Tìm theo
Etonogestrel
Các tên gọi khác (4 ) :
  • 3-Ketodesogestrel
  • 3-Oxodesogestrel
  • Etonogestrelum
  • Implanon
contraceptive agents
Thuốc Gốc
Small Molecule
CAS: 54048-10-1
ATC: G03AC08
ĐG : Diversified Healthcare Services Inc. , http://www.dhscorp.com
CTHH: C22H28O2
PTK: 324.4565
Etonogestrel is a molecule used in hormonal contraceptives, most notably the subdermal implant Implanon. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H28O2
Phân tử khối
324.4565
Monoisotopic mass
324.20893014
InChI
InChI=1S/C22H28O2/c1-4-21-13-14(3)20-17-9-7-16(23)12-15(17)6-8-18(20)19(21)10-11-22(21,24)5-2/h2,12,17-20,24H,3-4,6-11,13H2,1H3/t17-,18-,19-,20+,21-,22-/m0/s1
InChI Key
InChIKey=GCKFUYQCUCGESZ-BPIQYHPVSA-N
IUPAC Name
(1S,2R,10S,11S,14R,15S)-15-ethyl-14-ethynyl-14-hydroxy-17-methylidenetetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
Traditional IUPAC Name
etonogestrel
SMILES
[H][[email protected]@]12CC[[email protected]@](O)(C#C)[[email protected]@]1(CC)CC(=C)[[email protected]]1([H])[[email protected]@]3([H])CCC(=O)C=C3CC[[email protected]@]21[H]
Độ hòa tan
7.37e-03 g/l
logP
3.4
logS
-4.6
pKa (strongest acidic)
17.99
pKa (Strongest Basic)
-1.5
PSA
37.3 Å2
Refractivity
96.35 m3·mol-1
Polarizability
37.77 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Etonogestrel is used as a female contraceptive. Etonogestrel 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. Etonogestrel 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 : Etonogestrel is a molecule used in hormonal contraceptives, most notably the subdermal implant Implanon. [Wikipedia] Etonogestrel 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 etonogestrel 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 :

▧ Volume of Distribution :
* 201 L
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Excretion of ENG and its metabolites, either as free steroid or as conjugates, is mainly in urine and to a lesser extent in feces.
▧ Half Life :
25 hours
Độc Tính : Symptoms of overdose include nausea, vomiting, vaginal bleeding, and other menstrual irregularities.
Chỉ Định : For use as a female contraceptive (depot).
Tương Tác Thuốc :
  • Artemether Artemether may decrease the effectiveness of etonogestrel 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 etonogestrel, 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 Etonogestrel. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
  • Tretinoin Oral Tretinoin may decrease the effect of oral contraceptive, Etonogestrel. An alternate form of contraception should be used during concomitant therapy.
  • Warfarin Etonogestrel may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if etonogestrel is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Implant - Transdermal
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Implanon 68 mg implant
    Giá bán buôn : USD >714.34
    Đơn vị tính : each
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Implanon
  • Công ty :
    Sản phẩm biệt dược : Nexplanon
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