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PubMed1978

Antimotility and antisecretory activity of some aryl substituted amidinoureas.

A number of aryl substituted amidinoureas have been prepared and examined for their gastrointestinal spasmolytic, antimotility, antidiarrheal and antisecretory effects. In general, antisecretory and antimotility effects have been found to be associated with each other in these compounds. The structure-activity relationships found show that substitution of the aromatic ring in positions other than 2 and 6 correlates poorly with potency, and potency of such compounds is low. In contrast to this, 2,6-disubstitution confers high potency. The potency of 2,6-disubstituted compounds declines sharply with increasing weight of substitution of the amidinourea chain, with the important exception of the N-alkoxyamidinoureas. Increasing the molecular weight of an N-alkoxy substituent has a much less profound effect than the corresponding increase has in an N-alkyl substituent. High potency in an amidinourea may well be related to low basicity (or a high pKa value for its conjugate salt) but there is insufficient data to support this hypothesis fully. The actual tautomeric structure of an amidinourea probably affects its potency and this is discussed briefly.

Amidines↗
PubMedDate not supplied

[Diet therapy of enteritis in children (experience in 929 cases)].

929 cases of acute enteritis are reviewed. They were admitted since 1972 to 1981 in the first Pediatric Department of Modena, and treated with dietetic therapy. The periods of stool normalisation according the treatment received are discussed (oral rehydrating therapy versus casein hydrolysate). The results are compared with the evolution of diarrhea in 322 children treated with antidiarrheal adsorbents. According to our experience the diet with casein hydrolysate results to be an effective therapy of acute diarrhea, affording a nearly complete reduction in the use of intravenous infusions.

Acute Disease↗
PubMed1982

Effect of berberine on intestinal secretion mediated by Escherichia coli heat-stable enterotoxin in jejunum of pigs.

Intraluminal perfusion with Escherichia coli heat-stable enterotoxin (ST) reversed water and electrolyte movements from net absorption to net secretion in porcine jejunal segments. Addition of berberine hydrochloride (3.2 X 10(-5) M) to the perfusate reduced the jejunal secretory response of water, sodium, potassium, and chloride to ST and enhanced water and electrolyte absorption in control segments. At lower concentrations (1.1 X 10(-5) M), berberine reduced the secretory response in ST-exposed segments, but only the decrease of sodium flux was significant. In the presence of berberine, the mucosal enzyme activities of adenosine triphosphatase and disaccharidases were not significantly different between control and ST-exposed segments. Doses of 1, 2, 3, 4, 5, and 10 mg of berberine were injected into ligated loops of proximal part of the jejunum with 1 ml of ST filtrate. At doses of 2 or more mg/loop, berberine was effective in reducing water and electrolyte secretions induced by ST; the effect was dose-dependent. These findings indicate that berberine may be an effective antidiarrheal agent in E coli heat-stable enterotoxin mediated secretory diarrhea and provide a basis for the frequent empirical use of berberine alkaloid and berberine-containing plants in gastroenteritis and infectious diarrhea in Asian and other countries.

Animals↗
PubMed1995

[Sandostatin in the treatment of diarrhea of different origins].

Antidiarrheal action of sandostatin (octreotide) was studied in dumping syndrome, diabetic enteropathy, short-bowel syndrome, Crohn's disease and ulcerative colitis. Sandostatin proved effective in diarrhea of secretory, motor and osmotic origin. Dumping syndrome, diabetic enteropathy, Crohn's disease and short-bowel syndrome responded completely. In ulcerative colitis the effect was paradoxical: intensive diarrhea discontinued, but moderate diarrhea became more intensive. Sandostatin indications in ulcerative colitis should receive further investigations.

Antidiarrheals↗
PubMed1995

[Effect of C-terminal derivatives of sorbin on duodenal ion transports in rats].

