Tìm theo
Carboprost Tromethamine
Các tên gọi khác (8 ) :
  • (15S)-15-Methyl-pgf2alpha tromethamine salt
  • (15S)-15-Methylprostaglandin F2alpha tromethamine
  • 1,3-Dihydroxy-2-(hydroxymethyl)propan-2-aminium (5Z,9alpha,11beta,13e,15S)-9,11,15-trihydroxy-15-methylprosta-5,13-dien-1-oate
  • 15(S)-15-Methyl-pgf2alpha tromethamine salt
  • 15(S)-15-Methylprostaglandin F2alpha tromethamine
  • Carboprost
  • Carboprost trometamol
  • Methyldinoprost
Thuốc Gốc
Small Molecule
CAS: 58551-69-2
ATC: G02AD04
ĐG : Hospira Inc. , http://www.hospira.com
CTHH: C25H47NO8
PTK: 489.6426
A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of pregnancy. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H47NO8
Phân tử khối
489.6426
Monoisotopic mass
489.330167485
InChI
InChI=1S/C21H36O5.C4H11NO3/c1-3-4-9-13-21(2,26)14-12-17-16(18(22)15-19(17)23)10-7-5-6-8-11-20(24)25;5-4(1-6,2-7)3-8/h5,7,12,14,16-19,22-23,26H,3-4,6,8-11,13,15H2,1-2H3,(H,24,25);6-8H,1-3,5H2/b7-5-,14-12+;/t16-,17-,18+,19+,21+;/m1./s1
InChI Key
InChIKey=UMMADZJLZAPZAW-OVXHCKHTSA-N
IUPAC Name
1,3-dihydroxy-2-(hydroxymethyl)propan-2-aminium (5Z)-7-[(1R,2R,3S,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-3-methyloct-1-en-1-yl]cyclopentyl]hept-5-enoate
Traditional IUPAC Name
carboprost(1-); htris
SMILES
OCC([NH3+])(CO)CO.CCCCC[C@@](O)(C)\C=C\[C@H]1[C@@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(=O)[O-]
Độ tan chảy
95-105 °C
Độ hòa tan
Carboprost tromethamine dissolves readily in water at room temperature at a concentration greater than 75 mg/mL.
logP
3.3
logS
-3.9
pKa (strongest acidic)
4.36
pKa (Strongest Basic)
-1.3
PSA
100.82 Å2
Refractivity
115.95 m3·mol-1
Polarizability
42.51 Å3
Rotatable Bond Count
15
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Carboprost tromethamine administered intramuscularly stimulates in the gravid uterus myometrial contractions similar to labor contractions at the end of a full term pregnancy. Whether or not these contractions result from a direct effect of carboprost on the myome-trium has not been determined. Nonetheless, they evacuate the products of conception from the uterus in most cases. Postpartum, the resultant myometrial contractions provide hemostasis at the site of placentation. Carboprost tromethamine also stimulates the smooth muscle of the human gastrointestinal tract. This activity may produce the vomiting or diarrhea or both that is common when carbo-prost tromethamine is used to terminate pregnancy and for use postpartum. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost trometh-amine used for the termination of pregnancy, and for use postpartum, some patients do experience transient temperature increases. In laboratory animals and in humans large doses of carboprost tromethamine can raise blood pressure, probably by contracting the vascular smooth muscle. With the doses of carboprost tromethamine used for terminating pregnancy, this effect has not been clinically significant. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost tromethamine used for the termination of pregnancy, some patients do experience temperature increases. In some patients, carboprost tromethamine may cause transient bronchoconstriction.
Cơ Chế Tác Dụng : A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of pregnancy. [PubChem] Carboprost is a synthetic prostaglandin. It binds the prostaglandin E2 receptor, causing myometrial contractions, casuing the induction of labour or the expulsion of the placenta. Prostaglandins occur naturally in the body and act at several sites in the body including the womb (uterus). They act on the muscles of the womb, causing them to contract.
Dược Động Học :

▧ Metabolism :
Metabolized in the lungs and liver. Metabolites are excreted in urine.
Độc Tính : Symptoms of overdose include irritation, nausea, vomiting, diarrhea, coughing, dyspnea, asthma, hypertension, flushing, and pyrexia.
Chỉ Định : For aborting pregnancy between the 13th and 20th weeks of gestation as calculated from the first day of the last normal menstrual period and in the following conditions related to second trimester abortion: 1. Failure of expulsion of the fetus during the course of treatment by another method; 2. Premature rupture of membranes in intrauterine methods with loss of drug and insufficient or absent uterine activity; 3. Requirement of a repeat intrauterine instillation of drug for expulsion of the fetus; 4. Inadvertent or spontaneous rupture of membranes in the presence of a previable fetus and absence of adequate activity for expulsion. Also for the treatment of postpartum hemorrhage due to uterine atony which has not responded to conventional methods of management.
Tương Tác Thuốc :
  • Oxytocin Avoid combination due to enhanced oxytocic effects.
Liều Lượng & Cách Dùng : Solution - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Hemabate 250 mcg/ml ampul
    Giá bán buôn : USD >92.89
    Đơn vị tính : ml
  • Biệt dược thương mại : Tham iv solution
    Giá bán buôn : USD >0.49
    Đơn vị tính : ml
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Carboprost
  • Công ty : Dr. Reddy's
    Sản phẩm biệt dược : Deviprost
  • Công ty : Upjohn
    Sản phẩm biệt dược : Hemabate
  • Công ty : Pfizer
    Sản phẩm biệt dược : Prostin 15M
  • Công ty : Pfizer
    Sản phẩm biệt dược : Prostinfenem
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Prostodin
  • Công ty :
    Sản phẩm biệt dược : Tham
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00429
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00682
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0009-0856-05
PharmGKB
http://www.pharmgkb.org/drug/PA164754883
RxList
http://www.rxlist.com/cgi/generic/hemabate.htm
Drugs.com
http://www.drugs.com/mtm/carboprost.html
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