Genomes and Genes
Summary: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
Publications230 found, 100 shown here
- Comparison of the peripheral and central effects of the opioid agonists loperamide and morphine in the formalin test in ratsHarlan E Shannon
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Neuropharmacology 42:253-61. 2002The effects of the peripherally restricted opioid agonist loperamide were compared to those of morphine in the formalin test in rats...
- Antidiarrhoeal activity of hot water extract of black tea (Camellia sinensis)S E Besra
Division of Pharmacology and Experimental Therapeutics, Indian Institute of Chemical Biology, 4 Raja S C Mullick Road, Calcutta 700032, India
Phytother Res 17:380-4. 2003..Naloxone (0.5 mg/kg i.p.) significantly inhibited the antidiarrhoeal activity of the extract as well as loperamide, thus indicating a role of the opioid system in the antidiarrhoeal activity of the extract.
- The effects of loperamide, or loperamide plus simethicone, on the distribution of gut water as assessed by MRI in a mannitol model of secretory diarrhoeaE Placidi
Sir Peter Mansfield Magnetic Resonance Centre, University of Nottingham, UK
Aliment Pharmacol Ther 36:64-73. 2012b>Loperamide (LOP) is an anti-diarrhoeal agent which is thought to act largely by slowing transit with an uncertain effect on the fluid content of the small and large bowel in humans...
- Control of irinotecan-induced diarrhea by octreotide after loperamide failureV Barbounis
2nd Department of Medical Oncology, St Saves Hospital, Athens, Greece
Support Care Cancer 9:258-60. 2001..Standard antidiarrheal treatment is based on high-dose loperamide, but this agent is associated with a significant failure rate...
- Hydrolysis of capecitabine to 5'-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamideS K Quinney
Department of Pharmacy Practice, Purdue University, Indianapolis, IN 46202, USA
J Pharmacol Exp Ther 313:1011-6. 2005..b>Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC(50) = 0.44 mM)...
- Urinary bladder relaxation through activation of opioid μ-receptors induced by loperamide is increased in diabetic ratsL M Lee
Department of Urology, College of Medicine, Taipei Medical University Wan Fang Hospital, Wang Fang, Taipei City, Taiwan
Exp Clin Endocrinol Diabetes 120:323-8. 2012..Thus, we used loperamide to activate opioid μ-receptors for urinary bladder relaxation and compared the differences between normal and ..
- Targeted nanoparticles that mimic immune cells in pain control inducing analgesic and anti-inflammatory actions: a potential novel treatment of acute and chronic pain conditionSusan Hua
University of Newcastle, Newcastle, Australia and The University of Queensland, Brisbane, Australia
Pain Physician 16:E199-216. 2013....
- Peripherally acting mu-opioid receptor agonist attenuates neuropathic pain in rats after L5 spinal nerve injuryYun Guan
Department of Anesthesiology and Critical Care Medicine, The Johns Hopkins University, 720 Rutland Avenue, Ross 350, Baltimore, MD 21205, USA
Pain 138:318-29. 2008..Systemic loperamide hydrochloride (0.3-10 mg/kg, s.c...
- Targeting the central nervous system: in vivo experiments with peptide-derivatized nanoparticles loaded with Loperamide and Rhodamine-123G Tosi
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Modena, Italy
J Control Release 122:1-9. 2007..In this research, g-7 Np were loaded with Loperamide in order to assess their ability as drug carriers for CNS, and with Rhodamine-123, in order to qualitatively ..
- P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamideWilliam C Kreisl
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
J Nucl Med 51:559-66. 2010..P-gp almost completely blocks brain entry of the PET radiotracer (11)C-N-desmethyl-loperamide ((11)C-dLop)...
- Relative contribution of peripheral versus central opioid receptors to antinociceptionDominika Labuz
Klinik fur Anaesthesiologie und operative Intensivmedizin, Charite Universitatsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 30, D 12200 Berlin, Germany
Brain Res 1160:30-8. 2007..population to antinociception elicited by systemically administered centrally penetrating opioids, and by loperamide (a peripherally restricted opioid). Nociception (abdominal writhes) was induced by intraperitoneally (i.p...
- Characterization of two models of drug-induced constipation in mice and evaluation of mustard oil in these modelsRyosuke Kojima
Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
Pharmacology 84:227-33. 2009Although it is known that both clonidine and loperamide cause delayed colonic transit in mice, these models of drug-induced experimental constipation have not yet been fully characterized...
- Guidelines for adults on self-medication for the treatment of acute diarrhoeaD Wingate
St Bartholomew s and the Royal London School of Medicine and Dentistry, Gastrointestinal Science Research Unit, London, UK
Aliment Pharmacol Ther 15:773-82. 2001..There is no evidence that it prolongs the illness. Self-medication in otherwise healthy adults is safe. Oral loperamide is the treatment of choice...
- Lactic acid fermentation of germinated barley fiber and proliferative function of colonic epithelial cells in loperamide-induced ratsJeong Ryae Jeon
Department of Food and Nutrition, Yeungnam University, Gyeongsan, Republic of Korea
J Med Food 13:950-60. 2010..The effect of GBFY on colonic epithelial proliferation was investigated through loperamide (LPM)-induced constipation in rats...
- Laxative activities of Mareya micrantha (Benth.) Müll. Arg. (Euphorbiaceae) leaf aqueous extract in ratsSouleymane Méité
Laboratoire de pharmacodynamie biochimique, UFR Biosciences, Université de Cocody Abidjan, 22 BP 582 Abidjan 22, Cote d Ivoire
BMC Complement Altern Med 10:7. 2010..The present study was carried out to investigate the laxative activity of Mareya micrantha in albino's Wistar rats...
