loperamide / Generic mfg. - LARVOL DELTA

Clinical, anatomic, and histologic determinants of gastrointestinal disease burden and survival in systemic AL amyloidosis: A cohort study of 560 patients (ASH 2025) - "Improvement was most often due to treatment of bacterial overgrowth(11/35 pts; 68%) and loperamide (54/59 pts; 91%).In AL, meaningful GI involvement is defined by nausea, diarrhea, occurrence of bleeding, andmalnutrition...In AL, meaningful GI involvement is defined by nausea, diarrhea, occurrence of bleeding, andmalnutrition. These are primarily associated with mucosal infiltration. GI symptoms can occur in the faceof autonomic involvement."

Clinical • Amyloidosis • Cachexia • Gastroenterology • Gastrointestinal Disorder

Multi-disciplinary combination to explore the laxation mechanism of Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex. (PubMed, Anal Biochem) - "This study revealed the synergistic effect of the combination of RR and MO in improving the constipation from the perspective of bioinformatics and metabolomics. Furthermore, the integrated method of multi-omics could contribute to exploring the potential compatibility mechanism of traditional Chinese medicines."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Metabolic Disorders • PACERR • PLA2G2A • PTGS2

Saccharomyces cerevisiae var. boulardii (HO12) Improves Loperamide-Induced Constipation in Rats via Modulation of Intestinal Neurotransmitters and SCFA Production. (PubMed, J Microbiol Biotechnol) - "In conclusion, our results demonstrate that HO12 alleviates loperamide-induced constipation by modulating intestinal neurotransmitters, enhancing intestinal motility, and increasing SCFA production. These findings suggest that S. boulardii HO12 has strong potential as a therapeutic probiotic for constipation management."

Journal • Preclinical • Constipation • Gastroenterology • Gastrointestinal Disorder

Butyrate prevents chemotherapy-induced gastrointestinal toxicity and microbial dysbiosis. (PubMed, Sci Rep) - "Loperamide reduced GI motility of irinotecan treated mice, however tolerance developed with chronic use, consistent with clinical findings of loperamide refractory diarrhea in patients. Irinotecan treatment produced a significant shift in the β diversity of the fecal microbiome that was mitigated by butyrate. The microbial dysbiosis was associated with increases in the mucin degrading bacteria Akkermansia muciniphilia and the hydrogen sulfide producing Desulfovibrio sp10575755 that was reduced with butyrate treatment."

Journal • Mucositis • Oncology

Preventive stRategy for IMMU132-relatED AEs in TNBC or Luminal Breast Cancer- PRIMED (clinicaltrials.gov) - P2 | N=50 | Completed | Sponsor: MedSIR | Active, not recruiting ➔ Completed

Trial completion • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Neutropenia • Oncology • Solid Tumor • Triple Negative Breast Cancer • ER • HER-2 • PGR

Loperamide-Induced Ventricular Arrhythmia and Seizures. (PubMed, JACC Case Rep) - "Although loperamide is an over-the-counter medication, life threatening cardiotoxicity and neurotoxicity can occur with high doses."

Journal • Cardiovascular • CNS Disorders • Epilepsy • Substance Abuse • Ventricular Tachycardia

Effectiveness of a 5-Hydroxytryptamine Type 3 Receptor Antagonist for Treating Nintedanib-Induced Diarrhea: A Prospective Observational Study. (PubMed, J Clin Med) - " Between October 2022 and March 2025, we enrolled patients with severe nintedanib-induced diarrhea that was uncontrolled by loperamide and/or probiotics. No prominent adverse events were associated with ramosetron administration. Ramosetron, a 5-HT3 antagonist, improved stool frequency and stool form in patients with severe nintedanib-induced diarrhea."

