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药品详细

Progesterone(黄体激素)

化学结构式图
中文名
黄体激素
英文名
Progesterone
分子式
C21H30O2
化学名
(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
分子量
Average: 314.4617
Monoisotopic: 314.224580204
CAS号
57-83-0
ATC分类
G03A 未知;G03D 未知;G03D 未知;G03D 未知;L02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

The major progestational steroid that is secreted primarily by the corpus luteum and the placenta. Progesterone acts on the uterus, the mammary glands, and the brain. It is required in embryo implantation, pregnancy maintenance, and the development of mammary tissue for milk production. Progesterone, converted from pregnenolone, also serves as an intermediate in the biosynthesis of gonadal steroid hormones and adrenal corticosteroids. [PubChem]

生产厂家
  • Alza corp
  • Amarin pharmaceuticals inc
  • App pharmaceuticals llc
  • Bristol myers squibb
  • Eli lilly and co
  • Esi pharmacal
  • Ferring pharmaceuticals inc
  • Pharmaforce inc
  • Solvay pharmaceuticals
  • Unimed pharmaceuticals llc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Allen WM: THE ISOLATION OF CRYSTALLINE PROGESTIN. Science. 1935 Aug 2;82(2118):89-93. Pubmed
  2. Allen WM: Progesterone: how did the name originate? South Med J. 1970 Oct;63(10):1151-5. Pubmed
  3. Schumacher M, Guennoun R, Robert F, Carelli C, Gago N, Ghoumari A, Gonzalez Deniselle MC, Gonzalez SL, Ibanez C, Labombarda F, Coirini H, Baulieu EE, De Nicola AF: Local synthesis and dual actions of progesterone in the nervous system: neuroprotection and myelination. Growth Horm IGF Res. 2004 Jun;14 Suppl A:S18-33. Pubmed
  4. Hould FS, Fried GM, Fazekas AG, Tremblay S, Mersereau WA: Progesterone receptors regulate gallbladder motility. J Surg Res. 1988 Dec;45(6):505-12. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Steroids and Steroid Derivatives
Substructures
  • Steroids and Steroid Derivatives
  • Alkanes and Alkenes
  • Cyclohexenes and Derivatives
  • Ketones
适应症
药理
Indication For progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) treatment for infertile women with progesterone deficiency and for the treatment of secondary amenorrhea. Also used for the reduction of the incidence of endometrial hyperplasia and the attendant risk of endometrial carcinoma in postmenopausal women receiving estrogen replacement therapy, as well as treatment of abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology such as fibroids or uterine cancer.
Pharmacodynamics Progesterone is a naturally occuring progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Progesterone tricks the body processes into thinking that ovulation has already occurred by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.
Mechanism of action Progesterone shares the pharmacological actions of the progestins. Progesterone binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Progesterone will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. In women who have adequate endogenous estrogen, progesterone transforms a proliferative endometrium into a secretory one. Progesterone is essential for the development of decidual tissue and is necessary to increase endometrial receptivity for implantation of an embryo. Once an embryo has been implanted, progesterone acts to maintain the pregnancy. Progesterone also stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has little estrogenic and androgenic activity.
Absorption Progesterone absorption is prolonged with an absorption half-life of approximately 25-50 hours.
Volume of distribution Not Available
Protein binding 96%-99%
Metabolism
Progesterone is metabolized primarily by the liver largely to pregnanediols and pregnanolones.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Progesterone
6(beta)-hydroxyprogesterone Details
Progesterone
6-beta-hydroxyprogesterone Details
Progesterone
    		3-alpha,20-alpha-Dihydroxy-5-beta-pregnane 3-glucuronide Details
    Progesterone
      		11-Hydroxyprogesterone 11-glucuronide Details
      Route of elimination The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces. Progesterone metabolites are excreted mainly by the kidneys.
      Half life 34.8-55.13 hours
      Clearance
      • 2510 +/- 135 L/day [cycling women]
      Toxicity Not Available
      Affected organisms
      • Humans and other mammals
      Pathways Not Available
      理化性质
      Properties
      State solid
      Experimental Properties
      Property Value Source
      melting point 121 °C PhysProp
      water solubility 8.81 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
      logP 3.87 HANSCH,C ET AL. (1995)
      logS -4.43 ADME Research, USCD
      Caco2 permeability -4.37 ADME Research, USCD
      Predicted Properties
      Property Value Source
      water solubility 5.46e-03 g/l ALOGPS
      logP 3.58 ALOGPS
      logP 4.15 ChemAxon
      logS -4.8 ALOGPS
      pKa (strongest acidic) 18.92 ChemAxon
      pKa (strongest basic) -4.8 ChemAxon
      physiological charge 0 ChemAxon
      hydrogen acceptor count 2 ChemAxon
      hydrogen donor count 0 ChemAxon
      polar surface area 34.14 ChemAxon
      rotatable bond count 1 ChemAxon
      refractivity 92.71 ChemAxon
      polarizability 37.15 ChemAxon
      药物相互作用
      Drug Interaction
      Topotecan The p-glycoprotein inhibitor, Progesterone, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
      食物相互作用
      • Avoid alcohol.
      • Avoid excessive quantities of coffee or tea (Caffeine).
      • Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
      • Take at the same time everyday.
      • Take with food.

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