Loperamide

한글명:Loperamide

카스 번호53179-11-6

상품명:Loperamide

CBNumberCB7402928

분자식C29H33ClN2O2

포뮬러 무게477.04

MOL 파일53179-11-6.mol

화학적 성질

끓는 점	647.2±55.0 °C(Predicted)
밀도	1.187±0.06 g/cm3(Predicted)
산도 계수 (pKa)	pKa 8.66(H2O) (Uncertain)
BCS Class	4
LogP	2.641 at 25℃ and pH6.95
CAS 데이터베이스	53179-11-6(CAS DataBase Reference)
NIST	Loperamide(53179-11-6)

위험 및 안전 성명

유해 물질 데이터

53179-11-6(Hazardous Substances Data)

그림문자(GHS)

Loperamide 화학적 특성, 용도, 생산

용도
Loperamide is presently used more often as an antidiarrheal drug than as an analgesic, and it is also included in the list of over-the-counter drugs because of its insignificant action on the CNS. It reduces intestinal smooth muscle tone and motility as a result of binding to intestinal opiate receptors. It is used for symptomatic treatment of severe and chronic diarrhea of various origins. The most popular synonym for loperamide is imodium.
정의
ChEBI: A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.
World Health Organization (WHO)
Loperamide, an inhibitor of intestinal peristalsis, was introduced in 1975 for the treatment of acute and chronic diarrhoea. In many countries its use was discouraged in young children. In late 1989, treatment of infants in Pakistan was associated with 19 cases of paralytic ileus, 6 of which have been fatal. This has subsequently led the major manufacturer to withdraw all drop formulations of the drug worldwide as well as the lower dose syrup forms from countries where there is a programme for the control of diarrhoeal diseases. The WHO Control of Diarrhoeal Diseases Programme recommends that loperamide should not be used in children below five year of age. (Reference: (LJJ) Letter to WHO from Johnson & Johnson, , , 21 June 1990)
일반 설명
Loperamide (Imodium) is a 4-phenylypiperidine with amethadone-like structure attached to the piperidine nitrogen. It acts as an antidiarrheal by directly binding tothe opiate receptors in the gut wall. Loperamide inhibitsacetylcholine and prostaglandin release, decreasing peristalsisand fluid secretion thus increasing the GI transit time andreducing the volume of fecal matter.Loperamide is sufficiently lipophilic to cross the blood-brain barrier, yet itdisplays no CNS-opioid effects. The reason for this is that itis actively pumped out of the brain via the P-glycoproteinpump (MDR1). Knockout mice with the P-glycoproteinpump genetically removed were given radiolabeled loperamideand sacrificed 4 hours later. The [³H]loperamideconcentrations were measured and compared with wild-typemice. A 13.5-fold increase in loperamide concentration wasfound in the brain of the knockouts. In addition, the micelacking the P-glycoprotein pump displayed pronouncedsigns of central opiate agonism. Loperamide is availableas 2-mg capsules for treatment of acute and chronic diarrhea.Recommended dosage is 4 mg initially, with 2 mgafter each loose stool for a maximum of 16 mg/d.

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