- Administration of loperamide and addition of wheat bran to the diets of weaner pigs decrease the incidence of diarrhoea and enhance their gut maturationFrancesc Molist Gasa
Grup de Nutrició, Maneig i Benestar Animal, Departament de Ciencia Animal i dels Aliments, Universitat Autonoma de Barcelona, Bellaterra 08193, Barcelona, Spain
Br J Nutr 103:879-85. 2010..For these experiments, wheat bran (WB) was used as fibre source and loperamide as a drug (LOP) to increase the digesta transit time...
- Tariquidar, a selective P-glycoprotein inhibitor, does not potentiate loperamide's opioid brain effects in humans despite full inhibition of lymphocyte P-glycoproteinDaniel Kurnik
Division of Clinical Pharmacology, Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
Anesthesiology 109:1092-9. 2008b>Loperamide, a potent opioid, has been used as an in vivo probe to assess P-glycoprotein activity at the blood-brain barrier, because P-glycoprotein inhibition allows loperamide to cross the blood-brain barrier and exert its central opioid ..
- No effect of MDR1 C3435T variant on loperamide disposition and central nervous system effectsChristiane Pauli-Magnus
Department of Biopharmaceutical Sciences, University of California, San Francisco, CA 94143 0446, USA
Clin Pharmacol Ther 74:487-98. 2003..The aim of this study was to investigate the effect of this polymorphism on disposition and brain entry of the P-glycoprotein substrate loperamide.
- P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeysJeih San Liow
Molecular Imaging Branch, PET Department, Clinical Center, National Institutes of Health, Bethesda, Maryland 20892 2035, USA
J Nucl Med 50:108-15. 200911C-Loperamide is an avid substrate for P-glycoprotein (P-gp), but it is rapidly metabolized to 11C-N-desmethyl-loperamide (11C-dLop), which is also a substrate for P-gp and thereby contaminates the radioactive signal in the brain...
- Efficacy of methylcellulose and loperamide in managing fecal incontinenceEddie H M Sze
Department of Obstetrics, Gynecology, and Reproductive Sciences, Division of Urogynecology and Reconstructive Pelvic Surgery, Yale University School of Medicine, New Haven, CT 06520, USA
Acta Obstet Gynecol Scand 88:766-71. 2009To evaluate the efficacy of methylcellulose (Citrucel) and loperamide (Imodium) in managing fecal incontinence by comparing cure rates with expectant management.
- Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptorsAntonio Mazzella di Bosco
Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49 80131 Napoli, Italy
Chem Biol Drug Des 71:328-35. 2008b>Loperamide is a piperidine analogue, acting as agonist on peripheral opioid receptors, exhibiting affinity and selectivity for the cloned mu human opioid receptor compared with the delta human opioid receptor...
- Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in miceKoichi Tan-No
Department of Pharmacology, Tohoku Pharmaceutical University, 4 4 1 Komatsushima Aoba ku, Sendai 981 8558, Japan
Eur J Pharm Sci 20:357-63. 2003The inhibitory effect of repetitiously administered loperamide, a peripheral mu-opioid receptor agonist and well-recognized antidiarrheal agent, on mouse gastrointestinal transit was compared with that of morphine in order to examine the ..
- Liquid chromatography-tandem mass spectrometry for analysis of intestinal permeability of loperamide in physiological bufferMiriam S Rubelt
Department of Anesthesiology, Charite, Campus Benjamin Franklin, Berlin, Germany
PLoS ONE 7:e48502. 2012..we developed and validated a fast, sensitive and selective method based on LC-MS/MS for the determination of loperamide in HEPES-buffered Ringer's solution. Chromatographic separation was achieved with an Atlantis dC18 column, 2...
- Loperamide-induced rat prostate relaxation through activation of peripheral µ-opioid receptorsJuei Tang Cheng
Department of Medical Research, Chi Mei Medical Center, Yong Kang City, Tainan, Taiwan
Neurourol Urodyn 30:468-71. 2011The effect of µ-opioid receptor (MOR) agonist, loperamide on prostate relaxation and the role of potassium channel in this action were studied in isolated Wistar rat prostate.
- Effect of metoclopramide, bethanechol, and loperamide on gastric residence time, gastric emptying, and mouth-to-cecum transit timeM G Kirby
University of North Carolina School of Pharmacy, Chapel Hill
Pharmacotherapy 9:226-31. 1989The effects of metoclopramide, bethanechol, and loperamide on the gastric residence time (GRT), gastric emptying (GE), and mouth-to-cecum transit time (MCTT) of a solution were investigated in three separate studies of five healthy male ..
- Effects of surface modification of PLGA-PEG-PLGA nanoparticles on loperamide delivery efficiency across the blood-brain barrierYung Chu Chen
Tissue Regeneration Product Technology Division, Industrial Technology Research Institute, Hsinchu 31040, Taiwan
J Biomater Appl 27:909-22. 2013..The nanoparticle consisting of loperamide and poly(lactide-co-glycolide)-poly(ethylene glycol)-poly(lactide-co-glycolide) (PLGA-PEG-PLGA) triblock ..
- Optimization of the preparation of loperamide-loaded poly (L-lactide) nanoparticles by high pressure emulsification-solvent evaporationM Ueda
, , Frankfurt am Main, Germany
J Microencapsul 14:593-605. 1997The entrapment of loperamide hydrochloride (LPM) in biodegradable polymeric drug carriers such as nanoparticles might enable its passage across the blood-brain barrier...