Journal • Observational data • Fibrosis • Gastrointestinal Disorder • Idiopathic Pulmonary Fibrosis • Immunology • Interstitial Lung Disease • Pulmonary Disease • Respiratory Diseases

Classifying Effluxable Versus Non-Effluxable Compounds Using a Permeability Threshold Based on Fundamental Energy Constraints. (PubMed, Pharmaceutics) - "Concentration-dependent measurements for Amprenavir, Eletriptan, Loperamide, and Quinidine-chosen because these borderline compounds exhibited the highest Pm×Cext while still being actively effluxed-enabled the most accurate determination of the threshold. In contrast, more than 60% of the compounds analyzed without significant ER values (123 compounds) fell above the threshold, in strong agreement with our theory of an energy limitation to active transport. This permeability threshold thus provides a simple and broadly applicable criterion to identify compounds for which active efflux is energetically not feasible and may serve as a practical tool for early drug discovery and optimization, pending further validation in practical applications."

Journal • ABCB1

Cistanche deserticola-derived exosome-like nanovesicles target the Microbiota-GABA signaling axis to ameliorate loperamide-induced constipation. (PubMed, Front Pharmacol) - "Crucially, the therapeutic effects of CELNs were entirely abolished by a GABAA R antagonist, confirming that their action is dependent on GABAA R signaling activation. In summary, our study reveals a novel mechanism through which CELNs enhance intestinal motility via the microbiota-metabolite-host axis, offering a conceptual foundation and a potential nanotherapeutic strategy for the targeted treatment of constipation by modulating microbial homeostasis."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder

Structural characterization of fructans from Polygonatum kingianum and their effects on LOP-induced constipation in mice. (PubMed, Carbohydr Polym) - "Pharmacological evaluation in a loperamide-induced murine constipation model demonstrated that PKF administration significantly alleviated constipation symptoms. Notably, PKF elicited comparable or superior therapeutic effects to the positive control lactulose (2.5 g/kg) at significantly lower doses (100-400 mg/kg). These findings establish a theoretical foundation for the potential applications of low molecular weight carbohydrate compounds derived from P. kingianum."

Journal • Preclinical • Constipation • Gastroenterology • Gastrointestinal Disorder • KIT

Marksans Pharma announced USFDA final approval of the Company's wholly owned subsidiary Marksans Pharma Inc.'s Abbreviated New Drug Application (ANDA) for Loperamide Hydrochloride Tablets USP, 2 mg (OTC) (Business Standard) - "This product is bioequivalent to the reference listed drug (RLD), Imodium A-D Tablets, 2mg, of Kenvue Brands LLC (Kenvue) NDA - 019860. Loperamide Hydrochloride is an anti-diarrheal medication used to control symptoms of acute and chronic diarrhea."

ANDA • Gastrointestinal Disorder

Kaempferol Ameliorates Functional Constipation in Mice by Regulating Autophagy of Interstitial Cells of Cajal via the p53/AMPK/mTOR Axis. (PubMed, Dig Dis Sci) - "Kaempferol ameliorates functional constipation by inhibiting excessive autophagy in ICCs via activation of the p53/AMPK/mTOR pathway, providing new insights into its mechanism and supporting its potential as a therapeutic agent for FC."

Journal • Preclinical • Constipation • Gastroenterology • Gastrointestinal Disorder • AMPK • BECN1 • KIT

Ganoderma lucidum dietary fiber and lactobacillus fermentum CECT5716 alleviate constipation via regulation of gut barrier and microbiota. (PubMed, Int J Biol Macromol) - "In this study, we investigated the effect of Ganoderma lucidum dietary fiber (GLDF) and Lactobacillus fermentum CECT5716 on ameliorating constipation induced by loperamide (LOP) and elucidated the underlying mechanism...Moreover, the GLDF and L. fermentum CECT5716 complex proficiently regulates gut microbiota while augmenting the generation of short-chain fatty acids (SCFAs)-with acetic acid, propionic acid, and butyric acid as the primary elevated metabolites. Our findings suggest that GLDF and L. fermentum CECT5716 mitigated constipation in mice, highlighting their potential as a combined functional food."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder

Polypharmacy Beyond Prescriptions: A Case of Acute Interstitial Nephritis and Hyponatremia Induced by a Spanish Herbal Supplement (KIDNEY WEEK 2025) - "She had recently taken a single dose of Trimethoprim-sulfamethoxazole and intermittently used azole antifungals, loperamide, and a Spanish supplement (Feminabiane CU Flash) marketed for urinary tract symptoms...She was started on prednisone 60 mg daily, with Trimethoprim-sulfamethoxazole and famotidine for prophylaxis...Greater awareness is needed to recognize supplements as a potential and underappreciated cause of AIN. Ingredients"

