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Traveler's diarrhea.

Travelers' diarrhea is common. Between 8% and 50% of travelers develop diarrhea; incidence depends on the country visited. The attack rate is highest for travelers from a developed country who visit a developing country. Children are at particular risk. Travelers' diarrhea is usually acquired through ingestion of fecally contaminated food and water. Most cases are due to a bacterial pathogen, commonly, Escherichia coli, and occur within the first few days after arrival in a foreign country. More than 90% of episodes develop within the first 2 wk of initiation of travel. Dehydration is the most common complication. Water and electrolyte replenishment is important and can usually be accomplished with an oral rehydration solution. Judicious use of an antimotility agent and antimicrobial therapy reduces the duration and severity of diarrhea. Pretravel education on hygiene and on the safe selection of food items is important in minimizing episodes. Dukoraltrade mark (Aventis Pharma Ltd., Auckland, New Zealand) vaccine should be considered for travelers who are 2 y of age or older and who will be visiting an area associated with risk of infection due to enterotoxigenic E coli or Vibrio cholerae. Typhoid vaccine is recommended for travelers who will be visiting areas with poor sanitation and hygiene.

Anti-Infective Agents↗
PubMed2006

Current status of anti-diarrheal and anti-secretory drugs in the management of acute childhood diarrhea.

Each year 1.8 million children die due to diarrheal diseases. Indiscriminate use of antibiotics has resulted in increasing resistance to commonly used antibiotics. Moreover the recent outbreaks of shigella and cholera have revealed multi-drug resistance strains. There is a need for review of recommended antibiotics for shigellosis. From recent data it emerges that fluoroquinolones should be the first line of therapy and cephalosporins to be used as the second line. Among the anti-cholera antibiotics, tetracyclines which were the drug of choice for adults, has the advantage of high sensitivity and low cost. Single dose doxycycline would have minimal side effects, hence can be the drug of choice even in children. We should not allow the business pressures to force usage of probiotics and racecadotril as their role in the management of acute diarrhea is yet to be established. Nitazoxanide has high efficacy against Cryptosporodial diarrhea only. Strict adherence to the recommendations for the management of acute childhood diarrhea is needed or else we dilute the effect of standard management.

Acute Disease↗
PubMed2006

Synthesis and smooth muscle-selective relaxant activity of a piperidine analogue: 1-(4'-fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride.

The antispasmodic and vasodilator activities of a newly synthesized piperidine derivative (1-(4'-fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride) were studied in vitro. The test compound exhibited a dose-dependent relaxant effect on the spontaneous and K+ (75 mM)-induced contractions of isolated rabbit jejunum with respective EC50 values of 0.01 mM (0.01-0.02, 95% Cl) and 0.30 mM (0.17-0.56). The Ca++ channel blocking (CCB) activity was confirmed when the test compound (0.1-0.2 mM) shifted the Ca++ dose-response curves to the right, similar to that produced by verapamil (0.1-1.0 microM), a standard CCB. In the isolated rabbit aorta, the test compound showed a dose-dependent vasodilator effect on K+ (75 mM)-induced contractions with an EC50 value of 0.08 mM (0.02-0.26) while also suppressed the norepinephrine (1 microM) control peak responses with EC50 value of 0.08 mM (0.05-0.13, n=5). When tested in Langendorff perfused rabbit heart preparation, the test compound exhibited a negligible inhibitory effect on the rate or force of atrial and ventricular contractions when tested up to 5 mM. The results show smooth muscle-selective relaxant effect of the test compound on intestinal and vascular preparations mediated possibly via blockade of voltage and receptor-operated Ca++ channels.

Acetylcholine↗
PubMed2004

[Fecal incontinence].

Diagnosis and management of fecal incontinence requires exact understanding of the anatomic and pathophysiologic principles involved and demands a methodical, stepwise approach. Despite the potential appeal of surgical intervention, a considerable number of patients can be helped by comparatively simple, noninvasive measures. Initial treatment should be medical, including biofeedback in combination with a bowel management program. In the presence of a severely denervated pelvic floor, physiotherapeutic techniques rarely give rise to a satisfactory and long-lasting response. Obvious external sphincter defects and patients who failed medical management are treated surgically. Many injuries of the external sphincter can be treated by direct sphincter repair. If patients with intact external sphincters are unresponsive to medical measures, descending perineum and resultant idiopathic fecal incontinence will improve by radio-frequency delivery, sacral nerve stimulation, or postanal plication. Patients with complex neurologic disorders or extensive sphincter defects or who have undergone previous unsuccessful attempts at repair of the puborectalis itself should be considered for dynamic gracilis plastic or an artificial sphincter.

