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At least 91 records · Page 5Linked to original sources
PubMed1978

Effects of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent on the cardiovascular and central nervous systems.

1-(2,6-Dimethylphenyl)-3-methylamidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride) has been reported to be a potent antidiarrheal agent in laboratory animals. This study defines its effects on the cardiovascular and central nervous systems. At doses greater than 1 mg/kg i.v., WHR-1142A reduced cardiac output in the anesthetized dog primarily by depressing heart rate; the blood pressure was slightly elevated due to an increase in peripheral resistance. WHR-1142A was effective in reverting ouabain-induced ventricular arrhythmias to a sinus rhythm. Unlike diphenoxylate, WHR-1142A did not potentiate the CNS depressant effects of hexobarbital or ethanol. WHR-1142A did not block pentetrazole-induced convulsions, electroshock seizures or amphetamine aggregate toxicity. At high doses WHR-1142A caused a general CNS depressant effect was not related to a neuroleptic- or barbiturate-like action.

Amidines↗
PubMed1978

Pharmacological properties of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent.

1-(2',6'-Dimethylphenyl)-3-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride), a potent, unique antidiarrheal agent, was tested for other pharmacological properties. It inhibited gastric acid secretion in both 4-h and 22-h pylorus-ligated rats and reduced mortality and gastric ulcer severity in the latter test. WHR-1142A also exhibited local anesthetic activity in the rabbit corneal reflex and guinea pig intradermal wheal tests and reverisbly blocked conduction in isolated frog nerves. Low doses of WHR-1142A increased plasma glucose concentration in fasted mice and rats and prolonged the hyperglycemia in response to a glucose meal. WHR-1142A showed mild diuretic activity but had no anti-inflammatory or antibacterial activity. The acute oral LD50 of WHR-1142A was 260 (208,328) mg/kg in male mice, 267 (212,336) mg/kg in male rats and 160 130,197) mg/kg in female rats.

Amidines↗
PubMed1983

Fatal interaction between thiamylal sodium and a proprietary antidiarrheal preparation in the dog.

A drug interaction involving thiamylal sodium and a proprietary antidiarrheal preparation caused fatal ventricular fibrillation in a dog. Trials involving 4 dogs were conducted to recreate the interaction, and 1 of the 4 dogs died after ventricular fibrillation developed. The nature of the interaction was hypothesized to be mediated through the anticholinergic drug diphemanil methylsulfate, producing an autonomic imbalance.

Anesthetics↗
PubMed1982

[Histological survey on the behaviour of antidiarrheal drugs under in vitro conditions (author's transl)].

The effect of four antidiarrheal drugs (China clay, bentonite, pectin, Kaoprompt H) on the epithelia of murine small intestine and colon was studied under in vitro conditions with histological techniques. In this experiment, the drugs coarsely coated the guts' surface without outlining details or protruding into clefts. The resistance of the layers to rinsing is slightly different. None of the substances was able to protrude between the microvilli. Best intrusion was shown by pectin. The transfer of the experimental results to in vivo conditions is discussed.

Animals↗
PubMed1982

[The behavior of antidiarrheal drugs in experiments].

Four antidiarrheal drugs (China clay, bentonite, pectin, Kaoprompt H) are fed to mice by a gastric probe. Eight hours later, samples are taken from small intestine and colon to study the behaviour of the drugs in the gut. Any interactions with the brushborder of the villi at best are possible in the case of pectin. The viscosities of the suspended drugs depending on selected steps of pH are tested. The results are supporting the histological findings. The mechanical effects which may be put on the gut by the drugs are discussed.

Animals↗
PubMed1976

Antidiarrheal agents in the treatment of acute diarrhea in children.

To evaluate the efficacy of antidiarrheal agents in the treatment of diarrheal illnesses, a study was conducted with children in Guatemala who had an acute diarrheal illness. Eighty patients, aged 3 to 11 years, were hospitalized and treated for two days with one of five agents: kaolin-pectin suspension concentrate (Kao-Con), kaolin suspension, pectin suspension, diphenoxylate-atropine liquid (Lomotil), or placebo. Although the patients receiving kaolin-pectin produced stools that tended to be more formed than those of the placebo-treated group patients, the study did not demonstrate any effect by any of the agents tested in influencing the frequency of bowel movement, the water content of the stools, or the weight of stools. Kaolin-pectin suspension and diphenoxylate-atropine liquid do not appear to be useful in the relief of acute nonspecific diarrhea in children.

