loperamide / Generic mfg. 
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  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  P2Y1 receptor in the colonic submucosa of rats and its association with opioid‑induced constipation. (Pubmed Central) -  Jan 7, 2023   
    The aim of the present study was to explore the expression changes of P2Y purinergic receptor 1 (P2Y1) in the distal colonic submucosa of opioid-induced constipation (OIC) rats and its association with the occurrence of OIC, an OIC rat model was generated by intraperitoneal injection of loperamide hydrochloride, a selective agonist of µ-opioid receptors (MORs)...GI transit ratio analysis suggested that the P2Y agonist ATP significantly relieved constipation symptoms in rats, while the P2Y inhibitor MRS2179 aggravated these symptoms. Finally, P2Y1 expression change was shown to be associated with the occurrence of OIC, while expression of MOR and P2Y1 was associated with OIC development in rats.
  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  Evaluations of the in vivo laxative effects of aqueous root extracts of Euclea racemosa L. in mice. (Pubmed Central) -  Jan 7, 2023   
    The plant extract also significantly accelerated the charcoal meal in gastrointestinal motility test of loperamide-constipated mice...The aqueous root extract of E. racemosa L. revealed the presence of terpenes, saponins, flavonoids and phenols when it was subjected to phytochemical screening. The investigation obtained from this study suggested that E. racemosa L. has a beneficial effect in producing laxative effect and this substantiate the traditional use of the plant for its claimed indication.
  • ||||||||||  pantoprazole / Generic mfg., loperamide / Generic mfg.
    UNUSUAL PRESENTATION OF MACROSCOPIC T WAVE ALTERNANS IN CIRRHOTIC PATIENTS (Poster Hall_Hall F) -  Jan 4, 2023 - Abstract #ACCWCC2023ACC_WCC_435;    
    Besides electrolyte metabolic abnormalities and impaired drug metabolism, patients with cirrhosis can have prolonged QT due to autonomic dysfunction and poorly understood cardiac ion channel remodeling. Initiation of TVP and chronotropic medications can shorten QT interval, likely preventing life threatening electrical storm.
  • ||||||||||  budesonide / Generic mfg., loperamide / Generic mfg.
    Journal:  Fecal calprotectin - a valuable predictor of microscopic colitis. (Pubmed Central) -  Jan 3, 2023   
    Measures to improve quality of life, should be of prime concern. In-depth research is required to better understand MC and to find better treatment options which can be used on a long-term basis, instead of anti-motility drugs which are able to control the acute episodes, but when discontinued result in an increased tendency to have relapses.
  • ||||||||||  verapamil / Generic mfg., loperamide / Generic mfg., papaverine / Generic mfg.
    PK/PD data, Preclinical, Journal:  The Detailed Pharmacodynamics of the Gut Relaxant Effect and GC-MS Analysis of the Grewia tenax Fruit Extract: In Vivo and Ex Vivo Approach. (Pubmed Central) -  Dec 24, 2022   
    In isolated rat ileum, G. tenax completely inhibited the carbamylcholine (CCh; 1 µM) and KCl (high K; 80 mM)-evoked spasms in a concentrations-mediated manner (0.03 to 3 mg/mL) by expressing equal potencies (p > 0.05) against both types of evoked spasms, similar to papaverine, having dual inhibitory actions at phosphodiesterase enzyme (PDE) and Ca channels (CCB)...Whereas, pre-incubating the tissue with 0.3 and 1 mg/mL of G. tenax established the CCB-like effect by non-specific inhibition of CaCl-mediated concentration-response curves towards the right with suppression of the maximum peaks, similar to verapamil, a standard CCB. Thus, the present investigation revealed the phytochemical constituents and explored the detailed pharmacodynamic basis for the curative use of G. tenax in diarrhea and hyperactive gut motility disorders.
  • ||||||||||  loperamide / Generic mfg.