OBJECTIVES AND METHODS: Synthetic derivatives of sorbin have been shown to inhibit VIP stimulated fluxes in the ileum in decreasing plasma-to-mucosa Na and Cl effluxes. The effect of this group of new peptides, without homology with any known peptides, was determined in rat duodenum where ion transport mechanisms differ. The improved technique of ligated loops in situ, was used, permitting the simultaneous measurement of net fluxes, influxes and effluxes for Na and Cl, in an integrated in vivo model. To determine the minimal active fragment of sorbin, synthetic C5, C7 and C20 peptides were tested and compared with known anti-secretor drugs such as loperamide, neuropeptide Y, somatostatine and metenkephalinamide. RESULTS: C7-sorbin was the minimal peptide able to decrease duodenal VIP-stimulated fluxes of water, Na and bicarbonate. It intervenes in increasing Na influx and more slightly Cl influx, which have been decreased by VIP. It does not modify much Na and Cl effluxes stimulated by VIP. Sorbin effect is in contrast with those of known antidiarrheic agents like somatostatine, loperamide, NPY and metenkephalinamide which chiefly decrease Cl efflux. CONCLUSIONS: Sorbin acts like an activator of absorption in the duodenum, in contrast to the other peptides or drugs and to its own anti-secretor effect in the ileum.

Animals↗
PubMed1994

[Therapeutic guidelines in diarrhea].

In acute diarrhea water and electrolyte losses are compensated for by oral or intravenous rehydration. Oral rehydration solutions contain primarily glucose or glucose polymers and sodium as well as other electrolytes. In acute and chronic diarrhea, loperamide is the most potent and safe antidiarrheal drug. Antibiotics are used without hesitation only in invasive diarrhea. In chronic diarrhea, diagnostic work up must precede therapy. Potentially diarrheogenic drugs or foods have to be eliminated. In most cases, when the diagnosis has been established, specific therapeutic measures are available.

Acute Disease↗
PubMed1995

Attitudes of Bolivian pharmacists in dealing with diarrhea cases.

To help learn about the recommendations made by Bolivian pharmacists dealing with diarrhea cases, 498 pharmacies in three Bolivian cities (Cochabamba, El Alto, and La Paz) were visited by female interviewers who indicated they were seeking treatment for a child with diarrhea. Ninety-eight of the Cochabamba pharmacies were also visited by a male interviewer who indicated he was suffering from diarrhea and was seeking treatment. In response, fewer than 2% of the pharmacists recommended using oral rehydration salts (ORS), increasing fluid intake, or consulting a physician. Most recommended antimicrobials, antidiarrheals, or some combination of the two. At 329 (66%) of the pharmacies, oral rehydration salts were unavailable, and those that did have such salts rarely offered them to customers. At the time of the survey, pharmacists were not integrated into the Bolivian National Health Secretariat's training program for control of diarrheal diseases. Steps have since been taken to resolve this matter.

Adult↗
PubMed1996

Treatment of irritable bowel syndrome with Lacteol Fort: a randomized, double-blind, cross-over trial.

OBJECTIVE: To assess the efficacy of Lacteol Fort, an antidiarrheal drug, in patients suffering from the chronic intestinal disease known as irritable bowel syndrome (IBS). DESIGN: The randomized, double-blind, cross-over trial versus placebo was carried out from 1992 to 1994. This trial consisted of administering a 6-wk treatment with a first drug (Lacteol Fort or placebo), followed by a wash-out period of 2 wk, and then the administration of a second drug for a further 6 wk (placebo or Lacteol Fort). Among the 29 patients eligible after recruitment, 18 adults with well documented IBS fulfilled the inclusion criteria. Four patients were dropped for loss of materials used in the study and seven for lack of compliance. The patient's initial state was assessed using a questionnaire relating to six criteria: abdominal pain, bloating or gas, daily number of stools, consistency, mucus content, and general physical state. During the treatment, these criteria were evaluated daily by the patients themselves. RESULTS: All investigated criteria were scored, and then a daily mean index was calculated. The statistical analysis of the daily mean index values showed that the number of patients (nine cases) obtaining better results with Lacteol Fort than with placebo was statistically significant (p = 0.018). CONCLUSIONS: This double-blind, placebo-controlled, cross-over trial demonstrated that Lacteol Fort leads to a statistically significant therapeutic benefit in 50% of patients, when taking into consideration all of the six selected clinical criteria considered representative of IBS.