- Influence of the preparation methods on the drug release behaviour of loperamide-loaded nanoparticlesM Ueda
, , Frankfurt Main, Germany
J Microencapsul 15:361-72. 1998Polylactide (PLA) or poly(lactide-coglycolide) (PLGA) nanoparticles containing loperamide (LPM) were prepared by an incorporation or adsorption method with the objective of developing nanoparticles with a rapid drug release...
- Phase behaviour analysis of solid dispersions of loperamide and two structurally related compounds with the polymers PVP-K30 and PVP-VA64Ilse Weuts
Laboratorium voor Farmacotechnologie en Biofarmacie, University of Leuven, Herestraat 49, B 3000 Leuven, Belgium
Eur J Pharm Sci 22:375-85. 2004..of the present study was to investigate the influence of the structure of a poorly water soluble model drug (loperamide) on the phase behaviour in solid dispersions with PVP-K30...
- Effects of Ficus carica paste on loperamide-induced constipation in ratsHak Yong Lee
BIOSOLOMON, Inc, Jeonju, Republic of Korea
Food Chem Toxicol 50:895-902. 2012Constipation is one of the most common gastrointestinal complaints worldwide. This study examined the effects of fig (Ficus carica L.) paste for the treatment of loperamide-induced constipation in a rat model.
- Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomesKyoung Ah Kim
Department of Pharmacology, Gil Medical Center, Gachon Medical School, 1198 Kuwol dong, 405 760, Incheon, Namdong gu, Korea
Eur J Clin Pharmacol 60:575-81. 2004The 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.
- Antinociceptive effect of intrathecal loperamide: role of mu-opioid receptor and calcium channelsRakesh Kumar
Department of Anatomy, All India Institute of Medical Sciences, Ansari Nagar, New Delhi 110029, India
Eur J Pharmacol 696:77-82. 2012..Peripherally administered loperamide lacks effect on the central nervous system as it is a substrate for the permeability glycoprotein (P-gp) efflux ..
- Effect of colic vein ligature in rats with loperamide-induced constipationFlavia Neri
Department of General Surgery and Transplantation, S Orsola Malpighi Hospital, University of Bologna, 40126 Bologna, Italy
J Biomed Biotechnol 2012:896162. 2012..Medical treatment in chronic constipation is not always successful. Surgery is indicated in unresponsive selected severe cases. This study presents the distal venous colic ligation in rat as a novel surgical approach...
- Study of the physicochemical properties and stability of solid dispersions of loperamide and PEG6000 prepared by spray dryingIlse Weuts
Laboratorium voor Farmacotechnologie en Biofarmacie, University of Leuven, Leuven, Belgium
Eur J Pharm Biopharm 59:119-26. 2005Solid dispersions of PEG6000 and loperamide-a poorly water-soluble agent-were prepared by spray drying. Their physicochemical properties were evaluated immediately after preparation...
- Fitting the elementary rate constants of the P-gp transporter network in the hMDR1-MDCK confluent cell monolayer using a particle swarm algorithmDeep Agnani
Department of Biology, Drexel University, Philadelphia, Pennsylvania, United States of America
PLoS ONE 6:e25086. 2011..Transport of a range of concentrations of amprenavir, loperamide, quinidine and digoxin across the confluent monolayer of cells was measured in both directions, apical to ..
- Novel pharmacological activity of loperamide and CP-339,818 on human HCN channels characterized with an automated electrophysiology assayYan T Lee
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, United States
Eur J Pharmacol 581:97-104. 2008..Two blockers known for their activity at opioid/Ca(2+) channels and K(+) channels, loperamide and CP-339,818 (respectively), are described to block HCN1 more potently than HCN4...
- Comparison of racecadotril and loperamide in adults with acute diarrhoeaJ M Vetel
Centre Hospitalier, Le Mans, Paris, France
Aliment Pharmacol Ther 13:21-6. 1999..was carried out to compare the efficacy, tolerability, and safety of racecadotril (100 mg three times daily) and loperamide (2 mg after each diarrhoeic stool) in 157 adults with acute diarrhoea...
- Loperamide, an FDA-approved antidiarrhea drug, effectively reverses the resistance of multidrug resistant MCF-7/MDR1 human breast cancer cells to doxorubicin-induced cytotoxicityYanfei Zhou
Department of Oral Pathology, Howard University, Washington, DC, USA
Cancer Invest 30:119-25. 2012b>Loperamide is an FDA-approved antidiarrhea drug which acts on the μ-opioid receptors in the mesenteric plexus of large intestine and exhibits limited side effects...
- N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrierPavitra Kannan
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
Drug Metab Dispos 38:917-22. 201011)C]N-desmethyl-Loperamide ([(11)C]dLop) is used in positron emission tomography (PET) to measure the in vivo activity of efflux transporters that block the passage of drugs across the blood-brain barrier...
- The role of loperamide in gastrointestinal disordersStephen B Hanauer
Section of Gastroenterology, Hepatology, and Nutrition, University of Chicago, Chicago, Illinois, USA
Rev Gastroenterol Disord 8:15-20. 2008b>Loperamide is an effective therapy for a variety of diarrheal syndromes, including acute, nonspecific (infectious) diarrhea; traveler's diarrhea; and chemotherapy-related and protease inhibitor?associated diarrhea...
- Analgesic action of loperamide, an opioid agonist, and its blocking action on voltage-dependent Ca2+ channelsKunie Hagiwara
Department of Molecular Pharmacology, Tohoku University Graduate School of Medicine, 2 1 Seiryomachi Aobaku, Sendai 980 8575, Japan
Neurosci Res 46:493-7. 2003We investigated the relationship between the antinociceptive effect of the opiate agonist loperamide at the spinal level and its inhibitory effect on calcium influx...
