4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide
Loperamide
CAS: 53179-11-6
Molecular Formula: C29H33ClN2O2
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Names and Identifiers
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Physico-chemical Properties
| Molecular Formula | C29H33ClN2O2 |
| Molar Mass | 477.04 |
| Density | 1.187±0.06 g/cm3(Predicted) |
| Boling Point | 647.2±55.0 °C(Predicted) |
| pKa | pKa 8.66(H2O) (Uncertain) |
| Physical and Chemical Properties | Chemical properties of loperamide hydrochloride: C29H33ClN2O2? HCl. [34552-83-5]. Crystallization from isopropanol, melting point 222-223 °c. UV maximum absorption (0.1mol/L hydrochloric acid/2-propanol, 10ml/90 ml):253,259,265,273nm (φ532, 648,581,233). Solubility (g/100ml): Water (pH 1.7)0.14, citrate-phosphate (pH 6.1)0.008, citrate-phosphate (pH 7.9)<0.001, methanol 28.6, ethanol 5.37, 2-chemical book propanol 1.11, dichloromethane 35.1, acetone 0.20, ethyl acetate 0.035, diethyl ether <0.001, hexane <0.001, toluene 0.001, dimethylformamide 10.3, tetrahydrofuran 0.32, 4-methyl-2-pentanone 0.020, propylene glycol 5.64, polyethylene glycol 4001.40, dimethyl sulfoxide 20.5, 2-butanone 0.18. PKA 8.66. In the physiological pH range of a few insoluble in water (0.002%). Stable, under normal conditions can be stored for several years. Non-hygroscopic, not sensitive to light. Acute toxicity. Mice (mg/kg):75 subcutaneous injection; 105 oral. Acute toxicity LD50 rats (mg/kg):185 oral. |
| Use | The use of a strong long-acting anti-diarrhea drugs. Its chemical structure is similar to haloperidol and pethidine, but the therapeutic dose has no effect on the central nervous system. It is suitable for acute Diarrhea and chronic Diarrhea caused by various causes, such as ulcerative colitis, nonspecific colitis, irritable bowel syndrome and the treatment of chronic Diarrhea caused by partial gastrectomy and hyperthyroidism. |
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Adverse reactions of loperamide and rational drug use
from VIP Journal Professional Edition
Author:
Abstract:
The chemical structure of loperamide (loperamide, also known as chlorphenamide, bendosamine, epimine, Diarrhea pyridine) is similar to that of haloperidol and pethidine, but the therapeutic dose has no effect on the central nervous system ^[1]. Loperamide is a long-acting anti-Diarrhea drug that acts on opioid receptors in the intestinal wall, prevents the binding of naloxone and other ligands to opioid receptors, prevents the release of acetylcholine and prostaglandins, and thus inhibits intestinal peristalsis, prolong the passage time of the contents. It also increases the tone of the anal sphincter, thereby inhibiting fecal incontinence and urgency [2].
Key words:
loperamide rational drug use adverse reactions Central nervous system opioid receptor anal sphincter haloperidol Chemical Structure
cited:
year:
2009
Last Update：2024-01-02 23:10:35
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Effect of loperamide on expression of aquaporin-4 in Colon of Diarrhea model rats
from titanium academic
Author:
Abstract:
objective to detect the changes of aquaporin-4 (AQP4)mRNA expression in the colonic mucosa of Diarrhea model rats treated with loperamide, to investigate the molecular mechanism of loperamide in colonic water metabolism. Methods reverse transcription polymerase chain reaction (RT-PCR) was used to semi-quantitatively analyze the expression of AQP4 mRNA in ascending and descending colon mucosa cells of rats in loperamide treatment group, model control group and normal control group. Results ①the expression of AQP4 mRNA in ascending and descending colon in loperamide treatment group was higher than that in model control group and normal control group (P0.01). The expression of AQP4 mRNA in the ascending colon of the model control group was lower than that of the normal control group (P0.05), while there was no significant difference in the expression of the descending colon (P0.05). Conclusion loperamide can up-regulate the expression of AQP4 in the colonic mucosa of Diarrhea rats at the transcriptional level, and increase the absorption of water in the colon.
Key words:
loperamide Diarrhea aquaporin 4 colon
DOI:
10.3969/j.issn.1006-5709.2013.12.017
cited:
year:
2009
Last Update：2023-08-16 22:09:50
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Pediatric Loperamide Hydrochloride Granules and its preparation process
from Palm Bridge research
Application (patent) number:
CN201410828216.7
application date:
2014-12-25
Public/Announcement Number:
CN104546736A
Public/announcement date:
2015.04.29
applicant (patent):
Beijing Keyuan Chuanxin Technology Co., Ltd.
inventor:
National and provincial code:
CN110114
Abstract:
The invention belongs to the technical field of medicine, in particular to a pediatric loperamide hydrochloride granule and a preparation process. The invention adopts a new prescription process, which can effectively improve the dissolution rate and content uniformity of the product, and the product quality is obviously better than that of the foreign original research products, and is suitable for industrial production.
Last Update：2023-08-16 22:09:50
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-N,N-dimethyl-2,2-diphenyl-butanamide - Film preparation containing loperamide hydrochloride
from titanium academic
Application (patent) number:
CN200980133412.X
application date:
2009-08-25
Public/Announcement Number:
CN102131507A
Public/announcement date:
2011.07.20
applicant (patent):
Emergency Medicine Industry Corporation; Xinxing Corporation
inventor:
suicunu , shikawa , micaomin male
National and provincial code:
JP
Abstract:
The present invention provides a film preparation characterized in that, on both sides of a drug-containing intermediate layer containing loperamide hydrochloride, a terpene, and a film-forming agent, the laminate is provided with a coating layer containing a film-forming agent and a plasticizer (but without terpenes). Thus, since the bitter taste from loperamide hydrochloride is masked, the unpleasant feeling at the time of administration can be alleviated. In addition, since the film preparation can be rapidly dissolved only by the water in the oral cavity (rapid dissolution), the film preparation is quick in effect and excellent in portability.
Last Update：2023-08-16 22:09:50
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