Adult↗
PubMed1977

[Acute gastroenteritis. Clinical evolution without use of antibiotics (author's transl)].

Authors present a prospective study upon 193 cases of acute gastroenteritis in infants 1 to 24 months of age, giving special attention to clinical evolution of the disease without any use of therapy of either antibiotics or other antidiarrheal agents. Data on epidemiology and etiology of this series are similar to those previously reported by other authors. Mean duration of diarrhea was 2,5 days, whereas mean hospital stay was 7,5 days. The number of cases of prolonged diarrhea was 13, from which six were cases of lactose intolerance, six were cases of cow's milk protein intolerance and one was a case of intractable diarrhea. The little use fulness of antibiotics in the treatment of acute diarrhea is commented and also a discussion is made of the different factors involved in the onset of the complications above mentioned.

Acute Disease↗
PubMed1997

Synthesis and pharmacological activity of 2-(substituted phenyl)-3-[2 or 3-[(4-substituted phenyl-4-hydroxy)piperidino]ethyl or propyl]-1,3-thiazolidin-4-ones.

A series of aryl-hydroxy-piperidinoalkyl-thiazolidinones was synthesized and evaluated to inhibit castor oil-induced diarrhea in mice. The dose dependent antidiarrheal activity of the most active compound 2-(p-nitrophenyl)-3-¿2-[(4-(p-chlorophenyl)-4-hydroxy)piperidino]ethyl]- 1, 3-thiazolidin-4-one (6) was counteracted by naloxone, resulting comparable with that of loperamide, a mu opiate agonist.

Animals↗
PubMed1990

Diabetic diarrhea. Pathophysiology, diagnosis, and management.

Idiopathic diarrhea is a common complication of diabetes mellitus. It occurs frequently, but not exclusively, in patients with poorly controlled insulin-dependent diabetes who also have evidence of diabetic peripheral and autonomic neuropathy. Associated steatorrhea is common and does not necessarily imply a concomitant gastrointestinal disease. The diarrhea is often intermittent; it may alternate with periods of normal bowel movements, or with constipation. It is typically painless, and occurs during the day as well as at night and may be associated with fecal incontinence. Multiple pathogenic mechanisms have been implicated, autonomic neuropathy, bacterial overgrowth, and pancreatic exocrine insufficiency being the most important underlying aberrations. However, diabetic diarrhea does not have a uniform and unequivocal pathogenesis. The diagnosis depends on a judicious clinical assessment accompanied by a stepwise laboratory evaluation, which allows the differentiation idiopathic diabetic diarrhea from the many other causes of diarrhea that can occur in diabetic and nondiabetic patients. The management can be difficult but many therapies, including antibiotics to eradicate bacterial overgrowth, as well as antidiarrheal agents, oral and topical clonidine, and somatostatin analogues may be effective in controlling diabetic diarrhea.

Diabetes Mellitus, Type 1↗
PubMed2007

Symptomatic overlap between irritable bowel syndrome and microscopic colitis.

