Tìm theo
Norelgestromin
Các tên gọi khác (1) :
  • 17-Deacylnorgestimate
contraceptive agents, contraceptives oral combined
Thuốc Gốc
Small Molecule
CAS: 53016-31-2
ATC: G03AA13
CTHH: C21H29NO2
PTK: 327.4605
Norelgestromin is a drug used in contraception. Norelgestromin is the active progestin responsible for the progestational activity that occurs in women after application of ORTHO EVRA patch.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H29NO2
Phân tử khối
327.4605
Monoisotopic mass
327.219829177
InChI
InChI=1S/C21H29NO2/c1-3-20-11-9-17-16-8-6-15(22-24)13-14(16)5-7-18(17)19(20)10-12-21(20,23)4-2/h2,13,16-19,23-24H,3,5-12H2,1H3/b22-15-
InChI Key
InChIKey=ISHXLNHNDMZNMC-JCMHNJIXSA-N
IUPAC Name
15-ethyl-14-ethynyl-5-(hydroxyimino)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-ol
Traditional IUPAC Name
15-ethyl-14-ethynyl-5-(hydroxyimino)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-ol
SMILES
CCC12CCC3C(CCC4=CC(CCC34)=NO)C1CCC2(O)C#C
Độ hòa tan
6.05e-03 g/l
logP
3.67
logS
-4.7
pKa (strongest acidic)
11.47
pKa (Strongest Basic)
3.12
PSA
52.82 Å2
Refractivity
95.85 m3·mol-1
Polarizability
38.53 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Norelgestromin is used for contraception and menopausal hormonal therapy transdermally or in combination with ethinyl estradiol as a vaginal ring. Norelgestromin, in combination with ethinyl estradiol inhibits ovulation by suppressing gonadotropins.
Cơ Chế Tác Dụng : Norelgestromin is a drug used in contraception. Norelgestromin is the active progestin responsible for the progestational activity that occurs in women after application of ORTHO EVRA patch. Norelgestromin inhibits estrone sulfatase, which converts sulfated steroid precursors to estrogen during pregnancy. Norgelgestromin/ethinylestradiol suppresses follicular development, induces changes to the endometrium, which decreases chances of implantation and thickens the cervical mucus, impeding sperm swimming into the uterus. It also has similar agonisting binding affinities as its parent compound, Norgestimate, for progesterone and estrogen receptors.
Chỉ Định : Norelgestromin is used for contraception and menopausal hormonal therapy. Norelgestromin may potentially be used in breast cancer treatment due to its inhibitory effect on estrone sulfatase . They convert sulfated steroid precursors to estrogen during pregnancy.
Tương Tác Thuốc :
  • Artemether Artemether may decrease the effectiveness of norelgestromin 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 norelgestromin, 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.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06713
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=13752005
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443265
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05205
Wikipedia
http://en.wikipedia.org/wiki/Norelgestromin
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