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At least 199 records · Page 11Linked to original sources
PubMed1986

Loperamide, an opiate analogue, inhibits plasma ACTH levels in patients with Addison's disease.

The effects of loperamide, an opiate analogue of the piperidine class on pituitary hormone secretion were evaluated in eight patients with Addison's disease. In all patients loperamide administration (16 mg orally) induced a marked fall in plasma ACTH levels (P less than 0.01), without affecting GH, PRL and LH levels. Plasma ACTH concentration fell significantly from 854 +/- 167 pg/ml (mean +/- SEM) to 460 +/- 123 pg/ml at 60 min (P less than 0.01). The inhibition persisted throughout the whole test period, the nadir being reached at 300 min. Low dose naloxone infusion 180 min after loperamide administration caused plasma ACTH to rise from 181 +/- 61 pg/ml to 539 +/- 99 pg/ml (P less than 0.01). The present data suggest that the opiate analogue loperamide is a potent inhibitor of ACTH secretion in patients with Addison's disease, which may be acting on mu receptors, since its effect is blocked by low doses of naloxone.

Addison Disease↗
PubMed1982

A double-blind crossover study of the effect of loperamide hydrochloride and codeine phosphate on ileostomy output.

Loperamide hydrochloride (4 mg t.d.s.) was compared with codeine phosphate (60 mg t.d.s.) in a double blind crossover study of patients with loose output from their ileostomies. Both drugs significantly decreased the daily output and water content of ileostomy fluid. Daily losses of sodium and potassium were less when the patients were treated with loperamide. Loperamide was also associated with less side effects. It is concluded that loperamide hydrochloride was more effective in the treatment of ileostomy diarrhoea than codeine phosphate. In this group of patients those with the highest outputs from their ileostomies benefited most from this treatment.

Adult↗
PubMed1985

A comparative trial of cholestyramine and loperamide for acute diarrhoea in infants treated as outpatients.

Infants aged 4 to 36 months with acute diarrhoea (rotavirus 66%) were treated as outpatients with oral fluids and a rapid return to full feedings. In addition, the infants were randomized to receive for 3 days either cholestyramine 2 g twice daily (N = 10), an equivalent placebo 2 g twice daily (N = 15), or loperamide 0.10 mg/kg divided in three doses (N = 16). The duration of watery diarrhoea from the beginning of treatment was 0.9 +/- 1.0 days in the cholestyramine group, 2.5 +/- 1.3 days in the loperamide group, and 3.3 +/- 1.6 days in the placebo group (p less than 0.001 cholestyramine vs. placebo, p less than 0.005 cholestyramine vs. loperamide). The infants receiving cholestyramine also had a better weight gain than those receiving the placebo, and their metabolic acidosis was corrected sooner. There was no hyperchloraemia associated with the cholestyramine treatment. It is concluded that cholestyramine 2 g twice daily for 3 days can be safely used to shorten the course of acute diarrhoea. The use of loperamide in acute infantile diarrhoea does not appear justified.

Acute Disease↗
PubMed1981

Influence of 1,8-dihydroxyanthraquinone and loperamide on the paracellular permeability across colonic mucosa.

Administration of 1,8-dihydroxyanthraquinone (DHA) markedly increases the permeability of guinea-pig colonic mucosa. In 1 h 25% of the administered dose of 99mTc-EDTA complex leaks through the mucosa. Orally administered loperamide blocks the 99mTc-EDTA transfer after DHA administration. Loperamide injected in situ in the ligated colon segment shows the same blocking properties of the transfer rate of the complex. These findings suggest that the opposing action on fluid transport of the laxative DHA and the antidiarrhoeal loperamide could be due to these drugs affecting the permeability of the colonic mucosa. The minimal dose of loperamide, able to restore normal permeability, was as low as 0.01 mg kg-1.

Animals↗
PubMed1992

Optimal dosing of trimethoprim-sulfamethoxazole when used with loperamide to treat traveler's diarrhea.