BACKGROUND: Microscopic colitis is diagnosed on the basis of histologic criteria, and irritable bowel syndrome (IBS) is diagnosed by symptom-based criteria. There has been little investigation into the symptomatic overlap between these conditions. Our aim was to assess the prevalence of symptoms of irritable bowel syndrome in a population-based cohort of patients with microscopic colitis. METHODS: The Rochester Epidemiology Project (REP), a medical records linkage system providing all health care data for the defined population of Olmsted County, Minnesota, was used to identify all county residents with a diagnosis of microscopic colitis between 1985 and 2001. The medical records of these individuals were reviewed to ascertain symptoms consistent with Rome, Rome II, and Manning criteria for irritable bowel syndrome. RESULTS: One hundred thirty-one cases of microscopic colitis were identified. Median age at diagnosis was 68 years (range, 24-95); 71% were women. Sixty-nine (53%) and 73 (56%) met Rome and Rome II criteria for irritable bowel syndrome, respectively. Fifty-four (41%) had three or more Manning criteria. Forty-three (33%) had previously been diagnosed with irritable bowel syndrome. CONCLUSIONS: In this population-based cohort of histologically confirmed microscopic colitis, approximately one-half met symptom-based criteria for the diagnosis of irritable bowel syndrome. The clinical symptom-based criteria for irritable bowel syndrome are not specific enough to rule out the diagnosis of microscopic colitis. Therefore, patients with suspected diarrhea-predominant irritable bowel syndrome should undergo biopsies of the colon to investigate for possible microscopic colitis if symptoms are not well controlled by antidiarrheal therapy.

Adult↗
PubMed1979

Human pharmacokinetics and comparative bioavailability of loperamide hydrochloride.

A pharmacokinetic study of the antidiarrheal agent loperamide hydrochloride (Imodium) was conducted in six male subjects. The study utilized a random crossover design and employed a 2-mg capsule and a 0.2-mg/ml syrup formulation. Each treatment consisted of a single oral dose of 8 mg loperamide HCl followed by a two-week interval before the next treatment. Serum and urine samples obtained at various times after drug administration were assayed for loperamide using a radioimmunoassay specific for the drug. The mean biologic half-life, calculated from the elimination phase of the log serum concentration-versus-time data, was 10.8 +/- 0.6 hours for the overall study, 10.2 +/- 0.6 hours for the syrup formulation, and 11.2 +/- 0.8 hours for the capsules. The loperamide from the syrup was absorbed more rapidly than from the capsule formulation, with the peak serum levels observed at a mean time of 2.4 +/- 0.7 hours for the syrup and 5.2 +/- 0.3 hours for the capsule formulation. The relative areas under the serum loperamide concentration-versus-time curves suggested that the two formulations have comparable physiologic availability. The maximum observed serum concentrations were also similar, indicating the safety of the syrup formulation. Excretion of approximately 1 per cent of the dose in the urine as unchanged loperamide after seven days was observed independent of the particular dosage form that was administered.

Adult↗
PubMedDate not supplied

Discriminative stimulus properties of delta 9-tetrahydrocannabinol: mechanistic studies.

delta 9-Tetrahydrocannabinol (THC) produces a multiplicity of pharmacologic effects including analgesic, antiinflammatory, anticonvulsant, antidiarrheal, antiglaucoma, antihypertensive, and sedative effects. Efforts to elucidate the neurochemical systems mediating the THC effects have used these and related endpoints. However, animal models useful for evaluating the mechanisms by which THC produces its unique subjective effects have only recently been established. The use of drugs as discriminative stimuli provides a means for studying such mechanisms, since generalization data from this test closely correlate with subjective properties observed in clinical studies. The present study examined the ability of various drugs to mimic or block the cue produced by THC in rats. In animals trained to discriminate 3.2 mg/kg THC from vehicle, generalization occurred consistently with cannabinoids such as 11-OH-THC, HHC, and nabilone. Stereoselective generalization was also obtained with isomers of a potent analgesic, nantradol; potencies were consistent with results from other endpoints. In contrast, THC cueing was not produced by agents acting on adrenergic, cholinergic, serotonergic, GABAergic, or opiate systems. Similarly, a number of drugs previously reported to antagonize various nonunique effects of THC uniformly failed to block its subjective properties. These results indicate that the subjective properties of THC are mediated through as yet unidentified neurochemical systems.

Animals↗
PubMedDate not supplied

Effectiveness of nantradol in blocking narcotic withdrawal signs through nonnarcotic mechanisms.

