Loperamide hydrochloride是阿片类受体激动剂,是长效止泻剂。
Loperamide HCl is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] DeHaven-Hudkins DL, et al. J Pharmacol Exp Ther,?999, 289(1), 494-502.
分子式 C29H34Cl2N2O2 |
分子量 513.5 |
CAS号 34552-83-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 22 mg/mL |
Water <1 mg/mL |
Ethanol 4 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00778115 | Healthy | Drug: Loperamide HCl 2 mg and simethicone 125 mg tablets | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2004-11-01 | 2008-10-22 | |
NCT02711891 | Pain | Drug: Loperamide|Drug: Drug, placebo gel | Rush University Medical Center | Early Phase 1 | 2015-03-01 | 2016-03-16 |
NCT00591357 | Antibiotic-Associated Diarrhea|Clostridium Difficile | Drug: loperamide|Drug: placebo | VA Medical Center, Houston | Phase 4 | 2007-10-01 | 2016-05-02 |
NCT02263365 | Dehydration, Diverting Ileostomy, Loperamide | Drug: Loperamide | Cedars-Sinai Medical Center | Phase 3 | 2014-10-01 | 2017-01-30 |
NCT02266849 | Rectal Cancer|Ulcerative Colitis|Short Bowel Syndrome | Drug: Loperamide|Drug: Placebo | Odense University Hospital | Phase 3 | 2014-10-01 | 2016-10-09 |
NCT00806299 | Drug Interaction | Drug: Loperamide / Red Grapefruit Juice|Drug: Loperamide/ White Grapefruit Juice|Drug: Loperamide / Pink Grapefruit Juice | Johnson & Johnson Consumer and Personal Products Worldwide | Phase 1 | 2008-11-01 | 2011-10-04 |
NCT02008565 | Fecal Incontinence | Drug: Loperamide|Drug: Placebo|Behavioral: Anal exercises with biofeedback|Behavioral: Usual Care | NICHD Pelvic Floor Disorders Network|The Cleveland Clinic|University of Alabama at Birmingham|University of California, San Diego|Duke University|National Institutes of Health (NIH)|University of New Mexico|Women and Infants Hospital of Rhode Island|RTI International|University of Pennsylvania|University of Pittsburgh|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) | Phase 3 | 2014-02-01 | 2016-08-12 |
NCT00359970 | Diarrhea | Drug: Azithromycin 500 mg|Drug: Azithromycin 1000 mg|Drug: Loperamide|Other: Placebo | The University of Texas Health Science Center, Houston | Phase 4 | 2002-06-01 | 2015-06-17 |
NCT02340481 | Diarrhea | Drug: Loperamide hydrochloride + simethicone chewable tablet|Drug: Loperamide hydrochloride|Drug: Loperamide hydrochloride + simethicone chewable placebo tablet|Drug: Loperamide hydrochloride placebo capsule | Xian-Janssen Pharmaceutical Ltd. | Phase 3 | 2005-07-01 | 2016-01-06 |
NCT00933465 | Fecal Incontinence | Drug: Imodium (Loperamide Hydrochloride) syrup|Drug: Imodium (Loperamide hydrochloride) tablets | University Hospital Southampton NHS Foundation Trust|University of Southampton | Phase 4 | 2009-10-01 | 2014-11-17 |
NCT00292344 | Travelers' Diarrhea | Drug: Rifaximin and loperamide | The University of Texas Health Science Center, Houston|Valeant Pharmaceuticals International, Inc. | Phase 4 | 2004-06-01 | 2009-04-17 |
NCT02400476 | Early Stage HER2+ Breast Cancer | Drug: Neratinib|Drug: Loperamide|Drug: Budesonide|Drug: Colestipol|Drug: Bismuth Subsalicylate or Mesalamine | Puma Biotechnology, Inc. | Phase 2 | 2015-02-01 | 2017-02-17 |
NCT00807326 | Diarrhea | Drug: Loperamide/simeticone 2 mg/125 mg caplets|Drug: Loperamide/simeticone 2 mg/125 mg chewable tablets|Drug: Probiotic Saccharomyces boulardii 250 mg capsules | McNeil AB|Johnson & Johnson Consumer and Personal Products Worldwide | Phase 4 | 2008-11-01 | 2012-07-06 |
NCT00685607 | Diarrhea | Drug: loperamide-simethicone|Drug: matching placebo | Johnson & Johnson Consumer and Personal Products Worldwide | Phase 4 | 2008-10-01 | 2011-10-04 |
NCT00003057 | Colorectal Cancer|Diarrhea | Drug: loperamide hydrochloride|Drug: octreotide acetate | Eastern Cooperative Oncology Group|National Cancer Institute (NCI)|Southwest Oncology Group|Cancer and Leukemia Group B | Phase 3 | 1996-11-01 | 2009-05-09 |
NCT02251119 | Healthy | Drug: Tipranavir|Drug: Ritonavir|Drug: Loperamide | Boehringer Ingelheim | Phase 1 | 2002-07-01 | 2014-09-25 |
NCT01596764 | Intestinal Obstruction | Drug: Loperamide placebo|Drug: Loperamide|Device: Colon Transit|Drug: Sulfasalazine|Drug: Placebo of MNTX and NLX|Drug: Naloxone|Drug: Methylnaltrexone | University Medicine Greifswald | Phase 1 | 2011-05-01 | 2012-05-09 |
NCT02217982 | Relapsing Remitting Multiple Sclerosis | Drug: Simethicone|Drug: Loperamide|Other: Peanut Butter | Rocky Mountain MS Research Group, LLC|Biogen | Phase 4 | 2014-07-01 | 2017-02-20 |
NCT01596777 | Intestinal Obstruction | Drug: Loperamide|Drug: Loperamide placebo|Drug: Methylnaltrexone placebo|Drug: Methylnaltrexone 12 mg sc.|Drug: Methylnaltrexone IR capsule|Drug: Methylnaltrexone ER capsule|Device: Colon Transit|Drug: Sulfasalazine | University Medicine Greifswald | Phase 1 | 2010-01-01 | 2016-10-25 |
NCT00444093 | Diarrhea|Enteritis|Cancer | Drug: Tinctura opii | Philipps University Marburg Medical Center|Maros Arzneimittel GmbH | Phase 3 | 2007-09-01 | 2007-08-31 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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