- Effects of loperamide on mechanical allodynia induced by herpes simplex virus type-1 in miceAtsushi Sasaki
Department of Applied Pharmacology, Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930 0194, Japan
J Pharmacol Sci 104:218-24. 2007In the present study, we investigated whether the peripherally acting micro-opioid receptor agonist loperamide would inhibit allodynia in the non-inflamed dermatome of mice with herpetic pain. Subcutaneous (s.c...
- Loperamide therapy for acute diarrhea in children: systematic review and meta-analysisSu Ting T Li
Department of Pediatrics, University of California Davis, Sacramento, California, United States of America
PLoS Med 4:e98. 2007b>Loperamide is widely used in adults for acute diarrhea. However, its use in children has been discouraged by the World Health Organization and the American Academy of Pediatrics owing to concerns over safety and efficacy in young children.
- Antihyperalgesic effects of loperamide in a model of rat neuropathic pain are mediated by peripheral delta-opioid receptorsKatsumi Shinoda
Pharmaceutical Research Center, Kyowa Hakko Kogyo Co, Ltd, 1188 Shimotogari, Nagaizumi cho, Sunto gun, Shizuoka ken 411 8731, Japan
Neurosci Lett 411:143-6. 2007The possible antihyperalgesic and antiallodynic activity of loperamide, an opioid agonist which does not readily penetrate the blood-brain barrier, were examined in the spinal nerve ligation model of experimental neuropathic pain...
- Potential roles of P-gp and calcium channels in loperamide and diphenoxylate transportAndrew Crowe
School of Pharmacy, Curtin University of Technology, GPO Box U1987, Perth, Western Australia, 6845, Australia
Toxicol Appl Pharmacol 193:127-37. 2003..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...
- The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood-brain barrierLieselotte Moerman
Laboratory of Radiopharmacy, Ghent University, B 9000 Ghent, Belgium
Nucl Med Biol 39:121-5. 2012..Thereby, this study investigated the influence of mass dose of laniquidar, desmethyl-loperamide and loperamide on the P-glycoprotein-mediated brain uptake of, respectively, [(11)C]-laniquidar and [(11)C]-N-..
- Determination of loperamide in mdr1a/1b knock-out mouse brain tissue using matrix-assisted laser desorption/ionization mass spectrometry and comparison with quantitative electrospray-triple quadrupole mass spectrometry analysisYoung G Shin
Department of Drug Metabolism and Pharmacokinetics, Genentech, South San Francisco, CA 94080, USA
Arch Pharm Res 34:1983-8. 2011..In this study, the quantitative determination of loperamide, an antidiarrheal agent and a P-glycoprotein substrate, in mdr1a/1b (-/-) mouse brain tissue sections using ..
- Competitive substrates for P-glycoprotein and organic anion protein transporters differentially reduce blood organ transport of fentanyl and loperamide: pharmacokinetics and pharmacodynamics in Sprague-Dawley ratsIman A Elkiweri
College of Nursing, King Saud Bin Abdulaziz University for Health Sciences, Jeddah, Saudi Arabia
Anesth Analg 108:149-59. 2009..We hypothesized that transport proteins P-gp and Oatp mediate opioid uptake in a drug and organ-specific manner, making them excellent potential targets for therapeutic intervention...
- A multinational comparison of racecadotril and loperamide in the treatment of acute watery diarrhoea in adultsD Prado
Hospital Centro Médico, Guatemala City, Guatemala
Scand J Gastroenterol 37:656-61. 2002..The aim of this study was to compare the efficacy, safety and tolerability of racecadotril with those of loperamide by assessing their effects on the resolution of the signs and symptoms of diarrhoea in patients in developing ..
- Racecadotril versus loperamide: antidiarrheal research revisitedS Huighebaert
Consultant Pharmaceutical Sciences, La Hulpe, Belgium
Dig Dis Sci 48:239-50. 2003..inhibitor, presented as a purely antisecretory agent with advantages over the opiate-receptor agonist loperamide in the treatment of diarrhea. A critical review of the literature and the models used was performed...
- Use of loperamide as a phenotypic probe of mdr1a status in CF-1 miceJ Cory Kalvass
Division of Drug Delivery and Disposition, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA
Pharm Res 21:1867-70. 2004..Mice lacking the mdr1a gene represent an important research tool to study the potential effects of P-gp on CNS substrate disposition...
- Effects of fasting on evaluation of gastrointestinal transit with charcoal mealS W Mittelstadt
Drug Safety Assessment, Procter and Gamble Pharmaceuticals, Miami Valley Innovation Center, Cincinnati, OH 45252, USA
J Pharmacol Toxicol Methods 52:154-8. 2005..The purpose of this study was to investigate the effects of food on the pharmacological effects on gastrointestinal transit...
- Loperamide-induced enhancement of moxidectin availability in cattleA Lifschitz
Laboratorio de Farmacologia, Departamento de Fisiopatologia, Facultad de Ciencias Veterinarias, Universidad Nacional del Centro, Tandil, Argentina
J Vet Pharmacol Ther 25:111-20. 2002..b>Loperamide (LPM) is an opioid derivative, whose main pharmacological action is to abolish intestinal propulsive peristaltic ..
- Local loperamide inhibits thermal hyperalgesia but not mechanical allodynia induced by intratibial inoculation of melanoma cells in miceVerdad Curto-Reyes
Laboratorio de Farmacologia, Facultad de Medicina, Instituto Universitario de Oncologia del Principado de Asturias IUOPA, Universidad de Oviedo, C Julian Claveria 6, 33006 Oviedo, Asturias, Spain
Cell Mol Neurobiol 28:981-90. 2008..Intraplantar administration of loperamide (15 microg, 30 min before) inhibited thermal hyperalgesia, but did not modify the intense mechanical allodynia...