Clinical • Cardiovascular • CNS Disorders • Heart Failure • Huntington's Disease • Inflammation • Insomnia • Movement Disorders • Nephrology • Renal Disease • Sleep Disorder

Rectal Fidaxomicin as Salvage Therapy in Fulminant Clostridioides difficile Infection After Total Colectomy: A Case Report. (PubMed, HCA Healthc J Med) - "The 2021 guidelines from the Infectious Diseases Society of America (IDSA) and Society for Healthcare Epidemiology of America (SHEA) recommend vancomycin and metronidazole for fulminant CDI (FCDI), with consideration of rectal vancomycin for cases with ileus...Our case study involves a 79-year-old man with worsening symptoms post-amoxicillin/clavulanic acid use...He was eventually started on rectal fidaxomicin and loperamide, resulting in rapid improvement...In summary, this case underscores the complexity of FCDI management and highlights the potential of rectal fidaxomicin as a salvage therapy. Further research is warranted to elucidate its role in treating FCDI and incorporating it into clinical practice guidelines."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Septic Shock

Fluoxetine enhances the treatment of depression linked to opioid-induced constipation in mice by influencing the metabolomic profile. (PubMed, Neurosci Res) - "We established a mouse model of chronic unpredictable mild stress (CUMS) and used loperamide to induce constipation based on the CUMS mice, generating a mouse model of depression associated with OIC (CUMS+OIC). Through cluster analysis, we identified metabolites deregulated by CUMS+OIC and restored by Flx. Conclusively, Flx can improve the behavior and metabolic profile changes of CUMS associated with OIC, providing a basis for treating depression-related constipation."

Journal • Preclinical • CNS Disorders • Constipation • Depression • Gastroenterology • Gastrointestinal Disorder • Metabolic Disorders • Mood Disorders • Psychiatry

Resistance to thyroid hormone: clinical and biochemical paradox. (PubMed, BMJ Case Rep) - "Treatment included propranolol, amitriptyline, loperamide and vitamin D supplementation, resulting in symptomatic improvement. It also highlights the phenotypic variability of THRβ and the need for individualised management. Differential diagnoses like TSH-producing adenoma (TSHoma), laboratory assay interference and drug-induced thyroid dysfunction were ruled out."

Journal • Cardiovascular • Endocrine Disorders • Urinary Incontinence

Structural snapshots capture nucleotide release at the μ-opioid receptor. (PubMed, Nature) - "Naloxone stalls MOR in a 'latent' state, whereas loperamide promotes an 'engaged' state, which is structurally poised for opening of the AHD domain and subsequent GDP release. These findings, supported by molecular dynamics simulations, identify GDP-bound intermediates and AHD conformations as key determinants of nucleotide exchange rates, providing structural and mechanistic insights into G protein activation and ligand efficacy with broad implications for G protein-coupled receptor pharmacology."

Journal

Burst-patterned stimulation restores colonic motility in preclinical models. (PubMed, Sci Transl Med) - "We validated the optimized pattern of stimulation by measuring defecatory behavior in a loperamide model of constipation in rats...Further, we systematically varied stimulation frequency, stimulation duration, and interburst interval and determined the minimum effective parameters to maximize anorectal contractions. We demonstrated that a precise temporal pattern of sacral nerve stimulation relieves constipation in rats, establishing preclinical evidence and the foundational principles for translation to future pilot clinical trials."

Journal • Preclinical • Constipation • Gastroenterology • Gastrointestinal Disorder

Therapeutic effects of three-strain probiotic combination on slow transit constipation: mechanistic insights into MAPK signaling pathway and gut microbiota restoration. (PubMed, Front Pharmacol) - "In this study, we demonstrated that Golden Bifid alleviates loperamide-induced constipation by coordinately modulating host transcriptomic profiles, particularly the MAPK and serotonin signaling pathways, and restoring gut microbiota composition and diversity...Additionally, 16S rDNA sequencing demonstrated that the Golden Bifid partially restored gut microbiota structure, increased microbial diversity, and reversed the dysbiosis induced by LOP, notably reducing the abundance of Patescibacteria and modulating microbial taxa at both the phylum and genus levels to resemble the gut microbiota composition of the control group. These findings suggest that Golden Bifid alleviate STC by enhancing c-kit and 5-HT signaling, modulating the MAPK signaling pathway and pathway and restoring gut microbiota balance, offering promising therapeutic potential for STC treatment."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Oncology • KIT • TNFA

