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Loperamide

产品号 DB00836 公司名称 DrugBank
CAS号 53179-11-6 公司网站 http://www.ualberta.ca/
分子式 C29H33ClN2O2 电 话 (780) 492-3111
分子量 477.03752 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 715

产品价格信息

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产品别名

标题
Loperamide
IUPAC标准名
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide
IUPAC传统名
loperamide
商标名
Imodium
Diarr-Eze
Apo-Loperamide
Loperacap
Imodium A-D
Imodium A-D Caplets
Ioperamide
Kaopectate II
Loperamida [INN-Spanish]
Loperamide HCL
Loperamidum [INN-Latin]
Maalox Anti-Diarrheal
Nu-Loperamide
PMS-Loperamide
Rho-Loperamide
Pepto Diarrhea Control

产品登记号

CAS号 53179-11-6
PubChem SID 46504591
PubChem CID 3955

产品性质

疏水性(logP) 5.5
溶解度 Slight

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description 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. [PubChem]
Indication For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease or gastroenteritis. Also used for reducing the volume of discharge from ileostomies.
Pharmacology Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.
Toxicity Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic
Absorption Not significantly absorbed from the gut
Half Life 9.1 to 14.4 hours (average 10.8 hours)
Protein Binding 97%
Elimination Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

参考文献