药品详细
Chlorotrianisene(氯烯)
化学结构式图
中文名
氯烯
英文名
Chlorotrianisene
分子式
C23H21ClO3
化学名
1-[2-chloro-1,2-bis(4-methoxyphenyl)ethenyl]-4-methoxybenzene
分子量
Average: 380.864
Monoisotopic: 380.117922245
Monoisotopic: 380.117922245
CAS号
569-57-3
ATC分类
G03C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A powerful synthetic, non-steroidal estrogen. [PubChem]
生产厂家
- Banner pharmacaps inc
- Sanofi aventis us llc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | Used to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. Chlorotrianisene may also be used to prevent breast engorgement following childbirth. |
| Pharmacodynamics | Chlorotrianisene is a nonsteroidal synthetic estrogen. After menopause, when the body no longer produces estrogen, chlorotrianisene is used as a simple replacement of estrogen. The estrogen-stimulated endometrium may bleed within 48-72 hours after discontinuance of estrogen therapy. Paradoxically, prolonged estrogen therapy may cause shrinkage of the endometrium and an increase in size of the myometrium. Estrogens have a weak anabolic effect and may cause sodium retention with associated fluid retention and edema. Estrogens may also decrease elevated blood cholesterol and phospholipid concentrations. Estrogens affect bone by increasing calcium deposition and accelerating epiphyseal closure, following initial growth stimulation. During the preovulatory or nonovulatory phase of the menstrual cycle, estrogen is the principal determinant in the onset of menstruation. A decline of estrogenic activity at the end of the menstrual cycle also may induce menstruation; however, the cessation of progesterone secretion is the most important factor during the mature ovulatory phase of the menstrual cycle. The benefit derived from estrogen therapy in the prevention of postpartum breast engorgement must be carefully weighed against the potential increased risk of puerperal thromboembolism associated with the use of large doses of estrogens. |
| Mechanism of action | Chlorotrianisene binds to the estrogen receptor on various estrogen receptor bearing cells. Target cells include cells in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. |
| Absorption | Absorption following oral administration is rapid. |
| Volume of distribution | Not Available |
| Protein binding | 50-80% |
| Metabolism |
Metabolized principally in the liver, although the kidneys, gonads, and muscle tissues may be involved to some extent. The metabolic fate of the synthetic estrogens has not been fully elucidated.
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| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Acute overdosage of large doses of oral contraceptives in chidren reportedly produces almost no toxicity except nausea and vomiting. Acute overdosage of estrogens may cause nausea, and withdrawal bleeding may occur in females. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Fosphenytoin | The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, chlorotrianisene. |
| Griseofulvin | The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, chlorotrianisene. |
| Phenobarbital | The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, chlorotrianisene. |
| Phenytoin | The enzyme inducer, phenytoin, decreases the effect of the hormone agent, chlorotrianisene. |
| Prednisolone | The estrogenic agent, chlorotrianisene, may increase the effect of the corticosteroid, prednisolone. |
| Prednisone | The estrogenic agent, chlorotrianisene, may increase the effect of corticosteroid, prednisone. |
| Primidone | The enzyme inducer, primidone, decreases the effect of the hormone agent, chlorotrianisene. |
| Raloxifene | Association not recommended |
食物相互作用
Not Available
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