To explore the optimal dosing regimen for trimethoprim-sulfamethoxazole (TMP-SMX) when used in combination with loperamide to treat traveler's diarrhea, 190 U.S. adults with acute diarrhea were enrolled in a double-blind, randomized trial in Guadalajara, Mexico. All patients received loperamide (4-mg loading dose; 2 mg after each loose stool, not to exceed 16 mg/day for 3 days) and were randomized to receive a 3-day course of TMP-SMX (160:800 mg twice daily for six doses) (group A), a single large dose of TMP-SMX (320:1,600 mg) (group B), or a large loading dose (320:1,600 mg) followed by standard doses for 3 days (160:800 mg twice daily for five doses) (group C). Patients in group C responded best (P < 0.01), with 75% of subjects recovered from diarrhea in 12 h compared with 34 h (group A) and 33 h (group B). Similar differences in favor of group C were noted in the subset of patients who presented with moderate to severe diarrhea. On average, patients in group C took significantly (P < 0.05) less loperamide (1.2 mg) after the 4-mg loading dose compared with patients in group A (2.4 mg) or group B (2.0 mg). We conclude that the most efficacious treatment of traveler's diarrhea in the interior of Mexico is to take loperamide in usual doses to control symptoms in combination with a single large dose of TMP-SMX, which should then be continued for 3 days in standard doses.

Acute Disease↗
PubMed1982

Antidiarrhoeal activity of loperamide: studies of its influence on ion transport across rabbit ileal mucosa in vitro.

Loperamide is a well-established antidiarrhoeal agent with effects on gastrointestinal motility. We have now shown that the drug influences ion transport. In isolated rabbit ileal mucosa loperamide caused a dose-related fall in potential difference and short-circuit current and reduced the serosa to mucosa flux of chloride. The electrical effects were inhibited by naloxone (10(-6)M) suggesting that they were mediated by opiate receptors. Loperamide (10(-6)M) inhibited secretion provoked by heat stable and heat labile E. coli toxins and by prostaglandin E2. We conclude that loperamide is able to inhibit secretion mediated by cAMP or cGNP, and that this may be relevant to its antidiarrhoeal properties.

Animals↗
PubMed1985

Effect of loperamide and naloxone on mouth-to-caecum transit time evaluated by lactulose hydrogen breath test.

The effect of loperamide and naloxone on mouth-to-caecum transit time was evaluated by the lactulose hydrogen breath test in four men and four women. Each subject underwent tests during the administration of placebo, loperamide (12-16 mg po), naloxone (40 micrograms/kg/h by a three-hour intravenous infusion), and loperamide plus naloxone, carried out at intervals of one or two weeks. The transit time was significantly longer after loperamide, and this effect was antagonised by the concomitant administration of naloxone whereas naloxone administered alone had no effect on mean transit time. No clinically important side effects were reported.

Adult↗
PubMed2001

Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells.

Although opioid peptides are involved in the regulation of the hypothalamic-pituitary-adrenal axis, their role in pro-opiomelanocortin (POMC) gene expression at the pituitary level is not known. We therefore examined the effects of opioid receptor agonists, including recently discovered endogenous opioid peptides, on POMC gene expression using the AtT20PL cell line, a subclone of AtT20 in which the rat POMC 5'-promoter-luciferase fusion gene was stably incorporated. The endogenous mu-opioid receptor agonists endomorphin 1 and 2 had no effect on either basal or corticotropin-stimulating-hormone-induced POMC expression. This was also the case with the delta-agonist BUBUC, the kappa-agonist U50488H and the orphan receptor agonist orphanin FQ. In contrast, the synthetic mu-agonist loperamide significantly inhibited basal and yet enhanced cAMP-induced POMC expression. The inhibitory effect of loperamide was mimicked by the calmodulin antagonist W7 and antagonized by the calcium channel blocker nifedipine, whereas neither the inhibitory nor the enhancing effect of loperamide was influenced by the opioid antagonist naloxone. These results suggest that the synthetic mu-agonist loperamide has a modulatory effect on the 5'-promoter activity of the POMC gene. This effect does not seem to be mediated through the classical mu-opioid receptor but rather in part through a calcium/calmodulin-related mechanism.

Animals↗
PubMed2000

Comparison of the antidiarrheal effects of wood creosote and loperamide in the rat jejunum and colon in vitro.

Wood creosote, a mixture of guaiacol, creosol and related compounds, has long been used as an antidiarrheal agent. The goal of our study was to investigate the antisecretory effect of wood creosote and to compare it to the effect of loperamide, a synthetic opioid widely used in the treatment of diarrhea. Experiments were performed in rat jejunal and colonic mucosal sheets, mounted in modified Ussing chambers. Active electrogenic transport was monitored electrically as short circuit current (Isc) and hypersecretory responses were induced by acetylcholine (ACh). Neither loperamide nor wood creosote had any significant effect on basal lsc, when added to the serosal bathing solution at concentrations of 0.1-50microg/ml. In contrast, under hypersecretory conditions, both agents showed concentration-dependent (0.1--100microg/ml) antisecretory effects inhibiting ACh-induced responses in the jejunum and colon. However, the effects suggest regional differences, with loperamide being most potent in the jejunum, while wood creosote showed equal potency in both jejunum and colon. Based upon these in vitro findings, we conclude that like loperamide, the antidiarrheal action of wood creosote is due, at least in part, to its antisecretory activity.