- Agarwood induced laxative effects via acetylcholine receptors on loperamide-induced constipation in miceMamoru Kakino
Department of Biofunctional Evaluation, Molecular Pharmacology, Gifu Pharmaceutical University, Gifu, Japan
Biosci Biotechnol Biochem 74:1550-5. 2010..of EEAs (mangiferin, and genkwanin-5-O-primeveroside), and senna increased the frequency and weight of stools in loperamide-induced constipation model mice...
- pH dependent uptake of loperamide across the gastrointestinal tract: an in vitro studyAndrew Crowe
School of Pharmacy, Curtin University of Technology, Perth, Western Australia
Drug Dev Ind Pharm 30:449-59. 2004b>Loperamide is a peripherally acting antidiarrheal opioid with some affinity for P-glycoprotein (P-gp)...
- Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivityD L Dehaven-Hudkins
Adolor Corporation, Malvern, Pennsylvania, USA
J Pharmacol Exp Ther 289:494-502. 1999The antihyperalgesic properties of the opiate antidiarrheal agent loperamide (ADL 2-1294) were investigated in a variety of inflammatory pain models in rodents...
- Comparison of racecadotril and loperamide in children with acute diarrhoeaD Turck
Hopital Jeanne de Flandre, Lille, Paris, France
Aliment Pharmacol Ther 13:27-32. 1999..double-placebo study was carried out to compare the efficacy, tolerability, and safety of racecadotril and loperamide in children aged 2 to 10 years who were suffering from acute diarrhoea. Patients received racecadotril (1...
- Loperamide: a pharmacological reviewDaniel E Baker
College of Pharmacy, Washington State University Spokane, Spokane, Washington, USA
Rev Gastroenterol Disord 7:S11-8. 2007b>Loperamide is an antidiarrheal medication approved for the control of diarrhea symptoms and is available without a prescription...
- Direct inhibition of Ih by analgesic loperamide in rat DRG neuronsDmitry V Vasilyev
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
J Neurophysiol 97:3713-21. 2007..We found that the known analgesic loperamide inhibited I(h) channels in rat DRG neurons...
- Toxicological evaluation of aqueous extract of Aloe ferox Mill. in loperamide-induced constipated ratsO A Wintola
Department of Botany, University of Fort Hare, Alice, South Africa
Hum Exp Toxicol 30:425-31. 2011..mg/kg body weight for 7 days on the haematological parameters as well as liver and kidney function indices in loperamide-induced constipated rats. The extract did not cause any significant (p > 0...
- Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoproteinNicholas Seneca
National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
J Nucl Med 50:807-13. 2009..At the blood-brain barrier, P-gp blocks the entry of both loperamide and its metabolite, N-desmethyl-loperamide (N-dLop), and thereby prevents central opiate effects...
- Activation of opioid mu-receptors by loperamide to improve interleukin-6-induced inhibition of insulin signals in myoblast C2C12 cellsT F Tzeng
Department of Internal Medicine, Pao Chien Hospital, Ping Tung City, Taiwan, Republic of China
Diabetologia 48:1386-92. 2005..This study investigated the role of opioid mu-receptor activation in the improvement of insulin resistance...
- The steady-state Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant KmJoe Bentz
Department of Bioscience and Biotechnology, Drexel University, Philadelphia, Pennsylvania, 19104, USA
Pharm Res 22:1667-77. 2005....
- Kinetic identification of membrane transporters that assist P-glycoprotein-mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cellsPoulomi Acharya
Department of Bioscience and Biotechnology, Drexel University, 32nd and Chestnut Sts, Philadelphia, PA 19104, USA
Drug Metab Dispos 36:452-60. 2008..MDCKII-hMDR1 cells, we have determined the elementary rate constants for the P-gp efflux of amprenavir, digoxin, loperamide, and quinidine. For amprenavir and quinidine, transport was fitted with just P-gp and passive permeability...
- The effect of Aloe ferox Mill. in the treatment of loperamide-induced constipation in Wistar ratsOlubunmi A Wintola
Department of Botany, University of Fort Hare, Alice 5700, South Africa
BMC Gastroenterol 10:95. 2010..In this study, the efficacy of aqueous leaf extract of Aloe ferox Mill. was studied against loperamide-induced constipation in Wistar rats.
- Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp functionNeva Lazarova
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 1103, USA
J Med Chem 51:6034-43. 200811)C]Loperamide has been proposed for imaging P-glycoprotein (P-gp) function with positron emission tomography (PET), but its metabolism to [N-methyl-(11)C] N-desmethyl-loperamide ([(11)C]dLop; [(11)C]3) precludes quantification...
- Loperamide cause of prolonged urinary retention after acute gastroenteritisB Focarelli
Department of Paediatric Science, Urodynamic Laboratory, Catholic University Medical School, Rome, Italy
Eur Rev Med Pharmacol Sci 11:65-7. 2007Urinary retention is uncommon in children and only one case has been described in literature with loperamide treatment...
- Influence of senna, fibre, and fibre + senna on colonic transit in loperamide-induced constipationK Ewe
I Medizinische Klinik und Poliklinik, Johannes Gutenberg Universitat Mainz, FRG
Pharmacology 47:242-8. 1993..Twelve persons taking a normal diet received loperamide in a dose sufficient to double the individual transit time...
- [Ileus after the use of loperamide in a child with acute diarrhea]J Dudink
Leids Universitair Medisch Centrum, afd Kindergeneeskunde, Postbus 9600, 2300 RC Leiden
Ned Tijdschr Geneeskd 147:670-2. 2003..girl was diagnosed as having acute gastroenteritis with severe diarrhoea, for which she was prescribed a loperamide solution. Following this she developed paralytic ileus...
