Tìm theo
Dutasteride
Các tên gọi khác (2) :
  • (5alpha,17beta)-N-(2,5-Bis(trifluoromethyl)phenyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
  • alpha,alpha,alpha,Alpha',alpha',alpha'-hexafluoro-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxy-2',5'-xylidide
Thuốc lợi tiểu
Thuốc Gốc
Small Molecule
CAS: 164656-23-9
ATC: G04CB02
ĐG : Catalent Pharma Solutions , http://www.catalent.com
CTHH: C27H30F6N2O2
PTK: 528.5297
Dutasteride belongs to a class of drugs called 5-alpha-reductase inhibitors, which block the action of the 5-alpha-reductase enzymes that convert testosterone into dihydrotestosterone (DHT). Finasteride also belongs to this group, but while dutasteride inhibits both isoforms of 5-alpha reductase, finasteride inhibits only one. Even so, a clinical study done by GlaxoSmithKline, the EPICS trial, did not find dutasteride to be more effective than finasteride in treating BPH. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H30F6N2O2
Phân tử khối
528.5297
Monoisotopic mass
528.221147444
InChI
InChI=1S/C27H30F6N2O2/c1-24-11-9-17-15(4-8-21-25(17,2)12-10-22(36)35-21)16(24)6-7-19(24)23(37)34-20-13-14(26(28,29)30)3-5-18(20)27(31,32)33/h3,5,10,12-13,15-17,19,21H,4,6-9,11H2,1-2H3,(H,34,37)(H,35,36)/t15-,16-,17-,19+,21+,24-,25+/m0/s1
InChI Key
InChIKey=JWJOTENAMICLJG-QWBYCMEYSA-N
IUPAC Name
(1S,2R,7R,10S,11S,14S,15S)-N-[2,5-bis(trifluoromethyl)phenyl]-2,15-dimethyl-5-oxo-6-azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxamide
Traditional IUPAC Name
dutasteride
SMILES
[H][C@@]1(CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])NC(=O)C=C[C@]4(C)[C@@]3([H])CC[C@]12C)C(=O)NC1=CC(=CC=C1C(F)(F)F)C(F)(F)F
Độ hòa tan
9.08e-04 g/l
logP
6.8
logS
-5.8
pKa (strongest acidic)
12.56
pKa (Strongest Basic)
2.17
PSA
58.2 Å2
Refractivity
127.9 m3·mol-1
Polarizability
50.13 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
5
Bioavailability
0
Dược Lực Học : Dutasteride is a synthetic 4-azasteroid compound that is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5 alpha-reductase (5AR), intracellular enzymes that convert testosterone to 5 alpha-dihydrotestosterone (DHT). Type I 5a-reductase is predominant in the sebaceous glands of most regions of skin, including scalp, and liver. Type I 5a-reductase is responsible for approximately one-third of circulating DHT. The Type II 5a-reductase isozyme is primarily found in prostate, seminal vesicles, epididymides, and hair follicles as well as liver, and is responsible for two-thirds of circulating DHT.
Cơ Chế Tác Dụng : Dutasteride belongs to a class of drugs called 5-alpha-reductase inhibitors, which block the action of the 5-alpha-reductase enzymes that convert testosterone into dihydrotestosterone (DHT). Finasteride also belongs to this group, but while dutasteride inhibits both isoforms of 5-alpha reductase, finasteride inhibits only one. Even so, a clinical study done by GlaxoSmithKline, the EPICS trial, did not find dutasteride to be more effective than finasteride in treating BPH. [Wikipedia] Dutasteride inhibits the conversion of testosterone to 5 alpha-dihydrotestosterone (DHT), which is the androgen primarily responsible for the initial development and subsequent enlargement of the prostate gland. Testosterone is converted to DHT by the enzyme 5 alpha-reductase, which exists as 2 isoforms, type 1 and type 2. Dutasteride is a competitive and specific inhibitor of both type 1 and type 2 5 alpha-reductase isoenzymes, with which it forms a stable enzyme complex. Dissociation from this complex has been evaluated under in vitro and in vivo conditions and is extremely slow. Dutasteride does not bind to the human androgen receptor.
Dược Động Học :
▧ Absorption :
60%
▧ Volume of Distribution :
* 300 to 500 L
▧ Protein binding :
Highly bound to albumin (99%) and α-1 acid glycoprotein (96.6%).
▧ Metabolism :
Hepatic. Extensively metabolized by CYP3A4 and CYP3A5 to active metabolites.
▧ Route of Elimination :
Dutasteride is extensively metabolized in humans. Dutasteride and its metabolites were excreted mainly in feces.
▧ Half Life :
5 weeks
Chỉ Định : For the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate gland to improve symptoms, and reduce the risk of acute urinary retention and the need for surgery.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Avodart 0.5 mg softgel
    Giá bán buôn : USD >4.06
    Đơn vị tính : softgel capsule
  • Biệt dược thương mại : Avodart 0.5 mg capsule
    Giá bán buôn : USD >4.12
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Avodart
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01126
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03820
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0173-0712-15
PharmGKB
http://www.pharmgkb.org/drug/PA164749300
Wikipedia
http://en.wikipedia.org/wiki/Dutasteride
RxList
http://www.rxlist.com/cgi/generic3/duagen.htm
Drugs.com
http://www.drugs.com/cdi/dutasteride.html
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