Tìm theo
Cyproterone acetate
Các tên gọi khác (1) :
  • Cyproterone 17-O-acetate
Thuốc Gốc
Small Molecule
CAS: 427-51-0
ATC: G03HA01
CTHH: C24H29ClO4
PTK: 416.938
An anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H29ClO4
Phân tử khối
416.938
Monoisotopic mass
416.175437123
InChI
InChI=1/C24H29ClO4/c1-12(26)24(29-13(2)27)8-6-16-14-10-20(25)19-11-21(28)15-9-18(15)23(19,4)17(14)5-7-22(16,24)3/h10-11,14-18H,5-9H2,1-4H3/t14-,15+,16-,17-,18-,22-,23-,24-/s2
InChI Key
InChIKey=UWFYSQMTEOIJJG-HEULQOMWNA-N
IUPAC Name
(1S,2S,3S,5R,11R,12S,15R,16S)-15-acetyl-9-chloro-2,16-dimethyl-6-oxopentacyclo[9.7.0.0²,⁸.0³,⁵.0¹²,¹⁶]octadeca-7,9-dien-15-yl acetate
Traditional IUPAC Name
cyproterone acetate
SMILES
[H][C@@]12C[C@]1([H])[C@@]1(C)C(=CC2=O)C(Cl)=C[C@@]2([H])[C@]3([H])CC[C@](OC(C)=O)(C(C)=O)[C@@]3(C)CC[C@]12[H]
Độ tan chảy
200-201
Độ hòa tan
1.52e-03 g/l
logP
3.64
logS
-5.4
pKa (strongest acidic)
17.83
pKa (Strongest Basic)
-5.6
PSA
60.44 Å2
Refractivity
111.81 m3·mol-1
Polarizability
44.65 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Cyproterone is an antiandrogen. It suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels).
Cơ Chế Tác Dụng : An anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem] The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.
Dược Động Học :
▧ Absorption :
Completely absorbed following oral administration.
▧ Metabolism :
Primarily hepatic. Cyproterone acetate is metabolized by the CYP3A4 enzyme, forming the active metabolite 15beta-hydroxycyproterone acetate, which retains its antiandrogen activity, but has reduced progestational activity.
▧ Route of Elimination :
It is excreted approximately 60% in the bile and 33% through the kidneys.
▧ Half Life :
Elimination Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.
Chỉ Định : For the palliative treatment of patients with advanced prostatic carcinoma.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Bayer
    Sản phẩm biệt dược : Androcur
  • Công ty : Bayer
    Sản phẩm biệt dược : Cyprostat
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04839
PharmGKB
http://www.pharmgkb.org/drug/PA10049
Wikipedia
http://en.wikipedia.org/wiki/Cyproterone_acetate
... loading
... loading