- Signals in the activation of opioid mu-receptors by loperamide to enhance glucose uptake into cultured C2C12 cellsI M Liu
The Department of Pharmacy, Tajen Institute of Technology, Yen Pou, Ping Tung Shien, Taiwan 90701, ROC
Horm Metab Res 36:210-4. 2004In an attempt to understand the signal pathways of opioid mu-receptors for glucose metabolism, we used loperamide to investigate the glucose uptake into the myoblast C2C12 cells...
- Loperamide increases glucose ultilization in streptozotocin-induced diabetic ratsT F Tzeng
Department of Internal Medicine, Pao Chien Hospital, Ping Tung City, Taiwan
Clin Exp Pharmacol Physiol 30:734-8. 20031. Loperamide has an ability to lower the plasma glucose concentration in streptozotocin (STZ)-induced diabetic rats...
- Analgesic effects of morphine and loperamide in the rat formalin test: interactions with NMDA receptor antagonistsNatalja Sevostianova
Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318 Frankfurt am Main, Germany
Eur J Pharmacol 525:83-90. 2005To reveal peripheral components of opiate analgesia, effects of loperamide, opioid agonist which does not penetrate the blood-brain barrier, were examined in formalin and acute thermal pain tests in comparison with morphine...
- Treatment of travelers' diarrhea: randomized trial comparing rifaximin, rifaximin plus loperamide, and loperamide aloneHerbert L DuPont
Center for Infectious Diseases, University of Texas School of Public Health, Houston, Texas, USA
Clin Gastroenterol Hepatol 5:451-6. 2007..This study evaluated the efficacy and safety of rifaximin-loperamide in the treatment of travelers' diarrhea.
- Fibre supplementation in addition to loperamide for faecal incontinence in adults: a randomized trialM Lauti
Department of Surgery, Dunedin School of Medicine, University of Otago, Dunedin, New Zealand
Colorectal Dis 10:553-62. 2008..Clinician opinion varies as to which initial approach is best. This study compared these treatments in routine clinical practice...
- Spinal antinociceptive action of loperamide is mediated by opioid receptors in the formalin test in ratsSubrata Basu Ray
Department of Anesthesiology, University of California San Diego, La Jolla, CA 92093 0818, USA
Neurosci Lett 448:260-2. 2008..Being hydrophilic in nature, morphine also spreads rostrally which leads to respiratory depression. Loperamide has been reported to produce antinociception after both intracisternal and intrathecal administration...
- Analgesic effects of loperamide in bone cancer pain in miceLuis Menéndez
Laboratorio de Farmacologia, Instituto Universitario de Oncologia del Principado de Asturias IUOPA, Facultad de Medicina, Universidad de Oviedo, C Julian Claveria 6, 33006 Oviedo, Asturias, Spain
Pharmacol Biochem Behav 81:114-21. 2005..Here, we initially describe that this osteosarcoma induces mechanical as well as thermal hyperalgesia. Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia ..
- Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoproteinChristoph Wandel
Division of Clinical Pharmacology, Vanderbilt University, Nashville, Tennessee, USA
Anesthesiology 96:913-20. 2002..cassette superfamily, is a major determinant of the pharmacokinetics and pharmacodynamics of the opioid loperamide, a well-recognized antidiarrheal agent...
- P-Glycoprotein (P-gp) expressed in a confluent monolayer of hMDR1-MDCKII cells has more than one efflux pathway with cooperative binding sitesPoulomi Acharya
Department of Bioscience and Biotechnology, Drexel University, Philadelphia, Pennsylvania 19104, USA
Biochemistry 45:15505-19. 2006..e., the inhibitor became effective. These data and their analysis show that the binding of these substrates must be cooperative, either positive or negative...
- Antiallodynic effects of loperamide and fentanyl against topical capsaicin-induced allodynia in unanesthetized primatesEduardo R Butelman
The Rockefeller University, Box 171, 1230 York Ave, New York, NY 10021, USA
J Pharmacol Exp Ther 311:155-63. 2004..g., on primary afferent neurons). These studies examined the ability of loperamide (0.1-1 mg/kg s.c...
- Loperamide toxicity in a collie with the MDR1 mutation associated with ivermectin sensitivityLaura L Sartor
Department of Medical Sciences, College of Veterinary Medicine, University of Wisconsin, Madison, WI, USA
J Vet Intern Med 18:117-8. 2004
- Effects of racecadotril and loperamide on bacterial proliferation and on the central nervous system of the newborn gnotobiotic pigletY Duval-Iflah
Institut National de la Recherche Agronomique, Unité d Ecologie et de Physiologie du Système Digestif, Centre de Recherche de Jouy, Jouy en Josas, France
Aliment Pharmacol Ther 13:9-14. 1999..of two drugs, an enkephalinase inhibitor (the antisecretory agent, racecadotril) and a mu-receptor agonist (loperamide), on intestinal growth of a bacterial nonpathogenic strain (Escherichia coli E 404) and on the central nervous ..
- Sulfated polysaccharides, but not cellulose, increase colonic mucus in rats with loperamide-induced constipationA Shimotoyodome
Biological Science Laboratories, Kao Corporation, Haga-gun, Tochigi, Japan
Dig Dis Sci 46:1482-9. 2001..the fecal excretion, epithelial mucin production, thickness of the mucous layer, and amount of luminal mucus in loperamide-administered rats. Sodium alginate, 5 mg/day, thickened the mucus layer at the fecal surface...