Aged↗
PubMed2004

Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes.

OBJECTIVE: The purpose of the present study was to elucidate the cytochrome P450 (P450) isoform(s) involved in the metabolism of loperamide (LOP) to N-demethylated LOP (DLOP) in human liver microsomes. METHODS: Three established approaches were used to identify the P450 isoforms responsible for LOP N-demethylation using human liver microsomes and cDNA-expressed P450 isoforms: (1) correlation of LOP N-demethylation activity with marker P450 activities in a panel of human liver microsomes, (2) inhibition of enzyme activity by P450-selective inhibitors, and (3) measurement of DLOP formation by cDNA-expressed P450 isoforms. The relative contribution of P450 isoforms involved in LOP N-demethylation in human liver microsomes were estimated by applying relative activity factor (RAF) values. RESULTS: The formation rate of DLOP showed biphasic kinetics, suggesting the involvement of multiple P450 isoforms. Apparent Km and Vmax values were 21.1 microM and 122.3 pmol/min per milligram of protein for the high-affinity component and 83.9 microM and 412.0 pmol/min per milligram of protein for the low-affinity component, respectively. Of the cDNA-expressed P450 s tested, CYP2B6, CYP2C8, CYP2D6, and CYP3A4 catalyzed LOP N-demethylation. LOP N-demethylation was significantly inhibited when coincubated with quercetin (a CYP2C8 inhibitor) and ketoconazole (a CYP3A4 inhibitor) by 40 and 90%, respectively, but other chemical inhibitors tested showed weak or no significant inhibition. DLOP formation was highly correlated with CYP3A4-catalyzed midazolam 1-hydroxylation (rs=0.829; P<0.01), CYP2B6-catalzyed 7-ethoxy-4-trifluoromethylcoumarin O-deethylation (rs=0.691; P<0.05), and CYP2C8-catalyzed paclitaxel 6alpha-hydroxylation (rs=0.797; P<0.05). CONCLUSION: CYP2B6, CYP2C8, CYP2D6, and CYP3A4 catalyze LOP N-demethylation in human liver microsomes, and among them, CYP2C8 and CYP3A4 may play a crucial role in LOP metabolism at the therapeutic concentrations of LOP. Coadministration of these P450 inhibitors may cause drug interactions with LOP. However, the clinical significance of potential interaction of LOP metabolism by CYP2C8 and CYP3A4 inhibitors should be studied further.

Antidiarrheals↗
PubMed2005

Effects of berberine on the blood concentration of cyclosporin A in renal transplanted recipients: clinical and pharmacokinetic study.

OBJECTIVE: To study the effects of berberine (BBR) on the blood concentration and pharmacokinetics of cyclosporin A (CsA) in renal-transplant recipients. METHODS: In a randomized and controlled clinical trial, 52 renal-transplant recipients were treated with CsA and 0.2 g BBR three times daily for 3 months, while another 52 subjects received CsA without BBR co-administration. Blood trough concentration of CsA and biochemistry indexes for hepatic and renal functions were determined. For the pharmacokinetic study, six renal-transplant recipients were included with a 3-mg/kg dosage of CsA twice daily before and after oral co-administration of 0.2 g BBR three times daily for 12 days. RESULTS: The trough blood concentrations and the ratios of concentration/dose of CsA in the BBR-treated group increased by 88.9% and 98.4%, respectively, compared with those at baseline (P < 0.05). As for the BBR-free group, they rose by 64.5% and 69.4%, respectively, relative to those at baseline (P < 0.01). Nevertheless, the final blood concentrations and the ratios of concentration/dose of CsA in BBR-treated patients were still 29.3% and 27.8%, respectively, higher than those in BBR-free patients (P < 0.05). No significant effects on liver or renal functions were observed under coadministration of BBR. After co-administration of BBR in six patients for 12 days, the mean AUC of CsA was increased by 34.5% (P < 0.05). The mean time taken to reach the peak blood concentration (t(max)) and the mean half-life (t(1/2)) of CsA were increased by 1.7 h and 2.7 h, respectively (P < 0.05). The average percentage increases in the steady-state drug concentration (Css) and minimum blood concentration (Cmin) were 34.5% and 88.3%, respectively (P < 0.05). In addition, the average percentage decrease in CL/F was 40.4% (P < 0.05) and the peak-to-through fluctuation index was significantly reduced (P < 0.01). CONCLUSION: The BBR can markedly elevate the blood concentration of CsA in renal-transplant recipients in both clinical and pharmacokinetic studies. This combination may allow a reduction of the CsA dosage. The mechanism for this interaction is most likely explained by inhibition of CYP3A4 by BBR in the liver and/or small intestine.