Acetylcholine↗
PubMed1977

[Effects of loperamide on the gastric and intestinal motilities in the guinea pig and dog (author's transl)].

In anesthetized dogs, intravenous administration or intrajejunal infusion of Loperamide produced the excitatory effect of gastric, small and large bowel motilities accompanied with elevation of the muscle tone. The excitatory response was slightly suppressed by administration of atropine. Such effects were similar to those of morphine and methadone. In non-anesthetized spinal guinea pigs, Loperamide increased colonic motility accompanied with the augmentation of the colonic muscle tone, but the conduction of the contraction waves was prevented. In anesthetized guinea pigs, intravenous administration of Loperamide reduced the rate of the rhythmic contraction waves of the small intestine, but its effect on the muscle tone was not evident. The activity of Loperamide as an antidiarrheal agent was discussed.

Animals↗
PubMed1987

Loperamide in treatment of irritable bowel syndrome--a double-blind placebo controlled study.

The effects of loperamide in patients with IBS (all had diarrhoea as a main symptom) were studied in a double-blind placebo controlled trial. Subjective overall response stool consistency and six individual symptoms (urgency, pain, frequency, flatulence, borborygmi and painful propulsions) were studied over a 13 week long treatment period. Twenty-one patients out of 25 completed the trial, 11 in the loperamide group and 10 in the placebo group. A significant advantage for loperamide was found for stool consistency (p less than 0.001), pain (p less than 0.02) and urgency (p less than 0.05). Subjective overall response was also significantly better in the loperamide group (p less than 0.03). Self-titration of dose and administration in a single nightly dose was safe and efficient.

Adolescent↗
PubMed1987

Loperamide treatment of the irritable bowel syndrome.

The effect of loperamide was investigated in a double-blind, placebo-controlled study in 60 patients with irritable bowel syndrome (IBS). Active treatment was given in low dosage (4 mg nocte). The effect of treatment was assessed in clinical subgroups. In a group of patients with painless diarrhoea (n = 16) there was a highly significant improvement in stool frequency and consistency. In a group with alternating bowel habits and abdominal pain (n = 21) there was also a statistically significant improvement in stool frequency and consistency as well as significantly fewer painful days during loperamide treatment. Patients with alternating bowel habits and no pain (n = 12) experienced no symptomatic improvement, and patients with constipation (n = 9) generally felt worse on loperamide. No side effects were encountered. It is concluded that loperamide can be considered an alternative symptomatic treatment in some IBS patients whose main symptoms are painless diarrhoea or alternating bowel habits associated with abdominal pain.

Clinical Trials as Topic↗
PubMed1993

The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide.

The antidiarrhoeal properties of acetorphan, an inhibitor of enkephalinase (EC 3.4.24.11) that prevents endogenous enkephalin degradation, and loperamide, a mu opiate receptor agonist, were compared. The double-blind study included 69 patients with acute diarrhoea of presumed infectious origin, allocated at random to two parallel groups. Acetorphan and loperamide were both rapidly and similarly effective, diarrhoea resolving in both cases in nearly 2 days. With acetorphan, however, abdominal distension vanished significantly more rapidly, and reactive constipation was less frequent (8% versus 31% with loperamide). These differences can be accounted for by the distinct mechanisms of antidiarrhoeal activity of the two drugs--that is, primary antitransit effect for loperamide and antisecretory activity for acetorphan.

Acute Disease↗
PubMedDate not supplied

Potentiation of the antiproliferative activity of MKT-077 by loperamide, diltiazem and tamoxifen.