- A blind, randomized comparison of racecadotril and loperamide for stopping acute diarrhea in adultsHwang Huei Wang
Division of Gastroenterology, Department of Internal Medicine, China Medical University Hospital, 2 Yuh Der Road, Taichung, Taiwan, China
World J Gastroenterol 11:1540-3. 2005..b>Loperamide is an effective anti-diarrheal agent, but it usually induces constipation...
- Prospective randomized double-blind trial of racecadotril compared with loperamide in elderly people with gastroenteritis living in nursing homesLuca Gallelli
School of Medicine and Surgery, Department of Experimental and Clinical Medicine, University Magna Graecia of Catanzaro, Mater Domini University Hospital, Catanzaro, Italy
Eur J Clin Pharmacol 66:137-44. 2010Our aim was to compare the efficacy and tolerability of loperamide and racecadotril in elderly patients with acute diarrhea.
- Loperamide inhibits tachykinin NK3-receptor-triggered serotonin release without affecting NK2-receptor-triggered serotonin release from guinea pig colonic mucosaShu Ichi Kojima
Department of Pharmacology, Dokkyo University School of Medicine, Tochigi, Japan
J Pharmacol Sci 98:175-80. 2005The effect of loperamide on tachykinin NK(2)- and NK(3)-receptor-mediated 5-HT outflow from guinea pig colonic mucosa was investigated in vitro...
- The elementary mass action rate constants of P-gp transport for a confluent monolayer of MDCKII-hMDR1 cellsThuy Thanh Tran
Department of Bioscience and Biotechnology, Drexel University, Philadelphia, Pennsylvania 19104, USA
Biophys J 88:715-38. 2005..For three P-gp substrates (amprenavir, loperamide, and quinidine), we have successfully fitted the elementary rate constants, i.e...
- Substantial activity of budesonide in patients with irinotecan (CPT-11) and 5-fluorouracil induced diarrhea and failure of loperamide treatmentB H Lenfers
Department of Medicine Gastroenterology Medical Oncology Endocrinology, Staedtische Kliniken Dortmund, Germany
Ann Oncol 10:1251-3. 1999..Standard therapy consists of high-dose loperamide, but is associated with frequent failure. Other therapeutic regimens are still experimental...
- Randomized, double-blind, placebo-controlled clinical trial of loperamide plus simethicone versus loperamide alone and simethicone alone in the treatment of acute diarrhea with gas-related abdominal discomfortStephen B Hanauer
Section of Gastroenterology and Nutrition, University of Chicago, Chicago, IL 60637, USA
Curr Med Res Opin 23:1033-43. 2007To compare efficacy and tolerability of a loperamide/simethicone (LOP/SIM) combination product with that of loperamide (LOP) alone, simethicone (SIM) alone, and placebo (PBO) for acute nonspecific diarrhea with gas-related abdominal ..
- Traveler's diarrheaN N Ramzan
Division of Gastroenterology and Hepatology, Department of Medicine, Mayo Medical School, Scottsdale, Arizona, USA
Gastroenterol Clin North Am 30:665-78, viii. 2001..Treatment and prevention of this common problem is described in some detail. Finally, a practical and cost-effective approach to evaluating and treating a returning traveler is presented...
- Lethal gastroenteritis associated with clozapine and loperamideMarkku Eronen
Am J Psychiatry 160:2242-3. 2003
- Prevention and self-treatment of traveler's diarrheaDavid J Diemert
Human Hookworm Vaccine Initiative, Sabin Vaccine Institute, 1889 F St NW, Suite 200S, Washington, DC 20006, USA
Clin Microbiol Rev 19:583-94. 2006..In the future, vaccines-several of which are in the advanced stages of clinical testing-may be added to the list of prophylactic measures...
- Use of probiotics for prevention of radiation-induced diarrheaP Delia
Institute of Radiology, Oncologic Radiotherapy Unit, Azienda Ospedaliera Universitaria, Messina, Italy
World J Gastroenterol 13:912-5. 2007..To investigate the efficacy of a high-potency probiotic preparation on prevention of radiation-induced diarrhea in cancer patients...
- [Drug treatment of irritable bowel syndrome: an unmet need]Fermin Mearin
Instituto de Trastornos Funcionales y Motores Digestivos, Servicio de Aparato Digestivo, Centro Medico Teknon, Barcelona, Espana
Gastroenterol Hepatol 30:130-7. 2007
- Irritable bowel syndromeHoward R Mertz
Department of Medicine, Division of Gastroenterology, Vanderbilt University, Nashville, USA
N Engl J Med 349:2136-46. 2003
- Antidiarrhoeal activity of seed extract of Albizzia lebbeck BenthS E Besra
Division of Pharmacology and Experimental Therapeutics, Indian Institute of Chemical Biology, Calcutta 700 032, India
Phytother Res 16:529-33. 2002..The extract (2.5-5 mg/kg i.p.) potentiated the antidiarrhoeal activity of loperamide (1 mg/kg i.p.). Nalaxone (0.5 mg/kg i.p...
- Limited effects of beta-endorphin compared to loperamide or fentanyl in a neuroendocrine biomarker assay in non-human primatesEduardo R Butelman
Laboratory on the Biology of Addictive Diseases, The Rockefeller University, 1230 York Avenue, New York, NY 10065, USA
Psychoneuroendocrinology 33:292-304. 2008..32 mg/kg; i.v.) in gonadally intact male rhesus monkeys (n=4) to that of the peripherally selective mu-agonist loperamide (0.01-0.32 mg/kg; i.v.) and the centrally penetrating mu-agonist fentanyl (0.0056-0.018 mg/kg; i.v.)...