Adult↗
PubMed2002

Copper speciation and accumulation in the gill microenvironment of carp ( Cyprinus carpio) in the presence of kaolin particles.

Carp were exposed to copper adsorbed on kaolin particles at various concentrations (0-2.4 mg/L), and net accumulation due to elevated adsorbed copper in the surrounding water was observed. Copper speciation in the water and fish gill microenvironment was modeled in the presence and absence of kaolin using a chemical speciation program (MINTEQA2). The adsorption affinity constants of kaolin for copper at various pH values used in the speciation calculations were experimentally determined, and the quantitative relationship between the affinity constant and pH was modeled. Copper accumulations in fish gills exposed to kaolin-adsorbed copper was then observed. The results indicate that desorption occurred in the fish gill microenvironment due to both mucus competition of copper and slight increase in water pH. Furthermore, the available copper species increased as a result of desorption, causing a net accumulation of Cu by the gills.

Adsorption↗
PubMed1998

Pouchitis: risk factors, etiology, and treatment.

A Medline literature review of pouchitis has been conducted, and relevant information from this search and the authors' own experience has been used to produce an overview on pouchitis at the current time. Particular attention is given to etiology, pathophysiology, and clinical management.

Antidiarrheals↗
PubMed2005

American ginseng berry extract and ginsenoside Re attenuate cisplatin-induced kaolin intake in rats.

PURPOSE: Cisplatin, a chemotherapeutic agent, causes significant nausea and vomiting. It is postulated that cisplatin-induced oxidant stress may be responsible for these symptoms. We tested whether pretreatment with American ginseng berry extract (AGBE), an herb with potent antioxidant capacity, and one of its active antioxidant constituents, ginsenoside Re, could counter cisplatin-induced emesis using a rat pica model. METHODS: In rats, exposure to emetic stimuli such as cisplatin causes significant kaolin intake, a phenomenon called pica. We therefore measured cisplatin-induced kaolin intake as an indicator of the emetic response. Rats were pretreated with vehicle, AGBE (dose range 50-150 mg/kg, IP) or ginsenoside Re (2 and 5 mg/kg, IP). Rats were treated with cisplatin (3 mg/kg, IP) 30 min later. Kaolin intake, food intake, and body weight were measured every 24 h for 120 h. Additionally, the free radical scavenging activity of AGBE was measured in vitro using ESR spectroscopy. RESULTS: A significant dose-response relationship was observed between increasing doses of pretreatment with AGBE and reduction in cisplatin-induced pica. Kaolin intake was maximally attenuated by AGBE at a dose of 100 mg/kg. Food intake also improved significantly at this dose (P<0.05). Pretreatment with ginsenoside Re (5 mg/kg) also decreased kaolin intake (P<0.05). In vitro studies demonstrated a concentration-response relationship between AGBE and its ability to scavenge superoxide and hydroxyl radicals. CONCLUSION: Pretreatment with AGBE and its major constituent, Re, attenuated cisplatin-induced pica, and demonstrated potential for the treatment of chemotherapy-induced nausea and vomiting. Significant recovery of food intake further strengthens the conclusion that AGBE may exert an antinausea/antiemetic effect.

Animals↗
PubMed2006

Optimal antidiarrhea treatment for antitumor agent irinotecan hydrochloride (CPT-11)-induced delayed diarrhea.