MKT-077, a delocalized lipophilic cation, selectively targets cancer cells. MKT-077 has been reported to inhibit the growth of several tumor types and has undergone phase I clinical testing. We have examined the effect of MKT-077, alone and in combination with the antidiarrheal drug loperamide. Ten human cancer cell lines, four prostate (PC3, DU145, LNCaP, MDA-PCA-2B), two breast (MCF-7 and MDA-MB-231) and four colon (LoVo, Colo320DM, SW1116 and LS174t) were tested in vitro. Cells were grown to confluency prior to treatment. Loperamide potentiated the antiproliferative effect of MKT-077 in all ten cell lines, in a dose-dependent manner. The sensitivity of MDA-PCA-2B cells, the two breast and four colon cancer cell lines to MKT-077 was relatively low (>2.5 microg/ml MKT-077 required to inhibit growth by 95%). In these cell lines, 0.5-5 microg/ml (1-10 microM) loperamide caused a marked increase in the response to MKT-077. Loperamide is known to activate micro-opioid receptors at nanomolar concentrations and block voltage-gated calcium channels at micromolar doses. We found that calcium channel-blockers diltiazem and nifedipine (10-20 microg/ml), as well as tamoxifen (1.5-2.5 microg/ml) can also potentiate the growth-inhibitory effects of MKT-077. These synergistic interactions could be exploited for therapeutic benefit.

Antidiarrheals↗
PubMed2003

Effect of loperamide on gastro-oesophageal reflux.

BACKGROUND: We have recently shown that morphine reduces gastro-oesophageal reflux (GOR) by stimulating opioid receptors. Our aim was therefore to investigate the effect of loperamide, a peripheral opioid agonist, on GOR. METHODS: Nine patients with GOR disease underwent two ambulatory 24-h intra-oesophageal pH monitoring sessions separated by a period of at least 7 days under double-blind randomized conditions during the administration of placebo or loperamide solution p.o. (8 mg + 4 mg + 4 mg, 12 h and 2 h before, and 7 h after the start of the recording). RESULTS: Twenty-four-hour oesophageal acid exposure and the number of reflux episodes/hour were similar under the two experimental conditions: a median (IQ range) of 6.2% (3.3%-11.0%) of the time at pH < 4 and 2.6 (1.6-3.5)/h during placebo versus 8.8% (3.7%-14.8%) and 2.8 (2.3-4.9)/h during loperamide (P = ns). Acid clearance time was also similar: 1.8 +/- 0.3 min versus 1.6 +/- 0.2 min (P = ns). CONCLUSIONS: Loperamide did not decrease GOR, thus suggesting that an opioid agonist may not be useful in the treatment of GOR disease.

Adult↗
PubMed1990

Autoradiographic demonstration of [3H] loperamide binding to opioid receptors in rat and human small intestine.

Loperamide has an anti-diarrhoeal action which has been suggested to be mediated by opioid receptors associated with gut motility. There is now evidence to suggest that loperamide also affects intestinal transport. In this study we have used in vitro autoradiography to localize [3H] loperamide binding sites in both rat and human small intestine and the displacement of [3H] loperamide binding by mu- and delta-selective ligands.

Animals↗
PubMed1990

Treatment of traveler's diarrhea with sulfamethoxazole and trimethoprim and loperamide.

In a randomized, double-blind, placebo-controlled trial, 227 US adults with acute diarrhea in Mexico received a single dose of sulfamethoxazole and trimethoprim (1600/320 mg) or 3 days of therapy with loperamide hydrochloride (4-mg loading dose, then 2 mg orally after each loose stool), sulfamethoxazole-trimethoprim (800/160 mg orally twice daily), or the combination of both. Subjects treated with the combination had the shortest average duration of diarrhea compared with the placebo group (1 hour vs 59 hours), took the least amount of loperamide after the loading dose (3.8 mg), and had the shortest duration of diarrhea associated with fecal leukocytes or blood-tinged stools (4.5 hours). A single dose of sulfamethoxazole-trimethoprim was also efficacious (28 vs 59 hours), but loperamide alone was significantly effective only when treatment failures were treated with antibiotics (33 vs 58 hours). The combination of sulfamethoxazole-trimethoprim plus loperamide can be highly recommended for the treatment of most patients with traveler's diarrhea.

Adult↗
PubMed1987

Loperamide--an opiate receptor agonist with gastrointestinal motility effects.

Loperamide is an opiate agonist, also exerting activity by inhibiting the action of calmodulin. The mode of action in the clinic is probably mainly due to its action on opiate receptors, since the effects of loperamide can be reversed by naloxone. The exclusive action in the gut is explained by the specific distribution of loperamide with extensive distribution to the gut and minimal influence on opiate receptors in CNS. Loperamide is well absorbed after oral administration and extensively metabolized. The pharmacokinetic properties are linear over a wide dose range.

Gastrointestinal Motility↗