Tìm theo
Conjugated Estrogens
Các tên gọi khác (13 ) :
  • 17-Oxoestra-1,3,5(10)-trien-3-yl sodium sulfate
  • Conestoral
  • Estrogenic substances (conjugated)
  • Estrogens
  • Estrone sodium sulfate
  • Estrone sulfate sodium
  • Estrone-3-sulfate sodium salt
  • Evex
  • Hyhorin
  • Morestin
  • Oestrone-3-sulphate sodium salt
  • Premarin
  • Sodium estrone 3-sulfate
estrogens
Thuốc Gốc
Small Molecule
CAS: 438-67-5
ATC: G03CA57
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C18H21NaO5S
PTK: 372.411
Conjugated estrogens, a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H21NaO5S
Phân tử khối
372.411
Monoisotopic mass
372.100739147
InChI
InChI=1S/C18H22O5S.Na/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);/q;+1/p-1/t14-,15-,16+,18+;/m1./s1
InChI Key
InChIKey=VUCAHVBMSFIGAI-ZFINNJDLSA-M
IUPAC Name
sodium (1S,10R,11S,15S)-15-methyl-14-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-trien-5-yl sulfate
Traditional IUPAC Name
sodium estrone 3-sulfate
SMILES
[Na+].[H][C@@]12CCC(=O)[C@@]1(C)CC[C@]1([H])C3=CC=C(OS([O-])(=O)=O)C=C3CC[C@@]21[H]
Độ tan chảy
173 °C
Độ hòa tan
0.0036 mg/ml
logP
3.83
logS
-4.9
pKa (strongest acidic)
-1.7
pKa (Strongest Basic)
-7.5
PSA
83.5 Å2
Refractivity
87.95 m3·mol-1
Polarizability
36.47 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Conjugated estrogens, a mixture of the water soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics. They promote growth and development of the vagina, uterus, and fallopian tubes, and enlargement of the breasts. Indirectly, they contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones that allow for the pubertal growth spurt and its termination, growth of axillary and pubic hair, and pigmentation of the nipples and genitals. Decline of estrogenic activity at the end of the menstrual cycle can bring on menstruation, although the cessation of progesterone secretion is the most important factor in the mature ovulatory cycle. However, in the preovulatory or nonovulatory cycle, estrogen is the primary determinant in the onset of menstruation. Estrogens also affect the release of pituitary gonadotropins. The pharmacologic effects of conjugated estrogens are similar to those of endogenous estrogens.
Cơ Chế Tác Dụng : Conjugated estrogens, a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics. Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. Estrogens decrease the secretion of gonadotropin-releasing hormone by the hypothalamus, reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary.
Dược Động Học :
▧ Absorption :
Well absorbed
▧ Protein binding :
90% bound to plasma proteins
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Estradiol, estrone, and estriol are excreted in the urine, along with glucuronide and sulfate conjugates. Exogenous estrogens are metabolized in the same manner as endogenous estrogens.
▧ Half Life :
7.4 hours
Độc Tính : Nausea and vomiting
Chỉ Định : For the treatment of moderate to severe vasomotor symptoms associated with the menopause, atrophic vaginitis, osteoporosis, hypoestrogenism due to hypogonadism, castration, primary ovarian failure, breast cancer (for palliation only), and Advanced androgen-dependent carcinoma of the prostate (for palliation only)
Tương Tác Thuốc :
  • Amobarbital The enzyme inducer, amobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Aprobarbital The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Butabarbital The enzyme inducer, butabarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Butalbital The enzyme inducer, butalbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Butethal The enzyme inducer, butethal, decreases the effect of the hormone agent, conjugated estrogens.
  • Ethotoin The enzyme inducer, ethotoin, decreases the effect of the hormone agent, conjugated estrogens.
  • Fosphenytoin The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, conjugated estrogens.
  • Griseofulvin The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, conjugated estrogens.
  • Heptabarbital The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Hexobarbital The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Mephenytoin The enzyme inducer, mephenytoin, decreases the effect of the hormone agent, conjugated estrogens.
  • Methohexital The enzyme inducer, methohexital, decreases the effect of the hormone agent, conjugated estrogens.
  • Methylphenobarbital The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Phenobarbital The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Phenytoin The enzyme inducer, phenytoin, decreases the effect of the hormone agent, conjugated estrogens.
  • Prednisolone The estrogenic agent may increase the effect of the corticosteroid, prednisolone.
  • Prednisone The estrogenic agent may increase the effect of corticosteroid, prednisone.
  • Primidone The enzyme inducer, primidone, decreases the effect of the hormone agent, conjugated estrogens.
  • Raloxifene Association not recommended
  • Secobarbital The enzyme inducer, secobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Talbutal The enzyme inducer, talbutal, decreases the effect of the hormone agent, conjugated estrogens.
  • Tipranavir Conjugated estrogens may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Conjugated estrogens. Monitor for estrogen deficiency during concomitant therapy.
  • Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Liều Lượng & Cách Dùng : Cream - Topical
Powder, for solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cenestin
  • Công ty :
    Sản phẩm biệt dược : ENJUVIA
  • Công ty :
    Sản phẩm biệt dược : Premarin
  • Công ty :
    Sản phẩm biệt dược : Premarin Vaginal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00286
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=23667301
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505680
ChemSpider
http://www.chemspider.com/Chemical-Structure.9532.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0046-0872-93
PharmGKB
http://www.pharmgkb.org/drug/PA164754789
RxList
http://www.rxlist.com/cgi/generic/conest.htm
Drugs.com
http://www.drugs.com/cdi/conjugated-estrogens.html
... loading
... loading