Tìm theo
Ethynodiol
Các tên gọi khác (12 ) :
  • 17alpha-Ethynyl-19-norandrost-4-ene-3beta,17-beta-diol diacetate
  • 17alpha-Ethynyl-3,17-dihydroxy-4-estrene diacetate
  • 17alpha-Ethynyl-4-estrene-3beta,17beta-diol diacetate
  • 17alpha-Ethynylestr-4-ene-3beta,17beta-diol acetate
  • 19-Nor-17alpha-pregn-4-en-20-yne-3beta,17-diol diacetate
  • 3beta, 17beta-Diacetoxy-17alpha-ethynyl-4-oestrene
  • 3beta,17beta-Diacetoxy-19-nor-17alpha-pregn-4-en-20-yne
  • Ethynodiol diacetate
  • Etinodiol
  • Étynodiol
  • Etynodiol
  • Etynodiolum
contraceptives oral synthetic
Thuốc Gốc
Small Molecule
CAS: 297-76-7
ĐG : Barr Pharmaceuticals
CTHH: C24H32O4
PTK: 384.5085
A synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H32O4
Phân tử khối
384.5085
Monoisotopic mass
384.230059512
InChI
InChI=1S/C24H32O4/c1-5-24(28-16(3)26)13-11-22-21-8-6-17-14-18(27-15(2)25)7-9-19(17)20(21)10-12-23(22,24)4/h1,14,18-22H,6-13H2,2-4H3/t18-,19-,20+,21+,22-,23-,24-/m0/s1
InChI Key
InChIKey=ONKUMRGIYFNPJW-KIEAKMPYSA-N
IUPAC Name
(1S,2R,5S,10R,11S,14R,15S)-5-(acetyloxy)-14-ethynyl-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-yl acetate
Traditional IUPAC Name
ethynodiol diacetate
SMILES
[H][C@@]12CC[C@@](OC(C)=O)(C#C)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CC[C@H](OC(C)=O)C=C3CC[C@@]21[H]
Độ tan chảy
126-127
Độ hòa tan
3.97e-03 g/l
logP
5
logS
-5
pKa (Strongest Basic)
-6.7
PSA
52.6 Å2
Refractivity
106.62 m3·mol-1
Polarizability
44.11 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ethynodiol Diacetate is used as a female contraceptive. Ethynodiol Diacetate is a progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Ethynodiol Diacetate tricks the body processes into thinking that ovulation has already occurred, by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.
Cơ Chế Tác Dụng : A synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive. [PubChem] Binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Ethynodiol Diacetate will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.
Dược Động Học :

▧ Protein binding :
50-85%
Chỉ Định : For the prevention of pregnancy in women who elect to use this product as a method of contraception.
Tương Tác Thuốc :
  • Artemether Artemether may decrease the effectiveness of ethynodiol diacetate by increasing its metabolism via CYP3A4. Consider an alternate non-hormonal means of contraception during artemether therapy.
  • Bexarotene Bexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of ethynodiol diacetate it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
  • Colesevelam Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider alternatives in order to avoid this combination when possible, due to the risk for impaired contraceptive effectiveness.
  • Thiopental Thiopental may decrease the effect of Ethynodiol diacetate. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
  • Tretinoin Oral Tretinoin may decrease the effect of oral contraceptive, Ethynodiol Diacetate. An alternate form of contraception should be used during concomitant therapy.
  • Warfarin Ethynodiol diacetate may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if ethynodiol diacetate is initiated, discontinued or dose
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Searle
    Sản phẩm biệt dược : Conova
  • Công ty :
    Sản phẩm biệt dược : Continuin
  • Công ty : Searle
    Sản phẩm biệt dược : Dernulen
  • Công ty : Pfizer
    Sản phẩm biệt dược : Femulen
  • Công ty :
    Sản phẩm biệt dược : Luteonorm
  • Công ty :
    Sản phẩm biệt dược : Luto-Metrodiol
  • Công ty :
    Sản phẩm biệt dược : Metrodiol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00823
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9270
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506993
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C12724
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01294
ChemSpider
http://www.chemspider.com/Chemical-Structure.8913.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749157
Wikipedia
http://en.wikipedia.org/wiki/Ethynodiol_diacetate
RxList
http://www.rxlist.com/cgi/generic/ethynoc.htm
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