Acute Disease↗
PubMed1995

Study of genotoxic effects of antidiarrheal medicinal herbs on human cells in vitro.

The use of medicinal herbs has been a common practice in Asia but their genotoxic properties are little known. In the present study, genotoxic effects of three antidiarrheal herbs, guava leaf, mangosteen peel and pomegranate peel, were examined using established human cell lines, Raji and P3HR-1. Cells were treated with boiled-water extract of the herbs at various concentrations for 24 and 48 hours in vitro. Cell growth and viability were dose dependently reduced. No apparent chromosomal aberrations were induced by the treatment. Administration of pomegranate extract induced apoptotic DNA fragmentation. This genotoxicity test system is simple and convenient for the primary screening.

Antidiarrheals↗
PubMed1993

Loperamide. Survey of studies on mechanism of its antidiarrheal activity.

In castor oil challenged rats, low doses of loperamide inhibit diarrhea and normalize intestinal propulsion. Unlike other opioids, loperamide is devoid of central opiate-like effects, including blockade of intestinal propulsion, up to the highest subtoxic oral dose. Nevertheless, the antidiarrheal action of loperamide can be considered to be mu-opiate receptor mediated, only a few in vitro effects at rather high concentrations being not naloxone-reversible. There is little evidence that interactions with intestinal opiate receptors directly change epithelial cell function. When secretory stimuli increase mucosal tension, however, loperamide may reverse the elevated hydrostatic tissue pressure that opposes normal absorption. This antisecretory effect at the mucosal level is accompanied by motor effects when loperamide reaches the myenteric mu-opiate receptors. At therapeutic doses for the treatment of acute diarrhea, it is likely that the mucosal effect prevails.

Animals↗
PubMed1993

Quantitative, noninvasive assessment of antidiarrheal actions of codeine using an experimental model of diarrhea in man.

Enteric coating of a capsule has been used to deliver a bolus of radioisotope to the ileocecal region. This has allowed quantitative assessment of regional colonic transit in a group of healthy subjects whose proximal colonic transit was accelerated by lactulose 20 ml thrice daily. In this experimental model of diarrhea, codeine delayed transit from mouth to terminal ileum and also delayed transit through the ascending colon from 5.3 +/- 2.5 hr to 7.4 +/- 2.5 hr, N = 11, P < 0.05. Furthermore, codeine delayed whole colon transit, as assessed by geometric center analysis, which showed the delay to be most marked in the right colon with little effect noted in the left colon. In addition, codeine significantly reduced the number of retrograde movements observed and reduced the colonic response to eating. The antidiarrheal effect of codeine appears to be due to a combination of delayed mouth-cecum transit plus an additional delay in the ascending colon. This colonic delay may be partially explained by a reduction in postprandial propulsive movements that were seen in this model of diarrhea.

Adult↗
PubMed1992

Antidiarrheal and colonic antipropulsive effects of spinal and supraspinal administration of the natural delta opioid receptor agonist, [D-Ala2]deltorphin II, in the rat.

The ability of the natural selective delta opioid receptor agonist, [D-Ala2]deltorphin II (DADELT II), to inhibit the diarrhea induced by castor oil and colonic glass bead expulsion, was studied in rats after supraspinal and spinal administration. When injected intracerebroventricularly, DADELT II (0.2, 1, 10 micrograms/rat) inhibited diarrhea and colonic bead expulsion in a dose-related fashion but did not affect the rate of small intestine transit. Similar results were obtained when the same dose of DADELT II was administered spinally. The antidiarrheal and colonic antipropulsive effects of supraspinally and spinally DADELT II were partially or completely antagonized by subcutaneous pretreatment with 1 and 10 mg/kg, respectively, of naltrindole, a selective delta opioid receptor antagonist. These findings indicate that, in the rat, supraspinal and spinal delta opioid receptors play a role in modulating diarrhea and colonic propulsion and that DADELT II is a useful tool for investigating the role of the delta opioid system in gastrointestinal function.

