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Loperamide¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Loperamide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to NMDA receptors and to calmodulin.
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| Pharmacology |
Loperamide¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
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| Metabolism |
Loperamide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Loperamide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 97%
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| Half-life |
Loperamide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 9.1 to 14.4 hours (average 10.8 hours)
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| Absorption |
Loperamide¿¡ ´ëÇÑ Absorption Á¤º¸ Not significantly absorbed from the gut
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| Pharmacokinetics |
Loperamide HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : °æ±¸ : 1-3 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4 ½Ã°£
- Èí¼ö : °æ±¸ : 40 %
- ´Ü¹é°áÇÕ :97 %
- ´ë»ç : °£¿¡¼ ¹ÌȰ¼º ´ë»çü·Î ´ë»ç (Glucuronide)
- ¹Ý°¨±â : 7-15 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 5 ½Ã°£
- ¼Ò½Ç : ¹Ìº¯Èü(30-40 %)·Î ´¢ ¹× º¯À¸·Î ¹è¼³
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| Biotransformation |
Loperamide¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Loperamide¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
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| Drug Interactions |
Loperamide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Loperamide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals. Increase liquid intake.
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| Drug Target |
[Drug Target]
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| Description |
Berberine¿¡ ´ëÇÑ Description Á¤º¸ An alkaloid from Hydrastis canadensis L., Berberidaceae. It is also found in many other plants. It is relatively toxic parenterally, but has been used orally for various parasitic and fungal infections and as antidiarrheal. [PubChem]
Loperamide¿¡ ´ëÇÑ Description Á¤º¸ 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]
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| Dosage Form |
Loperamide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution OralTablet Oral
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| Drug Category |
Berberine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Not Available
Loperamide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antidiarrheals
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| Smiles String Canonical |
Berberine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=C2C=C3C4=CC5=C(OCO5)C=C4CC[N+]3=CC2=C1OC
Loperamide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1
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| Smiles String Isomeric |
Berberine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=C2C=C3C4=CC5=C(OCO5)C=C4CC[N+]3=CC2=C1OC
Loperamide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1
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| InChI Identifier |
Berberine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H18NO4/c1-22-17-4-3-12-7-16-14-9-19-18(24-11-25-19)8-13(14)5-6-21(16)10-15(12)20(17)23-2/h3-4,7-10H,5-6,11H2,1-2H3/q+1
Loperamide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C29H33ClN2O2/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23/h3-16,34H,17-22H2,1-2H3
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| Chemical IUPAC Name |
Berberine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 16,17-dimethoxy-5,7-dioxa-13$l^{5}-azapentacyclo[11.8.0.0^{2,10}.0^{4,8}.0^{15,20}]henicosa-1(21),2(10),3,8,13,15(20),16,18-octaen-13-ylium
Loperamide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-di(phenyl)butanamide
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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