Tìm theo
Estropipate
Các tên gọi khác (9 ) :
  • 3-Hydroxyestra-1,3,5(10)-trien-17-one hydrogen sulphate
  • Estrone 3-sulfate
  • Estrone hydrogen sulfate
  • Estrone sulfate
  • Estrone sulphate
  • Estropipate
  • OGEN
  • Ogen (TN)
  • Ogen 2.5
contraceptive agents, hormone replacement agents
Thuốc Gốc
Small Molecule
CAS: 7280-37-7
CTHH: C18H22O5S
PTK: 350.429
Estropipate is a form of estrogen. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics,treatment of vaginal atrophy,treatment of some types of breast cancer (particularly in men and postmenopausal women), treatment of prostate cancer and prevention of osteoporosis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H22O5S
Phân tử khối
350.429
Monoisotopic mass
350.118794504
InChI
InChI=1S/C18H22O5S/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22)/t14-,15-,16+,18+/m1/s1
InChI Key
InChIKey=JKKFKPJIXZFSSB-CBZIJGRNSA-N
IUPAC Name
[(1S,10R,11S,15S)-15-methyl-14-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-5-yl]oxidanesulfonic acid
Traditional IUPAC Name
estrone sulfate
SMILES
C[C@]12CC[C@H]3[C@@H](CCC4=C3C=CC(OS(O)(=O)=O)=C4)[C@@H]1CCC2=O
Độ hòa tan
5.90e-03 g/l
logP
3.83
logS
-4.8
pKa (strongest acidic)
-1.7
pKa (Strongest Basic)
-7.5
PSA
80.67 Å2
Refractivity
89.07 m3·mol-1
Polarizability
36.64 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Estropipate is an estrogenic substance. It acts as naturally produced estrogen does. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.
Cơ Chế Tác Dụng : Estropipate is a form of estrogen. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics,treatment of vaginal atrophy,treatment of some types of breast cancer (particularly in men and postmenopausal women), treatment of prostate cancer and prevention of osteoporosis. Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
Dược Động Học :
▧ Absorption :
Estropipate is well absorbed through the skin and gastrointestinal tract. When applied for a local action, absorption is usually sufficient to cause systemic effects.
▧ Metabolism :
Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.
▧ Route of Elimination :
Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates
Chỉ Định : Estropipate is used for the treatment of moderate to severe vasomotor symptoms associated with the monopause, and moderate to severe symptoms of vulval and vaginal atrophy associated with the menopause. It is also used to treat hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and prevent postmenopausal osteoporosis.
Tương Tác Thuốc :
  • Fosphenytoin The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estropipate.
  • Griseofulvin The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estropipate.
  • Phenobarbital The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, estropipate.
  • Phenytoin The enzyme inducer, phenytoin, decreases the effect of the hormone agent, estropipate.
  • Prednisolone The estrogenic agent, estropipate, may increase the effect of the corticosteroid, prednisolone.
  • Prednisone The estrogenic agent, estropipate, may increase the effect of corticosteroid, prednisone.
  • Primidone The enzyme inducer, primidone, decreases the effect of the hormone agent, estropipate.
  • Raloxifene Association not recommended
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Ogen
  • Công ty :
    Sản phẩm biệt dược : ORTHO-EST
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04574
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5284555
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508976
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00948
PharmGKB
http://www.pharmgkb.org/drug/PA165958342
Wikipedia
http://en.wikipedia.org/wiki/Estropipate
RxList
http://www.rxlist.com/ogen-drug.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=oge1308.html&contentName=Ogen&contentId=547
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