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药品详细

Norelgestromin(Norelgestromin)

化学结构式图
中文名
Norelgestromin
英文名
Norelgestromin
分子式
C21H29NO2
化学名
15-ethyl-14-ethynyl-5-(hydroxyimino)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-ol
分子量
Average: 327.4605
Monoisotopic: 327.219829177
CAS号
53016-31-2
ATC分类
G03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Norelgestromin is a drug used in contraception. Norelgestromin is the active progestin responsible for the progestational activity that occurs in women after application of ORTHO EVRA patch.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Goa KL, Warner GT, Easthope SE: Transdermal ethinylestradiol/norelgestromin: a review of its use in hormonal contraception. Treat Endocrinol. 2003;2(3):191-206. Pubmed
    2. Henzl MR: Norgestimate. From the laboratory to three clinical indications. J Reprod Med. 2001 Jul;46(7):647-61. Pubmed
    3. Abrams LS, Skee DM, Wong FA, Anderson NJ, Leese PT: Pharmacokinetics of norelgestromin and ethinyl estradiol from two consecutive contraceptive patches. J Clin Pharmacol. 2001 Nov;41(11):1232-7. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Steroids and Steroid Derivatives
    Substructures
    • Steroids and Steroid Derivatives
    • Hydroxy Compounds
    • Alkanes and Alkenes
    • Alkynes
    • Alcohols and Polyols
    • Imines
    • Cyclohexenes and Derivatives
    • Oximes and Derivatives
    适应症
    药理
    Indication Norelgestromin is used for contraception and menopausal hormonal therapy. Norelgestromin may potentially be used in breast cancer treatment due to its inhibitory effect on estrone sulfatase . They convert sulfated steroid precursors to estrogen during pregnancy.
    Pharmacodynamics Norelgestromin is used for contraception and menopausal hormonal therapy transdermally or in combination with ethinyl estradiol as a vaginal ring. Norelgestromin, in combination with ethinyl estradiol inhibits ovulation by suppressing gonadotropins.
    Mechanism of action Norelgestromin inhibits estrone sulfatase, which converts sulfated steroid precursors to estrogen during pregnancy. Norgelgestromin/ethinylestradiol suppresses follicular development, induces changes to the endometrium, which decreases chances of implantation and thickens the cervical mucus, impeding sperm swimming into the uterus. It also has similar agonisting binding affinities as its parent compound, Norgestimate, for progesterone and estrogen receptors.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 6.05e-03 g/l ALOGPS
    logP 3.18 ALOGPS
    logP 3.67 ChemAxon
    logS -4.7 ALOGPS
    pKa (strongest acidic) 11.47 ChemAxon
    pKa (strongest basic) 3.12 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 52.82 ChemAxon
    rotatable bond count 1 ChemAxon
    refractivity 95.85 ChemAxon
    polarizability 38.53 ChemAxon
    药物相互作用
    Drug Interaction
    Artemether Artemether may decrease the effectiveness of norelgestromin by increasing its metabolism via CYP3A4. Consider an alternate non-hormonal means of contraception during artemether therapy.
    Bexarotene Bexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of norelgestromin, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
    Colesevelam Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider alternatives in order to avoid this combination when possible, due to the risk for impaired contraceptive effectiveness.
    食物相互作用
    Not Available

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