Male rats were made narcotic dependent through continuous intravenous infusion of morphine. During withdrawal, nantradol, clonidine, and morphine were found to block withdrawal signs in a dose-dependent manner. Almost complete alleviation of withdrawal occurred with nantradol or clonidine at 0.16 mg/kg and with morphine at 40 mg/kg. The effectiveness of morphine, but not of nantradol or clonidine, was reversed by naloxone. Likewise, in naive rats given castor oil, naloxone did not block the antidiarrheal effect of nantradol or clonidine. In order to compare possible subjective effects of nantradol with other antiwithdrawal drugs, naive rats were trained to discriminate either morphine, cyclazocine, or clonidine from vehicle by selecting different levers for reinforcement. Nantradol failed to produce any generalization to morphine, cycloazocine, or clonidine, suggesting that this drug does not produce central subjective effects like those of the training drugs. In additional testing in behavioral experiments, nantradol failed to produce any sign of anxiogenic activity.

Animals↗
PubMed1975

In vitro adsorption of diphenoxylate hydrochloride on activated charcoal and its relationship to pharmacological effects of drug in vivo. I.

The adsorption of diphenoxylate hydrochloride, a potent antidiarrheal agent, on activated charcoal powder was studied in vitro. Langmuir adsorption isotherms were established at pH 4 and 7, and the maximum adsorption capacity of charcoal for this drug was estimated using these values. Activated charcoal modified the bioavailability of diphenoxylate hydrochloride in vivo. The antipropulsive action of diphenoxylate in the mouse was strongly inhibited in the presence of activated charcoal. A comparative evaluation of charcoal and chromium oxide used as inert, nonabsorbable markers revealed that chromium oxide may be the marker of choic in GI transit studies in laboratory animals since it does not influence the bioavailability of diphenoxylate hydrochloride.

Adsorption↗
PubMed1983

Carcinoma of the anal canal.

J.W. is a 68-year-old white female who noted an "anal growth" 1 year prior to admission. She also complained of bleeding from her rectum when she was constipated. She attributed these symptoms to hemorrhoids. She noted increasing pain and more bleeding 1 month prior to admission. Locally applied hemorrhoid remedies gave her no relief. She was then admitted to a hospital where a biopsy of the anal mass was performed, and then referred to Rush-Presbyterian-St. Luke's Medical Center. On physical examination the patient was noted to be obese. There was no inguinal lymphadenopathy. There were no abdominal masses or hepatosplenomegaly. Rectal examination revealed a 3 X 4 cm mass protruding from the anus. Examination and protoscopy done under anesthesia revealed this mass to be approximately 4 X 5 cm and arising from the proximal anal canal. The mass was freely moveable and bled spontaneously when manipulated. Pelvic examination revealed a normal uterus and adnexa with no obvious tumor involvement of the vagina. Proctoscopic examination revealed no tumor proximal to the lesion described. Further evaluation included a liver-spleen scan that was negative for metastatic disease and intravenous pyelogram that showed no lesions. A barium enema revealed only diverticula. A gallium scan showed marked uptake at the area of the anal tumor but no other lesions. The chest x-ray was within normal limits. A CT scan of the abdomen and pelvis revealed no masses or lymphadenopathy. The CEA was 1.3 ng/ml. The patient underwent concomitant radiation therapy and chemotherapy. Over a 4-week period the patient received 5000 rads to the anal region. In addition, during the first week of radiation therapy and the fourth week of radiation therapy, the patient received 5-fluorouracil, 800 mg/m2 by continuous infusion for 5 days. In addition, the patient received mitomycin C, 15 mg/m2 on the first day of the first week of chemotherapy and the first day of the last week of chemotherapy. During the treatment period, the patient had mild diarrhea, perineal desquamation, and mild ulceration at the site of the anal tumor. During the third week of treatment, the patient had a white blood cell count nadir of 2800 and a platelet count of 86,000 per cubic millimeter. Her symptoms were managed with local emolients and antidiarrheal medications.(ABSTRACT TRUNCATED AT 400 WORDS)

Aged↗