PURPOSE: An antitumor camptothecin derivative CPT-11 has proven a broad spectrum of solid tumor malignancy, but its severe diarrhea has often limited its more widespread use. We have demonstrated from a rat model that intestinal beta-glucuronidase may play a key role in the development of CPT-11-induced delayed diarrhea by the deconjugation of the luminal SN-38 glucuronide, and the elimination of the intestinal microflora by antibiotics or dosing of TJ-14, a Kampo medicine that contains beta-glucuronidase inhibitor baicalin, exerted a protective effect. In the present study, we assessed the efficacy of several potential treatments in our rat model to clarify which is the most promising treatment for CPT-11-induced delayed diarrhea. METHODS AND RESULTS: Oral dosing (twice daily from days -1 to 4) of streptomycin 20 mg/kg and penicillin 10 mg/kg (Str/Pen), neomycin 20 mg/kg and bacitracin 10 mg/kg (Neo/Bac), both of which inhibited almost completely the fecal beta-glucuronidase activity, or TJ-14 1,000 mg/kg improved the decrease in body weight and the delayed diarrhea symptoms induced by CPT-11 (60 mg/kg i.v. from days 1 to 4) to a similar extent. The efficacy was less but significant in activated charcoal (1,000 mg/kg p.o. twice daily from days -1 to 4). In a separate experiment using rats bearing breast cancer (Walker 256-TC), TJ-14, Neo/Bac, and charcoal at the same dose regimen improved CPT-11-induced intestinal toxicity without reducing CPT-11's antitumor activity. In contrast, oral dosing (twice a day) of cyclosporin A (50 mg/kg), a P-glycoprotein and cMOAT/MRP2 inhibitor or valproic acid (200 mg/kg), a UDP-glucuronosyltranferase inhibitor, exacerbated the intestinal toxicity without modifying CPT-11's antitumor activity. CONCLUSIONS: The result clearly demonstrated the ability of Neo/Bac, Str/Pen, and TJ-14, less but significant ability of activated charcoal, to ameliorate CPT-11-induced delayed-onset diarrhea, suggesting the treatments decreasing the exposure of the intestines to the luminal SN-38 are valuable for improvement of CPT-11-induced intestinal toxicity. In contrast, the treatments affecting the biliary excretion of CPT-11 and its metabolites might have undesirable results.

Animals↗
PubMed2006

Adsorption of irinotecan onto oral adsorbent AST-120 (Kremezin) for preventing delayed diarrhea.

PURPOSE: One of the significant dose-limiting toxicities of irinotecan hydrochloride (CPT-11) is severe diarrhea due to impairment of the intestinal membrane induced by the excreted CPT-11 and its metabolites. AST-120 (Kremezin) is a prominent oral adsorbent that consists of porous spherical carbonic particles. To evaluate whether Kremezin can prevent the diarrhea induced by CPT-11, we investigated the adsorption characteristics of CPT-11 and its metabolites onto Kremezin in vitro and in vivo. METHODS: For in vitro studies, Kremezin was added to each solution containing one of the camptothecin drugs (CPT-11, SN-38, and SN-38-glucuronide), and adsorption activities were determined under various conditions. For in vivo studies, CPT-11 was consecutively administered, and the occurrence of diarrhea was compared between Kremezin-treated and non-treated rats. RESULTS: Kremezin drastically adsorbed the camptothecin drugs in vitro, and the adsorption percentages of the camptothecin drugs for 60 min were more than 85%. In addition, the frequency of diarrhea in Kremezin-treated rats decreased by approximately half of that in the non-treated rats. CONCLUSION: Kremezin showed potent adsorption capacities for the camptothecin drugs and mitigated the symptoms of diarrhea in rats. These results suggest that Kremezin is useful to prevent the diarrhea in clinical CPT-11 chemotherapy.

Administration, Oral↗
PubMed2000

[Imaging of orbital metastasis of small-intestine carcinoid by octreotide scintigraphy. A critical evaluation of the methodology].