Animals↗
PubMed2003

Antidiarrheal activity of the methanol extract of Ludwigia hyssopifolia Linn.

Dried whole plant parts of Ludwigia hyssopifolia were subjected to successive cold extraction with n-hexane, ethylacetate and methanol. The methanol extract (LHM), obtained as 1% yield, showed significant antidiarrheal property by reducing diarrheal episodes in castor oil and serotonin induced diarrhea in laboratory mice at a dose of higher than 100 mg/kg body weight as compared to standard drug loperamide given at a dose of 66.67 microg/kg body weight. The percent reduction in diarrheal episode by 56.32 and 89.66 after castor oil challenge and 59.09 and 86.36 in serotonin induced diarrhea was observed at doses of 200 mg/kg and 400 mg/kg body weight of the extract respectively. The extract LHM was also found to reduce the gastrointestinal motility by 53.8% at a dose of 100 mg/kg body weight as compared to control, while no remarkable inhibition of gastrointestinal motility was seen at a dose of 50 mg/kg body weight of the extract.

Journal Article↗
PubMed1989

[Antidiarrheal and anti-inflammatory effects of berberine].

Berberine sulfate (Ber) 40 and 80 mg/kg ig reduced the purging effects of castor oil or Cassia angustifolia leaf in mice, but did not affect the gastrointestinal transport function of Chinese ink in normal mice. Ber 60 mg/kg ig significantly inhibited the increased vascular permeability induced by ip 0.7% acetic acid in mice. Ber 20 and 50 mg/kg sc markedly inhibited the increased vascular permeability induced by histamine 100 micrograms/0.1 ml ic in rats. Ber 4 and 8 mg/kg sc produced obvious inhibition in the xylene-induced swelling of mouse ear. The anti-inflammatory effects were enhanced in a dose-dependent manner. It is suggested that the antidiarrheal effect of Ber is relative to its restriction against exudative inflammation to a certain extent.

Animals↗
PubMed1976

Loperamide: a new antidiarrheal agent in the treatment of chronic diarrhea.

Twenty-seven patients with chronic diarrhea due to Crohn's disease, ulcerative colitis, short bowel syndrome, and idiopathic (functional) causes participated in a multiphase study (open, double blind, and long term open) of loperamide HCl, a new single entity, oral antidiarrheal agent. In the open phase of the study, loperamide effectively relieved symptoms of diarrhea in 21 of 27 patients. The average number of stools dropped from eight in the initial relapse period to two stools after 1 month of treatment (P = 0.0001). Efficacy was confirmed in the double blind and long term open phases of the study. Four patients who were not relieved while on therapy had discontinued the drug because of abdominal cramping. No other side effects attributable to the drug were observed. Loperamide has been found to be a safe and effective agent for the treatment of chronic diarrhea.

Adult↗
PubMed1978

Loperamide, a new antidiarrheal agent in the treatment of chronic diarrhea.

Loperamide is an effective and safe antidiarrheal agent which served as a very useful adjunct in the treatment in 79% of 47 patients with chronic diarrhea. One of the major advantages of loperamide to the patient with chronic diarrhea is its convenience. Usually, a single dose in the morning effectively controlled diarrhea during the day. Patients with nocturnal or early morning diarrhea obtained good control with a second bedtime dose of the drug.

Adult↗
PubMedDate not supplied

Antidiarrheal effects of dihydroergotamine.

Dihydroergotamine (DHE), an alpha-adrenergic blocking agent, rapidly improved 121 out of 123 diarrheal patients. A hypotonic sigmoid and a hyperreactive rectum were found in these patients. Manometric studies of the distal colon showed that DHE counteracts the rectal hyperactivity and increases sigmoidal tone. On the other hand, anticholinergic drugs and/or emotional stimuli accentuate the rectal hyperactivity of diarrheal patients. Both features could be due to an unbalanced neurologic control of the gastrointestinal tract with dominance of the alpha-adrenergic over the cholinergic activity. Diphenoxylate (DPO) suppressed the diarrhea in two patients not improved by DHE. Furthermore, DPO reinforced the therapeutic success of DHE in 11 lactose intolerance diarrheal patients, suggesting that the two drugs exert their effects by means of different mechanisms.

Adolescent↗