Effect of Levilactobacillus brevis KU15159 on Intestinal Function and Bowel Activity in Loperamide-Induced Constipation in Sprague-Dawley Rats. (PubMed, Prev Nutr Food Sci) - "The activities of intestinal harmful enzymes (β-glucosidase, nitroreductase, and β-glucuronidase) were also significantly inhibited in the L-KU15159 group (P<0.05). Therefore, L. brevis KU15159 can be considered a functional food that can improve intestinal function, defecation activity, and constipation through its antioxidant and anti-inflammatory effects."

Journal • Preclinical • Constipation • Gastroenterology • Gastrointestinal Disorder

The Hidden Villain: Chronic Diarrhea and Weight Loss Revealing Olmesartan Enteropathy (ACG 2025) - "Empiric trials of pancrelipase, cholestyramine, loperamide, and low-lactose diet failed to alleviate symptoms. Clinicians should maintain awareness of medication-induced enteropathies, particularly in elderly patients with unexplained malabsorptive symptoms and long-term ARB use. Abstract written with AI corrections.Figure: Villous atrophy seen during capsule endoscopy"

Cardiovascular • Celiac Disease • Gastrointestinal Disorder • Hypertension • Immunology • Infectious Disease • Novel Coronavirus Disease

Exacerbation of Microscopic Colitis Following Pancreatic Enzyme Replacement Therapy (PERT): A Case of Severe Diarrhea Leading to Hospitalization (ACG 2025) - "Symptoms were refractory to loperamide and diphenoxylate-atropine...Started on Budesonide 9 mg daily...Clinicians should consider MC in patients who develop worsening diarrhea after starting PERT and pursue colonoscopy with biopsies when appropriate. This case highlights the importance of a broad differential and cautious interpretation of fecal pancreatic testing."

Clinical • Cardiovascular • Colonic Polyps • Gastroenterology • Gastrointestinal Disorder • Hypertension • Immunology • GAST

Diarrhea with Depression: Sertraline-Induced Microscopic Colitis (ACG 2025) - "2 months ago, she had switched from duloxetine to sertraline 100mg for uncontrolled mood symptoms without psychiatric consultation...Per guidelines, sertraline was held, and budesonide, loperamide, cholestyramine, and dicyclomine were started. Symptoms resolved at 4 weeks.Since sertraline is a commonly used and well-tolerated first-line agent for mood disorders, clinicians should suspect MC in patients with chronic diarrhea after starting it. Discontinuation and close follow-up to monitor for relapses are key to management.Figure: Colonoscopy"

Chronic Obstructive Pulmonary Disease • CNS Disorders • Colonic Polyps • Depression • Fatigue • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Mood Disorders • Peptic Ulcer • Psychiatry • Respiratory Diseases

Immune Mediated Colitis With Visible Endoscopic Changes and Lymphocytic Histologic Changes: A Diagnostic Conundrum (ACG 2025) - "She reported onset of symptoms 3 weeks prior and described watery diarrhea 4 to 5 times per day despite taking loperamide...She was receiving carboplatin, paclitaxel, and pembrolizumab and last received pembrolizumab one and a half months ago; this regimen was initiated around 3 months prior to presentation...She noticed rapid improvement in her symptoms after budesonide initiation. Ultimately, this case is unique because there seems to be discordance in the diagnosis based on endoscopic and pathologic findings...The confounder in this scenario is the use of escitalopram, which is known to cause microscopic colitis. Therefore, this case presents unique endoscopic and pathologic findings incited by checkpoint inhibitor use or concomitant effects from both checkpoint inhibitor use and SSRI use. This case is important in the age of growing checkpoint inhibitor use for cancers and various presentations of immune mediated colitis with potential microscopic colitis..."

Breast Cancer • Gastroenterology • Gastrointestinal Disorder • Immunology • Solid Tumor