BACKGROUND: An orbital carcinoid metastasis can be specifically imaged by octreotide scintigraphy. Orbital metastases of carcinoid tumors are rare. In the current literature only 27 cases have been published. CASE REPORT: We report on a 59 year-old woman who presented with diplopia 6 years after resection of a carcinoid tumor of the ileum. She also complained about flush and diarrhea. The diplopia was caused by limited extensibility of the right inferior muscle. Computed tomography with contrast revealed an enhancing tumor in the area of the right inferior rectus muscle, which appeared in the MRT as an isointense structure in the T1-weighted image. On staging, we found a contrast-enhancing nodular hepatic lesion. In octreotide scintigraphy, enhancement of the liver, thoracic and abdominal para-aortic lymph nodes and of the right inferior orbit was found. CONCLUSION: The survival times of patients with orbital metastasis of carcinoid tumors range between 7 months and 11 years. No specific treatment is available. Surgical excision is indicated for a symptomatic solitary metastasis. Octreotide is helpful in two ways: (1) as a radiolabeled tracer to detect extra-abdominal and extrahepatic secondary tumors; (2) as a treatment modality for flush and diarrhea, which is successful in over 60% of patients (life expectancy uninfluenced). Our patient is presently being treated with 200 micrograms of octreotide three times a day subcutaneously. Flush episodes and diarrhea have been reduced, but her ophthalmologic symptoms remain unchanged, and she has recently developed cardiac insufficiency.

Antidiarrheals↗
PubMed2001

Does loperamide affect motor activity after proctocolectomy and ileal pouch-anal anastomosis? An experimental study in dogs.

This study investigated the effect of loperamide on the motor function of small intestine and J-pouch. Proctocolectomy and ileal pouch-anal anastomosis were performed in four dogs. Motility was recorded by serosal electrodes and strain gauge transducers. The intestinal transit time was determined radiologically. Multiple measurements were performed before and during chronic administration of loperamide. This treatment led to a significant decrease in median stool frequency from 11 (10-13) to 9 stools/day (8-12) and a tendential increase in intestinal transit time from 60 (50-105) to 70 min (60-90). This was not accompanied by significant changes in fasted or postprandial motility. There were no significant differences in the characteristics of the migrating myoelectric complex or in the fed pattern, either in the small intestine or in the pouch. Loperamide thus does not significantly affect intestinal motility after ileal pouch-anal anastomosis. The reduction in stool frequency seems to be due to antisecretory effects in the first line.

Animals↗
PubMed2002

The hypocholesterolemic effect of lemon peels, lemon pectin, and the waste stream material of lemon peels in hybrid F1B hamsters.

BACKGROUND: We found in preliminary studies with hamsters that citrus peels have a cholesterol lowering effect comparable to that of pectin extracted from these peels. AIM OF THE STUDY: We wanted to examine whether the cholesterol lowering effect of the peels could be completely accounted for by the pectin in the peels. METHODS: We fed cholesterol enriched (0.1 %,w/w) semipurified diets containing 3% (w/w) of cellulose, lemon peels, lemon pectin, and the waste stream material of the lemon peels to hybrid F1B hamsters for a period of 8 weeks. The waste stream of the lemon peels is the left over after extraction of the lemon pectin. RESULTS: Feeding the semipurified diets resulted in an increase of plasma cholesterol levels in all the dietary groups after 2 and 4 weeks on the diets. Cholesterol concentrations in the cellulose fed hamsters continued to increase after 4 weeks on the diet, whereas cholesterol levels in the other groups had reached a plateau. As a consequence, the plasma cholesterol levels in the hamsters fed the peels (5.59 +/- 0.74 mmol/L, mean +/- SD, n = 14), pectin (5.19 +/- 0.48 mmol/L), or waste stream (5.53 +/- 0.94 mmol/L) were lower than those in the hamsters fed cellulose (6.71 +/- 1.52 mmol/L) after 8 weeks on the diets. Differences in total plasma cholesterol were reflected in differences in both VLDL and LDL cholesterol concentration, but this effect was more distinct for the VLDL. There was no effect of the type of fiber on HDL cholesterol levels. Liver cholesterol concentrations paralleled. the concentrations of plasma cholesterol and the liver cholesterol concentrations in the hamsters fed the peels (3.57+/- 1.01 micromol/g liver, mean +/- SD, n = 14), pectin (4.86 +/- 1.42), and the waste stream (4.96 +/- 1.89) were lower than those in the cellulose group (7.19 +/- 2.32). The hamsters fed the peels, pectin, or waste stream tended to have a higher excretion of fecal bile acids and neutral sterols then the cellulose fed hamsters. CONCLUSION: The results of this study suggest that lemon peels and the waste stream of the lemon peels are as effective in lowering plasma and liver cholesterol in hamsters as the pectin extracted from the peels and that also compounds other than pectin are probably responsible for the cholesterol lowering effect of the citrus peels.

Analysis of Variance↗