Tìm theo
Metoclopramide
Các tên gọi khác (9 ) :
  • 2-Methoxy-4-amino-5-chloro-N,N-(dimethylaminoethyl)benzamide
  • 2-methoxy-5-chloroprocainamide
  • 4-amino-5-chloro-2-Methoxy-N-(beta-diethylaminoethyl)benzamide
  • 4-amino-5-chloro-N-(2-(Diethylamino)ethyl)-2-methoxybenzamide
  • 4-amino-5-chloro-N-(2-(Diethylamino)ethyl)-O-anisamide
  • Elieten
  • Metoclopramida
  • Metoclopramidum
  • Reliveran
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 364-62-5
ATC: A03FA01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C14H22ClN3O2
PTK: 299.796
A dopamine D2 antagonist that is used as an antiemetic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22ClN3O2
Phân tử khối
299.796
Monoisotopic mass
299.14005467
InChI
InChI=1S/C14H22ClN3O2/c1-4-18(5-2)7-6-17-14(19)10-8-11(15)12(16)9-13(10)20-3/h8-9H,4-7,16H2,1-3H3,(H,17,19)
InChI Key
InChIKey=TTWJBBZEZQICBI-UHFFFAOYSA-N
IUPAC Name
4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxybenzamide
Traditional IUPAC Name
metoclopramide
SMILES
CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC
Độ tan chảy
147.25 °C
Độ hòa tan
200 mg/L (at 25 °C)
logP
2.62
logS
-3.18
pKa (strongest acidic)
14.49
pKa (Strongest Basic)
9.04
PSA
67.59 Å2
Refractivity
83.52 m3·mol-1
Polarizability
32.7 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.27 (at 25 °C)
Dược Lực Học : Metoclopramide, although chemically related to procainamide, does not possess local anesthetic or antiarrhythmic properties. Metoclopramide is used to enhance GI motility, to treat diabetic gastroparesis, as an antinauseant, and to facilitate intubation of the small bowel during radiologic examination. Metoclopramide may be used to treat chemotherapy-induced emesis and as a radiosensitizing agents in the treatment of non-small cell lung carcinoma and glioblastomas in the future.
Cơ Chế Tác Dụng : A dopamine D2 antagonist that is used as an antiemetic. [PubChem] Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals.
Dược Động Học :
▧ Absorption :
Rapidly and well absorbed (oral bioavailability 80±15.5%).
▧ Volume of Distribution :
* 4.4±0.65 L/kg
▧ Protein binding :
30%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Approximately 85% of the radioactivity of an orally administered dose appears in the urine within 72 hours.
▧ Half Life :
5-6 hr
▧ Clearance :
* 0.67 +/- 0.14 L/hr/kg [infants (0.9-5.4 months) with gastroesophageal reflux (GER)]
Độc Tính : Oral, mouse LD50: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.
Chỉ Định : For the treatment of gastroesophageal reflux disease (GERD). It is also used in treating nausea and vomiting, and to increase gastric emptying.
Tương Tác Thuốc :
  • Cyclosporine Metoclopramide increases serum levels of cyclosporine
  • L-DOPA Levodopa decreases the effect of metoclopramide
  • Lurasidone Increases toxicity and risk of extrapyramidal effects of lurasidone by antidopaminergic effects. Concomitant therapy should be avoided.
  • Paliperidone Metoclopramide may increase the risk of extrapyramidal side effects of paliperidone. Concomitant therapy should be avoided.
  • Tacrolimus Metoclopramide may increase the concentration of Tacrolimus in the blood. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Metoclopramide therapy is initiated, discontinued or altered.
  • Tetrabenazine Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
  • Venlafaxine Possible serotoninergic syndrome with this combination
  • Vilazodone Seek alternatives to this combination when possible. Monitor patients receiving metoclopramide with selective serotonin reuptake inhibitors for signs of extrapyramidal symptoms, neuroleptic malignant syndrome, and serotonin syndrome.
  • Zuclopenthixol Additive dopamine D2 receptor antagonism may cause dopaminergic imbalance in the nigrostriatal (dopamine D1 receptors) and striatopallidal (dopamine D2 receptors). Increased risk of extrapyramidal reactions and neuroleptic malignant syndrome. Concomitant therapy should be avoided.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Liquid - Intravenous
Liquid - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cerucal
  • Công ty :
    Sản phẩm biệt dược : Degan
  • Công ty :
    Sản phẩm biệt dược : Elieten
  • Công ty :
    Sản phẩm biệt dược : Maxeran
  • Công ty :
    Sản phẩm biệt dược : Maxolon
  • Công ty :
    Sản phẩm biệt dược : METOZOLV
  • Công ty :
    Sản phẩm biệt dược : Plasil1
  • Công ty :
    Sản phẩm biệt dược : Plazilin
  • Công ty :
    Sản phẩm biệt dược : Pramin
  • Công ty :
    Sản phẩm biệt dược : Primperan
  • Công ty :
    Sản phẩm biệt dược : Pulin
  • Công ty :
    Sản phẩm biệt dược : Pylomid
  • Công ty :
    Sản phẩm biệt dược : Reglan
  • Công ty :
    Sản phẩm biệt dược : Reliveran
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01233
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4168
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505631
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07868
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00726
ChemSpider
http://www.chemspider.com/Chemical-Structure.4024.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50000491
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0591-2228-05
PharmGKB
http://www.pharmgkb.org/drug/PA450475
Wikipedia
http://en.wikipedia.org/wiki/Metoclopramide
RxList
http://www.rxlist.com/cgi/generic2/metoclo.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/reg1369.shtml
Drugs.com
http://www.drugs.com/metoclopramide.html
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