    Review, Journal:  Risk of Cardiac Lesion with Chronic and Acute Use of Loperamide-An Integrative Review. (Pubmed Central) -  Dec 23, 2022   
    In addition, loperamide can inhibit voltage-gated sodium (Na) channels (Nav1.5), impairing electrical cardiac conduction and potentiating QRS interval widening. Therefore, QTc prolongation, torsades de pointes, and other ECG alterations are of particular concern regarding loperamide toxicity, particularly when overdosed.
  • ||||||||||  Irene (pyrotinib) / Jiangsu Hengrui Pharma
    Trial completion, Trial completion date, Trial primary completion date:  Effect of Montmorillonite Power or Loperamide on the Pharmacokinetics of Pyrotinib in Healthy Subjects (clinicaltrials.gov) -  Dec 23, 2022   
    P1,  N=36, Completed, 
    Therefore, QTc prolongation, torsades de pointes, and other ECG alterations are of particular concern regarding loperamide toxicity, particularly when overdosed. Not yet recruiting --> Completed | Trial completion date: Mar 2022 --> Aug 2022 | Trial primary completion date: Mar 2022 --> Aug 2022
  • ||||||||||  loperamide / Generic mfg.
    Journal:  Whipple's disease - A typical endoscopic finding of a rare disease. (Pubmed Central) -  Dec 2, 2022   
    Since the upper GI endoscopy and colonoscopy had no macroscopic abnormalities, the patient underwent a capsule endoscopy, which revealed continuous mucosal lesion with lymphangiectasia, oedema, villous atrophy and areas of denudation with hematinic punctate from the duodenum to the ileum. Diagnosis of Whipple's Disease was made with typical histology findings in duodenum material and a positive PCR for Tropheryma whipplei.
  • ||||||||||  Journal, PD(L)-1 Biomarker, IO biomarker:  Gastrointestinal toxicity of systemic oncology immunotherapy. (Pubmed Central) -  Nov 29, 2022   
    Prompt proper dia gnostics and immediate vigorous therapy infl uence the outcome of patients signifi cantly. A strictly individualized approach is indispensable.
  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  Anti-Diarrheal Activities of Hydromethanolic Crude Extract and Solvent Fractions of Acacia seyal (Fabaceae) Roots in Mice. (Pubmed Central) -  Nov 23, 2022   
    Group V mice (positive control) were given 3 mg/kg Loperamide for the castor oil-induced diarrhea and enteropooling test...Only at 400 mg/kg did the aqueous fraction statistically (P < 0.01) prolonged the onset of diarrhea and impeded gastrointestinal motility. According to this study, the hydromethanolic crude extract and solvent fractions of Acacia seyal roots have promising antidiarrheal effects.
  • ||||||||||  Cidine (cinitapride) / Almirall
    Journal:  CYP2C8*3 and *4 define CYP2C8 phenotype: An approach with the substrate cinitapride. (Pubmed Central) -  Nov 16, 2022   
    In this study, we properly characterized RMs, NMs, and IMs; however, additional studies are required to properly characterize UMs and PMs. These findings should be relevant with respect to cinitapride, but also to numerous CYP2C8 substrates such as imatinib, loperamide, montelukast, ibuprofen, paclitaxel, pioglitazone, repaglinide, or rosiglitazone.
  • ||||||||||  loperamide / Generic mfg.
    Journal:  Engineered 5-HT producing gut probiotic improves gastrointestinal motility and behavior disorder. (Pubmed Central) -  Nov 8, 2022   
    Then, we examined the effects of EcN-5-HT on intestinal motility in a loperamide-induced constipation mouse model...We also observed improved microbiota composition during EcN-5-HT treatment. This work suggests that gut microbiota-derived 5-HT might promise a potential therapeutic strategy for constipation and related behavioral disorders.
  • ||||||||||  fentanyl citrate / Generic mfg., loperamide / Generic mfg.