- Treatment of diarrhea in patients with inflammatory bowel disease: concepts and cautionsShamita B Shah
Section of Gastroenterology, Hepatology, and Nutrition, Department of Medicine, University of Chicago, Chicago, Illinois, USA
Rev Gastroenterol Disord 7:S3-10. 2007..Other medications, including loperamide, diphenoxylate, codeine sulfate, and tinctures of opium, slow motility and increase the absorption of fluids and ..
- Inhibitory effects of ramosetron, a potent and selective 5-HT3-receptor antagonist, on conditioned fear stress-induced abnormal defecation and normal defecation in rats: comparative studies with antidiarrheal and spasmolytic agentsTakuya Hirata
Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
J Pharmacol Sci 106:264-70. 2008..defecation and normal (non-stressed) defecation in rats and compared ramosetron with the antidiarrheal agent loperamide and the spasmolytic agents trimebutine and tiquizium...
- Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in ratsTakuya Hirata
Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba, Ibaraki 305 8585, Japan
Eur J Pharmacol 587:281-4. 2008..of 5-HT(3) receptor antagonists including ramosetron, alosetron, and cilansetron, and the antidiarrheal agent loperamide, in this model...
- Efficacy of prophylactic anti-diarrhoeal treatment in patients receiving Campto for advanced colorectal cancerJ Duffour
Hopital La Timone, 264 rue St Pierre, Marseille, France
Anticancer Res 22:3727-31. 2002..In the case of severe diarrhoea, preventive treatment was replaced by loperamide(12 mg/d) and diosmectite (9 g/d). Grade 3 delayed diarrhoea occurred in 18% of patients (90% CI: [9.5-28...
- Injury-Induced Pain: Chemical Modulation of NociceptorsSrinivasa N Raja; Fiscal Year: 2013..Using the L5 spinal nerve ligation model in rodents, we found that loperamide, a peripherally acting opioid, alleviates behavioral signs of NP...
- Cannabinoid Mechanisms in Human Gastrointestinal Motor and Sensory FunctionsMICHAEL L CAMILLERI; Fiscal Year: 2010..These actions may be relevant to develop new treatments for IBS. The studies will also provide further understanding of the potential of medications like medical marijuana on stomach function that may be relevant to appetite control. ..
- ALPHA 2 ADRENERGIC CONTROL IN IRRITABLE BOWEL SYNDROMEMichael Camilleri; Fiscal Year: 2008..Significance: This project will characterize pharmacogenetic mechanisms determining the response to clonidine through studies of candidate genes that control alpha2-adrenoreceptor function and norepinephrine transport in IBS. ..
- ALPHA-2 ADRENERGIC CONTROL OF COLONIC FUNCTION IN IBSMichael Camilleri; Fiscal Year: 2007..abstract_text> ..
- Canine model for assessing CNS access P-gp substratesKATRINA MEALEY; Fiscal Year: 2005....
- NABTC CENTRAL OPERATION GRANT (UCSF PROJECT LEADER)Michael Prados; Fiscal Year: 2008..The NABTC will treat patients using novel therapeutic agents with the ultimate goal to increase quality, and hopefully, overall survival in this patient population. ..
- kappa-agonist effects of the hallucinogen Salvinorin AEduardo Butelman; Fiscal Year: 2008....
- Effect of ethanol on retinoid metabolism and signaling in zebrafish embryosWILLIAM BOSRON; Fiscal Year: 2007..We will assess the feasibility of performing targeted proteomics studies with tissues from other populations that express different SNPs in alcohol metabolizing enzymes. [unreadable] [unreadable] [unreadable]..
- Retinoid Metabolism in Hepatitic Stellate CellsWILLIAM BOSRON; Fiscal Year: 2005..Inhibitors of retinyl ester hydrolysis in stellate cells may be an effective therapeutic strategy for arresting stellate cell activation early in hepatic fibrosis. ..
- Colon Polyp Screening with Colonoscopy in WomenPhilip Schoenfeld; Fiscal Year: 2005..Ultimately, the proposed research studies, didactic coursework, and mentoring hopefully will lead to successful R01 applications. ..
- Multi-site Trial of Azathioprine Dosing in Crohn DiseaseStephen Hanauer; Fiscal Year: 2004..Predictive models will be performed to assess responsiveness based upon initial and inducible TPMT activity and achievable 6-TGN and 6-MMPR metabolite based upon incremental AZA dosing. ..
- Xenogen's IVIS 100 Imaging SystemMark Kieran; Fiscal Year: 2004..This luciferase-based technology affords a superior method to achieve this aim. ..
- Multi-site Trial of Azathioprine Dosing in Crohn DiseaseStephen Hanauer; Fiscal Year: 2003..Predictive models will be performed to assess responsiveness based upon initial and inducible TPMT activity and achievable 6-TGN and 6-MMPR metabolite based upon incremental AZA dosing. ..
- PEDIATRIC BRAIN TUMOR CLINICAL TRIAL CONSORTIUMMichael Prados; Fiscal Year: 2003..The aim of these treatment approaches is to increase disease-free and overall survival in children with brain tumors. ..
- HARVARD PEDIATRIC BRAIN TUMOR CENTERMark Kieran; Fiscal Year: 2003..David Louis). In summary, we will bring the full thrust of a Comprehensive Cancer Center and the full services of a pediatric center to enhance the Consortium and our mutual missions. ..
- CPT11 activation by carboxylesterases in colon cancerWILLIAM BOSRON; Fiscal Year: 2003..If there is a positive correlation, a future multi-institutional study will be proposed. ..
- EFFECTS OF SYSTEMICALLY ADMINISTERED DYNORPHINSEduardo Butelman; Fiscal Year: 2002....