and therapeutic approach to the adult patient with diarrhea. Basic pathophysiologic mechanisms are described. Important causes and clinical features of each type of diarrhea are highlighted. A step-by-step diagnostic evaluation is suggested, and an overview of treatment options is presented.

Acute Disease↗