Tìm theo
Clomifene
Các tên gọi khác (4 ) :
  • Clomifene
  • Clomifeno
  • Clomifenum
  • Clomiphene
fertility agents female, estrogen antagonists, selective estrogen receptor modulators
Thuốc Gốc
Small Molecule
CAS: 911-45-5
ATC: G03GB02
ĐG : Dispensing Solutions , http://www.drxdispensing.com
CTHH: C26H28ClNO
PTK: 405.96
A triphenyl ethylene stilbene derivative which is an estrogen agonist or antagonist depending on the target tissue. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H28ClNO
Phân tử khối
405.96
Monoisotopic mass
405.18594223
InChI
InChI=1S/C26H28ClNO/c1-3-28(4-2)19-20-29-24-17-15-22(16-18-24)25(21-11-7-5-8-12-21)26(27)23-13-9-6-10-14-23/h5-18H,3-4,19-20H2,1-2H3/b26-25+
InChI Key
InChIKey=GKIRPKYJQBWNGO-OCEACIFDSA-N
IUPAC Name
{2-[4-(2-chloro-1,2-diphenylethenyl)phenoxy]ethyl}diethylamine
Traditional IUPAC Name
clomiphene
SMILES
CCN(CC)CCOC1=CC=C(C=C1)C(=C(Cl)C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
116.5-118
Độ hòa tan
Slightly soluble
logP
7.2
logS
-6
pKa (Strongest Basic)
9.31
PSA
12.47 Å2
Refractivity
133.76 m3·mol-1
Polarizability
46.7 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Clomifene (previously clomiphene) is an orally administered, non steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). Clomifene can lead to multiple ovulation, and hence increase the risk of conceiving twins. In comparison to purified FSH, the rate of ovarian hyperstimulation syndrome is low. There may be an increased risk of ovarian cancer and weight gain. Clomifene is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracellular estrogen receptors. Clomifene initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event, in response to a course of clomifene therapy, is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.
Cơ Chế Tác Dụng : A triphenyl ethylene stilbene derivative which is an estrogen agonist or antagonist depending on the target tissue. [PubChem] Clomifene has both estrogenic and anti-estrogenic properties, but its precise mechanism of action has not been determined. Clomifene appears to stumulate the release of gonadotropins, follicle-stimulating hormone (FSH), and leuteinizing hormone (LH), which leads to the development and maturation of ovarian follicle, ovulation, and subsequent development and function of the coprus luteum, thus resulting in pregnancy. Gonadotropin release may result from direct stimulation of the hypothalamic-pituitary axis or from a decreased inhibitory influence of estrogens on the hypothalamic-pituitary axis by competing with the endogenous estrogens of the uterus, pituitary, or hypothalamus. Clomifene has no apparent progestational, androgenic, or antrandrogenic effects and does not appear to interfere with pituitary-adrenal or pituitary-thyroid function.
Dược Động Học :
▧ Absorption :
Based on early studies with 14 C-labeled clomifene, the drug was shown to be readily absorbed orally in humans.
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Based on early studies with 14C-labeled clomiphene citrate, the drug was shown to be readily absorbed orally in humans and excreted principally in the feces. Mean urinary excretion was approximately 8% with fecal excretion of about 42%.
▧ Half Life :
5-7 days
Độc Tính : The acute oral LD50 of clomifene is 1700 mg/kg in mice and 5750 mg/kg in rats. The toxic dose in humans is not known. Toxic effects accompanying acute overdosage of clomifene have not been reported. Signs and symptoms of overdosage as a result of the use of more than the recommended dose during clomifene therapy include nausea, vomiting, vasomotor flushes, visual blurring, spots or flashes, scotomata, ovarian enlargement with pelvic or abdominal pain.
Chỉ Định : Used mainly in female infertility due to anovulation (e.g. due to polycystic ovary syndrome) to induce ovulation.
Tương Tác Thuốc :
  • Amobarbital The enzyme inducer, amobarbital, decreases the effect of the hormone agent, clomifene.
  • Aprobarbital The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, clomifene.
  • Butabarbital The enzyme inducer, butabarbital, decreases the effect of the hormone agent, clomifene.
  • Butalbital The enzyme inducer, butalbital, decreases the effect of the hormone agent, clomifene.
  • Butethal The enzyme inducer, butethal, decreases the effect of the hormone agent, clomifene.
  • Ethotoin The enzyme inducer, ethotoin, decreases the effect of the hormone agent, clomifene.
  • Fosphenytoin The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, clomifene.
  • Griseofulvin The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, clomifene.
  • Heptabarbital The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, clomifene.
  • Hexobarbital The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, clomifene.
  • Mephenytoin The enzyme inducer, mephenytoin, decreases the effect of the hormone agent, clomifene.
  • Methohexital The enzyme inducer, methohexital, decreases the effect of the hormone agent, clomifene.
  • Methylphenobarbital The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, clomifene.
  • Pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, clomifene.
  • Phenobarbital The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, clomifene.
  • Phenytoin The enzyme inducer, phenytoin, decreases the effect of the hormone agent, clomifene.
  • Prednisolone The estrogenic agent, clomifene, may increase the effect of the corticosteroid, prednisolone.
  • Prednisone The estrogenic agent, clomifene, may increase the effect of corticosteroid, prednisone.
  • Primidone The enzyme inducer, primidone, decreases the effect of the hormone agent, clomifene.
  • Raloxifene Association not recommended
  • Secobarbital The enzyme inducer, secobarbital, decreases the effect of the hormone agent, clomifene.
  • Talbutal The enzyme inducer, talbutal, decreases the effect of the hormone agent, clomifene.
  • Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Androxal
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Clomid
  • Công ty :
    Sản phẩm biệt dược : Clomifert
  • Công ty : Egis
    Sản phẩm biệt dược : Clostilbegyt
  • Công ty : Sanofi
    Sản phẩm biệt dược : Omifin
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Serophene
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00882
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06917
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00962
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50170640
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0068-0226-30
PharmGKB
http://www.pharmgkb.org/drug/PA449046
Wikipedia
http://en.wikipedia.org/wiki/Clomifene
RxList
http://www.rxlist.com/cgi/generic/clomiph.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/clo1088.shtml
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