    Journal:  An Opioid Hiding in Plain Sight: Loperamide-Induced False-Positive Fentanyl and Buprenorphine Immunoassay Results. (Pubmed Central) -  Nov 2, 2022   
    Correlative studies, including measurement of circulating inflammatory cytokine levels and mutant allele burden are ongoing and will be presented. Laboratories using these assays should be aware of the potential for false-positive screening results due to the presence of high concentrations of loperamide and its metabolite dLop.
  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  Antidiarrheal Activity of Dialium guineense Willd Fruit Pulp in Wistar Rats. (Pubmed Central) -  Nov 2, 2022   
    The fruit pulp of D. guineense has showed antidiarrheal activities in Wistar rats by reducing the frequency of defecation, the amount of diarrheal fecal matter emitted as well as the water content. It also delayed the onset of diarrhea and significantly reduced the purging index like loperamide.
  • ||||||||||  loperamide / Generic mfg.
    Trial primary completion date:  4FMFES-PET Imaging of Endometrial and Ovarian Cancers (clinicaltrials.gov) -  Nov 1, 2022   
    P1/2,  N=72, Recruiting, 
    This study suggests the possibility that VP30-EPS can be applied to fermented and/or functional foods to relieve constipation. Trial primary completion date: Aug 2022 --> Aug 2023
  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  Effect and mechanism of functional compound fruit drink on gut microbiota in constipation mice. (Pubmed Central) -  Oct 26, 2022   
    Loperamide hydrochloride was used to establish a mouse model of constipation...Furthermore, CFD increased the abundance of potentially beneficial bacteria and reduced the number of potentially pathogenic bacteria. This study indicated that CFD was a promising functional drink for effectively relieving constipation.
  • ||||||||||  Trodelvy (sacituzumab govitecan-hziy) / Gilead
    Trial initiation date, Metastases:  Preventive stRategy for IMMU132-relatED AEs in TNBC - PRIMED (clinicaltrials.gov) -  Oct 21, 2022   
    P2,  N=50, Not yet recruiting, 
    Based on the above results, Li01 may have the potential to effectively alleviate constipation by regulating the 5-HT pathway and alteration of the gut microbiota. Initiation date: Oct 2022 --> Jan 2023
  • ||||||||||  loperamide / Generic mfg.
    Preclinical, Journal:  Evaluation of Anticolitis and Antioxidant Properties of Bixa orellana (Bixaceae) Leaf Hydroethanolic Extract on Acetic Acid-Induced Ulcerative Colitis in Rats. (Pubmed Central) -  Oct 11, 2022   
    The normal control group and the colitis control group received PO distilled water (10 mL/kg), the positive control received orally loperamide (5 mg/kg, and the 3 test groups received orally the hydroethanolic extract of Bixa orellana at 100, 200, and 400 mg/kg, respectively...Catalase and superoxide dismutase activity and glutathione concentrations all increased significantly (P < 0.01) in blood and colon in all extract-treated animals, whereas levels of malondialdehyde and nitric oxide were significantly decreased (P < 0.01) compared with the colitis control animals. The hydroethanolic extract of Bixa orellana leaves had protective effects against acetic acid-induced ulcerative colitis in rats that was associated with inhibited production of free radicals believed to be responsible for oxidative stress, hematological disorders, and tissue damage in this animal model.
  • ||||||||||  Journal, Adverse events:  Use of tracking drugs for the search of intra-hospital adverse reactions: a pharmacovigilance study. (Pubmed Central) -  Oct 9, 2022   
    The hydroethanolic extract of Bixa orellana leaves had protective effects against acetic acid-induced ulcerative colitis in rats that was associated with inhibited production of free radicals believed to be responsible for oxidative stress, hematological disorders, and tissue damage in this animal model. This study indicates that the use of trackers can be a tool to  estimate the occurrence of adverse drug reactions and to establish adverse  events related to the use of medications, which should be reported to the  pharmacovigilance service, with a view to patient safety.