Tìm theo
Diphenoxylate
Các tên gọi khác (8 ) :
  • 1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-isonipecotic acid ethyl ester
  • 2,2-Diphenyl-4-(4-carbethoxy-4-phenylpiperidino)butyronitrile
  • 4-Ethoxycarbonyl-alpha,alpha,4-triphenyl-1-piperidinebutyronitrile
  • Difenossilato
  • Difenoxilato
  • Diphenoxylatum
  • Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylate
  • Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylisonipecotate
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 915-30-0
ATC: A07DA01
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C30H32N2O2
PTK: 452.5873
A meperidine congener used as an antidiarrheal, usually in combination with atropine. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C30H32N2O2
Phân tử khối
452.5873
Monoisotopic mass
452.246378278
InChI
InChI=1S/C30H32N2O2/c1-2-34-28(33)29(25-12-6-3-7-13-25)18-21-32(22-19-29)23-20-30(24-31,26-14-8-4-9-15-26)27-16-10-5-11-17-27/h3-17H,2,18-23H2,1H3
InChI Key
InChIKey=HYPPXZBJBPSRLK-UHFFFAOYSA-N
IUPAC Name
ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate
Traditional IUPAC Name
diphenoxylate
SMILES
CCOC(=O)C1(CCN(CCC(C#N)(C2=CC=CC=C2)C2=CC=CC=C2)CC1)C1=CC=CC=C1
Độ tan chảy
220.5-222
Độ hòa tan
800 mg/L (at 25 °C)
logP
6.3
logS
-5.5
pKa (Strongest Basic)
8.5
PSA
53.33 Å2
Refractivity
146.76 m3·mol-1
Polarizability
51.58 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Diphenoxylate, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Diphenoxylate is rapidly and extensively metabolized in man by ester hydrolysis to diphenoxylic acid (difenoxine), which is biologically active and the major metabolite in the blood.
Cơ Chế Tác Dụng : A meperidine congener used as an antidiarrheal, usually in combination with atropine. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II. Diphenoxylate is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Diphenoxylate has a direct effect on circular smooth muscle of the bowel, that conceivably results in segmentation and prolongation of gastrointestinal transit time. The clinical antidiarrheal action of diphenoxylate may thus be a consequence of enhanced segmentation that allows increased contact of the intraluminal contents with the intestinal mucosa.
Dược Động Học :
▧ Absorption :
90%
▧ Protein binding :
74-95%
▧ Metabolism :
Hepatic
▧ Half Life :
12-14 hours
Độc Tính : Coma, dry skin and mucous membranes, enlarged pupils of the eyes, extremely high body temperature, flushing, involuntary eyeball movement, lower than normal muscle tone, pinpoint pupils, rapid heartbeat, restlessness, sluggishness, suppressed breathing
Chỉ Định : For as adjunctive therapy in the management of diarrhea
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
Liều Lượng & Cách Dùng : Solution - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01081
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=13505
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507130
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00301
ChemSpider
http://www.chemspider.com/Chemical-Structure.12919.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-0427-5
PharmGKB
http://www.pharmgkb.org/drug/PA164746539
Wikipedia
http://en.wikipedia.org/wiki/Diphenoxylate
RxList
http://www.rxlist.com/cgi/generic3/diphenoxylate.htm
... loading
... loading